Search Result
Results for "
diseases
" in MCE Product Catalog:
9627
Inhibitors & Agonists
117
Biochemical Assay Reagents
977
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
-
- HY-P4040
-
-
- HY-147108
-
-
- HY-137431A
-
(R)-Asundexian
(R)-BAY-2433334
|
Others
|
Cardiovascular Disease
|
(R)-Asundexian ((R)-BAY-2433334) is the enantiomer of Asundexian (HY-137431). (R)-Asundexian can be used in studies of cardiovascular disease (especially thrombotic or thromboembolic disease), edema, and ophthalmic disease.
|
-
- HY-122105
-
-
- HY-153427
-
Tau protein aggregation-IN-1
|
Tau Protein
|
Neurological Disease
|
Tau protein aggregation-IN-1 (Compound 0c) is a Tau protein aggregation inhibitor. Tau protein aggregation-IN-1 can be used in the study of protein folding disorders such as Alzheimer's disease, dementia, Parkinson's disease, Huntington's disease and prion-based spongiform encephalopathies.
|
-
- HY-132594
-
-
- HY-118284
-
Vicagrel
|
P2Y Receptor
|
Cardiovascular Disease
|
Vicagrel is a potent, safe and orally active antiplatelet agent, which works by irreversibly inhibiting P2Y12 receptor. Vicagrel can be used for the research of blood clots in coronary artery disease, peripheral vascular disease, and cerebrovascular disease.
|
-
- 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-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-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-107337
-
-
- HY-P99356
-
Cinpanemab
BIIB054; Anti-Alpha-synuclein Reference Antibody (cinpanemab)
|
α-synuclein
|
Neurological Disease
|
Cinpanemab (BIIB054) is a human-derived monoclonal antibody that binds to α-synuclein. Cinpanemab can be used for the research of Parkinson's disease.
|
-
- HY-147240
-
-
- HY-40294
-
Indazole
|
Monoamine Oxidase
GSK-3
LRRK2
|
Cancer
Neurological Disease
Cardiovascular Disease
|
Indazole, also called isoindazole, a heterocyclic aromatic organic compound. Its derivatives display a broad variety of biological activities including anti-inflammatory, antibacterial, anti-HIV, antiarrhythmic, antifungal and antitumour properties. Indazole and its derivatives can be used for research of cancer, neurological disorders, cardiovascular diseases, gastrointestinal diseases.
|
-
- HY-147579
-
Axl-IN-12
|
TAM Receptor
|
Cancer
Infection
Inflammation/Immunology
|
Axl-IN-12 (Example 2) is a potent AXL inhibitor. Axl-IN-12 can be used for the research of proliferative diseases, autoimmune diseases, allergic diseases, inflammatory diseases, transplant rejection, cancers, viral infectious diseases or other diseases of mammals.
|
-
- HY-147578
-
Axl-IN-11
|
TAM Receptor
|
Cancer
Infection
Inflammation/Immunology
|
Axl-IN-11 (Example 1) is a potent AXL inhibitor. Axl-IN-11 can be used for the research of proliferative diseases, autoimmune diseases, allergic diseases, inflammatory diseases, transplant rejection, cancers, viral infectious diseases or other diseases of mammals.
|
-
- HY-145584
-
-
- HY-150018
-
N-Demethyl MK-6884
|
mAChR
|
Neurological Disease
|
N-Demethyl MK-6884 (compound 34) is a potent M4 mAChR allosteric modulator. N-Demethyl MK-6884 can be used in the studies of alzheimer's disease and other diseases mediated by the M4 mAChR.
|
-
- HY-90009B
-
-
- HY-121340
-
-
- 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-B1680
-
-
- HY-103499
-
-
- HY-135601
-
-
- HY-144399
-
CD33 splicing modulator 1
|
Others
|
Neurological Disease
|
CD33 splicing modulator 1 (Compound 1) is a CD33 splicing modulator. CD33/Siglec 3 is a myeloid lineage cell surface receptor that is known to regulate microglia activity. CD33 splicing modulator 1 increases exon 2 skipping in cellular mRNA pools. CD33 splicing modulator 1 has the potential for the research of neurodegenerative disease including Alzheimer's disease.
|
-
- HY-144399A
-
CD33 splicing modulator 1 hydrochloride
|
Others
|
Neurological Disease
|
CD33 splicing modulator 1 (Compound 1) hydrochloride is a CD33 splicing modulator. CD33/Siglec 3 is a myeloid lineage cell surface receptor that is known to regulate microglia activity. CD33 splicing modulator 1 hydrochloride increases exon 2 skipping in cellular mRNA pools. CD33 splicing modulator 1 hydrochloride has the potential for the research of neurodegenerative disease including Alzheimer's disease.
|
-
- HY-144682
-
O-GlcNAcase-IN-4
|
Others
|
Neurological Disease
|
O-GlcNAcase-IN-4 is a O-GlcNAcase inhibitor extracted from patent WO2018140299A1 Formulaic Ic. O-GlcNAcase-IN-4 can be used for the research of neurodegenerative diseases and disorders, such as Alzheimer's disease.
|
-
- HY-105545
-
Dexetimide
(+)-Benzetimide; (S)-(+)-Dexetimide; Dexbenzetimide
|
mAChR
|
Neurological Disease
|
Dexetimide ((+)-Benzetimide; (S)-(+)-Dexetimide; Dexbenzetimide) is a piperidine anticholinergic and a high-affinity muscarinic receptor antagonist. Dexetimide can be used in studies of parkinson's disease.
|
-
- HY-123176
-
-
- HY-115919
-
-
- HY-100411
-
MLi-2
|
LRRK2
|
Neurological Disease
|
MLi-2 is an orally active and highly selective LRRK2 inhibitor with an IC50 of 0.76 nM. MLi-2 has the potential for Parkinson’s disease.
|
-
- HY-147233
-
-
- HY-147296
-
-
- HY-P1362A
-
β-Amyloid (42-1), human TFA
Amyloid β Peptide (42-1)(human) TFA
|
Amyloid-β
|
Neurological Disease
|
β-Amyloid (42-1), human TFA is the inactive form of Amyloid β Peptide (1-42). β-Amyloid (42-1), human TFA is a 42-amino acid peptide which plays a key role in the pathogenesis of Alzheimer disease.
|
-
- HY-121949
-
U-0521
|
Others
|
Neurological Disease
|
U-0521 is the inhibitor of the catechol-O-methyltransferase (COMT). U-0521 has the potential for the research of Parkinson's disease.
|
-
- HY-144776
-
NAT
|
NAMPT
|
Neurological Disease
Cancer
|
NAT is an initial hit of NAMPT activator. NAMPT is the rate-limiting enzyme in the NAD salvage pathway, which makes it an attractive target for the research of many diseases associated with NAD exhaustion such as neurodegenerative diseases.
|
-
- HY-B1786A
-
-
- HY-147134
-
-
- HY-132821A
-
-
- HY-113969
-
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline
|
Endogenous Metabolite
|
Neurological Disease
|
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline (compound 11), a tetrahydroisoquinoline (THIQ) derivative, is a selective phenylethanolamine N-methyltransferase (PNMT) inhibitor with a Ki value of 0.3 μM. 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline can be used in research on psychiatric disorders related to Alzheimer's disease and Parkinson's disease.
|
-
- HY-144764
-
-
- HY-132821
-
-
- HY-19490A
-
(S)-VQW-765
(S)-AQW-051
|
nAChR
|
Neurological Disease
|
(S)-VQW-765 ((S)-AQW-051) is an orally active, selective and effective α7 nicotinic ACh receptor (nAChR) partial agonist. (S)-VQW-765 has potential applications in cognitive disorders related to neurological diseases, such as Alzheimer's disease or schizophrenia.
|
-
- HY-147576
-
Axl-IN-9
|
TAM Receptor
|
Cancer
Inflammation/Immunology
|
Axl-IN-9 (Example 10) is a potent AXL inhibitor, with an IC50 of 26 nM. Axl-IN-9 has excellent transmembrane properties. Axl-IN-9 exhibits excellent pharmacokinetic properties in an animal body. Axl-IN-9 can be used for the research of proliferative diseases, autoimmune diseases, allergic diseases, inflammatory diseases, transplant rejection, cancer, or other diseases in mammals.
|
-
- HY-147577
-
Axl-IN-10
|
TAM Receptor
|
Cancer
Inflammation/Immunology
|
Axl-IN-10 (Example 1) is a potent AXL inhibitor, with an IC50 of 5 nM. Axl-IN-10 has excellent transmembrane properties.Axl-IN-10 exhibits excellent pharmacokinetic properties in an animal body. Axl-IN-10 can be used for the research of proliferative diseases, autoimmune diseases, allergic diseases, inflammatory diseases, transplant rejection, cancer, or other diseases in mammals.
|
-
- HY-147976
-
-
- HY-W040146
-
-
- HY-148108
-
-
- HY-122908
-
Atuliflapon
AZD5718
|
FLAP
|
Cardiovascular Disease
|
Atuliflapon (AZD5718) is an orally active inhibitor of FLAP (5‑Lipoxygenase activating protein), with an IC50 of 2 nM. Atuliflapon is used in the study for coronary artery disease.
|
-
- HY-N7745
-
Glucosylsphingosine
Glucopsychosine; Lyso-Gb1
|
Others
|
Metabolic Disease
|
Glucosylsphingosine (lyso-Gb1) is a deacylated form of glucosylceramide and is also degraded by the glucocerebrosidase. Glucosylsphingosine is a very promising, reliable and specific biomarker for monitoring Gaucher disease.
|
-
- HY-152111
-
-
- 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-146068
-
AEP-IN-1
|
Others
|
Neurological Disease
|
AEP-IN-1 (Compound 13e) is a CNS agent-like non-covalent inhibitor of asparagine endopeptidase (AEP), with the IC50 of 89 nM. AEP-IN-1 can be used for the research of numerous neurological diseases such as Alzheimer’s disease (AD).
|
-
- HY-101321
-
-
- HY-146456
-
A1AR antagonist 3
|
Adenosine Receptor
|
Neurological Disease
|
A1AR antagonist 3 (compound 13) is a selective adenosine 1 (A1) receptor antagonist with Kis of 9.69 nM and 0.529 nM for human A1 and rat A1, respectively. A1AR antagonist 3 can be used for researching neurological diseases.
|
-
- HY-105170B
-
ABT-418 hydrochloride
|
nAChR
|
Neurological Disease
|
ABT-418 hydrochloride is a potent and selective agonist of nAChRs with cognitive enhancing and anxiolytic activities. ABT-418 hydrochloride activates cholinergic channel and can be used for research of Alzheimer's disease.
|
-
- HY-13410
-
Xanomeline oxalate
LY246708 oxalate
|
mAChR
|
Neurological Disease
|
Xanomeline oxalate (LY246708 oxalate) is a potent and selective muscarinic receptor agonist (SMRA) and stimulates phosphoinositide hydrolysis in vivo. Xanomeline oxalate can be used for the research of Alzheimer’s disease.
|
-
- 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-P99216
-
Ponezumab
PF-04360365; RN 1219
|
EGFR
|
Neurological Disease
|
Ponezumab (PF-04360365) is a humanised anti-amyloid IgG2 monoclonal antibody. Ponezumab reduces Aβ levels in the central nervous system and improves performance in mice in various models of learning and memory. Ponezumab can be used in study of Alzheimer's disease.
|
-
- HY-107660
-
-
- HY-151536
-
-
- HY-P3909
-
-
- HY-W015514
-
-
- HY-B1363
-
Bendroflumethiazide
Bendrofluazide
|
Others
|
Cardiovascular Disease
|
Bendroflumethiazide is an orally active diuretic. Bendroflumethiazide is an antihypertensive agent. Bendroflumethiazide has the potential for the research of arterial hypertensive disease.
|
-
- HY-101321A
-
Immepip dihydrobromide
|
Itk
|
Neurological Disease
|
Immepip dihydrobromide is a H3 agonist. Immepip dihydrobromide can reduce cortical histamine release. Immepip dihydrobromide can be used for the research of neurological diseases.
|
-
- HY-P1060
-
LPYFD-NH2
|
Amyloid-β
|
Neurological Disease
|
LPYFD-NH2, a pentapeptide, exerts some inhibitory effect on the aggregation of Aβ(1-42). LPYFD-NH2 can be used for the research of Alzheimer’s disease.
|
-
- HY-W062697
-
HTL14242
HTL0014242
|
mGluR
|
Neurological Disease
|
HTL14242 (HTL0014242) is an advanced and orally active mGlu5 NAM with a pKi and a pIC50 of 9.3 and 9.2, respectively. HTL14242 can be used for the research of parkinson’s disease.
|
-
- HY-144762
-
-
- HY-105445
-
-
- HY-128057
-
-
- HY-P1060A
-
-
- HY-145905
-
-
- HY-132821B
-
-
- HY-144681
-
LY3372689
|
Tau Protein
|
Neurological Disease
|
LY3372689 (Formulaic Ia) is an orally active O-GlcNAcase (OGA) enzyme inhibitor. LY3372689 can be used for tauopathies research, including Alzheimer’s disease.
|
-
- HY-14936
-
Sofigatran
MCC-977
|
Thrombin
|
Cardiovascular Disease
|
Sofigatran (MCC-977) is an orally active factor IIa (thrombin) inhibitor, acts as an anticoagulant. Sofigatran is used for the research of cardiovascular disease.
|
-
- HY-B0590
-
Tetrabenazine
Ro 1-9569
|
Monoamine Transporter
|
Neurological Disease
|
Tetrabenazine (Ro 1-9569) is a reversible inhibitor of the vesicular monoamine transporter VMAT2 with the Kd value of 1.34 nM. Tetrabenazine can be used for research on diseases related to hyperactive movement disorders such as Huntington's disease.
|
-
- HY-B0590E
-
Tetrabenazine mesylate
Ro 1-9569 mesylate
|
Monoamine Transporter
|
Neurological Disease
|
Tetrabenazine (Ro 1-9569) mesylate is a reversible inhibitor of the vesicular monoamine transporter VMAT2 with the Kd value of 1.34 nM. Tetrabenazine mesylate can be used for research on diseases related to hyperactive movement disorders such as Huntington's disease.
|
-
- HY-14838
-
-
- HY-N2195
-
Nootkatone
(+)-Nootkatone
|
Others
|
Neurological Disease
|
Nootkatone, a neuroprotective agent from Vitis vinifera, has antioxidant and anti-inflammatory effects. Nootkatone improves cognitive impairment in lipopolysaccharide-induced mouse model of Alzheimer's disease.
|
-
- HY-14838A
-
-
- HY-137447A
-
Pirepemat fumarate
IRL752 fumarate
|
Others
|
Neurological Disease
|
Pirepemat (IRL752) fumarate is a corticalpreferring catecholamine- and cognition-promoting agent. Pirepemat fumarate is used for the study of Parkinson's disease.
|
-
- HY-148382
-
-
- HY-112071
-
-
- HY-146478
-
A1/A3 AR antagonist 1
|
Adenosine Receptor
|
Inflammation/Immunology
Neurological Disease
|
A1/A3 AR antagonist 1 (compound 10) is a potent adenosine 1 (A1) and adenosine 3 (A3) receptor dual antagonist with Kis of 36.7 nM, 25.4 nM and 1.47 nM for human A1, human A3 and rat A1, respectively. A1/A3 AR antagonist 1 can be used for researching kidney failure, inflammatory pulmonary diseases, and Alzheimer’s disease.
|
-
- HY-148187
-
-
- HY-W027553
-
Ipidacrine
|
Cholinesterase (ChE)
|
Neurological Disease
|
2,3,5,6,7,8-Hexahydro-1H-cyclopenta[b]quinolin-9-amine is a pharmaceutically active compound which is a nootropic agent that acts as cholinesterase inhibitor and is used in research of Alzheimer disease.
|
-
- 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-148650
-
Sortilin antagonist 1
|
Neurotensin Receptor
|
Neurological Disease
|
Sortilin antagonist 1 (compound 44) is a sortilin antagonist with an IC50 value of 20 nM for inhibiting Neurotensin (NTS) binds to sortilin. Neurotensin is a sortilin ligand. Sortilin antagonist 1 can be used for the research of neurological disease.
|
-
- HY-119943
-
PF-06256142
|
Dopamine Receptor
|
Neurological Disease
|
PF-06256142 is a potent, selective, CNS-penetrant and orally active agonist of the D1 receptor, with an EC50 and Ki of 33 nM and 12 nM, respectively. PF-06256142 has the potential for the research of schizophrenia and Parkinson's disease.
|
-
- HY-137447
-
Pirepemat
IRL752
|
Others
|
Neurological Disease
|
Pirepemat (IRL752) is a corticalpreferring catecholamine- and cognition-promoting agent. Pirepemat (IRL752) is used for the study of Parkinson's disease.
|
-
- HY-151522
-
-
- 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-136311
-
NCT-504
|
Others
|
Neurological Disease
|
NCT-504 is a selective allosteric inhibitor of PIP4Kγ, with an IC50 of 15.8 μM. NCT-504 is potential for the research of Huntington's disease.
|
-
- HY-113303
-
-
- HY-144753
-
-
- HY-153279
-
-
- HY-17020A
-
-
- HY-17020
-
-
- HY-147846
-
-
- HY-151370
-
-
- HY-107922
-
Ethopropazine hydrochloride
Isothazine hydrochloride; Lysivane hydrochloride; Parsidol hydrochloride
|
Cholinesterase (ChE)
|
Neurological Disease
|
Ethopropazine (Isothazine) hydrochloride is a potent, selective BChE inhibitor and a poor AChE inhibitor. Ethopropazine hydrochloride is a phenothiazine compound with anticholinergic properties. Ethopropazine hydrochloride can be used for the research of Parkinson’s disease.
|
-
- HY-N8728
-
-
- HY-112266
-
MARK-IN-4
|
AMPK
|
Neurological Disease
|
MARK-IN-4 is a potent microtubule affinity regulating kinase (MARK) inhibitor with an IC50 of 1 nM. Inhibition of microtubule affinity regulating kinase (MARK) represents a potentially attractive means of arresting neurofibrillary tangle pathology in Alzheimer's disease.
|
-
- HY-B1084
-
Cinoctramide
|
Others
|
Others
|
Cinoctramide is an intermediate of pharmaceutical synthesis. Cinoctramide can be used for the research of autoimmune diseases.
|
-
- HY-151616
-
sEH inhibitor-10
|
Epoxide Hydrolase
|
Metabolic Disease
Inflammation/Immunology
Cardiovascular Disease
|
sEH inhibitor-10 (Compound 37) is a selective soluble epoxide hydrolase (sEH) inhibitor (IC50=0.5 μM). sEH inhibitor-10 maintains high cycloeicosatrienoic acid (EETs) levels by inhibiting sEH, thereby reducing inflammation, regulating endothelial tone, improving mitochondrial function, and reducing oxidative stress. sEH inhibitor-10 has good research potential in metabolic, renal and cardiovascular diseases.
|
-
- HY-153092
-
BI-685509
|
Others
|
Metabolic Disease
Cardiovascular Disease
|
BI-685509 is a potent and orally active sGC activator. BI-685509 restores cyclic guanosine monophosphate (cGMP) and improves functionality of nitric oxide (NO) pathways. BI-685509 can be used in research of chronic kidney disease (CKD) and diabetic kidney disease (DKD).
|
-
- HY-120419
-
PF9601N
|
Monoamine Oxidase
|
Neurological Disease
|
PF9601N, an monoamine oxidase B (MAO-B) inhibitor, possesses neuroprotective properties in several in vitro and in vivo models of Parkinson's disease (PD). PF9601N can be used for the research of neurodegenerative diseases mediated by excitotoxicity.
|
-
- HY-11070
-
-
- HY-106432A
-
Sabcomeline hydrochloride
SB-202026 hydrochloride; Memric hydrochloride
|
mAChR
|
Neurological Disease
|
Sabcomeline (SB-202026) hydrochloride is a potent and functionally selective muscarinic M1 receptor partial agonist that improve cognition. Sabcomeline hydrochloride can be used for Alzheimer's disease research.
|
-
- HY-106432
-
Sabcomeline
SB-202026; Memric
|
mAChR
|
Neurological Disease
|
Sabcomeline (SB-202026) is a potent and functionally selective muscarinic M1 receptor partial agonist that improve cognition. Sabcomeline can be used for Alzheimer's disease research.
|
-
- HY-B0203A
-
Nebivolol hydrochloride
R 065824 hydrochloride
|
Adrenergic Receptor
|
Cardiovascular Disease
Endocrinology
|
Nebivolol (R 065824) hydrochloride is an orally active beta receptor blocker and has the high beta(1)-receptor affinity.Nebivolol hydrochloride has direct vasodilator properties and adrenergic blocking characteristics. Nebivolol hydrochloride can be used for the research of kinds of diseases such as hypertension, coronary artery disease, congestive heart failure and ischemic heart disease.
|
-
- HY-B0203
-
Nebivolol
R 065824
|
Adrenergic Receptor
|
Cardiovascular Disease
Endocrinology
|
Nebivolol (R 065824) is an orally active beta receptor blocker and has the high beta(1)-receptor affinity. Nebivolol has direct vasodilator properties and adrenergic blocking characteristics. Nebivolol can be used for the research of kinds of diseases such as hypertension, coronary artery disease, congestive heart failure and ischemic heart disease.
|
-
- HY-105647
-
Ambuphylline
Bufylline
|
Phosphodiesterase (PDE)
|
Cardiovascular Disease
|
Ambuphylline (Bufylline) is a bronchodilator. Ambuphylline is a theophylline derivative possibly acting through phosphodiesterase inhibition. Ambuphylline can be used for the research of asthma and other lung diseases.
|
-
- HY-143329
-
-
- HY-142698
-
SGC agonist 2
|
Others
|
Cardiovascular Disease
|
SGC agonist 2 is a potent agonist of soluble guanylate cyclase (SGC). Soluble guanylate cyclase is a key signal transduction enzyme in the NO-sGC-cGMP signaling pathway. SGC agonist 2 has the potential for the research of cardiovascular disease (heart failure, pulmonary hypertension, angina, myocardial infarction) and fibrotic diseases (renal fibrosis, systemic sclerosis) (extracted from patent WO2021219088A1, compound 031).
|
-
- HY-103162
-
ANR94
|
Adenosine Receptor
|
Neurological Disease
|
ANR94 is a potent and selective adenosine A2A receptor (AA2AR) antagonist with an Ki of 46 nM for hAA2AR. ANR94 has the potential for the research of Parkinson's disease.
|
-
- HY-151338
-
-
- HY-145888
-
Antioxidant agent-2
|
Amyloid-β
|
Neurological Disease
|
Antioxidant agent-2 (comp 3c), an BBB-penetrated antioxidant agent and a selective metal ions chelator, presents good neuroprotective effect and hepatoprotective effect for the study of Alzheimer’s disease.
|
-
- HY-147574
-
Axl-IN-7
|
TAM Receptor
|
Cancer
Inflammation/Immunology
Cardiovascular Disease
|
Axl-IN-7 (Chemie 22) is a potent AXL inhibitor. Axl-IN-7 can be used for Axl-related diseases research, for example cancers (such as acute myeloid leukemia, melanoma, breast cancer, pancreatic cancer, and glial tumors), renal disease, immune system disorders, and cardiovascular disease.
|
-
- HY-13720
-
-
- HY-119943A
-
(Rac)-PF-06256142
|
Dopamine Receptor
|
Neurological Disease
|
(Rac)-PF-06256142 is the less effective enantiomer of PF-06256142 (HY-119943). (Rac)-PF-06256142 is an agonist of D1 receptor, with an EC50 of 107 nM. (Rac)-PF-06256142 can be used for the research of schizophrenia and Parkinson's disease.
|
-
- HY-105003
-
ST 1535
|
Adenosine Receptor
|
Neurological Disease
|
ST 1535 is a potent and orally active A2A adenosine receptor antagonist. ST 1535 shows antiparkinsonian activity and antitremorigenic effects. ST 1535 has the potential for the research of Parkinson’s disease.
|
-
- HY-148215
-
Hsp90-IN-17
|
HSP
|
Cancer
|
Hsp90-IN-17 (Example 5) is an HSP90 inhibitor that can be used in the study of proliferative diseases, such as cancer and neurodegenerative diseases.
|
-
- HY-148215A
-
Hsp90-IN-17 hydrochloride
|
HSP
|
Cancer
|
Hsp90-IN-17 (Example 5) hydrochloride is an HSP90 inhibitor that can be used in the study of proliferative diseases, such as cancer and neurodegenerative diseases.
|
-
- HY-P99452
-
Axatilimab
SNDX-6352
|
c-Fms
|
Cancer
Inflammation/Immunology
|
Axatilimab (SNDX-6352) is a humanized IgG4 antibody with high affinity to CSF-1R. Axatilimab can be used for the research of chronic graft versus host disease (cGVHD) and neoplastic diseases.
|
-
- HY-116418
-
Virodhamine
|
Endogenous Metabolite
Cannabinoid Receptor
|
Neurological Disease
|
Virodhamine is an endocannabinoid, it regulates neurotransmission by activating the cannabinoid (CB) receptors. Virodhamine is an antagonist of CB1 receptor and an agonist of CB2 receptor. Virodhamine induces megakaryocytic differentiation by triggering MAPK signaling and ROS production. Virodhamine can be used for the research of various neurological disorders such as Alzheimer's and Parkinson's diseases.
|
-
- HY-116868
-
Anecortave acetate
Anecortave
|
PAI-1
|
Cardiovascular Disease
|
Anecortave acetate is a potent ocular angiostatic agent. Anecortave acetate inhibits neovascularization which is induced by many different angiogenic factors, and increases plasminogen activator inhibitor-1 (PAI-1) mRNA expression. Anecortave acetate can be used to research ocular neovascular diseases.
