Search Result
Results for "
brain
" in MCE Product Catalog:
1058
Inhibitors & Agonists
8
Biochemical Assay Reagents
104
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
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- HY-P3601
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- HY-P1519B
-
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- HY-P1519
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- HY-148548
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- HY-16940
-
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24(S)-Hydroxycholesterol
24S-OHC; 24S-HC; Cerebrosterol
|
LXR
iGluR
Endogenous Metabolite
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Metabolic Disease
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24(S)-Hydroxycholesterol (24S-OHC), the major brain cholesterol metabolite, plays an important role to maintain homeostasis of cholesterol in the brain. 24(S)-Hydroxycholesterol (24S-OHC) is one of the most efficient endogenous LXR agonist known and is present in the brain and in the circulation at relatively high levels. 24(S)-Hydroxycholesterol (24S-OHC) is a very potent, direct, and selective positive allosteric modulator of NMDARs with a mechanism that does not overlapthat of other allosteric modulators.
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- HY-A0171A
-
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- HY-147151
-
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AMCPy
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Others
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Others
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AMCPy is a potent electron paramagnetic resonance (EPR) brain imaging agent, possessing excellent lipophilicity for blood−brain barrier (BBB) penetration.
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- HY-109058
-
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Firibastat
QGC001; RB150
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Aminopeptidase
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Cardiovascular Disease
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Firibastat (QGC001), an orally active brain penetrating prodrug of EC33, is a first-in-class brain aminopeptidase A (APA) inhibitor (Ki=200 nM). Firibastat selectively and specifically inhibits conversion of brain angiotensin-II into angiotensin-III and decreases blood pressure in hypertensive rats.
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- HY-13459
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PF-5274857
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Smo
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Cancer
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PF-5274857 is a potent, selective, orally active and brain-penetrant antagonist of Smo, with an IC50 of 5.8 nM and Ki of 4.6 nM. PF-5274857 has potential for research of tumor types including brain tumors and brain metastasis driven by an activated Hh pathway.
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- HY-13459A
-
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PF-5274857 hydrochloride
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Smo
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Cancer
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PF-5274857 hydrochloride is a potent, selective, orally active and brain-penetrant antagonist of Smo, with an IC50 of 5.8 nM and Ki of 4.6 nM. PF-5274857 hydrochloride has potential for research of tumor types including brain tumors and brain metastasis driven by an activated Hh pathway.
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- HY-118635
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- HY-118402
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PD 119819
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Dopamine Receptor
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Neurological Disease
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PD 119819 is a highly selective benzopyran-4-one brain dopamine autoreceptor agonist. PD 119819, a heterocyclic piperazine, inhibits spontaneous locomotor activity and brain dopamine synthesis.
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- HY-106840
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L-365260
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Cholecystokinin Receptor
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Metabolic Disease
Neurological Disease
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L-365260 is an orally active and selective antagonist of non-peptide gastrin and brain cholecystokinin receptor (CCK-B), with Kis of 1.9 nM and 2.0 nM, respectively. L-365260 interacts in a stereoselective and competitive manner with guinea pig stomach gastrin and brain CCK receptors. L-365260 can enhance Morphine analgesia and prevents Morphine tolerance.
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- HY-106840A
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L-365260 hemihydrate
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Cholecystokinin Receptor
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Metabolic Disease
Neurological Disease
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L-365260 hemihydrate is an orally active and selective antagonist of non-peptide gastrin and brain cholecystokinin receptor (CCK-B), with Kis of 1.9 nM and 2.0 nM, respectively. L-365260 hemihydrate interacts in a stereoselective and competitive manner with guinea pig stomach gastrin and brain CCK receptors. L-365260 hemihydrate can enhance Morphine analgesia and prevents Morphine tolerance.
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- HY-15608
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- HY-B2150
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4-Hydroxyantipyrine
4-Hydroxyphenazone; NSC 174055
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Drug Metabolite
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Others
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4-Hydroxyantipyrine (4-Hydroxyphenazone; NSC 174055) is the major metabolite of Antipyrine (HY-B0171), can be as a biodistribution promoter. 4-Hydroxyantipyrine can increase distribution of concentration ratio of Citicoline and Antipyrine in the brain.
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- HY-B2150S
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4-Hydroxyantipyrine-d3
4-Hydroxyphenazone-d3; NSC 174055-d3
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Isotope-Labeled Compounds
Drug Metabolite
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Others
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4-Hydroxyantipyrine-d3 is the deuterium labeled 4-Hydroxyantipyrine. 4-Hydroxyantipyrine is the major metabolite of Antipyrine, can be as a biodistribution promoter. 4-Hydroxyantipyrine can increase distribution of concentration ratio of Citicoline and Antipyrine in the brain[1][2][3].
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- HY-P3219
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- HY-150209
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- HY-120878A
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(R,R)-CXCR2-IN-2
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CXCR
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Inflammation/Immunology
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(R,R)-CXCR2-IN-2, diastereoisomer of CXCR2-IN-2 (compound 68), is a brain penetrant CXCR2 antagonist with a pIC50 of 9 and 6.8 in the Tango assay and d in the HWB Gro-α induced CD11b expression assay, respectively.
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- HY-148465
-
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Gadoteric acid
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Biochemical Assay Reagents
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Cancer
Cardiovascular Disease
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Gadoteric acid is a macrocyclic, paramagnetic, gadolinium-based contrast agent that can be used for magnetic resonance imaging (MRI) of the brain, spine, and related tissues. In particular, Gadoteric acid is able to detect and visualize areas of blood-brain barrier disruption and abnormal vascular distribution.
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- HY-W017443
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- HY-12938
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AMG-8718
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Beta-secretase
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Neurological Disease
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AMG-8718 is a potent, selective and orally active BACE1 inhibitor with IC50 values of 0.0007, 0.005 µM for BACE1 and BACE2, respectively. AMG-8718 significantly decreases Aβ40 levels in the CSF and brain.
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- HY-D1704
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- HY-148233S
-
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JNJ-6204
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Casein Kinase
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Others
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JNJ-6204 is a dual inhibitor for CSNK1D (Casein Kinase 1 Delta) and CSNK1E (Casein Kinase 1 Epsilon) (CSNK1D IC50=2.3 nM; CSNK1E IC50=137 nM). JNJ-6204 shows good brain exposure[1][2].
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- HY-N8115
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- HY-120947
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AV-105
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Others
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Neurological Disease
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AV-105 is a Florbetapir ( 18F)-radiolabeled slyrylpyridine tosylate precursor extracted from patent WO2010078370A1, example 1.5. AV-105 can synthesize 18F-radiolabeled compounds, which are used for positron emission tomography (PET) imaging of neurodegenerative diseases of the brain.
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- HY-148304
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- HY-148304A
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- HY-121488
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- HY-138879
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CP-601927
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nAChR
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Neurological Disease
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CP-601927 is a selective α4β2 nicotinic acetylcholine receptor (nAChR) partial agonist (Ki=1.2 nM; EC50=2.6 μM). CP-601927 shows good brain penetration and antidepressant-like properties.
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- HY-101872A
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GSK-872 hydrochloride
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RIP kinase
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Inflammation/Immunology
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GSK-872 hydrochloride is a RIPK3 inhibitor, which binds RIP3 kinase domain with an IC50 of 1.8 nM, and inhibits kinase activity with an IC50 of 1.3 nM. GSK-872 hydrochloride decreases the RIPK3-mediated necroptosis and subsequent cytoplasmic translocation and expression of HMGB1, as well as ameliorates brain edema and neurological deficits in early brain injury.
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- HY-P1061
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Colivelin
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STAT
Amyloid-β
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Neurological Disease
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Colivelin is a brain penetrant neuroprotective peptide and a potent activator of STAT3, suppresses neuronal death by activating STAT3 in vitro. Colivelin exhibits long-term beneficial effects against neurotoxicity, Aβ deposition, neuronal apoptosis, and synaptic plasticity deficits in neurodegenerative disease. Colivelin has the potential for the treatment of alzheimer's disease and ischemic brain injury
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- HY-101872
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GSK-872
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RIP kinase
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Inflammation/Immunology
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GSK-872 is a RIPK3 inhibitor, which binds RIP3 kinase domain with an IC50 of 1.8 nM, and inhibits kinase activity with an IC50 of 1.3 nM. GSK-872 decreases the RIPK3-mediated necroptosis and subsequent cytoplasmic translocation and expression of HMGB1, as well as ameliorates brain edema and neurological deficits in early brain injury.
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- HY-145887
-
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BCR-ABL1-IN-1
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Bcr-Abl
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Neurological Disease
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BCR-ABL1-IN-1 is a potent, orally active, and specific inhibitor of ABL kinase. BCR-ABL1-IN-1 has potential for elucidating the role of ABL kinases in the brain in non-clinical studies.
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- HY-P1061A
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Colivelin TFA
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STAT
Amyloid-β
Apoptosis
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Neurological Disease
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Colivelin TFA is a brain penetrant neuroprotective peptide and a potent activator of STAT3, suppresses neuronal death by activating STAT3 in vitro. Colivelin TFA exhibits long-term beneficial effects against neurotoxicity, Aβ deposition, neuronal apoptosis, and synaptic plasticity deficits in neurodegenerative disease. Colivelin TFA has the potential for the treatment of alzheimer's disease and ischemic brain injury.
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- HY-134661A
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CVN424
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GPR6
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Neurological Disease
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CVN424 is an orally active and selective GPR6 inverse agonist with a Ki of 9.4 nM and an EC50 of 38 nM. CVN424 is brain-penetrant and has the potential for Parkinson disease research.
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- HY-107731
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- HY-145127
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ETZ
C3-CA-DTZ
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Fluorescent Dye
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Neurological Disease
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ETZ (C3-CA-DTZ) is a promising luciferase substrate (prosubstrate) activatable in vivo by nonspecific esterase to enhance the brain delivery of the luciferin.
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- HY-100605
-
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VU0483605
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mGluR
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Others
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VU0483605 is a potent and brain-penetrated mGlu1 receptor positive allosteric modulator (PAM). VU0483605 shows excellent mGlu1 PAM activity at both human and rat, with EC50 values of 390 and 356 nM, respectively.
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- HY-N4134
-
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Ciwujianoside C3
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NO Synthase
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Inflammation/Immunology
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Ciwujianoside C3, an orally active and brain penetrated compound, is isolated the leaves of Acanthopanax henryi Harms. Ciwujianoside C3 has anti-inflammatory effect and can reinforces object recognition memory.
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- HY-103530
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CGP35348
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GABA Receptor
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Neurological Disease
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CGP 35348 is a selective, brain penetrant, centrally active GABAB receptor antagonist with an EC50 of 34 μM. CGP 35348 shows affinity for the GABAB receptor only. CGP 35348 has a potential to improve neuromuscular coordination and spatial learning in albino mouse following neonatal brain damage.
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- HY-W076067
-
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Ammonium tetrathiomolybdate(VI)
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Others
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Neurological Disease
|
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Ammonium tetrathiomolybdate(VI) is a copper chelator and also is a class of sulfide donor. Ammonium tetrathiomolybdate(VI) has neuroprotection effects. Ammonium tetrathiomolybdate(VI) can be used for the research of brain ischemia.
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- HY-13452
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- HY-130609A
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Aβ42-IN-1 free base
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γ-secretase
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Neurological Disease
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Aβ42-IN-1 free base (compound 1v) is an orally active, high brain exposure γ-secretase modulator. Aβ42-IN-1 free base potently reduces Aβ42 levels with an IC50 value of 0.091 µM, and significantly reduces brain Aβ42 levels in mice. Aβ42-IN-1 free base is a promising compound for the treatment of Alzheimer’s disease.
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- HY-N2433
-
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Paederosidic acid methyl ester
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Potassium Channel
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Neurological Disease
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Paederosidic acid methyl ester is a ATP‐sensitive K + channel activator, isolated from P. scandens. Paederosidic acid methyl ester exhibits significant central analgesic activity, and enhances the threshold of pain by activating ATP‐sensitive K + channel in the brain and spinal cord level.
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- HY-118140
-
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ZCZ011
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Cannabinoid Receptor
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Inflammation/Immunology
Neurological Disease
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ZCZ011 is a potent and brain penetrant cannabinoid 1 (CB1) receptor positive allosteric modulator. ZCZ011 potentiates binding of CP55,940 to the CB1 receptor, enhances anandamide (AEA)-stimulated GTPγS binding in mouse brain membranes. ZCZ011 increases β-arrestin recruitment and ERK phosphorylation in hCB1 cells. ZCZ011 can be used for researching neuropathic and inflammatory pain.
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- HY-N6906
-
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Oleuroside
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Others
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Neurological Disease
|
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Oleuroside is a phenolic secoiridoid in olive. Oleuroside can protect against mitochondrial dysfunction in models of early Alzheimer's disease and brain ageing.
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- HY-106968
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ZD-9379
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iGluR
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Neurological Disease
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ZD-9379 is a potent, orally active, and brain penetrant full antagonist at the glycine site of the NMDA receptor. ZD-9379 has neuroprotective effect.
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- HY-12624
-
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Narazaciclib
ON123300
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CDK
AMPK
PDGFR
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Cancer
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Narazaciclib (ON123300), a strong and brain-penetrant multi-kinase inhibitor, inhibits CDK4 (IC50=3.9 nM), Ark5 (IC50=5 nM), PDGFRβ (IC50=26 nM), FGFR1 (IC50=26 nM), RET (IC50=9.2 nM), and FYN (IC50=11 nM). Single agent Narazaciclib causes a dose-dependent suppression of phosphorylation of Akt as well as activation of Erk in brain tumors. Narazaciclib inhibits CDK6 with an IC50 of 9.82 nM.
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- HY-149025
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DPTIP-prodrug 18
P18
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Phospholipase
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Inflammation/Immunology
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DPTIP-prodrug 18 (P18) is a orally active and brain-penetrable prodrug of DPTIP (HY-131002). DPTIP-prodrug 18 is a potent nSMase2 inhibitor. DPTIP-prodrug 18 significantly inhibits IL-1β-induced EV (extracellular vesicle) release by inhibition of nSMase2 (neutral sphingomyelinase-2) activity. DPTIP-prodrug 18 can be used for brain injury research.
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- HY-101988
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- HY-139300
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Epitinib
HMPL-813
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EGFR
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Cancer
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Epitinib is an orally active and selective epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI) designed for optimal brain penetration. Epitinib can be used for the research of cancer.
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- HY-111475
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- HY-131036
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MAO-IN-M30 dihydrochloride
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Monoamine Oxidase
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Neurological Disease
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MAO-IN-M30 dihydrochloride is an orally active, brain-permeable, and brain selective irreversible MAO-A (IC50=37 nM) and MAO-B (IC50=57 nM) inhibitor. MAO-IN-M30 dihydrochloride is a potent iron chelator and radical scavenger. MAO-IN-M30 dihydrochloride has a neuroprotective effect against Dexamethasone-induced brain cell apoptosis. MAO-IN-M30 dihydrochloride also exhibits neurorestorative activity in post MPTP and lactacystin models of Parkinson's disease.
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- HY-139300A
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Epitinib succinate
HMPL-813 succinate
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EGFR
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Cancer
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Epitinib succinate is an orally active and selective epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI) designed for optimal brain penetration. Epitinib succinate can be used for the research of cancer.
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- HY-137499
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NT1-O12B
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Endogenous Metabolite
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Neurological Disease
|
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NT1-O12B, an endogenous chemical and a neurotransmitter-derived lipidoid (NT-lipidoid), is an effective carrier for enhanced brain delivery of several blood-brain barrier (BBB)-impermeable cargos. Doping NT1-O12B into BBB-impermeable lipid nanoparticles (LNPs) gives the LNPs the ability to cross the BBB. NT-lipidoids formulation not only facilitate cargo crossing of the BBB, but also delivery of the cargo into neuronal cells for functional gene silencing or gene recombination.
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- HY-132579
-
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Tominersen
RG6042; IONIS-HTTRx
|
Huntingtin
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Neurological Disease
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Tominersen (RG6042) is a second-generation 2′-O-(2-methoxyethyl) antisense oligonucleotide that targets huntingtin protein (HTT) mRNA and potently suppresses HTT production. Tominersen improves survival and reduces brain atrophy in mice. Tominersen can be used for the research of Huntington’s disease (HD).
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- HY-116663
-
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(±)20-HDHA
(±)20-HDoHE
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Endogenous Metabolite
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Neurological Disease
|
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(±)20-HDHA ((±)20-HDoHE) is a racemic mixture and is an autoxidation product of Docosahexaenoic acid (DHA). (±)20-HDHA is also formed by peroxidation process in human platelets and rat brain homogenate.
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- HY-P9967
-
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Aducanumab
BIIB037
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Amyloid-β
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Neurological Disease
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Aducanumab (BIIB037), a human monoclonal antibody selective for aggregated forms of amyloid beta (Aβ). Aducanumab shows brain penetration, and can be used for Alzheimer's disease (AD) research.
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- HY-B0033
-
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Vigabatrin hydrochloride
γ-Vinyl-GABA hydrochloride
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GABA Receptor
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Neurological Disease
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Vigabatrin hydrochloride (γ-Vinyl-GABA hydrochloride), a inhibitory neurotransmitter GABA vinyl-derivative, is an orally active and irreversible GABA transaminase inhibitor. Vigabatrin hydrochloride is an antiepileptic agent, which acts by increasing GABA levels in the brain by inhibiting the catabolism of GABA by GABA transaminase.
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- HY-15399
-
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Vigabatrin
γ-Vinyl-GABA
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GABA Receptor
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Neurological Disease
|
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Vigabatrin (γ-Vinyl-GABA), an inhibitory neurotransmitter GABA vinyl-derivative, is an orally active and irreversible GABA transaminase inhibitor. Vigabatrin is an antiepileptic agent, which acts by increasing GABA levels in the brain by inhibiting the catabolism of GABA by GABA transaminase.
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- HY-N10528
-
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- HY-112248A
-
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- HY-17001
-
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- HY-105155
-
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Lobradimil
RMP 7
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Bradykinin Receptor
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Cancer
|
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Lobradimil (RMP 7), a synthetic bradykinin analog, is a potent and selective bradykinin B2 receptor agonist (Ki: 0.54 nM). Lobradimil increases the permeability of the BBB. Lobradimil can be used in the research of brain tumors.
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- HY-W278944
-
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Antiproliferative agent-15
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Others
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Cancer
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Antiproliferative agent-15 is an anticancer agent. Antiproliferative agent-15 shows antiproliferative activity against human colon (HCT116 and HCT15) and brain (LN-229 and GBM-10) cancer cell lines.
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- HY-116565
-
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Usmarapride
SUVN-D4010
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5-HT Receptor
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Neurological Disease
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Usmarapride (SUVN-D4010) is a potent, selective, orally active and brain penetrant 5-HT4 receptor partial agonist (EC50=44 nM). Usmarapride (SUVN-D4010) can be used for the research of cognitive deficits associated with Alzheimer's disease.
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- HY-P2136
-
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- HY-151391
-
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LPA5 antagonist 1
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Others
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Neurological Disease
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LPA5 antagonist 1 (Compound 66) is a potent and selective lysophosphatidic acid receptor 5 (LPA5) antagonist (IC50=32 nM). LPA5 antagonist 1 shows high brain permeability and anti-nociceptive activity. LPA5 antagonist 1 can be used in inflammatory and neuropathic pain research.
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- HY-148246
-
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MU1700
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TGF-β Receptor
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Cancer
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MU1700 is an orally active and potent ALK1/2 inhibitor with IC50s of 13 nM and 6 nM, respectively. MU1700 shows cell membrane permeability and high brain permeability.
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- HY-101247
-
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MTPG
|
mGluR
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Neurological Disease
|
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MTPG is a potent mGluR2 and mGluR3 antagonist. MTPG can block the induction of brain ischemic tolerance induced by cerebral ischemic preconditioning. MTPG also significantly attenuates the inhibitory effect of L-CCG-1 on the KCl-evoked dopamine release.
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- HY-115766
-
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Anabaseine
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nAChR
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Neurological Disease
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Anabaseine is a non-selective nicotinic agonist. Anabaseine stimulates all AChRs, preferentially stimulates skeletal muscle and brain α7 subtypes. Anabaseine is also a weak partial agonist at α4β2 nAChRs.
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- HY-102050
-
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- HY-147873
-
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NMDAR/HDAC-IN-1
|
iGluR
HDAC
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Neurological Disease
|
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NMDAR/HDAC-IN-1 (Compound 9d) is a dual NMDAR and HDAC inhibitor with a Ki of 0.59 μM for NMDAR and IC50 values of 2.67, 8.00, 2.21, 0.18 and 0.62 μM for HDAC1, HDAC2, HDAC3, HDAC6 and HDAC8, respectively. NMDAR/HDAC-IN-1 efficiently penetrates the blood brain barrier.
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- HY-P3883
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- HY-116565A
-
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Usmarapride free base
SUVN-D4010 free base
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5-HT Receptor
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Neurological Disease
|
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Usmarapride (SUVN-D4010) free base is a potent, selective, orally active and brain penetrant 5-HT4 receptor partial agonist (EC50=44 nM). Usmarapride (SUVN-D4010) free base can be used for the research of cognitive deficits associated with Alzheimer's disease.
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- HY-109097
-
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Otaplimastat
SP-8203
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MMP
iGluR
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Neurological Disease
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Otaplimastat (SP-8203), a matrix metalloproteinase (MMP) inhibitor, blocks N-methyl-D-aspartate (NMDA) receptor-mediated excitotoxicity in a competitive manner. Otaplimastat also exhibits anti-oxidant activity. Otaplimastat can be used for the research of brain ischemic injury.
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- HY-13977A
-
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PKR-IN-C16
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Apoptosis
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Neurological Disease
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PKR-IN-C16 (Compound C16) is a specific double-stranded RNA-dependent protein kinase (PKR) inhibitor. PKR-IN-C16 shows promising neuroprotective properties and can rescue acute brain lesions.
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- HY-N3383
-
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Ligustroside
Ligstroside
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Mitochondrial Metabolism
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Neurological Disease
|
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Ligustroside (Ligstroside), a secoiridoid derivative, has outstanding performance on mitochondrial bioenergetics in models of early Alzheimer's disease (AD) and brain ageing by mechanisms that may not interfere with Aβ production. Ligustroside significantly inhibits nitric oxide production in lipopolysaccharide-activated RAW264.7 macrophages.
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- HY-10936
-
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S 18986
|
iGluR
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Neurological Disease
|
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S 18986 is a selective, orally active, brain penetrant positive allosteric modulator of AMPA-type receptors. S 18986 shows cognitive enhancing properties in rodents. S 18986 activates the release of noradrenaline and acetylcholine in rat hippocampus and enhances rat memory in object-recognition tests.
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- HY-135507
-
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NAS-181
|
5-HT Receptor
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Neurological Disease
|
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NAS-181 is a potent and selective rat 5-hydroxytryptamine1B (r5-HT1B) antagonist with an Ki value of 47 nM. NAS-181 increases the 5-HTP accumulation in rat brain regions.
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- HY-103463
-
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SA57
|
FAAH
MAGL
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Neurological Disease
|
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SA57 is a potent, selective FAAH inhibitor with IC50s of 3.2 nM and 1.9 nM for mouse and human FAAH. SA57 also inhibits the 2-arachidonoylglycerol hydrolases MAGL (IC50s of 410 nM and 1.4 μM for mouse and human MAGL) and mouse α/β-hydrolase domain-containing protein 6 (mABHD6; IC50 of 850 nM), but not other brain serine hydrolases.
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- HY-14325
-
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L-745870
|
Dopamine Receptor
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Neurological Disease
|
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L-745870 is a potent, selective, brain-penetrant and orally active dopamine D4 receptor antagonist with a Ki of 0.43 nM. L-745870 shows weaker affinity for D2 (Ki of 960 nM) and D3 (Ki of 2300 nM) receptors, and exhibits moderate affinity for 5-HT2 receptors, sigma sites and α-adrenoceptors.
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- HY-145906
-
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D4R antagonis-2
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Dopamine Receptor
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Neurological Disease
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D4R antagonist-2 is a potent and selective D4R antagonist with an IC50 of 6.52 µM. D4R antagonist-2 displays very favorable in vitro PK parameters and has good brain penetration. D4R antagonist-2 has the potential for the research of Parkinson’s disease.
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-
- HY-14325B
-
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L-745870 hydrochloride
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Dopamine Receptor
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Neurological Disease
|
|
L-745870 hydrochloride is a potent, selective, brain-penetrant and orally active dopamine D4 receptor antagonist with a Ki of 0.43 nM. L-745870 hydrochloride shows weaker affinity for D2 (Ki of 960 nM) and D3 (Ki of 2300 nM) receptors, and exhibits moderate affinity for 5-HT2 receptors, sigma sites and α-adrenoceptors.
|
-
- HY-148137
-
-
- HY-139662
-
|
HB007
|
E1/E2/E3 Enzyme
|
Cancer
|
|
HB007 is a small ubiquitin-related modifier 1 (SUMO1) degrader. HB007 induces ubiquitination and degradation of SUMO1, resulting in reduced tumor growth in vivo. HB007 can be used for the research of brain, breast, colon, and lung cancers.
|
-
- HY-107666
-
-
- HY-117516
-
|
SR10067
|
REV-ERB
|
Metabolic Disease
Neurological Disease
|
|
SR10067 is a potent, selective and brain penetrant REV-ERB agonist. SR10067 has high affinity for Rev-Erbβ and Rev-Erbα with IC50 values of 160 nM and 170 nM, respectively. SR10067 can be used for the research of metabolic diseases and neuropsychiatric disorders.
|
-
- HY-114153
-
|
PLX5622
|
c-Fms
|
Neurological Disease
|
|
PLX5622 is a highly selective brain penetrant and orally active CSF1R inhibitor (IC50=0.016 µM; Ki=5.9 nM). PLX5622 allows for extended and specific microglial cells elimination, preceding and during pathology development. PLX5622 demonstrates desirable PK properties in varies animals.
|
-
- HY-151248
-
|
HDAC2-IN-1
|
HDAC
|
Neurological Disease
|
|
HDAC2-IN-1 (Compound 17) is a brain penetrant, orally active, competitive HDAC2 inhibitor with an IC50 of 0.5 μM. HDAC2-IN-1 also inhibits HDAC1 and HDAC8 with IC50s of 1.61 μM and 0.98 μM, respectively.
|
-
- HY-114452A
-
|
LY2940094 tartrate
BTRX-246040 tartrate
|
Opioid Receptor
|
Neurological Disease
|
|
LY2940094 (BTRX-246040) tartrate is a potent, brain penetrant, selective and orally available N/OFQ peptide (NOP) receptor antagonist with high affinity (Ki=0.105 nM) and antagonist potency (Kb=0.166 nM). LY2940094 tartrate reduces Ethanol self-administration and Ethanol seeking in animal models.
|
-
- HY-117764
-
|
LSP4-2022
|
mGluR
|
Neurological Disease
|
|
LSP4-2022 is a potent and brain-penetrant mGlu4-selective orthosteric agonist, with an EC50 of 0.11 μM. LSP4-2022 inhibits neurotransmission in cerebellar slices from wild-type but not mGlu4 receptor-knockout mice. LSP4-2022 shows pro-depressant activity.
|
-
- HY-150503
-
|
KH-259
|
HDAC
|
Neurological Disease
|
|
KH-259 (compound 1) is a potent, selective and CNS-penetrant HDAC6 inhibitor, with an IC50 of 0.26 μM. KH-259 has antidepressant effects in mice through the inhibition of HDAC6 in the brain. KH-259 can be used for neurodegenerative diseases research.
|
-
- HY-145196
-
|
RTICBM-189
|
Cannabinoid Receptor
|
Neurological Disease
|
|
RTICBM-189 is a potent, brain-penetrant allosteric modulator of the cannabinoid type-1 (CB1) receptor with a pIC50 of 7.54 in Ca 2+ mobilization assay. RTICBM-189 has pIC50s of 5.29 and 6.25 for hCB1 and mCB1, respectively. RTICBM-189 significantly and selectively attenuates the reinstatement of the cocaine-seeking behavior in rats.
|
-
- HY-10865
-
|
LY2183240
|
FAAH
Autophagy
|
Neurological Disease
|
|
LY2183240 is a highly potent blocker of anandamide uptake (IC50= 270 pM; Ki=540 nM). LY2183240 is a potent, covalent inhibitor of the endocannabinoid-degrading enzyme fatty acid amide hydrolase (FAAH) with an IC50 of 12.4 nM. LY2183240 inactivates FAAH by carbamylation of the enzyme's serine nucleophile. LY2183240 also inhibits several other brain serine hydrolases with IC50s of 5.3, 0.09, 8.2 nM for MAG lipase, bh6 and KIAA1363, respectively .
|
-
- HY-B1941
-
|
4-tert-Octylphenol
|
Endogenous Metabolite
Apoptosis
|
Endocrinology
Neurological Disease
|
|
4-tert-Octylphenol, a endocrine-disrupting chemical, is an estrogenic drug. 4-tert-Octylphenol induces apoptosis in neuronal progenitor cells in offspring mouse brain. 4-tert-Octylphenol reduces bromodeoxyuridine (BrdU), mitotic marker Ki67, and phospho-histone H3 (p-Histone-H3), resulting in a reduction of neuronal progenitor proliferation. 4-tert-Octylphenol disrupts brain development and behavior in mice.
|
-
- HY-114153A
-
|
PLX5622 hemifumarate
|
c-Fms
|
Neurological Disease
|
|
PLX5622 hemifumarate is a highly selective brain penetrant and orally active CSF1R inhibitor (IC50=0.016 µM; Ki=5.9 nM). PLX5622 hemifumarate allows for extended and specific microglial elimination, preceding and during pathology development. PLX5622 hemifumarate demonstrates desirable PK properties in varies animals.
|
-
- HY-151368
-
|
AChE/BChE-IN-10
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
AChE/BChE-IN-10 (Compound 7b) is a potent dual AChE and BChE inhibitor with IC50 values of 0.176, and 0.47 μM, respectively. AChE/BChE-IN-10 shows good blood brain barrier permeability. AChE/BChE-IN-10 can inhibit Aβ-aggregation and be used in Alzheimer’s disease (AD) research.
|
-
- HY-114883A
-
|
Homocarnosine TFA
L-Homocarnosine TFA; γ-Aminobutyryl-L-histidine TFA
|
GABA Receptor
Endogenous Metabolite
|
Neurological Disease
|
|
Homocarnosine TFA is a dipeptide of γ-aminobutyric acid (GABA) and histidine unique to brain. Homocarnosine TFA is an inhibitory neuromodulator synthesized in the neuron from GABA and exhibiting anticonvulsant effects. Homocarnosine TFA has antioxidant and anti-inflammatory actions, prevention of DNA damage, and inhibition of advanced glycation end-product formation.
|
-
- HY-144446
-
|
BuChE-IN-1
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
BuChE-IN-1 (Compound 23) is a potent inhibitor of butyrylcholinesterase (BuChE). Butyrylcholinesterase (BuChE) is recently regarded as a biomarker in progressed Alzheimer’s disease (AD). BuChE-IN-1 shows low cytotoxicity and high blood brain barrier (BBB) permeability. BuChE-IN-1 is a promising BuChE inhibitor for the research of AD.
|
-
- HY-101059
-
|
FGIN 1-27
|
Others
|
Neurological Disease
|
|
FGIN 1-27, an indoleacetamide, is a specific peripheral benzodiazepine receptor (PBR) ligand with a Ki of 5.0 nM. FGIN 1-27 can penetrate the blood brain barrier (BBB). FGIN 1-27 inhibits the onset of Isoniazid-induced convulsions.
|
-
- HY-102064
-
|
SR 57227A
|
5-HT Receptor
|
Neurological Disease
|
|
SR 57227A is a potent, orally active and selective 5-HT3 receptor agonist, with ability to cross the blood brain barrier. SR 57227A has affinities (IC50) varying between 2.8 and 250 nM for 5-HT3 receptor binding sites in rat cortical membranes and on whole NG 108-15 cells or their membranes. Anti-depressant effects.
|
-
- HY-122218
-
|
JHU-083
|
Glutaminase
|
Neurological Disease
|
|
JHU-083, a prodrug of 6-diazo-5-oxo-L-norleucine (DON; HY-108357), is an orally active and selective glutaminase antagonist. JHU-083 blocks glutaminase activity in brain CD11b + cells and experimental cerebral malaria (ECM) resulting in a net decrease of glutamate levels in the animals.
|
-
- HY-120124
-
|
Samelisant
SUVN-G3031
|
Histamine Receptor
|
Neurological Disease
|
|
Samelisant (SUVN-G3031) is a potent and selective histamine H3 receptor (H3R) inverse agonist with good brain penetration and oral bioavailability. Samelisant has a similar binding affinity towards human (hH3R; Ki=8.7 nM) and rat (rH3R;Ki=9.8 nM) H3R indicating no inter-species differences. Samelisant can be used for the research of sleep-related disorders.
|
-
- HY-110146
-
|
XAP044
|
mGluR
|
Neurological Disease
|
|
XAP044 is a potent and selective antagonist of mGlu7. The metabotropic glutamate receptor subtype 7 (mGlu7) is an important presynaptic regulator of neurotransmission in the mammalian CNS. XAP044 demonstrates good brain exposure and wide spectrum anti-stress and antidepressant- and anxiolytic-like efficacy in rodent behavioral paradigms.
|
-
- HY-145313
-
|
TTBK1-IN-2
|
Others
|
Neurological Disease
|
|
TTBK1-IN-2 (compound 29) is a potent Tau-Tubulin kinase (TTBK1) inhibitor with IC50s of 0.24 and 4.22 µM, respectively. TTBK1-IN-2 reveals good brain penetration in vivo and is able to reduce TDP-43 phosphorylation not only in cell cultures but also in the spinal cord of transgenic TDP-43 mice.
|
-
- HY-122608
-
|
Samelisant free base
SUVN-G3031 free base
|
Histamine Receptor
|
Neurological Disease
|
|
Samelisant (SUVN-G3031) free base is a potent and selective histamine H3 receptor (H3R) inverse agonist with good brain penetration and oral bioavailability. Samelisant free base has a similar binding affinity towards human (hH3R; Ki=8.7 nM) and rat (rH3R;Ki=9.8 nM) H3R indicating no inter-species differences. Samelisant free base can be used for the research of sleep-related disorders.
|
-
- HY-105670
-
|
PHA-543613
|
nAChR
|
Neurological Disease
|
|
PHA-543613 is a potent, orally active, brain-penetrant and selective α7 nAChR agonist with a Ki of 8.8 nM. PHA-543613 displays selectivity for α7-nAChR over α3β4, α1β1γδ, α4β2 and 5-HT3 receptors. PHA-543613 can be used for the cognitive deficits of Alzheimer's disease and schizophrenia research.
|
-
- HY-11044
-
-
- HY-103210
-
|
DSP-4 hydrochloride
Neurotoxin DSP 4 hydrochloride
|
Others
|
Neurological Disease
|
|
DSP-4 hydrochloride is a highly and selective adrenergic neurotoxin. DSP-4 hydrochloride can cross the blood brain barrier. DSP-4 hydrochloride can be used for the temporary selective degradation of the central and peripheral noradrenergic neurons.
|
-
- HY-120596
-
-
- HY-12959
-
|
Repinotan
BAY x 3702 free base
|
5-HT Receptor
|
Neurological Disease
|
|
Repinotan (BAY x 3702 free base) is a potent, selective, brain-penetrant and orally active 5-HT1A receptor agonist, with Ki values of 0.19 nM (calf hippocampus), 0.25 nM (rat and human cortex), and 0.59 nM (rat hippocampus). Repinotan has a weak affinity for other related receptors. Repinotan has pronounced neuroprotective effects.
|
-
- HY-101446
-
|
HIOC
|
Trk Receptor
ERK
Apoptosis
|
Neurological Disease
|
|
HIOC is a potent and selective activator of TrkB (tropomyosin related kinase B) receptor. HIOC can pass the blood-brain and blood-retinal barriers.HIOC activates TrkB/ERK pathway and decreases neuronal cell apoptosis. HIOC attenuates early brain injury after SAH (subarachnoid hemorrhage). HIOC shows protective activity in an animal model for light-induced retinal degeneration.
|
-
- HY-12844
-
|
Ro 64-6198
|
Opioid Receptor
|
Neurological Disease
|
|
Ro 64-6198 is a potent, selective, nonpeptide, high-affinity, high cellular permeability and brain penetration N/OFQ receptor (NOP) agonist with an EC50 value of 25.6 nM. Ro 64-6198 is at least 100 times more selective for the NOP receptor over the classic opioid receptors. Ro 64-6198 can be used for stress and anxiety, addiction, neuropathic pain, cough, and anorexia.
|
-
- HY-105670B
-
|
PHA-543613 dihydrochloride
|
nAChR
|
Neurological Disease
|
|
PHA-543613 dihydrochloride is a potent, orally active, brain-penetrant and selective α7 nAChR agonist with a Ki value of 8.8 nM. PHA-543613 dihydrochloride displays selectivity for α7-nAChR over α3β4, α1β1γδ, α4β2 and 5-HT3 receptors. PHA-543613 dihydrochloride can be used for the cognitive deficits of Alzheimer's disease and schizophrenia research.
|
-
- HY-101181
-
|
THK-5105
|
Microtubule/Tubulin
|
Neurological Disease
|
|
THK-5105, an arylquinoline derivative, displays high binding affinity to tau fibrils. THK-5105 has high binding affinity to tau protein aggregates and tau-rich Alzheimer disease (AD) brain homogenates. 18F-THK-5105 has the potential to act as a tau imaging PET probe.
|
-
- HY-N2326
-
|
(±)-Anatoxin A fumarate
|
nAChR
|
Neurological Disease
|
|
(±)-Anatoxin A fumarate is a natural alkaloid isolated from freshwater cyanobacterium.(±)-Anatoxin A fumarate is a potent nicotinic receptor agonist and exhibits Ki values of 1.25 nM and 1.84 μM for binding to putative α4β2-type nAChR and α7-type nAChR in rat brain membranes, respectively. (±)-Anatoxin A fumarate stimulates [ 3H]-dopamine release from rat striatal synaptosomes (EC50=134 nM).
|
-
- HY-14533
-
|
K 01-162
K162
|
Amyloid-β
|
Neurological Disease
|
|
K 01-162 (K162) inhibits the fibril formation of Aβ peptides and eliminates their neurotoxicity. K 01-162 binds with Aβ42 peptide with an EC50 value of 80 nM. K 01-162 binds directly to AβO with a KD value of 19 μM. K 01-162 is capable of penetrating the brain and can be used for the research of Alzheimer’s disease.
|
-
- HY-101182
-
|
THK-5117
|
Microtubule/Tubulin
|
Neurological Disease
|
|
THK-5117, an arylquinoline derivative, displays high binding affinity to tau fibrils with a Ki of 10.5 nM. THK-5117 has high binding affinity to tau protein aggregates and tau-rich Alzheimer disease (AD) brain homogenates. 18F-THK-5117 has the potential to act as a tau imaging PET probe.
|
-
- HY-B0007
-
|
Baclofen
|
GABA Receptor
|
Neurological Disease
|
|
Baclofen, a lipophilic derivative of γ-aminobutyric acid (GABA), is an orally active, selective metabotropic GABAB receptor (GABABR) agonist. Baclofen mimics the action of GABA and produces slow presynaptic inhibition through the GABAB receptor. Baclofen has high blood brain barrier penetrance. Baclofen has the potential for muscle spasticity research.
|
-
- HY-101834
-
|
ACT-462206
|
Orexin Receptor (OX Receptor)
|
Others
|
|
ACT-462206 is an orally active and potent dual Orexin 1/Orexin 2 receptor antagonist with IC50s of 60 nM (Orexin 1) and 11 nM (Orexin 2), respectively. ACT-462206 exhibits brain penetration properties, and can be used for insomnia, stress/anxiety-related disorders and addiction research.
|
-
- HY-B0007C
-
|
Baclofen hydrochloride
|
GABA Receptor
|
Neurological Disease
|
|
Baclofen hydrochloride, a lipophilic derivative of γ-aminobutyric acid (GABA), is an orally active, selective metabotropic GABAB receptor (GABABR) agonist. Baclofen hydrochloride mimics the action of GABA and produces slow presynaptic inhibition through the GABAB receptor. Baclofen hydrochloride has high blood brain barrier penetrance. Baclofen hydrochloride has the potential for muscle spasticity research.