|
-
- 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-117259
-
Valiltramiprosate
ALZ-801
|
Amyloid-β
|
Neurological Disease
|
ALZ-801 is a potent and orally available small-molecule β-amyloid (Aβ) anti-oligomer and aggregation inhibitor, valine-conjugated proagent of Tramiprosate with substantially improved PK properties and gastrointestinal tolerability compared with the parent compound. ALZ-801 is an advanced and markedly improved candidate for the treatment of alzheimer’s disease.
|
-
- HY-P99164
-
-
- 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-117861
-
ML198
|
Glucosidase
|
Metabolic Disease
|
ML198 is a glucocerebrosidase (GCase) modulator with an EC50 of 0.4 μM. ML198 is an activator and non-inhibitory chaperone of glucocerebrosidase. ML198 can be used for the research of Gaucher disease.
|
-
- HY-143465
-
-
- HY-N10408
-
Tripchlorolide
|
Apoptosis
Autophagy
|
Cancer
Neurological Disease
|
Tripchlorolide is a neuroprotective agent that can be found in Tripterygium wilfordii. Tripchlorolide prevents tumor growth by inducing apoptosis and autophagy. Tripchlorolide improves cognitive deficits in Alzheimer's disease.
|
-
- 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-146387
-
SIRT5 inhibitor 3
|
Sirtuin
|
Cancer
Neurological Disease
|
SIRT5 inhibitor 3 (compound 46) is a potent and competitive SIRT5 inhibitor with an IC50 value of 5.9 μM. SIRT5 inhibitor 3 can inhibit SIRT5 desuccinylation. SIRT5 inhibitor 3 can be used for researching cancer and neurodegenerative diseases.
|
-
- HY-151810
-
CYP4A11/CYP4F2-IN-2
|
Cytochrome P450
|
Metabolic Disease
|
CYP4A11/CYP4F2-IN-2 is a potent and orally active dual inhibitor of cytochrome P450 (CYP) 4A11 and CYP4F2, with IC50s of 140 nM and 40 nM, respectively. CYP4A11/CYP4F2-IN-2 has potential for the research of renal diseases.
|
-
- HY-151809
-
CYP4A11/CYP4F2-IN-1
|
Cytochrome P450
|
Metabolic Disease
|
CYP4A11/CYP4F2-IN-1 is a potent dual inhibitor of cytochrome P450 (CYP) 4A11 and CYP4F2, with IC50s of 19 nM and 17 nM, respectively. CYP4A11/CYP4F2-IN-1 has potential for the research of renal diseases.
|
-
- HY-16759
-
Verubecestat
MK-8931
|
Beta-secretase
|
Neurological Disease
|
Verubecestat (MK-8931) is an orally active, high-affinity BACE1 and BACE2 inhibitor with Ki values of 2.2 nM and 0.38 nM. Verubecestat effectively reduces Aβ40 and has the potential for Alzheimer's Disease.
|
-
- HY-146155
-
-
- HY-107509
-
LY2389575 hydrochloride
|
mGluR
|
Neurological Disease
|
LY2389575 hydrochloride is a selective and noncompetitive mGlu3 negative allosteric modulator (NAM), with an IC50 value of 190 nM. LY2389575 hydrochloride induces an increase in Mrc1 levels. LY2389575 hydrochloride also independently amplifies Amyloid beta (Aβ) toxicity and can be used in study of Alzheimer's disease.
|
-
- HY-149242
-
MAO-B-IN-20
|
Monoamine Oxidase
|
Neurological Disease
|
MAO-B-IN-20 (Compound C14) is a potent MAO-B inhibitor with an IC50 of 0.037 μM. MAO-B-IN-20 displays good metabolic stability and brain-blood barrier permeability. MAO-B-IN-20 can be used for the research of Parkinson's disease.
|
-
- 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-B0702
-
-
- HY-147608
-
-
- HY-124063
-
-
- HY-148253
-
-
- HY-U00058
-
-
- HY-14679
-
-
- 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-146386
-
SIRT5 inhibitor 2
|
Sirtuin
|
Cancer
Neurological Disease
|
SIRT5 inhibitor 2 (compound 49) is a potent SIRT5 inhibitor with an IC50 value of 2.3 μM. SIRT5 inhibitor 2 has inhibitory activity against the SIRT5-dependent desuccinylation. SIRT5 inhibitor 2 can be used for researching cancer and neurodegenerative diseases.
|
-
- HY-16482
-
Teglicar
|
Endogenous Metabolite
|
Metabolic Disease
Neurological Disease
|
Teglicar is a selective and reversible orally active liver isoform of carnitine palmitoyl-transferase 1 (L-CPT1) inhibitor with an IC50 value of 0.68 μM and a Ki value of 0.36 μM. Teglicar has a potential antihyperglycemic propert. Teglicar can be used for the research of diabetes and neurodegenerative disease including Huntington's disease (HD).
|
-
- HY-P99491
-
Camoteskimab
AVTX-007; CERC-007; MEDI 2338
|
Interleukin Related
|
Inflammation/Immunology
|
Camoteskimab (AVTX-007) is a fully human, high-affinity anti-IL-18 monoclonal antibody. Camoteskimab has the potential for the autoinflammatory diseases research, including adult-onset Still’s disease (AOSD).
|
-
- HY-133712
-
Yonkenafil
Tunodafil
|
Phosphodiesterase (PDE)
|
Neurological Disease
|
Yonkenafil (Tunodafil), a novel phosphodiesterase 5 (PDE5) inhibitor, is effective in reducing cerebral infarction, neurological deficits, edema, and neuronal damage in the infarcted area. Yonkenafil may improve cognitive function by modulating neurogenesis and has a potential therapeutic effect on Alzheimer's disease.
|
-
- HY-P3859
-
-
- HY-P1061
-
Colivelin
|
STAT
Amyloid-β
|
Neurological Disease
|
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
|
-
- HY-110135
-
NBI-31772
|
IGF-1R
|
Others
|
NBI-31772 is the potent and nonselective inhibitor of IGFBP with a Ki value of 47 nM. NBI-31772 has the potential for the research of IGF-responsive diseases.
|
-
- HY-152264
-
-
- 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-144826
-
ZDWX-25
|
GSK-3
|
Neurological Disease
|
ZDWX-25 is a highly potent GSK-3β and DYRK1A dual inhibitor with an IC50 value of 71 nM for GSK-3β. ZDWX-25 possesses significant cytotoxic activities against SH-SY5Y and HL-7702 cells. ZDWX-25 can be used for researching alzheimer's disease.
|
-
- HY-N2043
-
-
- HY-132582
-
IONIS-MAPTRx
BIIB080; ISIS 814907
|
Tau Protein
|
Neurological Disease
|
IONIS-MAPTRx (BIIB080) is the first Tau-lowering antisense oligonucleotide (ASO). IONIS-MAPTRx has the potential for the research of Alzheimer Disease. ( MCE IONIS-MAPTRx for murine use: Tau ASO-12 sequence – 5′ GCTTTTACTGACCATGCGAG 3′ )
|
-
- HY-B0757A
-
-
- HY-106392
-
-
- HY-107580
-
-
- HY-N10151
-
Notoginsenoside R3
|
Others
|
Cardiovascular Disease
|
Notoginsenoside R3 is an active principle components of P. notoginseng. Notoginsenoside R3 act as a signaling molecule that is associated with various physiological effects. P. notoginseng and its components are used as traditional Chinese medicine for cardiovascular disease.
|
-
- HY-130750
-
-
- HY-P1061A
-
Colivelin TFA
|
STAT
Amyloid-β
Apoptosis
|
Neurological Disease
|
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.
|
-
- HY-109150
-
Mesdopetam
IRL790
|
Dopamine Receptor
|
Neurological Disease
|
Mesdopetam (IRL790) is a dopamine D3 receptor antagonist (Ki=90 nM; IC50=9.8 μM for human recombinant D3 receptor) with psychomotor stabilizing properties. Mesdopetam is used for the research of motor and psychiatric complications in Parkinson disease.
|
-
- HY-P9930
-
Evolocumab
AMG 145
|
Ser/Thr Protease
|
Metabolic Disease
Cancer
|
Evolocumab (AMG 145) is a human monoclonal antibody that inhibits PCSK9. Evolocumab binds to the circulating PCSK9 protein, inhibiting it from binding to the LDLR. Evolocumab can be used for the research of hypercholesterolemia and atherosclerotic cardiovascular diseases.
|
-
- HY-101376
-
(+)-N-Allylnormetazocine hydrochloride
(+)-SKF 10047 hydrochloride; (+)-N-Allyl-N-normetazocine hydrochloride
|
Opioid Receptor
|
Neurological Disease
|
(+)-N-Allylnormetazocine ((+)-SKF 10047) hydrochloride is a benzomorphan opioid with psychotomi metic effects. (+)-N-Allylnormetazocine hydrochloride is an opioid receptor antagonist with Ki values of 300 nM and 27 μM for σ1 and σ2 opioid receptors, respectively. (+)-N-Allylnormetazocine hydrochloride can be used for the research of neurological disease.
|
-
- HY-144108
-
HCV-IN-35
|
HCV
|
Infection
|
HCV-IN-35 (Compound (R)-3h) is a potent inhibitor of HCV. HCV-IN-35 has the potential for the research infection diseases.
|
-
- HY-143721
-
SSAO inhibitor-2
|
Monoamine Oxidase
|
Metabolic Disease
Cardiovascular Disease
Inflammation/Immunology
|
SSAO inhibitor-2 (Compound 1) is a semicarbazide-sensitive amine oxidase (SSAO) inhibitor with IC50s of <10 nM, and 10-100 μM for human SSAO and MAO-A, respectively. SSAO inhibitor-3 can be used for the research of atherosclerosis, diabetes and its complications, obesity, stroke, chronic kidney disease, retinopathy, chronic obstructive pulmonary disease (COPD), autoimmune diseases, multiple sclerosis, etc.
|
-
- HY-146528
-
c-ABL-IN-3
|
Others
|
Cancer
Neurological Disease
|
c-ABL-IN-3 is a potent inhibitor of c-Abl. Activation of c-Abl has been implicated in various diseases, notably cancer. c-ABL-IN-3 has the potential for the research of neurodegenerative diseases (amyotrophic lateral sclerosis (ALS) and Parkinson’s disease (PD) and cancer (extracted from patent WO2021048567A1, compound 50).
|
-
- HY-146527
-
c-ABL-IN-2
|
Bcr-Abl
|
Cancer
Neurological Disease
|
c-ABL-IN-2 is a potent inhibitor of c-Abl. Activation of c-Abl has been implicated in various diseases, notably cancer. c-ABL-IN-2 has the potential for the research of neurodegenerative diseases (amyotrophic lateral sclerosis (ALS) and Parkinson’s disease (PD) and cancer (extracted from patent WO2020260871A1, compound 25).
|
-
- HY-146530
-
c-ABL-IN-4
|
Others
|
Cancer
Neurological Disease
|
c-ABL-IN-4 is a potent inhibitor of c-Abl. Activation of c-Abl has been implicated in various diseases, notably cancer. c-ABL-IN-4 has the potential for the research of neurodegenerative diseases (amyotrophic lateral sclerosis (ALS) and Parkinson’s disease (PD) and cancer (extracted from patent WO2021048567A1, compound 54).
|
-
- HY-101918
-
DS-1040 Tosylate
|
Others
|
Cardiovascular Disease
|
DS-1040 Tosylate is an orally active, selective inhibitor of activated thrombin-activatable fibrinolysis inhibitor (TAFIa) with IC50s of 5.92 nM and 8.01 nM for human and rat TAFIa. DS-1040 Tosylate is a fibrinolysis enhancer for thromboembolic diseases.
|
-
- HY-N6959
-
Osmundacetone
|
Reactive Oxygen Species
Apoptosis
|
Metabolic Disease
|
Osmundacetone is a natural product isolated from Osmundae Rhizoma, with neuroprotective and anti-apoptotic effects. Osmundacetone has DPPH scavenging activity and protects neurological cell from oxidative stress. Osmundacetone can be a potential agent for the research of neurodegenerative diseases.
|
-
- HY-109150A
-
Mesdopetam hemitartrate
IRL790 hemitartrate
|
Dopamine Receptor
|
Neurological Disease
|
Mesdopetam (IRL790) hemitartrate is a dopamine D3 receptor antagonist (Ki=90 nM; IC50=9.8 μM for human recombinant D3 receptor) with psychomotor stabilizing properties. Mesdopetam hemitartrate is used for the research of motor and psychiatric complications in Parkinson disease.
|
-
- HY-10979
-
AN0128
|
Bacterial
|
Infection
Inflammation/Immunology
|
AN0128 is a boron-containing antibacterial and anti-inflammatory agent. AN0128 against S. aureus, S. epidermidis, P. acnes, B. subtilis with minimum inhibitory concentration (MIC) values of 1, 0.5, 0.3, 1 μg/mL. AN0128 can be used for the research of periodontal disease and cutaneous diseases.
|
-
- HY-106616
-
Muzolimine
BAY-g 2821; Edrul
|
Others
|
Cardiovascular Disease
|
Muzolimine (BAY-g 282) is a slow and long lasting diuresis agent. Muzolimine produces a diuresis in the loop of Henle and also shows anti-hypertensive effects. Muzolimine can be used for the research of cardiovascular disease.
|
-
- HY-W015546
-
β-N-methylamino-L-alanine hydrochloride
BMAA hydrochloride; β-N-methylamino-L-alanine hydrochloride
|
Others
|
Neurological Disease
|
β-N-methylamino-L-alanine hydrochloride (BMAA hydrochloride) is a neurotoxin produced by cyanobacteria. β-N-methylamino-L-alanine hydrochloride could cause amyotrophic lateral sclerosis (ALS) and possibly other neurodegenerative diseases.
|
-
- HY-N8260
-
-
- HY-44154
-
PSB-CB5
|
Others
|
Metabolic Disease
|
PSB-CB5 is a potent and selective antagonist of GRP18. PSB-CB5 has the potential for the research of metabolic disease and obesity.
|
-
- HY-P3858
-
-
- HY-B1371
-
-
- HY-136866
-
Aβ42-IN-2
|
γ-secretase
|
Neurological Disease
|
Aβ42-IN-2 is a γ-secretase modulator extracted from patent WO2016070107, compound example 36. Aβ42-IN-2 has an IC50 of 6.5 nM for Αβ42. Aβ42-IN-2 can be used for the research of Alzheimer's disease.
|
-
- HY-143723
-
SSAO inhibitor-3
|
Monoamine Oxidase
|
Metabolic Disease
Cardiovascular Disease
Inflammation/Immunology
|
SSAO inhibitor-3 (Compound 2) is a semicarbazide-sensitive amine oxidase (SSAO) inhibitor with IC50s of <10 nM, and 0.1-10 μM for human SSAO and AOC1, respectively. SSAO inhibitor-3 can be used for the research of atherosclerosis, diabetes and its complications, obesity, stroke, chronic kidney disease, retinopathy, chronic obstructive pulmonary disease (COPD), autoimmune diseases, multiple sclerosis, etc.
|
-
- HY-151208
-
-
- HY-14431
-
Cerlapirdine
SAM-531; PF-05212365
|
5-HT Receptor
|
Neurological Disease
|
Cerlapirdine (SAM-531, PF-05212365) is a selective and potent full antagonist of the 5-hydroxytryptamine 6 (5-HT6) receptor. Cerlapirdine has the potential for researching the Alzheimer's disease.
|
-
- HY-105327
-
P11149
|
Cholinesterase (ChE)
|
Neurological Disease
|
P11149 is a competitive, BBB-penetarated weakly, orally active and selective inhibitor of AChE. P11149 exhibits an IC50 of 1.3 μM for rat BChE/AChE. P11149, a Galanthamine derivative, demonstrates central cholinergic activity, behavioral efficacy and safety. P11149 is used in the study for Alzheimer's disease.
|
-
- HY-109055
-
-
- HY-P3846
-
(Glu20)-Amyloid β-Protein (1-42)
|
Amyloid-β
|
Neurological Disease
|
(Glu20)-Amyloid β-Protein (1-42) is a slower fibrillizing variant of amyloid β-protein (Aβ). The Glu20 mutation reduces the aggregation propensity of Aβ42 and prevents accumulation of the slowly fibrillizing peptide. Amyloid β-protein is the primary component of both vascular and parenchymal amyloid deposits in Alzheimer's disease.
|
-
- HY-115494
-
Neladenoson dalanate hydrochloride
Neladenoson bialanate hydrochloride; BAY-1067197 hydrochloride
|
Adenosine Receptor
|
Cardiovascular Disease
|
Neladenoson dalanate (Neladenoson bialanate; BAY-1067197) hydrochloride is a orally active agonist precursor of partial Adenosine A1 Receptor. Neladenoson dalanate hydrochloride has a good pharmacokinetic and safety profile, can be used for the chronic heart diseases.
|
-
- HY-123353
-
Neladenoson dalanate
Neladenoson bialanate; BAY-1067197
|
Adenosine Receptor
|
Cardiovascular Disease
|
Neladenoson dalanate (Neladenoson bialanate; BAY-1067197) is a orally active agonist precursor of partial Adenosine A1 Receptor. Neladenoson dalanate has a good pharmacokinetic and safety profile, can be used for the chronic heart diseases.
|
-
- HY-P99399
-
Semorinemab
RG 6100; RO7105705; MTAU-9937A
|
Tau Protein
|
Neurological Disease
|
Semorinemab (RG 6100) is an anti-Tau humanized IgG4 monoclonal antibody, targets the N-terminal portion of the Tau protein (amino acid residues 6-23). Semorinemab binds with human Tau with a Kd value of 3.8 nM. Semorinemab can be used for the research of Alzheimer's Disease.
|
-
- HY-P1387
-
β-Amyloid (1-40) (rat)
|
Amyloid-β
Apoptosis
|
Neurological Disease
|
β-Amyloid (1-40) (rat) is a rat form of the amyloid β-peptide, which accumulates as an insoluble extracellular deposit around neurons, giving rise to the senile plaques associated with Alzheimer's disease (AD). β-Amyloid (1-40) (rat) increases 45Ca 2+ influx, induces neurodegeneration in the rat hippocampal neurons of the CA1 subfield. β-Amyloid (1-40) (rat) induces apoptosis. β-Amyloid (1-40) (rat) can be used for the research of Alzheimer's disease.
|
-
- HY-W017500
-
-
- HY-119857
-
AGK7
SIRT2 Inhibitor,Inactive Control
|
Sirtuin
|
Neurological Disease
|
AGK7 is a potent inhibitor of sirtuin 2 (SIRT2). AGK7 rescues alpha-synuclein toxicity and modified inclusion morphology in a cellular model of Parkinson's disease. AGK7 protects against dopaminergic cell death both in vitro and in a Drosophila model of Parkinson's disease.
|
-
- HY-17609
-
Difelikefalin
CR-845; FE-202845
|
Opioid Receptor
|
Neurological Disease
|
Difelikefalin (CR-845; FE-202845) is a peripherally restricted and selective agonist of kappa opioid receptor (KOR). Difelikefalin produces anti-inflammatory effects and has the potential in modulating pruritus in conditions such as chronic kidney disease.
|
-
- HY-122647
-
Valiglurax
VU0652957; VU2957
|
mGluR
|
Neurological Disease
|
Valiglurax (VU0652957) is a potent, orally active and selective mGlu4 positive allosteric modulator with EC50 values of 64.6 nM and 197 nM for hmGlu4/Gqi5 and rmGlu4 GIRK, respectively. Valiglurax is a central nervous system (CNS) penetrant. Valiglurax can be used in research of Parkinson's disease.
|
-
- HY-133589
-
-
- HY-139004
-
SGC-CK2-1
|
Casein Kinase
|
Neurological Disease
|
SGC-CK2-1 is a highly potent, ATP-competitive, and cell-active CK2 chemical probe with exclusive selectivity for both human CK2 isoforms, with IC50s of 36 and 16 nM for CK2α and CK2α′respectively in the nanoBRET assay. SGC-CK2-1 can be used for the research of neurodegenerative diseases.
|
-
- HY-N7950
-
16-Oxoalisol A
|
Others
|
Metabolic Disease
|
16-Oxoalisol A is a triterpene in Rhizoma Alismatis. Rhizoma Alismatis is a commonly used traditional Chinese medicine (TCM). Rhizoma Alismatis can be used for the research of urinary tract diseases.
|
-
- HY-P99190
-
Eldelumab
BMS-936557; MDX-1100
|
CXCR
|
Inflammation/Immunology
|
Eldelumab (BMS-936557) is a humanised anti-CXCL10 (IP-10) monoclonal antibody (IgG1 type). Eldelumab selectively binds to CXCL10 and blocks CXCL10-induced calcium flux and cell migration. Eldelumab can be used in studies of autoimmune and auto-inflammatory diseases such as rheumatoid arthritis, ulcerative colitis and crohn's disease.
|
-
- HY-B0143A
-
Niacin hydrochloride
Nicotinic acid hydrochloride; Vitamin B3 hydrochloride
|
Endogenous Metabolite
Apoptosis
|
Cancer
Metabolic Disease
Cardiovascular Disease
|
Niacin (Vitamin B3; Nicotinic acid) hydrochloride is an orally active B3 vitamin that is an essential nutrient for humans. Niacin hydrochloride plays a key role in energy metabolism, cell signaling cascades regulating gene expression and apoptosis. Niacin hydrochloride is also used in the study of cardiovascular diseases.
|
-
- HY-147584
-
BTK-IN-14
|
Btk
|
Cancer
Inflammation/Immunology
|
BTK-IN-14 is a potent inhibitor of BTK. BTK plays an important role in signaling mediated by B cell antigen receptor (BCR) and Fcγreceptor (FcγR) in B cells and myeloid cells, respectively. BTK-IN-14 has the potential for the research of related diseases, especially autoimmune diseases, inflammatory diseases or cancer (extracted from patent WO2022057894A1, compound 1).
|
-
- HY-P99292
-
Fontolizumab
HuZAF; Anti-Human IFNG Recombinant Antibody
|
IFNAR
|
Inflammation/Immunology
|
Fontolizumab (HuZAF) is a humanized monoclonal anti-IFN-gamma antibody. Fontolizumab is an immunosuppressive agent. Fontolizumab can be used in research of Crohn’s disease.
|
-
- HY-75992
-
trans-Doxercalciferol
|
VD/VDR
|
Others
|
trans-Doxercalciferol is an isomer of Doxercalciferol. Doxercalciferol is a Vitamin D2 analog, acts as an activator of Vitamin D receptor, and prevent renal disease.
|
-
- HY-146958
-
MAO-B-IN-8
|
Monoamine Oxidase
|
Neurological Disease
|
MAO-B-IN-8 is a potent reversible MAO-B inhibitor and an inhibitor of microglial production of neuroinflammatory mediator. MAO-B-IN-8 can be used for neurodegenerative disease research.
|
-
- HY-147938
-
AChE-IN-19
|
Cholinesterase (ChE)
Amyloid-β
|
Neurological Disease
|
AChE-IN-19 (compound A15) is a highly potent AChE inhibitor with an IC50 value of 0.56 μM, also inhibits Aβ aggregation. AChE-IN-19 has potent neuroprotective activities and nearly no toxicity on SH-SY5Y cells. AChE-IN-19 can be used for researching Alzheimer's disease.
|
-
- HY-116565
-
Usmarapride
SUVN-D4010
|
5-HT Receptor
|
Neurological Disease
|
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.
|
-
- HY-148475
-
-
- HY-19660
-
Inogatran
H-314-27
|
Thrombin
|
Cardiovascular Disease
|
Inogatran (H-314-27) is a synthetic thrombin inhibitor, developed for the possible treatment and prophylaxis of arterial and venous thrombotic diseases.
|
-
- HY-108237
-
-
- HY-147581
-
BTK-IN-11
|
Btk
|
Cancer
Inflammation/Immunology
|
BTK-IN-11 is a potent inhibitor of BTK. BTK plays an important role in signaling mediated by B cell antigen receptor (BCR) and Fcγreceptor (FcγR) in B cells and myeloid cells, respectively. BTK-IN-11 has the potential for the research of related diseases, especially autoimmune diseases, inflammatory diseases or cancer (extracted from patent WO2022063101A1, compound Z2).
|
-
- HY-121392
-
-
- HY-106579S
-
Tiaprofenic acid-d3
|
COX
|
Inflammation/Immunology
|
Tiaprofenic acid-d3 is a deuterium labeled Tiaprofenic acid. Tiaprofenic acid is a nonsteroidal anti-inflammatory agent (NSAID) mainly used in the treatment of rheumatic diseases[1].
|
-
- HY-100723
-
THK-523
|
Amyloid-β
|
Neurological Disease
|
THK-523 has demonstrated its high affinity and selectivity for tau pathology both in vitro and in vivo. 18F-THK523 is a potent tau imaging radiotracer. 18F-THK523 is a potent in vivo tau imaging ligand for Alzheimer's disease.
|
-
- HY-148132
-
GSK-3β inhibitor 11
|
GSK-3
|
Neurological Disease
|
GSK-3β inhibitor 11 (compound 21) is a glycogen synthase kinase-3β (GSK-3β) inhibitor (IC50=10.02 μM). GSK-3β inhibitor 11 can be used in neurodegenerative disease research.