|
-
- HY-N0148
-
|
Rutin
Rutoside; Quercetin 3-O-rutinoside
|
Amyloid-β
Autophagy
Apoptosis
Endogenous Metabolite
|
Inflammation/Immunology
Cancer
|
|
Rutin (Rutoside) is a flavonoid found in many plants and shows a wide range of biological activities including anti-inflammatory, antidiabetic, antioxidant, neuroprotective, nephroprotective, hepatoprotective and reducing Aβ oligomer activities. Rutin can cross the blood brain barrier. Rutin attenuates vancomycin-induced renal tubular cell apoptosis via suppression of apoptosis, mitochondrial dysfunction, and oxidative stress.
|
-
- HY-133016
-
|
M8891
|
Others
|
Cancer
Cardiovascular Disease
|
|
M8891 is an orally active, reversible and brain penetrant Methionine Aminopeptidase-2 (MetAP-2) inhibitor with an IC50 of 54 nM and a Ki of 4.33 nM. M8891 does not inhibit MetAP-1 (IC50>10 µM). M8891 inhibits growth of primary endothelial cells as well as tumor cells and demonstrates antiangiogenic and antitumoral activity.
|
-
- HY-N0148A
-
|
Rutin hydrate
Rutoside hydrate; Quercetin 3-O-rutinoside hydrate
|
Amyloid-β
Autophagy
Apoptosis
Endogenous Metabolite
|
Cancer
Neurological Disease
|
|
Rutin (Rutoside) hydrate is a flavonoid found in many plants and shows a wide range of biological activities including anti-inflammatory, antidiabetic, antioxidant, neuroprotective, nephroprotective, hepatoprotective and reducing Aβ oligomer activities. Rutin hydrate can cross the blood brain barrier. Rutin hydrate attenuates vancomycin-induced renal tubular cell apoptosis via suppression of apoptosis, mitochondrial dysfunction, and oxidative stress.
|
-
- HY-148236
-
|
BAY-390
|
TRP Channel
|
Inflammation/Immunology
|
|
BAY-390 is a selective, across species active and brain penetrating TRPA1 inhibitor. BAY-390 inhibits hTRPA1 FLIPR, hTRPA1 Ephys, rTRPA1 FLIPR and rDRG Ephys with IC50s of 16, 82, 63 and 35 nM, respectively. BAY-390 can be used for the research of inflammation.
|
-
- HY-14405A
-
|
Casopitant mesylate
GW679769B
|
Neurokinin Receptor
Cytochrome P450
|
Neurological Disease
Cancer
|
|
Casopitant mesylate (GW679769B) is a potent, selective, brain permeable and orally active neurokinin 1 (NK1) receptor antagonist. Casopitant mesylate is a second in the class of antiemetics that acts to antagonise the emetogenic effect of substance P. Casopitant mesylate is also a substrate and a weak-to-moderate inhibitor of CYP3A4. Casopitant mesylate can be used for chemotherapy-induced nausea and vomiting (CINV) and postoperative nausea and vomiting (PONV).
|
-
- HY-123410
-
|
KM-233
|
Cannabinoid Receptor
|
Cancer
|
|
KM-233 is a classical cannabinoid with good blood brain barrier penetration. KM-233 possesses a selective affinity for the CB2 receptors relative to THC. KM-233 is effective at reducing U87 glioma tumor burden, and can be used for glioma research.
|
-
- HY-151547
-
|
MRS4719
|
P2X Receptor
|
Neurological Disease
|
|
MRS4719 is a potent P2X4 receptor antagonist with an IC50 value of 0.503 μM for human P2X4 receptor. MRS4719 can reduce infarct volume and reduce brain atrophy, showing neuroprotective and neuro-rehabilitative activities in ischemic stroke model. MRS4719 also reduces ATP-induced [Ca 2+]i influx in primary human monocyte-derived macrophages. MRS4719 can be used to research ischemic stroke.
|
-
- HY-152148
-
|
JZP-MA-11
|
MAGL
|
Neurological Disease
|
|
JZP-MA-11 is a positron emission tomography (PET) ligand targeting the endocannabinoid α/β-hydrolase domain 6 (ABHD6) enzyme. JZP-MA-11 selectively inhibits ABHD6 with an IC50 value of 126 nM. JZP-MA-11 can cross the blood-brain barrier (BBB). [18F]JZP-MA-11 has the potential for preclinical evaluation targeting the brain ABHD6 in mice and nonhuman primate (NHP).
|
-
- HY-120251A
-
|
Leteprinim potassium
AIT-082
|
Reactive Oxygen Species
|
Neurological Disease
|
|
Leteprinim potassium (AIT-082) is a hypoxanthine derivative neurotrophic agent. Leteprinim potassium can induce brain-derived neurotrophic factor (BDNF) mRNA production following spinal cord lesions, and nerve growth factor (NGF) mRNA production in basal forebrain. Leteprinim potassium reduces glutamate toxicity in cultured hippocampal neurons. Leteprinim potassium increases heme-oxygenase 1 and 2 mRNA levels that play role in cellular defense against reactive oxygen species. Leteprinim potassium has neuroprotective activity.
|
-
- HY-148825
-
-
- HY-B0007S
-
|
Baclofen-d4
|
GABA Receptor
|
Neurological Disease
|
|
Baclofen-d4 is the deuterium labeled Baclofen. Baclofen, a lipophilic derivative of γ-aminobutyric acid (GABA), is an orally active, selective metabotropic GABAB receptor (GABABR) agonist. Baclofen mimics the action of GABA and produces slow presynaptic inhibition through the GABAB receptor. Baclofen has high blood brain barrier penetrance. Baclofen has the potential for muscle spasticity research[1][2][3].
|
-
- HY-143877
-
|
NN-390
|
HDAC
|
Cancer
|
|
NN-390 is a potent and selective HDAC6 inhibitor, with an IC50 of 9.8 nM. NN-390 penetrates the blood-brain barrier (BBB). NN-390 shows study potential in metastatic Group 3 MB (medulloblastoma).
|
-
- HY-103157
-
|
PD146176
NSC168807
|
Autophagy
Ferroptosis
|
Cardiovascular Disease
|
|
PD146176 (NSC168807), a 15-Lipoxygenase (15-LO) inhibitor, inhibits rabbit reticulocyte 15-LO (Ki=197 nM, IC50=0.54 μM). PD146176 reverses cognitive impairment, brain amyloidosis, and tau pathology by stimulating autophagy in aged triple transgenic mice.
|
-
- HY-B0205
-
-
- HY-110206
-
|
AM6545
|
Cannabinoid Receptor
|
Metabolic Disease
|
|
AM6545 is a peripherally active, cannabinoid receptor antagonist with limited brain penetration. AM6545 binds to CB1 and CB2 receptors with Kis of 1.7 nM and 523 nM, respectively. AM6545 is a neutral antagonist. AM6545 can be used for the research of obesity and its complications.
|
-
- HY-126899
-
|
TPI-287
|
Microtubule/Tubulin
|
Cancer
|
|
TPI-287, a blood-brain barrier-permeable microtubule stabilizer, can significantly reduce metastatic colonization of breast cancer in the brain.
|
-
- HY-120878
-
|
CXCR2-IN-2
|
CXCR
|
Inflammation/Immunology
|
|
CXCR2-IN-2 is a selective, brain penetrant, and orally bioavailable CXCR2 antagonist (IC50=5.2 nM/1 nM in β-arrestin assay/CXCR2 Tango assay, respectively). CXCR2-IN-2 displays ~730-fold selectivity over CXCR1 and >1900-fold selectivity over all other chemokine receptors. CXCR2-IN-2 inhibits human whole blood Gro-α induced CD11b expression with an IC50 of 0.04 μM.
|
-
- HY-13779
-
|
J-147
|
Monoamine Oxidase
Dopamine Transporter
|
Neurological Disease
|
|
J-147 is an exceptionally potent, orally active, neuroprotective agent for cognitive enhancement. J-147 can readily pass the blood brain barrier (BBB). J-147 can inhibit monoamine oxidase B (MAO B) and the dopamine transporter with EC50 values of 1.88 μM and 0.649 μM, respectively. J-147 has potential for the treatment of Alzheimer’s disease (AD).
|
-
- HY-144874
-
|
AZ3391
|
PARP
|
Cancer
Neurological Disease
|
|
AZ3391 is a potent inhibitor of PARP. AZ3391 is a quinoxaline derivative. PARP family of enzymes play an important role in a number of cellular processes, such as replication, recombination, chromatin remodeling, and DNA damage repair. AZ3391 has the potential for the research of diseases and conditions occurring in tissues in the central nervous system, such as the brain and spinal cord (extracted from patent WO2021260092A1, compound 23).
|
-
- HY-18698
-
|
L-701324
|
iGluR
|
Neurological Disease
|
|
L-701324 is a potent, orally active NMDA receptor antagonist that antagonizes the activity of the NMDA receptor by blocking its glycine B binding site. L-701324 binds with high affinity to rat brain membranes (IC50=2 nM). L-701324 has antidepressant activity.
|
-
- HY-112016
-
-
- HY-121962
-
-
- HY-136233
-
|
PSB 0777 ammonium
|
Adenosine Receptor
|
Inflammation/Immunology
|
|
PSB 0777 ammonium is a potent and selective adenosine A2A receptor full agonist with Ki values of 44.4 nM, 360 nM for rat and human A2A receptors, respectively. PSB 0777 ammonium has Ki values of ≥10000 nM, 541 nM for rat and human A1 receptors, respectively. PSB 0777 ammonium shows poor brain penetrant and perorally non-absorbable effect. PSB 0777 ammonium has the potential for inflammatory bowel disease (IBS) research research.
|
-
- HY-N9480
-
|
Vinaxanthone
SM-345431
|
Phospholipase
|
Cancer
|
|
Vinaxanthone (SM-345431) is a potent and selective semaphorin3A inhibitor. Vinaxanthone exhibits semaphorin3A inhibiting activity with an IC50 of 0.1-0.2 μM. Vinaxanthone shows selective inhibitory activity against phospholipase C (PLC) from rat brain, mutine colon 26 Adenocarcinoma and murine fibroblasts NIH3T3 with IC50s being 5.4, 9.3 and 44 μM, respectively.
|
-
- HY-W017462
-
-
- HY-109509
-
|
Enoxaparin
PK 10169; Enoxaparin sodium; Lovenox
|
Factor Xa
Thrombin
SARS-CoV
|
Infection
Inflammation/Immunology
Neurological Disease
Cardiovascular Disease
|
|
Enoxaparin (PK 10169), a low-molecular-weight heparin (LMWH) derivative. Enoxaparin exerts anticoagulant activity through antithrombin III, an endogenous inhibitor of factor Xa and thrombin IIa. Enoxaparin protect the rat hippocampus against TBI (traumatic brain injury) via antioxidant and anti-inflammatory properties. Enoxaparin can be used for the research of deep vein thrombosis (DVT), pulmonary embolism, TBI and COVID-19.
|
-
- HY-107531
-
|
A 1070722
|
GSK-3
|
Cancer
|
|
A 1070722 is a potent and selective glycogen synthase kinase 3 (GSK-3) inhibitor, with a Ki of 0.6 nM for both GSK-3α and GSK-3β. A 1070722 can penetrate the blood-brain barrier (BBB) and accumulates in brain regions, thus potential for PET radiotracer for the quantification of GSK-3 in brain.
|
-
- HY-101188
-
|
INCB38579
|
Histamine Receptor
|
Infection
|
|
INCB38579 is an orally active, highly brain penetrable, and selective histamine H4 receptor (HH4R) antagonist (hH4R IC50=4.8 nM, mH4R IC50=42 nM, rH4R IC50=32 nM). INCB38579 shows anti-inflammatory pain and anti-pruritic activities.
|
-
- HY-145858
-
|
Chalcones A-N-5
|
Ferroptosis
|
Cancer
|
|
Chalcones A-N-5 is a trihydroxy chalcone derivative compound. Chalcones A-N-5 doesn’t show cytotoxicity at the concentration lower than 100 µM (with IC50 > 1 mM), but has a significant effect on promoting cell proliferation. Chalcones A-N-5 potentially promotes neuronal cell growth in the damaged brain tissue. Chalcones A-N-5 also inhibits ferroptosis induced by RSL or erastin and reduces the lipid peroxidation levels induced by Aβ1-42 protein aggregation. Chalcones A-N-5 is a promising molecular skeleton candidate for further development of lead compound for in vivo test to research AD.
|
-
- HY-108295
-
|
Pivagabine
CXB-722
|
GABA Receptor
|
Neurological Disease
|
|
Pivagabine (CXB 722) is a hydrophobic 4-aminobutyric acid derivative with neuromodulatory activity. Pivagabine penetrates the blood-brain barrier in rats. Pivagabine antagonizes the effects of foot shock on both GABAA receptor function and corticotropin-releasing factor (CRF) concentrations in rat brain.
|
-
- HY-N2530
-
-
- HY-124813
-
|
PDZ1i
113B7
|
FAK
EGFR
MMP
|
Cancer
|
|
PDZ1i is a potent, BBB-penetrated and specific MDA-9/Syntenin inhibitor. PDZ1i inhibits crucial GBM (glioblastoma multiforme) signaling involving FAK and EGFRvIII. PDZ1i reduces MMP secretion. PDZ1i can improve survival of brain tumor-bearing mice and reduce tumor invasion.
|
-
- HY-132392S
-
-
- HY-N0435
-
-
- HY-W010347S
-
-
- HY-103253
-
|
LY231617
|
Others
|
Neurological Disease
|
|
LY231617 is a potent and blood-brain barrier penetrable antioxidant. LY231617 is a neuroprotective agent in brain, it can be used for the research of nervous disease.
|
-
- HY-W017462S
-
-
- HY-128976
-
-
- HY-109012A
-
-
- HY-P2986
-
-
- HY-123857
-
-
- HY-132310
-
|
MAGL-IN-4
|
MAGL
|
Neurological Disease
|
|
MAGL-IN-4 is an orally active, selective and reversible monoacylglycerol lipase (MAGL) inhibitor with an IC50 of 6.2 nM. MAGL-IN-4 can penetrate the blood-brain barrier (BBB). MAGL-IN-4 enhances endocannabinoid signaling mostly by the increase in the level of 2-AG via selective MAGL inhibition in the brain.
|
-
- HY-116673
-
|
TTK21
|
Histone Acetyltransferase
|
Neurological Disease
|
|
TTK21 is an activator of the histone acetyltransferases CBP/p300. TTK21 passes the blood–brain barrier, induces no toxicity, and reaches different parts of the brain when conjugated to glucose-based carbon nanosphere (CSP). TTK21 has beneficial implications for the brain functions of adult neurogenesis and long-term memory.
|
-
- HY-W105835
-
-
- HY-111653
-
-
- HY-100813
-
|
Saclofen
|
GABA Receptor
|
Neurological Disease
|
|
Saclofen is a competitive antagonist of the GABAB receptor with an IC50 of 7.8 μM. Saclofen can be used to determine the functional roles for the GABAB receptor as a mediator of slow inhibitory postsynaptic potentials in the brain.
|
-
- HY-109012
-
|
Seltorexant
JNJ-42847922
|
Orexin Receptor (OX Receptor)
|
Neurological Disease
Endocrinology
|
|
Seltorexant (JNJ-42847922) is an orally active, high-affinity, and selective orexin-2 receptor (OX2R) antagonist (pKi values of 8.0 and 8.1 for human and rat OX2R). Seltorexant (JNJ-42847922) crosses the blood-brain barrier and quickly occupies OX2R binding sites in the rat brain.
|
-
- HY-110254
-
-
- HY-139192
-
|
NMDAR/TRPM4-IN-2
|
iGluR
TRP Channel
ERK
|
Neurological Disease
|
|
NMDAR/TRPM4-IN-2 (compound 8) is a potent NMDAR/TRPM4 interaction interface inhibitor. NMDAR/TRPM4-IN-2 shows neuroprotective activity. NMDAR/TRPM4-IN-2 prevents NMDA-induced cell death and mitochondrial dysfunction in hippocampal neurons, with an IC50 of 2.1 μM. NMDAR/TRPM4-IN-2 protects mice from MCAO-induced brain damage and NMDA-induced retinal ganglion cell loss.
|
-
- HY-W010936
-
|
Nitrobenzylthioinosine
NBMPR
|
Adenosine Receptor
|
Neurological Disease
|
|
Nitrobenzylthioinosine is an ENT1 transporter inhibitor that binds to ENT1 transporter with high affinity. Nitrobenzylthioinosine is a photoaffinity probe for adenosine uptake sites in brain. Nitrobenzylthioinosine can cross the blood-brain barrier.
|
-
- HY-136201
-
|
Sodium Glucoheptonate
|
Others
|
Cancer
|
|
Sodium Glucoheptonate is used as a kit for radio-labeling with Tc-99m. Tc-99m glucoheptonate is kidney- and brain-imaging agent, and can be used in brain-tumor detection.
|
-
- HY-100921
-
-
- HY-131693
-
-
- HY-116477
-
|
URB937
|
FAAH
|
Inflammation/Immunology
Neurological Disease
|
|
URB937 is an orally active and peripherally restricted FAAH inhibitor (IC50=26.8 nM) and increases anandamide levels. URB937 fails to affect FAAH activity in the brain (not penetrate the blood-brain barrier).
|
-
- HY-147409
-
|
Ulecaciclib
|
CDK
|
Cancer
|
|
Ulecaciclib is an orally activitive inhibitor of cyclin-dependent kinase (CDK), with Ki values of 0.62 μM (CDK2/Cyclin A), 0.2 nM (CDK4/Cyclin D1), 3 nM (CDK6/Cyclin D3), and 0.63 μM (CDK7/Cyclin H), respectively. Ulecaciclib can cross blood brain barrier and has good pharmacokinetic characteristics.
|
-
- HY-W040821
-
-
- HY-12947
-
|
GNE-3511
|
MAP3K
|
Neurological Disease
|
|
GNE-3511 is an orally active bioavailable and brain-penetrant dual leucine zipper kinase (DLK) inhibitor with a Ki of 0.5 nM. GNE-3511 can cross the blood-brain-barrier and can be used for the research of neurodegenerative diseases.
|
-
- HY-107688A
-
|
UB-165 fumarate
|
nAChR
|
Neurological Disease
|
|
UB-165 fumarate is a nAChR agonist, being a full agonist of the α3β2 isoform and a partial agonist of the α4β2* isoform, with a Ki value of 0.27 nM for nicotine binding in rat brain.
|
-
- HY-N0304
-
|
L-DOPA
Levodopa; 3,4-Dihydroxyphenylalanine
|
Dopamine Receptor
Endogenous Metabolite
|
Neurological Disease
|
|
L-DOPA (Levodopa) is an orally active metabolic precursor of neurotransmitters dopamine. L-DOPA can cross the blood-brain barrier and is converted into dopamine in the brain. L-DOPA has anti-allodynic effects and the potential for Parkinson's disease.
|
-
- HY-139192A
-
|
NMDAR/TRPM4-IN-2 free base
|
iGluR
TRP Channel
ERK
|
Neurological Disease
|
|
NMDAR/TRPM4-IN-2 free base (compound 8) is a potent NMDAR/TRPM4 interaction interface inhibitor. NMDAR/TRPM4-IN-2 free base shows neuroprotective activity. NMDAR/TRPM4-IN-2 free base prevents NMDA-induced cell death and mitochondrial dysfunction in hippocampal neurons, with an IC50 of 2.1 μM. NMDAR/TRPM4-IN-2 free base protects mice from MCAO-induced brain damage and NMDA-induced retinal ganglion cell loss.
|
-
- HY-12829
-
-
- HY-129441
-
-
- HY-151615
-
|
DCI-Br-3
|
Fluorescent Dye
|
Neurological Disease
|
|
DCI-Br-3 is a rapid, highly sensitive, and selective probe to monitor thiols in the epileptic brain. (λex=537 nm, λem=675 nm).DCI-Br-3 can effectively cross the blood-brain barrier (BBB).
|
-
- HY-107688
-
|
UB-165
|
nAChR
|
Neurological Disease
|
|
UB-165 is a nAChR agonist, being a full agonist of the α3β2 isoform and a partial agonist of the α4β2* isoform, with a Ki value of 0.27 nM for [ 3H]-nicotine binding in rat brain.
|
-
- HY-101724
-
-
- HY-N0304A
-
|
L-DOPA sodium
Levodopa sodium; 3,4-Dihydroxyphenylalanine sodium
|
Dopamine Receptor
Endogenous Metabolite
|
Neurological Disease
|
|
L-DOPA (Levodopa) sodium is an orally active metabolic precursor of neurotransmitters dopamine. L-DOPA sodium can cross the blood-brain barrier and is converted into dopamine in the brain. L-DOPA sodium has anti-allodynic effects, and can be used for Parkinson's disease research.
|
-
- HY-100614
-
-
- HY-101183
-
-
- HY-B1206
-
-
- HY-136094
-
-
- HY-44157
-
|
ALS-I
|
Biochemical Assay Reagents
|
Neurological Disease
|
|
ALS-I, an acid-Liable surfactant, is adopted for in-solution enzymatic digestions, can help to solubilize hydrophobic proteins. ALS-I is significantly enhanced peptide recovery for mass spectrometry (MS) mapping in the study of the proteomes of regenerating rat retina and mouse brain.
|
-
- HY-18163A
-
-
- HY-18163
-
-
- HY-W010388
-
-
- HY-U00153
-
-
- HY-13796
-
-
- HY-N7109
-
|
Erucic acid
|
PI3K
Endogenous Metabolite
|
Neurological Disease
|
|
Erucic acid, a monounsaturated fatty acid (MUFA), is isolated from the seed of Raphanus sativus L. Erucic acid can readily cross the blood-brain barrier (BBB), it has been reported to normalize the accumulation of very long-chain fatty acids in the brain. Erucic acid can improve cognitive impairment and be effective against dementia
.
|
-
- HY-E70074
-
|
Monoamine oxidase
|
Monoamine Oxidase
|
Neurological Disease
|
|
Monoamine oxidase is an enzyme composed of different polypeptides. Monoamine oxidation catalyzes the oxidative deamination of various biological amines in brain and peripheral tissues by producing hydrogen peroxide. Monoamine oxidase plays an important role in maintaining the regulation of synaptic transmission, emotional behavior and other brain functions.
|
-
- HY-133554
-
-
- HY-103169
-
|
SCH442416
|
Adenosine Receptor
|
Neurological Disease
|
|
SCH442416 is a potent, selective and brain-penetrant antagonist of adenosine A2A receptor (A2AR), with Kis of 0.048 and 0.5 nM for human and rat A2AR respectively. SCH442416 displays more than 23000-fold selectivity over A1R, A2BR, and A3R (Ki=1111, 10000, and 10000 nM, respectively). SCH442416 can be used for imaging of adenosine A2A receptors in rat and primate brain.
|
-
- HY-12477
-
-
- HY-100026
-
|
PQR620
|
mTOR
|
Cancer
|
|
PQR620 is an orally bioavailable and selective brain penetrant inhibitor of mTORC1/2.
|
-
- HY-110281
-
-
- HY-139674
-
-
- HY-115727
-
-
- HY-18738
-
-
- HY-N0067S1
-
|
γ-Aminobutyric acid-d2
4-Aminobutyric acid-d2
|
GABA Receptor
Endogenous Metabolite
|
Neurological Disease
|
|
γ-Aminobutyric acid-d2 is the deuterium labeled γ-Aminobutyric acid. γ-Aminobutyric acid (4-Aminobutyric acid) is a major inhibitory neurotransmitter in the adult mammalian brain[1][2], binding to the ionotropic GABA receptors (GABAA receptors) and metabotropic receptors (GABAB receptors)[2].
|
-
- HY-P1303
-
|
CART(62-76)(human,rat)
|
5-HT Receptor
|
Neurological Disease
|
|
CART(62-76)(human,rat) is a neuropeptide (62-76 residues of the CART peptide) with neurotransmitter-like effects. CART(62-76)(human,rat) can modulate the activity of striatal noradrenergic and corticostriatal and hypothalamic serotoninergic (5-HT) system in the rat brain.
|
-
- HY-N0067S
-
|
γ-Aminobutyric acid-d6
4-Aminobutyric acid-d6
|
GABA Receptor
Endogenous Metabolite
|
Neurological Disease
|
|
γ-Aminobutyric acid-d6 is the deuterium labeled γ-Aminobutyric acid. γ-Aminobutyric acid (4-Aminobutyric acid) is a major inhibitory neurotransmitter in the adult mammalian brain[1][2], binding to the ionotropic GABA receptors (GABAA receptors) and metabotropic receptors (GABAB receptors)[2].
|
-
- HY-N0304S
-
|
L-DOPA-d6
Levodopa-d6; 3,4-Dihydroxyphenylalanine-d6
|
Dopamine Receptor
Endogenous Metabolite
|
Neurological Disease
|
|
L-DOPA-d6 is the deuterium labeled L-DOPA. L-DOPA (Levodopa) is an orally active metabolic precursor of neurotransmitters dopamine. L-DOPA can cross the blood-brain barrier and is converted into dopamine in the brain. L-DOPA has anti-allodynic effects and the potential for Parkinson's disease[1][2][3].
|
-
- HY-N0067S3
-
|
γ-Aminobutyric acid-13C4
4-Aminobutyric acid-13C4
|
GABA Receptor
Endogenous Metabolite
|
Neurological Disease
|
|
γ-Aminobutyric acid- 13C4 is the 13C-labeled γ-Aminobutyric acid. γ-Aminobutyric acid (4-Aminobutyric acid) is a major inhibitory neurotransmitter in the adult mammalian brain[1][2], binding to the ionotropic GABA receptors (GABAA receptors) and metabotropic receptors (GABAB receptors)[2].
|
-
- HY-P1303A
-
|
CART(62-76)(human,rat) TFA
|
5-HT Receptor
|
Neurological Disease
|
|
CART(62-76)(human,rat) TFA is a neuropeptide (62-76 residues of the CART peptide) with neurotransmitter-like effects. CART(62-76)(human,rat) TFA can modulate the activity of striatal noradrenergic and corticostriatal and hypothalamic serotoninergic (5-HT) system in the rat brain.
|
-
- HY-101175
-
|
3-Bromo-7-nitroindazole
|
NO Synthase
|
Neurological Disease
|
|
3-Bromo-7-nitroindazole is a more potent and selective inhibitor of neuronal nitric oxide synthase (nNOS) than eNOS or inducible nitric oxide synthase (iNOS). 3-Bromo-7-nitroindazole affects the intercellular messenger nitric oxide (NO) synthesis throughout the body and brain.
|
-
- HY-102020
-
-
- HY-119624
-
|
MOMIPP
|
PIKfyve
|
Cancer
|
|
MOMIPP, a macropinocytosis inducer, is a PIKfyve inhibitor. MOMIPP penetrates the blood-brain barrier (BBB).
|
-
- HY-N0667
-
-
- HY-P0212
-
-
- HY-16691
-
-
- HY-113149
-
|
Argininosuccinic acid
|
Endogenous Metabolite
Reactive Oxygen Species
|
Inflammation/Immunology
|
|
Argininosuccinic acid participates in the fourth step of the urea cycle, with being cleaved to arginine and fumaric acid by argininosuccinic acid lyase (ASL). Argininosuccinic acid reduces reduced glutathione (GSH) level, and increases the production of reactive oxygen species in cerebral cortex and striatum. Argininosuccinic acid causes lipid peroxidation and protein oxidation, and induces oxidative stress in the developing rat brain.
|
-
- HY-N10183
-
|
Crocin-4
|
Reactive Oxygen Species
|
Neurological Disease
|
|
Crocin-4, a carotenoid constituent of saffron, is a potent and brain-penetrant antioxidant agent. Crocin-4 can inhibit the aggregation and the concomitant deposition of Aβ fibrils in the brain. Crocin-4 can be used for the research of Alzheimer's Disease. Crocin-4 also exhibits antitumor and anti-inflammatory activities.
|
-
- HY-N0067S2
-
|
γ-Aminobutyric acid-4,4-d2
4-Aminobutyric acid-4,4-d2
|
GABA Receptor
Endogenous Metabolite
|
Neurological Disease
|
|
γ-Aminobutyric acid-4,4-d2 is the deuterium labeled γ-Aminobutyric acid. γ-Aminobutyric acid (4-Aminobutyric acid) is a major inhibitory neurotransmitter in the adult mammalian brain[1][2], binding to the ionotropic GABA receptors (GABAA receptors) and metabotropic receptors (GABAB receptors)[2].
|
-
- HY-15112
-
|
JTP-4819
|
Prolyl Endopeptidase (PREP)
|
|
|
JTP-4819 is a potent and specific inhibitor of prolyl endopeptidase (PREP) with IC50s of 0.83 nM (in rat brain supernatant) and 5.43 nM (in Flavobacterium meningosepticum). JTP-4819 has blood-brain penetration, also improves the retention time of amnesia rats induced by Scopolamine (HY-N2096).
|
-
- HY-N10512
-
|
Gangliotetraose
Gg4
|
Others
|
Neurological Disease
|
|
Gangliotetraose (Gg4) is a tetrasccharide, exhibits major components including GM1 and its sialylated derivatives. GM1 facilitates efflux of nuclear Ca 2+ and reduces the level of nuclear Ca 2+ that characterizes the differentiated neuron. GM1 affects neuronal plasticity and repair mechanisms, as well as neurotrophin release in the brain.
|
-
- HY-15121
-
|
L-Theanine
L-Glutamic Acid γ-ethyl amide; Nγ-Ethyl-L-glutamine
|
Apoptosis
Endogenous Metabolite
Reactive Oxygen Species
|
Cancer
Neurological Disease
|
|
L-Theanine (L-Glutamic Acid γ-ethyl amide) is a non-protein amino acid contained in green tea leaves, which blocks the binding of L-glutamic acid to glutamate receptors in the brain, and with neuroprotective, anticancer and anti-oxidative activities. L-Theanine can pass through the blood–brain barrier and is orally active.
|
-
- HY-P0212A
-
-
- HY-13753
-
-
- HY-15084
-
-
- HY-N0318
-
-
- HY-128351
-
-
- HY-122489
-
-
- HY-125880
-
-
- HY-104028
-
-
- HY-110256
-
-
- HY-131881
-
|
JHU37160
|
mAChR
|
Neurological Disease
|
|
JHU37160 is a potent and brain-penetrant DREADD agonist, with EC50s of 18.5 nM and 0.2 nM for hM3Dq and hM4Di DREADDs in HEK-293 cells, respectively. JHU37160 exhibits selective [ 3H]Clozapine displacement from DREADDs and not from other Clozapine-binding sites in mice brain tissue.
|
-
- HY-P3860
-
-
- HY-E70007
-
|
Catechol O-methyltransferase
COMT
|
Endogenous Metabolite
|
Neurological Disease
|
|
Catechol O-methyltransferase (COMT) the magnesium-dependent transfer of methyl groups from S-adenosyl methionine to a hydroxyl group on dopamine, converting it to 3-methoxytyramine. Catechol O-methyltransferase has two forms in tissues, a soluble form (S-COMT) and a membrane-bound form (MB-COMT). Catechol O-methyltransferase is to regulate epinephrine, norepinephrine, and dopamine levels in the brain.
|
-
- HY-131891
-
|
JHU37152
|
mAChR
|
Neurological Disease
|
|
JHU37152 is a potent and brain-penetrant DREADD agonist, with EC50s of 5 nM and 0.5 nM for hM3Dq and hM4Di DREADDs in HEK-293 cells, respectively. JHU37152 exhibits selective [ 3H]Clozapine displacement from DREADDs and not from other Clozapine-binding sites in mice brain tissue.
|
-
- HY-132246
-
|
WWL123
|
MAGL
|
Neurological Disease
|
|
WWL123 is a potent and selective ABHD6 inhibitor with an IC50 of 430 nM. WWL123 crosses the blood-brain-barrier and inhibits ABHD6 in brain parenchyma. ABHD6 blockade by WWL123 exerts an antiepileptic effect in Pentylenetetrazole (PTZ)-induced epileptiform seizures and spontaneous seizures in R6/2 mice.
|
-
- HY-109566
-
-
- HY-11054
-
|
TH-237A
meso-GS 164
|
Others
|
Neurological Disease
|
|
TH-237A(meso-GS 164) is a novel neuroprotective agent exhibiting favorable permeation across the blood brain barrier.
|
-
- HY-148332
-
-
- HY-19740
-
-
- HY-13510
-
-
- HY-W000133
-
-
- HY-110255
-
-
- HY-110255A
-
-
- HY-108616
-
|
VU 0364739 hydrochloride
|
Phospholipase
|
Cancer
|
|
VU 0364739 hydrochloride is a highly selective phospholipase D2 (PLD2) inhibitor with IC50s of 20 and 1500 nM for PLD2 and PLD1, respectively. VU 0364739 hydrochloride induces apoptosis and it can be used for cancer research.
|
-
- HY-W013075
-
|
Rutin trihydrate
Rutoside trihydrate; Quercetin 3-O-rutinoside trihydrate
|
Apoptosis
Endogenous Metabolite
|
Neurological Disease
Cancer
|
|
Rutin (Rutoside) trihydrate is a multifunctional natural flavonoid glycoside. Rutin trihydrate has been demonstrating excellent antioxidant, anti-inflammatory, anti-diabetic, and anti-carcinogenic properties. Cardioprotective and neuroprotective activities .
|
-
- HY-118152
-
|
Org-12962
|
5-HT Receptor
|
Neurological Disease
|
|
Org-12962 is a potent, selective and orally active 5-HT2C receptor agonist with a pEC50 value of 7.01. Org-12962 also exhibits high effacy for the 5-HT2A and 5-HT2B receptor with pEC50s of 6.38 and 6.28, respectively.Org-12962 displays antiaversive effects in a rat model of panic-like anxiety.
|
-
- HY-P0252B
-
|
α-MSH free acid
α-Melanocyte-Stimulating Hormone free acid
|
Melanocortin Receptor
|
Neurological Disease
|
|
α-MSH free acid (α-Melanocyte-Stimulating Hormone free acid) is an MC3R and MC4R agonist with EC50s of 0.16 nM and 5.6 nM, respectively. α-MSH free acid activates cAMP generation at MC3R and MC4R.
|
-
- HY-21994
-
|
Org-12962 hydrochloride
|
5-HT Receptor
|
Neurological Disease
|
|
Org 12962 hydrochloride is a potent, selective and efficacious 5-HT2C receptor agonist and exhibits pEC50 values of 7.01, 6.38 and 6.28 for 5-HT2C, 5-HT2A and 5-HT2A, respectively. Org 12962 hydrochloride is effective in panic-like anxiety animal model.
|
-
- HY-15079
-
|
Talampanel
GYKI-53773; LY-300164
|
iGluR
Apoptosis
|
Neurological Disease
Cancer
|
|
Talampanel (LY300164) is an orally and selective α-amino-3-hydroxy-5-methyl-4-isoxazolepropionate (AMPA) receptor antagonis with anti-seizure activity. Talampanel (IVAX) has neuroprotective effects in rodent stroke models. Talampanel attenuates caspase-3 dependent apoptosis in mouse brain.
|
-
- HY-A0223
-
-
- HY-13929
-
-
- HY-128569
-
-
- HY-10629
-
-
- HY-114926
-
|
KT185
|
MAGL
|
Neurological Disease
|
|
KT185 is an orally-bioavailable, brain-penetrant and selective ABHD6 inhibitor, with an IC50 0.21 nM in Neuro2A cells.
|
-
- HY-N0229
-
-
- HY-12763
-
|
GNE-317
|
PI3K
mTOR
|
Cancer
|
|
GNE-317 is a PI3K/mTOR inhibitor, is able to cross the blood-brain barrier (BBB).
|
-
- HY-110274
-
-
- HY-B1017
-
-
- HY-133813A
-
-
- HY-17646
-
-
- HY-107663
-
|
MIF-1
Pro-Leu-Gly-NH2; Melanostatin
|
Dopamine Receptor
|
Neurological Disease
|
|
MIF-1 (Melanostatin), an endogenous brain peptide, is a potent dopamine receptor allosteric modulator. MIF-1 inhibits melanin formation. MIF-1 blocks the effects of opioid receptor activation to modulate the analgesic effects of morphine and stress-induced analgesia (SIA). MIF-1 accesses from the blood to the CNS by directly crossing the blood-brain barrier (BBB).
|
-
- HY-13918
-
|
Etimizol
Ethimizole; Ethymisol; Ethymisole
|
Others
|
Neurological Disease
|
|
Etimizol(Ethymisole; Antiffine; Ethylnorantifein) was shown to relieve amnesia effectively in the origin of which there is the hypoxic component (hypobaric hypoxia, actinomycin D, mechanical injury of the brain).
|
-
- HY-100366
-
-
- HY-137441
-
-
- HY-N6685
-
-
- HY-119156
-
-
- HY-100792
-
|
URB602
|
Bacterial
|
Cancer
|
|
URB602 is a selective monoacylglycerol lipase (MGL) inhibitor, which inhibits rat brain MGL with IC50 of 28±4 μM through a noncompetitive mechanism.
|
-
- HY-147519
-
|
ARUK3001185
|
Wnt
|
Cancer
|
|
ARUK3001185 (Compound 8l) is a potent, selective, orally active and brain-penetrant inhibitor of Notum activity with an IC50 of 6.7 nM.
|
-
- HY-B0099
-
-
- HY-131002
-
-
- HY-131031
-
|
KCC-07
|
DNA Alkylator/Crosslinker
|
Cancer
|
|
KCC-07 is a potent, selective and brain-penetrant MBD2 (methyl-CpG-binding domain protein 2) inhibitor. KCC-07 prevents binding of MBD2 to methylated DNA and activates brain specific angiogenesis inhibitor 1 (BAI1) inducing anti-proliferative BAI1/p53/p21 signaling. Anticancer activity.
|
-
- HY-P1318
-
|
Ac-RYYRIK-NH2
|
Opioid Receptor
|
Neurological Disease
|
|
Ac-RYYRIK-NH2 is a potent and partial agonist on ORL1 transfected in CHO cells (Kd=1.5 nM) and behaves as a endogenous ligand of ORL1. Ac-RYYRIK-NH2 is a specific antagonist for the activation of G protein and competitively antagonizes the stimulation of [ 35S]-GTPgS binding to G proteins by nociceptin/orphanin FQ (noc/OFQ) in membranes and sections of rat brain.
|
-
- HY-14174
-
|
MRK-560
|
γ-secretase
|
Cancer
Neurological Disease
|
|
MRK-560 is an orally active, brain barrier-penetrating γ-Secretase inhibitor, can potently reduces Aβ peptide in rat brain and cerebrospinal fluid. MRK-560 also decreases mutant NOTCH1 processing by selectively inhibiting PSEN1. MRK-560 can be used in studies of Alzheimer's disease and T-cell acute lymphoblastic leukaemia (T-ALL).
|
-
- HY-137442
-
|
Inupadenant
EOS-850
|
Adenosine Receptor
|
Cancer
|
|
Inupadenant is an orally active, highly selective A2A receptor antagonist. Inupadenant is not brain-penetrant. Inupadenant has potent anti-tumor activity.
|
-
- HY-19396
-
|
Ingliforib
CP 368296; GPi 296
|
Others
|
Cardiovascular Disease
|
|
Ingliforib (CP 368296) is a glycogen phosphorylase inhibitor, with IC50s of 52, 352 and 150 nM for liver, muscle and brain glycogen phosphorylase, and has cardioprotective activity.
|
-
- HY-B2167
-
-
- HY-W010388AS
-
-
- HY-W015309
-
|
Decanoic acid
Decanoic Acid (C10)
|
iGluR
|
Neurological Disease
|
|
Decanoic acid, a component of medium chain triclycerides, is a brain-penetrant and non-competitive inhibitor of AMPA receptor. Decanoic acid has antiseizure effects.
|
-
- HY-B0315
-
-
- HY-14503
-
|
MDR-1339
DWK-1339
|
Amyloid-β
|
Neurological Disease
|
|
MDR-1339 (DWK-1339) is an orally active and blood-brain-barrier-permeable Aβ-aggregation inhibitor, used in the research of Alzheimer's disease.
|
-
- HY-125039
-
|
N-Acetyl lysyltyrosylcysteine amide
|
Glutathione Peroxidase
|
Neurological Disease
Cardiovascular Disease
|
|
N-Acetyl lysyltyrosylcysteine amide is a potent, reversible, specific, and non-toxic tripeptide inhibitor of myeloperoxidase (MPO). N-Acetyl lysyltyrosylcysteine amide effectively inhibits MPO generation of toxic oxidants in vivo. N-Acetyl lysyltyrosylcysteine amide reduces neuronal damage and preserves brain tissue and neurological function in the stroked brain. N-Acetyl lysyltyrosylcysteine amide inhibits MPO-dependent hypochlorous acid (HOCl) generation, protein nitration, and LDL oxidation.