|
-
- HY-108681
-
-
- HY-120314
-
-
- HY-145155
-
Calpain-2-IN-1
|
Proteasome
|
Neurological Disease
|
Calpain-2-IN-1 (Formula 1A) is a isoform-specific calpain-2 inhibitor with Kis of 181 nM and 7.8 nM for calpain-1, and calpain-2, respectively. Calpain-2-IN-1 can be used for the research of neurodegenerative diseases and other diseases of synaptic function.
|
-
- HY-122958
-
Peucedanocoumarin III
|
α-synuclein
|
Neurological Disease
|
Peucedanocoumarin III is an inhibitor of α-synuclein and Huntington protein aggregates that enhances the clearance of nuclear and cytoplasmic β23 aggregates and prevents cytotoxicity induced by disease-associated proteins (i.e., mutant Huntington proteins and α-synuclein). Peucedanocoumarin III may be used in Parkinson's disease research.
|
-
- HY-111338
-
Tacrine
|
Cholinesterase (ChE)
|
Neurological Disease
|
Tacrine is a potent acetylcholinesterse (AChE) inhibitor (IC50=109 nM), also acting as a CYP1A2 substrate agent. Tacrine exhibits certain hepatotoxicity in some individuals. Tacrine can be used for researching Alzheimer's disease (AD).
|
-
- HY-12866B
-
-
- HY-137553
-
-
- HY-122957
-
Huperzine C
|
Cholinesterase (ChE)
|
Neurological Disease
|
Huperzine C is an alkaloid isolated from Huperzia serrate. Huperzine C is an acetylcholinesterase (AChE) inhibotor, with an IC50 of 0.6 μM. Huperzine C can be used for the research of Alzheimer’s disease.
|
-
- HY-N10742
-
Maritimetin
|
Reactive Oxygen Species
|
Cardiovascular Disease
|
Maritimein is an aurone that can be isolated from Coreopsis tinctoria. Maritimein shows strong diphenyl(2,4,6-trinitrophenyl)iminoazanium (DPPH) radical-scavenging activity with an IC50 value of 4.12 μM. Maritimein can be used for the research of cardiovascular disease.
|
-
- HY-P3908
-
-
- HY-15800
-
CZC-25146 hydrochloride
|
LRRK2
|
Inflammation/Immunology
Neurological Disease
|
CZC-25146 hydrochloride is a potent LRRK2 inhibitor with IC50 values of 4.76 nM and 6.87 nM for wild-type LRRK2 and G2019S LRRK2, respectively. CZC-25146 hydrochloride inhibits PLK4, GAK, TNK1, CAMKK2 and PIP4K2C as well. CZC-25146 hydrochloride prevents mutant LRRK2-induced injury of neurons in vitro. CZC-25146 hydrochloride exhibits relatively favorable pharmacokinetic properties in mice. CZC-25146 hydrochloride can increase normal α-1-antitrypsin (AAT) secretion and reduce inflammatory cytokines. CZC-25146 hydrochloride can be used to research Parkinson's disease and liver diseases.
|
-
- HY-132596
-
-
- HY-P3392
-
Zilganersen
ION373
|
FAP
|
Neurological Disease
|
Zilganersen (ION373) is a glial fibrillary acidic protein (GFAP) inhibitor, an antisense oligonucleotide. Zilganersen can be used in Alexander disease (AxD) research.
|
-
- HY-N2807
-
-
- HY-B1039
-
Ambroxol
NA-872
|
Glucosidase
Autophagy
|
Metabolic Disease
Neurological Disease
|
Ambroxol (NA-872), an active metabolite of the proagent Bromhexine, has potent expectorant effects. Ambroxol is a glucocerebrosidase (GCase) chaperone and increases glucocerebrosidase activity. Ambroxol induces lung autophagy and has the potential for Parkinson disease and neuronopathic Gaucher disease research.
|
-
- HY-B1039A
-
Ambroxol hydrochloride
NA-872 hydrochloride
|
Glucosidase
Autophagy
|
Metabolic Disease
Neurological Disease
|
Ambroxol hydrochloride (NA-872 hydrochloride), an active metabolite of the proagent Bromhexine, has potent expectorant effects. Ambroxol hydrochloride is a glucocerebrosidase (GCase) chaperone and increases glucocerebrosidase activity. Ambroxol hydrochloride induces lung autophagy and has the potential for Parkinson disease and neuronopathic Gaucher disease research.
|
-
- HY-143614
-
THR-β agonist 3
|
Others
|
Metabolic Disease
|
THR-β agonist 3 is a potent agonist of THR-β. THR-β agonist 3 has the potential for the research of metabolic diseases such as obesity, hyperlipidemia, hypercholesterolemia, diabetes and other conditions such as steatosis and non-alcoholic steatohepatitis (NASH), atherosclerosis and other related conditions and diseases (extracted from patent WO2021129827A1, compound 6).
|
-
- HY-143613
-
THR-β agonist 2
|
Others
|
Metabolic Disease
|
THR-β agonist 2 is a potent agonist of THR-β. THR-β agonist 2 has the potential for the research of metabolic diseases such as obesity, hyperlipidemia, hypercholesterolemia, diabetes and other conditions such as steatosis and non-alcoholic steatohepatitis (NASH), atherosclerosis and other related conditions and diseases (extracted from patent WO2021121210A1, compound 3).
|
-
- HY-150728
-
AChE-IN-22
|
Cholinesterase (ChE)
|
Neurological Disease
|
AChE-IN-22 (compound 10q) is a selective acetylcholinesterase (AChE) inhibitor against AChE and BuChE with the IC50 values of 0.88 μM and 10 μM, respectively. AChE-IN-22 can bind to both the CAS (catalytic active site) and PAS (peripheral anionic site) of AChE and has the potential for the research of Alzheimer's disease.
|
-
- HY-142917
-
THR-β agonist 4
|
Others
|
Metabolic Disease
|
THR-β agonist 4 is a potent agonist of THR-β. THR-β agonist 4 has the potential for the research of metabolic diseases such as obesity, hyperlipidemia, hypercholesterolemia, diabetes and other conditions such as steatosis and non-alcoholic steatohepatitis (NASH), atherosclerosis and other related conditions and diseases (extracted from patent WO2021143706A1, compound 72).
|
-
- HY-116565A
-
Usmarapride free base
SUVN-D4010 free base
|
5-HT Receptor
|
Neurological Disease
|
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.
|
-
- HY-101357A
-
-
- HY-138935
-
Iclepertin
BI-425809
|
GlyT
|
Neurological Disease
|
Iclepertin (BI-425809) is a potent, selective and orally active glycine transporter 1 (GlyT1) inhibitor. Iclepertin is inactive against GlyT2. Iclepertin can be used for Alzheimer disease and schizophrenia research.
|
-
- HY-151387
-
A2AAR antagonist 1
|
Others
|
Neurological Disease
|
A2AAR antagonist 1 (compound 21a) is an A2AAR (adenosine A2A receptor) antagonist with a Ki value of 20 nM. A2AAR antagonist 1 shows high ligand efficiency, and it can be used for the research of neurodegenerative diseases.
|
-
- HY-W104304
-
-
- HY-15608
-
-
- 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-N10283
-
-
- HY-142949
-
ALK5-IN-7
|
TGF-β Receptor
|
Cancer
Inflammation/Immunology
|
ALK5-IN-7 is a potent inhibitor of ALK5. Transforming growth factor beta (TGF-β) is a multifunctional cytokine that is involved in regulating cell proliferation, differentiation and apoptosis through complex receptor signaling pathways on the cell surface in an autocrine, paracrine and endocrine manner. ALK5-IN-7 has the potential for the research of TGF-β-related diseases and conditions, including but not limited to tumors, fibrotic diseases, inflammatory diseases, autoimmune diseases, etc (extracted from patent WO2021129621A1, compound 4).
|
-
- HY-142950
-
ALK5-IN-6
|
TGF-β Receptor
|
Cancer
Inflammation/Immunology
|
ALK5-IN-6 is a potent inhibitor of ALK5. Transforming growth factor beta (TGF-β) is a multifunctional cytokine that is involved in regulating cell proliferation, differentiation and apoptosis through complex receptor signaling pathways on the cell surface in an autocrine, paracrine and endocrine manner. ALK5-IN-6 has the potential for the research of TGF-β-related diseases and conditions, including but not limited to tumors, fibrotic diseases, inflammatory diseases, autoimmune diseases, etc (extracted from patent WO2021129621A1, compound 1).
|
-
- HY-P1913
-
-
- HY-13206
-
MTEP hydrochloride
|
mGluR
|
Neurological Disease
|
MTEP hydrochloride is a potent, non-competitive and highly selective mGluR5 antagonist, with an IC50 of 5 nM and a Ki of 16 nM. MTEP hydrochloride shows antidepressant and anxiolytic-like effects. MTEP hydrochloride can be used for Parkinson's disease research.
|
-
- HY-13206A
-
MTEP
|
mGluR
|
Neurological Disease
|
MTEP is a potent, non-competitive and highly selective mGluR5 antagonist, with an IC50 of 5 nM and a Ki of 16 nM. MTEP shows antidepressant and anxiolytic-like effects. MTEP can be used for Parkinson's disease research.
|
-
- HY-B0143
-
Niacin
Nicotinic acid; Vitamin B3
|
Autophagy
Endogenous Metabolite
|
Cancer
Metabolic Disease
Cardiovascular Disease
|
Niacin (Vitamin B3) is an orally active water-soluble B3 vitamin that is an essential nutrient for humans. Niacin (Vitamin B3) plays a key role in energy metabolism, cell signaling cascades regulating gene expression and apoptosis. Niacin (Vitamin B3) is also used in the study of cardiovascular diseases.
|
-
- HY-15800A
-
CZC-25146
|
LRRK2
|
Inflammation/Immunology
Neurological Disease
|
CZC-25146 is a potent and orally active LRRK2 inhibitor with IC50 values of 4.76 nM and 6.87 nM for wild-type LRRK2 and G2019S LRRK2, respectively. CZC-25146 inhibits PLK4, GAK, TNK1, CAMKK2 and PIP4K2C as well. CZC-25146 prevents mutant LRRK2-induced injury of neurons in vitro. CZC-25146 exhibits relatively favorable pharmacokinetic properties in mice. CZC-25146 can increase normal α-1-antitrypsin (AAT) secretion and reduce inflammatory cytokines. CZC-25146 can be used to research Parkinson's disease and liver diseases.
|
-
- HY-146742
-
-
- 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-112555
-
-
- HY-B0623A
-
Ropinirole hydrochloride
SKF 101468 hydrochloride
|
Dopamine Receptor
|
Neurological Disease
|
Ropinirole (SKF 101468) hydrochloride is an orally active, potent D3/D2 receptor agonist with a Ki of 29 nM for D2 receptor. Ropinirole hydrochloride has pEC50s of 7.4, 8.4 and 6.8 for hD2, hD3 and hD4 receptors, respectively. Ropinirole hydrochloride has no affinity for the D1 receptors. Ropinirole hydrochloride has the potential for Parkinson's disease.
|
-
- HY-B0623
-
Ropinirole
SKF 101468
|
Dopamine Receptor
|
Neurological Disease
|
Ropinirole (SKF 101468) is an orally active, potent D3/D2 receptor agonist with a Ki of 29 nM for D2 receptor. Ropinirole has pEC50s of 7.4, 8.4 and 6.8 for hD2, hD3 and hD4 receptors, respectively. Ropinirole has no affinity for the D1 receptors. Ropinirole has the potential for Parkinson's disease.
|
-
- HY-111935
-
3,3'-Diethyl-9-methylthiacarbocyanine iodide
|
Microtubule/Tubulin
|
Neurological Disease
|
3,3'-Diethyl-9-methylthiacarbocyanine iodide is a cyanine dye, also a tau aggregation inhibitor, with an IC50 value of 0.28 μM for tau. 3,3'-Diethyl-9-methylthiacarbocyanine iodide can cause misfunction of the microtubule cytoskeleton. 3,3'-Diethyl-9-methylthiacarbocyanine iodide can be used for researching Alzheimer’s disease.
|
-
- HY-139066
-
Punicic acid
Trichosanic acid
|
Others
|
Metabolic Disease
|
Punicic acid is a bioactive compound of pomegranate seed oil. Punicic acid is an isomer of conjugated α-linolenic acid and a ω-5 polyunsaturated fatty acid. Punicic acid has the potential for the research of various chronic diseases.
|
-
- HY-116020
-
FAUC 365
|
Dopamine Receptor
|
Neurological Disease
|
FAUC 365 is a highly dopamine D3 receptor-selective antagonist with Ki values of 0.5 nM, 340, 2600, and 3600 nM at D3, D4.4, D2short, and D2Long receptors, respectively. FAUC 365 can be used for the research of schizophrenia, and Parkinson's disease.
|
-
- 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-A0009
-
Galanthamine hydrobromide
Galantamine hydrobromide
|
Cholinesterase (ChE)
nAChR
|
Neurological Disease
|
Galanthamine hydrobromide (Galantamine hydrobromide) is a selective, reversible, competitive, alkaloid AChE inhibitor, with an IC50 of 0.35 µM. Galanthamine hydrobromide is a potent allosteric potentiating ligand (APL) of human α3β4, α4β2, α6β4 nicotinic receptors ( nAChRs). Galanthamine hydrobromide is developed for the research of Alzheimer's disease (AD).
|
-
- HY-145906
-
D4R antagonis-2
|
Dopamine Receptor
|
Neurological Disease
|
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.
|
-
- HY-145988
-
COX-2-IN-11
|
COX
|
Inflammation/Immunology
|
COX-2-IN-11 (compound 7b2) is a potent and selective inhibitor of COX-2. COX-2-IN-11 has the potential for the research of inflammation diseases.
|
-
- HY-137789
-
Tazofelone
LY 213829
|
COX
|
Cancer
|
Tazofelone (LY 213829) is a cyclooxygenase-II (COX-II) inhibitor. Tazofelone transform into sulfoxide and quinol metabolites is primarily mediated by CYP3A. Tazofelone can be used for the research of inflammatory bowel disease.
|
-
- HY-P1913A
-
-
- HY-110325
-
-
- HY-P99022
-
Gantenerumab
|
Amyloid-β
|
Neurological Disease
|
Gantenerumab is a fully human anti-amyloid-β (Aβ) IgG1 monoclonal antibody demonstrates sustained cerebral amyloid-β binding. Gantenerumab can be used for Alzheimer's disease research.
|
-
- HY-136341
-
-
- HY-12452
-
-
- HY-150049
-
γ-Secretase modulator 13
|
Amyloid-β
|
Neurological Disease
|
γ-Secretase modulator 13 (compound 4) is a gamma-secretase modulator (GSMs) that inhibits the production of the aggregated amyloid β-peptide Aβ42 with an IC50 value of 163 nM. γ-Secretase modulator 13 can be used in the study of Alzheimer's disease.
|
-
- HY-W004284
-
-
- HY-15470
-
GW791343 trihydrochloride
|
P2X Receptor
|
Neurological Disease
|
GW791343 trihydrochloride is a potent human P2X7 receptor negative allosteric modulator (exhibits species-specific activity), produces a non-competitive antagonist effect on human P2X7 receptor, with a pIC50 of 6.9-7.2. GW791343 trihydrochloride can enhance ATP rhythm. GW791343 trihydrochloride can be used in study of neurological disease.
|
-
- HY-15469
-
GW791343 dihydrochloride
|
P2X Receptor
|
Neurological Disease
|
GW791343 dihydrochloride is a potent human P2X7 receptor negative allosteric modulator (exhibits species-specific activity), produces a non-competitive antagonist effect on human P2X7 receptor, with a pIC50 of 6.9-7.2. GW791343 dihydrochloride can enhance ATP rhythm. GW791343 dihydrochloride can be used in study of neurological disease.
|
-
- HY-128128
-
ASN04421891
|
Others
|
Neurological Disease
|
ASN04421891 is a potent GPR17 receptor modulator, with an EC50 of 3.67 nM in [35S]GTPγS binding assay. ASN04421891 can be used for neurodegenerative diseases research.
|
-
- HY-103374
-
Phenserine
(-)-Eseroline phenylcarbamate; (-)-Phenserine
|
Cholinesterase (ChE)
Amyloid-β
|
Neurological Disease
|
Phenserine ((-)-Eseroline phenylcarbamate) is a derivative of Physostigmine and is a potent, noncompetitive, long-acting and selective AChE inhibitor. Phenserine reduces β-amyloid precursor protein (APP) and β-amyloid peptide (Aβ) formation. Phenserine improves cognitive performance and attenuates the progression of Alzheimer's disease.
|
-
- HY-W263279
-
(E)-Guanabenz
(E)-Wy-8678
|
Adrenergic Receptor
|
Neurological Disease
Cardiovascular Disease
|
(E)-Guanabenz ((E)-Wy-8678) is an orally active central α2-adrenoceptor agonist. (E)-Guanabenz has antihypertensive activity, acts via stimulating central α2-adrenoceptors, and reducing net sympathetic outflow into the periphery. (E)-Guanabenz also directly binds to and inhibits GADD34, and has neuroprotective activity. (E)-Guanabenz can be used for researching hypertension and Parkinson disease.
|
-
- HY-146137
-
-
- 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-135902
-
Synucleozid
NSC 377363
|
DNA/RNA Synthesis
|
Neurological Disease
|
Synucleozid (NSC 377363) is a potent inhibitor of the SNCA mRNA that encodes α-synuclein protein. Synucleozid selectively targets the α-synuclein mRNA 5′ UTR at the designed IRE site, decreases the amount of SNCA mRNA loaded into polysomes and thereby inhibits SNCA translation. Synucleozid has the potential for the investigation of Parkinson’s disease.
|
-
- HY-135902A
-
Synucleozid hydrochloride
NSC 377363 hydrochloride
|
DNA/RNA Synthesis
|
Neurological Disease
|
Synucleozid hydrochloride (NSC 377363 hydrochloride) is a potent inhibitor of the SNCA mRNA that encodes α-synuclein protein. Synucleozid selectively targets the α-synuclein mRNA 5′ UTR at the designed IRE site, decreases the amount of SNCA mRNA loaded into polysomes and thereby inhibits SNCA translation. Synucleozid has the potential for the investigation of Parkinson’s disease.
|
-
- HY-153476
-
GIP/GLP-1 dual receptor agonist-1
|
GCGR
|
Metabolic Disease
|
GIP/GLP-1 dual receptor agonist-1 (compound 4) is a GIP/GLP-1 receptor agonist. GIP/GLP-1 dual receptor agonist-1 can be used in the research of metabolic disorders and fatty liver diseases, including nonalcoholic steatohepatitis (NASH) and nonalcoholic fatty liver disease (NAFLD).
|
-
- HY-148385
-
Ganglioside GM2
|
Others
|
Cancer
|
Ganglioside GM2 is a human tumor antigen (OFA-I-1). Ganglioside GM2 is the major lysosomal storage compound of Tay-Sachs disease.
|
-
- HY-N10488
-
-
- HY-P99821
-
-
- HY-143485
-
IRAK4-IN-9
|
IRAK
|
Cancer
Inflammation/Immunology
|
IRAK4-IN-9 (compound 73) is a potent IRAK4 inhibitor with an IC50 of 1.5 nM. IRAK4-IN-9 blocks MyD88 dependent signaling. IRAK4-IN-9 has the potential for the research of inflammatory diseases, autoimmune diseases, and cancer.
|
-
- HY-143486
-
IRAK4-IN-10
|
IRAK
|
Cancer
Inflammation/Immunology
|
IRAK4-IN-10 (compound 75) is a potent IRAK4 inhibitor with an IC50 of 1.5 nM. IRAK4-IN-10 blocks MyD88 dependent signaling. IRAK4-IN-9 has the potential for the research of inflammatory diseases, autoimmune diseases, and cancer.
|
-
- HY-18681
-
Voxelotor
GBT 440
|
Others
|
Cardiovascular Disease
|
Voxelotor (GBT 440) is a potent inhibitor of haemoglobin S (HbS) polymerization. Voxelotor has the potential for sickle cell disease (SCD) treatment.
|
-
- HY-P99485
-
Brazikumab
AMG 139; MEDI2070
|
Interleukin Related
|
Inflammation/Immunology
|
Brazikumab (AMG 139) is a human IgG2 monoclonal antibody, selectively binds the p19 subunit of IL-23, with a KD of 0.138 nM for human IL-23. Brazikumab can be used for the research of Crohn's disease.
|
-
- HY-111372
-
Finerenone
BAY 94-8862
|
Mineralocorticoid Receptor
|
Cardiovascular Disease
|
Finerenone (BAY 94-8862) is a third-generation, selective, and orally available nonsteroidal mineralocorticoid receptor (MR) antagonist (IC50=18 nM). Finerenone displays excellent selectivity versus glucocorticoid receptor (GR), androgen receptor (AR), and progesterone receptor (>500-fold). Finerenone has the potential for cardiorenal diseases research, such as type 2 diabetes mellitus and chronic kidney disease.
|
-
- 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-151539
-
-
- HY-15280
-
GSK2292767
|
PI3K
|
Inflammation/Immunology
|
GSK2292767 is a potent and selective inhibitor of PI3Kδ, with a pIC50 of 10.1. GSK2292767 showing greater than 500-fold selective over the other PI3K isoforms. GSK2292767 can be used for the research of respiratory disease.
|
-
- HY-139974
-
BChE-IN-2
|
Cholinesterase (ChE)
|
Neurological Disease
|
BChE-IN-2 (compound 22) is a potent inhibitor of BChE with a Ki of 0.099 μM. BChE-IN-2 is a pyrimidine and pyridine derivative. BChE-IN-2 has the potential for the research of Alzheimer’s disease (AD) .
|
-
- HY-151210
-
-
- HY-147644
-
-
- HY-P3648
-
-
- HY-111313
-
JNJ-26070109
|
Cholecystokinin Receptor
|
Metabolic Disease
|
JNJ-26070109 is a high-affinity, competitive, orally bioactive, and selective cholecystokinin 2 (CCK2) receptor antagonist with good pharmacokinetic properties, with pKis of 8.49, 7.99, and 7.70 for human, rat, and dog CCK2 receptors, respectively. The dual function of CCK2 receptors in regulating gastric acid secretion and growth of the gastrointestinal mucosa make this an attractive and novel target for the research of gastroesophageal reflux disease.
|
-
- HY-150585
-
BuChE-IN-5
|
Amyloid-β
Cholinesterase (ChE)
Tau Protein
|
Neurological Disease
|
BuChE-IN-5 (compound 25b) is a potent BuChE inhibitor with an IC50 value of 1.94 μM. BuChE-IN-5 efficiently inhibits aggregation Aβ and tau protein in Escherichia coli. BuChE-IN-5 also has free radical scavenging capacity and antioxidant activity. BuChE-IN-5 can be used for researching Alzheimer’s disease.
|
-
- HY-132593
-
Rovanersen
WVE-120101
|
Huntingtin
|
Neurological Disease
|
Rovanersen (WVE-120101) is an antisense oligonucleotide that specifically targets mutated mRNA copies of the huntington (HTT) gene without affecting healthy mRNA of HTT gene, thereby preventing the production of faulty Huntingtin protein. Rovanersen can be used for huntington’s disease research.
|
-
- 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-151348
-
BACE1-IN-11
|
Beta-secretase
|
Neurological Disease
|
BACE1-IN-11 is a BACE1 inhibitor. BACE1-IN-11 has the BACE1 inhibitory activity with an IC50 value of 72 μM. BACE1-IN-11 can be used for the research of Alzheimer’s disease (AD) .
|
-
- HY-14415
-
SR8278
|
REV-ERB
|
Metabolic Disease
Neurological Disease
|
SR8278 is a REV-ERBα antagonist and inhibits the REV-ERBα transcriptional repression activity with an EC50 of 0.47 μM. SR8278 is used to regulate the metabolism in organisms and study biological rhythm. SR8278 also can be used for the research of Duchenne muscular dystrophy and Alzheimer's disease.
|
-
- HY-14418
-
VU0361737
ML-128
|
mGluR
|
Neurological Disease
|
VU0361737 (ML-128) is a potent, selective and CNS penetrant positive allosteric modulator of metabotropic glutamate receptor 4 (mGluR4 PAM), with EC50s of 240 nM and 110 nM for human and rat mGluR4 receptors, respectively. VU0361737 has neuroprotective effect. VU0361737 is potential for Parkinson's disease research.
|
-
- HY-143221
-
AS-Inclisiran
|
Ser/Thr Protease
|
Cardiovascular Disease
|
AS-Inclisiran is the antisense of Inclisiran. Inclisiran (ALN-PCSsc) is a double-stranded small interfering RNA (siRNA) molecule that inhibits the transcription of PCSK-9. Inclisiran can be used for hyperlipidemia and cardiovascular disease (CVD) research.
|
-
- HY-N10356
-
4,27-Dimethyl withaferin A
|
Others
|
Neurological Disease
|
4,27-Dimethyl withaferin A is a synthetic analog of withanolide natural products. 4,27-Dimethyl withaferin A has the potential for the research of neurodegenerative diseases (extracted from patent WO2015077780A1).
|
-
- HY-13993B
-
Ro 25-6981 hydrochloride
|
iGluR
|
Neurological Disease
|
Ro 25-6981 hydrochloride is a potent, selective and activity-dependent NR2B subunit specific NMDA receptor antagonist. Ro 25-6981 hydrochloride shows anticonvulsant and anti-parkinsonian activity. Ro 25-6981 hydrochloride has the potential for the research of parkinson's disease (PD).
|
-
- HY-13993
-
Ro 25-6981
|
iGluR
|
Neurological Disease
|
Ro 25-6981 is a potent, selective and activity-dependent NR2B subunit specific NMDA receptor antagonist. Ro 25-6981 shows anticonvulsant and anti-parkinsonian activity. Ro 25-6981 has the potential for the research of parkinson's disease (PD).