|
-
- HY-59201A
-
|
A-582941 dihydrochloride
|
nAChR
5-HT Receptor
|
Neurological Disease
|
|
A-582941 dihydrochloride is a potent, selective and brain-penetrant partial agonist of α7 nAChR, with Kis of 10.8 and 16.7 nM in rat brain membranes and human frontal cortex, respectively. A-582941 dihydrochloride also binds to human 5-HT3 receptor with a Ki of 150 nM. A-582941 has the potential for cognitive deficits associated with various neurodegenerative and psychiatric disorders research.
|
-
- HY-P1318A
-
|
Ac-RYYRIK-NH2 TFA
|
Opioid Receptor
|
Neurological Disease
|
|
Ac-RYYRIK-NH2 TFA is a potent and partial agonist on ORL1 transfected in CHO cells (Kd=1.5 nM) and behaves as a endogenous ligand of ORL1. Ac-RYYRIK-NH2 is a specific antagonist for the activation of G protein and competitively antagonizes the stimulation of [ 35S]-GTPgS binding to G proteins by nociceptin/orphanin FQ (noc/OFQ) in membranes and sections of rat brain.
|
-
- HY-124591
-
|
TC-2153
|
5-HT Receptor
Monoamine Oxidase
|
Neurological Disease
|
|
TC-2153 is a selective inhibitor of striatal-enriched protein tyrosine phosphatase (STEP), with psychotropic activity and low acute toxicity. TC-2153 increases the expression of brain-derived neurotropic factor (BDNF) in the brain. And it decreases MAOA and 5-HT1A receptors mRNA level in midbrain. TC-2153 also inhibits 5-HT2A receptor-mediated signaling.
|
-
- HY-146151
-
|
γ-Secretase modulator 12
|
γ-secretase
Amyloid-β
|
Neurological Disease
|
|
γ-Secretase modulator 12 (Compound 1a) is a γ-secretase modulator that can selectively decrease amyloid-β42 (Aβ42) levels (IC50 of 0.39 µM). γ-Secretase modulator 12 can be used for Alzheimer’s disease research. γ-Secretase modulator 12 has a good brain/plasma ratio (Kp, brain = 0.72) in mice.
|
-
- HY-107663A
-
|
MIF-1 TFA
Pro-Leu-Gly-NH2 TFA; Melanostatin TFA
|
Dopamine Receptor
|
Neurological Disease
|
|
MIF-1 TFA (Melanostatin), an endogenous brain peptide, is a potent dopamine receptor allosteric modulator. MIF-1 TFA inhibits melanin formation. MIF-1 TFA blocks the effects of opioid receptor activation to modulate the analgesic effects of morphine and stress-induced analgesia (SIA). MIF-1 TFA accesses from the blood to the CNS by directly crossing the blood-brain barrier (BBB).
|
-
- HY-112305
-
|
AZ32
|
ATM/ATR
|
Cancer
|
|
AZ32 is an orally bioavailable and blood-brain barrier-penetrating ATM inhibitor with an IC50 of <6.2 nM for ATM enzyme, and an IC50 of 0.31 μM for ATM in cell.
|
-
- HY-107617
-
|
PTIQ
|
MMP
|
Neurological Disease
|
|
PTIQ can suppress MMP-3 production, can enter the brain and provide neuroprotection. PTIQ has anti-inflammatory effects on microglial cells.
|
-
- HY-112623
-
-
- HY-W014180
-
-
- HY-P99164
-
-
- HY-P3964
-
-
- HY-128868D
-
|
FITC-Dextran (MW 40000)
|
Fluorescent Dye
|
Others
|
|
FITC-Dextran (MW 40000) is a fluorescent probe for fluorescein isothiocyanate (FITC) dextran (Ex=495 nm; Em=525 nm). FITC-Dextran (MW 40000) can be used as a marker to reveal heat shock-induced cell damage and to study the early and late stages of apoptosis. FITC-Dextran (MW 40000) can also be used for cell permeability studies, such as blood-brain barrier permeability and determination of the extent of blood-brain barrier disruption.
|
-
- HY-128868
-
|
FITC-Dextran (MW 10000)
|
Fluorescent Dye
|
Others
|
|
FITC-Dextran (MW 10000) is a fluorescent probe for fluorescein isothiocyanate (FITC) dextran (Ex=495 nm; Em=525 nm). FITC-Dextran (MW 10000) can be used as a marker to reveal heat shock-induced cell damage and to study the early and late stages of apoptosis. FITC-Dextran (MW 10000) can also be used for cell permeability studies, such as blood-brain barrier permeability and determination of the extent of blood-brain barrier disruption.
|
-
- HY-128868A
-
|
FITC-Dextran (MW 4000)
|
Fluorescent Dye
|
Others
|
|
FITC-Dextran (MW 4000) is a fluorescent probe for fluorescein isothiocyanate (FITC) dextran (Ex=495 nm; Em=525 nm). FITC-Dextran (MW 4000) can be used as a marker to reveal heat shock-induced cell damage and to study the early and late stages of apoptosis. FITC-Dextran (MW 4000) can also be used for cell permeability studies, such as blood-brain barrier permeability and determination of the extent of blood-brain barrier disruption.
|
-
- HY-15978
-
|
P7C3-A20
|
Others
|
Neurological Disease
|
|
P7C3-A20 is a derivative of P7C3 with potent proneurogenic and neuroprotective activity. P7C3-A20 exerts an antidepressant-like effect. P7C3-A20 can cross the blood-brain barrier and therefore has the potential for brain injury treatment.
|
-
- HY-119243
-
-
- HY-130609
-
|
Aβ42-IN-1
|
γ-secretase
|
Neurological Disease
|
|
Aβ42-IN-1, compound 1v, is a novel, potent and orally active γ-secretase modulator (GSM). Aβ42-IN-1 potently reduced Aβ42 levels with an IC50 value of 0.091 µM without CYP3A4 inhibition. Aβ42-IN-1 shows a sustained pharmacokinetic profile.
|
-
- HY-100740
-
|
Lanabecestat
AZD3293; LY3314814
|
Beta-secretase
|
Neurological Disease
|
|
Lanabecestat (AZD3293) is a potent, orally active and blood-brain barrier penetrating BACE1 inhibitor with a Ki of 0.4 nM. Lanabecestat is used for the research of Alzheimer's disease.
|
-
- HY-138639
-
|
PW0787
|
GPR52
|
Neurological Disease
|
|
PW0787 is a potent, selective, orally active, and brain-penetrant GPR52 agonist (EC50=135 nM). PW0787 suppresses psychostimulant behavior.
|
-
- HY-111409
-
-
- HY-N9343
-
-
- HY-113416
-
|
Dehydroepiandrosterone sulfate
DHEA sulfate; Prasterone sulfate
|
Others
|
Neurological Disease
|
|
Dehydroepiandrosterone sulfate, a neuroactive neurosteroid, plays a major role in brain development and aging by influencing the migration of neurons, arborization of dendrites, and formation of new synapses.
|
-
- HY-117501
-
-
- HY-12981
-
-
- HY-B0318
-
-
- HY-N2070
-
-
- HY-14781
-
-
- HY-103240
-
|
Methoxy-X04
|
Amyloid-β
|
Others
|
|
Methoxy-X04 is a fluorescent dye that crosses the blood-brain barrier and selectively binds to beta-pleated sheets found in dense core amyloid Aβ plaques.
|
-
- HY-133555
-
-
- HY-110123
-
-
- HY-100182
-
-
- HY-W278021
-
|
BTA-1
|
Others
|
Others
|
|
BTA-1 is an uncharged derivative of thioflavin-T. BTA-1 has high affinity for Aβ fibrils and shows very good brain entry and clearance.
|
-
- HY-130012
-
-
- HY-112723
-
-
- HY-120332
-
-
- HY-Y1787
-
|
Dimethyl malonate
|
Apoptosis
|
Neurological Disease
|
|
Dimethyl malonate is a competitive inhibitor of succinate dehydrogenase (SDH). Dimethyl malonate is able to cross the blood-brain barrier and hydrolyse to malonate. Dimethyl malonate reduces neuronal apoptosis.
|
-
- HY-15796
-
|
GNE0877
|
LRRK2
|
Neurological Disease
|
|
GNE0877 is a highly selective, orally active and brain-penetrant LRRK2 inhibitor with an IC50 of 3 nM and a Ki of 0.7 nM. GNE0877 can be used for the research of neuroscience.
|
-
- HY-139624
-
|
JNK3 inhibitor-1
|
JNK
|
Others
|
|
JNK3 inhibitor-1 is a potent and selective JNK3 inhibitor (IC50 = 0.005 μM). JNK3 inhibitor-1 is orally bioavailable and brain penetrant.
|
-
- HY-12332
-
|
JW 642
|
MAGL
|
Neurological Disease
|
|
JW 642 is a potent inhibitor of monoacylglycerol lipase (MAGL) that displays IC50 values of 7.6, 14, and 3.7 nM for inhibition of MAGL in mouse, rat, and human brain membranes, respectively.
|
-
- HY-N0667S5
-
-
- HY-W011522
-
|
Taurolidine
|
Bacterial
Apoptosis
Antibiotic
|
Cancer
Infection
|
|
Taurolidine is a broad-spectrum antimicrobial for the prevention of central venous catheter-related infections. Taurolidine has a direct and selective antineoplastic effect on brain tumor cells by the induction of apoptosis.
|
-
- HY-128868G
-
|
FITC-Dextran (MW 150000)
|
Fluorescent Dye
|
Cancer
Neurological Disease
|
|
FITC-Dextran (MW 150000) is a fluorescent probe for fluorescein isothiocyanate (FITC) dextran (Ex=495 nm; Em=525 nm). FITC-Dextran (MW 150000) can be used as a marker to reveal heat shock-induced cell damage and to study the early and late stages of apoptosis. FITC-Dextran FITC-Dextran (MW 150000) can also be used for cell permeability studies, such as blood-brain barrier permeability and determination of the extent of blood-brain barrier disruption.
|
-
- HY-124475
-
|
Antalarmin
|
CRFR
|
Neurological Disease
|
|
Antalarmin is a selective nonpeptide corticotropin-releasing factor receptor 1 (CRHR1) antagonist with a Ki of 2.7 nM. Antalarmin can pass through the blood–brain barrier.
|
-
- HY-W017540
-
|
Cyclocreatine
|
Others
|
Cardiovascular Disease
|
|
Cyclocreatine is a Creatine analogue and acts as a potent bioenergetic protective agent by providing high levels of ATP. Cyclocreatine crosses membranes, enters the brain, and can be phosphorylated and dephosphorylated by creatine kinases.
|
-
- HY-114396
-
|
BR351
|
MMP
|
Cancer
|
|
BR351 is a brain penetrant MMP inhibitor with IC50s of 4, 2, 11, 50 nM for MMP2, MMP8, MMP9 and MMP13, respectively.
|
-
- HY-12599
-
-
- HY-121599
-
|
CGP 36742
SGS-742
|
GABA Receptor
|
Neurological Disease
|
|
CGP 36742 is a selective GABAB receptor antagonist that can penetrate the blood–brain barrier after peripheral administration, with an IC50 of 32 μM. CGP 36742 is useful in treatment of depression.
|
-
- HY-B1726
-
|
Phenacaine
Holocaine
|
Phosphodiesterase (PDE)
|
Metabolic Disease
|
|
Phenacaine (Holocaine) is a local anesthetic. Phenacaine inhibits the specific calmodulin-dependent stimulation of erythrocyte Ca 2+-ATPase and cyclic nucleotide phosphodiesterases from brain and heart.
|
-
- HY-B0303A
-
-
- HY-107409
-
|
GNE 5729
|
iGluR
|
Neurological Disease
|
|
GNE 5729 is a brain permeable positive allosteric modulator of NMDAR, with an EC50 of 37 nM for GluN2A, 4.7 and 9.5 μM for GluN2C and GluN2D, respectively.
|
-
- HY-106147
-
|
Frakefamide
|
Opioid Receptor
|
Neurological Disease
|
|
Frakefamide is a potent analgesic that acts as a peripheral active μ-selective receptor agonist. Frakefamide is unable to penetrate the blood-brain-barrier and enter the central nervous system.
|
-
- HY-113643
-
-
- HY-B0303
-
-
- HY-114384B
-
|
NV-5138 hydrochloride
|
mTOR
|
Neurological Disease
|
|
NV-5138 hydrochloride, a leucine analog, is the first selective and orally active brain mTORC1 activator, binding to Sestrin2. NV-5138 hydrochloride is used for antidepressant studies.
|
-
- HY-13909
-
|
RGFP966
|
HDAC
|
Cancer
|
|
RGFP966 is a highly selective HDAC3 inhibitor with an IC50 of 80 nM and shows no inhibition to other HDACs at concentrations up to 15 μM. RGFP966 can penetrate the blood brain barrier (BBB).
|
-
- HY-114384
-
|
NV-5138
|
mTOR
|
Neurological Disease
|
|
NV-5138, a leucine analog, is the first selective and orally active brain mTORC1 activator, binding to Sestrin2. NV-5138 is used for antidepressant studies.
|
-
- HY-112157
-
-
- HY-66010A
-
|
Cinepazide
|
Calcium Channel
|
Cardiovascular Disease
|
|
Cinepazide is a piperazine derivative and acts as a weak calcium channel blocker. Cinepazide is a potent vasodilator and can be used for the research of cerebrovascular diseases, including ischemic stroke, brain infarct et. al.
|
-
- HY-N5057
-
|
Przewalskinic acid A
|
Others
|
Cardiovascular Disease
|
|
Przewalskinic acid A is a phenolic acid found in the Salvia przewalskii Maxim herb. Phenolic acids show potent antioxidant activities and potential effects in protecting against brain and heart damage caused by ischemia reperfusion.
|
-
- HY-10231
-
-
- HY-N0667S2
-
|
L-Asparagine-15N2 monohydrate
(-)-Asparagine-15N2 (monohydrate); Asn-15N2 (monohydrate); Asparamide-15N2 (monohydrate)
|
Endogenous Metabolite
|
Neurological Disease
|
|
L-Asparagine- 15N2 (monohydrate) is the 15N-labeled L-Asparagine. L-Asparagine ((-)-Asparagine) is a non-essential amino acid that is involved in the metabolic control of cell functions in nerve and brain tissue.
|
-
- HY-104003
-
-
- HY-106147B
-
|
Frakefamide TFA
|
Opioid Receptor
|
Neurological Disease
|
|
Frakefamide TFA is a potent analgesic that acts as a peripheral active μ-selective receptor agonist. Frakefamide is unable to penetrate the blood-brain-barrier and enter the central nervous system.
|
-
- HY-W017443S1
-
-
- HY-116916
-
|
Acetophenazine
|
Dopamine Receptor
|
Neurological Disease
|
|
Acetophenazine, a phenothiazine derivative, is an antipsychotic agent. Acetophenazine primarily blocks dopamine D2 receptors in the brain. Acetophenazine can be used for researching psychotic disorders such as schizophrenia and anxious depression.
|
-
- HY-W013372
-
-
- HY-N0667S3
-
|
L-Asparagine-13C4 monohydrate
(-)-Asparagine-13C4 (monohydrate); Asn-13C4 (monohydrate); Asparamide-13C4 (monohydrate)
|
Endogenous Metabolite
|
Neurological Disease
|
|
L-Asparagine- 13C4 (monohydrate) is the 13C-labeled L-Asparagine. L-Asparagine ((-)-Asparagine) is a non-essential amino acid that is involved in the metabolic control of cell functions in nerve and brain tissue.
|
-
- HY-112636
-
|
Astrophloxine
|
Amyloid-β
Others
|
Others
|
|
Astrophloxine is a fluorescent imaging probe capable of targeting antiparallel dimers. Astrophloxine can be used to detect aggregated Aβ in brain tissue and cerebrospinal fluid samples of Alzheimer's disease (AD) mice.
|
-
- HY-147720
-
|
γ-Secretase modulator 11
|
γ-secretase
|
Neurological Disease
|
|
5-{8-[(3,4'- difluoro [1,1'- biphenyl]-4-yl) methoxy] - 2-methylimidazo [1,2-a] pyridin-3-yl}-n-methylpyridin-2-formamide (1o) showed high potency in vitro and brain exposure, inducing brain a β 42 levels were significantly reduced and showed undetectable inhibition of cytochrome P450 enzymes. In addition, compound 1o showed excellent anti cognitive deficit effect in AD model mice.
|
-
- HY-16936
-
|
JH-II-127
|
LRRK2
|
Neurological Disease
|
|
JH-II-127 is an orally active, highly potent, selective and brain-permeable LRRK2 inhibitor, with IC50s of 6, 2 and 48 nM for wild-type LRRK2 and LRRK2-G2019S and mutant LRRK2-A2016T. JH-II-127 inhibits Ser935 phosphorylation in all tissues of mice, including the brain. JH-II-127 can be used in the study of parkinson's syndrome.
|
-
- HY-13438
-
|
AZD3839 free base
|
Beta-secretase
|
Cancer
|
|
AZD3839 free base is a potent and selective orally active, brain-permeable BACE1 inhibitor (Ki=26 nM). AZD3839 free base shows 14 and >1000-fold selectivity against BACE2 and cathepsin D, respectively. AZD3839 free base exhibits dose- and time-dependent lowering of plasma, brain, and cerebrospinal fluid Aβ levels in mouse, guinea pig, and non-human primate. AZD3839 free base can be used for the research of Alzheimer's disease.
|
-
- HY-131688
-
|
2-Chlorohexadecanoic acid
|
Others
|
Inflammation/Immunology
|
|
2-Chlorohexadecanoic acid, an inflammatory lipid mediator, interferes with protein palmitoylation,induces ER-stress markers, reduced the ER ATP content, and activates transcription and secretion of IL-6 as well as IL-8.2-Chlorohexadecanoic acid disrupts the mitochondrial membrane potential and induces procaspase-3 and PARP cleavage.2-Chlorohexadecanoic acid can across blood-brain barrier (BBB) and compromises ER- and mitochondrial functions in the human brain endothelial cell line hCMEC/D3.
|
-
- HY-16636
-
|
ML337
|
mGluR
|
Neurological Disease
|
|
ML337 is a selective and brain-penetrant negative allosteric modulator of mGlu3, with an IC50 of 593 nM. ML337 possesses a favorable dystrophia myotonica protein kinase (DMPK) and ancillary pharmacology profile.
|
-
- HY-146334
-
|
DFBTA
|
Chloride Channel
|
Inflammation/Immunology
|
|
DFBTA is an orally active, potent and little brain penetrated ANO1 (Calcium-activated chloride channel anoctamin-1) inhibitor, with an IC50 of 24 nM. DFBTA shows analgesic efficacy for inflammatory pain.
|
-
- HY-18610
-
|
Diclofensine hydrochloride
Ro 8-4650 hydrochloride
|
Dopamine Transporter
|
Neurological Disease
|
|
Diclofensine hydrochloride (Ro-8-4650 hydrochloride) is a potent inhibitor of monoamine reuptake, blocking the uptake of dopamine, noradrenaline, and serotonin by rat brain synaptosomes with IC50 values of 0.74, 2.3, and 3.7 nM, respectively.
|
-
- HY-N0667S4
-
|
L-Asparagine-4-13C monohydrate
(-)-Asparagine-4-13C (monohydrate); Asn-4-13C (monohydrate); Asparamide-4-13C (monohydrate)
|
Endogenous Metabolite
|
Neurological Disease
|
|
L-Asparagine-4- 13C (monohydrate) is the 13C-labeled L-Asparagine. L-Asparagine ((-)-Asparagine) is a non-essential amino acid that is involved in the metabolic control of cell functions in nerve and brain tissue.
|
-
- HY-145339
-
-
- HY-110278
-
|
ADX71743
|
mGluR
|
Neurological Disease
|
|
ADX71743 is a highly selective, noncompetitive and brain-penetrant metabotropic glutamate receptor 7 negative allosteric modulator (mGlu7 NAM). ADX71743 has anxiolytic-like activity.
|
-
- HY-111351
-
-
- HY-105860
-
|
Selurampanel
BGG 492
|
iGluR
|
Neurological Disease
|
|
Selurampanel (BGG 492) is an orally active and competitive AMPA receptor antagonist with an IC50 of 190 nM. Selurampanel has reasonable blood-brain barrier penetration. Selurampanel can be used for epilepsy research.
|
-
- HY-10622
-
-
- HY-112217A
-
|
PSEM 89S TFA
|
nAChR
|
Neurological Disease
|
|
PSEM 89S TFA is a selective and brain penetrant agonists for the resulting ion channels. PSEM 89S TFA is orthogonally selective for Q79G and L141F, respectively.
|
-
- HY-146101
-
-
- HY-15649
-
|
UNC1215
|
Histone Methyltransferase
Apoptosis
|
Cancer
|
|
UNC1215 is a potent and selective inhibitor for the methyllysine (Kme) reading domain function of L3MBTL3 with a Kd value of 120 nM and an IC50 of 40 nM. UNC1215 has the potential to treat malignant brain tumor.
|
-
- HY-16425
-
|
RG2833
RGFP109
|
HDAC
|
Cancer
|
|
RG2833 is a brain-penetrant HDAC inhibitor with IC50s of 60 nM and 50 nM for HDAC1 and HDAC3, respectively. The Ki values for HDAC1 and HDAC3 are 32 and 5 nM, respectively.
|
-
- HY-113303
-
-
- HY-18610A
-
|
Diclofensine
Ro 8-4650
|
Dopamine Transporter
|
Neurological Disease
|
|
Diclofensine(Ro-8-4650) is a potent inhibitor of monoamine reuptake, blocking the uptake of dopamine, noradrenaline, and serotonin by rat brain synaptosomes with IC50 values of 0.74, 2.3, and 3.7 nM, respectively.
|
-
- HY-145706
-
-
- HY-114452
-
|
LY2940094
BTRX-246040
|
Opioid Receptor
|
Neurological Disease
|
|
LY2940094 (BTRX-246040) is a potent, selective and orally available nociceptin receptor (NOP receptor) antagonist with high affinity (Ki=0.105 nM) and antagonist potency (Kb=0.166 nM). LY2940094 reduces ethanol self-administration in animal models.
|
-
- HY-121268
-
-
- HY-126129
-
|
Desacetylcefotaxime
|
Bacterial
|
Infection
|
|
Desacetylcefotaxime, the in vivo metabolite of Cefotaxime (CTX), possesses significant in vitro antimicrobial activity similar to the parent compound against a variety of aerobic and anaerobic bacteria.
|
-
- HY-118301
-
|
ADX71441
|
GABA Receptor
|
Neurological Disease
|
|
ADX71441 is a potent and selective positive allosteric modulator of the GABAB receptor. ADX71441 is bioavailable after oral administration and is brain penetrant. ADX71441 has the potential for research of anxiety, pain and spasticity.
|
-
- HY-N0229S13
-
-
- HY-108337
-
|
GNE-0723
|
iGluR
|
Neurological Disease
|
|
GNE-0723 is a brain permeable positive allosteric modulator of NMDAR, with an EC50 of 21 nM for GluN2A, 7.4 and 6.2 μM for GluN2C and GluN2D, respectively.
|
-
- HY-N0229S3
-
-
- HY-N0229S12
-
-
- HY-125740
-
|
Malvidin-3-glucoside chloride
Malvidin-3-O-glucoside chloride; Oenin chloride
|
Others
|
Inflammation/Immunology
|
|
Malvidin-3-glucoside chloride (Malvidin-3-O-glucoside chloride), a major wine anthocyanin, is effective in promoting resilience against stress by modulating brain synaptic plasticity and peripheral inflammation.
|
-
- HY-108703
-
|
Foliglurax
PXT002331
|
mGluR
|
Neurological Disease
|
|
Foliglurax (PXT002331) is a highly selective and potent, brain-penetrant metabotropic glutamate receptor 4 positive allosteric modulator (mGluR4 PAM) with an EC50 of 79 nM. Antiparkinsonian effect.
|
-
- HY-17399
-
|
Racecadotril
Acetorphan
|
Neprilysin
|
Metabolic Disease
|
|
Racecadotril (Acetorphan) is a neutral endopeptidase (NEP) inhibitor. Racecadotril and its active metabolite Thiorphan inhibits purified NEP activity from mouse brain with Kis of 4500 and 6.1 nM, , respectively. Antidiarrheal agent.
|
-
- HY-101485
-
|
AUTEN-99 hydrobromide
Autophagy enhancer-99 hydrobromide
|
Others
|
Neurological Disease
|
|
AUTEN-99 (hydrobromide) is a novel inhibitor of the myotubularin phosphatase Jumpy (also called MTMR14). AUTEN-99 (hydrobromide) crosses the blood-brain barrier and exerts potent neuroprotective effects.
|
-
- HY-103242
-
|
CRANAD-2
|
Amyloid-β
|
Neurological Disease
|
|
CRANAD-2 is a near-infrared (NIR) Aβ plaque-specific fluorescent probe. CRANAD 2 penetrates the blood brain barrier and has a high affinity for Aβ aggregates with a Kd of 38 nM.
|
-
- HY-B1730
-
|
Phensuximide
|
Others
|
Metabolic Disease
Neurological Disease
|
|
Phensuximide is an orally active succinimide antiepileptic and anticonvulsant agent. Phensuximide inhibits cyclic AMP and cyclic GMP accumulation in depolarized brain tissue. Phensuximide can be used for the study of seizure and petit mal.
|
-
- HY-109024
-
-
- HY-50879
-
|
Elacridar
GF120918; GW0918; GG918; GW120918
|
P-glycoprotein
BCRP
|
Cancer
|
|
Elacridar is an orally active P-glycoprotein (Pgp) and breast cancer resistance protein (BCRP) inhibitor. Elacridar can be used to examine the influence of efflux transporters on drug distribution to brain and the research of cancer.
|
-
- HY-100732
-
|
Cambinol
|
Sirtuin
Apoptosis
Phospholipase
|
Cancer
|
|
Cambinol is a SIRT1 and SIRT2 inhibitor with IC50 values of 56 μM and 59 μM, respectively. Cambinol is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor).
|
-
- HY-13637B
-
|
Ganciclovir hydrate
BW-759 hydrate; 2'-Nor-2'-deoxyguanosine hydrate
|
CMV
HSV
Antibiotic
Nucleoside Antimetabolite/Analog
|
Cancer
Infection
|
|
Ganciclovir (BW 759) hydrate, a nucleoside analogue, is an orally active antiviral agent with activity against CMV. Ganciclovir hydrate also has activity in vitro against members of the herpes group and some other DNA viruses. Ganciclovir hydrate inhibits the in vitro replication of human herpes viruses (HSV 1 and 2, CMV) and adenovirus serotypes 1, 2, 4, 6, 8, 10, 19, 22 and 28. Ganciclovir hydrate has an IC50 of 5.2 μM for feline herpesvirus type-1 (FHV-1) and can diffuse into the brain.
|
-
- HY-13637
-
|
Ganciclovir
BW 759; 2'-Nor-2'-deoxyguanosine
|
CMV
HSV
Antibiotic
Nucleoside Antimetabolite/Analog
|
Infection
Cancer
|
|
Ganciclovir (BW 759), a nucleoside analogue, is an orally active antiviral agent with activity against CMV. Ganciclovir also has activity in vitro against members of the herpes group and some other DNA viruses. Ganciclovir inhibits the in vitro replication of human herpes viruses (HSV 1 and 2, CMV) and adenovirus serotypes 1, 2, 4, 6, 8, 10, 19, 22 and 28. Ganciclovir has an IC50 of 5.2 μM for feline herpesvirus type-1 (FHV-1) and can diffuse into the brain.
|
-
- HY-13637A
-
|
Ganciclovir sodium
BW 759 sodium; 2'-Nor-2'-deoxyguanosine sodium
|
CMV
HSV
Antibiotic
Nucleoside Antimetabolite/Analog
|
Infection
Cancer
|
|
Ganciclovir (BW 759) sodium, a nucleoside analogue, is an orally active antiviral agent with activity against CMV. Ganciclovir sodium also has activity in vitro against members of the herpes group and some other DNA viruses. Ganciclovir sodium inhibits the in vitro replication of human herpes viruses (HSV 1 and 2, CMV) and adenovirus serotypes 1, 2, 4, 6, 8, 10, 19, 22 and 28. Ganciclovir sodium has an IC50 of 5.2 μM for feline herpesvirus type-1 (FHV-1) and can diffuse into the brain.
|
-
- HY-W015309S1
-
|
Decanoic acid-d19
|
iGluR
|
Neurological Disease
|
|
Decanoic acid-d199 is the deuterium labeled Decanoic acid. Decanoic acid, a component of medium chain triclycerides, is a brain-penetrant and non-competitive inhibitor of AMPA receptor. Decanoic acid has antiseizure effects[1][2][3].
|
-
- HY-107434S
-
|
Molindone-d8
(±)-Molindone-d8; SPN-810M-d8
|
Dopamine Receptor
|
Neurological Disease
|
|
Molindone-d8 is the deuterium labeled Molindone. Molindone hydrochloride (EN-1733A) is a therapeutic antipsychotic, used in the treatment of schizophrenia, works by blocking the effects of dopamine in the brain, leading to diminished psychoses[1][2].
|
-
- HY-131703
-
|
UGT8-IN-1
|
Others
|
Metabolic Disease
|
|
UGT8-IN-1 is a brain penetrable and orally active inhibitor of ceramide galactosyltransferase enzyme (UGT8). UGT8-IN-1 can be used in the study for lysosomal storage disorders.
|
-
- HY-14859
-
|
Dipraglurant
ADX48621
|
mGluR
|
Neurological Disease
|
|
Dipraglurant (ADX48621) is a potent, selective, orally active and brain penetrant mGluR5 negative allosteric modulator (NAM), with an IC50 of 21 nM. Dipraglurant can reduce Levodopa-induced dyskinesia (LID) in vivo.
|
-
- HY-B2167S
-
-
- HY-W015309S3
-
|
Decanoic acid-d5
|
iGluR
|
|
|
Decanoic acid-d5 is the deuterium labeled Decanoic acid. Decanoic acid, a component of medium chain triclycerides, is a brain-penetrant and non-competitive inhibitor of AMPA receptor. Decanoic acid has antiseizure effects[1][2][3].
|
-
- HY-14136
-
-
- HY-131006
-
|
FFN200 dihydrochloride
|
Monoamine Transporter
|
Neurological Disease
|
|
FFN200 dihydrochloride, a fluorescent substrate of VMAT2, selectively trace monoamine exocytosis in both neuronal cell culture and brain tissue. The fluorescence excitation and emission maxima of FFN200 are determined to be 352 and 451 nm, respectively.
|
-
- HY-127086
-
|
Dicarbine
|
Dopamine Receptor
|
Neurological Disease
|
|
Dicarbine blocks dopamine receptors in various brain parts and prevents the depression of the conditioned defence reflexes caused by stimulation of the mesencephalic portion of the reticular formation. Dicarbine could be used in the schizophrenia and alcoholic psychosis studies.
|
-
- HY-14605
-
-
- HY-10900
-
-
- HY-W015309S
-
|
Decanoic acid-d3
|
iGluR
|
Neurological Disease
|
|
Decanoic acid-d3 is the deuterium labeled Decanoic acid. Decanoic acid, a component of medium chain triclycerides, is a brain-penetrant and non-competitive inhibitor of AMPA receptor. Decanoic acid has antiseizure effects[1][2][3].
|
-
- HY-14605A
-
|
Rasagiline
(R)-AGN1135; TVP1012
|
Monoamine Oxidase
|
Neurological Disease
|
|
Rasagiline (R-AGN1135) is a highly potent selective irreversible mitochondrial monoamine oxidase (MAO) inhibitor with IC50s of 4.43 nM and 412 nM for rat brain MAO B and A activity, respectively.
|
-
- HY-136660
-
|
PQR626
|
mTOR
|
Neurological Disease
|
|
PQR626, a rapamycin derivative, is a potent, selective, orally active, and brain-penetrant mTOR inhibitor, with an IC50 and Ki of 5 nM and 3.6 nM, respectively. PQR626 can be can be used for the research of neurological disorders.
|
-
- HY-66010
-
|
Cinepazide Maleate
MD-67350
|
Calcium Channel
|
Cardiovascular Disease
|
|
Cinepazide Maleate (MD-67350) is a piperazine derivative and acts as a weak calcium channel blocker. Cinepazide Maleate is a potent vasodilator and can be used for the research of cerebrovascular diseases, including ischemic stroke, brain infarct et. al.
|
-
- HY-B1262
-
|
Acetophenazine dimaleate
|
Dopamine Receptor
|
Neurological Disease
|
|
Acetophenazine dimaleate, a phenothiazine derivative, is an antipsychotic agent. Acetophenazine dimaleate primarily blocks dopamine D2 receptors in the brain. Acetophenazine dimaleate can be used for researching psychotic disorders such as schizophrenia and anxious depression.
|
-
- HY-120085
-
|
PFE-360
PF-06685360
|
LRRK2
|
Neurological Disease
|
|
PFE-360 (PF-06685360) is a potent, selective, brain penetrated and orally active leucine-rich repeat kinase 2 (LRRK2) inhibitor with a mean IC50 of 2.3 nM in vivo.
|
-
- HY-W015309S2
-
|
Decanoic acid-d2
|
iGluR
|
Neurological Disease
|
|
Decanoic acid-d2 is the deuterium labeled Decanoic acid. Decanoic acid, a component of medium chain triclycerides, is a brain-penetrant and non-competitive inhibitor of AMPA receptor. Decanoic acid has antiseizure effects[1][2][3].
|
-
- HY-U00046
-
|
Apyramide
|
COX
|
Inflammation/Immunology
|
|
Apyramide is an anti-inflammatory agent (NSAID) and behaves as a prodrug of indomethacin (HY-14397). Indomethacin is a potent, blood-brain permeable and nonselective inhibitor of COX1 and COX2.
|
-
- HY-151797
-
|
Ph-HTBA
|
CaMK
|
Neurological Disease
|
|
Ph-HTBA is a high-affinity, brain-penetrating modulator for CaMKIIα. Ph-HTBA has binding affinity for CaMKIIα with a Kd value of 757 nM. Ph-HTBA can be used for the research of ischemia and neurodegenerative disorders.
|
-
- HY-B0534
-
|
Moclobemide
Ro111163
|
Monoamine Oxidase
|
Neurological Disease
|
|
Moclobemide (Ro111163) is a brain-penetrant and reversible monoamine oxidase (MAO-A) inhibitor with an IC50 of 6.061 μM for hMAO-A.Moclobemide up-regulates proliferation of hippocampal progenitor cells in chronically stressed mice.
|
-
- HY-15722
-
-
- HY-B0762
-
|
Acetyl-L-carnitine hydrochloride
O-Acetyl-L-carnitine hydrochloride; ALCAR hydrochloride
|
Endogenous Metabolite
|
Neurological Disease
|
|
Acetyl-L-carnitine (O-Acetyl-L-carnitine) hydrochloride is a blood-brain permeable acetyl ester of the amino acid L-carnitine found in the body. Acetyl-L-carnitine hydrochloride is often used as a dietary supplement, and exibits anti-stress-related psychiatric disorders.
|
-
- HY-10959
-
|
RG7112
RO5045337
|
MDM-2/p53
E1/E2/E3 Enzyme
|
Cancer
|
|
RG7112 is a potent, selective, first clinical, orally active and blood-brain barrier crossed MDM2-p53 inhibitor, with an IC50 of 18 nM and a KD of 11 nM for binding to MDM2.
|
-
- HY-13662
-
-
- HY-14880A
-
-
- HY-136146
-
|
SUVN-911
|
nAChR
|
Neurological Disease
|
|
SUVN-911 is a potent, selective, brain penetrated and orally bioavailable neuronal nicotinic acetylcholine α4β2 receptor antagonist, with a Ki of 1.5 nM. SUVN-911 has antidepressant activity.
|
-
- HY-108703A
-
|
Foliglurax monohydrochloride
PXT002331 (monohydrochloride)
|
mGluR
|
Neurological Disease
|
|
Foliglurax monohydrochloride (PXT002331 monohydrochloride) is a highly selective and potent, brain-penetrant metabotropic glutamate receptor 4 positive allosteric modulator (mGluR4 PAM) , with an EC50 of 79 nM. Antiparkinsonian effect.
|
-
- HY-147982
-
|
GABA-AT-IN-1
|
GABA Receptor
|
Neurological Disease
|
|
GABA-AT-IN-1 (Compound 6) is a γ-aminobutyric acid aminotransferase (GABA-AT) inhibitor and significantly elevates the mouse brain GABA level. GABA-AT-IN-1 has the ability to cross the BBB and can be used as an anticonvulsant.
|
-
- HY-N0229S8
-
-
- HY-14880B
-
-
- HY-141866
-
-
- HY-N0229S9
-
-
- HY-14880
-
-
- HY-128349
-
-
- HY-111540
-
-
- HY-107664A
-
|
SR 142948 dihydrochloride
|
Neurotensin Receptor
|
Neurological Disease
|
|
SR 142948 dihydrochloride is an orally active and selective non-peptide neurotensin receptor (NT) antagonist with IC50s of 1.19 nM, 0.32 nM, 3.96 nM in h-NTR1-CHO cells, HT-29 cells, and adult rat brain, respectively. SR 142948 dihydrochloride antagonizes NT-induced inositol monophosphate formation in HT-29 cells with an IC50 of 3.9 nM. SR 142948 dihydrochloride blocks hypothermia, analgesia and steering behavior induced by NT in vivo. SR 142948 dihydrochloride shows blood-brain permeability and can be used in study of psychiatric disorders.
|
-
- HY-107664
-
|
SR 142948
|
Neurotensin Receptor
|
Neurological Disease
|
|
SR 142948 is an orally active and selective non-peptide neurotensin receptor (NT) antagonist with IC50s of 1.19 nM, 0.32 nM, 3.96 nM in h-NTR1-CHO cells, HT-29 cells, and adult rat brain, respectively. SR 142948 antagonizes NT-induced inositol monophosphate formation in HT-29 cells with an IC50 of 3.9 nM. SR 142948 blocks hypothermia, analgesia and steering behavior induced by NT in vivo. SR 142948 shows blood-brain permeability and can be used in study of psychiatric disorders.
|
-
- HY-W016586
-
|
Acivicin
AT-125; U-42126
|
Parasite
|
Cancer
Infection
|
|
Acivicin (AT-125), a natural product produced by Streptomyces sviceus is a γ-glutamyl transpeptidase (GGT) inhibitor. Acivicin can across the blood-brain barrier and has anti-cancer, anti-parasitic properties.
|
-
- HY-N0229S7
-
-
- HY-B1410
-
|
Ioversol
MP-328
|
Others
|
Others
|
|
Ioversol (MP-328) is a nonionic iodinated contrast medium (CM) that is used during a CT scan or x-ray in animal experiment. Ioversol does not damage the blood-brain barrier (BBB) in animal.
|
-
- HY-134829
-
|
BMS-986176
LX-9211; AAK1-IN-1
|
AAK1
|
Neurological Disease
|
|
BMS-986176 (LX-9211) is a highly selective, brain-penetrant, potent AAK1 (adaptor associated kinase 1) inhibitor with an IC50 of 2 nM. BMS-986176 can be used for neurodegenerative diseases research.
|
-
- HY-B0186A
-
|
Cefoselis hydrochloride
|
Bacterial
Antibiotic
|
Infection
|
|
Cefoselis hydrochloride, the fourth gen-eration of cephalosporin, is a β-lactam antibiotic. Cefoselis hydrochloride exhibits good activity against a wide range of Gram-positive and Gram-negative organisms. Cefoselis hydrochloride penetrates the blood-brain barrier.
|
-
- HY-N1501
-
|
Beta-asarone
|
Others
|
Inflammation/Immunology
Neurological Disease
|
|
Beta-asarone is a major ingredient of Acorus tatarinowii Schott, penetrates blood brain barrier, with the properties of
immunosuppression, central nervous system inhibition, sedation, and hypothermy. Beta-asarone protects against Parkinson’s disease.
|
-
- HY-B0627
-
-
- HY-112612A
-
|
RTI-13951-33 hydrochloride
|
GPR88
|
Neurological Disease
|
|
RTI-13951-33 hydrochloride is a potent, selective, and brain-penetrant GPR88 agonist, with an EC50 of 25 nM in GPR88 cAMP functional assay. RTI-13951-33 hydrochloride reduces alcohol reinforcement and intake behaviors in rats.
|
-
- HY-B1395A
-
-
- HY-N0229S6
-
-
- HY-132845
-
|
Utreloxastat
|
α-synuclein
|
Neurological Disease
|
|
Utreloxastat is a compound used for the research of the disorders including α-synucleinopathies, tauopathies, Amyotrophic lateral sclerosis (ALS), traumatic brain injury, and ischemic-reperfusion related injuries (patent WO2020081879A2, example A1).
|
-
- HY-120576
-
|
ML169
VU0405652
|
mAChR
|
Neurological Disease
|
|
ML169 (VU0405652) is a potent, selective and brain penetrant positive allosteric modulator (PAM) of M1 mAChR, with an EC50 of 1.38 µM. ML169 is a MLPCN probe and can be used for Alzheimer’s disease.
|
-
- HY-N2080
-
|
Songorine
|
GABA Receptor
|
Cancer
|
|
Songorine is a diterpenoid alkaloid isolated from the genus Aconitum. Songorine is a GABAA receptor antagonist in rat brain and has anti cancer, antiarrhythmic and anti-inflammatory activities. Songorine has the potential for the treatment of Epithelial ovarian cancer (EOC).
|
-
- HY-100642
-
|
3-O-Methyltolcapone
Ro 40-7591
|
COMT
|
Neurological Disease
|
|
3-O-Methyltolcapone (Ro 40-7591) is a metabolite of Tolcapone. Tolcapone is an orally active, reversible, selective and potent COMT inhibitor. Tolcapone crosses the blood-brain barrier, and can be used for treatment of Parkinson's disease.
|
-
- HY-110176
-
|
ASP2535
|
GlyT
|
Neurological Disease
|
|
ASP2535 is a potent, orally bioavailable, selective, brain permeable and centrally-active glycine transporter-1 (GlyT1) inhibitor. ASP2535 can improve cognitive impairment in animal models of schizophrenia and Alzheimer's disease.
|
-
- HY-N0229S4
-
-
- HY-N0229S1
-
-
- HY-14200
-
|
(S)-Rasagiline
TVP1022; S-PAI
|
Monoamine Oxidase
|
Neurological Disease
|
|
(S)-Rasagiline (TVP1022) is the relatively inactive S-enantiomer form of Rasagiline. Rasagiline is a highly potent selective irreversible MAO inhibitor with IC50s of 4.43 nM and 412 nM for rat brain MAO B and A activity, respectively.
|
-
- HY-112612
-
|
RTI-13951-33
|
GPR88
|
Neurological Disease
|
|
RTI-13951-33 is a potent, selective, and brain-penetrant GPR88 agonist, with an EC50 of 25 nM in GPR88 cAMP functional assay. RTI-13951-33 reduces alcohol reinforcement and intake behaviors in rats.
|
-
- HY-50098
-
-
- HY-133016A
-
|
(R)-M8891
|
Others
|
Others
|
|
(R)-M8891 (compound R-9) is a less active isomer of M8891. M8891 is an orally active, reversible and brain penetrant Methionine Aminopeptidase-2 (MetAP-2) inhibitor.
|
-
- HY-W016586A
-
|
Acivicin hydrochloride
AT-125 hydrochloride; U-42126 hydrochloride
|
Parasite
|
Cancer
Infection
|
|
Acivicin hydrochloride (AT-125 hydrochloride), a natural product produced by Streptomyces sviceus, is a γ-glutamyl transpeptidase (GGT) inhibitor. Acivicin hydrochloride can across the blood-brain barrier and has anti-cancer, anti-parasitic properties.
|
-
- HY-50098A
-
|
Mardepodect hydrochloride
PF-2545920 hydrochloride
|
Phosphodiesterase (PDE)
|
Cancer
|
|
Mardepodect hydrochloride (PF-2545920 hydrochloride) is a potent, orally active and selective PDE10A inhibitor with an IC50 of 0.37 nM, with >1000-fold selectivity over other PDEs. Mardepodect hydrochloride can cross the blood-brain barrier.
|
-
- HY-N0229S2
-
-
- HY-14200A
-
|
(S)-Rasagiline mesylate
TVP1022 mesylate; S-PAI mesylate
|
Monoamine Oxidase
|
Neurological Disease
|
|
(S)-Rasagiline (TVP1022) mesylate is the relatively inactive S-enantiomer form of Rasagiline mesylate. Rasagiline mesylate is a highly potent selective irreversible MAO inhibitor with IC50s of 4.43 nM and 412 nM for rat brain MAO B and A activity, respectively.
|
-
- HY-148711
-
-
- HY-15976
-
|
P7C3
|
Others
|
Neurological Disease
|
|
P7C3 is an orally bioavailable and blood-brain barrier penetrant aminopropyl carbazole, with neuroprotective effects. P7C3 can be used for the research of neurodegenerative diseases, including Parkinson's disease.
|
-
- HY-43586
-
|
BR351 precursor
|
MMP
|
Cancer
|
|
BR351 precursor is a precursor of BR351. BR351 is a brain penetrant MMP inhibitor with IC50s of 4, 2, 11, 50 nM for MMP2, MMP8, MMP9 and MMP13, respectively.
|
-
- HY-B0186
-
|
Cefoselis
|
Bacterial
Antibiotic
|
Infection
|
|
Cefoselis, the fourth gen-eration of cephalosporin, is a β-lactam antibiotic. Cefoselis exhibits good activity against a wide range of Gram-positive and Gram-negative organisms. Cefoselis penetrates the blood-brain barrier.
|
-
- HY-109061
-
|
Lazertinib
YH25448; GNS-1480
|
EGFR
|
Cancer
|
|
Lazertinib (YH25448) is a potent, highly mutant-selective, blood-brain barrier permeable, orally available and irreversible third-generation EGFR tyrosine kinase inhibitor, and can be used in the research of non-small cell lung cancer.
|
-
- HY-B1395
-
-
- HY-P2457
-
|
rCRAMP (rat)
|
Bacterial
|
Infection
Inflammation/Immunology
|
|
rCRAMP (rat) is the rat cathelin-related antimicrobial peptide. rCRAMP (rat) contributes to the antibacterial activity in rat brain peptide/protein extracts. rCRAMP (rat) is a potential key player in the innate immune system of rat CNS.
|
-
- HY-151546
-
|
MRS4596
|
P2X Receptor
|
Neurological Disease
|
|
MRS4596 is a potent and selective P2X4 receptor antagonist with an IC50 value of 1.38 μM for human P2X4 receptor. MRS4596 has neuroprotective and neuro-rehabilitative activities in ischemic stroke model. MRS4596 can be used in research of ischemic stroke .
|
-
- HY-119513
-
|
Nizofenone
|
Others
|
Neurological Disease
|
|
Nizofenone is a neuroprotective agent which protects neurons from death following cerebral ischemia or anoxia. Nizofenone can be used in the research of acute neurological conditions, such as stroke.
|
-
- HY-112248
-
-
- HY-112198
-
|
AZ31
|
ATM/ATR
|
Cancer
|
|
AZ31 is a a potent, highly selective, and orally active ATM inhibitor with an IC50 of <1.2 nM for ATM enzyme, and an IC50 of 46 nM for ATM in cell. AZ31 shows excellent selectivity over ATR (>500-fold) and excellent PIKK-family selectivity and pan-kinase selectivity. AZ31 is a potent radiosensitizer in vitro, it can be used for the research of cancer.
|
-
- HY-B0250
-
|
Lamivudine
BCH-189
|
HIV
Reverse Transcriptase
HBV
|
Infection
Cancer
|
|
Lamivudine (BCH-189) is an orally active nucleoside reverse transcriptase inhibitor (NRTI). Lamivudine can inhibit HIV reverse transcriptase 1/2 and also the reverse transcriptase of hepatitis B virus. Lamivudine salicylate can penetrate the CNS.
|
-
- HY-10397A
-
|
MX1013
CV1013; Z-VD-FMK
|
Caspase
|
Cancer
|
|
MX1013 is a potent, irreversible dipeptide caspase inhibitor vith antiapoptotic activity. MX1013 inhibits recombinant human caspase 3 with an IC50 of 30 nM.
|
-
- HY-114759
-
-
- HY-103331
-
-
- HY-100937
-
|
DPCPX
PD 116948
|
Adenosine Receptor
|
Cardiovascular Disease
|
|
DPCPX (PD 116948), a xanthine derivative, is a highly potent and selective Adenosine A1 receptor antagonist, with a Ki of 0.46 nM in 3H-CHA binding to A1 receptors in rat whole brain membranes.
|
-
- HY-117508
-
-
- HY-13058
-
|
ADX-47273
|
mGluR
|
Neurological Disease
|
|
ADX-47273 is a potent, selective and brain-penetrant mGluR5 positive allosteric modulator (PAM), with an EC50 of 0.17 μM for potentiation of glutamate (50 nM) response. ADX-47273 has antipsychotic and procognitive activities.
|
-
- HY-N0667S1
-
-
- HY-115383
-
-
- HY-N4097
-
|
Incensole
|
Others
|
Neurological Disease
|
|
Incensole, a 14-membered diterpenoid, is isolated from both essential oils and resins of frankincense. Incensole has shown anti-inflammatory and anti-depression activities due to their ability to activate ion channels in the brain to alleviate anxiety or depression.
|
-
- HY-B0099S
-
|
Edaravone-d5
MCI-186-d5
|
MMP
Apoptosis
|
Neurological Disease
|
|
Edaravone-d5 is a deuterium labeled Edaravone. Edaravone is a strong novel free radical scavenger, and inhibits MMP-9-related brain hemorrhage in rats treated with tissue plasminogen activator[1][2][3][4].
|
-
- HY-N0003
-
|
Honokiol
NSC 293100
|
Akt
Autophagy
HCV
ERK
|
Cancer
|
|
Honokiol is a bioactive, biphenolic phytochemical that possesses potent antioxidative, anti-inflammatory, antiangiogenic, and anticancer activities by targeting a variety of signaling molecules. It inhibits the activation of Akt. Honokiol can readily cross the blood brain barrier.
|
-
- HY-B0303AS1
-
-
- HY-148331
-
-
- HY-B0692A
-
|
Cefepime chloride
BMY-28142 chloride
|
Antibiotic
Bacterial
|
Infection
|
|
Cefepime (BMY-28142) chloride is a broad-spectrum and cross the blood-brain barrier cephalosporin. Cefepime chloride shows antibacterial effects against both Gram-positive and Gram-negative aerobic bacteria. Cefepime chloride induces neurotoxicity.
|
-
- HY-N2072
-
|
Transcrocetin
trans-Crocetin
|
iGluR
Endogenous Metabolite
|
Cancer
|
|
Transcrocetin (trans-Crocetin), extracted from saffron (Crocus sativus L.), acts as an NMDA receptor antagonist with high affinity. Transcrocetin (trans-Crocetin) is capable of crossing the blood-brain barrier and reach the central nervous system (CNS).
|
-
- HY-122935
-
|
Nigranoic acid
|
HIV
Reverse Transcriptase
|
Infection
|
|
Nigranoic acid is a triterpenoid separated from Schisandra chinensis. Nigranoic acid inhibits HIV-1 reverse transcriptase. Nigranoic acid exhibits protective effects on brain through PARP/AIF signaling pathway in cerebral ischemia-reperfusion animal model.
|
-
- HY-145317
-
|
LRRK2-IN-2
|
LRRK2
|
Neurological Disease
|
|
LRRK2-IN-2 (compoubd 22) is a potent, selective, orally active and brain-penetrant inhibitor LRRK2, with IC50 of <0.6 nM. LRRK2-IN-2 can be used for the research of Parkinson's disease.
|
-
- HY-B0303AS
-
-
- HY-B0692
-
|
Cefepime
BMY-28142
|
Antibiotic
Bacterial
|
Infection
Cancer
|
|
Cefepime (BMY-28142) is a broad-spectrum and cross the blood-brain barrier cephalosporin. Cefepime shows antibacterial effects against both Gram-positive and Gram-negative aerobic bacteria. Cefepime induces neurotoxicity.
|
-
- HY-15249
-
|
JZL 184
|
MAGL
|
Neurological Disease
|
|
JZL 184 is a potent, selective and irreversible MAGL inhibitor that blocks 2-Arachidonoylglycerol (2-AG) hydrolysis in brain membranes (IC50 of 8 nM). JZL 184 displays >300-fold selectivity for MAGL over FAAH.
|
-
- HY-111455
-
|
LP-211
|
5-HT Receptor
|
Neurological Disease
|
|
LP-211 is a selective and blood−brain barrier penetrant 5-HT7 receptor agonist, with a Ki of 0.58 nM, with high selectivity over 5-HT1A receptor (Ki, 188 nM) and D2 receptor (Ki, 142 nM).
|
-
- HY-121883
-
|
Lignoceric acid
Tetracosanoic acid
|
Endogenous Metabolite
|
Neurological Disease
|
|
Lignoceric acid (Tetracosanoic acid) is a 24-carbon saturated (24:0) fatty acid, which is synthesized in the developing brain. Lignoceric acid is also a by-product of lignin production. Lignoceric acid can be used for Zellweger cerebro‐hepato‐renal syndrome and adrenoleukodystrophy research.
|
-
- HY-W017443S3
-
-
- HY-152632
-
|
BuChE-IN-7
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
BuChE-IN-7 is a highly selective inhibitor of hBuChe and eqBuChE with IC50 values of 40 nM, 80 nM respectively. BuChE-IN-7 can promote cognitive with blood-brain penetration and improves situational and phobic memory, showing preference for new things.
|
-
- HY-11030
-
-
- HY-P99530
-
|
Valanafusp alfa
AGT-181; HIRMAb-IDUA
|
Insulin Receptor
|
Metabolic Disease
|
|
Valanafusp alfa (AGT-181) is a brain penetrating recombinant fusion protein of a chimeric monoclonal antibody against the human insulin receptor (HIR) and human iduronidase (IDUA). Valanafusp alfa can be used for the research of Mucopolysaccharidosis type I (MPS I) .
|
-
- HY-122015
-
|
ASP2905
|
Potassium Channel
|
Neurological Disease
|
|
ASP2905 is a potent and selective potassium channel Kv12.2 inhibitor encoded by the Kcnh3/BEC1 gene. ASP2905 can cross the blood-brain barrier and has antipsychotic activities.
|
-
- HY-B0318A
-
-
- HY-50880
-
|
Elacridar hydrochloride
GF120918A
|
P-glycoprotein
BCRP
|
Cancer
|
|
Elacridar hydrochloride (GF120918A) is an orally active P-glycoprotein (P-gp) and breast cancer resistance protein (BCRP) inhibitor. Elacridar hydrochloride can be used to examine the influence of efflux transporters on drug distribution to brain and it can be used for the research of cancer.
|
-
- HY-119696
-
|
MTIC
|
Drug Metabolite
|
Cancer
Neurological Disease
|
|
MTIC is the active metabolite of Temozolomide (TMZ). MITC has lower bioavailability in the brain compared with TMZ, because the drug’s permeability through biological barriers and tumor cell membranes affects bioavailability. MITC exhibits low affinity to biological membrane.
|
-
- HY-103244
-
|
CITCO
|
Apoptosis
|
Cancer
|
|
CITCO, an imidazothiazole derivative, is a selective Constitutive androstane receptor (CAR) agonist. CITCO inhibits growth and expansion of brain tumour stem cells (BTSCs) and has an EC50 of 49 nM over pregnane X receptor (PXR), and no activity on other nuclear receptors.
|
-
- HY-126985
-
|
4,9-Anhydrotetrodotoxin
Anhydroepitetrodotoxin
|
Sodium Channel
|
Neurological Disease
|
|
4,9-Anhydrotetrodotoxin is a selective voltage-gated sodium channel (VGSC) inhibitor that blocks Nav1.1 and Nav1.6 in human brain and induces a hyperpolarizing shift in the voltage dependence of inactivated Nav1.6.
|
-
- HY-145318
-
|
LRRK2-IN-3
|
LRRK2
|
Neurological Disease
|
|
LRRK2-IN-3 (compoubd 24) is a potent, selective, orally active and brain-penetrant inhibitor LRRK2, with IC50 of 2.6 nM in human PBMCs. LRRK2-IN-3 can be used for the research of Parkinson's disease.
|
-
- HY-107559
-
|
GT-2016
|
Histamine Receptor
|
Neurological Disease
|
|
GT-2016 is a potent, selective, and brain penetrant histamine H3 receptor antagonist with a Ki of 43.8 nM. GT-2016 displays selectivity against H1 and H2 receptors, and has non-active against histamine methyltransferase.
|
-
- HY-W017443S
-
-
- HY-12206
-
|
Thioperamide
MR-12842
|
Histamine Receptor
|
Neurological Disease
|
|
Thioperamide (MR-12842) is a potent, orally available, brain penetrant and selective H3 receptor antagonist with a Ki of 4.3 nM for inhibition of [ 3H]histamine release. Thioperamide inhibits [ 3H]histamine synthesis with a Ki of 31 nM.
|
-
- HY-N0229S15
-
|
L-Alanine-13C2,15N
L-2-Aminopropionic acid-13C2,15N
|
Endogenous Metabolite
|
|
|
L-Alanine- 13C2, 15N is the 13C- and 15N-labeled L-Alanine. L-Alanine is a non-essential amino acid, involved in sugar and acid metabolism, increases immunity, and provides energy for muscle tissue, brain, and central nervous system.
|
-
- HY-W014941
-
-
- HY-101456
-
-
- HY-108234
-
|
VU 0255035
VU 255035
|
mAChR
|
Neurological Disease
|
|
VU 0255035 is a highly selective, competitive and brain penetrant muscarinic M1 receptor antagonist with an IC50 of 130 nM. VU 0255035 reduces pilocarpine-induced seizures in mice. VU0255035 is used to examine the role of the M1 receptor in diverse situations.
|
-
- HY-14781S2
-
-
- HY-110180
-
|
VU0409106
|
mGluR
|
Neurological Disease
|
|
VU0409106 is a potent and selective mGlu5 negative allosteric modulator (NAM) with an IC50 of 24 nM. VU0409106 shows anxiolytic effects in rat models in a concentration-dependent manner. VU0409106 also penetrates the blood-brain barrier (BBB).
|
-
- HY-125017
-
|
Bozitinib
PLB-1001; CBT-101; Vebreltinib
|
c-Met/HGFR
|
Cancer
|
|
Bozitinib (PLB-1001) is a highly selective c-MET kinase inhibitor with blood-brain barrier permeability. Bozitinib (PLB-1001) is a ATP-competitive small-molecule inhibitor, binds to the conventional ATP-binding pocket of the tyrosine kinase superfamily.
|
-
- HY-148165
-
-
- HY-N0229S10
-
-
- HY-15370
-
|
SB-269970
|
5-HT Receptor
|
Neurological Disease
|
|
SB-269970 is a potent, selective and brain-penetrant 5-HT7 receptor antagonist with a pKi of 8.3. SB-269970 exhibits >50-fold selectivity against other 5-HT receptors.
|
-
- HY-10328
-
|
Neflamapimod
VX-745
|
p38 MAPK
Autophagy
|
Inflammation/Immunology
|
|
Neflamapimod (VX-745) is a potent, blood-brain barrier penetrant, highly selective inhibitor of p38α inhibitor with an IC50 for p38α of 10 nM and for p38β of 220 nM. Neflamapimod (VX-745) possesses anti-inflammatory activity.
|
-
- HY-D0873
-
|
HEPPS
EPPS
|
Amyloid-β
|
Neurological Disease
|
|
HEPPS (EPPS) is a buffering agent with the useful pH range from 7.3 ~ 8.7. HEPPS reduces Aβ-aggregate-induced memory deficits and rescues cognitive deficits in mice. EPPS is orally active and penetrates the blood-brain barrier.
|
-
- HY-15370A
-
-
- HY-105077A
-
|
Nemifitide diTFA
INN 00835 diTFA
|
5-HT Receptor
|
Neurological Disease
|
|
Nemifitide diTFA (INN 00835 diTFA) is a synthetic pentapeptide antidepressant with a potential for rapid onset of action. Nemifitide diTFA is a peptide analog of melanocyte-inhibiting factor (MIF). Nemifitide diTFA can cross the blood-brain barrier.
|
-
- HY-143464
-
|
BChE-IN-4
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
BChE-IN-4 is a potent and cross the blood-brain barrier BChE inhibitor. BChE-IN-4 attenuates learning and memory deficits caused by cholinergic deficit in mouse model. BChE-IN-4 has the potential for the research of alzheimer’s disease.
|
-
- HY-108589
-
|
PNU 37883 hydrochloride
PNU 37883A
|
Potassium Channel
|
Neurological Disease
|
|
PNU 37883 hydrochloride (PNU 37883A) is a selective vascular ATP-sensitive potassium (Kir6, KATP) channels blocker. PNU 37883 hydrochloride has diuretic effects with specific binding in kidney and vascular smooth muscle rather than in brain or pancreatic beta cells.
|
-
- HY-B0315S
-
-
- HY-12206A
-
|
Thioperamide maleate
MR-12842 maleate
|
Histamine Receptor
|
Neurological Disease
|
|
Thioperamide maleate (MR-12842 maleate) is a potent, orally available, brain penetrant and selective H3 receptor antagonist with a Ki of 4.3 nM for inhibition of [ 3H]histamine release. Thioperamide maleate inhibits [ 3H]histamine synthesis with a Ki of 31 nM.
|
-
- HY-P3585
-
|
Epobis
|
TNF Receptor
|
Inflammation/Immunology
Neurological Disease
|
|
Epobis, a dendrimeric peptide, is a recombinant form of erythropoietin. Epobis is a potent erythropoietin receptor agonist. Epobis promotes neuritogenesis in primary motoneurons. Epobis decrease TNF release and crosses the blood-brain barrier. Epobis has anti-inflammatory and memory enhancing properties.
|
-
- HY-N0229S14
-
-
- HY-13662B
-
|
(R)-Lansoprazole
Dexlansoprazole
|
Proton Pump
|
Inflammation/Immunology
|
|
(R)-Lansoprazole is the R enantiomer of Lansoprazole, Lansoprazole (AG 1749) is an orally active proton pump inhibitor which prevents the stomach from producing acid. Lansoprazole (AG 1749) is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor).
|
-
- HY-146588
-
|
NMDA receptor antagonist 4
|
iGluR
Others
|
Neurological Disease
|
|
NMDA receptor antagonist 4 (IIc) is a uncompetitive, voltage-dependent, orally active NMDAR blocker, with an IC50 of 1.93 µM. NMDA receptor antagonist 4 shows a positive predicted blood-brain-barrier (BBB) permeability, and can be studied in Alzheimer's disease.
|
-
- HY-N0229S11
-
-
- HY-12768
-
|
Sotuletinib
BLZ945
|
c-Fms
|
Cancer
|
|
Sotuletinib (BLZ945) is a potent, selective and brain-penetrant CSF-1R (c-Fms) inhibitor with an IC50 of 1 nM, showing more than 1,000-fold selectivity against its closest receptor tyrosine kinase homologs.
|
-
- HY-17423E
-
|
Abacavir hydrochloride
|
HIV
Apoptosis
Reverse Transcriptase
Telomerase
|
Cancer
Infection
|
|
Abacavir hydrochloride is a competitive, orally active nucleoside reverse transcriptase inhibitor. Abacavir hydrochloride can inhibits the replication of HIV. Abacavir hydrochloride shows anticancer activity in prostate cancer cell lines. Abacavir hydrochloride can trespass the blood-brain-barrier and suppresses telomerase activity.
|
-
- HY-134968
-
|
TTBK1-IN-1
|
Tau Protein
|
Neurological Disease
|
|
TTBK1-IN-1 is a potent, selective and brain-penetrant tau tubulin kinase 1 (TTBK1) inhibitor with an IC50 of 2.7 nM. TTBK1-IN-1 can be used for the research of alzheimer’s disease and related tauopathies.
|
-
- HY-100238
-
-
- HY-17423
-
|
Abacavir
|
HIV
Reverse Transcriptase
Telomerase
Apoptosis
|
Cancer
Infection
|
|
Abacavir is an orally active and competitive nucleoside reverse transcriptase inhibitor. Abacavir can inhibits the replication of HIV. Abacavir shows anticancer activity in prostate cancer cell lines. Abacavir can trespass the blood-brain-barrier and suppresses telomerase activity.
|
-
- HY-N0506
-
|
Rosarin
|
Interleukin Related
|
Neurological Disease
|
|
Rosarin is a cinnamyl alcohol glycoside isolated from Rhodiola rosea. Rosarin has anti-inflammatory and neuroprotective effects. Rosarin supresses the expression of the proinflammatory factors iNOS, IL-1 β, and TNF- α in the kidney and prefrontal cortex of brain in mice .
|
-
- HY-B0762S
-
|
Acetyl-L-carnitine-d3 hydrochloride
O-Acetyl-L-carnitine-d3 (hydrochloride)
|
Endogenous Metabolite
|
Neurological Disease
|
|
Acetyl-L-carnitine-d3 (hydrochloride) is the deuterium labeled Acetyl-L-carnitine hydrochloride. Acetyl-L-carnitine hydrochloride is a blood-brain permeable acetyl ester of the amino acid L-carnitine found in the body. Acetyl-L-carnitine hydrochloride is often used as a dietary supplement, and exibits anti-stress-related psychiatric disorders[1].
|
-
- HY-148419
-
|
TNG908
|
Histone Methyltransferase
|
Cancer
|
|
TNG908 is a MTAP-cooperative PRMT5 inhibitor that can pass through the blood-brain barrier. TNG908 is 15 times more selective for MTAP null cell lines than MTAP WT cell lines, and can be used in cancer research.
|
-
- HY-148565
-
-
- HY-N11061
-
|
Withaphysalin D
|
iGluR
|
Neurological Disease
|
|
Withaphysalin D is a selective antagonist against the N-methyl-D-aspartate receptor (NMDAR) containing GluN2B. Withaphysalin D can be isolated from water lilies and has neuroprotective properties. Withaphysalin D is able to cross the blood-brain barrier.
|
-
- HY-17399S
-
|
Racecadotril-d5
Acetorphan-d5
|
Neprilysin
|
Metabolic Disease
|
|
Racecadotril-d5 is the deuterium labeled Racecadotril. Racecadotril (Acetorphan) is a neutral endopeptidase (NEP) inhibitor. Racecadotril and its active metabolite Thiorphan inhibits purified NEP activity from mouse brain with Kis of 4500 and 6.1 nM, , respectively. Antidiarrheal agent[1].
|
-
- HY-A0160
-
|
Indalpine
LM 5008
|
Serotonin Transporter
|
Neurological Disease
|
|
Indalpine (LM 5008) is a potent and selective 5-HT uptake blocker. Indalpine is potent in displacing 3H-5-HT bound to brain membranes with the IC50 of 36 μM. Indalpine, two antidepressant agent.
|
-
- HY-14569
-
|
CDPPB
|
mGluR
|
Neurological Disease
|
|
CDPPB is a potent, selective and brain penetrant positive allosteric modulator of the metabotropic glutamate receptor subtype 5 (mGluR5), with an EC50 of 27 nM in Chinese hamster ovary cells expressing human mGluR5. CDPPB may provide an approach for development of antipsychotic agents.
|
-
- HY-145778
-
|
AGI-41998
|
Somatostatin Receptor
|
Neurological Disease
|
|
AGI-41998 is a potent inhibitor of methionine adenosyltransferase 2A (MAT2A). AGI-41998 is a brain-penetrant compound. AGI-41998 has the potential for exploring the effects of SAM modulation in the central nervous system (CNS) and research of cancer disease.
|
-
- HY-144270
-
-
- HY-15262
-
|
SRT 2104
|
Sirtuin
|
Metabolic Disease
Neurological Disease
Cancer
|
|
SRT 2104 is a first-in-class, highly selective and brain-permeable activator of the NAD + dependent deacetylase Sirt1, increases Sirt1 protein, but shows no effect on Sirt1 mRNA. Used in the research of diabetes mellitus and Huntington’s disease.
|
-
- HY-18678
-
|
Bremelanotide
PT-141
|
Melanocortin Receptor
|
Endocrinology
|
|
Bremelanotide (PT-141) is an analogue of α-melanocyte-stimulating hormone (α-MSH). Bremelanotide activates the mPOA and other hypothalamic and limbic regions of the brain involved in sexual behavior. Bremelanotide can be used for researching hypoactive sexual desire disorders.
|
-
- HY-N6608
-
|
Physostigmine
Eserine
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
Physostigmine (Eserine) is a reversible acetylcholinesterase (AChE) inhibitor. Physostigmine can crosses the blood-brain barrier and stimulates central cholinergic neurotransmission. Physostigmine can reverse memory deficits in transgenic mice with Alzheimer's disease. Physostigmine is also an antidote for anticholinergic poisoning.
|
-
- HY-14450
-
-
- HY-N2160
-
|
6'''-Feruloylspinosin
|
GABA Receptor
|
Neurological Disease
|
|
6'''-Feruloylspinosin is a flavonoid isolated from seeds of Ziziphus jujuba. 6'''-Feruloylspinosin can across the blood-brain barrier and enhance the expression of GABAAα1, GABAAα5, and GABABR1 mRNA in rat hippocampal neurons.
|
-
- HY-128420
-
|
Lobeline sulfate
α-Lobeline sulfate; L-Lobeline sulfate
|
Endogenous Metabolite
|
Neurological Disease
|
|
Lobeline sulfate (α-Lobeline sulfate; L-Lobeline sulfate) is a nonstimulant medication that can alter dopamine uptake in brain. Lobeline sulfate (α-Lobeline sulfate; L-Lobeline sulfate) inhibits nicotine-induced hyperactivity and is effective in smoking cessation.
|
-
- HY-118952
-
|
PF-06456384
|
LRRK2
|
Neurological Disease
|
|
PF-06447475 is a highly potent, selective, brain penetrant LRRK2 kinase inhibitor with IC50 values of 3 nM and 11 nM for WT LRRK and G2019S LRRK2, respectively. PF-06447475 can be used for parkinson's disease (PD) research.
|
-
- HY-14136S
-
-
- HY-111791
-
|
ACY-1083
|
HDAC
|
Cancer
|
|
ACY-1083 is a selective and brain-penetrating HDAC6 inhibitor with an IC50 of 3 nM and is 260-fold more selective for HDAC6 than all other classes of HDAC isoforms. ACY-1083 effectively reverses chemotherapy-induced peripheral neuropathy.
|
-
- HY-15084B
-
|
Dizocilpine
MK-801
|
iGluR
|
Neurological Disease
|
|
Dizocilpine (MK-801), a potent anticonvulsant, is a selective and non-competitive NMDA receptor antagonist, with a Kd of 37.2 nM in rat brain membranes. Dizocilpine acts by binding to a site located within the NMDA associated ion channel and thus prevents Ca 2+ flux.
|
-
- HY-100999
-
-
- HY-118952A
-
|
PF-06456384 trihydrochloride
|
LRRK2
|
Neurological Disease
|
|
PF-06447475 trihydrochloride is a highly potent, selective, brain penetrant LRRK2 kinase inhibitor with IC50 values of 3 nM and 11 nM for WT LRRK and G2019S LRRK2, respectively. PF-06447475 trihydrochloride can be used for parkinson's disease (PD) research.
|
-
- HY-18236
-
|
MDL-28170
Calpain Inhibitor III
|
Proteasome
|
Inflammation/Immunology
Neurological Disease
|
|
MDL-28170 (Calpain Inhibitor III) is a potent, selective and membrane-permeable cysteine protease inhibitor of calpain that rapidly penetrates the blood-brain barrier following systemic administration. MDL-28170 also block γ-secretase.
|
-
- HY-W050031
-
|
(S)-3-Hydroxybutanoic acid
(S)-β-Hydroxybutanoic acid; L-(+)-3-Hydroxybutyric acid; L-β-Hydroxybutyric acid
|
Endogenous Metabolite
|
Others
|
|
(S)-3-Hydroxybutanoic acid is a normal human metabolite, that has been found elevated in geriatric patients remitting from depression. In humans, 3-Hydroxybutyric acid is synthesized in the liver from acetyl-CoA, and can be used as an energy source by the brain when blood glucose is low.
|
-
- HY-112855
-
|
PF-06454589
|
LRRK2
|
Neurological Disease
|
|
PF-06447475 is a highly potent, selective, brain penetrant LRRK2 kinase inhibitor with IC50 values of 3 nM and 11 nM for WT LRRK and G2019S LRRK2, respectively. PF-06447475 can be used for parkinson's disease (PD) research.
|
-
- HY-B0762S1
-
|
Acetyl-L-carnitine-d3-1 hydrochloride
O-Acetyl-L-carnitine-d3-1 (hydrochloride)
|
Endogenous Metabolite
|
Neurological Disease
|
|
Acetyl-L-carnitine-d3-1 (hydrochloride) is the deuterium labeled Acetyl-L-carnitine hydrochloride. Acetyl-L-carnitine hydrochloride is a blood-brain permeable acetyl ester of the amino acid L-carnitine found in the body. Acetyl-L-carnitine hydrochloride is often used as a dietary supplement, and exibits anti-stress-related psychiatric disorders[1].
|
-
- HY-N0496
-
|
Ruscogenin
|
NOD-like Receptor (NLR)
|
Cardiovascular Disease
|
|
Ruscogenin, an important steroid sapogenin derived from Ophiopogon japonicus, attenuates cerebral ischemia-induced blood-brain barrier dysfunction by suppressing TXNIP/NLRP3 inflammasome activation and the MAPK pathway and exerts significant anti-inflammatory and anti-thrombotic activities.
|
-
- HY-16748
-
|
Nelonicline
ABT-126
|
nAChR
|
Neurological Disease
|
|
Nelonicline (ABT-126) is an orally active and selective α7 nicotinic receptor agonist with high affinity to α7 nAChRs in human brain (Ki=12.3 nM). Nelonicline is used for the research of shizophrenia and Alzheimer's disease.
|
-
- HY-B0534S1
-
|
Moclobemide-d4
Ro111163-d4
|
Monoamine Oxidase
|
Neurological Disease
|
|
Moclobemide-d4 is deuterium labeled Moclobemide. Moclobemide (Ro111163) is a brain-penetrant and reversible monoamine oxidase (MAO-A) inhibitor with an IC50 of 6.061 μM for hMAO-A[1].Moclobemide up-regulates proliferation of hippocampal progenitor cells in chronically stressed mice.
|
-
- HY-119744
-
|
BAY 38-7271
|
Cannabinoid Receptor
|
Neurological Disease
|
|
BAY 38-7271 is selective and highly potent and cannabinoid CB1/CB2 receptor agonist, with Kis of 1.85 nM and 5.96 nM for recombinant human CB1 receptor and CB2 receptor, respectively. BAY 38-7271 has strong neuroprotective properties.
|
-
- HY-135046
-
|
MTOB sodium
|
Others
|
Cancer
Inflammation/Immunology
Neurological Disease
|
|
MTOB sodium is a potent C-terminal binding protein (CtBP) inhibitor. MTOB sodium attenuates repetitive head injury-elicited neurologic dysfunction and neuroinflammation via inhibition of the transactivation activity of CtBP1 and CtBP2. MTOB sodium antagonizes the transcriptional regulatory activity of CtBP1 and CtBP2 by eviction from their target promoters in breast cancer cell lines.
|
-
- HY-16743
-
|
Ibiglustat
Venglustat; SAR402671; GZ402671
|
Glucosylceramide Synthase (GCS)
|
Metabolic Disease
|
|
Ibiglustat (Venglustat) is an orally active, brain-penetrant glucosylceramide synthase (GCS) inhibitor. Ibiglustat can be used for the research of Gaucher disease type 3, Parkinson's disease associated with GBA mutations, Fabry disease, GM2 gangliosidosis, and autosomal dominant polycystic kidney disease.
|
-
- HY-145777
-
|
AGI-43192
|
Somatostatin Receptor
|
Cancer
Neurological Disease
|
|
AGI-43192 is a potent inhibitor of methionine adenosyltransferase 2A (MAT2A). AGI-43192 is a potent, but limited brain-penetrant compound. AGI-43192 has the potential for exploring the effects of SAM modulation in the central nervous system (CNS) and research of cancer disease.
|
-
- HY-152141
-
|
hCAII-IN-9
|
Carbonic Anhydrase
|
Others
|
|
hCAII-IN-9 is a potent carbonic anhydrase inhibitor with IC50s of 1.18 μM (hCA II), 0.17 μM (hCA IX), and 2.99 μM (hCA XII), respectively. hCAII-IN-9 has no blood-brain barrier permeability.
|
-
- HY-B0309
-
|
Felodipine
|
Calcium Channel
Autophagy
|
Cardiovascular Disease
|
|
Felodipine, a dihydropyridine, is a potent, vasoselective calcium channel antagonist. Felodipine lowers blood pressure (BP) by selective action on vascular smooth muscle, especially in the resistance vessels. Felodipine, an anti-hypertensive agent, induces autophagy. Felodipine can cross the blood-brain barrier.
|
-
- HY-139464
-
-
- HY-144302
-
|
AAK1-IN-3
|
AAK1
|
Neurological Disease
|
AAK1-IN-3, a quinoline analogue, is a brain-penetrant adaptor protein 2-associated kinase 1 (AAK1) inhibitor with an IC50 of 11 nM. AAK1-IN-3 has the potential for neuropathic pain research.
|
-
- HY-14602
-
|
Tramiprosate
Homotaurine; 3-Amino-1-propanesulfonic acid
|
Amyloid-β
|
Cancer
|
|
Tramiprosate (Homotaurine), an orally active and brain-penetrant natural amino acid found in various species of red marine algae. Tramiprosate binds to soluble Aβ and maintains Aβ in a non-fibrillar form. Tramiprosate is also a GABA analog and possess neuroprotection, anticonvulsion and antihypertension effects.
|
-
- HY-107855
-
|
DL-Mevalonolactone
(±)-Mevalonolactone; Mevalolactone
|
Endogenous Metabolite
|
Metabolic Disease
|
|
DL-Mevalonolactone ((±)-Mevalonolactone;Mevalolactone) is the δ-lactone form of mevalonic acid, a precursor in the mevalonate pathway. DL-Mevalonolactone (Mevalonolactone) decreases mitochondrial membrane potential (∆Ψm), NAD(P)H content and the capacity to retain Ca 2+ in the brain, besides inducing mitochondrial swelling.
|
-
- HY-13788
-
-
- HY-15760
-
-
- HY-N0229S
-
-
- HY-B0186B
-
|
Cefoselis sulfate
FK-037
|
Bacterial
Antibiotic
|
Infection
|
|
Cefoselis sulfate (FK-037), the fourth gen-eration of cephalosporin, is a β-lactam antibiotic. Cefoselis sulfate exhibits good activity against a wide range of Gram-positive and Gram-negative organisms. Cefoselis sulfate penetrates the blood-brain barrier.
|
-
- HY-11030A
-
-
- HY-120738
-
|
p-MPPI hydrochloride
|
5-HT Receptor
|
Neurological Disease
|
|
p-MPPI hydrochloride is a selective 5-HT1A receptor antagonist with high affinity for 5-HT1A receptors. p-MPPI hydrochloride can crosses the blood-brain barrier, and has clear antidepressant and anxiolytic-like effects.
|
-
- HY-13788B
-
-
- HY-50682
-
|
Azeliragon
TTP488; PF-04494700
|
Amyloid-β
|
Neurological Disease
|
|
Azeliragon (TTP488) is an orally bioavailable inhibitor of the receptor for advanced glycation end products (RAGE) in development as a potential treatment to slow disease progression in patients with mild Alzheimer’s disease (AD). Azeliragon also can cross the blood-brain barrier (BBB).
|
-
- HY-W017443S2
-
-
- HY-128346
-
|
PQM130
|
Amyloid-β
|
Neurological Disease
|
|
PQM130, a Feruloyl-Donepezil Hybrid compound with brain penatration, is a multitarget drug candidate against the neurotoxicity induced by Aβ1-42 oligomer (AβO) and shows anti-inflammatory activity. PQM130 acts as a neuroprotective compound for anti-AD drug development.
|
-
- HY-108683
-
|
ACT-335827
|
Orexin Receptor (OX Receptor)
|
Neurological Disease
|
|
ACT-335827 is a selective, orally active, brain-penetrant orexin type 1 receptor antagonist. ACT-33582 acts on OXR1 and OXR2 with IC50 values of 6 nM and 417 nM, respectively. ACT-33582 can be used in studies related to neurological disorders.
|
-
- HY-15981
-
|
Omarigliptin
MK-3102
|
Dipeptidyl Peptidase
|
Metabolic Disease
Neurological Disease
|
|
Omarigliptin (MK-3102) is a potent, selective, orally active and cross the blood-brain barrier dipeptidyl peptidase 4 (DPP-4) inhibitor. Omarigliptin shows anti-parkinsonian activity. Omarigliptin has the neuroprotective effect to improve diabetes-associated cognitive dysfunction.
|
-
- HY-17547
-
|
NMS-E973
|
HSP
|
Cancer
|
|
NMS-E973 is a potent and selective inhibitor of HSP90. NMS-E973 binds to the ATP binding site of Hsp90α with a DC50 of <10 nM. NMS-E973 is able to cross the blood-brain barrier (BBB). Antitumor efficacy.