|
-
- HY-143475
-
-
- HY-143474
-
-
- HY-151173
-
-
- HY-N11081
-
Hexanorcucurbitacin D
|
Others
|
Cardiovascular Disease
|
Hexanorcucurbitacin D is a cucurbitacin. Hexanorcucurbitacin D can be isolated from Trichosanthes cucumeroides roots. Hexanorcucurbitacin D can be used for the research of cardiovascular disease (CVD).
|
-
- HY-N10490
-
Blestrin D
|
Cholinesterase (ChE)
|
Neurological Disease
|
Blestrin D is a potent butyrylcholinesterase (BChE) mixed-type inhibitor with an IC50 value of 8.1 μM. Blestrin D can be isolated from Bletilla striata. Blestrin D can be used for the research of Alzheimer's disease (AD).
|
-
- HY-14338A
-
Idalopirdine Hydrochloride
Lu AE58054 Hydrochloride
|
5-HT Receptor
|
Neurological Disease
|
Idalopirdine Hydrochloride (Lu AE58054 Hydrochloride) is a potent, selective 5-HT6 receptor antagonist with a Ki value of 0.83 nM. Idalopirdine Hydrochloride may be used in studies of Alzheimer's disease and schizophrenia, among other related disorders.
|
-
- HY-14338
-
Idalopirdine
Lu AE58054
|
5-HT Receptor
|
Neurological Disease
|
Idalopirdine (Lu AE58054 ) is a potent, selective 5-HT6 receptor antagonist with a Ki value of 0.83 nM. Idalopirdine may be used in studies of Alzheimer's disease and schizophrenia, among other related disorders.
|
-
- HY-134661A
-
CVN424
|
GPR6
|
Neurological Disease
|
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.
|
-
- HY-132591
-
-
- HY-15295
-
Vonoprazan Fumarate
TAK-438
|
Proton Pump
|
Metabolic Disease
|
Vonoprazan Fumarate (TAK-438), a proton pump inhibitor (PPI), is a potent and orally active potassium-competitive acid blocker (P-CAB), with antisecretory activity. Vonoprazan Fumarate inhibits H +,K +-ATPase activity in porcine gastric microsomes with an IC50 of 19 nM at pH 6.5. Vonoprazan Fumarate is developed for the research of acid-related diseases, such as gastroesophageal reflux disease and peptic ulcer disease.
|
-
- HY-152235
-
HDAC6-IN-15
|
HDAC
|
Cancer
Neurological Disease
|
HDAC6-IN-15 is a selective histone deacetylase 6 (HDAC6) inhibitor. HDAC6-IN-15 has potent inhibitory activity for HDAC6 with IC50 value of 38.2 nM. HDAC6-IN-15 can be used for the research of cancer and neurodegenerative diseases.
|
-
- HY-P99185
-
-
- HY-121826
-
-
- HY-13993A
-
Ro 25-6981 Maleate
|
iGluR
|
Neurological Disease
|
Ro 25-6981 Maleate is a potent, selective and activity-dependent NR2B subunit specific NMDA receptor antagonist. Ro 25-6981 Maleat shows anticonvulsant and anti-parkinsonian activity. Ro 25-6981 Maleate has the potential for the research of parkinson's disease (PD).
|
-
- HY-146039
-
AChE-IN-15
|
Cholinesterase (ChE)
|
Neurological Disease
|
AChE-IN-15 (Compound 3d) is a reversible human acetylcholinesterase (huAChE) (IC50=6.8 μM) and human butyrylcholinesterase (huBChE) (IC50=16.1 μM) inhibitor. AChE-IN-15 shows significant antioxidant potency, AChE-IN-15 can be used for the research of Alzheimer’s disease.
|
-
- HY-11052A
-
Trap-101 hydrochloride
|
Opioid Receptor
|
Neurological Disease
|
Trap-101 hydrochloride is a potent, selective and competitive antagonist of NOP receptors over classical opioid receptors. Trap-101 stimulates GTPγ 35S binding to CHOhNOP membranes with pKi values of 8.65, 6.60, 6.14 and <5 for NOP, μ-, κ-, and δ-opioid receptors, respectively. Trap-101 attenuates motor deficits in a rat model of parkinson's disease and can be used for the research of nervous system diseases.
|
-
- HY-150003
-
Aβ1–42 aggregation inhibitor 1
|
Cholinesterase (ChE)
Amyloid-β
|
Neurological Disease
|
Aβ1-42 aggregation inhibitor 1 inhibits AChE (acetylcholinesterase) and BuChE (butyrylcholinesterase) with the IC50 value of 2.64 μM and 1.29 μM, respectively. Aβ1-42 aggregation inhibitor 1 inhibits self-mediated Aβ1-42 aggregation by 51.29% at a concentration of 25 μM. Aβ1-42 aggregation inhibitor 1 has the potential for the research of anti-Alzheimer's disease.
|
-
- HY-120596
-
-
- HY-144058
-
JAK-IN-18
|
JAK
|
Inflammation/Immunology
|
JAK-IN-18 is a potent inhibitor of JAK. JAK-IN-18 is useful for the research of multiple diseases, particularly ocular, skin, and respiratory diseases (extracted from patent WO2018204238A1, compound 1).
|
-
- HY-118342
-
PQCA
|
mAChR
|
Neurological Disease
|
PQCA is a highly selective and potent muscarinic M1 receptor positive allosteric modulator. PQCA has an EC50 value of 49 nM and 135 nM on rhesus and human M1 receptor, respectively. PQCA is inactive for other muscarinic receptors. PQCA has potential to reduce the cognitive deficits associated with Alzheimer's disease.
|
-
- HY-117822
-
BRD0209
|
GSK-3
|
Neurological Disease
|
BRD0209 is a potent, selective and dual inhibitor of GSK3α/β inhibitor (GSK3α IC50 = 19 nM; GSK3β IC50 = 5 nM). BRD0209 is also a reversible ATP-competitive inhibitor with fast-off kinetics (Ki = 4.2 nM, respectively). BRD0209 is a tricyclic pyrazolotetrahydroquinolinone compound. BRD0209 has the potential for the research of mood disorder diseases.
|
-
- HY-134398
-
Kinetin triphosphate
6-Fu-ATP; KTP
|
Others
|
Neurological Disease
|
Kinetin triphosphate(6-Fu-ATP; KTP) is an ATP analogue that regulates or enhances kinase function with higher catalytic efficiency than its endogenous substrate, ATP. Kinetin triphosphate can be used in Parkinson's disease research.
|
-
- HY-P99405
-
Prasinezumab
PRX 002; RG 7935; RO 7046015
|
α-synuclein
|
Neurological Disease
|
Prasinezumab (PRX 002) is a humanized IgG1 monoclonal antibody directed against aggregated α-synuclein. Prasinezumab has the potential for Parkinson's disease research.
|
-
- HY-20457
-
-
- HY-147564
-
RET-IN-18
|
RET
|
Cancer
Neurological Disease
|
RET-IN-18 is a pyridone compound. is a potent inhibitor of RET. RET-IN-18 is a potent inhibitor of RET. RET-IN-18 has the potential for the research of diseases related to irritable bowel syndrome (IBS) and other gastrointestinal disorders, as well as cancers, and neurodegenerative diseases (extracted from patent WO2022017524A1, compound 1).
|
-
- HY-142778
-
Lp-PLA2-IN-10
|
Phospholipase
|
Metabolic Disease
Neurological Disease
|
Lp-PLA2-IN-10 is a potent inhibitor of lipoprotein-associated phospholipase A2 (Lp-PLA2). Lp-PLA2 previously known as platelet- activating factor acetylhydrolase (PAF-AH), is a phospholipase A2 enzyme involved in hydrolysis of lipoprotein lipids or phospholipids. Lp-PLA2-IN-10 has the potential for the research of neurodegenerative-related diseases such as Alzheimer's disease (AD), glaucoma, age-related macular degeneration (AMD), or cardiovascular diseases including atherosclerosis (extracted from patent WO2022001881A1, compound 4).
|
-
- HY-144057
-
JAK-IN-17
|
JAK
|
Inflammation/Immunology
|
JAK-IN-17 is a potent inhibitor of JAK. JAK-IN-17 is useful for the research of multiple diseases, particularly ocular, skin, and respiratory diseases (extracted from patent WO2021185305A1, compound 9-1).
|
-
- 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-16747
-
Maralixibat chloride
SHP625 chloride; LUM001 chloride; Lopixibat chloride
|
Apical Sodium-Dependent Bile Acid Transporter
|
Metabolic Disease
|
Maralixibat (SHP625) chloride is an orally active ileal bile acid transporter (IBAT) inhibitor. Maralixibat chloride can be used for the research of rare cholestatic liver diseases including Alagille syndrome (ALGS), progressive familial intrahepatic cholestasis (PFIC) and biliary atresia.
|
-
- HY-W020050
-
Cystamine (dihydrochloride)
|
Caspase
Glutaminase
Apoptosis
|
Cancer
Neurological Disease
|
Cystamine (dihydrochloride) is the disulfide form of the free thiol, cysteamine. Cystamine is an orally active transglutaminase (Tgase) inhibitor. Cystamine also has inhibition activity for caspase-3 with an IC50 value of 23.6 μM. Cystamine can be used for the research of severals diseases including Huntington's disease (HD) .
|
-
- HY-18286
-
NCGC00229600
|
TSH Receptor
|
Endocrinology
|
NCGC00229600 is an allosteric inverse agonist of thyrotropin receptor (TSHR). NCGC00229600 inhibits both TSH and stimulating antibody activation of TSHRs endogenously expressed in Graves' disease.
|
-
- HY-147243
-
Ansornitinib
ANG-3070
|
VEGFR
PDGFR
|
Inflammation/Immunology
Cardiovascular Disease
|
Ansornitinib is an orally active dual kinase inhibitor that inhibits platelet-derived growth factor receptor (PDGFR) and vascular endothelial growth factor receptor (VEGFR2). Ansornitinib can be used as an antifibrotic agent in lung, liver, kidney, and gastrointestinal fibrotic diseases.
|
-
- HY-10096
-
TCS2002
|
GSK-3
|
Neurological Disease
|
TCS2002 (Compound 9b) is a highly selective, orally bioavailable and potent GSK-3β inhibitor with the IC50 of 35 nM. TCS2002 shows good pharmacokinetic profiles including favorable BBB penetration. TCS2002 can be used for the research of Alzheimer’s disease.
|
-
- HY-146345
-
Antiviral agent 18
|
Antibiotic
|
Infection
|
Antiviral agent 18 (Compound 5) is an anti-infection agent. Antiviral agent 18 results in good antiviral activity against murine norovirus. Antiviral agent 18 has the potential for the research of infectious and malignant diseases.
|
-
- HY-147387
-
DSS30
|
CDK
Amyloid-β
|
Inflammation/Immunology
|
DSS30 is a P25/CDK5 inhibitor that reduces β-amyloid (Aβ) secretion by inhibiting amyloid precursor protein lyase 1 (BACEl) phosphorylation. DSS30 can be used in the study of neurodegenerative diseases such as Alzheimer's disease.
|
-
- HY-P3140
-
α-Synuclein (61-75)
|
α-synuclein
|
Neurological Disease
|
α-Synuclein (61-75) is the 61-75 fragment of α-Synuclein. α-Synuclein is an abundant neuronal protein that is highly enriched in presynaptic nerve terminals. α-Synuclein is a potential biomarker for Parkinson's disease (PD).
|
-
- HY-142919
-
-
- HY-142918
-
-
- HY-N8658
-
-
- HY-124775
-
-
- HY-109001
-
Alicapistat
ABT-957
|
Proteasome
|
Neurological Disease
|
Alicapistat (ABT-957) is an orally active selective inhibitor of human calpains 1 and 2 for the potential application of Alzheimer's disease (AD). Alicapistat mitigates the metabolic liability of carbonyl reduction and inhibits calpain 1 with an IC50 value of 395 nM.
|
-
- HY-136459
-
NMDA receptor antagonist 2
|
iGluR
|
Neurological Disease
|
NMDA receptor antagonist 2 is a potent and orally active NR2B subtype-selective NMDA antagonist with an IC50 and a Ki of 1.0 nM and 0.88 nM, respectively. NMDA receptor antagonist 2 is used for the study of neuropathic pain and Parkinson’s disease.
|
-
- HY-P3507
-
Dalazatide
ShK-186
|
Potassium Channel
|
Metabolic Disease
Inflammation/Immunology
|
Dalazatide (ShK-186) is a specific Kv1.3 potassium channel peptide inhibitor. Dalazatide can be used in the study of autoimmune diseases such as multiple sclerosis (MS), lupus erythematosus, psoriasis, rheumatoid arthritis, type 1 diabetes and inflammatory bowel disease.
|
-
- HY-149010
-
NXPZ-2
|
Keap1-Nrf2
|
Neurological Disease
|
NXPZ-2 is an orally active Keap1-Nrf2 protein–protein interaction (PPI) inhibitor with a Ki value of 95 nM, EC50 value of 120 and 170 nM. NXPZ-2 can dose-dependently ameliorate Aβ[1-42]-Induced cognitive dysfunction, improve brain tissue pathological changes in Alzheimer’s disease (AD) mouse by increasing neuron quantity and function. NXPZ-2 can inhibit oxidative stress by increasing Nrf2 expression levels and promoting its cytoplasm to nuclear translocation, which is helpful for Keap1-Nrf2 PPI inhibitors and AD associated disease research.
|
-
- HY-N0690
-
Schisandrin C
Schizandrin-C; Wuweizisu-C
|
Apoptosis
Virus Protease
Molecular Glues
|
Cancer
|
Schisandrin C (Schizandrin-C) is a phytochemical lignan isolated from Schizandra chinensis. Schisandrin C has diverse biological activities, including anticancer, anti-inflammatory and antioxidant effects. Schisandrin C is a molecular glue. Schisandrin C can be used for cancer, alzheimer’s disease, and liver diseases research. Schisandrin C induces cell apoptosis.
|
-
- HY-N8440
-
Gibberellin A4
|
Others
|
Infection
|
Gibberellin A4 is a natural compound that can be isolated from Sphaceloma manihoticola. Gibberellin A4 is a causal agent of cassava superelongation disease.
|
-
- HY-120441
-
-
- 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-P3140A
-
α-Synuclein (61-75) (TFA)
|
α-synuclein
|
Neurological Disease
|
α-Synuclein (61-75) TFA is the 61-75 fragment of α-Synuclein. α-Synuclein is an abundant neuronal protein that is highly enriched in presynaptic nerve terminals. α-Synuclein is a potential biomarker for Parkinson's disease (PD).
|
-
- HY-143313
-
-
- HY-128511
-
Piridoxilate
Piridoxylate
|
Others
|
Cardiovascular Disease
|
Piridoxilate (Piridoxylate), a glyoxylate derivative, is an anti-anoxic agent. Piridoxilate can be used in research on vascular diseases and coronary occlusion.
|
-
- HY-N6906
-
Oleuroside
|
Others
|
Neurological Disease
|
Oleuroside is a phenolic secoiridoid in olive. Oleuroside can protect against mitochondrial dysfunction in models of early Alzheimer's disease and brain ageing.
|
-
- HY-B0311A
-
Carbidopa monohydrate
(S)-(-)-Carbidopa monohydrate
|
Aryl Hydrocarbon Receptor
|
Cancer
Neurological Disease
|
Carbidopa ((S)-(-)-Carbidopa) monohydrate, a peripheral decarboxylase inhibitor, can be used for the research of Parkinson's disease. Carbidopa monohydrate is a selective aryl hydrocarbon receptor (AhR) modulator. Carbidopa monohydrate inhibits pancreatic cancer cell and tumor growth.
|
-
- HY-B0311
-
Carbidopa
(S)-(-)-Carbidopa
|
Aryl Hydrocarbon Receptor
|
Cancer
Neurological Disease
|
Carbidopa ((S)-(-)-Carbidopa), a peripheral decarboxylase inhibitor, can be used for the research of Parkinson's disease. Carbidopa is a selective aryl hydrocarbon receptor (AhR) modulator. Carbidopa inhibits pancreatic cancer cell and tumor growth.
|
-
- HY-143300
-
-
- HY-B0955
-
Oxethazaine
Oxetacaine
|
HBV
|
Neurological Disease
|
Oxethazaine (Oxetacaine), a precursor of phentermine acidic, is an acid-resistent and orally active analgesic agent. Oxethazaine (Oxetacaine) has the potential for the relief of pain associated with peptic ulcer disease or esophagitis.
|
-
- HY-N10489
-
BChE-IN-12
|
Cholinesterase (ChE)
|
Neurological Disease
|
BChE-IN-12 (compound 12) is a potent butyrylcholinesterase (BChE) non-competitive inhibitor with an IC50 value of 2.3 μM. BChE-IN-12 can be isolated from Bletilla striata. BChE-IN-12 can be used for the research of Alzheimer's disease (AD).
|
-
- HY-N10486
-
BChE-IN-10
|
Cholinesterase (ChE)
|
Neurological Disease
|
BChE-IN-10 (compound 6) is a potent butyrylcholinesterase (BChE) mixed-type inhibitor with an IC50 value of 6.4 μM. BChE-IN-10 can be isolated from Bletilla striata. BChE-IN-10 can be used for the research of Alzheimer's disease (AD).
|
-
- HY-P3507A
-
Dalazatide TFA
ShK-186 TFA
|
Potassium Channel
|
Metabolic Disease
Inflammation/Immunology
|
Dalazatide (ShK-186) TFA is a specific Kv1.3 potassium channel peptide inhibitor. Dalazatide TFA can be used in the study of autoimmune diseases such as multiple sclerosis (MS), lupus erythematosus, psoriasis, rheumatoid arthritis, type 1 diabetes and inflammatory bowel disease.
|
-
- HY-P3780
-
Cys-Gly-Lys-Lys-Gly-Amyloid β-Protein (36-42)
|
Amyloid-β
|
Neurological Disease
|
Cys-Gly-Lys-Lys-Gly-Amyloid β-Protein (36-42) is the 36-42 fragment of Amyloid β-Protein. β-amyloid, a polypeptide made up of 36-43 amino acids, is the main component of amyloid plaques found in the brains of people with Alzheimer's disease. β-amyloid oligomers (Aβos) plays A key role in the progression of Alzheimer's disease (AD) by inducing neuronal damage and cognitive impairment.
|
-
- HY-N3345
-
Macrocarpal B
|
Bacterial
|
Infection
|
Macrocarpal B is an antibacterial compounds. Macrocarpal B can be isolated from the branch of Eucalyptus globulus. Macrocarpal B can be used for the research of periodontal disease.
|
-
- HY-B0341
-
Nicorandil
SG-75
|
Potassium Channel
|
Cardiovascular Disease
|
Nicorandil (SG-75) is a potent potassium channel activator and targets vascular nucleoside diphosphate-dependent K + channels and cardiac ATP-sensitive K + channels (KATP). Nicorandil is a nicotinamide ester with vasodilatory and cardioprotective effects and has the potential for angina and forischemic heart diseases.
|
-
- HY-15381
-
-
- HY-B0160
-
-
- HY-149102
-
-
- HY-130609A
-
Aβ42-IN-1 free base
|
γ-secretase
|
Neurological Disease
|
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.
|
-
- HY-151963
-
-
- HY-143275
-
HL-8
|
PI3K
|
Cancer
|
HL-8 is a PROTAC molecule targeting PI3K kinase. HL-8 has a significant and complete degradation effect on PI3K kinase at a concentration of 10 μM within 8 h. HL-8 has the potential for the research of cancer diseases.
|
-
- HY-P99859
-
Donanemab
LY3002813
|
Amyloid-β
|
Neurological Disease
|
Donanemab (LY3002813) is a humanized IgG1 monoclonal antibody directed at an N‐terminal pyroglutamate amyloid beta (Aβ) epitope. Donanemab has the potential for early Alzheimer's disease research.
|
-
- HY-101277
-
Vadadustat
PG-1016548; AKB-6548
|
HIF/HIF Prolyl-Hydroxylase
|
Cardiovascular Disease
|
Vadadustat (PG-1016548) is a titratable, oral hypoxia-inducible factor prolyl hydroxylase (HIF-PH) inhibitor. Vadadustat is an erythropoiesis-stimulating agent and has the potential for anemia treatment in chronic kidney disease in vivo.
|
-
- HY-150223
-
-
- HY-19948
-
Leucomethylene blue mesylate
TRx0237 mesylate; Methylene blue leuco base mesylate
|
Amyloid-β
|
Neurological Disease
|
Leucomethylene blue (TRx0237) mesylate, an orally active second-generation tau protein aggregation inhibitor (Ki of 0.12 μM), could be used for the study of Alzheimer's Disease. Leucomethylene blue mesylate is a common reduced form of Methylene Blue, Methylene Blue is a member of the thiazine class of dyes.
|
-
- HY-151405
-
Z164597606
|
Cholinesterase (ChE)
|
Neurological Disease
|
Z164597606 is a selective BChE inhibitor (IC50: 1.3 and 1.7 μM for eqBChE and hBChE). Z164597606 forms a π-π stacking interaction with the amino acid Trp82 of hBChE. Z164597606 can be used for the research of Alzheimer’s disease (AD).
|
-
- HY-145578
-
Linaprazan glurate
X842
|
Others
|
Inflammation/Immunology
|
Linaprazan glurate inhibits exogenously or endogenously stimulated gastric acid secretion. Linaprazan glurate exhibits several advantageous properties, such as fast onset, high in vivo potency and/or long duration of action. Linaprazan glurate is useful in the research of gastrointestinal inflammatory diseases and peptic ulcer diseases (extracted from patent WO2010063876A1).
|
-
- HY-B0715
-
Pentoxifylline
BL-191; PTX; Oxpentifylline
|
Phosphodiesterase (PDE)
Autophagy
HIV
|
Cardiovascular Disease
Cancer
|
Pentoxifylline (BL-191), a haemorheological agent, is an orally active non-selective phosphodiesterase (PDE) inhibitor, with immune modulation, anti-inflammatory, hemorheological, anti-fibrinolytic and anti-proliferation effects. Pentoxifylline can be used for the research of peripheral vascular disease, cerebrovascular disease and a number of other conditions involving a defective regional microcirculation.
|
-
- 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-103442
-
CGP52411
DAPH
|
EGFR
Amyloid-β
|
Cancer
Neurological Disease
|
CGP52411 (DAPH) is a high selective, potent, orally active and ATP-competitive EGFR inhibitor with an IC50 of 0.3 μM. CGP52411 blocks the toxic influx of Ca 2+ ions into neuronal cells, and dramatic inhibits and reverses the formation of β-amyloid (Aβ42) fibril aggregates associated with Alzheimer's disease.
|
-
- HY-121508
-
(E/Z)-IT-603
|
NF-κB
|
Cancer
Inflammation/Immunology
|
(E/Z)-IT-603 is a mixture of E-IT-603 and Z-IT-603 (IT-603). IT-603 is a c-Rel inhibitor with an IC50 of 3 μM. IT-603 has anti-tumor activity. (E/Z)-IT-603 is a promising modulator of T-cell responses in the context of graft-versus-host disease (GVHD) and malignant diseases.
|
-
- HY-139725
-
CDK5-IN-1
|
CDK
|
Metabolic Disease
|
CDK5-IN-1, a potent CDK5 inhibitor, is against CDK5 activity less than 10 nM. CDK5-IN-1 is used for kidney diseases research.
|
-
- HY-124244
-
-
- HY-14280
-
Entacapone
|
COMT
|
Neurological Disease
|
Entacapone is a potent, reversible, peripherally acting and orally active catechol-O-methyltransferase (COMT) inhibitor. Entacapone inhibits COMT from rat brain, erythrocytes and liver with IC50 values of 10 nM, 20 nM, and 160 nM, respectively. Entacapone is selective for COMT over other catecholamine metabolizing enzymes, including MAO-A, MAO-B, phenolsulphotransferase M (PST-M) and PST-P (IC50s>50 µM). Entacapone can be used for the research of Parkinson's disease. Entacapone serves as a inhibitor of FTO demethylation with an IC50 of 3.5 μM, can be used for the research of metabolic disorders.
|
-
- HY-144074
-
LRRK2-IN-4
|
LRRK2
|
Neurological Disease
|
LRRK2-IN-4 is a potent, selective, CNS-penetran and orally active leucine-rich repeat kinase 2 (LRRK2) inhobitor with an IC50 of 2.6 nM. LRRK2-IN-4 has the potential for the research of Parkinson’s disease.
|
-
- HY-148112
-
Casein kinase 1δ-IN-1
|
Casein Kinase
|
Neurological Disease
|
Casein kinase 1δ-IN-1 (compound 822) is an inhibitor of casein kinase 1 delta (CK1δ), exhibits inhibition of greater than 5%. Casein kinase 1δ-IN-1 can be used for neurodegenerative disorders such as Alzheimer's disease research.
|
-
- HY-121538
-
CUDA
|
Epoxide Hydrolase
PPAR
|
Cardiovascular Disease
|
CUDA is a potent inhibitor of soluble epoxide hydrolase (sEH), with IC50s of 11.1 nM and 112 nM for mouse sEH and human sEH, respectively. CUDA selectively increases peroxisome proliferator-activated receptor (PPAR) alpha activity. CUDA may be valuable for the research of cardiovascular disease.
|
-
- HY-116090
-
Conoidin A
|
Parasite
|
Infection
Neurological Disease
Cardiovascular Disease
|
Conoidin A is a cell permeable inhibitor of T. gondii enzyme peroxiredoxin II (TgPrxII) with nematicidal properties. Conoidin A covalently binds to the peroxidatic Cys47 of TgPrxII, irreversibly inhibiting its hyperperoxidation activity with an IC50 of 23 µM. Conoidin A also inhibits hyperoxidation of mammalian PrxI and PrxII (but not PrxIII). Conoidin A has antioxidant, neuroprotective effects and can be used for the research of ischaemic heart disease.
|
-
- HY-145443
-
Fludarabine-Cl
|
Others
|
Cancer
|
Fludarabine-Cl has inhibition effect on RNA adenosine deaminase 1(ADAR1), and can be used for preventing and/or researching cancer or tumor-related diseases.
|
-
- HY-15452
-
Selisistat
EX-527
|
Sirtuin
|
Cancer
Inflammation/Immunology
|
Selisistat (EX-527) is a potent and selective SirT1 (Sir2 in Drosophila melanogaster) inhibitor with an IC50 of 123 nM for SirT1. Selisistat alleviates pathology in multiple animal and cell models of Huntington's disease.
|
-
- HY-17623C
-
(R)-Tegoprazan
(R)-CJ-12420; (R)-RQ-00000004
|
Proton Pump
|
Metabolic Disease
|
(R)-Tegoprazan (example 3), a benzimidazole derivative, is a potent kidney H +/K +-ATPase inhibitor with an IC50 of 98 nM of canine kidney Na +/K +-ATPase. (R)-Tegoprazan has the potential for gastrointestinal diseases research.
|
-
- HY-N8598
-
Caulophine
|
Others
|
Cardiovascular Disease
|
Caulophine is a fluoroketone alkaloid isolated from Caulophyllum robustum MAXIM. Caulophine has antioxidant activity and the ability to protect cardiomyocytes from oxidative and ischemic damage, providing potential value for coronary heart disease research.
|
-
- HY-139293
-
PF-07059013
|
Others
|
Cardiovascular Disease
|
PF-07059013 is an orally active and potent noncovalent modulator of sickled hemoglobin (HbS). PF-07059013 specifically binds to Hb with nanomolar affinity and displays strong partitioning into red blood cells (RBCs). PF-07059013 can be used for sickle cell disease (SCD) research.
|
-
- HY-P99609
-
Exidavnemab
ABBV-0805; BAN-0805
|
α-synuclein
|
Neurological Disease
|
Exidavnemab (ABBV-0805; BAN-0805) is a human IgG4 monoclonal antibody that selectively targets soluble human α-synuclein aggregates with a KD value of 18.5 pM and a KD value of 2.2 μM for α-synuclein monomers. Exidavnemab is used in Parkinson's disease research.
|
-
- HY-W094474
-
Lithium chloride hydrate
hydrate/monohydrateortrihydrate
|
GSK-3
Apoptosis
|
Infection
Neurological Disease
|
Lithium chloride hydrate, an orally active mood stabilizer, is a potent virus inhibitor and effective immunomodulatory agent. Lithium chloride hydrate has antidepressant activity by inhibiting GSK3β and promoting neurogenesis. Lithium chloride hydrate alleviates cognition dysfunction and the symptoms of acute mania and depression. Lithium chloride hydrate can also be used for research of virus infection and Alzheimer's disease.
|
-
- HY-N10397
-
Maceneolignan H
|
CCR
|
Inflammation/Immunology
|
Maceneolignan H (Compound 8) is a neolignane compound isolated from the arils of Myristica fragrans. Maceneolignan H is a selective CCR3 antagonist (EC50 = 1.4 μM). Maceneolignan H has the potential for the research of allergic diseases.
|
-
- HY-P99678
-
Izokibep
ABY-035
|
Interleukin Related
|
Inflammation/Immunology
|
Izokibep (ABY-035) is a selective and antibody mimetic interleukin 17A (IL-17A) inhibitor with high potency and long half-life. Izokibep can be used for the research of ankylosing spondylitis, atherosclerosis and skin disease.
|
-
- 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-13720A
-
Pergolide mesylate
Pergolide methanesulfonate; LY127809
|
Dopamine Receptor
|
Neurological Disease
|
Pergolide mesylate (Pergolide methanesulfonate), an Ergoline derivative, is a potent and orally active dopamine D1 and D2 receptors agonist. Pergolide mesylate can be used for Parkinson's disease and hyperprolactinaemia research.
|
-
- HY-145585
-
Onfasprodil
|
iGluR
|
Neurological Disease
|
Onfasprodil is negative allosteric modulator of NR2B. Onfasprodil in combination with GABA receptor regulator has the potential for the research of Alzheimer's disease (extracted from patent CN111481543A).
|
-
- HY-P0198B
-
-
- HY-70081A
-
Sumanirole maleate
U-95666E; PNU-95666
|
Dopamine Receptor
|
Neurological Disease
|
Sumanirole maleate (U-95666E; PNU-95666E) is a highly selective D2 receptor full agonist with an ED50 of about 46 nM. Sumanirole was developed for the treatment of Parkinson's disease and restless leg syndrome.
|
-
- HY-145708
-
-
- HY-P3709
-
TRAF6 peptide
|
E1/E2/E3 Enzyme
|
Neurological Disease
|
TRAF6 peptide is a specific TRAF6-p62 inhibitor. TRAF6 peptide potently abrogates NGF-dependent TrkA ubiquitination. TRAF6 peptide has good research potential in neurological diseases such as alzheimer's disease (AD), parkinson's, ALS, head trauma, epilepsy and stroke.
|
-
- HY-107757
-
GMQ
|
Sodium Channel
|
Neurological Disease
|
GMQ is a ASIC (acid-sensing ion) channel activator with an EC50 value of 1.83 mM for ASIC3 at pH 7.4. GMQ opens only ASIC3 but no other ASICs at pH 7.4. GMQ can be used for neurological disease research.
|
-
- HY-109193
-
-
- HY-148133
-
GSK-3β inhibitor 12
|
GSK-3
|
Neurological Disease
|
GSK-3β inhibitor 12 (compound 15) is an inhibitor of GSK-3β. GSK-3β inhibitor 12 inhibits 49.11% and 37.11% activity of 25 μM and 50 μM GSK-3β, respectively. GSK-3β inhibitor 12 can be used for the research of neurodegenerative diseases.
|
-
- HY-131417
-
-
- HY-133011
-
nAChR agonist 1
|
nAChR
|
Neurological Disease
|
nAChR agonist 1 is a potent, brain-permeable, and orally efficacious positive allosteric modulator of α7 nicotinic acetylcholine receptor (α7 nAChR). nAChR agonist 1 has the EC50 of 0.32 µM in a Ca 2+ mobilization assay (PNU-282987-induced, FLIPR based) in human IMR-32 neuroblastoma cells that endogenously express α7 nAChR. nAChR agonist 1 can be develpoped for the treatment of Alzheimer’s disease.
|
-
- 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-141511
-
Coppersensor 1
|
Fluorescent Dye
|
Cancer
Neurological Disease
|
Coppersensor-1 (CS1) is a membrane-permeable fluorescent dye. Coppersensor-1 has a picomolar affinity for Cu + with high selectivity over competing cellular metalions. Coppersensor-1 as a probe, can selective and sensitive detection of copper(I) ions (Cu +) in biological samples, including live cells. Coppersensor-1 can be used for the research of imaging of severe diseases such as cancer, cardiovascular disorders and neurogenerative diseases. Storage: protect from light.
|
-
- HY-103165
-
PSB-0788
|
Adenosine Receptor
|
Cancer
Infection
|
PSB-0788 is a new selective high-affinity A2B antagonist with IC50 value of 3.64 nM and Ki value of 0.393 nM, respeactively. PSB-0788 can be used for the research for chronic inflammatory lung diseases.
|
-
- HY-N10487
-
Bleformin A
|
Cholinesterase (ChE)
|
Neurological Disease
|
Bleformin A is a potent BChE inhibitor with an IC50 value of 5.2 μM. Bleformin A is a nature product that could be isolated from Bletilla striata. Bleformin A can be used for research of Alzheimer's disease (AD).
|
-
- HY-147135
-
TEAD-IN-3
|
YAP
|
Cancer
|
TEAD-IN-3 (compound I-177) is a potent TEAD transcription factor inhibitor. TEAD-IN-3 can be used for the research of proliferative diseases (such as cancer) .
|
-
- HY-145640
-
Vimnerixin
AZD4721; RIST4721
|
CXCR
|
Inflammation/Immunology
|
Vimnerixin (AZD4721) is the potent and orally active antagonist of acidic CXC chemokine receptor 2 (CXCR2). Vimnerixin has the potential for the research of inflammatory disease.
|
-
- HY-151281
-
ALK5-IN-31
|
TGF-β Receptor
|
Cancer
|
ALK5-IN-31 (compound Ex-08) is a selective ALK-5 inhibitor (IC50≤10 nM), inhibits TGF-β-induced SMAD signaling. ALK5-IN-31 has the potential to inhibit growth of tumour in vivo. ALK5-IN-31 can be used in study of proliferative diseases such as cancer, fibrotic diseases, and systemic sclerosis.
|
-
- HY-151275
-
ALK5-IN-28
|
TGF-β Receptor
TGF-beta/Smad
|
Cancer
|
ALK5-IN-28 (compound Ex-05) is a selective ALK-5 inhibitor (IC50≤10 nM), inhibits TGF-β-induced SMAD signaling. ALK5-IN-28 has the potential to inhibit growth of tumour in vivo. ALK5-IN-28 can be used in study of proliferative diseases such as cancer, fibrotic diseases, and systemic sclerosis.
|
-
- HY-151282
-
ALK5-IN-32
|
TGF-β Receptor
TGF-beta/Smad
|
Cancer
|
ALK5-IN-32 (compound EX-09) is a selective ALK-5 inhibitor (10 nM<IC50<100 nM), inhibits TGF-β-induced SMAD signaling. ALK5-IN-32 has the potential to inhibit growth of tumour in vivo. ALK5-IN-32 can be used in study of proliferative diseases such as cancer, fibrotic diseases, and systemic sclerosis.
|
-
- HY-153011
-
-
- HY-N10443
-
Mammea A/BA
|
Parasite
Apoptosis
Autophagy
Reactive Oxygen Species
|
Infection
|
Mammea A/BA has potent activity against Trypanosoma cruzi (T. cruzi). Mammea A/BA induces mitochondrial dysfunction, reactive oxygen species (ROS) production and DNA fragmentation, and increases number of acidic vacuoles. Mammea A/BA can induce apoptosis, autophagy and necrosis. Mammea A/BA can be used for researching chagas disease.
|
-
- 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-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-44809A
-
Izilendustat hydrochloride
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
Inflammation/Immunology
|
Izilendustat (hydrochloride) is a potent inhibitor of prolyl hydroxylase which stabilizes hypoxia inducible factor- 1 alpha (HIF- lα), as well as hypoxia inducible factor-2 (HIF-2). Izilendustat (hydrochloride) has the potential for the research of HIF- lα related diseases including Peripheral Vascular Disease (PVD), Coronary Artery Disease (CAD), heart failure, ischemia, anemia, colitis, and other inflammatory bowel diseases (extracted from patent WO2011057115A1/WO2011057112A1/WO2011057121A1).
|
-
- HY-N5077
-
-
- HY-P3845
-
(Gly22)-Amyloid β-Protein (1-42)
|
Amyloid-β
|
Neurological Disease
|
(Gly22)-Amyloid β-Protein (1-42) is a peptide fragment of amyloid β-protein (Aβ). Amyloid β-protein is the primary component of both vascular and parenchymal amyloid deposits in Alzheimer's disease. Mutation of Glu22 to Gly22 in Aβ can increase aggregation.
|
-
- HY-139560
-
-
- HY-136449
-
-
- HY-147321
-
-
- HY-146272
-
-
- HY-N0702
-
Tenuifolin
|
Beta-secretase
Cholinesterase (ChE)
|
Neurological Disease
|
Tenuifolin is a triterpene isolated from Polygala tenuifolia Willd, has neuroprotective effects. Tenuifolin reduces Aβ secretion by inhibiting β-secretase. Tenuifolin improves learning and memory in aged mice by decreasing AChE activity and has the potential for Alzheimer’s disease (AD) treatment.
|
-
- HY-13204
-
Biperiden hydrochloride
KL 373 hydrochloride
|
mAChR
|
Neurological Disease
|
Biperiden (KL 373) hydrochloride is a non-selective muscarinic receptor antagonist that competitively binds to M1 muscarinic receptors, thereby inhibiting acetylcholine and enhancing dopamine signaling in the central nervous system. Biperiden hydrochloride has the potential for the research of Parkinson's disease and other related psychiatric disorders.
|
-
- HY-135825
-
TFEB activator 1
|
Autophagy
|
Neurological Disease
|
TFEB activator 1 is an orally effective, mTOR-independent activator of TFEB. TFEB activator 1 significantly promotes the nuclear translocation of Flag-TFEB with an EC50 of 2167 nM. TFEB activator 1 enhances autophagy without inhibiting the mTOR pathway and has the potential for neurodegenerative diseases treatment.
|
-
- HY-13204A
-
Biperiden
KL 373
|
mAChR
|
Neurological Disease
|
Biperiden (KL 373) is a non-selective muscarinic receptor antagonist that competitively binds to M1 muscarinic receptors, thereby inhibiting acetylcholine and enhancing dopamine signaling in the central nervous system. Biperiden has the potential for the research of Parkinson's disease and other related psychiatric disorders.
|
-
- HY-146757
-
RIPK1-IN-13
|
RIP kinase
|
Inflammation/Immunology
|
RIPK1-IN-13 (Compound 8) is a potent inhibitor of RIPK1 with an IC50 value of 1139 nM. RIPK1-IN-13 blocks the activation of the necroptosis pathway via the inhibition of RIPK1. RIPK1-IN-13 has the potential for the research of inflammation diseases.
|
-
- HY-147527
-
CDK8-IN-5
|
CDK
|
Inflammation/Immunology
|
CDK8-IN-5 is a potent CDK8 inhibitor with an IC50 of 72 nM. CDK8-IN-5 shows anti-inflammatory activities with 43% IL-10 enhancement rate. CDK8-IN-5 has the potential for the research of inflammatory bowel disease.
|
-
- HY-143615
-
RET-IN-10
|
RET
|
Cancer
|
RET-IN-10 is a potent inhibitor of RET. RET loss of function mutations leads to Hirschsprung's disease, while its gain of function mutations is associated with a variety of human tumors. RET-IN-10 has the potential for the research of cancer diseases (extracted from patent WO2021135938A1, compound 18).
|
-
- HY-14399
-
Itanapraced
CHF5074; CSP-1103
|
γ-secretase
Apoptosis
|
Neurological Disease
|
Itanapraced (CHF5074) is an orally active γ-secretase modulator and a non-steroidal anti-inflammatory derivative. Itanapraced reduces Aβ42 and Aβ40 secretion with IC50 values of 3.6 and 18.4 μM, respectively. Itanapraced inhibits cell apoptosis of hippocampal neurons induced by oxygen and glucose deprivation (OGD). Itanapraced can be used for the research of Alzheimer's disease.
|
-
- HY-B0972
-
Cinchophen
|
Bacterial
|
Inflammation/Immunology
|
Cinchophen is a potent and orally active non-steroidal anti-inflammatory agent, has analgesic and antimicrobial effects. Cinchophen can be used for the research of arthritis and some liver diseases.
|
-
- HY-131728
-
-
- HY-N7887
-
-
- HY-P9967
-
Aducanumab
BIIB037
|
Amyloid-β
|
Neurological Disease
|
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.
|
-
- HY-113643
-
-
- HY-150205
-
Succinate/succinate receptor antagonist 1
|
Others
|
Inflammation/Immunology
|
Succinate/succinate receptor antagonist 1 (compound 7a) is a succinate/succinate receptor antagonist. Succinate/succinate receptor antagonist 1 blocks succinate signaling in gingival tissue. Succinate/succinate receptor antagonist 1 inhibits the activation of succinate receptor 1 (SucnRl) with an IC50 value of 20 μΜ. Succinate/succinate receptor antagonist 1 can be used for the research of periodontal disease.
|
-
- HY-144619
-
TLR7/8 antagonist 2
|
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
TLR7/8 antagonist 2 (Compound 15) is a potent and orally active agonist of TLR7/8 with IC50s of 4.9 and 0.6 nM, respectively. Inappropriate activation of TLR7 and TLR8 is linked to several autoimmune diseases, such as lupus erythematosus. TLR7/8 antagonist 2 has the potential for the research of autoimmune diseases.
|
-
- HY-N7560
-
Safranal
|
Others
|
Inflammation/Immunology
Neurological Disease
|
Safranal is an orally active main component of Saffron (Crocus sativus) and is responsible for the unique aroma of this spice. Safranal has neuroprotective and anti-inflammatory effects and has the potential for Parkinson’s disease research.
|
-
- HY-14280A
-
Entacapone sodium salt
|
COMT
|
Neurological Disease
|
Entacapone sodium salt is a potent, reversible, peripherally acting and orally active catechol-O-methyltransferase (COMT) inhibitor. Entacapone sodium salt inhibits COMT from rat brain, erythrocytes and liver with IC50 values of 10 nM, 20 nM, and 160 nM, respectively. Entacapone sodium salt is selective for COMT over other catecholamine metabolizing enzymes, including MAO-A, MAO-B, phenolsulphotransferase M (PST-M) and PST-P (IC50s>50 µM). Entacapone sodium salt can be used for the research of Parkinson's disease. Entacapone sodium salt serves as as a inhibit of FTO demethylation with an IC50 of 3.5 μM, can be used for the research of metabolic disorders.
|
-
- HY-153224
-
GLPG2534
|
IRAK
|
Inflammation/Immunology
|
GLPG2534 is an orally active and selective IRAK4 inhibitor, with IC50 values of 6.4 nM and 3.5 nM for human and mouse IRAK4. GLPG2534 can be used for the research of inflammatory skin diseases.
|
-
- HY-N4113
-
Glycycoumarin
|
Keap1-Nrf2
AMPK
|
Cancer
|
Glycycoumarin is a potent antispasmodic agent. Glycycoumarin is a major bioactive coumarin of licorice and exhibits antispasmodic activity. Glycycoumarin also has hepatoprotective effect. Glycycoumarin can be used for the research of abdominal pain and liver diseases.
|
-
- HY-N11641
-
Methyl ganoderate A acetonide
|
Cholinesterase (ChE)
|
Neurological Disease
|
Methyl ganoderate A acetonide, a lanostane triterpene, is a natural product that could be isolated from the fruiting bodies of Ganoderma lucidum. Methyl ganoderate A acetonide is a potent AChE inhibitor with an IC50 value of 18.35 μM. Methyl ganoderate A acetonide can be used in research of Alzheimer’s disease (AD).
|
-
- HY-N5077B
-
-
- HY-U00341
-
ST4206
|
Adenosine Receptor
|
Neurological Disease
|
ST4206 is a potent and orally active adenosine A2A receptor antagonist, with Kis of 12 nM and 197 nM for adenosine A2A receptor and adenosine A1 receptor, respectively. ST4206 has the potential for Parkinson׳s disease research.
|
-
- 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-N3734
-
Deoxyneocryptotanshinone
|
Beta-secretase
Phosphatase
|
Neurological Disease
|
Deoxyneocryptotanshinone, a natural tanshinone, is a high affinity BACE1 (Beta-secretase) inhibitor with an IC50 value of 11.53 μM. Deoxyneocryptotanshinone shows a promising dose-dependent inhibition of protein tyrosine phosphatase 1B (PTP1B) with an IC50 value of 133.5 μM. Deoxyneocryptotanshinone can be used for Alzheimer's disease research.
|
-
- HY-15545
-
-
- HY-P99471
-
Bepranemab
UCB 0107
|
Tau Protein
|
Neurological Disease
|
Bepranemab (UCB 0107) is a humanized, full-length IgG4 monoclonal antibody that binds to a central tau epitope (amino acids 235-250). Bepranemab can be used for Alzheimer’s disease (AD) research.
|
-
- 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-148191
-
-
- 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-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-150058
-
Bocconoline
|
Others
|
Neurological Disease
|
Bocconoline is a potent early endosome antigen 1 (EEA1) inhibitor. Bocconoline can be isolated from Macleaya cordata. Bocconoline can be used for the research of Parkinson’s disease (PD).
|
-
- HY-B0247
-
Torsemide
Torasemide
|
Others
|
Metabolic Disease
Cardiovascular Disease
|
Torsemide (Torasemide) is an orally active loop diuretic. Torsemide has anti-aldosterone and vasodilatory effects. Torsemide also can be used for the research of heart failure, renal disease and hepatic cirrhosis.
|
-
- HY-148264
-
-
- HY-120577
-
BA 41899
|
Others
|
Cardiovascular Disease
|
BA 41899 is a purely calcium-sensitizing agent. BA 41899 is completely devoid of phosphodiesterase (PDE) III inhibitory activity or any other known inotropic mechanism. BA 41899 can be used for the research of cardiovascular diseases, such as congestive heart failure (CHF).
|
-
- HY-146344
-
Antiviral agent 17
|
Antibiotic
|
Infection
|
Antiviral agent 17 (Compound 4) is an anti-infection agent. Antiviral agent 17 retains its antiviral effect in a human replicon assay (EC50 = 0.015 μM). Antiviral agent 17 results in good antiviral activity against murine norovirus. Antiviral agent 17 has the potential for the research of infectious and malignant diseases.
|
-
- HY-151952
-
NLRP3-IN-12
|
NOD-like Receptor (NLR)
|
Inflammation/Immunology
|
NLRP3-IN-12 is a specific NLRP3 inflammasome inhibitor. NLRP3-IN-12 reduces the release of IL-1β by targeting the NLRP3 protein, with an IC50 of 0.45 μM. NLRP3-IN-12 can be used for the research of inflammatory bowel disease.
|
-
- HY-149006
-
CK156
|
DAPK
|
Inflammation/Immunology
Cancer
|
CK156 is a highly selective death-associated protein kinase (DAPK) inhibitor with IC50s of 182 nM,34 μM, and 39 μM in the DRAK1 NanoBRET assay for DRAK1, CK2a1, and CK2a2, respectively. CK156 can be used for the research of autoimmune and inflammatory diseases.
|
-
- HY-103308
-
TRAM-39
|
Potassium Channel
|
Neurological Disease
|
TRAM-39 is a selective blocker of intermediate conductance Ca2+-activated K+ (IKCa) channels. TRAM-39 inhibits KCa3.1 channel with an IC50 value of 60 nM. TRAM-39 can be used for the research of ataxia, epilepsy, memory disorders, schizophrenia and Parkinson’s disease.
|
-
- 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-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-N1428C
-
-
- HY-N1179
-
-
- HY-P1051
-
β-Amyloid (12-28)
Amyloid β-Protein (12-28)
|
Amyloid-β
|
Neurological Disease
|
β-Amyloid (12-28) (Amyloid β-Protein (12-28)) is a peptide fragment of β-amyloid protein (β1-42). β1-42, a 42 amino acid protein , is the major component of senile plaque cores. β-Amyloid (12-28) shows aggregation properties. β-Amyloid (12-28) has the potential for Alzheimer’s disease research.
|
-
- HY-12176B
-
Aliskiren fumarate
CGP 60536 fumarate; CGP60536B fumarate; SPP 100 fumarate
|
Renin
Autophagy
|
Cancer
Cardiovascular Disease
|
Aliskiren fumarate is an orally active, highly potent and selective renin inhibitor, with IC50 of 1.5 nM. Aliskiren fumarate can be used for the research of hypertension, cardiovascular diseases and cancer cachexia.
|
-
- HY-12176
-
Aliskiren
CGP 60536; CGP60536B; SPP 100
|
Renin
Autophagy
|
Cardiovascular Disease
Cancer
|
Aliskiren is an orally active, highly potent and selective renin inhibitor, with IC50 of 1.5 nM. Aliskiren can be used for the research of hypertension, cardiovascular diseases and cancer cachexia.
|
-
- HY-N3702
-
Dehydroabietinol
|
Syk
|
Inflammation/Immunology
|
Dehydroabietinol is an abietane diterpenoid. Dehydroabietinol has kinase inhibition activity for spleen tyrosine kinase (SYK) with an IC50 value of 46.4 μM. Dehydroabietinol can be used for the research of immune-mediated disease.
|
-
- HY-149243
-
BChE-IN-16
|
Cholinesterase (ChE)
|
Neurological Disease
|
BChE-IN-16 (compound 87) is a highly potent BChE inhibitor with an IC50 of 3.8 nM for hBChE. BChE-IN-16 has low cytotoxicity, potential CNS permeability, unique adaptability and can be used in Alzheimer's disease (AD) research.
|
-
- HY-142670
-
Lp-PLA2-IN-5
|
Phospholipase
|
Metabolic Disease
Neurological Disease
|
Lp-PLA2-IN-5 is a potent inhibitor of lipoprotein-associated phospholipase A2 (Lp-PLA2). Lp-PLA2 previously known as platelet- activating factor acetylhydrolase (PAF-AH), is a phospholipase A2 enzyme involved in hydrolysis of lipoprotein lipids or phospholipids. Lp-PLA2-IN-5 has the potential for the research of diseases associated with the activity of Lp-PLA2, for example atherosclerosis, Alzheimer's disease (extracted from patent WO2021228159A1, compound 32).