|
-
- HY-144302A
-
|
AAK1-IN-3 TFA
|
AAK1
|
Neurological Disease
|
AAK1-IN-3 TFA, a quinoline analogue, is a brain-penetrant adaptor protein 2-associated kinase 1 (AAK1) inhibitor with an IC50 of 11 nM. AAK1-IN-3 has the potential for neuropathic pain research.
|
-
- HY-B1066
-
|
Butylhydroxyanisole
Butylated hydroxyanisole; BHA; E320
|
Reactive Oxygen Species
Ferroptosis
|
Inflammation/Immunology
Neurological Disease
|
|
Butylhydroxyanisole (Butylated hydroxyanisole) is an antioxidant used as a food additive preservative. Butylhydroxyanisole mediates liver toxicity, retardation in reproductive organ development and learning, and sleep deficit. Butylhydroxyanisole exerts neurotoxic effects and leads to disruption of the brain and nerve development. Butylhydroxyanisole is a ferroptosis inducer.
|
-
- HY-W013215
-
|
Adrenic Acid
cis-7,10,13,16-Docosatetraenoic acid
|
Endogenous Metabolite
|
Metabolic Disease
Inflammation/Immunology
|
|
Adrenic Acid (cis-7,10,13,16-Docosatetraenoic acid) is a naturally polyunsaturated fatty acid in the adrenal gland, brain, kidney, and vasculature. Adrenic Acid can regulate the vascular tone in arteries of the adrenal cortex. Adrenic Acid also is an inflammation enhancer in non-alcoholic fatty liver disease.
|
-
- HY-N0067
-
|
γ-Aminobutyric acid
4-Aminobutyric acid
|
GABA Receptor
Endogenous Metabolite
|
Neurological Disease
|
|
γ-Aminobutyric acid (4-Aminobutyric acid) is a major inhibitory neurotransmitter in the adult mammalian brain, binding to the ionotropic GABA receptors (GABAA receptors) and metabotropic receptors (GABAB receptors. γ-Aminobutyric acid shows calming effect by blocking specific signals of central nervous system.
|
-
- HY-129411
-
|
Sinbaglustat
ACT-519276; OGT2378
|
Glucosylceramide Synthase (GCS)
|
Metabolic Disease
|
|
Sinbaglustat (OGT2378) is a dual inhibitor of glucosylceramide synthase (GCS) and non-lysosomal glucosyl ceramidase (GBA2). Sinbaglustat is an orally available N-alkyl iminosugar that crosses the blood-brain barrier. Sinbaglustat can be used for the research of central neurodegenerative diseases associated with lysosomal dysfunctions.
|
-
- HY-N0229S5
-
|
L-Alanine-13C3,15N,d4
L-2-Aminopropionic acid-13C3,15N,d4
|
Endogenous Metabolite
|
Metabolic Disease
Neurological Disease
|
|
L-Alanine- 13C3, 15N,d4 is the deuterium, 13C-, and 15-labeled L-Alanine. L-Alanine is a non-essential amino acid, involved in sugar and acid metabolism, increases immunity, and provides energy for muscle tissue, brain, and central nervous system.
|
-
- HY-113273B
-
|
Diadenosine pentaphosphate pentaammonium
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Diadenosine pentaphosphate pentaammonium is an endogenous vasoactive purine dinucleotide which has been isolated from thrombocytes. Diadenosine polyphosphates (ApnA, n=2–7) have been identified as constituents of secretory vesicles such as in platelets, chromaffin cells, Torpedo synaptic terminals and brain synaptosomes.
|
-
- HY-124713
-
|
ML372
|
DNA/RNA Synthesis
|
Neurological Disease
|
|
ML372 inhibits survival motor neuron (SMN) protein ubiquitination, increases SMN protein stability without affecting mRNA expression. ML372 improves spinal muscular atrophy (SMA) in mice. ML372 is brain penetrant and has a reasonable exposure and half-life in vivo.
|
-
- HY-108448
-
|
N-Oleoyldopamine
OLDA
|
TRP Channel
|
Cardiovascular Disease
|
|
N-Oleoyldopamine (OLDA) is a product of condensation of oleic acid and dopamine (DA) and an endogenous TRPV1 selective agonist. N-Oleoyldopamine (OLDA) can crosses the blood-brain barrier. N-oleoyl-dopamine protects the heart against ischemia-reperfusion injury via activation of TRPV1.
|
-
- HY-113273C
-
|
Diadenosine pentaphosphate pentalithium
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Diadenosine pentaphosphate pentalithium is an endogenous vasoactive purine dinucleotide which has been isolated from thrombocytes. Diadenosine polyphosphates (ApnA, n=2–7) have been identified as constituents of secretory vesicles such as in platelets, chromaffin cells, Torpedo synaptic terminals and brain synaptosomes.
|
-
- HY-16748A
-
|
Nelonicline citrate
ABT-126 citrate
|
nAChR
|
Neurological Disease
|
|
Nelonicline (ABT-126) citrate is an orally active and selective α7 nicotinic receptor agonist with high affinity to α7 nAChRs in human brain (Ki=12.3 nM). Nelonicline citrate is used for the research of shizophrenia and Alzheimer's disease.
|
-
- HY-B0002A
-
|
Ondansetron hydrochloride dihydrate
GR 38032 hydrochloride dihydrate; SN 307 hydrochloride dihydrate
|
5-HT Receptor
|
Neurological Disease
|
|
Ondansetron (GR 38032) hydrochloride dehydrate is an orally active, highly selective and competitive 5-HT3 receptor antagonist (crosses the blood-brain barrier). Ondansetron hydrochloride dehydrate can be used in studies of preventing nausea and vomiting associated with cancer chemotherapy, radiation therapy and surgery.
|
-
- HY-144266
-
-
- HY-113273A
-
|
Diadenosine pentaphosphate pentasodium
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Diadenosine pentaphosphate pentasodium is an endogenous vasoactive purine dinucleotide which has been isolated from thrombocytes. Diadenosine polyphosphates (ApnA, n=2–7) have been identified as constituents of secretory vesicles such as in platelets, chromaffin cells, Torpedo synaptic terminals and brain synaptosomes.
|
-
- HY-103234
-
|
GYKI 52466
|
iGluR
|
Neurological Disease
|
|
GYKI 52466 is an orally active, highly selective and noncompetitive AMPA/kainate receptor antagonist with the IC50 values of 7.5 and 11μM, respectively. GYKI 52466 has good blood brain barrier permeability and anticonvulsant effect. GYKI 52466 can be used in Parkinson's disease research.
|
-
- HY-P1091
-
|
Hemopressin (human, mouse)
|
Cannabinoid Receptor
|
Neurological Disease
|
|
Hemopressin is a nonapeptide derived from the α1-chain of hemoglobin, is originally isolated from rat brain homogenates. Hemopressin is orally active, selective and inverse agonist of CB1 cannabinoid receptors. Hemopressin exerts antinociceptive action in inflammatory pain models.
|
-
- HY-N0667S
-
-
- HY-112340
-
|
TM38837
|
Cannabinoid Receptor
|
Metabolic Disease
|
|
TM38837 is a peripheral selective cannabinoid receptor type 1 (CB1) receptor antagonist. TM38837 shows limited penetrance to the brain in order to minimize or prevent CNS adverse reactions, and preserves potential antiobesity effects. TM38837 reduces propensity for psychiatric side effects.
|
-
- HY-103234A
-
|
GYKI 52466 dihydrochloride
|
iGluR
|
Neurological Disease
|
|
GYKI 52466 dihydrochloride is an orally active, highly selective and noncompetitive AMPA/kainate receptor antagonist with the IC50 values of 7.5 and 11μM, respectively. GYKI 52466 dihydrochloride has good blood brain barrier permeability and anticonvulsant effect. GYKI 52466 dihydrochloride can be used in Parkinson's disease research.
|
-
- HY-144301
-
|
AAK1-IN-2
|
AAK1
|
Neurological Disease
|
|
AAK1-IN-2 (compound (S)-31) is a potent, selective and brain-penetrant inhibitor of Adaptor Protein 2-Associated Kinase 1 (AAK1), with an IC50 of 5.8 nM. AAK1-IN-2 can be used for the research of neuropathic pain.
|
-
- HY-103200
-
-
- HY-W083062
-
|
hMAO-B-IN-5
|
Monoamine Oxidase
|
Neurological Disease
|
|
hMAO-B-IN-5(B15) is a potent, selective and reversible inhibitor of human monoamine oxidase hMAO-B with IC50 of 0.12 μM. hMAO-B-IN-5 can pass through the blood-brain barrier and can be used in the research of neurodegenerative diseases.
|
-
- HY-16743B
-
|
Ibiglustat succinate
Venglustat succinate; SAR402671 succinate; GZ402671 succinate
|
Glucosylceramide Synthase (GCS)
|
Neurological Disease
|
|
Ibiglustat (Venglustat) succinate is an orally active, brain-penetrant glucosylceramide synthase (GCS) inhibitor. Ibiglustat succinate can be used for the research of Gaucher disease type 3, Parkinson's disease associated with GBA mutations, Fabry disease, GM2 gangliosidosis, and autosomal dominant polycystic kidney disease.
|
-
- HY-142118
-
|
Trabedersen
AP 12009
|
TGF-beta/Smad
|
Cancer
|
|
Trabedersen (AP 12009) is an antisense oligodeoxynucleotide that specifically inhibits TGF-β2 (TGF-beta/Smad). Trabedersen can be used for the study of malignant brain tumors and other solid tumors overexpressing TGF-β2, such as those of the skin, pancreas and colon.
|
-
- HY-N7062
-
|
JNJ-1661010
Takeda-25
|
FAAH
|
Neurological Disease
|
|
JNJ-1661010 (Takeda-25) a potent and selective fatty acid amide hydrolase (FAAH) inhibitor with IC50s of 34 and 33 nM for rat FAAH and human FAAH, respectively. JNJ-1661010 can cross the blood-brain barrier and used as broad-spectrum analgesics.
|
-
- HY-100672
-
-
- HY-121736
-
-
- HY-17423B
-
|
Abacavir monosulfate
|
HIV
Reverse Transcriptase
Telomerase
Apoptosis
|
Cancer
Infection
|
|
Abacavir monosulfate is a competitive, orally active nucleoside reverse transcriptase inhibitor. Abacavir monosulfate can inhibits the replication of HIV. Abacavir monosulfate shows anticancer activity in prostate cancer cell lines. Abacavir monosulfate can trespass the blood-brain-barrier and suppresses telomerase activity.
|
-
- HY-146049
-
|
Antitrypanosomal agent 4
|
Parasite
|
Infection
|
|
Antitrypanosomal agent 4 (compound 19) is a potent and blood-brain barrier permeable antitrypanosomal agent. Antitrypanosomal agent 4 has good activity against Trypanosoma cruzi (T. cruzi) and Trypanosoma brucei brucei (T. b. brucei) with IC50s of 1.2 μM and 70 nM, respectively.
|
-
- HY-108625
-
|
SHA 68
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
SHA 68 is a potent and selective non-peptide neuropeptide S receptor (NPSR) antagonist with IC50s of 22.0 and 23.8 nM for NPSR Asn 107 and NPSR Ile 107, respectively. SHA 68 has limited the blood-brain barrier (BBB) penetration and the activity in neuralgia.
|
-
- HY-101282
-
|
Glutaminyl Cyclase Inhibitor 3
|
Amyloid-β
|
Neurological Disease
|
|
Glutaminyl Cyclase Inhibitor 3 (compound 212 ), a designed anti-Alzheimer’s compound, is a potent human Glutaminyl Cyclase (GC) inhibitor, with an IC50 of 4.5 nM. Glutaminyl Cyclase-IN-1 (compound 212) significantly reduced the brain concentrations of pyroform Aβ and total Aβ and restored cognitive functions.
|
-
- HY-137472
-
|
SAR502250
|
GSK-3
|
Neurological Disease
|
|
SAR502250 is a potent, selective, ATP competitive, orally active and brain-penetrant inhibitor of GSK3, with an IC50 of 12 nM for human GSK-3β. SAR502250 displays antidepressant-like activity. SAR502250 can be used for the research of Alzheimer’s disease (AD).
|
-
- HY-144610
-
|
Mu opioid receptor antagonist 5
|
Opioid Receptor
|
Neurological Disease
|
|
Mu opioid receptor antagonist 5 (compound NAP) is a selective and blood-brain barrier (BBB) penetrant μ opioid receptor (MOR) antagonist with an EC50 value of 1.14 nM and a Ki value of 0.37 nM. Mu opioid receptor antagonist 5 can be used for researching opioid use disorders (OUD).
|
-
- HY-115475
-
|
SW-100
|
HDAC
|
Neurological Disease
|
|
SW-100, a selective histone deacetylase 6 (HDAC6) inhibitor with an IC50 of 2.3 nM, shows at least 1000-fold selectivity for HDAC6 relative to all other HDAC isozymes. SW-100 displays a significantly improved ability to cross the blood-brain-barrier.
|
-
- HY-W020468
-
|
Linopirdine
DuP 996
|
Potassium Channel
TRP Channel
|
Neurological Disease
|
|
Linopirdine (DuP 996) is an orally active, selective M-type K + current (IM; Kv7; KCNQ Channels) inhibitor with an IC50 of 2.4 μM. Linopirdine is a TRPV1 agonist. Linopirdine, a putative cognition enhancing drug, increases acetylcholine release in rat brain tissue.
|
-
- HY-120110
-
-
- HY-143264
-
|
FAAH/MAGL-IN-2
|
FAAH
MAGL
|
Neurological Disease
|
|
FAAH/MAGL-IN-2 is a potent, reversible, orally active, and cross the blood-brain barrier FAAH and MAGL inhibitor with IC50s of 11 nM and 36 nM (Kis of 28 nM and 60 nM), respectively . FAAH/MAGL-IN-2 has the potential to treat neuropathic pain without causing locomotion impairment.
|
-
- HY-119696S
-
|
MTIC-d3
|
Drug Metabolite
|
Cancer
Neurological Disease
|
|
MTIC-d3 is deuterium labeled MTIC. MTIC is the active metabolite of Temozolomide (TMZ). MITC has lower bioavailability in the brain compared with TMZ, because the drug’s permeability through biological barriers and tumor cell membranes affects bioavailability. MITC exhibits low affinity to biological membrane[1].
|
-
- HY-B1266
-
|
Physostigmine salicylate
Eserine salicylate
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
Physostigmine salicylate (Eserine salicylate) is a reversible acetylcholinesterase (AChE) inhibitor. Physostigmine salicylate crosses the blood-brain barrier and stimulates central cholinergic neurotransmission. Physostigmine salicylate can reverse memory deficits in transgenic mice with Alzheimer's disease. Physostigmine salicylate is also an antidote for anticholinergic poisoning.
|
-
- HY-A0230
-
|
Spirapril
SCH 33844
|
Angiotensin-converting Enzyme (ACE)
|
Cardiovascular Disease
|
|
Spirapril is a potent and cross the blood-brain barrier angiotensin converting enzyme (ACE) inhibitor with antihypertensive activity. Spirapril competitively binds to ACE and prevents the conversion of angiotensin I to angiotensin II. Spirapril is an orally active prodrug of Spiraprilat and can be used for the research of hypertension, congestive heart failure.
|
-
- HY-103415
-
|
Nemonapride
YM-09151-2; Emilace; Emonapride
|
Dopamine Receptor
5-HT Receptor
|
Neurological Disease
|
|
Nemonapride is a highly potent dopamine D2 receptor antagonist with a Ki of 0.06 nM. Nemonapride also activates 5-HT1A receptor with an IC50 of 34 nM. Nemonapride is an antipsychotic that readily passes through the blood brain barrier and exhibits potent neuroleptic effects in animals.
|
-
- HY-114883
-
|
Homocarnosine
L-Homocarnosine; γ-Aminobutyryl-L-histidine
|
GABA Receptor
Endogenous Metabolite
|
Inflammation/Immunology
Neurological Disease
|
|
Homocarnosine is a dipeptide of γ-aminobutyric acid (GABA) and histidine unique to brain. Homocarnosine is an inhibitory neuromodulator synthesized in the neuron from GABA and exhibiting anticonvulsant effects.Homocarnosine has antioxidant and anti-inflammatory actions, prevention of DNA damage, and inhibition of advanced glycation end-product formation.
|
-
- HY-110130
-
|
RN-1 dihydrochloride
|
Histone Demethylase
|
Cancer
Cardiovascular Disease
|
|
RN-1 dihydrochloride is a potent, brain-penetrant, irreversible and selective lysine-specific demethylase 1 (LSD1) inhibitor with an IC50 of 70 nM. RN-1 dihydrochloride exhibits selectivity for LSD1 over MAO-A and MAO-B with IC50 values of 0.51 μM and 2.785 μM respectively.
|
-
- HY-104044
-
|
Pamiparib
BGB-290
|
PARP
|
Cancer
|
|
Pamiparib (BGB-290) is an orally active, potent, highly selective PARP inhibitor, with IC50 values of 0.9 nM and 0.5 nM for PARP1 and PARP2, respectively. Pamiparib has potent PARP trapping, and capability to penetrate the brain, and can be used for the research of various cancers including the solid tumor.
|
-
- HY-P3155
-
|
Ac-hMCH(6-16)-NH2
|
MCHR1 (GPR24)
|
Metabolic Disease
|
|
Ac-hMCH(6-16)-NH2 binds to and activates equally well both human MCH receptors present in the brain (non-selective agonist), with IC50 values of 0.16 nM and 2.7 nM for MCH-1R and MCH-2R.
|
-
- HY-118256
-
|
LSN2814617
|
mGluR
|
Neurological Disease
|
|
LSN2814617 is an orally active, potent, brain-penetrant, and selective mGlu5 (metabotropic glutamate 5) positive allosteric modulator (PAM), with EC50 values of 52 nM (Human mGlu5) and 42 nM (rat mGlu5). LSN2814617 shows wake-promoting effect. LSN2814617 can be used for schizophrenia research.
|
-
- HY-121883S4
-
|
Lignoceric acid-d4-2
Tetracosanoic acid-d4-2
|
Endogenous Metabolite
|
|
|
Lignoceric acid-d4-2 is the deuterium labeled Lignoceric acid. Lignoceric acid (Tetracosanoic acid) is a 24-carbon saturated (24:0) fatty acid, which is synthesized in the developing brain. Lignoceric acid is also a by-product of lignin production. Lignoceric acid can be used for Zellweger cerebro‐hepato‐renal syndrome and adrenoleukodystrophy research[1][2].
|
-
- HY-P1136B
-
-
- HY-100642S
-
|
3-O-Methyltolcapone-d7
Ro 40-7591 d7
|
COMT
|
Neurological Disease
|
|
3-O-Methyltolcapone-d7 is a deuterium labeled 3-O-Methyltolcapone. 3-O-Methyltolcapone is a metabolite of Tolcapone. Tolcapone is an orally active, reversible, selective and potent COMT inhibitor. Tolcapone crosses the blood-brain barrier, and can be used for treatment of Parkinson's disease[1][2].
|
-
- HY-16743A
-
|
Ibiglustat (L-Malic acid)
Venglustat (L-Malic acid); SAR402671 (L-Malic acid); GZ402671 (L-Malic acid)
|
Glucosylceramide Synthase (GCS)
|
Metabolic Disease
|
|
Ibiglustat (Venglustat) L-Malic acid is an orally active, brain-penetrant glucosylceramide synthase (GCS) inhibitor. Ibiglustat L-Malic acid can be used for the research of Gaucher disease type 3, Parkinson's disease associated with GBA mutations, Fabry disease, GM2 gangliosidosis, and autosomal dominant polycystic kidney disease.
|
-
- HY-147953
-
|
MAO-B-IN-13
|
Monoamine Oxidase
|
Neurological Disease
|
|
MAO-B-IN-13 (compound 12a) is a highly potent, reversible and blood-brain barrier (BBB) penetrant MAO-B inhibitor with an IC50 value of 10 nM. MAO-B-IN-13 has neuroprotective and antioxidant activity. MAO-B-IN-13 can be used for researching Parkinson’s disease.
|
-
- HY-134990
-
|
Hematoporphyrin monomethyl ether
|
Apoptosis
|
Cancer
|
|
Hematoporphyrin monomethyl ether, second generation of porphyrin-related photosensitizer, is characterized by its single form, high yield of singlet oxygen, high selectivity, and low toxicity, which has been widely used in the diagnosis and treatment of various tumors, including lung cancer, bladder cancer, and nevus flammeus and brain glioma.
|
-
- HY-144301A
-
|
AAK1-IN-2 TFA
|
AAK1
|
Neurological Disease
|
|
AAK1-IN-2 TFA (compound (S)-31) is a potent, selective and brain-penetrant inhibitor of Adaptor Protein 2-Associated Kinase 1 (AAK1), with an IC50 of 5.8 nM. AAK1-IN-2 TFA can be used for the research of neuropathic pain.
|
-
- HY-151808
-
|
JS25
|
Btk
|
Cancer
|
|
JS25 is a selective and covalent inhibitor of BTK that inactivates BTK with an IC50 value of 5.8 nM by chelating Tyr551. JS25 inhibits cancer cells proliferation, pronounces cell death, and promotes murine xenograft model of Burkitt’s lymphoma. JS25 effectively crosses the blood-brain barrier.
|
-
- HY-101176
-
|
2-Iodomelatonin
|
Melatonin Receptor
|
Cancer
|
|
2-Iodomelatonin is a potent agonist of melatonin receptor 1 (MT1) with a Ki value of 28 pM, it is more 5-fold selective for MT1 over MT2. 2-iodomelatonin can be used to identify, characterize and localize melatonin binding sites in the brain and peripheral tissues.
|
-
- HY-12567
-
|
ML375
VU0483253
|
mAChR
|
Neurological Disease
|
|
ML375 (VU0483253) is a potent, highly selective, brain-penetrant and orally active M5 mAChR negative allosteric modulator (NAM) with IC50s of 300 nM and 790 nM for human and rat M5, respectively. ML375 is inactive at human and rat M1-M4.
|
-
- HY-128865
-
|
BPR1M97
|
Opioid Receptor
|
Neurological Disease
|
|
BPR1M97 is a dual-acting mu opioid receptor (MOP) and nociceptin-orphanin FQ peptide (NOP) receptor agonist with Ki values of 1.8 and 4.2 nM, respectively. BPR1M97 shows high potency and blood-brain barrier penetration, and produces potent antinociceptive effects.
|
-
- HY-13458S1
-
|
Droxidopa-13C2,15N hydrochloride
L-DOPS-13C2,15N (hydrochloride); DOPS-13C2,15N (hydrochloride); SM5688-13C2,15N (hydrochloride)
|
Isotope-Labeled Compounds
Adrenergic Receptor
|
Neurological Disease
|
|
Droxidopa- 13C2, 15N (hydrochloride) is deuterium labeled Droxidopa. Droxidopa(L-DOPS), the mixture of Droxidopa (w/w80%) and Pharmaceutical starch (w/w20%), acts as a prodrug to the neurotransmitters norepinephrine (noradrenaline) and epinephrine (adrenaline); Droxidopa(L-DOPS) is capable of crossing the protective blood–brain barrier[1][2].
|
-
- HY-151195
-
|
20S Proteasome-IN-4
|
Proteasome
Parasite
|
Infection
|
|
20S Proteasome-IN-4 (Compound 7) is a brain-penetrant, parasite-selective, orally active 20S proteasome inhibitor with an IC50 of 6.3 nM against T. b. brucei 20S proteasome. 20S Proteasome-IN-4 can be used for the research of human African trypanosomiasis (HAT).
|
-
- HY-121883S
-
|
Lignoceric acid-d47
Tetracosanoic acid-d47
|
Endogenous Metabolite
|
Neurological Disease
|
|
Lignoceric acid-d47 is the deuterium labeled Lignoceric acid. Lignoceric acid (Tetracosanoic acid) is a 24-carbon saturated (24:0) fatty acid, which is synthesized in the developing brain. Lignoceric acid is also a by-product of lignin production. Lignoceric acid can be used for Zellweger cerebro‐hepato‐renal syndrome and adrenoleukodystrophy research[1][2].
|
-
- HY-114320
-
|
BuChE-IN-TM-10
TM-10
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
BuChE-IN-TM-10 (TM-10) is a potent butyrylcholinesterase (BuChE) inhibitor, with an IC50 of 8.9 nM. BuChE inhibitor 1 inhibits and disaggregates self-induced Aβ aggregation, exhibiting potent antioxidant activity and good blood-brain barrier (BBB) penetration. Has potential to treat Alzheimer’s disease.
|
-
- HY-10864
-
|
URB-597
KDS-4103
|
FAAH
Autophagy
Mitophagy
|
Neurological Disease
|
|
URB-597 (KDS-4103) is an orally bioavailable and selective FAAH inhibitor. URB-597 inhibits FAAH activity with an IC50s of approximately 5 nM in rat brain membranes, 0.5 nM in intact rat neurons, 3 nM in human liver microsomes. Antidepressant-like effects. Analgesic activity.
|
-
- HY-P1090
-
|
Hemopressin(rat)
|
Cannabinoid Receptor
|
Neurological Disease
|
|
Hemopressin(rat) is a nonapeptide derived from the α1-chain of hemoglobin, is originally isolated from rat brain homogenates. Hemopressin(rat) is orally active, selective and inverse agonist of CB1 cannabinoid receptors. Hemopressin(rat) exerts antinociceptive action in inflammatory pain models.
|
-
- HY-127106
-
|
VU0810464
|
Potassium Channel
|
Neurological Disease
|
|
VU0810464 is a potent and selective non-ureaG protein-gated inwardly-rectifying potassium channels (GIRK, Kir3) activator. VU0810464 displays nanomolar potency for neuronal (EC50=165 nM) and GIRK1/4 (EC50=720 nM) channels with improved brain penetration.
|
-
- HY-101402
-
|
Cyclo(his-pro)
Cyclo(histidyl-proline); Histidylproline diketopiperazine
|
NF-κB
Endogenous Metabolite
|
Inflammation/Immunology
Neurological Disease
|
|
Cyclo(his-pro) (Cyclo(histidyl-proline)) is an orally active cyclic dipeptide structurally related to tyreotropin-releasing hormone. Cyclo(his-pro) could inhibit NF-κB nuclear accumulation. Cyclo(his-pro) can cross the brain-blood-barrier and affect diverse inflammatory and stress responses.
|
-
- HY-P1091A
-
|
Hemopressin(human, mouse) TFA
|
Cannabinoid Receptor
|
Neurological Disease
|
|
Hemopressin TFA is a nonapeptide derived from the α1-chain of hemoglobin, is originally isolated from rat brain homogenates. Hemopressin TFA is orally active, selective and inverse agonist of CB1 cannabinoid receptors. Hemopressin TFA exerts antinociceptive action in inflammatory pain models.
|
-
- HY-107365
-
|
PQR530
|
PI3K
mTOR
|
Cancer
|
|
PQR530 is a potent, ATP-competitive, orally bioavailable and brain-penetrant dual pan-PI3K/mTORC1/2 inhibitor, with a subnanomolar Kd toward PI3Kα and mTOR (0.84 and 0.33 nM, respectively). Antitumor activity.
|
-
- HY-N0745
-
|
Senkyunolide I
|
Caspase
|
Inflammation/Immunology
|
|
Senkyunolide I, isolated from Ligusticum chuanxiong Hort, is an anti-migraine compound. Senkyunolide I protects rat brain against focal cerebral ischemia-reperfusion injury by up-regulating p-Erk1/2, Nrf2/HO-1 and inhibiting caspase 3.
|
-
- HY-119033
-
|
MGL-IN-1
|
MAGL
|
Inflammation/Immunology
|
|
MGL-IN-1 is a potent and selective irreversible MGL (β-lactam-based monoacylglycerol lipase) inhibitor. MGL-IN-1 alleviates symptoms in a MS model in vivo and exhibits analgesic effects in an acute inflammatory pain model in vivo. MGL-IN-1 displays high membrane permeability and brain penetrant.
|
-
- HY-132280
-
|
Tirilazad
U 74006F free base
|
Antibiotic
|
Infection
Neurological Disease
|
|
Tirilazad is a nonglucocorticoid, 21-aminosteroid that inhibits lipid peroxidation. Tirilazad can attenuate brain or spinal cord injury caused by trauma, stroke, ischemia and reperfusion injury. Tirilazad has antiviral activities against nCoV. Tirilazad is neuroprotective for ischaemic stroke, can be used for subarachnoid hemorrhage research.
|
-
- HY-76772
-
|
Cevimeline hydrochloride hemihydrate
SNI-2011; AF102B hydrochloride hemihydrate
|
mAChR
|
Neurological Disease
Cancer
|
|
Cevimeline hydrochloride hemihydrate (SNI-2011) is a quinuclidine derivative of acetylcholine and a selective and orally active muscarinic M1 and M3 receptor agonist. Cevimeline hydrochloride hemihydrate stimulates secretion by the salivary glands and can be used as a sialogogue for xerostomia. Cevimeline hydrochloride hemihydrate can cross the blood-brain barrier (BBB).
|
-
- HY-120170
-
-
- HY-10847
-
-
- HY-A0168
-
|
Regadenoson
CVT-3146
|
Adenosine Receptor
|
Cardiovascular Disease
|
|
Regadenoson (CVT-3146) is a selective A2A adenosine receptor agonist and vasodilator that increases coronary blood flow, can be used in study of myocardial perfusion imaging. Regadenoson also increases the permeability of the blood-brain barrier (BBB) in rodents, can be used to study increased delivery of drugs to the human CNS.
|
-
- HY-131971
-
|
AChE/BChE-IN-1
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
AChE/BChE-IN-1 is a potent and brain-penetrant dual inhibitor of Acetylcholinesterase and Butyrylcholinesterase, with IC50s of 1.06 and 7.3 nM for hAChE and hBChE, respectively. AChE/BChE-IN-1 also has antioxidant activity. AChE/BChE-IN-1 can be used for the research of Alzheimer’s disease.
|
-
- HY-121883SS5
-
|
Lignoceric acid-d9
|
Endogenous Metabolite
|
|
|
Lignoceric acid-d9 is the deuterium labeled Lignoceric acid. Lignoceric acid (Tetracosanoic acid) is a 24-carbon saturated (24:0) fatty acid, which is synthesized in the developing brain. Lignoceric acid is also a by-product of lignin production. Lignoceric acid can be used for Zellweger cerebro‐hepato‐renal syndrome and adrenoleukodystrophy research[1][2].
|
-
- HY-15010
-
|
L-371,257
|
Oxytocin Receptor
Vasopressin Receptor
|
Endocrinology
|
|
L-371,257 is an orally bioavailable, non-blood-brain barrier penetrant, selective and competitive antagonist of oxytocin receptor (pA2=8.4) with high affinity at both the oxytocin receptor (Ki=19 nM) and vasopressin V1a receptor (Ki=3.7 nM).
|
-
- HY-17363
-
-
- HY-105692
-
|
DR2313
|
PARP
|
Neurological Disease
|
|
DR2313 is a potent, selective, competitive and brain-penetrant inhibitor of poly(ADP-ribose) polymerase (PARP), with IC50s of 0.20 μM and 0.24 μM for PARP-1 and PARP-2, respectively. DR2313 exhibits neuroprotective effects on ischemic injuries in vitro and in vivo.
|
-
- HY-N2320
-
|
Physostigmine hemisulfate
Eserine hemisulfate
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
Physostigmine hemisulfate (Eserine hemisulfate) is a reversible acetylcholinesterase (AChE) inhibitor. Physostigmine hemisulfate can crosses the blood-brain barrier and stimulates central cholinergic neurotransmission. Physostigmine hemisulfate can reverse memory deficits in transgenic mice with Alzheimer's disease. Physostigmine hemisulfate is also an antidote for anticholinergic poisoning.
|
-
- HY-121883S3
-
|
Lignoceric acid-d4-1
|
Endogenous Metabolite
|
Neurological Disease
|
|
Lignoceric acid-d4-11 is the deuterium labeled Lignoceric acid. Lignoceric acid (Tetracosanoic acid) is a 24-carbon saturated (24:0) fatty acid, which is synthesized in the developing brain. Lignoceric acid is also a by-product of lignin production. Lignoceric acid can be used for Zellweger cerebro‐hepato‐renal syndrome and adrenoleukodystrophy research[1][2].
|
-
- HY-134494
-
|
MS48107
|
GPR68
|
Neurological Disease
|
|
MS48107 is a potent and selective positive allosteric modulator of G protein-coupled receptor 68 (GPR68). MS48107 is selective for GPR68 over the closely related proton GPCRs, neurotransmitter transporters, and hERG ion channels. MS48107 can readily cross the blood-brain barrier (BBB) in mice.
|
-
- HY-119226
-
|
VU0152099
|
mAChR
|
Neurological Disease
|
|
VU0152099 is a potent, selective and brain-penetrant mAChR M4 positive allosteric modulator with an EC50 of 0.4 µM for rat M4 receptor. VU0152099 is inactive for other mAChR subtypes or other GPCRs. VU0152099 has no agonist activity but potentiated responses of M4 to acetylcholine.
|
-
- HY-P2911
-
|
Glutamate dehydrogenase (NAD(P))
GLDH
|
Mitochondrial Metabolism
|
Others
|
|
Glutamate dehydrogenase NAD(P) (GLDH) can be found in hepatocytes, renal tissue, brain, muscle, and intestinal cells. Glutamate dehydrogenase NAD(P) is often used in biochemical studies. Glutamate dehydrogenase is a mitochondrial enzyme, it catalyzes the reversible oxidative deamination of glutamate to α-ketoglutarate (α-KG) as part of the urea cycle.
|
-
- HY-100125
-
|
Timegadine
SR1368
|
COX
|
Inflammation/Immunology
|
|
Timegadine, a new antiinflammatory agent, is found to be a potent, competitive inhibitor of cyclo-oxygenase (COX) and lipo-oxygenase, with IC50s ranging from 5 nM (washed rabbit platelets) to 20 μM (rat brain) for COX and 100 μM for lipo-oxygenase both in the cytosol fraction of horse platelet homogenates, and in washed rabbit platelets.
|
-
- HY-150050
-
|
gamma-secretase modulator 5
|
Amyloid-β
|
Neurological Disease
|
|
gamma-secretase modulator 5 (compound 22d) is a brain-penetrant gamma-secretase modulator (GSMs) that inhibits the production of the aggregated amyloid β-peptide Aβ42 with an IC50 value of 60 nM. gamma-secretase modulator 5 can be used in the study of Alzheimer's disease.
|
-
- HY-120717
-
|
VU6001966
|
mGluR
|
Others
|
|
VU6001966 (compound 15m) is a potent and cross the blood-brain barrier mGlu2 (metabotropic glutamate receptor 2) negative allosteric modulator with IC50s of 78 nM and >30 µM for mGlu2 and mGlu3, respectively. VU6001966 can serve as an mGlu2 PET tracer.
|
-
- HY-15615A
-
|
TIC10
ONC-201
|
TNF Receptor
Apoptosis
|
Cancer
|
|
TIC10 (ONC-201) is a potent, orally active, and stable tumor necrosis factor-related apoptosis-inducing ligand (TRAIL) inducer which acts by inhibiting Akt and ERK, consequently activating Foxo3a and significantly inducing cell surface TRAIL. TIC10 can cross the blood-brain barrier.
|
-
- HY-70020B
-
|
Cevimeline hydrochloride
AF102B hydrochloride
|
mAChR
|
Neurological Disease
|
|
Cevimeline hydrochloride (AF102B hydrochloride) is a quinuclidine derivative of acetylcholine and a selective and orally active muscarinic M1 and M3 receptor agonist. Cevimeline hydrochloride stimulates secretion by the salivary glands and can be used as a sialogogue for xerostomia. Cevimeline hydrochloride can cross the blood-brain barrier (BBB).
|
-
- HY-147684
-
|
FGFR-IN-7
|
FGFR
|
Neurological Disease
|
|
FGFR-IN-7 (compound 17) is an orally active, potent and BBB-penetrated FGFR (fibroblast growth factor receptor) modulator. FGFR-IN-7 shows neuroprotective activity. FGFR-IN-7 improves brain exposure and reduced risk of phospholidosis. FGFR-IN-7 can be used for neurodegenerative diseases research.
|
-
- HY-10835
-
|
DG-041
|
Prostaglandin Receptor
|
Cardiovascular Disease
|
|
DG-041 is a potent, high affinity and selective EP3 receptor antagonist with IC50s of 4.6 nM and 8.1 nM in the binding and FLIPR assay, respectively. DG-041 inhibits PGE2 facilitation of platelet aggregation. DG-041 crosses the blood-brain barrier.
|
-
- HY-17423A
-
|
Abacavir sulfate
Abacavir Hemisulfate; ABC sulfate
|
Reverse Transcriptase
HIV
Telomerase
Apoptosis
|
Infection
|
|
Abacavir sulfate (Abacavir Hemisulfate) is a competitive, orally active nucleoside reverse transcriptase inhibitor. Abacavir sulfate can inhibits the replication of HIV. Abacavir sulfate shows anticancer activity in prostate cancer cell lines. Abacavir sulfate can trespass the blood-brain-barrier and suppresses telomerase activity.
|
-
- HY-N6608S
-
|
Physostigmine-d3
Eserine-d3
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
Physostigmine-d3 is the deuterium labeled Physostigmine. Physostigmine (Eserine) is a reversible acetylcholinesterase (AChE) inhibitor. Physostigmine can crosses the blood-brain barrier and stimulates central cholinergic neurotransmission. Physostigmine can reverse memory deficits in transgenic mice with Alzheimer's disease. Physostigmine is also an antidote for anticholinergic poisoning[1][2][3][4].
|
-
- HY-121883S1
-
|
Lignoceric acid-d3
Tetracosanoic acid-d3
|
Endogenous Metabolite
|
Neurological Disease
|
|
Lignoceric acid-d3 is the deuterium labeled Lignoceric acid[1]. Lignoceric acid (Tetracosanoic acid) is a 24-carbon saturated (24:0) fatty acid, which is synthesized in the developing brain. Lignoceric acid is also a by-product of lignin production. Lignoceric acid can be used for Zellweger cerebro‐hepato‐renal syndrome and adrenoleukodystrophy research[2][3].
|
-
- HY-12305
-
|
Q-VD-OPh
QVD-OPH; Quinoline-Val-Asp-Difluorophenoxymethylketone
|
Caspase
HIV
|
Cancer
Infection
|
|
Q-VD-OPh is an irreversible pan-caspase inhibitor with potent antiapoptotic properties; inhibits caspase 7 with an IC50 of 48 nM and 25-400 nM for other caspases including caspase 1, 3, 8, 9, 10, and 12. Q-VD-OPh can inhibits HIV infection. Q-VD-OPh is able to cross the blood-brain barrier.
|
-
- HY-16531A
-
|
YF-2 hydrochloride
|
Histone Acetyltransferase
|
Cancer
Neurological Disease
|
|
YF-2 hydrochloride is a highly selective, blood-brain-barrier permeable histone acetyltransferase activator, acetylates H3 in the hippocampus, with EC50s of 2.75 μM, 29.04 μM and 49.31 μM for CBP, PCAF, and GCN5, respectively, shows no effect on HDAC. Anti-cancer and anti-Alzheimer's disease.
|
-
- HY-107623
-
|
TC-MCH 7c
|
MCHR1 (GPR24)
|
Metabolic Disease
|
|
TC-MCH 7c, a phenylpyridone derivative, is an orally available, selective and brain-penetrable MCH1R antagonist with an IC50 of 5.6 nM for hMCH1R. TC-MCH 7c has Kis of 3.4 nM and 3.0 nM of human and mouse MCH1R, respectively.
|
-
- HY-B1334
-
|
Perhexiline
|
Mitochondrial Metabolism
Apoptosis
|
Cancer
Cardiovascular Disease
|
|
Perhexiline is an orally active CPT1 and CPT2 inhibitor that reduces fatty acid metabolism. Perhexiline induces mitochondrial dysfunction and apoptosis in hepatic cells. Perhexiline can cross the blood brain barrier (BBB) and shows anti-tumor activity. Perhexiline can be used in the research of cancers, and cardiovascular disease like angina.
|
-
- HY-106301
-
|
Devazepide
L-364,718; MK-329
|
Cholecystokinin Receptor
|
Metabolic Disease
|
|
Devazepide (L-364,718) is a potent, competitive, selective and orally active nonpeptide antagonist of cholecystokinin (CCK) receptor, with IC50s of 81 pM, 45 pM and 245 nM for rat pancreatic, bovine gallbladder and guinea pig brain CCK receptors, respectively. Devazepide (L-364,718) is effective for gastrointestinal disorders.