|
-
- HY-142669
-
Lp-PLA2-IN-4
|
Phospholipase
|
Metabolic Disease
Neurological Disease
|
Lp-PLA2-IN-4 is a potent inhibitor of lipoprotein-associated phospholipase A2 (Lp-PLA2). Lp-PLA2 previously known as platelet- activating factor acetylhydrolase (PAF-AH), is a phospholipase A2 enzyme involved in hydrolysis of lipoprotein lipids or phospholipids. Lp-PLA2-IN-4 has the potential for the research of diseases associated with the activity of Lp-PLA2, for example atherosclerosis, Alzheimer's disease (extracted from patent WO2021228159A1, compound 38).
|
-
- HY-148071
-
Epocholeone
|
Others
|
Others
|
Epocholeone is a growth regulator. Epocholeone can control fungal or physiological diseases of crops.
|
-
- HY-14179
-
PPQ-102
CFTR Inhibitor
|
CFTR
|
Others
|
PPQ-102 (CFTR Inhibitor) is a reversible CFTR inhibitor that completely inhibits CFTR chloride currents (IC50 ~90 nM). PPQ-102 is not affected by membrane potential-dependent cell allocation or blocking efficiency (uncharged at physiological pH) and effectively prevents cyst enlargement in polycystic kidney disease.
|
-
- HY-147529
-
mGluR2 modulator 3
|
mGluR
|
Neurological Disease
|
mGluR2 modulator 3 (compound 1) is a potent mGluR2 positive allosteric modulator with an EC50 value of 0.87 μM. mGluR2 modulator 3 has activity in psychosis disease models such as methamphetamine-induced hyperactivity and mescaline-induced scratching in mice.
|
-
- HY-14202
-
Lazabemide hydrochloride
Ro 19-6327 hydrochloride
|
Monoamine Oxidase
|
Neurological Disease
|
Lazabemide hydrochloride (Ro 19-6327 hydrochloride) is a selective, reversible inhibitor of monoamine oxidase B (MAO-B) (IC50=0.03 μM) but less active for MAO-A (IC50>100 μM). Lazabemide inhibits monoamine uptake at high concentrations, the IC50 values are 86 μM, 123 μM and >500 μM for noradrenalin, serotonin and dopamine uptake, respectively. Lazabemide can be used for the research of parkinson and alzheimer′s disease.
|
-
- HY-14201
-
Lazabemide
Ro 19-6327
|
Monoamine Oxidase
|
Neurological Disease
|
Lazabemide (Ro 19-6327) is a selective, reversible inhibitor of monoamine oxidase B (MAO-B) (IC50=0.03 μM) but less active for MAO-A (IC50>100 μM). Lazabemide inhibits monoamine uptake at high concentrations, the IC50 values are 86 μM, 123 μM and >500 μM for noradrenalin, serotonin and dopamine uptake, respectively. Lazabemide can be used for the research of parkinson and alzheimer′s disease.
|
-
- HY-116228
-
Cadrofloxacin
Caderofloxacin; CS-940
|
Bacterial
|
Infection
|
Cadrofloxacin (Caderofloxacin; CS-940), a orally active fluoroquinolone, is effective against aerobic/anaerobic Gram-positive and Gram-negative bacteria. Cadrofloxacin can be used for the research of infectious diseases.
|
-
- HY-151388
-
hMAO-B/MB-COMT-IN-1
|
Monoamine Oxidase
COMT
|
Neurological Disease
|
hMAO-B/MB-COMT-IN-1 is a dual MAO-B/MB-COMT inhibitor (IC50s: 2.5 μΜ for hMAO-B, 3.84 μΜ for MB-COMT). hMAO-B/MB-COMT-IN-1 protects cells against oxidative damage. hMAO-B/MB-COMT-IN-1 can be used in the research of neurodegeneration disease, such as Parkinson’s Disease (PD).
|
-
- HY-151390
-
hMAO-B/MB-COMT-IN-2
|
Monoamine Oxidase
COMT
|
Neurological Disease
|
hMAO-B/MB-COMT-IN-2 is a dual MAO-B/MB-COMT inhibitor (IC50s: 4.27 μΜ for hMAO-B, 2.69 μΜ for MB-COMT). hMAO-B/MB-COMT-IN-2 protects cells against oxidative damage. hMAO-B/MB-COMT-IN-2 can be used in the research of neurodegeneration disease, such as Parkinson’s Disease (PD).
|
-
- HY-153593
-
BET bromodomain inhibitor 3
|
Epigenetic Reader Domain
|
Cancer
|
BET bromodomain inhibitor 3 is BET bromodomain inhibitor. BET bromodomain inhibitor 3 has inhibitory effect against BrdT with Ki value of > 40 µM. BET bromodomain inhibitor 3 can be used for the research of contraception, cancer, and heart disease.
|
-
- HY-13733
-
-
- HY-13733A
-
-
- HY-126362
-
ML266
|
Glucosidase
|
Others
|
ML266 is glucocerebrosidase (GCase) molecule chaperone with IC50 of 2.5 µM. ML266 binds to GCase and transports of the mutant protein to the lysosome, and resume the activity of GCase. ML266 dose not inhibit the GCase enzyme’s action. ML266 has the potential for the research of gaucher disease.
|
-
- HY-18137
-
PF-04995274
|
5-HT Receptor
|
Neurological Disease
|
PF-04995274 is a potent, high-affinity, orally active and partial serotonin 4 receptor (5-HT4R) agonist. PF-04995274 has an EC50 range of 0.26-0.47 nM for human 5-HT4A/4B/4D/4E (Ki range of 0.15-0.46 nM), and has an EC50 range of 0.59-0.65 nM for rat 5-HT4S/4L/4E (Ki of 0.30 nM for rat 5-HT4S). PF-04995274 is brain penetrant and can be used for cognitive disorders associated with Alzheimer's disease.
|
-
- HY-11044
-
-
- HY-117661
-
SPHINX31
|
SRPK
VEGFR
|
Cancer
Cardiovascular Disease
|
SPHINX31 is a potent and selective SRPK1 inhibitor, with an IC50 of 5.9 nM. SPHINX31 inhibits phosphorylation of serine/arginine-rich splicing factor 1 (SRSF1). SPHINX31 also decreases the mRNA expression of pro-angiogenic VEGF-A165a isoform. SPHINX31 can be used to research neovascular eye disease.
|
-
- HY-145428
-
BT-GSI
|
Notch
γ-secretase
|
Cancer
|
BT-GSI is a γ-secretase inhibitor (GSI) and a bone-targeted Notch inhibitor. BT-GSI has dual anti-myeloma and anti-resorptive properties, which can be used for the research of multiple myeloma and associated bone disease. BT-GSI inhibits tumor growth and osteolytic disease progression.
|
-
- HY-144270
-
-
- HY-B1487
-
Procyclidine hydrochloride
Tricyclamol hydrochloride; (±)-Procyclidine hydrochloride
|
iGluR
mAChR
|
Neurological Disease
|
Procyclidine (Tricyclamol, (±)-Procyclidine) hydrochloride , an anticholinergic agent, is a muscarinic receptor antagonist that also has the properties of an N-methyl-D-aspartate (NMDA) antagonist. Procyclidine hydrochloride can be used in studies of Parkinson's disease and related psychiatric disorders such as Soman-induced epilepsy.
|
-
- HY-B1487A
-
Procyclidine
Tricyclamol; (±)-Procyclidine
|
mAChR
iGluR
|
Neurological Disease
|
Procyclidine (Tricyclamol; (±)-Procyclidine), an anticholinergic agent, is a muscarinic receptor antagonist that also has the properties of an N-methyl-D-aspartate (NMDA) antagonist. Procyclidine can be used in studies of Parkinson's disease and related psychiatric disorders such as Soman-induced epilepsy.
|
-
- HY-P1051A
-
β-Amyloid (12-28) (TFA)
Amyloid β-Protein (12-28) (TFA); Amyloid Beta-Peptide (12-28) (human) TFA; β-Amyloid protein fragment(12-28) TFA
|
Amyloid-β
|
Neurological Disease
|
β-Amyloid (12-28) (TFA) (Amyloid β-Protein (12-28) (TFA)) is a peptide fragment of β-amyloid protein (β1-42). β1-42, a 42 amino acid protein , is the major component of senile plaque cores. β-Amyloid (12-28) (TFA) shows aggregation properties. β-Amyloid (12-28) (TFA) has the potential for Alzheimer’s disease research.
|
-
- HY-138281
-
Complement factor D-IN-2
|
Complement System
|
Inflammation/Immunology
|
Complement factor D-IN-2 is an inhibitor of complement factor D extracted from patent WO2015130838A1, compound 190. Complement factor D-IN-2 targets factor D and inhibits the complement cascade at an early and essential point in the alternative complement pathway. Complement factor D-IN-2 can be used for the research of autoimmune diseases.
|
-
- HY-144032
-
Tyk2-IN-9
|
JAK
|
Inflammation/Immunology
|
Tyk2-IN-9 (Compound 26) is a selective Tyk-2 inhibitor with IC50s of 0.076 and 1.8 nM for TYK2-JH2 and JAK1-JH2, respectively. Tyk2-IN-9 can be used for the research of inflammatory or autoimmune disease.
|
-
- 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-146033
-
HPV18-IN-1
|
HPV
|
Cancer
|
HPV18-IN-1 (Compound H1) is a potent inhibitor of HPV18. HPV18-IN-1 prevents cervical cancer cells from premature cell procession and abnormal proliferation. HPV18-IN-1 supresses E7-Rb-E2F cellular pathway and DNA methylation. HPV18-IN-1 has the potential for the research of cancer diseases.
|
-
- HY-142779
-
Lp-PLA2-IN-11
|
Phospholipase
|
Metabolic Disease
Neurological Disease
|
Lp-PLA2-IN-11 is a potent inhibitor of lipoprotein-associated phospholipase A2 (Lp-PLA2). Lp-PLA2 previously known as platelet- activating factor acetylhydrolase (PAF-AH), is a phospholipase A2 enzyme involved in hydrolysis of lipoprotein lipids or phospholipids. Lp-PLA2-IN-11 has the potential for the research of diseases associated with the activity of Lp-PLA2, for example atherosclerosis, Alzheimer's disease (extracted from patent WO2014114249A1, compound E145).
|
-
- HY-148092
-
(S)-PM-43I
|
STAT
|
Cancer
Inflammation/Immunology
|
(S)-PM-43I is a potent STAT6 inhibitor and can reduce STAT6 phosphorylation level. (S)-PM-43I can be used in allergic lung disease, allergic rhinitis, chronic pulmonary obstructive disease and cancer research[1].
|
-
- HY-B1015
-
Etosalamide
Ethosalamide
|
Others
|
Inflammation/Immunology
|
Etosalamide (Ethosalamide) is an antipyretic and analgesic agent. Etosalamide has anti-inflammatory activity and can be used for allergic disease research.
|
-
- HY-103033
-
T.cruzi-IN-1
|
Parasite
|
Infection
|
T.cruzi-IN-1 is a potent Trypanosoma cruzi inhibitor with an IC50 of 8 nM. T.cruzi-IN-1, a 4-trifluoromethyl substituted analog, has the potential for both the acute and chronic stages of Chagas disease.
|
-
- HY-142059
-
-
- HY-144324
-
AChE-IN-6
|
Cholinesterase (ChE)
|
Neurological Disease
|
AChE-IN-6 (Compound 12a) is an optimal multifunctional ligand with significant inhibition of AChE (EeAChE, IC50 = 0.20 μM; HuAChE, IC50 = 37.02 nM) and anti-Aβ activity (IC50 = 1.92 μM for self-induced Aβ1-42 aggregation; IC50 = 1.80 μM for disaggregation of Aβ1-42 fibrils; IC50 = 2.18 μM for Cu2+-induced Aβ1-42 aggregation; IC50 = 1.17 μM for disaggregation of Cu2+-induced Aβ1-42 fibrils). AChE-IN-6 has the potential for the research of Alzheimer's disease.
|
-
- HY-107901
-
Pparδ agonist 1
|
PPAR
|
Metabolic Disease
Cardiovascular Disease
|
Pparδ agonist 1 is a PPAR-δ agonist, with an EC50 of 5.06 nM, used in the research of PPAR-delta related diseases, such as mitochondrial diseases, muscular diseases, vascular diseases, demyelinating diseases and metabolic diseases.
|
-
- HY-122052
-
UK‑396082
|
Others
|
Metabolic Disease
|
UK‑396082 is a potent thrombin activated fibrinolytic inhibitor (TAFI) inhibitor. UK‑396082 increases plasmin activity and induces a parallel decrease in ECM levels. UK‑396082 can be used in research of chronic kidney disease (CKD).
|
-
- HY-137122
-
-
- HY-120274
-
-
- HY-146035
-
AChE-IN-14
|
Cholinesterase (ChE)
Histamine Receptor
|
Neurological Disease
|
AChE-IN-14 (compound 5) is a potent cholinesterase inhibitor with IC50s of 0.46 , 0.48, and 0.44 μM for electric eel acetylcholinesterase (eeAChE), human recombinant acetylcholinesterase (hAChE), and equine serum butyrylcholinesterase (eqBuChE), respectively. AChE-IN-14 exhibits high affinity toward human H3 receptor (H3R; Ki= 159.8 nM). AChE-IN-14 can be used for the research of Alzheimer’s disease.
|
-
- HY-12282
-
GNE-9605
|
LRRK2
|
Neurological Disease
|
GNE-9605 is a potent, orally active, selective Leucine-rich repeat kinase 2 (LRRK2) inhibitor with an IC50 value of 18.7 nM. GNE-9605 inhibits LRRK2 Ser1292 autophosphorylation. GNE-9605 can be used in research of Parkinson's disease (PD) .
|
-
- HY-120970
-
-
- HY-13204B
-
Biperiden lactate
KL 373 lactate
|
mAChR
|
Neurological Disease
|
Biperiden (KL 373) lactate is an orally active non-selective muscarinic receptor antagonist that competitively binds to M1 muscarinic receptors. Biperiden (KL 373) lactate inhibits acetylcholine and enhances dopamine signaling in the central nervous system. Biperiden (KL 373) lactate has the potential for the research of Parkinson's disease and other related psychiatric disorders.
|
-
- HY-N10701
-
AChE/BChE-IN-11
|
Cholinesterase (ChE)
|
Neurological Disease
|
AChE/BChE-IN-11 (compound 1) is a potent is a dual AChE and BChE inhibitor with IC50 values of 70 and 71 μM for AChE and BChE, respectively. AChE/BChE-IN-11 is a natural product that could be isolated from the leaf of artichoke . AChE/BChE-IN-11 can be used in research of Alzheimer’s disease (AD) research.
|
-
- HY-144316
-
ZLWH-23
|
Cholinesterase (ChE)
GSK-3
|
Neurological Disease
|
ZLWH-23 is a selective AChE inhibitor (IC50=0.27 μM) with GSK-3β inhibitory property (IC50=6.78 μM). ZLWH-23 possesses selectivity for AChE over BChE (IC50=20.82 μM) and for GSK-3β over multi-kinases. ZLWH-23 has the potential for the research of Alzheimer's disease.
|
-
- HY-148141
-
JPE-1375
|
Complement System
|
Inflammation/Immunology
|
JPE-1375 is a complement C5a receptor 1 (C5aR1) antagonist. JPE-1375 effectively inhibits polymorphonuclear leukocyte mobilization (EC50=6.9 µM) and reduces TNF levels (EC50=4.5 µM) in mice. JPE-1375 can be used in studies of autoimmune and inflammatory diseases.
|
-
- HY-144087
-
TYK2-IN-11
|
JAK
|
Inflammation/Immunology
|
TYK2-IN-11 (Compound 5B) is a selective Tyk-2 inhibitor with IC50s of 0.016 and 0.31 nM for TYK2-JH2 and JAK1-JH2, respectively. TYK2-IN-11 can be used for the research of inflammatory or autoimmune disease.
|
-
- HY-16361A
-
Omigapil maleate
CGP3466B; CGP3446 maleate; TCH346 maleate
|
Apoptosis
|
Metabolic Disease
Neurological Disease
|
Omigapil maleate, an orally bioavailable GAPDH nitrosylation inhibitor, abrogates Aβ1-42-induced tau acetylation, memory impairment, and locomotor dysfunction in mice. Omigapil maleate has the potential for the research of Alzheimer's disease. Omigapil maleate (CGP3446B maleate) is a apoptosis inhibitor. Omigapil maleate can be used for the research of congenital muscular dystrophy (CMD).
|
-
- HY-10563
-
Sarpogrelate
MCI-9042 free acid
|
5-HT Receptor
|
Infection
|
Sarpogrelate (MCI-9042) is a new, specific orally active 5-HT2 receptor antagonist, Sarpogrelate increases platelet aggregation and has hemostasis effect, and can be used for the research of Buerger’s disease.
|
-
- HY-148068
-
STING agonist-20
|
STING
|
Cancer
Inflammation/Immunology
|
STING agonist-20 (compound 95) is a potent STING agonist used in the synthesis of XMT-2056. STING agonist-20 can be used as a vaccine adjuvant in the study of cancer and other inflammatory, immune diseases.
|
-
- HY-70069
-
-
- HY-114231B
-
ELX-02 disulfate
NB-124 disulfate
|
Others
|
Metabolic Disease
|
ELX-02 disulfate (NB-124 disulfate) is an investigational, advanced synthetic eukaryotic ribosome selective glycoside (ERSG). ELX-02 disulfate is being developed as a therapy for genetic diseases caused by nonsense mutations.
|
-
- HY-114231C
-
ELX-02 sulfate
NB-124 sulfate
|
Others
|
Metabolic Disease
|
ELX-02 sulfate (NB-124 sulfate) is an investigational, advanced synthetic eukaryotic ribosome selective glycoside (ERSG). ELX-02 sulfate is being developed as a therapy for genetic diseases caused by nonsense mutations.
|
-
- HY-145581
-
Mitiperstat
AZD4831
|
Glutathione Peroxidase
|
Cardiovascular Disease
|
Mitiperstat (AZD4831) is the potent inhibitor of myeloperoxidase (MPO). Mitiperstat is particularly useful in the research of prophylaxis of cardiovascular disorders such as heart failure and coronary artery disease related conditions (extracted from patent US20160152623A1).
|
-
- HY-151152
-
AChE-IN-24
|
Cholinesterase (ChE)
|
Neurological Disease
|
AChE-IN-24 is a potent AChE inhibitor and can penetrate the BBB. AChE-IN-24 has the mighty inhibitory activity to hAChE with an IC50 value of 0.053 μM. AChE-IN-24 can be used for the research of Alzheimer s disease (AD).
|
-
- HY-111263
-
NIAD-4
|
Amyloid-β
|
Neurological Disease
|
NIAD-4 is a fluorophore for optical imaging of amyloid-β (Aβ) in the central nervous system (CNS) for Alzheimer’s disease (AD). NIAD-4 binds to the same Aβ site with the binding affinity (Ki) of 10 nM. Storage: protect from light.
|
-
- HY-142777
-
Lp-PLA2-IN-9
|
Phospholipase
|
Neurological Disease
|
Lp-PLA2-IN-9 (compound 17), a tetracyclic pyrimidinone compound, is a potent Lp-PLA2 inhibitor with a pIC50 of 10.1 for rhLp-PLA2. Lp-PLA2-IN-9 has the potential for neurodegenerative related diseases research.
|
-
- HY-142774
-
Lp-PLA2-IN-6
|
Phospholipase
|
Neurological Disease
|
Lp-PLA2-IN-6 (compound 18), a tetracyclic pyrimidinone compound, is a potent Lp-PLA2 inhibitor with a pIC50 of 10.0 for rhLp-PLA2. Lp-PLA2-IN-6 has the potential for neurodegenerative related diseases research.
|
-
- HY-A0270
-
Diphenidol
|
Others
|
Neurological Disease
|
Diphenidol is an orally active antiemetic. Diphenidol reduces abnormal neuropathic pain and TNF-α overexpression in rats following chronic compression injury. Diphenidol also has local anaesthetic activity and inhibits sodium currents. Diphenidol can be used in studies of meniere′s disease, anti-vertigo, antiemetic and analgesia.
|
-
- HY-109001A
-
(1S,2R)-Alicapistat
(1S,2R)-ABT-957
|
Proteasome
|
Neurological Disease
|
(1S,2R)-Alicapistat ((1S,2R)-ABT-957) is an orally active selective inhibitor of human calpains 1 and 2 for the potential application of Alzheimer's disease (AD). (1S,2R)-Alicapistat mitigates the metabolic liability of carbonyl reduction and inhibits calpain 1 with an IC50 value of 395 nM.
|
-
- HY-12176A
-
Aliskiren hydrochloride
CGP 60536 hydrochloride; CGP60536B hydrochloride; SPP 100 hydrochloride
|
Renin
Autophagy
|
Cancer
Cardiovascular Disease
|
Aliskiren (CGP 60536; CGP60536B; SPP 100) hydrochloride is an orally active and selective renin inhibitor, with IC50 of 1.5 nM. Aliskiren hydrochloride can be used for the research of hypertension, cardiovascular diseases and cancer cachexia -.
|
-
- 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-144266
-
-
- HY-P3761
-
Ac-Tyr-Val-Lys-Asp-aldehyde
|
Caspase
|
Others
|
Ac-Tyr-Val-Lys-Asp-aldehyde is a caspase-1 inhibitor, can be used for disease research including anemia-associated to chronic diseases, chemotherapy-induced anemia and Diamond-Blackfan anemia.
|
-
- HY-10469
-
-
- HY-144669
-
ALDH1A3-IN-2
|
Aldehyde Dehydrogenase (ALDH)
|
Cancer
|
ALDH1A3-IN-2 (Compound 15) is a potent inhibitor of ALDH1A3 with an IC50 of 1.29 μM. Aldehyde dehydrogenases (ALDHs) are overexpressed in various tumor types including prostate cancer. ALDH1A3-IN-2 has the potential for the research of cancer diseases.
|
-
- HY-144671
-
ALDH3A1-IN-2
|
Aldehyde Dehydrogenase (ALDH)
|
Cancer
|
ALDH3A1-IN-2 (Compound 19) is a potent inhibitor of ALDH3A1 with an IC50 of 1.29 μM. Aldehyde dehydrogenases (ALDHs) are overexpressed in various tumor types including prostate cancer. ALDH3A1-IN-2 has the potential for the research of cancer diseases.
|
-
- HY-151928
-
JNK3 inhibitor-3
|
JNK
|
Neurological Disease
|
JNK3 inhibitor-3 (compound 15g) is a selective, BBB permeable and orally active c-Jun N-terminal kinase 3 (JNK3) inhibitor. JNK3 inhibitor-3 has inhibitory activities to JNK1, JNK2 and JNK3 with IC50 values of 147.8, 44.0 and 4.1 nM, respectively. JNK3 inhibitor-3 significantly improves the memory in mouse dementia model. JNK3 inhibitor-3 can be used for the research of Alzheimer’s disease.
|
-
- HY-10035
-
TTA-P2
T-Type calcium channel inhibitor
|
Calcium Channel
|
Neurological Disease
|
TTA-P2 (T-Type calcium channel inhibitor) is a potent inhibitor of T-Type calcium channel. TTA-P2 penetrates well the CNS and blocks the native T-type currents in deep cerebellar nuclear neurons, the window current is completely abolished both for wild-type and mutant Cav3.1 channels. TTA-P2 has the potential for the research of neurology disease.
|
-
- 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-N10384
-
AChE-IN-17
|
Cholinesterase (ChE)
|
Neurological Disease
|
AChE-IN-17 (compound 1) is a potent AChE inhibitor with an IC50 value of 28.98 μM. AChE-IN-17 can significantly prevent H2O2-induced PC12 cell death, exhibiting excellent neuroprotective effect. AChE-IN-17 can be used for researching neurodegenerative diseases (NDs).
|
-
- HY-143438
-
2-PAT
|
Monoamine Oxidase
|
Neurological Disease
|
2-PAT, an analogue of Rasagiline and Selegiline, a reversible MAO-A inhibitor with an IC50 of 0.721 µM. 2-PAT is an inactivator of MAO-B with an IC50 of 14.6 µM. 2-PAT has the potential for Parkinson’s disease and depression research.
|
-
- HY-115910
-
Y13g
|
Cholinesterase (ChE)
Interleukin Related
|
Neurological Disease
|
Y13g is the potent inhibitor of both AChE and IL-6. Interleukin-6 (IL-6) and acetylcholinesterase (AChE) are two important targets implicated in progression of Alzheimer's Disease (AD). Y13g reverses the STZ-induced memory deficit, and shows histopathology similarly as in normal animals.
|
-
- HY-124729
-
BL-918
|
ULK
Autophagy
|
Neurological Disease
|
BL-918 is an orally active UNC-51-like kinase 1 (ULK1) activator with an EC50 of 24.14 nM. BL-918 exerts its cytoprotective autophagic effect by targeting ULK complex. BL-918 has the potential for Parkinson’s disease (PD) treatment.
|
-
- HY-152112
-
-
- HY-B0384
-
-
- HY-100713
-
-
- HY-146346
-
HD-TAC7
|
PROTACs
HDAC
|
Inflammation/Immunology
|
HD-TAC7 is a potent PROTAC HDAC degrader with IC50 values of 3.6 μM, 4.2 μM and 1.1 μM for HDAC1, HDAC2 and HDAC3, respectively. HD-TAC7 can decreases NF-κB p65 in RAW 264.7 macrophages. HD-TAC7 can be used for the research of inflammatory diseases like asthma and chronic obstructive pulmonary disease (COPD).
|
-
- HY-151483
-
TK-129
|
Histone Demethylase
|
Cardiovascular Disease
|
TK-129 is an orally active, low-toxicity, potent KDM5B inhibitor (with high affinity; IC50=44 nM). TK-129 exerts cardioprotective effects by inhibiting KDM5B and blocking the KDM5B-associated Wnt pathway. TK-129 reduces ang II-induced activation of cardiac fibroblasts in vitro and reduces isoprenaline-induced myocardial remodelling and fibrosis in vivo. TK-129 can be used in studies of cardiovascular disease.
|
-
- HY-110157
-
AC-186
|
Estrogen Receptor/ERR
|
Neurological Disease
|
AC-186 is a selective non-steroidal estrogen receptor β (ERβ) agonist with EC50s of 6 nM and 5000 nM for ERβ and ERα, respectively. AC-186 shows gender specific neuroprotection in a Parkinson’s Disease rat model.
|
-
- HY-150069
-
UBX1325
|
Bcl-2 Family
Apoptosis
|
Metabolic Disease
|
UBX1325 is an Bcl-xL inhibitor that promotes apoptosis in senescent cells. UBX1325 is a potent anti-aging agent that can be used in studies of age-related eye diseases such as diabetic macular oedema (DME), age-related macular degeneration (AMD) and diabetic retinopathy (DR).
|
-
- HY-136584
-
2,2,14,14-Tetramethyl-8-oxopentadecanedioic acid
|
Others
|
Metabolic Disease
Cardiovascular Disease
|
2,2,14,14-Tetramethyl-8-oxopentadecanedioic acid is a ketone compound extracted from patent WO2002030860A2, compound example II-9. 2,2,14,14-Tetramethyl-8-oxopentadecanedioic acid can be used for the research of cardiovascular diseases, dyslipidemias, dysproteinemias, and glucose metabolism disorders.
|
-
- HY-W193545A
-
EGR240
|
Others
|
Cancer
Inflammation/Immunology
|
EGR240 is a branched-chain amino acid aminotransferase 1 (BCAT1) inhibitor. EGR240 can be used for the research of cancer, rheumatoid arthritis, and bone disease.
|
-
- HY-144373
-
-
- HY-D1168
-
Oil Red O
|
Fluorescent Dye
|
Metabolic Disease
|
Oil Red O is a fat-soluble diazol dye, with a maximum absorption at 518 nm. Oil Red O stains neutral lipids and cholesteryl esters but not biological membranes. Oil Red O can be used for detecting and quantifying hepatic steatosis in mouse liver biopsies. Oil Red O staining efficiently helps to visualize the radical changes that occur in tissues as metabolic disease occurs and progresses.
|
-
- HY-116100
-
-
- HY-151488
-
CypD-IN-4
|
Sirtuin
|
Cancer
Metabolic Disease
Neurological Disease
|
CypD-IN-4 is a potent and subtype-selective cyclophilin D (CypD) inhibitor. CypD-IN-4 has CypD affinity with an IC50 value of 0.057 μM. CypD-IN-4 can be used for the research of several diseases including oxidative stress, neurodegenerative disorders, liver diseases, aging, autophagy and diabetes.
|
-
- HY-151487
-
CypD-IN-3
|
Sirtuin
|
Cancer
Metabolic Disease
Neurological Disease
|
CypD-IN-3 is a potent and subtype-selective cyclophilin D (CypD) inhibitor. CypD-IN-3 has CypD affinity with an IC50 value of 0.01 μM. CypD-IN-3 can be used for the research of several diseases including oxidative stress, neurodegenerative disorders, liver diseases, aging, autophagy and diabetes.
|
-
- HY-B1365
-
-
- HY-N3383
-
Ligustroside
Ligstroside
|
Mitochondrial Metabolism
|
Neurological Disease
|
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.
|
-
- HY-143260
-
GSK-3β inhibitor 6
|
GSK-3
|
Cancer
Metabolic Disease
Inflammation/Immunology
|
GSK-3β inhibitor 6 is a potent GSK-3β inhibitor with an IC50 value of 24.4 μM. GSK-3β inhibitor 6 shows high hepatocyte glucose uptake (38%). GSK-3β inhibitor 6 can be used in the research of numerous diseases like diabetes, inflammation, cancer, Alzheimer's disease, and bipolar disorder.
|
-
- HY-115744
-
-
- HY-P1206
-
CH 275
|
Somatostatin Receptor
|
Neurological Disease
|
CH 275 is a peptide analog of somatostatin and binds preferably to somatostatin receptor 1 (sst1) with a Ki of 52 nM. CH 275 acts as a potent and selective sst1 agonist (IC50=30.9 nM) and also displays IC50 values of 345 nM, >1 μM, >10 μM, >10 μM for human sst3, sst4, sst2 and sst5, respectively. CH 275 can be used for the research of alzheimer’s disease.
|
-
- HY-D0205A
-
-
- HY-P3410
-
Trichomide A
|
SHP2
Phosphatase
|
Inflammation/Immunology
|
Trichomide A is a potent activator of SHP2. Trichomide A is a natural cyclodepsipeptide. Trichomide A displays immunosuppressive activity against activated T lymphocyte–mediated immune responses in Con A-activated T cells. Trichomide A have the potential for the research of immune-related skin diseases.
|
-
- HY-110237
-
BX430
|
P2X Receptor
Calcium Channel
|
Cardiovascular Disease
|
BX430 is a potent and selective noncompetitive allosteric human P2X4 receptor channels antagonist with an IC50 of 0.54 μM. BX430 has species specificity. BX430 is used for chronic pain and cardiovascular disease.
|
-
- HY-12177
-
Aliskiren hemifumarate
CGP 60536 hemifumarate; CGP60536B hemifumarate; SPP 100 hemifumarate
|
Renin
Autophagy
|
Cardiovascular Disease
Cancer
|
Aliskiren (CGP 60536; CGP60536B; SPP 100) hemifumarate is an orally active and selective renin inhibitor, with IC50 of 1.5 nM. Aliskiren hemifumarate can be used for the research of hypertension, cardiovascular diseases and cancer cachexia.
|
-
- HY-146405
-
-
- HY-121765
-
Dacisteine
N,S-Diacetyl-L-cysteine
|
Endogenous Metabolite
|
Metabolic Disease
|
Dacisteine (N,S-Diacetyl-L-cysteine) is a cysteine derivative and displays a less New Delhi metallo-beta-lactamase-1 (NDM-1) inhibitor with an IC50 value of 1000 μM. Dacisteine can be used for the treatment of cardiovascular and cerebrovascular diseases caused by platelet aggregation.
|
-
- HY-125996
-
NR1H4 activator 1
|
FXR
|
Inflammation/Immunology
|
NR1H4 activator 1 is a potent and selective Famesoid X Receptor (FXR) agonist, extracted from patent WO2018152171A1, example 4. NR1H4 activator 1 shows strong FXR agonistic potency with a EC50 value of 1 nM in a Human FXR (NR1H4) Assay. NR1H4 activator 1 has the potential for treatment of gastrointestinal disease.
|
-
- HY-143792
-
HTT-D3
|
P-glycoprotein
|
Neurological Disease
|
HTT-D3 is a potent and orally active huntingtin (HTT) splicing modulator. HTT-D3 acts by promoting the inclusion of a pseudoexon containing a premature termination codon (stop-codon psiExon), leading to HTT mRNA degradation and reduction of HTT levels. HTT-D3 reduces p-glycoprotein (P-gp) efflux, and can be uesd for Huntington's disease research.
|
-
- HY-110279
-
Ogerin
|
GPR68
|
Neurological Disease
|
Ogerin is a selective GPR68 positive aliasing modulator (PAM) (pEC50=6.83) with a moderate antagonistic effect on A2A (Ki=220 nM). Ogerin inhibits the fear conditioning reflex in mice and also inhibits TGF-β-induced myofibroblast differentiation of fibroblasts from multiple organ systems. Ogerin can be used in the studies of fibrotic diseases and neurological disorders.
|
-
- HY-B0520A
-
Benztropine mesylate
Benzatropine mesylate; Benzotropine mesylate; Benztropine methanesulfonate
|
Dopamine Receptor
mAChR
Histamine Receptor
|
Cancer
Neurological Disease
|
Benztropine mesylate (Benzatropine mesylate) is an orally active centrally acting anticholinergic agent that can be used for Parkinson's disease research. Benztropine mesylate is an anti-histamine agent and a dopamine re-uptake inhibitor. Benztropine mesylate is also a human D2 dopamine receptor allosteric antagonist. Benztropine mesylate also has anti-CSCs (cancer stem cells) effects.
|
-
- 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-147720A
-
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.
|
-
- HY-131036
-
MAO-IN-M30 dihydrochloride
|
Monoamine Oxidase
|
Neurological Disease
|
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.
|
-
- HY-113489
-
14,15-Epoxyeicosatrienoic acid
14,15-EET
|
Others
|
Neurological Disease
Cardiovascular Disease
|
14,15-Epoxyeicosatrienoic acid (14,15-EET) is a metabolite of Arachidonic acid (HY-109590). 14,15-Epoxyeicosatrienoic acid is a potent inhibitor of in vivo platelet aggregation. 14,15-Epoxyeicosatrienoic acid facilitates astrocytic Aβ clearance. 14,15-Epoxyeicosatrienoic acid can be used for Alzheimer's Disease research.
|
-
- HY-44809
-
Izilendustat
|
HIF/HIF Prolyl-Hydroxylase
|
Inflammation/Immunology
Cardiovascular Disease
|
Izilendustat is a potent inhibitor of prolyl hydroxylase which can stabilize hypoxia inducible factor- 1 alpha (HIF- lα) and hypoxia inducible factor-2 (HIF-2). Izilendustat has the potential for researching diseases that relate to the body’s inmmune response like colitis and other inflammatory bowel diseases (extracted from patent WO2011057115A1 and WO2011057121A1).
|
-
- HY-137451A
-
-
- HY-143726
-
RIPK1-IN-8
|
RIP kinase
|
Inflammation/Immunology
|
RIPK1-IN-8 (example 16), an aminoimidazopyridine, is a potent and selective RIPK1 inhibitor with an IC50 of 4 nM. RIPK1-IN-8 has the potential for inflammatory diseases research.
|
-
- 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-144031S
-
Tyk2-IN-8
|
JAK
|
Inflammation/Immunology
|
Tyk2-IN-8 is a selective Tyk-2 inhibitor with an IC50 of 5.7 nM for TYK2-JH2. Tyk2-IN-8 inhibits JAK1-JH1 with IC50 of 3.0 nM. Tyk2-IN-8 can be used for the research of autoimmune disease[1].
|
-
- HY-120947
-
AV-105
|
Others
|
Neurological Disease
|
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.
|
-
- HY-N10317
-
-
- HY-16640
-
TCJL37
|
JAK
|
Inflammation/Immunology
|
TCJL37 is a potent, selective, and orally bioavailable TYK2 inhibitor with a Ki of 1.6 nM. TCJL37 can be used for the research of inflammatory bowel diseases (IBD).
|
-
- HY-111262
-
ABT-384
|
11β-HSD
|
Metabolic Disease
Neurological Disease
|
ABT-384 is a potent, selective 11-β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor. ABT-384 exhibits high affinity (Ki 0.1-2.7 nM) against rodent, monkey, and human 11β-HSD1. ABT-384 blocks regeneration of active cortisol. ABT-384 can be used for the research of Alzheimer’s disease (AD).
|
-
- HY-W281862
-
-
- HY-107676
-
SIB-1553A
|
nAChR
|
Neurological Disease
|
SIB-1553A is an orally bioavailable nicotinic acetylcholine receptors (nAChRs) agonist, with selectivity for β4 subunit-containing nAChRs. SIB-1553A is also a selective neuronal nAChR ligand. SIB-1553A is a cognitive enhancer, and has therapeutic potential for the symptomatic treatment of Alzheimer’s disease and other cognitive disorders.
|
-
- HY-B0202A
-
Irbesartan hydrochloride
SR-47436 hydrochloride; BMS-186295 hydrochloride
|
Angiotensin Receptor
Apoptosis
|
Metabolic Disease
Neurological Disease
|
Irbesartan (SR-47436) hydrochloride is an orally active Ang II type 1 (AT1) receptor blocker (ARB). Irbesartan hydrochloride can relax the blood vessels, low blood pressure and increase the supply of blood and oxygen to the heart. Irbesartan hydrochloride can be used for the research of high blood pressure, heart failure, and diabetic kidney disease.
|
-
- HY-115986
-
-
- HY-148096
-
STAT6-IN-1
|
STAT
|
Cancer
Inflammation/Immunology
|
STAT6-IN-1 (compound 19a) is a STAT6 inhibitor with a high affinity for the SH2 domain of STAT6 (IC50=0.028 µM). STAT6-IN-1 can be used in studies of allergic lung disease, allergic rhinitis, chronic obstructive pulmonary disease or cancer.
|
-
- HY-145919
-
-
- HY-124751
-
YTX-465
|
Stearoyl-CoA Desaturase (SCD)
|
Neurological Disease
|
YTX-465 is a stearoyl-CoA desaturase (Ole1/SCD) inhibitor. YTX-465 inhibits Ole1 and SCD1 with IC50s of 0.039 μM and 30.4 μM, respectively. YTX-465 can be used in the research of Parkinson’s disease and other synucleinopathies.
|
-
- HY-139308
-
T0467
|
Mitochondrial Metabolism
|
Neurological Disease
|
T0467 activates parkin mitochondrial translocation in a PINK1-dependent manner in vitro. T0467 do not induce mitochondrial accumulation of PINK1in dopaminergic neurons. T0467 is a potential compound for PINK1-Parkin signaling activation, and can be used for parkinson's disease and related disorders research.
|
-
- HY-147565
-
ATR-IN-13
|
ATM/ATR
|
Cancer
|
ATR-IN-13 (compound A9) is a potent ATR kinase inhibitor, with an IC50 of 2 nM. ATR-IN-13 can be used for ATR kinase mediated diseases research, such as proliferative diseases and cancer.
|
-
- HY-110125
-
ML-193
CID 1261822
|
GPR55
|
Neurological Disease
|
ML-193 (CID 1261822) is a potent and selective antagonist of GPR55, with an IC50 of 221 nM. ML-193 shows more than 27-fold selectivity for GPR55 over GPR35, CB1 and CB2. ML-193 can improve the motor and the sensorimotor deficits of Parkinson’s disease (PD) rats.
|
-
- HY-116815
-
Lalistat 1
|
Bacterial
|
Infection
Neurological Disease
|
Lalistat 1 is a potent, selective, and competitive inhibitor of lysosomal acid lipase (LAL) and against purified human LAL (phLAL) with an IC50 of 68 nM. Lalistat 1 is a inhibitor of immunoglobulin A1 protease (IgA1P) proteases for H. influenzae, has less effects on other serine hydrolases (trypsin or β-lactamase, etc.). Lalistat 1 can be used for the research of niemann-pick type C (NPC) disease.
|
-
- HY-F0004
-
β-Nicotinamide mononucleotide
β-NM; NMN
|
Endogenous Metabolite
|
Cancer
Neurological Disease
|
β-nicotinamide mononucleotide (β-NM) is a product of the nicotinamide phosphoribosyltransferase (NAMPT) reaction and a key NAD + intermediate. The pharmacological activities of β-nicotinamide mononucleotide include its role in cellular biochemical functions, cardioprotection, diabetes, Alzheimer's disease, and complications associated with obesity.
|
-
- HY-145430
-
IL-17A modulator-1
|
Interleukin Related
|
Cancer
Inflammation/Immunology
Neurological Disease
|
IL-17A modulator-1 is a IL-17A modulator, extracted from patent WO2021239743+A1, example 9. IL-17A modulator-1 inhibits the biological action of IL-17A with a pIC50 of 8.2. IL-17A modulator-1 can be used for the research of diseases or disorders associated with modulation of IL-17A activity including diseases with an immune component or autoimmune pathol, cancer and neurodegenerative disorders.
|
-
- HY-105321
-
PBT 1033
PBT 2
|
Bacterial
|
Neurological Disease
|
PBT 1033 (PBT 2) is an orally active copper/zinc ionophore. PBT 1033 restores cognition in mouse models of Alzheimer's disease (AD). PB 1033 also has antibacterial activity against Gram-positive bacteria.
|
-
- HY-149235
-
PI3Kδ-IN-12
|
PI3K
|
Inflammation/Immunology
|
PI3Kδ-IN-12 (compound 13) is a PI3Kδ inhibitor (pIC50 = 5.8), with pKi values of 8.0/6.5/6.4/6.7 for PI3Kδ/γ/β/α, respectively. PI3Kδ-IN-12 can be used in the study of chronic respiratory diseases such as asthma and chronic obstructive pulmonary disease (COPD).
|
-
- 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-152110
-
AChE/MAO-IN-2
|
Cholinesterase (ChE)
Monoamine Oxidase
|
Neurological Disease
|
Dual AChE-MAO B-IN-5, indanone derivative, is a potent dual AChE/MAO-B inhibitior with IC50 values of 0.0224, 0.0412, and 0.1116 μM for AChE, MAO-B and MAO-A, respectively. Dual AChE-MAO B-IN-5 has antioxidant activity and prevents β-amyloid plaque aggregation. Dual AChE-MAO B-IN-5 can be used for Alzheimer’s disease (AD) research.
|
-
- HY-107736
-
AI-3
|
Others
|
Cancer
Inflammation/Immunology
|
AI-3 is a potent ARE (antioxidant response element) activator. AI-3 increases the NQO1 at the transcript levels and protein expression levels. AI-3 has the potential for the research of oxidative stress related diseases.
|
-
- HY-144790
-
AChE-IN-12
|
Amyloid-β
Cholinesterase (ChE)
Monoamine Oxidase
|
Neurological Disease
|
AChE-IN-12 is a potent and blood-brain barrier (BBB) penetrant acetylcholinesterase (AChE) with IC50s of 0.41 μM and 1.88 μM for rat AChE and electric eel AChE. AChE-IN-12 is also a good antioxidant (ORAC = 3.3 eq), selective metal chelator and huMAO-B inhibitor (IC50 = 8.8 µM). AChE-IN-12 has remarkable inhibition of self- and Cu 2+-induced Aβ1-42 aggregation, as well as exhibits a good neuroprotective effect. AChE-IN-12 can be used for researching Alzheimer’s disease.
|
-
- HY-N6625
-
Chlorothalonil
|
Fungal
|
Infection
|
Chlorothalonil is a broad spectrum fungicide and is effective in protecting plants against fungal diseases caused mainly by Phytophthora infestans and Alternaria solani. Chlorothalonil is used for controlling of fungal foliar diseases of vegetables and crops.
|
-
- HY-152227
-
PROTAC TYK2 degradation agent1
|
PROTACs
JAK
|
Inflammation/Immunology
|
PROTAC TYK2 degradation agent1 is a potent and subtype-selective TYK2 degrader. PROTAC TYK2 degradation agent1 has TYK2 degradation activity with DC50 value of 14 nM. PROTAC TYK2 degradation agent1 can be used for the research of autoimmune disease.
|
-
- HY-122605
-
-
- HY-13995A
-
Sevelamer hydrochloride
|
FXR
Autophagy
|
Others
|
Sevelamer hydrochloride is an orally active and phosphate binding agent used for research of hyperphosphatemia with chronic kidney disease. Sevelamer hydrochloride consists of polyallylamine that is crosslinked with epichlorohydrin.
|
-
- HY-145373
-
BMS-986143
|
Btk
|
Inflammation/Immunology
|
BMS-986143 is an orally active, reversible BTK inhibitor with an IC50 of 0.26 nM. BMS-986143 also inhibits TEC, BLK, BMX, TXK FGR, YES1, ITK with IC50s of 3 nM, 5 nM, 7 nM, 10 nM, 15 nM,19 nM, 21 nM, respectively. BMS-986143 can be used for the research of autoimmune diseases.
|
-
- HY-107447
-
N-Deshydroxyethyl Dasatinib
N-Deshydroxyethyl BMS-354825
|
Drug Metabolite
|
Cancer
Inflammation/Immunology
|
N-Deshydroxyethyl Dasatinib (N-Deshydroxyethyl BMS-354825) is a metabolite of Dasatinib, Dasatinib is a multi-kinase inhibitor that potently inhibits Bcr-Abl, Src family and platelet-derived growth factor receptor kinases. N-Deshydroxyethyl Dasatinib can be used in cancer and immune disease research.
|
-
- HY-139973
-
OAB-14
|
Amyloid-β
|
Neurological Disease
|
OAB-14, is a Bexarotene (HY-14171) derivative, improves Alzheimer's disease-related pathologies and cognitive impairments by increasing β-amyloid clearance in APP/PS1 mice. OAB-14 effectively ameliorates the dysfunction of the endosomal-autophagic-lysosomal pathway in APP/PS1 transgenic mice.
|
-
- HY-122080
-
Memoquin
|
Cholinesterase (ChE)
Beta-secretase
Amyloid-β
|
Neurological Disease
|
Memoquin is an anti-amyloid and anti-oxidant multi-target-directed ligand. Memoquin is an orally active inhibitor of BACE-1 and AChE with IC50 values of 108 and 1.55 nM, respectively. Memoquin is a cognitive enhancer that prevents the Aβ-induced neurotoxicity mediated by oxidative stress. Memoquin can be used for the research of Alzheimer’s disease (AD).
|
-
- HY-148867
-
UCM-1306
2-(Fluoromethoxy)-4'-(S-methylsulfonimidoyl)-1,1'-biphenyl
|
Dopamine Receptor
|
Neurological Disease
|
UCM-1306 is a potent and orally active human dopamine D1 receptor allosteric modulator (PAM). UCM-1306 increases the endogenous dopamine (DA) maximal effect both in human and mouse D1 receptors. UCM-1306 is not only for improving motor symptoms but also for addressing the key comorbid cognitive impairment associated with long-term Parkinson’s disease (PD).
|
-
- HY-143261
-
GSK-3β inhibitor 7
|
GSK-3
|
Cancer
Metabolic Disease
Inflammation/Immunology
|
GSK-3β inhibitor 7 is a GSK-3β inhibitor with an IC50 value of 5.25 μM. GSK-3β inhibitor 7 is inserted into the ATP-binding binding pocket of GSK-3β and forms hydrogen-bond. GSK-3β inhibitor 7 shows high hepatocyte glucose uptake (83.5%), and can be used in the research of numerous diseases like diabetes, inflammation, cancer, Alzheimer's disease, and bipolar disorder.
|
-
- HY-32340
-
Lexacalcitol
KH1060
|
VD/VDR
|
Cancer
Inflammation/Immunology
|
Lexacalcitol (KH1060), a vitamin D analog, is a potent regulator of cell growth and immune responses. Lexacalcitol can be used for the research of graft rejection, psoriasis, cancer and auto-immune diseases.
|
-
- HY-139607
-
-
- HY-116016
-
Etilevodopa
L-DOPA ethyl ester; Levodopa ethyl ester
|
Dopamine Receptor
Drug Metabolite
|
Neurological Disease
|
Etilevodopa (L-Dopa ethyl ester), an ethyl-ester proagent of Levodopa, is rapidly hydrolyzed to Levodopa and ethanol by nonspecific esterases in the gastrointestinal tract. Etilevodopa is used for the treatment of Parkinson disease (PD). Levodopa is the direct precursor of dopamine and is a suitable proagent as it facilitates CNS penetration and delivers dopamine.
|
-
- HY-116016A
-
Etilevodopa hydrochloride
L-DOPA ethyl ester hydrochloride; Levodopa ethyl ester hydrochloride
|
Dopamine Receptor
Drug Metabolite
|
Neurological Disease
|
Etilevodopa (L-Dopa ethyl ester) hydrochloride, an ethyl-ester proagent of Levodopa, is rapidly hydrolyzed to Levodopa and ethanol by nonspecific esterases in the gastrointestinal tract. Etilevodopa hydrochloride is used for the treatment of Parkinson disease (PD). Levodopa is the direct precursor of dopamine and is a suitable proagent as it facilitates CNS penetration and delivers dopamine.
|
-
- HY-N2908
-
Atraric acid
Methyl atrarate
|
Androgen Receptor
NO Synthase
p38 MAPK
NF-κB
|
Cancer
Inflammation/Immunology
|
Atraric acid (Methyl atrarate) is a specific androgen receptor (AR) antagonist with anti-inflammatory and anticancer effects. Atraric acid represses the expression of the endogenous prostate specific antigen gene in both LNCaP and C4-2 cells. Atraric acid can also inhibit the synthesis of NO and cytokine, and suppress the MAPK-NFκB signaling pathway. Atraric acid can be used to research prostate diseases and inflammatory diseases.
|
-
- 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-139727
-
S(-)-Bisoprolol
|
Adrenergic Receptor
|
Cardiovascular Disease
|
S(-)-Bisoprolol is a S(-)-enantiomer of Bisoprolol. Bisoprolol is a potent, selective and orally active β1-adrenergic receptor blocker. Bisoprolol has little activity on β2-receptor and has the potential for hypertension, coronary artery disease and stable ventricular dysfunction research.
|
-
- HY-148795
-
-
- HY-151259
-
TK4b
|
JAK
|
Cancer
|
TK4b is a Janus kinase (JAK) inhibitor with the IC50 values of 19.40 nM and 18.42 nM for JAK2 and JAK3, respectively. TK4b can be used in lymphoid-derived diseases and leukemia cancer research.
|
-
- HY-151258
-
TK4g
|
JAK
|
Cancer
|
TK4g is a Janus kinase (JAK) inhibitor with the IC50 values of 12.61 nM and 15.80 nM for JAK2 and JAK3, respectively. TK4g can be used in lymphoid-derived diseases and leukemia cancer research.