|
-
- HY-146762
-
-
- HY-10399
-
|
Ladostigil
TV-3326
|
Monoamine Oxidase
Cholinesterase (ChE)
|
Neurological Disease
|
|
Ladostigil (TV-3326) is an orally active dual inhibitor of cholinesterase and brain-selective monoamine oxidase (MAO), with IC50s of 37.1 and 31.8 μM for MAO-B and AChE, respectively. Ladostigil exhibits neuroprotective, antioxidant and anti-inflammatory activities. Ladostigil can be used for the research of depression and Alzheimer's disease.
|
-
- HY-B1334A
-
|
Perhexiline maleate
|
Mitochondrial Metabolism
Apoptosis
|
Cancer
Cardiovascular Disease
|
|
Perhexiline maleate is an orally active CPT1 and CPT2 inhibitor that reduces fatty acid metabolism. Perhexiline maleate induces mitochondrial dysfunction and apoptosis in hepatic cells. Perhexiline maleate can cross the blood brain barrier (BBB) and shows anti-tumor activity. Perhexiline maleate can be used in the research of cancers, and cardiovascular disease like angina.
|
-
- HY-10399A
-
|
Ladostigil hydrochloride
TV-3326 hydrochloride
|
Monoamine Oxidase
Cholinesterase (ChE)
|
Neurological Disease
|
|
Ladostigil (TV-3326) hydrochloride is an orally active dual inhibitor of cholinesterase and brain-selective monoamine oxidase (MAO), with IC50s of 37.1 and 31.8 μM for MAO-B and AChE, respectively. Ladostigil hydrochloride exhibits neuroprotective, antioxidant and anti-inflammatory activities. Ladostigil can be used for the research of depression and Alzheimer's disease.
|
-
- HY-13662BS
-
|
(R)-Lansoprazole-d4
Dexlansoprazole-d4
|
Proton Pump
|
Inflammation/Immunology
|
|
(R)-Lansoprazole-d4 is deuterium labeled (R)-Lansoprazole. (R)-Lansoprazole is the R enantiomer of Lansoprazole, Lansoprazole (AG 1749) is an orally active proton pump inhibitor which prevents the stomach from producing acid. Lansoprazole (AG 1749) is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor)[1][2].
|
-
- HY-N6745
-
|
Citreoviridin
|
Na+/K+ ATPase
Apoptosis
|
Infection
Cardiovascular Disease
|
|
Citreoviridin, a toxin from Penicillium citreoviride NRRL 2579, inhibits brain synaptosomal Na +/K +-ATPase whereas in microsomes, both Na +/K +-ATPase and Mg 2+-ATPase activities are significantly stimulated in a dose-dependent manner. Citreoviridin inhibits cell proliferation and enhances apoptosis of human umbilical vein endothelial cells.
|
-
- HY-120789
-
|
PF-06648671
|
γ-secretase
|
Neurological Disease
|
|
PF-06648671 is a novel, brain-penetrable, and orally active γ-secretase modulator (GSM). PF-06648671 reduces Aβ42 and Aβ40, with concomitant increases in Aβ37 and Aβ38 in vitro. PF-06648671 is used for the study of Alzheimer’s disease.
|
-
- HY-U00322
-
-
- HY-112226
-
|
VRT-043198
|
Caspase
Drug Metabolite
|
Inflammation/Immunology
|
|
VRT-043198, the drug metabolite of VX-765 (Belnacasan), is a potent, selective and blood-brain barrier permeable inhibitor of interleukin-converting enzyme/caspase-1 subfamily caspases. VRT-043198 exhibits Ki values of 0.8 nM and 0.6 nM for ICE/caspase-1 and caspase-4, respectively.
|
-
- HY-136731
-
|
APE1-IN-1
|
DNA/RNA Synthesis
|
Cancer
|
|
APE1-IN-1 is a potent and blood-brain barrier (BBB) penetrant apurinic/apyrimidinic (AP) endonuclease 1 (APE1) inhibitor with an IC50 value of 2 μM. APE1-IN-1 can potentiate the cytotoxicity of the alkylating agents Methylmethane sulfonate and Temozolomide (HY-17364) to cancer cells.
|
-
- HY-16531
-
|
YF-2
|
Histone Acetyltransferase
|
Cancer
Neurological Disease
|
|
YF-2 is a highly selective, blood-brain-barrier permeable histone acetyltransferase activator, acetylates H3 in the hippocampus, with EC50s of 2.75 μM, 29.04 μM and 49.31 μM for CBP, PCAF, and GCN5, respectively, shows no effect on HDAC. Anti-cancer and anti-Alzheimer's disease.
|
-
- HY-100501
-
|
M2698
MSC2363318A
|
Ribosomal S6 Kinase (RSK)
Akt
|
Cancer
|
|
M2698 (MSC2363318A) is an orally active, ATP competitive, selective p70S6K and Akt dual-inhibitor with IC50s of 1 nM for p70S6K, Akt1 and Akt3. M2698 can cross the blood-brain barrier and has anti-cancer activity.
|
-
- HY-19838
-
|
JNJ-63533054
|
GPR139
|
Neurological Disease
|
|
JNJ-63533054 is a potent, selective and orally active GPR139 agonist with an EC50 of 16 nM for human GPR139 (hGPR139). JNJ-63533054 shows selective for GPR139 over other GPCRs, ion channels, and transporters. JNJ-63533054 can cross the blood-brain barrier (BBB).
|
-
- HY-103493
-
|
TAK-915
|
Phosphodiesterase (PDE)
|
Neurological Disease
|
|
TAK-915 is a potent, selective, brain-penetrant and orally active phosphodiesterase 2A (PDE2A) inhibitor with an IC50 of 0.61 nM. TAK-915 is >4100-fold more selectivity for PDE2A than PDE1A. TAK-915 has the potential for neuropsychiatric and neurodegenerative disorders treatment.
|
-
- HY-18078
-
|
PQ-10
|
Phosphodiesterase (PDE)
|
Neurological Disease
|
|
PQ-10 is a potent inhibitor of Phosphodiesterase 10A (PDE10A) with IC50 andED50 of 4.6 nM and 13 mg/kg, respectively. PQ-10 induces patterns of brain glucose metabolism which can be a potential translational biomarker. PQ-10 has the potential for researching psychiatric disorders like schizophrenia.
|
-
- HY-112037
-
|
IACS-010759
IACS-10759
|
Mitochondrial Metabolism
Apoptosis
|
Cancer
|
|
IACS-010759 is an orally active, potent mitochondrial complex I of oxidative phosphorylation (OXPHOS) inhibitor. IACS-010759 inhibits proliferation and induces apoptosis in models of brain cancer and acute myeloid leukemia (AML) reliant on OXPHOS. IACS-010759 has the potential for relapsed/refractory AML and solid tumors research.
|
-
- HY-12215
-
|
Lorlatinib
PF-06463922
|
Anaplastic lymphoma kinase (ALK)
ROS Kinase
Apoptosis
|
Cancer
|
|
Lorlatinib (PF-06463922) is a selective, orally active, brain-penetrant and ATP-competitive ROS1/ALK inhibitor. Lorlatinib has Kis of <0.025 nM, <0.07 nM, and 0.7 nM for ROS1, wild type ALK, and ALK L1196M, respectively. Lorlatinib has anticancer activity.
|
-
- HY-B0309S1
-
|
Felodipine-d5
|
Calcium Channel
Autophagy
|
Cardiovascular Disease
|
|
Felodipine-d5 is deuterium labeled Felodipine. Felodipine, a dihydropyridine, is a potent, vasoselective calcium channel antagonist. Felodipine lowers blood pressure (BP) by selective action on vascular smooth muscle, especially in the resistance vessels. Felodipine, an anti-hypertensive agent, induces autophagy. Felodipine can cross the blood-brain barrier[1][2][3].
|
-
- HY-P1256C
-
|
JMV 449 acetate
|
Neurotensin Receptor
|
Neurological Disease
|
|
JMV 449 acetate is a potent neurotensin receptor agonist. JMV 449 acetate shows an IC50 of 0.15 nM for inhibition of 125I-neurotensin binding to neonatal mouse brain and an EC50 of 1.9 nM in contracting the guinea-pig ileum. JMV 449 acetate has highly potent and long-lasting hypothermic and analgesic effects in the mouse.
|
-
- HY-101884
-
|
Biocytin
(+)-Biocytin
|
Endogenous Metabolite
|
Neurological Disease
|
|
Biocytin is a conjugate of D-biotin and L-lysine, where the carboxylate of D-biotin is coupled with the ϵ-amine of L-lysine via a secondary amide bond. Biocytin is a classical neuroanatomical tracer commonly used to map brain connectivity. Biocytin is used as a versatile marker in anterograde, retrograde and intracellular neuroanatomical investigations and in biotinidase assays.
|
-
- HY-120574
-
|
TH1338
|
Others
|
Cancer
|
|
TH1338 (compound 3b), an orally active camptothecin derivative and a potent chemotherapeutic agent for cancer, demonstrates excellent cytotoxic potency against human tumor cell lines in vitro. TH1338 (compound 3b) possesses significant brain penetration, favorable efflux pump properties, and hematological toxicity profile.
|
-
- HY-145761
-
|
AMPA-IN-1
|
iGluR
|
Neurological Disease
|
|
AMPA-IN-1 is a potent inhibitor of AMPA receptor. AMPA receptors are receptors that are widely expressed in the brain, and play a central role in the regulation of fast excitatory synaptic transmission and synaptic plasticity. AMPA-IN-1 has the potential for the research of various central diseases including epilepsy (extracted from patent WO2017082288A1, compound 14).
|
-
- HY-17552
-
|
sn-Glycero-3-phosphocholine
Choline Alfoscerate; Alpha-GPC; L-α-GPC
|
Cholinesterase (ChE)
Endogenous Metabolite
|
Neurological Disease
|
|
sn-Glycero-3-phosphocholine (Choline Alfoscerate) is a precursor in the biosynthesis of brain phospholipids and increases the bioavailability of choline in nervous tissue. sn-Glycero-3-phosphocholine (Choline Alfoscerate) has significant effects on cognitive function with a good safety profile and tolerability, and is effective in the treatment of Alzheimer's disease and dementia.
|
-
- HY-101795
-
|
Larixyl acetate
|
TRP Channel
HPV
|
Infection
Neurological Disease
|
|
Larixyl acetate is a potent and selective TRPC6 inhibitor with IC50 values of 0.58 μM and 6.83 μM against hTRPC6-YFP and hTRPC3-YFP, respectively. Larixyl acetate prevents HPV and is effective in protecting against traumatic brain injury-induced systemic endothelial dysfunction.
|
-
- HY-14602S
-
|
Tramiprosate-d6
Homotaurine-d6; 3-Amino-1-propanesulfonic acid-d6
|
Amyloid-β
|
Cancer
|
|
Tramiprosate-d6 is the deuterium labeled Tramiprosate. Tramiprosate (Homotaurine), an orally active and brain-penetrant natural amino acid found in various species of red marine algae. Tramiprosate binds to soluble Aβ and maintains Aβ in a non-fibrillar form. Tramiprosate is also a GABA analog and possess neuroprotection, anticonvulsion and antihypertension effects[1][2][3].
|
-
- HY-P1178
-
|
Cyclotraxin B
|
Trk Receptor
|
Neurological Disease
|
|
Cyclotraxin B, a cyclic peptide, is a highly potent and selective TrkB inhibitor without altering the binding of BDNF. Cyclotraxin B non-competitively inhibits BDNF-induced TrkB activity with an IC50 of 0.30 nM. Cyclotraxin B can crosse the blood-brain-barrier and has analgesic and anxiolytic-like behavioral effects.
|
-
- HY-B0309S2
-
|
Felodipine-d3
|
Calcium Channel
Autophagy
|
Cardiovascular Disease
|
|
Felodipine-d3 is the deuterium labeled Felodipine. Felodipine, a dihydropyridine, is a potent, vasoselective calcium channel antagonist. Felodipine lowers blood pressure (BP) by selective action on vascular smooth muscle, especially in the resistance vessels. Felodipine, an anti-hypertensive agent, induces autophagy. Felodipine can cross the blood-brain barrier[1][2][3].
|
-
- HY-13289A
-
|
Nepicastat hydrochloride
SYN-117 hydrochloride; RS-25560-197 hydrochloride
|
Dopamine β-hydroxylase
|
Cardiovascular Disease
|
|
Nepicastat hydrochloride (SYN-117 hydrochloride) is a selective, potent, and orally active inhibitor of dopamine-beta-hydroxylase. Nepicastat hydrochloride produces concentration-dependent inhibition of bovine (IC50=8.5 nM) and human (IC50=9 nM) dopamine-beta-hydroxylase. Nepicastat hydrochloride can cross the blood-brain barrier (BBB).
|
-
- HY-134004
-
|
Pentoxyverine
Carbetapentane
|
Sigma Receptor
|
Neurological Disease
|
|
Pentoxyverine (Carbetapentane) is a sigma-1 receptor agonist, with a Ki of 75 nM on guinea-pig brain membranes. Pentoxyverine is a centrally-acting cough suppressant with antimuscarinic and anticonvulsant properties. Pentoxyverine can be used for inhibiting bronchial interceptor, weakening of cough reflex, bronchial smooth muscle relaxation and reduction of airway resistance.
|
-
- HY-100642S1
-
|
3-O-Methyltolcapone-d4
Ro 40-7591-d4
|
COMT
|
Neurological Disease
|
|
3-O-Methyltolcapone-d4 is the deuterium labeled 3-O-Methyltolcapone. 3-O-Methyltolcapone (Ro 40-7591) is a metabolite of Tolcapone. Tolcapone is an orally active, reversible, selective and potent COMT inhibitor. Tolcapone crosses the blood-brain barrier, and can be used for treatment of Parkinson's disease[1][2].
|
-
- HY-N3940
-
|
Gelsevirine
|
Others
|
Cancer
Neurological Disease
|
|
Gelsevirine is the major alkaloid in Gelsemium elegans with potent anxiolytic effects. The anxiolytic mechanism of Gelsevirine may be involved in the agonist action of the glycine receptor in the brain. Gelsevirine has anti-proliferation activity with IC50 values of 1.41 mM and 1.22 mM for SW480 cells and MGC80-3 cells, respectively.
|
-
- HY-134189
-
|
EST73502
|
Opioid Receptor
Sigma Receptor
|
Neurological Disease
|
|
EST73502 is a selective, orally active and blood-brain barrier (BBB) penetrant dual μ-opioid receptor (MOR) agonist and σ1 receptor (σ1R) antagonist, with Kis of 64 nM and 118 nM for MOR and σ1R, respectively. EST73502 has antinociceptive activity.
|
-
- HY-122347A
-
|
Orvepitant maleate
GW823296 maleate
|
Neurokinin Receptor
|
Neurological Disease
|
|
Orvepitant maleate (GW823296 maleate) is potent, selective, orally active and well-tolerated neurokinin-1 receptor (NK-1) antagonist with a pKi of 10.2 for human neurokinin-1 receptor. Orvepitant maleate can across the blood-brain barrier. Orvepitant maleate has the potential for depressive disorder and chronic refractory cough (CRC) treatment.
|
-
- HY-P2713
-
|
OM99-2
|
Beta-secretase
|
Neurological Disease
|
|
OM99-2, an eight residue peptidomimetic, tight-binding inhibitor of human brain memapsin 2 with a Ki value of 9.58 nM. OM99-2 is significantly advanced the development of BACE1 inhibitor. OM99-2 has the potential for the research of the Alzheimer's disease.
|
-
- HY-P1256
-
|
JMV 449
|
Neurotensin Receptor
|
Neurological Disease
|
|
JMV 449 is a potent neurotensin receptor agonist. JMV 449 shows an IC50 of 0.15 nM for inhibition of [ 125I]-neurotensin binding to neonatal mouse brain and an EC50 of 1.9 nM in contracting the guinea-pig ileum. JMV 449 has highly potent and long-lasting hypothermic and analgesic effects in the mouse.
|
-
- HY-144309
-
-
- HY-131350
-
|
LXE408
|
Proteasome
Parasite
|
Infection
|
|
LXE408 is an orally active, non-competitive and kinetoplastid-selective proteasome inhibitor. LXE408 has an IC50 of 0.04 μM for L. donovani proteasome and an EC50 of 0.04 μM for L. donovani. LXE408 has a low propensity to cross the blood brain barrier. LXE408 has the potential for visceral leishmaniasis (VL) research.
|
-
- HY-70020
-
|
Cevimeline
AF102B
|
mAChR
|
Neurological Disease
|
|
Cevimeline (AF-102B) is a quinuclidine derivative of acetylcholine and a selective and orally active muscarinic M1 and M3 receptor agonist. Cevimeline stimulates secretion by the salivary glands and can be used as a sialogogue for xerostomia. Cevimeline can cross the blood-brain barrier (BBB).
|
-
- HY-103558
-
|
LY379268
|
mGluR
|
Neurological Disease
|
|
LY379268 is a potent, selective and brain-penetrant mGlu2/3R agonist with EC50 values of 2.69 nM (mGlu2) and 4.48 nM (mGlu3). LY379268 has no activity on human mGlu 1a, 4a, 5a or 7a receptors. LY379268 has antioxidant and neuroprotective effects.
|
-
- HY-109052
-
|
Atabecestat
JNJ-54861911
|
Beta-secretase
|
Neurological Disease
|
|
Atabecestat (JNJ-54861911) is a potent brain-penetrant and orally active β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor, achieves robust and high CSF Aβ reduction. Atabecestat s tolerated and displays a sustained pharmacokinetic (PK) and pharmacodynamic (PD) characteristics. Atabecestat has the potential for Alzheimer's Disease treatment.
|
-
- HY-101364A
-
|
CHPG sodium salt
|
mGluR
NF-κB
ERK
Akt
|
Inflammation/Immunology
Neurological Disease
|
|
CHPG sodium salt is a selective mGluR5 agonist, and attenuates SO2-induced oxidative stress and inflammation through TSG-6/NF-κB pathway in BV2 microglial cells. CHPG sodium salt protects against traumatic brain injury (TBI) in vitro and in vivo by activation of the ERK and Akt signaling pathways..
|
-
- HY-106003
-
-
- HY-W016420
-
|
Fosfomycin sodium
MK-0955 sodium
|
Bacterial
Antibiotic
|
Infection
Cancer
|
|
Fosfomycin (MK-0955) sodium is a blood-brain barrier penetrating, broad-spectrum antibiotic by irreversibly inhibiting an early stage in cell wall synthesis. Fosfomycin sodium shows both in vivo and in vitro activity against a wide range of bacteria, including multidrug-resistant (MDR), extensively drug-resistant (XDR), and pan-drug-resistant (PDR) bacteria.
|
-
- HY-126244
-
|
CDK4/6-IN-3
|
CDK
|
Cancer
|
|
CDK4/6-IN-3 is a brain-penetrant CDK4/CDK6 inhibitor with Kis of <0.3 nM and 2.2 nM, respectively. CDK4/6-IN-3 inhibits CDK1 with a Ki of 110 nM. CDK4/6-IN-3 can be used for the treatment of glioblastoma.
|
-
- HY-133596
-
|
12,14-Dichlorodehydroabietic acid
|
Potassium Channel
GABA Receptor
|
Neurological Disease
|
|
12,14-Dichlorodehydroabietic acid, a chlorinated resin acid, is a potent Ca 2+-activated K + (BK) channel opener. 12,14-Dichlorodehydroabietic acid blocks GABA-dependent chloride entry in mammalian brain and operates as a non-competitive GABAA antagonist. 12,14-Dichlorodehydroabietic acid increases cytosolic free Ca 2+ and stimulates transmitter release.
|
-
- HY-125693
-
|
L685818
|
Fungal
|
Infection
Neurological Disease
|
|
L685818 is a specific immunophilin ligand. L685818 was neuroregenerative and non-neuroprotective in primary brain cultures. L685818 protects dopaminergic neurons from toxic inhibition of MPP+ and 6-OHDA, reduces tyrosine hydroxylase (TH) loss, and promotes neuronal process regeneration. L685818 is also an antifungal reagent for Cryptococcus neoformans.
|
-
- HY-17364
-
|
Temozolomide
NSC 362856; CCRG 81045; TMZ
|
DNA Alkylator/Crosslinker
Autophagy
Apoptosis
|
Cancer
|
|
Temozolomide (NSC 362856) is an oral active DNA alkylating agent that crosses the blood-brain barrier. Temozolomide is also a proautophagic and proapoptotic agent. Temozolomide is effective against tumor cells that are characterized by low levels of O6-alkylguanine DNA alkyltransferase (OGAT) and a functional mismatch repair system. Temozolomide has antitumor and antiangiogenic effects.
|
-
- HY-116451
-
|
PF-04859989 hydrochloride
|
Others
|
Neurological Disease
|
|
PF-04859989 hydrochloride is a brain-penetrant, irreversible kynurenine aminotransferase (KAT) II inhibitor with IC50s of 23 and 263 nM for hKAT II and rKAT II. PF-04859989 hydrochloride is selective for KAT II over human KAT I, KAT III, and KAT IV (IC50s of 22, 11, and >50 μM, respectively).
|
-
- HY-13289
-
|
Nepicastat
SYN117; RS-25560-197
|
Dopamine β-hydroxylase
|
Cardiovascular Disease
|
|
Nepicastat (SYN117) is a selective, potent, and orally active inhibitor of dopamine-beta-hydroxylase. Nepicastat (SYN117) produces concentration-dependent inhibition of bovine (IC50=8.5 nM) and human (IC50=9 nM) dopamine-beta-hydroxylase. Nepicastat (SYN117) can cross the blood-brain barrier (BBB).
|
-
- HY-15771
-
|
Tirabrutinib
ONO-4059; GS-4059
|
Btk
Apoptosis
|
Cancer
Inflammation/Immunology
|
|
Tirabrutinib (ONO-4059) is an orally active Bruton’s Tyrosine Kinase (BTK) inhibitor (can cross the blood-brain barrier (BBB)), with an IC50 of 6.8 nM. Tirabrutinib irreversibly and covalently binds to BTK and inhibits aberrant B cell receptor signaling. Tirabrutinib can be used in studies of autoimmune diseases and hematological malignancies.
|
-
- HY-11045
-
-
- HY-150236
-
|
FITC-labeled Tominersen
|
Huntingtin
|
Neurological Disease
|
|
FITC-labeled Tominersen is Tominersen labeled with FITC. Tominersen (RG6042) is a second-generation 2′-O-(2-methoxyethyl) antisense oligonucleotide that targets huntingtin protein (HTT) mRNA and potently suppresses HTT production. Tominersen improves survival and reduces brain atrophy in mice. Tominersen can be used for the research of Huntington’s disease (HD).
|
-
- HY-14397S
-
|
Indomethacin-d4
Indometacin-d4
|
COX
Autophagy
|
Cancer
Inflammation/Immunology
|
|
Indomethacin-d4 is a deuterium labeled Indomethacin. Indomethacin is a potent, blood-brain permeable and nonselective inhibitor of COX1 and COX2, with IC50s of 18 nM and 26 nM for human COX-1 and COX-2, respectively, in CHO cells[1]. Indomethacin disrupts autophagic flux by disturbing the normal functioning of lysosomes[2].
|
-
- HY-101478
-
|
Fenobam
|
mGluR
|
Neurological Disease
|
|
Fenobam is a selective, orally active, and brain-penetrant mGluR5 antagonist acting at an allosteric modulatory site (Kds of 54 and 31 nM for rat and human recombinant mGlu5 receptors, respectively). Fenobam displays inverse agonist activity which blocks the mGlu5 receptor basal activity with an IC50 of 84 nM. Fenobam exerts anxiolytic activity.
|
-
- HY-100740C
-
|
(1α,1'S,4β)-Lanabecestat
(1α,1'S,4β)-AZD3293; (1α,1'S,4β)-LY3314814
|
Beta-secretase
|
Neurological Disease
|
|
(1α,1'S,4β)-Lanabecestat ((1α,1'S,4β)-AZD3293) a less active enantiomer of Lanabecestat. Lanabecestat is a potent, orally active and blood-brain barrier penetrating BACE1 inhibitor with a Ki of 0.4 nM.
|
-
- HY-10232
-
|
THIP
Gaboxadol
|
GABA Receptor
|
Neurological Disease
|
|
THIP (Gaboxadol) is a selective extrasynaptic GABAA receptors (eGABARs) agonist (with blood-brain barrier permeability), shows an EC50 value of 13 µM for δ-GABAAR. THIP induces strong tense GABAA-mediated currents in layer 2/3 neurons, but shows on effect on miniature IPSCs. THIP can be used in studies of sleep disorders.
|
-
- HY-111274
-
|
Indomethacin farnesil
Indometacin farnesil
|
COX
Autophagy
|
Inflammation/Immunology
|
|
Indomethacin farnesil is an orally active prodrug of Indomethacin. Indomethacin (Indometacin) is a potent, blood-brain permeable and nonselective inhibitor of COX1 and COX2, with IC50s of 18 nM and 26 nM for human COX-1 and COX-2, respectively, in CHO cells. Indomethacin disrupts autophagic flux by disturbing the normal functioning of lysosomes.
|
-
- HY-B1395S1
-
|
Mecamylamine hydrochloride-13C4,15N
|
nAChR
|
Neurological Disease
|
|
Mecamylamine (hydrochloride)- 13C4, 15N is the 13C-labeled and 15N-labeled Mecamylamine hydrochloride. Mecamylamine hydrochloride is an orally active, nonselective, noncompetitive nAChR antagonist that can treat various neuropsychiatric disorders. Mecamylamine hydrochloride is originally used as a ganglionic blocker in treating hypertension. Mecamylamine hydrochloride can easily crosses the blood-brain barrier[1][2].
|
-
- HY-101402A
-
|
Cyclo(his-pro) TFA
Cyclo(histidyl-proline) TFA; Histidylproline diketopiperazine TFA
|
NF-κB
Endogenous Metabolite
|
Inflammation/Immunology
Neurological Disease
|
|
Cyclo(his-pro) TFA (Cyclo(histidyl-proline) TFA) is an orally active cyclic dipeptide structurally related to tyreotropin-releasing hormone. Cyclo(his-pro) TFA could inhibit NF-κB nuclear accumulation. Cyclo(his-pro) TFA can cross the brain-blood-barrier and affect diverse inflammatory and stress responses.
|
-
- HY-P1136C
-
-
- HY-112037A
-
|
IACS-010759 hydrochloride
IACS-10759 hydrochloride
|
Mitochondrial Metabolism
Apoptosis
|
Cancer
|
|
IACS-010759 hydrochlorideis an orally active, potent mitochondrial complex I of oxidative phosphorylation (OXPHOS) inhibitor. IACS-010759 hydrochlorideinhibits proliferation and induces apoptosis in models of brain cancer and acute myeloid leukemia (AML) reliant on OXPHOS. IACS-010759 hydrochloride has the potential for relapsed/refractory AML and solid tumors research.
|
-
- HY-P2713A
-
|
OM99-2 TFA
|
Beta-secretase
|
Neurological Disease
|
|
OM99-2 TFA, an eight residue peptidomimetic, tight-binding inhibitor of human brain memapsin 2 with a Ki value of 9.58 nM. OM99-2 TFA is significantly advanced the development of BACE1 inhibitor. OM99-2 has the potential for the research of the Alzheimer's disease.
|
-
- HY-P1178A
-
|
Cyclotraxin B TFA
|
Trk Receptor
|
Neurological Disease
|
|
Cyclotraxin B TFA, a cyclic peptide, is a highly potent and selective TrkB inhibitor without altering the binding of BDNF. Cyclotraxin B TFA non-competitively inhibits BDNF-induced TrkB activity with an IC50 of 0.30 nM. Cyclotraxin B TFA can crosse the blood-brain-barrier and has analgesic and anxiolytic-like behavioral effects.
|
-
- HY-152292
-
|
Zidesamtinib
NVL-520
|
ROS Kinase
|
Cancer
|
|
Zidesamtinib (NVL-520) is a potent, selective, orally active and brain-penetrant inhibitor of diverse ROS1 fusions and resistance mutations, with IC50s of 0.7 and 7.9 nM for wild-type ROS1 and ROS1 G2032R, respectively, and spares TRK inhibition. Zidesamtinib can be used for the research of cancer.
|
-
- HY-101364
-
|
CHPG
|
mGluR
NF-κB
ERK
Akt
|
Inflammation/Immunology
Cardiovascular Disease
|
|
CHPG is a selective mGluR5 agonist, and attenuates SO2-induced oxidative stress and inflammation through TSG-6/NF-κB pathway in BV2 microglial cells. CHPG protects against traumatic brain injury (TBI) in vitro and in vivo by activation of the ERK and Akt signaling pathways.
|
-
- HY-B1075A
-
|
Fosfomycin
MK-0955
|
Bacterial
Antibiotic
|
Infection
|
|
Fosfomycin (MK-0955) is a broad-spectrum antibiotic. Fosfomycin can cross blood-brain barrier penetrating, and irreversibly inhibits an early stage in cell wall synthesis. Fosfomycin shows anti-bacteria activity for a range of bacteria, including multidrug-resistant (MDR), extensively drug-resistant (XDR), and pan-drug-resistant (PDR) bacteria.
|
-
- HY-A0067
-
|
Oxybenzone
Benzophenone 3
|
RAR/RXR
Autophagy
Apoptosis
|
Neurological Disease
|
|
Oxybenzone (Benzophenone 3) is a commonly used UV filter in sun tans and skin protectants. Oxybenzone act as endocrine disrupting chemicals (EDCs) and can pass through the placental and blood-brain barriers. Benzophenone-3 impairs autophagy, alters epigenetic status, and disrupts retinoid X receptor signaling in apoptotic neuronal cells.
|
-
- HY-134189A
-
-
- HY-115750
-
|
Nω-allyl-L-arginine
|
NO Synthase
|
Neurological Disease
|
|
Nω-allyl-L-arginine is a competitive and reversible inhibitor of bovine brain nitric oxide synthase (nNOS). Nω-allyl-L-arginine can inactivate nNOS in a time-dependent manner. Nω-allyl-L-arginine also is a substrate, producing L-arginine, acrolein, and H2O.
|
-
- HY-P2867
-
|
Phosphodiesterase II
|
Phosphodiesterase (PDE)
|
Neurological Disease
|
|
Phosphodiesterase II, namely phosphodiesterase 2, is mainly involved in the hydrolysis of the important second messengers cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP), and is often used in biochemical research. Phosphodiesterase II is expressed in a variety of tissues, such as the adrenal medulla, brain, heart, platelets, macrophages and endothelial cells, and is involved in the regulation of many different intracellular processes.
|
-
- HY-15771A
-
|
Tirabrutinib hydrochloride
ONO-4059 hydrochloride; GS-4059 hydrochloride
|
Btk
Apoptosis
|
Cancer
Inflammation/Immunology
|
|
Tirabrutinib (ONO-4059) hydrochloride is an orally active Bruton’s Tyrosine Kinase (BTK) inhibitor (can cross the blood-brain barrier (BBB)), with an IC50 of 6.8 nM. Tirabrutinib hydrochloride irreversibly and covalently binds to BTK and inhibits aberrant B cell receptor signaling. Tirabrutinib hydrochloride can be used in studies of autoimmune diseases and hematological malignancies.
|
-
- HY-107855S
-
|
DL-Mevalonolactone-d7
(±)-Mevalonolactone-d7; Mevalolactone-d7
|
Endogenous Metabolite
|
Metabolic Disease
|
|
DL-Mevalonolactone-d7 is the deuterium labeled DL-Mevalonolactone. DL-Mevalonolactone ((±)-Mevalonolactone) is the δ-lactone form of mevalonic acid, a precursor in the mevalonate pathway. DL-Mevalonolactone (Mevalonolactone) decreases mitochondrial membrane potential (∆Ψm), NAD(P)H content and the capacity to retain Ca2+ in the brain, besides inducing mitochondrial swelling[1][2].
|
-
- HY-13340
-
|
VU0152100
VU152100
|
mAChR
|
Neurological Disease
|
|
VU0152100 (VU152100) is a highly selective mAChR positive allosteric modulator (permeable to the blood-brain barrier). VU0152100 reverses Amphetamine-induced hypermotility in rats and increased levels of extracellular dopamine in nucleus accumbens and caudate-putamen. VU0152100 has good research potential in psychosis and cognitive impairment associated with mental disorders such as schizophrenia.
|
-
- HY-103461
-
|
FAAH-IN-6
|
FAAH
|
Neurological Disease
|
|
FAAH-IN-6 (compound 21d) is a potent, orally active and cross the blood-brain barrier fatty acid amide hydrolase (FAAH) inhibitor with IC50s of 0.72, 0.28 nM for hFAAH, rFAAH, respectively. FAAH-IN-6 shows dose-dependent analgesic efficacy in animal models of both neuropathic and inflammatory pain.
|
-
- HY-120619
-
|
BMS-193885
|
Neuropeptide Y Receptor
|
Neurological Disease
Endocrinology
|
|
BMS-193885 is a potent, selective, competitive, and brain penetrant neuropeptide Y1 receptor antagonist with a Ki of 3.3 nM, and has an IC50 of 5.9 nM for hY1, which displays > 100, > 160, > 160 and > 160-fold selectivity over α1, hY2, hY4 and hY5 receptors, respectively .
|
-
- HY-N3187
-
-
- HY-109192
-
|
Tolebrutinib
SAR442168; PRN2246
|
Btk
|
Neurological Disease
|
|
Tolebrutinib (SAR442168) is a potent, selective, orally active and brain-penetrant inhibitor of Bruton tyrosine kinase (BTK), with IC50s of 0.4 and 0.7 nM in Ramos B cells and in HMC microglia cells, respectively. Tolebrutinib exhibits efficacy in central nervous system immunity. Tolebrutinib can be used for the research of multiple sclerosis (MS).
|
-
- HY-144604
-
|
FPR2 agonist 2
|
Others
|
Infection
Neurological Disease
|
|
FPR2 agonist 2 is a potent and permeates the blood−brain barrier FPR2 agonist with an EC50 of 0.13 µM, 1.1 µM for FPR2 and FPR1, respectively. FPR2 agonist 2 inhibits the production of pro-inflammatory cytokines, counterbalances the changes in mitochondrial function, and inhibits caspase-3 activity.
|
-
- HY-P1090A
-
|
Hemopressin(rat) TFA
|
Cannabinoid Receptor
|
Neurological Disease
|
|
Hemopressin(rat) TFA is a nonapeptide derived from the α1-chain of hemoglobin, is originally isolated from rat brain homogenates. Hemopressin(rat) TFA is orally active, selective and inverse agonist of CB1 cannabinoid receptors. Hemopressin(rat) TFA exerts antinociceptive action in inflammatory pain models.
|
-
- HY-P99163
-
|
Tilavonemab
ABBV-8E12; C2N-8E12
|
Microtubule/Tubulin
|
Neurological Disease
|
|
Tilavonemab (ABBV-8E12) is a humanised anti-tau antibody that binds amino acids 25-30 near the N-terminal end of the tau protein. Tilavonemab blocks the ability of human and mouse neurons to take up tau aggregates and reduces brain atrophy. Tilavonemab can be used in the study of Alzheimer's disease.
|
-
- HY-P3035
-
|
Corazonin
|
G Protein-coupled Receptor Kinase (GRK)
|
Neurological Disease
|
|
Corazonin is a highly conserved neuropeptide hormone of wide-spread occurrence in insects, serves a central regulator of caste identity and behavior in social insects. Corazonin is also preferentially expressed in workers and/or foragers from other social insect species.
|
-
- HY-P3801
-
|
[Glp5,(Me)Phe8,Sar9] Substance P (5-11)
DiMe-C7
|
Neurokinin Receptor
|
Metabolic Disease
Neurological Disease
Others
|
|
[Glp5,(Me)Phe8,Sar9] Substance P (5-11) (DiMe-C7) is a Substance P (HY-P0201) analogue that has approximately the same effects as Substance P (HY-P0201) on neurokinin 1 receptor (NK1R) in rat brain, but with a much longer duration of action. [Glp5,(Me)Phe8,Sar9] Substance P (5-11) selectively activates dopamine metabolism in the mesencephalon and midbrain cortex of the rat brain. [Glp5,(Me)Phe8,Sar9] Substance P (5-11) also increases motor activity and induces recovery of cocaine-seeking behavior in rats.
|
-
- HY-124160
-
|
JNJ-56022486
|
iGluR
|
Neurological Disease
|
|
JNJ-56022486 is an orally active and potent negative AMPA receptor modulator (Ki=19 nM) selective for TARP-γ8. JNJ-56022486 is also a TARP-γ8 receptor antagonist, with blood brain barrier (BBB) permeability. JNJ-56022486 can be used for research of Epilepsy.
|
-
- HY-B1075
-
|
Fosfomycin calcium
MK-0955 calcium
|
Bacterial
Antibiotic
|
Infection
Cancer
|
|
Fosfomycin (MK-0955) calcium is a blood-brain barrier penetrating, broad-spectrum antibiotic by irreversibly inhibiting an early stage in cell wall synthesis. Fosfomycin calcium shows both in vivo and in vitro activity against a wide range of bacteria, including multidrug-resistant (MDR), extensively drug-resistant (XDR), and pan-drug-resistant (PDR) bacteria.
|
-
- HY-147149
-
|
BPN-15477
|
Others
|
Neurological Disease
|
|
BPN-15477 is a potent SMC (splicing modulator compound) that restores correct splicing of ELP1 (Elongator complex protein 1) exon 20. BPN-15477 corrects splicing of the ELP1 transcript, significantly increases the level of functional protein in vivo in all tissues, including brain. BPN-15477 can be used for frontotemporal dementia research.
|
-
- HY-B0609
-
|
Fosfomycin tromethamine
MK-0955 tromethamine
|
Bacterial
Antibiotic
|
Infection
Cancer
|
|
Fosfomycin (MK-0955) tromethamine is a blood-brain barrier penetrating, broad-spectrum antibiotic by irreversibly inhibiting an early stage in cell wall synthesis. Fosfomycin tromethamine shows both in vivo and in vitro activity against a wide range of bacteria, including multidrug-resistant (MDR), extensively drug-resistant (XDR), and pan-drug-resistant (PDR) bacteria.
|
-
- HY-10202A
-
|
Tandutinib hydrochloride
MLN518 hydrochloride; CT53518 hydrochloride
|
FLT3
c-Kit
PDGFR
Apoptosis
|
Cancer
|
|
Tandutinib hydrochloride (MLN518 hydrochloride) is a potent and selective inhibitor of the FLT3 with an IC50 of 0.22 μM, and also inhibits c-Kit and PDGFR with IC50s of 0.17 μM and 0.20 μM, respectively. Tandutinib hydrochloride can be used for acute myelogenous leukemia (AML). Tandutinib hydrochloride has the ability to cross the blood-brain barrier.
|
-
- HY-148417
-
|
ZZL-7
|
Serotonin Transporter
|
Neurological Disease
|
|
ZZL-7 is a fast-onset antidepressant agent. ZZL-7 works by disrupting the interaction between the serotonin transporter (SERT) and neuronal nitric oxide synthase (nNOS) in the dorsal raphe nucleus (DRN). ZZL-7 can cross the blood-brain barrier readily. ZZL-7 can be used for the research of major depressive disorder (MDD).
|
-
- HY-14397S1
-
|
Indomethacin-d4 Methyl Ester
|
COX
Autophagy
|
Cancer
Inflammation/Immunology
|
|
Indomethacin-d4 Methyl Ester is the deuterium labeled Indomethacin. Indomethacin (Indometacin) is a potent, blood-brain permeable and nonselective inhibitor of COX1 and COX2, with IC50s of 18 nM and 26 nM for human COX-1 and COX-2, respectively, in CHO cells[1]. Indomethacin disrupts autophagic flux by disturbing the normal functioning of lysosomes[2].
|
-
- HY-151985
-
|
TACC3 inhibitor 1
|
Apoptosis
|
Cancer
|
|
TACC3 inhibitor 1 is a potent and cross the blood-brain barrier TACC3 inhibitor. TACC3 inhibitor 1 induces apoptosis and cell cycle arrest at G2/M phase. TACC3 inhibitor 1 induces the generation of intracellular ROS. TACC3 inhibitor 1 shows antiproliferative and anti-tumor activity.
|
-
- HY-14325A
-
|
L-745870 trihydrochloride
|
Dopamine Receptor
|
Neurological Disease
|
|
L-745870 trihydrochloride is a potent, selective, brain-penetrant and orally active dopamine D4 receptor antagonist with a Ki of 0.43 nM. L-745870 trihydrochloride shows weaker affinity for D2 (Ki of 960 nM) and D3 (Ki of 2300 nM) receptors, and exhibits moderate affinity for 5-HT2 receptors, sigma sites and α-adrenoceptors.
|
-
- HY-33009
-
|
AS057278
|
Others
|
Neurological Disease
|
|
AS057278 is a potent, selective, orally active and blood-brain barrier (BBB) penetrant non-peptidic D-amino acid oxidase (DAAO) inhibitor with an IC50 value of 0.91 μM and EC50 of 2.2-3.95 μM. AS057278 can normalize phencyclidine (PCP)-induced prepulse inhibition in mice. AS057278 can be used for researching schizophrenia.
|
-
- HY-16688
-
|
RU 24969
|
5-HT Receptor
|
Neurological Disease
|
|
RU 24969 is a preferential 5-HT1B agonist, with a Ki of 0.38 nM, but also displays appreciable affinity for the 5-HT1A receptor (Ki=2.5 nM), and has low affinity for other receptor sites in the brain. RU 24969 could decrease fluid consumption and increase forward locomotion.
|
-
- HY-B0364A
-
|
Dyclonine hydrochloride
Dyclocaine hydrochloride
|
Bacterial
Fungal
Aldehyde Dehydrogenase (ALDH)
|
Cancer
Infection
|
|
Dyclonine (Dyclocaine) hydrochloride is an orally effective ALDH covalent inhibitor (crosses blood-brain barrier), with an IC50 of 35 µM for ALDH2 and 76 µM for ALDH3A1. Dyclonine hydrochloride has sensitizing activities for targeted cancer cells and antibacterial. Dyclonine hydrochloride is also a local anesthetic that blocks the transmission of various nerve impulses or stimuli and inhibits the sensation of touch and pain.
|
-
- HY-P3138
-
|
(Sar1)-Angiotensin II
|
Angiotensin Receptor
|
Cardiovascular Disease
|
|
(Sar1)-Angiotensin II, an analogue of Angiotensin II, is a specific agonist of angiotensin AT1 receptor. (Sar1)-Angiotensin II binds to brain membrane-rich particles, with a Kd of 2.7 nM. (Sar1)-Angiotensin II can stimulate protein synthesis and cell growth in embryonic chick myocytes.
|
-
- HY-10985
-
|
Marizomib
Salinosporamide A; NPI-0052
|
Proteasome
|
Cancer
|
|
Marizomib (Salinosporamide A) is a second-generation, irreversible, brain-penetrant, pan-proteasome inhibitor. Marizomib inhibits the CT-L (β5), CT-T-laspase-like (C-L, β1) and trypsin-like (T-L, β2) activities of the 20S proteasome (IC50=3.5, 28, and 430 nM, respectively).
|
-
- HY-10974
-
|
MK-0752
|
γ-secretase
|
Neurological Disease
Cancer
|
|
MK-0752 is a potent, orally active and specific γ-secretase inhibitor, showing dose-dependent reduction of Aβ40 with an IC50 of 5 nM in human SH-SY5Y cells. MK-0752 crosses the blood-brain barrier. MK-0752 reduces newly generated CNS Aβ in vivo.
|
-
- HY-B0033S
-
|
Vigabatrin-13C,d2 hydrochloride
γ-Vinyl-GABA-13C,d2 (hydrochloride)
|
GABA Receptor
|
Neurological Disease
|
|
Vigabatrin- 13C,d2 (hydrochloride) is the 13C- and deuterium labeled Vigabatrin (hydrochloride). Vigabatrin hydrochloride (γ-Vinyl-GABA hydrochloride), a inhibitory neurotransmitter GABA vinyl-derivative, is an orally active and irreversible GABA transaminase inhibitor. Vigabatrin hydrochloride is an antiepileptic agent, which acts by increasing GABA levels in the brain by inhibiting the catabolism of GABA by GABA transaminase[1][2][3].
|
-
- HY-130795
-
|
GSK-3β inhibitor 2
|
GSK-3
|
Neurological Disease
|
|
GSK-3β inhibitor 2 (Compound 3) is a potent, selective and orally active GSK-3β inhibitor with an IC50 of 1.1 nM. GSK-3β inhibitor 2 can cross the blood-brain barrier. GSK-3β inhibitor 2 has the potential for Alzheimer's disease.
|
-
- HY-134968A
-
|
(R)-TTBK1-IN-1
|
Tau Protein
|
Neurological Disease
|
|
(R)-TTBK1-IN-1 is a potent, selective and brain-penetrant tau tubulin kinase 1 (TTBK1) inhibitor. (R)-TTBK1-IN-1 is an enantiomer of TTBK1-IN-1 (HY-134968). (R)-TTBK1-IN-1 can be used in the research of alzheimer’s disease and related tauopathies.
|
-
- HY-112601
-
|
IDH1 Inhibitor 1
|
Isocitrate Dehydrogenase (IDH)
|
Cancer
|
|
IDH1 Inhibitor 1 is a potent, orally bioavailable, brain-penetrant and selective mutant IDH1 inhibitor with IC50s of 0.021 μM, 0.045 μM, and 2.52 μM for IDH1 R132H, IDH1 R132C, and IDH1 WT, respectively. Anticancer activity.
|
-
- HY-150791
-
|
FLDP-5
|
Reactive Oxygen Species
DNA/RNA Synthesis
|
Cancer
|
|
FLDP-5 is a blood-brain barrier (BBB) penetrant curcuminoid analogues. FLDP-5 can induce production of ROS (Reactive Oxygen Species), DNA damage and cell cycle S phase arrest. FLDP-5 exhibits highly potent tumour-suppressive effects with anti-proliferative and anti-migratory activities on LN-18 cells.
|
-
- HY-148030
-
|
XL01126
|
PROTACs
LRRK2
|
Neurological Disease
|
|
XL01126 is a potent degrader of LRRK2 with DC50s of 14 nM (G2019S LRRK2) and 32 nM (WT LRRK2), respectively. XL01126 can cross blood-brain barrier and be used as a degrader probe in Parkinson’s disease research. XL01126 exerts function of study of non-catalytic and scaffolding functions of LRRK2.
|
-
- HY-P4052
-
|
Pinealon
|
ROS Kinase
|
Neurological Disease
|
|
Pinealon is a 3-amino acid peptide and shows neuroprotective properties. Pinealon prevents reactive oxygenspecies (ROS) accumulation and supressesthe activation of ERK 1/2. Pinealon has the ability to stimulate the functional activity of the main cellular elements of brain tissue, reduce the level of spontaneous cell death. Pinealon protects the rat offspring from prenatal hyperhomocysteinemia.
|
-
- HY-114331
-
|
DLK-IN-1
|
MAP3K
|
Neurological Disease
|
|
DLK-IN-1 is a selective, orally active inhibitor of dual leucine zipper kinase (DLK, MAP3K12), with a Ki of 3 nM. DLK-IN-1 retains excellent CNS penetration and is well tolerated following multiple days of dosing at concentrations that exceed those required for DLK inhibition in the brain. DLK-IN-1 has activity in a model of Alzheimer’s Disease.
|
-
- HY-122607
-
|
DPA-714
|
Others
|
Cancer
Inflammation/Immunology
|
|
DPA-714 is a high affinity translocator protein (TSPO) ligand (Ki=7 nM), which is designed with a fluorine atom in its structure, allowing labelling with fluorine -18 and in vivo imaging using positron emission tomography. 18FDPA-714 successfully evaluates for the specific imaging of inflammation in various models of neuroinflammation and in a brain tumor model.
|
-
- HY-149014
-
-
- HY-126419
-
|
Kobophenol A
|
SARS-CoV
PKC
|
Infection
|
|
Kobophenol A, an oligomeric stilbene, blocks the interaction between the ACE2 receptor and S1-RBD with an IC50 of 1.81 μM and inhibits SARS-CoV-2 viral infection in cells with an EC50 of 71.6 μM. Kobophenol A inhibits the activity of partially purified rat brain protein kinase C (PKC) with an IC50 of 52 µM.
|
-
- HY-107855S1
-
|
DL-Mevalonolactone-d3
(±)-Mevalonolactone-d3; Mevalolactone-d3
|
Endogenous Metabolite
|
Metabolic Disease
|
|
DL-Mevalonolactone-d3 is the deuterium labeled DL-Mevalonolactone[1]. DL-Mevalonolactone ((±)-Mevalonolactone;Mevalolactone) is the δ-lactone form of mevalonic acid, a precursor in the mevalonate pathway. DL-Mevalonolactone (Mevalonolactone) decreases mitochondrial membrane potential (?Ψm), NAD(P)H content and the capacity to retain Ca2+ in the brain, besides inducing mitochondrial swelling[2][3].
|
-
- HY-10400
-
|
Ladostigil hemitartrate
TV-3326 hemitartrate
|
Monoamine Oxidase
Cholinesterase (ChE)
|
Neurological Disease
|
|
Ladostigil (TV-3326) hemitartrate is an orally active dual inhibitor of cholinesterase and brain-selective monoamine oxidase (MAO), with IC50s of 37.1 and 31.8 μM for MAO-B and AChE, respectively. Ladostigil hemitartrate exhibits neuroprotective, antioxidant and anti-inflammatory activities. Ladostigil hemitartrate can be used for the research of depression and Alzheimer's disease.
|
-
- HY-109502S
-
|
10-OH-NBP-d4
|
Isotope-Labeled Compounds
|
Neurological Disease
|
|
10-OH-NBP-d4 is deuterium labeled 10-OH-NBP. 10-OH-NBP is a Butylphthalide (3-n-Butylphthalide; NBP; HY-B0647) hydroxylated metabolite and can penetrates the blood-brain barrier (BBB). Butylphthalide exerts neuroprotective effects and has potential for cerebral ischemia research[1].
|
-
- HY-143413
-
|
BuChE-IN-2
|
Amyloid-β
|
Inflammation/Immunology
Neurological Disease
|
|
BuChE-IN-2 is an excellent butyrylcholinesterase (BuChE) inhibitor (IC50s of 1.28 μM and 0.67 μM for BuChE and NO). BuChE-IN-2 can inhibit the aggregation of Aβ, ROS formation and chelate Cu 2+, exhibiting proper blood-brain barrier (BBB) penetration. BuChE-IN-2 has potential to research Alzheimer’s disease.
|
-
- HY-10202
-
|
Tandutinib
MLN518; CT53518
|
FLT3
c-Kit
PDGFR
Apoptosis
|
Cancer
|
|
Tandutinib (MLN518) is a potent and selective inhibitor of the FLT3 with an IC50 of 0.22 μM, and also inhibits c-Kit and PDGFR with IC50s of 0.17 μM and 0.20 μM, respectively. Tandutinib can be used for acute myelogenous leukemia (AML). Tandutinib has the ability to cross the blood-brain barrier.
|
-
- HY-12959A
-
|
Repinotan hydrochloride
BAY x 3702
|
5-HT Receptor
|
Neurological Disease
|
|
Repinotan hydrochloride (BAY x 3702) is a potent, selective, brain-penetrant and orally active 5-HT1A receptor agonist, with Ki values of 0.19 nM (calf hippocampus), 0.25 nM (rat and human cortex), and 0.59 nM (rat hippocampus Repinotan hydrochloride has a weak affinity for other related receptors. Repinotan hydrochloride has pronounced neuroprotective effects.
|
-
- HY-10847A
-
|
SB-277011 dihydrochloride
SB-277011A dihydrochloride
|
Dopamine Receptor
|
Neurological Disease
|
|
SB-277011 dihydrochloride (SB-277011A dihydrochloride) is a potent, selective, orally bioavailable and brain penetrate dopamine D3 receptor antagonist, with pKis of 8.0, 6.0, <5.2 and 5.9 for D3, D2, 5-HT1B, and 5-HT1D receptors, respectively.
|
-
- HY-148250
-
|
TP-050
|
iGluR
|
Neurological Disease
|
|
TP-050 is a potent, orally active and selective NMDAR agonist with an EC50 value of 0.51 µM and 9.6 µM for GluN2A and GluN2D, respecticely. TP-050 can cross the blood-brain barrier (BBB). TP-050 induces hippocampal long-term (LPT) potentiation enhancemen and enhances neuronal signal transmission.
|
-
- HY-16688B
-
|
RU 24969 hemisuccinate
|
5-HT Receptor
|
Neurological Disease
|
|
RU 24969 hemisuccinate is a preferential 5-HT1B agonist, with a Ki of 0.38 nM, but also displays appreciable affinity for the 5-HT1A receptor (Ki=2.5 nM), and has low affinity for other receptor sites in the brain. RU 24969 hemisuccinate could decrease fluid consumption and increase forward locomotion.
|
-
- HY-B0688
-
|
Dapsone
4,4′-Diaminodiphenyl sulfone; DDS
|
Antibiotic
Parasite
Bacterial
Reactive Oxygen Species
|
Infection
Inflammation/Immunology
|
|
Dapsone (4,4′-Diaminodiphenyl sulfone) is an orally active and blood-brain penetrant sulfonamide antibiotic with bacteriostatic, antimycobacterial and antiprotozoal activities. Dapsone exerts effective antileprosy activity and inhibits folate synthesis in cell extracts of M. leprae. Dapsone is used for dermatologic disorder research, including leprosy, dermatitis herpetiformis, acne vulgaris et al.
|
-
- HY-12354
-
|
SB-3CT
|
MMP
|
Cancer
|
|
SB-3CT is a potent and competitive matrix metalloproteinase MMP-2 and MMP-9 inhibitor with Ki values of 13.9 and 600 nM, respectively. SB-3CT has high selectivity for gelatinases. SB-3CT shows blood-brain barrier permeability and has neuroprotective effects and anticancer activity.
|
-
- HY-50754
-
|
gamma-secretase modulator 2
|
γ-secretase
|
Neurological Disease
|
|
gamma-secretase modulator 2 is a potent and selective γ-secretase modulator for treatment of Alzheimer's disease
IC50 value:
Target: γ-secretase
γ-secretase modulator is modulation of the action of γ-secretase so as to Selectively attenuate production of Aβ(1-42) and hence find use in treatment or prevention of diseases associated with deposition of Aβ in the brain.
|
-
- HY-W094758A
-
|
4-Di-1-ASP
|
Fluorescent Dye
|
Cancer
|
|
4-Di-1-ASP is a styryl dye used to stain glioma cells in living brain tissue for analysis of cell structure, viability, proliferation and endocytosis, cytokinesis and phagocytosis, as well as for observation of mitochondrial structures in living cells. 4-Di-1-ASP fluoresces green when imaged microscopically (λex /λem = 475/606 nm) .
|
-
- HY-132670S
-
|
(R)-(-)-Felodipine-d5
|
Calcium Channel
Autophagy
|
Cardiovascular Disease
|
|
(R)-(-)-Felodipine-d5 is the deuterium labeled (R)-(-)-Felodipine. (R)-(-)-Felodipine is the S enantiomer of Felodipine. Felodipine, a dihydropyridine, is a potent, vasoselective calcium channel antagonist. Felodipine lowers blood pressure (BP) by selective action on vascular smooth muscle, especially in the resistance vessels. Felodipine, an anti-hypertensive agent, induces autophagy. Felodipine can cross the blood-brain barrier[1][2][3].
|
-
- HY-100822
-
|
(R)-(+)-HA-966
(+)-HA-966
|
iGluR
|
Neurological Disease
|
|
(R)-(+)-HA-966 ((+)-HA-966) is a partial agonist/antagonist of glycine site of the N-methyl-D-aspartate (NMDA) receptor complex. (R)-(+)-HA-966 selectively blocks the activation of the mesolimbic dopamine system by amphetamine. (R)-(+)-HA-966 can cross the blood-brain barrier and has the potential for neuropathic and acute pain.
|
-
- HY-12439
-
|
ML380
|
mAChR
|
Neurological Disease
|
|
ML380 is a potent, subtype-selective, and brain-penetrant positive allosteric modulator (PAM) of M5 mAChR, with EC50s of 190 and 610 nM for human and rat M5, respectively. ML380 exhibits moderate selectivity versus the M1 and M3 mAChR subtypes. ML380 could increase the affinity of ACh for the M5 mAChR.
|
-
- HY-120645
-
|
BMS-986122
|
Opioid Receptor
|
Neurological Disease
|
|
BMS-986122 is a selective, potent positive allosteric modulator of the mu-opioid receptor (µ-OR). BMS-986122 shows potentiation of orthosteric agonist-mediated β-arrestin recruitment, adenylyl cyclase inhibition, and G protein activation. BMS-986122 potentiates DAMGO-mediated [ 35S]GTPγS binding in mouse brain membranes.
|
-
- HY-104077S
-
|
Remdesivir-d5
GS-5734-d5
|
DNA/RNA Synthesis
SARS-CoV
|
Infection
|
|
Remdesivir-d5 is a deuterium labeled Remdesivir. Remdesivir (GS-5734) is a nucleoside analogue, with effective antiviral activity, with EC50s of 74 nM for SARS-CoV and MERS-CoV in HAE cells, and 30 nM for murine hepatitis virus in delayed brain tumor cells. Remdesivir is highly effective in the control of 2019-nCoV (COVID-19) infection in vitro[1][2].
|
-
- HY-19578B
-
|
Isamoltane hemifumarate
|
5-HT Receptor
Adrenergic Receptor
|
Neurological Disease
|
|
Isamoltane hemifumarate is a selective antagonist of 5-HT1B receptor, with an IC50 of 39 nM for inhibits the binding of [ 125I]ICYP to 5-HT1B recognition sites in rat brain membranes. Isamoltane hemifumarate is also a β-adrenoceptor ligand, with an IC50 of 8.4 nM. Isamoltane hemifumarate shows anxiolytic activity.
|
-
- HY-145845
-
|
HDAC1/MAO-B-IN-1
|
HDAC
Monoamine Oxidase
|
Neurological Disease
|
|
HDAC1/MAO-B-IN-1 is a potent, selective and cross the blood-brain barrier HDAC1/MAO-B inhibitor with IC50 values of 21.4 nM and 99.0 nM for HDAC1 and MAO-B, respectively. HDAC1/MAO-B-IN-1 has the potential for the research of Alzheimer’s disease.
|
-
- HY-111544
-
|
EML741
|
Histone Methyltransferase
|
Cancer
|
|
EML741 is a histone lysine methyltransferase G9a/GLP inhibitor, with an IC50 of 23 nM, Kd of 1.13 μM for G9a. EML741 also inhibits DNMT1 (IC50, 3.1 μM), with no effect on DNMT3a or DNMT3b. EML741 exhibits low cell toxicity, and is membrane permeable and blood-brain barrier penetrated.
|
-
- HY-145949
-
|
Remdesivir de(ethylbutyl 2-aminopropanoate)
|
Drug Metabolite
|
Infection
|
|
Remdesivir de(ethylbutyl 2-aminopropanoate) is an impurity of Remdesivir. Remdesivir, a nucleoside analogue with effective antiviral activity, has EC50s of 74 nM for SARS-CoV and MERS-CoV in HAE cells, and 30 nM for murine hepatitis virus in delayed brain tumor cells. Remdesivir is highly effective in the control of SARS-CoV-2 (COVID-19) infection in vitro.
|
-
- HY-111540A
-
|
(Rac)-IDO1-IN-5
|
Indoleamine 2,3-Dioxygenase (IDO)
|
Cancer
|
|
(Rac)-IDO1-IN-5 (Example 1) is a racemate of IDO1-IN-5. IDO1-IN-5 is a potent, selective and brain penetrated inhibitor of Indoleamine 2,3-Dioxygenase 1 (IDO1) activity, binds to apo-IDO1 lacking heme rather than mature heme-bound IDO1.
|
-
- HY-14552
-
|
Talnetant
SB 223412
|
Neurokinin Receptor
|
Neurological Disease
Endocrinology
|
|
Talnetant (SB 223412) is a selective, competitive, brain-permeable NK3 receptor antagonist with a Ki of 1.4 nM in hNK-3-CHO cells. Talnetant is 100-fold more selective for hNK-3 relative to the hNK-2 receptor and has no affinity for hNK-1. Talnetant can be used in schizophrenia-related studies.
|
-
- HY-10510
-
-
- HY-101988S
-
-
- HY-12098
-
|
Verubulin hydrochloride
MPC-6827 hydrochloride
|
Microtubule/Tubulin
|
Cancer
|
|
Verubulin hydrochloride (MPC-6827 hydrochloride) is a blood brain barrier permeable microtubule-disrupting agent, with potent and broad-spectrum in vitro and in vivo cytotoxic activities. Verubulin hydrochloride (MPC-6827 hydrochloride) exhibits potent anticancer activity in human MX-1 breast and other mouse xenograft cancer models. Verubulin hydrochloride (MPC 6827 hydrochloride) is a promising candidate for the treatment of multiple cancer types.
|
-
- HY-146315
-
|
AChE/BChE-IN-6
|
Cholinesterase (ChE)
Monoamine Oxidase
|
Neurological Disease
|
|
AChE/BChE-IN-6 (compound 22) is a potent dual AChE/BChE inhibitor with IC50 values of 0.809 µM, 2.248 µM and > 100 µM for hBChE, hAChE and hMAO-B, respectively. AChE/BChE-IN-6 penetrates the blood-brain barrier (BBB). AChE/BChE-IN-6 can be used for Alzheimer’s disease (AD) research.
|
-
- HY-125374
-
|
Larotaxel
XRP9881
|
Apoptosis
|
Cancer
|
|
Larotaxel (XRP9881) is a taxane analogue with preclinical activity against taxane-resistant breast cancer. Larotaxel (XRP9881) exerts its cytotoxic effect by promoting tubulin assembly and stabilizing microtubules, ultimately leading to cell death by apoptosis. It presents the ability to cross the blood brain barrier and has a much lower affinity for P-glycoprotein 1 than Docetaxel.
|
-
- HY-13290
-
|
KN-62
|
CaMK
P2X Receptor
|
Metabolic Disease
Cancer
|
|
KN-62 is a selective and reversible inhibitor of calmodulin-dependent protein kinase II (CaMK-II) with a Ki of 0.9 μM for rat brain CaMK-II. KN-62 directly binds to the calmodulin binding site of CaMK-II. KN-62 displays noncompetitive antagonism at P2X7 receptors in HEK293 cells, with an IC50 value of approximately 15 nM.
|
-
- HY-143245
-
|
Monoamine Oxidase B inhibitor 2
|
Monoamine Oxidase
|
Neurological Disease
|
|
Monoamine Oxidase B inhibitor 2 is a potent, reversible, orally active and selective monoamine oxidase B (MAO-B) inhibitor with an IC50 of 1.33 nM. Monoamine Oxidase B inhibitor 2 has antioxidant and anti-neuroinflammatory activities. Monoamine Oxidase B inhibitor 2 can across the blood-brain barrier (BBB), and can be used for Parkinson’s disease study.
|
-
- HY-151389
-
|
BChE-IN-14
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
BChE-IN-14 (compound 19c) is a selective butyrylcholinesterase (BChE) inhibitor with IC50s of 0.23 and 0.011 μM for eqBChE and hBChE, respectively. BChE-IN-14 shows good blood brain barrier permeation and primary cell safety. BChE-IN-14 is able to restore cognitive impairment in vivo, it can be used for the research of Alzheimer’s disease.
|
-
- HY-143244
-
|
Monoamine Oxidase B inhibitor 1
|
Monoamine Oxidase
|
Neurological Disease
|
|
Monoamine Oxidase B inhibitor 1 is a potent, reversible, orally active and selective monoamine oxidase B (MAO-B) inhibitor with an IC50 of 0.02 nM. Monoamine Oxidase B inhibitor 1 has antioxidant and anti-neuroinflammatory activities. Monoamine Oxidase B inhibitor 1 can across the blood-brain barrier (BBB), and can be used for Parkinson’s disease study.
|
-
- HY-101988S1
-
-
- HY-117709
-
|
BRD6688
|
HDAC
|
Neurological Disease
|
|
BRD6688 is a selective HDAC2 inhibitor. BRD6688 increases H4K12 and H3K9 histone acetylation in primary mouse neuronal cells. BRD6688 crosses the blood brain barrier and rescues the memory defects associated with p25 induced neurodegeneration in contextual fear conditioning in a CK-p25 mouse model.
|
-
- HY-137500
-
|
NT1-014B
|
Others
|
Neurological Disease
|
|
NT1-014B is a potent NT1-lipidoid encapsulated AmB (amphotericin B). NT1-014B dopes the NT-lipidoids into BBB-impermeable lipid nanoparticles (LNPs) gave the LNPs the ability to cross the BBB. NT1-014B enhances brain delivery through intravenous injection.
|
-
- HY-B0688S
-
|
Dapsone-d8
4,4′-Diaminodiphenyl sulfone-d8; DDS-d8
|
Antibiotic
Parasite
Bacterial
Reactive Oxygen Species
|
Cancer
Infection
Inflammation/Immunology
|
|
Dapsone-d8 is a deuterium labeled Dapsone. Dapsone is an orally active and blood-brain penetrant sulfonamide antibiotic with antibacterial, antigenic and anti-inflammatory activities[1]. Dapsone exerts effective antileprosy activity and inhibits folate synthesis in cell extracts of M. leprae. Dapsone can be used as an anticonvulsant and also in the research of skin and glioblastoma diseases[2][3][4][5].
|
-
- HY-17368
-
|
Rivastigmine
S-Rivastigmine
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
Rivastigmine (S-Rivastigmine) is an orally active and potent cholinesterase (ChE) inhibitor and inhibits butyrylcholinesterase (BChE) and acetylcholinesteras (AChE) with IC50s of 0.037 μM , 4.15 μM, respectively. Rivastigmine can pass the blood brain barrier (BBB). Rivastigmine is a parasympathomimetic or cholinergic agent used for the research of mild to moderate dementia of the Alzheimer's type and dementia due to Parkinson's disease.
|
-
- HY-B1126
-
|
Orphenadrine hydrochloride
|
iGluR
|
Neurological Disease
|
|
Orphenadrine hydrochloride is an orally active and non-competitive NMDA receptor antagonist (crosses the blood-brain barrier) with a Ki of 6.0 μM. Orphenadrine hydrochloride relieves stiffness, pain and discomfort due to muscle strains, sprains or other injuries. Orphenadrine hydrochloride is also used to relieve tremors associated with parkinson's disease. Orphenadrine citrate has good neuroprotective properties, can be used in studies of neurodegenerative diseases.
|
-
- HY-14552A
-
|
Talnetant hydrochloride
SB 223412 hydrochloride; SB 223412-A
|
Neurokinin Receptor
|
Neurological Disease
Endocrinology
|
|
Talnetant (SB 223412) hydrochloride is a selective, competitive, brain-permeable NK3 receptor antagonist with a Ki of 1.4 nM in hNK-3-CHO cells. Talnetant hydrochloride is 100-fold more selective for hNK-3 relative to the hNK-2 receptor and has no affinity for hNK-1. Talnetant hydrochloride can be used in schizophrenia-related studies.
|
-
- HY-B0113A
-
|
Omeprazole sodium
H 16868 sodium
|
Proton Pump
Autophagy
Bacterial
Phospholipase
|
Cancer
Infection
Metabolic Disease
|
|
Omeprazole sodium (H 16868 sodium), a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole sodium shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM. Omeprazole sodium also inhibits growth of Gram-positive and Gram-negative bacteria. Omeprazole is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor).
|
-
- HY-128463
-
-
- HY-137262
-
|
Protein deglycase DJ-1 against-1
|
Others
|
Neurological Disease
|
|
Protein deglycase DJ-1 against-1, a DJ-1-binding compound, dependently targets DJ1. Protein deglycase DJ-1 against-1 penetrates through the blood brain barrier (BBB). Protein deglycase DJ-1 against-1 is used as a neuroprotective agent and has the potential for Parkinson's disease research.
|
-
- HY-17387
-
|
(-)-Huperzine A
Huperzine A
|
Cholinesterase (ChE)
Apoptosis
iGluR
|
Neurological Disease
|
|
(-)-Huperzine A (Huperzine A) is an alkaloid isolated from Huperzia serrata, with neuroprotective activity. (-)-Huperzine A is a potent, highly specific, reversible and blood-brain barrier penetrant inhibitor of acetylcholinesterase (AChE), with an IC50 of 82 nM. (-)-Huperzine A also is non-competitive antagonist of N-methyl-D-aspartate glutamate (NMDA) receptor. (-)-Huperzine A is developed for the research of neurodegenerative diseases, including Alzheimer’s disease.
|
-
- HY-N2132
-
|
Flavokawain B
Flavokavain B
|
Apoptosis
|
Cancer
|
|
Flavokawain B (Flavokavain B) is a chalcone isolated from the root extracts of kava-kava plant and a potent apoptosis inducer for inhibiting the growth of various cancer cell lines. Flavokawain B (Flavokavain B) shows strong antiangiogenic activity. Flavokawain B (Flavokavain B) inhibits human brain endothelial cell (HUVEC) migration and tube formation with very low and non-toxic concentrations.
|
-
- HY-135749
-
|
BN201
|
Others
|
Inflammation/Immunology
Neurological Disease
|
|
BN201 promotes neuronal differentiation, the differentiation of precursor cells to mature oligodendrocytes (EC50 of 6.3 μM) in vitro, and the myelination of new axons (EC50 of 16.6 μM). BN201 is able to cross the blood-brain barrier by active transport and activate pathways (IGF-1 pathway) associated with the response to stress and neuron survival. BN201 has potently neuroprotective effects.
|
-
- HY-15008
-
|
L-368,899
|
Oxytocin Receptor
|
Endocrinology
|
|
L-368,899 is an orally active and selective OT (oxytocin ) receptor antagonist, with IC50s of 8.9 and 26 nM for uterus of rat and human, respectively. L-368,899 can cross the blood-brain barrier (BBB). L-368,899 inhibits oxytocin-stimulated uterine contractions in rats and can be used in study of preterm labor.
|
-
- HY-150702
-
|
MAGLi 432
|
MAGL
|
Inflammation/Immunology
Neurological Disease
|
|
MAGLi 432 is a non-covalent, potent, highly selective, and reversible MAGL inhibitor. MAGLi 432 binds with high affinity to the MAGL active site, with IC50 values of 4.2 nM (human enzyme) and 3.1 nM (mouse enzyme). MAGLi 432 can be used in the research of chronic inflammation, blood–brain barrier dysfunction, neurological disorders such as multiple sclerosis, Alzheimer’s disease and Parkinson’s disease.
|
-
- HY-100719
-
|
BRD-6929
|
HDAC
HIV
|
Infection
Cardiovascular Disease
|
|
BRD-6929 is a potent, selective brain-penetrant inhibitor of class I histone deacetylase HDAC1 and HDAC2 inhibitor with IC50 of 1 nM and 8 nM, respectively. BRD-6929 shows high-affinity to HDAC1 and HDAC2 with Ki of 0.2 and 1.5 nM, respectively. BRD-6929 can be used for mood-related behavioral model research.
|
-
- HY-17573A
-
|
Carbetocin acetate
|
Oxytocin Receptor
|
Endocrinology
Neurological Disease
|
|
Carbetocin acetate, an oxytocin (OT) analogue, is an oxytocin receptor agonist with a Ki of 7.1 nM. Carbetocin acetate has high affinity to chimeric N-terminus (E1) of the oxytocin receptor (Ki=1.17 μM). Carbetocin acetate has the potential for postpartum hemorrhage research. Carbetocin acetate can crosse the blood-brain barrier and produces antidepressant-like activity via activation of oxytocin receptors in the CNS.
|
-
- HY-114226
-
|
Olutasidenib
FT-2102
|
Isocitrate Dehydrogenase (IDH)
|
Cancer
Inflammation/Immunology
|
|
Olutasidenib (FT-2102) is a highly potent, orally active, brain penetrant and selective inhibitor of mutant Isocitrate dehydrogenase 1 (IDH1), with IC50 values of 21.2 nM and 114 nM for IDH1- R132H and IDH1- R132C, respectively . Olutasidenib (FT-2102) is under the study in the treatment of acute myeloid leukemia (AML) or myelodysplastic syndrome (MDS) .
|
-
- HY-W001601
-
|
Budipine
|
iGluR
|
Neurological Disease
|
|
Budipine is an anti-parkinson agent. Budipine also is a substrate of P-glycoprotein (P-gp), is mediated the uptake into the brain by P-gp. Budipine also is N-methyl-d-aspartate (NMDA) antagonist, and has indirect dopaminergic effects through an improved dopamine release, the inhibition of monoamine oxidase type B (MAO-B). Budipine can be used for the research of CNS disorders include Parkinson disease.
|
-
- HY-124634
-
|
PZ-2891
|
Others
|
Neurological Disease
|
|
PZ-2891 is an orally bioavailable, brain penetrant pantothenate kinase (PANK) modulator. PZ-2891 act as an orthosteric inhibitor at high concentrations and an allosteric activator at lower sub-saturating concentrations. PZ-2891 inhibits human pantothenate kinases PANK1β, PANK2, and PANK3 with IC50s of 40.2 nM, 0.7 nM and 1.3 nM, respectively.
|
-
- HY-137466
-
|
ARN-21934
|
Topoisomerase
|
Cancer
|
|
ARN-21934 is a potent, highly selective, blood-brain barrier (BBB) penetrant inhibitor for human topoisomerase II α over β. ARN-21934 inhibits DNA relaxation with an IC50 of 2 μM as compared to the anticancer agent Etoposide (IC50=120 μM). ARN-21934 exhibits a favorable in vivo pharmacokinetic profile and is a promising lead compound for anticancer research.
|
-
- HY-104077S1
-
|
Remdesivir-d4
GS-5734-d4
|
DNA/RNA Synthesis
SARS-CoV
|
Infection
|
|
Remdesivir-d4 is deuterium labeled Remdesivir. Remdesivir (GS-5734), a nucleoside analogue with effective antiviral activity, has EC50s of 74 nM for SARS-CoV and MERS-CoV in HAE cells, and 30 nM for murine hepatitis virus in delayed brain tumor cells. Remdesivir is highly effective in the control of SARS-CoV-2 (COVID-19) infection in vitro[1][2].
|
-
- HY-17573
-
|
Carbetocin
|
Oxytocin Receptor
|
Endocrinology
Neurological Disease
|
|
Carbetocin, an oxytocin (OT) analogue, is an oxytocin receptor agonist with a Ki of 7.1 nM. Carbetocin has high affinity to chimeric N-terminus (E1) of the oxytocin receptor (Ki=1.17 μM). Carbetocin has the potential for postpartum hemorrhage research. Carbetocin can crosse the blood-brain barrier and produces antidepressant-like activity via activation of oxytocin receptors in the CNS.
|
-
- HY-12248A
-
|
Telaglenastat hydrochloride
CB-839 hydrochloride
|
Glutaminase
Autophagy
|
Cancer
|
|
Telaglenastat (CB-839) hydrochloride is a first-in-class, selective, reversible and orally active glutaminase 1 (GLS1) inhibitor. Telaglenastat hydrochloride selectively inhibits GLS1 splice variants KGA (kidney-type glutaminase) and GAC (glutaminase C) compared to GLS2. The IC50s are 23 nM and 28 nM for endogenous glutaminase in mouse kidney and brain, respectively. Telaglenastat hydrochloride inudces autophagy and has antitumor activity.
|
-
- HY-10061
-
|
Lesogaberan
AZD-3355
|
GABA Receptor
|
Metabolic Disease
|
|
Lesogaberan (AZD-3355) is a potent and selective GABAB receptor agonist with an EC50 of 8.6 nM for human recombinant GABAB receptors. The affinity (Kis) of Lesogaberan for rat GABAB and GABAA receptors, as measured by displacement of [ 3H]GABA binding in brain membranes: 5.1 nM and 1.4 μM, respectively. Lesogaberan inhibits transient lower esophageal sphincter relaxation through a peripheral mode of action.
|
-
- HY-D1684
-
|
DCDAPH
|
Amyloid-β
|
Neurological Disease
|
|
DCDAPH (Compound 2c) is a novel smart NIRF probe for detection of β-amyloid (Aβ) plaques (λex/λem=597/665 nm in PBS). DCDAPH shows high affinity for Aβ aggregates (Ki=37 nM, Kd=27 nM). DCDAPH shows good blood brain barrier permeation and can meet most of the requirements for the detection of Aβ plaques both in vitro and in vivo.
|
-
- HY-147395
-
|
GPR52 agonist-1
|
Others
|
Neurological Disease
|
|
GPR52 agonist-1 is a potent, orally active and blood-brain barrier (BBB) penetrant GPR52 agonist with an pEC50 value of 7.53. GPR52 agonist-1 affects cAMP accumulation through direct interaction with GPR52. GPR52 agonist-1 can significantly suppress Methamphetamine-induced hyperactivity in mice. Antipsychotic activity.
|
-
- HY-B0369A
-
|
Orphenadrine citrate
|
iGluR
|
Neurological Disease
|
|
Orphenadrine citrate is an orally active and non-competitive NMDA receptor antagonist (crosses the blood-brain barrier) with a Ki of 6.0 μM. Orphenadrine citrate relieves stiffness, pain and discomfort due to muscle strains, sprains or other injuries. Orphenadrine citrate is also used to relieve tremors associated with parkinson's disease. Orphenadrine citrate has good neuroprotective properties, can be used in studies of neurodegenerative diseases.
|
-
- HY-12248
-
|
Telaglenastat
CB-839
|
Glutaminase
Autophagy
|
Cancer
|
|
Telaglenastat (CB-839) is a first-in-class, selective, reversible and orally active glutaminase 1 (GLS1) inhibitor. Telaglenastat selectively inhibits GLS1 splice variants KGA (kidney-type glutaminase) and GAC (glutaminase C) compared to GLS2. The IC50s are 23 nM and 28 nM for endogenous glutaminase in mouse kidney and brain, respectively. Telaglenastat inuduces autophagy and has antitumor activity.
|
-
- HY-101368A
-
|
WIN 64338 hydrochloride
|
Bradykinin Receptor
mAChR
|
Neurological Disease
|
|
WIN 64338 hydrochloride is a potent, selective, nonpeptide competitive antagonist of bradykinin B2 receptor. WIN 64338 hydrochloride inhibits [ 3H]-Bradykinin binding to the bradykinin B2 receptor on human IMR-90 cells with a Ki of 64 nM. WIN 64338 hydrochloride also can inhibits [ 3H]Quinuclidinyl benzilate binding to the rat brain muscarinic receptor (Ki=350 nM).
|
-
- HY-106004
-
|
Zamicastat
BIA 5-1058
|
Dopamine β-hydroxylase
P-glycoprotein
BCRP
|
Cancer
Cardiovascular Disease
|
|
Zamicastat (BIA 5-1058) is a dopamine β-hydroxylase (DBH) inhibitor and can cross the blood-brain barrier (BBB) to cause central as well as peripheral effects. Zamicastat is also a concentration-dependent dual P-gp and BCRP inhibitor with IC50 values of 73.8 μM and 17.0 μM, respectively. Zamicastat reduces high blood pressure.
|
-
- HY-10061B
-
|
Lesogaberan hydrochloride
AZD-3355 hydrochloride
|
GABA Receptor
|
Metabolic Disease
|
|
Lesogaberan (AZD-3355) hydrochloride is a potent and selective GABAB receptor agonist with an EC50 of 8.6 nM for human recombinant GABAB receptor. The affinity (Kis) of Lesogaberan hydrochloride for rat GABAB and GABAA receptors, as measured by displacement of [ 3H]GABA binding in brain membranes: 5.1 nM and 1.4 μM, respectively. Lesogaberan hydrochloride inhibits transient lower esophageal sphincter relaxation through a peripheral mode of action.
|
-
- HY-150639
-
|
Everafenib
|
Raf
|
Cancer
|
|
Everafenib is a potent and blood-brain barrier (BBB) penetrant BRAF inhibitor, also inhibits MAPK signaling. Everafenib has inhibitory activity against a panel of V600EBRAF melanoma cell lines with IC50 values of 2-10 nM, which is better than Dabrafenib (HY-14660) and Vemurafenib (HY-12057). Everafenib has efficacy in an intracranial mouse model of metastatic melanoma.
|
-
- HY-134188
-
|
JNJ-54717793
|
Orexin Receptor (OX Receptor)
|
Neurological Disease
|
|
JNJ-54717793, as a brain penetrant, is an orally active, selective and high affinity orexin-1 receptor (OX1R) antagonist (plasma EC50=85 ng/mL). The Ki values of JNJ-54717793 for hOX1R (human OX1R) and hOX2R are 16 nM and 700 nM, respectively. JNJ-54717793 is a potent compound of anxiety disorders.
|
-
- HY-N4190
-
|
Britannilactone diacetate
1,6-O,O-Diacetylbritannilactone; Di-O-acetylbritannilactone
|
NO Synthase
|
Inflammation/Immunology
Neurological Disease
|
|
Britannilactone diacetate (1,6-O,O-Diacetylbritannilactone; Compound 2) exhibits potential NO inhibition effect. Britannilactone diacetate exhibits activity against NO production induced by LPS in BV-2 microglial cells with the EC50 value of 6.3 μM. Britannilactone diacetate exhibits a favorable blood-brain barriers (BBB) penetration and absorption, distribution, metabolism, excretion, and toxicity (ADMET) property.
|
-
- HY-136390
-
|
ML417
|
Dopamine Receptor
|
Neurological Disease
|
|
ML417 is a selective and brain penetrant D3 dopamine receptor (D3R) agonist, with an EC50 of 38 nM. ML417 potently promotes D3R-mediated β-arrestin translocation, G protein mediated signaling, and pERK phosphorylation with minimal effects on other GPCR-mediated signaling. ML417 exhibits neuroprotection against toxin-induced neurodegeneration of dopaminergic neurons.
|
-
- HY-15121S
-
|
L-Theanine-d5
L-Glutamic Acid γ-ethyl amide-d5; Nγ-Ethyl-L-glutamine-d5
|
Apoptosis
Endogenous Metabolite
|
Neurological Disease
|
|
L-Theanine-d5 is the deuterium labeled L-Theanine. L-Theanine (L-Glutamic Acid γ-ethyl amide）is a non-protein amino acid contained in green tea leaves, which blocks the binding of L-glutamic acid to glutamate receptors in the brain, and with neuroprotective and anti-oxidative activities. L-Theanine causes anti-stress effects via the inhibition of cortical neuron excitation by oral intake[1][2][3].
|
-
- HY-B0410A
-
|
Pramipexole dihydrochloride hydrate
|
Dopamine Receptor
|
Neurological Disease
|
|
Pramipexole dihydrochloride hydrate is a selective and blood-brain barrier (BBB) penetrant dopamine D2-type receptor agonist, with Kis of 2.2 nM, 3.9 nM, 0.5 nM and 1.3 nM for D2-type receptor, D2, D3 and D4 receptors, respectively. Pramipexole dihydrochloride hydrate can be used for the research of Parkinson's disease (PD) and restless legs syndrome (RLS).
|
-
- HY-N2045
-
|
Musk ketone
|
PI3K
Akt
Apoptosis
|
Neurological Disease
|
|
Musk ketone (MK) is a widely used artificial fragrance. Musk ketone shows mutagenic and comutagenic effects in Hep G2 cells and induces neural stem cell proliferation and differentiation in cerebral ischemia via activation of the PI3K/Akt signaling pathway. In the brain, musk ketone is neuroprotective against stroke injury through inhibition of cell apoptosis.
|
-
- HY-109520
-
|
Glatiramer acetate
|
Others
|
Inflammation/Immunology
|
|
Glatiramer acetate, a synthetic analogue of myelin basic protein and an immunomodulating agent, can be used for the research of multiple sclerosis. Glatiramer acetate exhibits strong and promiscuous binding to MHC molecules and consequent competition with various myelin antigens for their presentation to T cells. A further aspect of its action is potent induction of specific suppressor cells of the T helper 2 (Th2) type that migrate to the brain and lead to in situ bystander suppression.
|
-
- HY-19918A
-
|
Anatabine dicitrate
|
NF-κB
Amyloid-β
nAChR
|
Inflammation/Immunology
Neurological Disease
|
|
Anatabine dicitrate is a tobacco alkaloid that can cross the blood-brain barrier. Anatabine dicitrate is a potent α4β2 nAChR agonist. Anatabine dicitrate inhibits NF-κB activation lower amyloid-β (Aβ) production by preventing the β-cleavage of amyloid precursor protein (APP). Anatabine dicitrate has anti-inflammatory effects and has the potential for neurodegenerative disorders treatment.
|
-
- HY-145804
-
|
AZD-9574
|
PPAR
|
Neurological Disease
|
|
AZD-9574 is a potent and brain penetrant PARP1 inhibitor and shows >8000-fold selectivity for PARP1 compared to PARP2/3/5a/6. AZD-9574 acts by selectively inhibiting and trapping PARP1 at the sites of SSBs. AZD-9574 is an anti-cancer agent and can be used for HRD + breast cancer and advanced solid malignancies research.
|
-
- HY-13863
-
|
Hydroxy-Dynasore
Dyngo-4a
|
Dynamin
|
Neurological Disease
|
|
Hydroxy Dynasore (Dyngo-4a), a structural analog of Dynasore (HY-15304), is an potency improved, low cytotoxicity and non‐specific binding dynamin inhibitor with IC50 values of 0.38 μM and 2.3 μM for brain dynamin I and recombinant rat dynamin II, respectively. Hydroxy Dynasore inhibits dynamin‐dependent endocytosis of transferrin with an IC50 of 5.7 μM in vitro.
|
-
- HY-109118A
-
|
Masupirdine mesylate
SUVN-502 mesylate
|
5-HT Receptor
|
Neurological Disease
|
|
Masupirdine mesylate (SUVN-502 mesylate) is a potent, selective, orally bioavailable, and brain penetrant 5-HT6 receptor antagonist (Ki of 2.04 nM for human 5-HT6 receptor). Masupirdine mesylate (SUVN-502 mesylate) shows high selectivity over 5-HT2A receptor and other 100 target sites, and has potential for treatment of Alzheimer's disease.
|
-
- HY-13821
-
|
Epoxomicin
BU-4061T
|
Proteasome
Apoptosis
|
Cancer
Inflammation/Immunology
|
|
Epoxomicin (BU-4061T) is an epoxyketone-containing natural product and a potent, selective and irreversible proteasome inhibitor. Epoxomicin covalently binds to the LMP7, X, MECL1, and Z catalytic subunits of the proteasome and potently inhibits primarily the chymotrypsin-like activity. Epoxomicin can cross the blood-brain barrier. Epoxomicin has strongly antitumor and anti-inflammatory activity.
|
-
- HY-107384
-
|
Asimadoline
EMD-61753
|
Opioid Receptor
|
Metabolic Disease
Inflammation/Immunology
Neurological Disease
|
|
Asimadoline (EMD-61753) is an orally active, selective and peripherally active κ-opioid agonist with IC50s of 5.6 nM (guinea pig) and 1.2 nM (human recombinant). Asimadoline has low permeability across the blood brain barrier and has peripheral anti-inflammatory actions. Asimadoline ameliorates allodynia in diabetic rats and has the potential for irritable bowel syndrome (IBS).
|
-
- HY-18679
-
|
TC-N 22A
|
mGluR
|
Neurological Disease
|
|
TC-N 22A is a potent, selective, orally active and brain-permeable mGlu4 PAM with an EC50 of 9 nM in human mGlu4-expressing BHK cells. TC-N 22A is less active (EC50>10 μM) in agonist and PAM model at mGlu 1, 2, 3, 5, and 7 receptors. TC-N 22A has the potential for research of CNS disease in vivo.
|
-
- HY-148114
-
|
MOPIPP
|
Others
|
Cancer
|
|
MOPIPP is a novel indolebased chalcone, and vacuolin-1, is a non-lethal vacuoleinducing 2-propyl analog of MOMIPP (HY-148114). MOPIPP induces cellular vacuolization and increases autophagosomes numbers. MOPIPP also triggers methuosis, and interrupts glucose uptake and glycolytic metabolism. MOPIPP can cross the blood-brain barrier and shows efficacy in suppressing tumor progression agaisnt glioblastoma cells.
|
-
- HY-107384A
-
|
Asimadoline hydrochloride
EMD-61753 hydrochloride
|
Opioid Receptor
|
Metabolic Disease
Inflammation/Immunology
Neurological Disease
|
|
Asimadoline (EMD-61753) hydrochloride is an orally active, selective and peripherally active κ-opioid agonist with IC50s of 5.6 nM (guinea pig) and 1.2 nM (human recombinant). Asimadoline hydrochloride has low permeability across the blood brain barrier and has peripheral anti-inflammatory actions. Asimadoline hydrochloride ameliorates allodynia in diabetic rats and has the potential for irritable bowel syndrome (IBS).
|
-
- HY-B0113
-
|
Omeprazole
H 16868
|
Proton Pump
Autophagy
Bacterial
Phospholipase
|
Cancer
Infection
Metabolic Disease
|
|
Omeprazole (H 16868), a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM. Omeprazole also inhibits growth of Gram-positive and Gram-negative bacteria.Omeprazole is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor).
|
-
- HY-141661
-
|
Aβ/tau aggregation-IN-1
|
Amyloid-β
|
Neurological Disease
|
|
Aβ/tau aggregation-IN-1 is a potent Aβ1-42 β-sheets formation and tau aggregation inhibitor. The KD values of Aβ/tau aggregation-IN-1 with Aβ1-42 and tau are 160 μM and 337 μM, respectively. Aβ/tau aggregation-IN-1 can permeate the blood-brain barrier.
|
-
- HY-134923
-
|
CA77.1
|
Autophagy
|
Neurological Disease
|
|
CA77.1 is a potent, brain-penetrant and orally active chaperone-mediated autophagy (CMA) activator with favorable pharmacokinetics. CA77.1 is a derivative of AR7 (HY-101106) and can increase the expression of the lysosomal receptor LAMP2A in lysosomes. CA77.1 improves behavior and neuropathology in PS19 mice model and can be used for alzheimer's disease research.
|
-
- HY-151886
-
-
- HY-N0307
-
|
Ciwujianoside B
|
Bcl-2 Family
|
Neurological Disease
|
|
Ciwujianoside B is isolated from Eleutherococcus senticosus leaf, is able to penetrate and work in the brain after the oral administration. Ciwujianoside B significantly enhances object recognition memory.
Ciwujianoside B shows radioprotective effects on the hematopoietic system in mice, which is associated with changes in the cell cycle, reduces DNA damage and down-regulates the ratio of Bax/Bcl-2 in bone marrow cells exposed to radiation.
|
-
- HY-144267
-
|
Glucosylceramide synthase-IN-2
|
Glucosylceramide Synthase (GCS)
|
Metabolic Disease
Neurological Disease
|
|
Glucosylceramide synthase-IN-2 (compound T-690) is a potent, brain-penetrant and orally active glucosylceramide synthase (GCS) inhibitor with IC50s of 15 nM and 190 nM for human GCS and mouse GCS, respectively.Glucosylceramide synthase-IN-2 exhibits noncompetitive type inhibition with C8-ceramide and UDP-glucose.Glucosylceramide synthase-IN-2 can be used for Gaucher's disease research.
|
-
- HY-17364S
-
|
Temozolomide-d3
|
DNA Alkylator/Crosslinker
Autophagy
Apoptosis
|
Cancer
|
|
Temozolomide-d3 is the deuterium labeled Temozolomide. Temozolomide (NSC 362856) is an oral active DNA alkylating agent that crosses the blood-brain barrier. Temozolomide is also a proautophagic and proapoptotic agent. Temozolomide is effective against tumor cells that are characterized by low levels of O6-alkylguanine DNA alkyltransferase (OGAT) and a functional mismatch repair system. Temozolomide has antitumor and antiangiogenic effects[1][2].
|
-
- HY-B0410
-
|
Pramipexole
|
Dopamine Receptor
|
Neurological Disease
|
|
Pramipexole is a selective and blood-brain barrier (BBB) penetrant dopamine D2-type receptor agonist, with Kis of 2.2 nM, 3.9 nM, 0.5 nM and 1.3 nM for D2-type receptor, D2, D3 and D4 receptors, respectively. Pramipexole can be used for the research of Parkinson's disease (PD) and restless legs syndrome (RLS).
|
-
- HY-105066
-
|
Davunetide
|
Microtubule/Tubulin
Amyloid-β
|
Neurological Disease
|
|
Davunetide is an eight amino acid snippet derived from activity-dependent neuroprotective protein (ADNP), a neurotrophic factor that exists in the mammalian CNS. Davunetide possesses neuroprotective, neurotrophic and cognitive protective roperties. Davunetide, a microtubule-stabilizing peptide, interacts with and stabilises neuron-specific βIII-tubulin in vitro. Davunetide penetrates the blood-brain barrier and is non-toxic. Davunetide inhibits Aβ aggregation and Aβ-induced neurotoxicity.
|
-
- HY-118858
-
|
UCPH-102
|
Others
|
Cancer
Neurological Disease
|
|
UCPH-102 is a highly selective EAAT1 inhibitor with an IC50 of 0.43 µM. UCPH-102 exhibits a specific anti-proliferative effect on T-ALL cells. UCPH-102 also shows good blood-brain permeability, which can be used in studies of amyotrophic lateral sclerosis, Alzheimer’s disease, chronic pain and obsessive compulsive disorder.
|
-
- HY-144632
-
|
Antifungal agent 22
|
Fungal
|
Infection
|
|
Antifungal agent 22 (compound D16) is a potential and orally active antifungal agent for CM (cryptococcal meningitis), with an IC50 of 0.5 μg/mL. Antifungal agent 22 can penetrate the blood-brain barrier and kill the C. neoformans H99 cells by destroying the integrity of fungal cell membranes. Antifungal agent 22 shows selective anti-Cryptococcus activity with good metabolic stability and low cytotoxicity.
|
-
- HY-106634
-
|
Mitoguazone
Methylglyoxal-bis(guanylhydrazone); MGBG; Methyl-GAG
|
HIV
Apoptosis
|
Cancer
Infection
|
|
Mitoguazone (Methylglyoxal-bis(guanylhydrazone)) is a synthetic polycarbonyl derivative with potent antineoplastic activity. Mitoguazone is a brain-penetrant and competitive S-adenosyl-methionine decarboxylase (SAMDC) inhibitor that disrupts polyamine biosynthesis. Mitoguazone induces cell apoptosis. Mitoguazone inhibits HIV DNA integration into the cellular DNA in both monocytes and macrophages. Mitoguazone has the potential for acute leukemia, Hodgkin's and non-Hodgkin's lymphoma treatment.
|
-
- HY-17355
-
|
Pramipexole dihydrochloride
|
Dopamine Receptor
|
Neurological Disease
|
|
Pramipexole dihydrochloride is a selective and blood-brain barrier (BBB) penetrant dopamine D2-type receptor agonist, with Kis of 2.2 nM, 3.9 nM, 0.5 nM and 1.3 nM for D2-type receptor, D2, D3 and D4 receptors, respectively. Pramipexole dihydrochloride can be used for the research of Parkinson's disease (PD) and restless legs syndrome (RLS).
|
-
- HY-151369
-
-
- HY-19752A
-
|
VU0357017 hydrochloride
CID-25010775
|
mAChR
|
Neurological Disease
|
|
VU0357017 hydrochloride (CID-25010775) is a potent, selective and brain-penetrant allosteric agonist of M1 muscarinic acetylcholine receptor, with an EC50 of 477 nM. VU0357017 hydrochloride is highly selective for M1 and has no activity at M2-M5 up to the highest concentrations tested (30 μM). VU0357017 hydrochloride can be used for the research of Alzheimer’s disease and schizophrenia.
|
-
- HY-P1263A
-
-
- HY-147352
-
-
- HY-P1263
-
-
- HY-141899
-
|
MK-6884
|
mAChR
|
Neurological Disease
|
|
MK-6884 is a M4 muscarinic receptor positive allosteric modulator (PAM) with a Ki value of 0.19 nM. MK-6884 can be used for the research of the neurodegenerative diseases. MK-6884 can be conveniently radiolabeled with carbon-11 and as a positron emission tomography (PET) imaging agent.
|
-
- HY-115681
-
|
(2R/S)-6-PNG
6-Prenylnaringenin
|
Calcium Channel
|
Neurological Disease
|
|
(2R/S)-6-PNG (6-Prenylnaringenin) is a potent and reversible Cav3.2 T-type Ca 2+ channels (T-channels) blocker. (2R/S)-6-PNG can penetrate the blood-brain barrier (BBB). (2R/S)-6-PNG suppresses neuropathic and visceral pain in mice.
|
-
- HY-108615
-
|
CP-316819
GPi 819
|
Others
|
Endocrinology
|
|
CP 316819 is a potent glycogen phosphorylase (GPase) inhibitor with antihyperglycemic effect (IC50 values are 17 and 34 nM against human skeletal muscle glycogen phosphorylase (huSMGPa) and liver glycogen phosphorylase (huLGPa) respectively).CP 316819 causes glycogen accumulation under normoglycemic conditions but permits glycogen utilization when glucose concentrations are low.CP-316819 prevents neuronal cell death and maintains brain electrical currents.
|
-
- HY-104077S2
-
|
Remdesivir impurity 9-d4
|
DNA/RNA Synthesis
SARS-CoV
|
Infection
|
|
Remdesivir impurity 9-d4 is deuterium labeled Remdesivir. Remdesivir (GS-5734), a nucleoside analogue with effective antiviral activity, has EC50s of 74 nM for SARS-CoV and MERS-CoV in HAE cells, and 30 nM for murine hepatitis virus in delayed brain tumor cells. Remdesivir is highly effective in the control of SARS-CoV-2 (COVID-19) infection in vitro[1][2].
|
-
- HY-12688
-
|
Succinyl phosphonate
|
Endogenous Metabolite
Reactive Oxygen Species
|
Neurological Disease
|
|
Succinyl phosphonate is an α-ketoglutarate dehydrogenase (KGDHC) inhibitor, effective inhibits (KGDHC) in muscle, bacterial, brain, and cultured human fibroblasts. Succinyl phosphonate trisodium salt is an 2-oxoglutarate dehydrogenase (OGDH) inhibitor, impairs viability of cancer cells in a cell-specific metabolism-dependent manner. Succinyl phosphonate trisodium salt inhibits the glutamate-induced ROS production in glutamate-stimulated hippocampal neurons in situ.
|
-
- HY-P3960
-
|
(Glu2)-TRH
|
Thyroid Hormone Receptor
Endogenous Metabolite
|
Neurological Disease
|
|
(Glu2)-TRH, a metabolically stable analogue of Thyrotropin-releasing hormone (TRH; HY-P0002), is a negative modulator for the cholinergic effect of TRH in the mouse brain. (Glu2)-TRH significantly attenuates TRH-induced hippocampal extracellular acetylcholine release. (Glu2)-TRH is not metabolized by thyroliberinase. (Glu2)-TRH manifests neuroprotective, antidepressant, anticonvulsant in the CNS.
|
-
- HY-11017
-
|
Rivastigmine tartrate
ENA 713; SDZ-ENA 713
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
Rivastigmine tartrate (ENA 713; SDZ-ENA 713) is an orally active and potent cholinesterase (ChE) inhibitor and inhibits butyrylcholinesterase (BChE) and acetylcholinesteras (AChE) with IC50s of 0.037 μM, 4.15 μM, respectively. Rivastigmine tartrate can pass the blood brain barrier (BBB). Rivastigmine tartrate is a parasympathomimetic or cholinergic agent used for the research of mild to moderate dementia of the Alzheimer's type and dementia due to Parkinson's disease.
|
-
- HY-119190
-
|
PF-06445974
|
Phosphodiesterase (PDE)
|
Neurological Disease
|
|
PF-06445974, a promising positron emission tomography (PET) lead, has exquisite potency at PDE4B with an IC50 <1 nM. The IC50 values are 36, 4.7 and 17 nM for PDE4D, PDE4A and PDE4C, respectively. PF-06445974 has good selectivity over PDE4D, excellent brain permeability, and a high level of specific binding in the "cold tracer" study.
|
-
- HY-B0688S1
-
|
Dapsone-d4
4,4′-Diaminodiphenyl sulfone-d4; DDS-d4
|
Antibiotic
Parasite
Bacterial
Reactive Oxygen Species
|
Infection
Inflammation/Immunology
|
|
Dapsone-d4 is the deuterium labeled Dapsone. Dapsone (4,4′-Diaminodiphenyl sulfone) is an orally active and blood-brain penetrant sulfonamide antibiotic with bacteriostatic, antimycobacterial and antiprotozoal activities[1]. Dapsone exerts effective antileprosy activity and inhibits folate synthesis in cell extracts of M. leprae. Dapsone is used for dermatologic disorder research, including leprosy, dermatitis herpetiformis, acne vulgaris et al[2][3].
|
-
- HY-104036
-
|
IDH-305
|
Isocitrate Dehydrogenase (IDH)
|
Cancer
|
|
IDH-305 is an orally available, mutant-selective and brain-penetrant IDH1 inhibitor that targets IDH1 (R132) mutation. IDH-305 exhibits greater than 200 fold selectivity for mutant IDH1 isoforms vs. WT (IC50= 27 nM (IDH1 R132H), 28 nM (IDH1 R132C), 6.14 µM (IDH1 WT)).
|
-
- HY-128656
-
|
LML134
|
Histamine Receptor
|
Neurological Disease
Endocrinology
|
|
LML134 (compound 18b) is an orally active and high selective Histamine 3 receptor (H3R) inverse agonist with Kis of 0.3 nM and 12 nM for hH3R cAMP and hH3R bdg. LML134 penetrates the brain rapidly, leading to high H3R occupancy, and disengages its target with a fast kinetic profile. LML134 has the potential for excessive sleep disorders.
|
-
- HY-108039
-
|
HE 3286
|
NF-κB
|
Metabolic Disease
Inflammation/Immunology
Neurological Disease
|
|
HE 3286 is a synthetic derivative of a natural anti-inflammatory steroid, β-AET. HE 3286 is an orally active partial NF-κB inhibitor. HE3286 reduces proinflammatory signals, including IL-6 and matrix metallopeptidase 3. HE 3286 freely penetrates the blood brain barrier in mice. HE 3286 can be used for the research of the ulcerative colitis, arthritis, experimental autoimmune encephalomyelitis.
|
-
- HY-N6022
-
|
Byakangelicin
|
Others
|
Metabolic Disease
|
|
Byakangelicin, one of the active compounds found in the roots of Angelica gigas, can serve as a modulator to improve brain accumulation of diverse active compounds (Umb, Cur, and Dox) and enhance therapeutic effects. Byakangelicin is likely to increase the expression of all PXR target genes (such as MDR1) and induce a wide range of drug-drug interactions. Byakangelicin can inhibit the effects of sex hormones, it may increase the catabolism of endogenous hormones.
|
-
- HY-144607
-
|
Mu opioid receptor antagonist 2
|
Opioid Receptor
|
Neurological Disease
|
|
Mu opioid receptor antagonist 2 (compound 25) is a potent, selective and blood-brain barrier (BBB) penetrant μ opioid receptor (MOR) antagonist with a Ki of 0.37 nM and an EC50 of 0.44 nM. Mu opioid receptor antagonist 2 has remarkable CNS antagonism against morphine, and precipitated fewer withdrawal symptoms than Naloxone. Mu opioid receptor antagonist 2 can be used for researching opioid use disorders (OUD).
|
-
- HY-10061A
-
|
Lesogaberan napadisylate
AZD-3355 napadisylate
|
GABA Receptor
|
Metabolic Disease
|
|
Lesogaberan (AZD-3355) napadisylate is a potent and selective GABAB receptor agonist with an EC50 of 8.6 nM for human recombinant GABAB receptors. The affinity (Kis) of Lesogaberan napadisylate for rat GABAB and GABAA receptors, as measured by displacement of [ 3H]GABA binding in brain membranes: 5.1 nM and 1.4 μM, respectively. Lesogaberan napadisylate inhibits transient lower esophageal sphincter relaxation through a peripheral mode of action.
|
-
- HY-103441
-
|
JNJ28871063 hydrochloride
|
EGFR
|
Cancer
|
|
JNJ28871063 hydrochloride is an orally active, highly selective and ATP competitive pan-ErbB kinase inhibitor with IC50 values of 22 nM, 38 nM, and 21 nM for ErbB1, ErbB2, and ErbB4, respectively. JNJ28871063 hydrochloride inhibits phosphorylation of functionally important tyrosine residues in both EGFR and ErbB2. JNJ28871063 hydrochloride crosses the blood-brain barrier and has antitumor activity in human tumor xenograft models that overexpress EGFR and ErbB2.
|
-
- HY-147056
-
|
PKRA83
PKRA7
|
Others
|
Cancer
|
|
PKRA83 (PKRA7) is a potent prokineticin (PK2) antagonist, which can compete for the binding of PK2 to its receptors PKR1 and PKR2. PKRA83 potently inhibits PK2 receptors, with IC50 values of 5.0 nM and 8.2 nM for PKR1 and PKR2, respectively. PKRA83 has anticancer and anti-angiogenic activities. PKRA83 can penetrate the blood-brain barrier.
|
-
- HY-110160
-
|
Pozanicline dihydrochloride
ABT-089 dihydrochloride
|
nAChR
|
Neurological Disease
|
|
Pozanicline dihydrochloride (ABT-089 dihydrochloride) is an orally bioavailable nicotinic acetylcholine receptor (nAChR) agonist with a Ki of 16.7 nM for binding to [ 3H]cytisine sites. Pozanicline is an α4β2-selective nAChR agonist, which binds to rat brain α4β2 nAChR with a Ki of 17 nM while binding to α7 nAChR is insignificant.
|
-
- HY-125469
-
|
ICA-105665
PF-04895162
|
Potassium Channel
|
Neurological Disease
|
|
ICA-105665 (PF-04895162) is a potent and orally active neuronal Kv7.2/7.3 and Kv7.3/7.5 potassium channels opener. ICA-105665 inhibits liver mitochondrial function and bile salt export protein (BSEP) transport (IC50 of 311 μM). ICA-105665 can penetrate the blood-brain barrier and has antiseizure effects.
|
-
- HY-129624A
-
|
Bisindolylmaleimide VIII acetate
Ro 31-7549 acetate; Bis VIII acetate
|
PKC
Apoptosis
|
Cancer
Inflammation/Immunology
|
|
Bisindolylmaleimide VIII acetate (Ro 31-7549 acetate) is a potent and selective protein kinase C (PKC) inhibitor with an IC50 of 158 nM for rat brain PKC. Bisindolylmaleimide VIII acetate has IC50s of 53, 195, 163, 213, and 175 nM for PKC-α, PKC-βI, PKC-βII, PKC-γ, PKC-ε, respectively. Bisindolylmaleimide VIII acetate facilitates Fas-mediated apoptosis and inhibits T cell-mediated autoimmune diseases.
|
-
- HY-100604
-
|
JNJ-40418677
|
γ-secretase
Amyloid-β
|
Neurological Disease
|
|
JNJ-40418677 is an orally active modulator of γ-secretase, can cross the blood-brain barrier. JNJ-40418677 inhibits Aβ42 and NS2B-NS3 protease, with IC50s of 200 nM and 3.9 μM, respectively. JNJ-40418677 displays good biological tolerance, can be use for Alzheimer’s disease research.
|
-
- HY-13240
-
|
LY2886721
|
Beta-secretase
|
Neurological Disease
|
|
LY2886721 is a potent, selective and orally active beta-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor with an IC50 of 20.3 nM for recombinant human BACE1. LY2886721 is selectivity against cathepsin D, pepsin, and renin, but lacking selectivity against BACE2 (IC50 of 10.2 nM). LY2886721 can across blood-brain barrier and has the potential for Alzheimer's disease treatment.
|
-
- HY-12868
-
|
Bimiralisib
PQR309
|
PI3K
mTOR
|
Cancer
|
|
Bimiralisib (PQR309) is a potent, brain-penetrant, orally bioavailable, pan-class I PI3K/mTOR inhibitor with IC50s of 33 nM, 451 nM, 661 nM, 708 nM and 89 nM for PI3Kα, PI3Kδ, PI3Kβ, PI3Kγ and mTOR, respectively. Bimiralisib is an mTORC1 and mTORC2 inhibitor.
|
-
- HY-16785
-
|
Veledimex
INXN-1001; RG-115932
|
Interleukin Related
|
Cancer
Inflammation/Immunology
|
|
Veledimex (INXN-1001), a synthetic analog of the insect molting hormone ecdysone, is an orally active activator ligand for a proprietary gene therapy promoter system. Veledimex can be used to activate certain genes using the ecdysone receptor (EcR)-based inducible gene regulation system, the RheoSwitch Therapeutic System (RTS). Veledimex can cross blood-brain barrier (BBB) in both orthotopic GL-261 mice and cynomolgus monkeys.
|
-
- HY-146077
-
-
- HY-152671
-
|
hMAO-B-IN-4
|
Monoamine Oxidase
|
Neurological Disease
|
|
hMAO-B-IN-4 (compound B10) is a selective, reversible and blood–brain barrier (BBB) penetrable human monoamine oxidase-B (hMAO-B) inhibitor with an IC50 value and a Ki value of 0.067 and 0.03 μM, respectively. hMAO-B-IN-4 inhibits hMAO-A with an IC50 value of 33.82 μM. hMAO-B-IN-4 can be used for Alzheimer’s disease (AD) and Parkinson’s disease (PD) research.
|
-
- HY-17368S1
-
|
(rac)-Rivastigmine-d6
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
(rac)-Rivastigmine-d6 is a labelled racemic Rivastigmine. Rivastigmine (S-Rivastigmine) is an orally active and potent cholinesterase (ChE) inhibitor and inhibits butyrylcholinesterase (BChE) and acetylcholinesteras (AChE) with IC50s of 0.037 μM , 4.15 μM, respectively. Rivastigmine can pass the blood brain barrier (BBB). Rivastigmine is a parasympathomimetic or cholinergic agent used for the research of mild to moderate dementia of the Alzheimer's type and dementia due to Parkinson's disease[1][2].
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- HY-136569
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DSR-141562
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Phosphodiesterase (PDE)
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Neurological Disease
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DSR-141562 is a novel, orally active, and selective brain-penetrant phosphodiesterase 1 (PDE1) inhibitor. DSR-141562 shows preferential selectivity for human PDE1B with an IC50 of 43.9 nM, and the IC50 values for human PDE1A and 1C are 97.6 and 431.8 nM, respectively. DSR-141562 can be used for the study of positive symptoms, negative symptoms and cognitive impairments associated with schizophrenia.
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- HY-152026
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NADPH oxidase-IN-1
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NADPH Oxidase
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Neurological Disease
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NADPH oxidase-IN-1 is an orally active NADPH oxidase (Nox) inhibitor, related with neuronal inflammation. NADPH oxidase-IN-1 can cross the blood-brain barrier (BBB), inhibits Nox2 and Nox4 with IC50s of 1.9 μM and 2.47 μM, respectively. NADPH oxidase-IN-1 suppresses pro-inflammatory cytokines production and LPS-mediated microglial migration, also has in vivo efficacy.
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- HY-14327
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FAUC 213
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Dopamine Receptor
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Neurological Disease
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FAUC 213 is an orally active and highly selective dopamine D4 receptor complete antagonist with a Ki of 2.2 nM for hD4.4. FAUC 213 has less activity on D2 and D3 receptors (Kis of 3.4 μM, 5.3 μM for hD2, hD3, respectively). FAUC 213 can cross the blood-brain barrier (BBB). FAUC 213 exhibits atypical antipsychotic characteristic.
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- HY-17366A
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Clozapine N-oxide dihydrochloride
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mAChR
Dopamine Receptor
Drug Metabolite
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Neurological Disease
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Clozapine N-oxide dihydrochloride is a major metabolite of Clozapine and a human muscarinic designer receptors (DREADDs) agonist. Clozapine N-oxide dihydrochloride activates the DREADD receptor hM3Dq and hM4Di. Clozapine N-oxide dihydrochloride can cross the blood-brain barrier. Clozapine is a potent dopamine antagonist and also a potent and selective muscarinic M4 receptor (EC50=11 nM) agonist.
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- HY-111520
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NVS-SM2
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DNA/RNA Synthesis
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Neurological Disease
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NVS-SM2 is a potent, orally active and brain-penetrant SMN2 splicing enhancer with an EC50 of 2 nM for SMN. NVS-SM2 enhances U1-pre-mRNA association. NVS-SM2 promotes exon 7 inclusion and restores normal survival motor neuron (SMN) protein expression. NVS-SM2 can be used for spinal muscular atrophy (SMA) research.
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- HY-152142
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DN-1289
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JNK
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Neurological Disease
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DN-1289 is an orally active and selective inhibitor of dual leucine zipper kinase (DLK; IC50=17 nM) and leucine zipper-bearing kinase (LZK; IC50=40 nM). DN-1289 results significant attenuation of optic nerve crush (ONC)-induced p-c-Jun in mice model. DN-1289 has excellent in vivo plasma half-life and blood-brain barrier permeability.
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- HY-17366
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Clozapine N-oxide
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mAChR
Dopamine Receptor
Drug Metabolite
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Neurological Disease
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Clozapine N-oxide is a major metabolite of Clozapine and a human muscarinic designer receptors (DREADDs) agonist. Clozapine N-oxide activates the DREADD receptor hM3Dq and hM4Di. Clozapine N-oxide can cross the blood-brain barrier. Clozapine is a potent dopamine antagonist and also a potent and selective muscarinic M4 receptor (EC50=11 nM) agonist.
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- HY-151444
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LRRK2-IN-6
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LRRK2
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Neurological Disease
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LRRK2-IN-6 (compound 22) is a potent, orally active, selective leucine rich repeat protein kinase 2 gene (LRRK2) inhibitor with IC50 values of 4.6 and 49 μM for GS LRRK2 and WT LRRK2, respectively. LRRK2-IN-6 inhibits LRRK2 Ser1292 and Ser925 autophosphorylation. LRRK2-IN-6 can cross the blood-brain barrier.
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- HY-N6947
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Lutein
Xanthophyll
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Endogenous Metabolite
Apoptosis
Reactive Oxygen Species
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Inflammation/Immunology
Neurological Disease
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Lutein (Xanthophyll) is a carotenoid with reported anti-inflammatory properties. A large body of evidence shows that lutein has several beneficial effects, especially on eye health. Lutein exerts its biological activities, including anti-inflammation, anti-oxidase and anti-apoptosis, through effects on reactive oxygen species (ROS). Lutein is able to arrive in the brain and shows antidepressant-like and neuroprotective effects. Lutein is orally active.
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- HY-B0573
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Propranolol hydrochloride
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Adrenergic Receptor
Bacterial
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Neurological Disease
Endocrinology
Cancer
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Propranolol hydrochloride is a nonselective β-adrenergic receptor (βAR) antagonist, has high affinity for the β1AR and β2AR with Ki values of 1.8 nM and 0.8 nM, respectively. Propranolol hydrochloride inhibits [ 3H]-DHA binding to rat brain membrane preparation with an IC50 of 12 nM. Propranolol hydrochloride is used for study of hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy.
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- HY-151441
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LRRK2-IN-5
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LRRK2
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Neurological Disease
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LRRK2-IN-5 (compound 25) is a potent, orally active, selective leucine rich repeat protein kinase 2 gene (LRRK2) inhibitor with IC50 values of 1.2 and 16 μM for GS LRRK2 and WT LRRK2, respectively. LRRK2-IN-5 inhibits LRRK2 Ser1292 and Ser925 autophosphorylation. LRRK2-IN-5 can cross the blood-brain barrier.
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- HY-103565
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AMN082
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mGluR
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Neurological Disease
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AMN082, a selective, orally active, and brain penetrant mGluR7 agonist, directly activates receptor signaling via an allosteric site in the transmembrane domain. AMN082 potently inhibits cAMP accumulation and stimulates GTPγS binding (EC50 values, 64-290 nM) at transfected mammalian cells expressing mGluR7. AMN082 shows selectivity over other mGluR subtypes and selected ionotropic glutamate receptors. Antidepressant effects.
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- HY-B0573B
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Propranolol
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Adrenergic Receptor
Bacterial
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Neurological Disease
Cardiovascular Disease
Endocrinology
Cancer
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Propranolol is a nonselective β-adrenergic receptor (βAR) antagonist, has high affinity for the β1AR and β2AR with Ki values of 1.8 nM and 0.8 nM, respectively. Propranolol inhibits [ 3H]-DHA binding to rat brain membrane preparation with an IC50 of 12 nM. Propranolol is used for the study of hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy.
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- HY-10063
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Ispronicline
TC-1734; ACD3480
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nAChR
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Neurological Disease
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Ispronicline (TC-1734), an orally active, brain-selective α4β2 nicotine acetylcholine receptor (nAChR) partial agonist, has shown memory-enhancing properties in rodents and a good tolerability profile. Ispronicline binds to the α4β2 nAChR with high affinity (Ki=11 nM) and is highly selective to other nAChRs such as α7 nAChR and α3β4 nAChR.
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- HY-124424
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VU0071063
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Potassium Channel
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Neurological Disease
Others
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VU0071063 is a potent and specific Kir6.2/SUR1 opener (EC50=7.44 μM) and can be used for investigating Kir6.2/SUR1 expressed in the pancreas and brain. VU0071063 inhibits insulin secretion by inducing hyperpolarization of β-cell membrane potential. VU0071063 chemotype has a very steep structure-activity relationships.
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- HY-122742
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HBT1
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iGluR
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Neurological Disease
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HBT1 is a potent α-Amino-3-hydroxy-5-methyl-4-isoxazole-propionic acid (AMPA) receptor (AMPA-R) potentiator. HBT1 bonds with S518 in the ligand-binding domain (LBD) of AMPA-R in a glutamate-dependent manner. HBT1 did not show remarkable bell-shaped response in brain-derived neurotrophic factor (BDNF) production in primary neurons.
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- HY-12688A
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Succinyl phosphonate trisodium salt
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Endogenous Metabolite
Reactive Oxygen Species
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Cancer
Metabolic Disease
Neurological Disease
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Succinyl phosphonate trisodium salt is an α-ketoglutarate dehydrogenase (KGDHC) inhibitor, effective inhibits (KGDHC) in muscle, bacterial, brain, and cultured human fibroblasts. Succinyl phosphonate trisodium salt is an 2-oxoglutarate dehydrogenase (OGDH) inhibitor, impairs viability of cancer cells in a cell-specific metabolism-dependent manner. Succinyl phosphonate trisodium salt inhibits the glutamate-induced ROS production in glutamate-stimulated hippocampal neurons in situ.
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- HY-17552S
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sn-Glycero-3-phosphocholine-d9
Choline Alfoscerate-d9; Alpha-GPC-d9; L-α-GPC-d9
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Cholinesterase (ChE)
Endogenous Metabolite
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Neurological Disease
|
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sn-Glycero-3-phosphocholine-d9 is the deuterium labeled sn-Glycero-3-phosphocholine. sn-Glycero-3-phosphocholine (Choline Alfoscerate) is a precursor in the biosynthesis of brain phospholipids and increases the bioavailability of choline in nervous tissue. sn-Glycero-3-phosphocholine (Choline Alfoscerate) has significant effects on cognitive function with a good safety profile and tolerability, and is effective in the treatment of Alzheimer's disease and dementia[1][2].
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- HY-106224B
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Orexin A (human, rat, mouse) (acetate)
Hypocretin-1 (human, rat, mouse) (acetate)
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Orexin Receptor (OX Receptor)
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Neurological Disease
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Orexin A (Hypocretin-1) (human, rat, mouse) acetate is a hypothalamic neuropeptide with analgesic properties (crosses the blood-brain barrier). Orexin A (human, rat, mouse) acetate is also an OX1R agonist that induces the expression of BDNF and TH proteins in SH-SY5Y cells in a time- and dose-dependent manner. Orexin A (human, rat, mouse) acetate can be used in studies of appetite regulation, neurodegenerative diseases and modulation of injurious messaging.
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- HY-W018643
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Ferulic acid methyl ester
Methyl ferulate
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p38 MAPK
Autophagy
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Inflammation/Immunology
Neurological Disease
Cancer
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Ferulic acid methyl ester (Methyl ferulate) is a derivative of ferulic acid, isolated from Stemona tuberosa, with anti-inflammatory and antioxidant properties. Ferulic acid methyl ester is a cell membrane and brain permeable compound, shows free radical scavenging ability, used in the research of neurodegenerative disorders. Ferulic acid methyl ester inhibits COX-2 expression, blocks p-p38 and p-JNK in primary bone marrow derived-macrophages.
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- HY-150407
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TSPO ligand-1
|
Ligands for Target Protein for PROTAC
Autophagy
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Cancer
Neurological Disease
Others
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|
TSPO ligand-1 is the ligand of AUTAC4 (HY-134640) that can be used in the synthesis of PROTACs. TSPO ligand-1 is a mitochondrial outer membrane transmembrane structural domain protein can bind to AUTAC4 and regulate mitochondrial autophagy to promote targeted mitochondrial renewal. TSPO ligand-1 is also involved in the transport of cholesterol from the outer to inner mitochondrial membrane and serves as a sensitive biomarker of brain injury and neurodegeneration.
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- HY-147720A
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γ-Secretase modulator 11 hydrochloride
|
γ-secretase
|
Neurological Disease
|
|
γ-Secretase modulator 11 hydrochloride (compound 1o) is a potent and orally active γ-secretase modulator with an IC50 of 0.029 µM. γ-Secretase modulator 11 hydrochloride induces a robust reduction in brain Aβ42 levels. γ-Secretase modulator 11 hydrochloride rescues cognitive deficits exhibited by AD model mice. γ-Secretase modulator 11 hydrochloride has the potential for the research of alzheimer's disease.
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- HY-144825
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