|
-
- HY-B2089
-
-
- HY-145150
-
TRPC5-IN-1
|
TRP Channel
|
Metabolic Disease
|
TRPC5-IN-1 (Compound 6j) is a selective TRPC5 inhibitor with 50.5 % Inhibition for TRPC5 at 3 μM. TRPC5-IN-1 can be used for the research of chronic kidney disease (CKD).
|
-
- HY-B1779
-
Sucrose
D-(+)-Saccharose
|
Endogenous Metabolite
|
Metabolic Disease
Cancer
|
Sucrose (D-(+)-Saccharose) is a disaccharide which is composed of two monosaccharides, glucose and fructose. Sucrose can be applied in some animal models, including metabolic disease, obesity, diet on preference, and diabetes, et al.
|
-
- HY-113074
-
-
- HY-12336
-
NIBR189
|
EBI2/GPR183
|
Inflammation/Immunology
|
NIBR189 is an EBI2 (Epstein-Barr virus-induced gene 2) antagonist. NIBR189 inhibits human and mouse EBI2 with IC50s of 11 and 16 nM, respectively. NIBR189 can be used for the research of autoimmune diseases.
|
-
- HY-N3963
-
-
- HY-P99238
-
-
- HY-136561
-
-
- 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-145831
-
-
- HY-150563
-
Neuroinflammatory-IN-2
|
Monoamine Oxidase
Amyloid-β
|
Inflammation/Immunology
Neurological Disease
|
Neuroinflammatory-IN-2 is a potent anti-neuroinflammatory agent with an IC50 value of 10.30 μM for MAO-B, and 96.33% inhibition of Aβ1-42 aggregation at 25 μM. Neuroinflammatory-IN-2 has neuroprotective activity in H2O2-induced PC-12 cell injury. Neuroinflammatory-IN-2 also has biometal chelating abilities, antioxidant activity, anti-neuroinflammatory activity and appropriate BBB permeability. Neuroinflammatory-IN-2 can be used for researching Alzheimer’s disease.
|
-
- HY-130437
-
p-nitro-Pifithrin-α
|
MDM-2/p53
TGF-β Receptor
Caspase
|
Infection
Metabolic Disease
|
p-nitro-Pifithrin-α, a cell-permeable analog of pifithrin-α, is a potent p53 inhibitor. p-nitro-Pifithrin-α suppresses p53-mediated TGF-β1 expression in HK-2 cells. p-nitro-Pifithrin-α inhibits the activation of caspase-3 by Zika virus (ZIKV) strains. p-nitro-Pifithrin-α attenuates steatosis and liver injury in mice fed a high-fat diet [4].
non-alcoholic fatty liver disease.
|
-
- HY-124476
-
Cystamine
|
Caspase
Glutaminase
Apoptosis
|
Cancer
|
Cystamine is the disulfide form of the free thiol, cysteamine. Cystamine is an orally active transglutaminase (Tgase) inhibitor. Cystamine also has inhibition activity for caspase-3 with an IC50 value of 23.6 μM. Cystamine can be used for the research of severals diseases including Huntington's disease (HD) .
|
-
- HY-132303
-
MK-8262
|
CETP
|
Metabolic Disease
Cardiovascular Disease
|
MK-8262 is an orally active and potent cholesteryl ester transfer protein (CETP) inhibitor with an IC50 of 53 nM and a log D of 5.3. MK-8262, a bistrifluoromethyl analogue, has the potential for coronary heart disease (CHD) correlated high-density lipoprotein (HDL) and low-density lipoprotein (LDL) research.
|
-
- HY-146727
-
JAK3-IN-11
|
JAK
|
Inflammation/Immunology
|
JAK3-IN-11 (Compound 12), a potent, noncytotoxic, irreversible, orally active JAK3 inhibitor with IC50 value of 1.7 nM, has excellent selectivity (>588-fold compared to other JAK isoforms), covalently bind to the ATP-binding pocket in JAK3. JAK3-IN-11 strongly inhibits JAK3-dependent signaling and T cell proliferation, is a promising tool for study autoimmune diseases.
|
-
- HY-125016
-
TT-10
TAZ-K
|
YAP
|
Cardiovascular Disease
|
TT-10 (TAZ-K) is an activator of YES-associated protein (YAP)-transcriptional enhancer factor domain (TEAD) activity. TT-10 can be used for the research of heart diseases accompanied by cardiomyocyte loss.
|
-
- HY-12820
-
Sibofimloc
Antibiotic-202
|
Bacterial
Antibiotic
|
Infection
|
Sibofimloc (Antibiotic-202) is a first-in-class, gut-restricted, orally active FimH adhesion inhibitor extracted from patent WO2014100158A1, Compound Example 202. Sibofimloc has anti-bacterial infective activity. Sibofimloc is developed for inflammatory bowel disease (IBD).
|
-
- HY-139727A
-
S(-)-Bisoprolol fumarate
|
Adrenergic Receptor
|
Cardiovascular Disease
|
S(-)-Bisoprolol fumarate is a S(-)-enantiomer of Bisoprolol fumarate. Bisoprolol fumarate is a potent, selective and orally active β1-adrenergic receptor blocker. Bisoprolol has little activity on β2-receptor and has the potential for hypertension, coronary artery disease and stable ventricular dysfunction research.
|
-
- 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-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-145832
-
-
- HY-147859
-
BChE-IN-8
|
Amyloid-β
|
Neurological Disease
|
BChE-IN-8 (compound 20) is an orally active, potent and BBB-penetrated BChE (butyrylcholinesterase) inhibitor, with IC50 values of 0.15 nM (eqBChE, equine serum BChE) and 45.2 nM (hBChE), respectively. High stability of BChE-IN-8 contributes to significantly improved blood concentration and tissue exposure. BChE-IN-8 can exert neuro-protecting and cognition improving properties through multiple modulations, including cholinergic system, Aβ aggregation, neuropeptide levels. BChE-IN-8 can be used for Alzheimer's disease (AD) research.
|
-
- HY-B0731A
-
Perospirone
SM-9018 free base
|
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
Perospirone (SM-9018 free base) is an orally active antagonist of 5-HT2A receptor (Ki=0.6 nM) and dopamine D2 receptor (Ki=1.4 nM), and also a partial agonist of 5-HT1A receptor (Ki=2.9 nM). Perospirone is an atypical antipsychotic agent and has the potential for schizophrenic disease research.
|
-
- HY-130452
-
NOS1-IN-1
|
NO Synthase
|
Neurological Disease
|
NOS1-IN-1 is a selective and cell-permeable nNOS inhibitor with a Ki of 120 nM. NOS1-IN-1 exhibits 2617-fold and 325-fold selectivity over eNOS (Ki=39 μM) and iNOS (Ki=325 μM) , respectively. NOS1-IN-1 can be used for the research of neurological disease, including cerebral palsy (CP).
|
-
- HY-115497
-
BRD5529
|
E1/E2/E3 Enzyme
|
Infection
Inflammation/Immunology
|
BRD5529 is an effective dose-dependent CARD9-TRIM62 protein–protein interaction (PPI) inhibitor with an IC50 value of 8.6 μM. BRD5529 has potency and complete inhibition of CARD9 ubiquitinylation in vitro, also has favorable solubility. BRD5529 can be used for the research of inflammatory bowel disease (IBD) such as Crohn’s disease (CD) and ulcerative colitis (UC).
|
-
- HY-15178
-
Oglemilast
GRC 3886
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
Oglemilast (GRC 3886) is a potent and orally active phosphodiesterase-4 (PDE4) inhibitor with an IC50 of 0.5 nM for PDE4D3. Oglemilast inhibits pulmonary cell infiltration, including eosinophilia and neutrophilia in vitro and in vivo. Oglemilast has the potential for inflammatory airway diseases.
|
-
- HY-N7698B
-
Hexa-N-acetylchitohexaose
|
Others
|
Cancer
Inflammation/Immunology
|
Hexa-N-acetylchitohexaose is an inducer of disease resistance in crop plants, which could elicit an increase of lignification-related and antioxidative enzymes in soybean plants. Hexa-N-acetylchitohexaose is a substrate of lysozyme. Hexa-N-acetylchitohexaose shows antitumor effect.
|
-
- HY-A0027
-
-
- HY-A0027A
-
Fenspiride
|
Histamine Receptor
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
Fenspiride, an orally active non-steroidal antiinflammatory agent, is an antagonist of H1-histamine receptor. Fenspiride inhibites phosphodiesterase 3 (PDE3), phosphodiesterase 4 (PDE4) and phosphodiesterase 5 (PDE5) activities with -log IC50 values of 3.44, 4.16 and approximately 3.8, respectively. Fenspiride can be used for the research of respiratory diseases.
|
-
- HY-117006
-
E1231
1-{4-[2-(5-Methylfuran-2-yl)quinoline-4-carbonyl]piperazin-1-yl}ethan-1-one
|
Sirtuin
|
Cardiovascular Disease
|
E1231 is an orally active activator of Sirtuin 1 (SIRT1) (EC50=0.83 μM), to modulate cholesterol and lipid metabolism. E1231 interactes with SIRT1 (KD=9.61 μM) and deacetylated liver X receptor-alpha (LXRα), and increases ATP-binding cassette transporter A1 (ABCA1) expression. E1231 also reduces atherosclerotic plaque development in ApoE -/- mice model. E1231 can be used for research in cholesterol and lipid disorder-related diseases.
|
-
- HY-B1806A
-
Tridihexethyl chloride
Pathilon chloride
|
mAChR
|
Inflammation/Immunology
Neurological Disease
|
Tridihexethyl (Pathilon) chloride is an orally active anticholinergic agent and mAChR antagonist, shows activities of antimuscarinic and anticholinergic. Tridihexethyl chloride shows pronounced antispasmodic and antisecretory effects on the gastrointestinal tract. Tridihexethyl chloride can be used in studies of peptic ulcer disease and acquired nystagmus .
|
-
- HY-139561
-
-
- HY-146195
-
-
- HY-136490
-
Psychosine
Galactosylsphingosine
|
PKC
|
Cancer
Neurological Disease
|
Psychosine (Galactosylsphingosine), a substrate of the galactocerebrosidase (GALC) enzyme, is a potential biomarker for Krabbe disease. Psychosine is a highly cytotoxic lipid, capable of inducing cell death in a wide variety of cell types including, most relevantly to globoid cell leukodystrophy (GLD), oligodendrocytes. Psychosine causes cell death at least in part via apoptosis. Psychosine also is an inhibitor of PKC.
|
-
- HY-N4005
-
Isoastilbin
|
Bacterial
Tyrosinase
|
Infection
Neurological Disease
|
Isoastilbin is a dihydroflavonol glycoside compound in Rhizoma Smilacis glabrae and Astragalus membranaceus. Isoastilbin inhibits glucosyltransferase (GTase) with an IC50 value of 54.3 μg/mL, and also inhibits tyrosinase activity. Isoastilbin shows neuroprotective, antioxidation, antimicrobial and anti-apoptotic properties and has the potential for Alzheimer’s disease research.
|
-
- HY-127150
-
Clofezone
Perclusone
|
Others
|
Inflammation/Immunology
|
Clofezone (Perclusone) is a antirheumatic agent. Clofezone can be used in the study of various rheumatic diseases, especially arthritis (RA) and ankylosing spondylitis (AS).
|
-
- HY-142673
-
ATR-IN-7
|
ATM/ATR
|
Cancer
|
ATR-IN-7 is a potent inhibitor of ATR. ATR is a class of protein kinases involved in genome stability and DNA damage repair, and is a member of the PIKK family. ATR-IN-7 has the potential for the research of ATR kinase-mediated diseases such as proliferative diseases and cancer (extracted from patent WO2021238999A1, compound 1).
|
-
- HY-146731
-
PPARγ agonist 1
|
PPAR
|
Metabolic Disease
Cardiovascular Disease
|
PPARγ agonist 1 (compound 15) is a potent agonist of PPARγ. PPARγ agonist 1 shows high efficacy to activate hPPARγ without raising a full agonism and probably avoiding adverse effects. PPARγ agonist 1 has the potential for the research of cardiovascular diseases associated with metabolic disorders.
|
-
- HY-149211
-
AChE/BChE-IN-12
|
Cholinesterase (ChE)
Beta-secretase
Amyloid-β
|
Neurological Disease
|
AChE/BChE-IN-12 (compound 10b), a 3,5-dimethoxy analogue, is a potent AChE, BChE, and β-secretase-1 (BACE-1) inhibitor, with IC50 values of 2.57, 3.26, and 10.65 μM, respectively. AChE/BChE-IN-12 crosses the blood-brain barrier via passive diffusion and inhibits the self-aggregation of amyloid-β monomers. AChE/BChE-IN-12 can be used for Alzheimer’s disease (AD) research.
|
-
- HY-W008947
-
SEW2871
|
LPL Receptor
ERK
Akt
|
Metabolic Disease
Inflammation/Immunology
Neurological Disease
|
SEW2871 is an orally active, potent, highly selective S1P1 (sphingosine-1-phosphate type 1 receptor) agonist, with an EC50 of 13.8 nM. SEW2871 activates ERK, Akt, and Rac signaling pathways and induces S1P1 internalization and recycling. SEW2871 reduces lymphocyte numbers in blood. SEW2871 can be used for the research of diabetes, Alzheimer’s disease, liver fibrosis, and inflammatory responses.
|
-
- HY-113089
-
Epsilon-(gamma-glutamyl)-lysine
H-Glu(H-Lys-OH)-OH; γ-Glu-ε-Lys
|
Endogenous Metabolite
|
Metabolic Disease
|
Epsilon-(gamma-glutamyl)-lysine is an N(6)-acyl-L-lysine derivative. The enzyme tissue transglutaminase (tTg) helps the formation of epsilon-(gamma-glutamyl)lysine bonds between ECM components in some disease, such as non-diabetic kidney, glaucoma filtration.
|
-
- HY-116044
-
BCATc Inhibitor 2
|
Others
|
Neurological Disease
|
BCATc Inhibitor 2 is a selective branched-chain aminotransferase (BCAT) inhibitor for research of neurodegenerative diseases. The IC50s of 0.2 μM, 0.8 μM and 3.0 μM for rat cytosolic isoenzyme rBCATc, human cytosolic isoenzyme hBCATc and rat mitochondrial isoenzyme rBCATm, respectively. BCATc, also called BCAT1, is in the cytoplasm.
|
-
- HY-D0961
-
Gallocyanine chloride
|
Wnt
|
Neurological Disease
|
Gallocyanine chloride, a synthetic blue dyestuff, blocks DKK1 inhibitory activity by disrupting DKK1/LRP6 interaction. Its association with LRP6 is weak (IC50 of about 3 μM in the inhibition of DKK1 binding). Gallocyanine dye acts as a potential agent for the research of Alzheimer's disease and related neurodegenerative tauopathies.
|
-
- HY-P3781
-
(Met(O)35)-Amyloid β-Protein (1-42)
|
Amyloid-β
|
Neurological Disease
|
(Met(O)35)-Amyloid β-Protein (1-42) is the oxidation form of Met35 in Aβ42. (Met(O)35)-Amyloid β-Protein (1-42) can yield an oligomer size distribution characteristic of Aβ40. (Met(O)35)-Amyloid β-Protein (1-42) can be used in the research of Alzheimer’s disease (AD).
|
-
- HY-117089
-
Tetraconazole
|
Fungal
|
Infection
|
Tetraconazole, a chiral triazole fungicide, is widely used for the prevention of plant disease in wheat fields. Tetraconazole alters the methionine and ergosterol biosynthesis pathways in Saccharomyces yeasts promoting changes on volatile derived compounds.
|
-
- HY-139414
-
-
- HY-W171071
-
-
- HY-103130
-
EMD386088
|
5-HT Receptor
|
Neurological Disease
|
EMD386088 is a potent serotonin 6 receptor (5-HT6R) agonist. EMD386088 induces cell death. EMD386088 regulates the activity of ERK1/2. EMD386088 has the potential for the research of alzheimer's disease (AD) and schizophrenia.
|
-
- HY-11109
-
-
- HY-15770
-
TR-14035
|
Integrin
|
Inflammation/Immunology
|
TR-14035 is a orally active dual α4β7/α4β1 integrin antagonist, with IC50 s of 7 nM and 87 nM for α4β7 and α4β1, respectively. TR-14035 can be used for the research of inflammation and autoimmune diseases.
|
-
- HY-128382
-
Brilliant Black BN
E 151
|
Enterovirus
|
Infection
|
Brilliant black BN (E151) is an azo dye and a food colorant. Brilliant black BN is a promising antiviral agent against EV71 infection via inhibiting the interaction between EV71 and its cellular uncoating factor cyclophilin A. Brilliant black BN has the potential for the investigation of contagious disease. Storage: protect from light.
|
-
- HY-N0450
-
Sinapine thiocyanate
|
P-glycoprotein
Cholinesterase (ChE)
|
Cancer
|
Sinapine thiocyanate is an alkaloid isolated from seeds of the cruciferous species. Sinapine thiocyanate exhibits anti-inflammatory, anti-oxidant, anti-tumor, anti-angiogenic and radio-protective effects. Sinapine thiocyanate is also an acetylcholinesterase (AChE) inhibitor and can be used for the research of Alzheimer’s disease, ataxia, myasthenia gravis, and Parkinson’s disease.
|
-
- HY-147681
-
SUN13837
|
FGFR
|
Neurological Disease
|
SUN13837 is an orally active, potent and BBB-penetrated FGFR (fibroblast growth factor receptor) modulator. SUN13837 shows neuroprotective activity. SUN13837 can be used for neurodegenerative diseases research.
|
-
- HY-P1047
-
β-Sheet Breaker Peptide iAβ5
[Pro18, Asp21] β-Amyloid (17-21)
|
Amyloid-β
|
Neurological Disease
|
β-Sheet Breaker Peptide iAβ5 is a potent degrader of cerebral amyloid-beta (Abeta). Abeta deposition is associatied with the Alzheimer disease (AD), due to its related toxicity linked to its beta-sheet conformation and/or aggregation. β-Sheet Breaker Peptide iAβ5 reproducibly induces in vivo disassembly of fibrillar amyloid deposits. Thus, β-Sheet Breaker Peptide iAβ5 prevents and/or reverses neuronal shrinkage caused by Abeta, and reduces the extent of interleukin-1beta positive microglia-like cells that surround the Abeta deposits. β-Sheet Breaker Peptide iAβ5 reduces the size and/or number of cerebral amyloid plaques in AD. β-Sheet Breaker Peptide iAβ5 labeled by hydrophobic benzyl alcohol (HBA) tag, can be used for quantitative assay by showing vivid blue color under acidic conditions.
|
-
- HY-145361
-
-
- HY-112294
-
-
- HY-108287
-
Trithiozine
|
Others
|
Endocrinology
|
Trithiozine is an orally active antisecretory and antiulcer agent. Trithiozine can be used for the research of peptic ulcer disease and hypersecretory disorders.
|
-
- HY-B1332
-
Ipratropium bromide hydrate
Sch 1000 bromide hydrate
|
mAChR
|
Inflammation/Immunology
Neurological Disease
|
Ipratropium bromide (Sch 1000) hydrate is a muscarinic receptor antagonist, with IC50s of 2.9 nM, 2 nM, and 1.7 nM for M1, M2, and M3 receptors, respectively. Ipratropium bromide hydrate relaxes smooth muscle, can be used in the research for COPD (chronic obstructive pulmonary disease) and asthma.
|
-
- HY-B0241
-
Ipratropium bromide
Sch 1000
|
mAChR
|
Inflammation/Immunology
Neurological Disease
|
Ipratropium bromide (Sch 1000) is a muscarinic receptor antagonist, with IC50s of 2.9 nM, 2 nM, and 1.7 nM for M1, M2, and M3 receptors, respectively. Ipratropium bromide relaxes smooth muscle, can be used in the research for COPD (chronic obstructive pulmonary disease) and asthma.
|
-
- HY-B1042
-
Oxolamine citrate
SKF-9976 citrate; AF-438 citrate
|
Others
|
Inflammation/Immunology
|
Oxolamine citrate (SKF-9976 citrate) is a cough suppressant that can be used for the research of respiratory tract diseases. Oxolamine citrate also exhibits anti-inflammatory effect.
|
-
- HY-110155
-
LM11A-31 dihydrochloride
|
Neurotensin Receptor
|
Neurological Disease
|
LM11A-31 dihydrochloride, a non-peptide p75 NTR (neurotrophin receptor p75) modulator, is an orally active and potent proNGF (nerve growth factor) antagonist. LM11A-31 dihydrochloride is an amino acid derivative with high blood-brain barrier permeability and blocks p75-mediated cell death. M11A-31 dihydrochloride reverses cholinergic neurite dystrophy in Alzheimer's disease mouse models with mid- to late-stage disease progression.
|
-
- HY-142672
-
ATR-IN-6
|
ATM/ATR
|
Cancer
|
ATR-IN-6 is a potent inhibitor of ATR. ATR is a class of protein kinases involved in genome stability and DNA damage repair, and is a member of the PIKK family. ATR-IN-6 has the potential for the research of ATR kinase-mediated diseases such as proliferative diseases and cancer (extracted from patent WO2021233376A1, compound A22).
|
-
- HY-142671
-
ATR-IN-5
|
ATM/ATR
|
Cancer
|
ATR-IN-5 is a potent inhibitor of ATR. ATR is a class of protein kinases involved in genome stability and DNA damage repair, and is a member of the PIKK family. ATR-IN-5 has the potential for the research of ATR kinase-mediated diseases such as proliferative diseases and cancer (extracted from patent CN112047938A, compound D24).
|
-
- HY-151489
-
CypE-IN-1
|
Sirtuin
|
Cancer
Metabolic Disease
Neurological Disease
|
CypD-IN-1 is a potent and subtype-selective cyclophilin E (CypE) inhibitor. CypD-IN-1 has CypE affinity with IC50 and Ki values of 0.013 μM and 0.072 μM, respectively. CypD-IN-1 can be used for the research of several diseases including oxidative stress, neurodegenerative disorders, liver diseases, aging, autophagy and diabetes.
|
-
- HY-B0731
-
Perospirone hydrochloride
SM-9018
|
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
Perospirone hydrochloride (SM-9018) is an orally active antagonist of 5-HT2A receptor (Ki of 0.6 nM) and dopamine D2 receptor (Ki of 1.4 nM). Perospirone hydrochloride is also a partial agonist of 5-HT1A receptor (Ki of 2.9 nM). Perospirone hydrochloride is an atypical antipsychotic agent and has the potential for schizophrenic disease research.
|
-
- HY-149065
-
D-685
|
α-synuclein
|
Neurological Disease
|
D-685, a prodrug of D-520, exhibits higher in vivo anti-Parkinsonian efficacy in a reserpinized Parkinson's disease (PD) animal model than the parent D-520. D-685 reduces accumulation of human α-synuclein (α-syn) protein. D-685 exhibits facile brain penetration.
|
-
- HY-122487
-
Troriluzole
BHV-4157
|
Others
|
Neurological Disease
|
Troriluzole, a third-generation, tripeptide proagent of Riluzole (HY-B0211), is an orally active glutamate modulator. Troriluzole reduces synaptic glutamate level and increases the synaptic glutamate absorption. Troriluzole has the potential for Alzheimer disease and generalized anxiety disorder (GAD).
|
-
- HY-B0202
-
Irbesartan
SR-47436; BMS-186295
|
Angiotensin Receptor
Apoptosis
|
Cardiovascular Disease
Endocrinology
|
Irbesartan (SR-47436) is an orally active Ang II type 1 (AT1) receptor blocker (ARB). Irbesartan can relax the blood vessels, low blood pressure and increase the supply of blood and oxygen to the heart. Irbesartan can be used for the research of high blood pressure, heart failure, and diabetic kidney disease.
|
-
- HY-125111
-
-
- HY-148335
-
-
- HY-B0843
-
Metalaxyl
|
Fungal
|
Infection
|
Metalaxyl is a fungicide agent that inhibits the protein synthesis in fungi. Metalaxyl against downy mildews and soil-borne diseases by Phytium ssp. and Phytophthora ssp..
|
-
- HY-18956
-
(E/Z)-Icerguastat
(E/Z)-Sephin1; (E/Z)-IFB-088
|
Phosphatase
|
Inflammation/Immunology
|
(E/Z)-Icerguastat ((E/Z)-Sephin1) is a selective inhibitor of the phosphatase regulatory subunit PPP1R15A (R15A). (E/Z)-Icerguastat can be used for protein misfolding diseases research.
|
-
- HY-B1858
-
Isoprothiolane
|
Fungal
|
Infection
|
Isoprothiolane is a systemic fungicide. Isoprothiolane is a rice blast controlling agent against the fungal disease of rice planty Pyvioutavia oryzae Cav.
|
-
- HY-148353
-
PF-06455943
|
LRRK2
|
Neurological Disease
|
PF-06455943 is a leucine rich repeat kinase 2 (LRRK2) inhibitor with IC50 value of 3 nM. PF-06455943 also is a PET radioligand. PF-06455943 can be used for the research of ADME/neuro PK characterization and Parkinson disease (PD).
|
-
- HY-152037
-
AChE/Nrf2 modulator 1
|
Cholinesterase (ChE)
Keap1-Nrf2
|
Neurological Disease
|
AChE/Nrf2 modulator 1 is an orally active acetylcholinesterase (AChE)/nuclear factor erythroid 2-related factor 2 (Nrf2) modulator. AChE/Nrf2 modulator 1 has Nrf2 inductive activity and AChE inhibitory activity for eeAChE and hAChE with IC50 values of 0.07 μM and 0.38 μM, respectively. AChE/Nrf2 modulator 1 can be used for the research of Alzheimer's disease.
|
-
- HY-146691
-
hMAO-B-IN-2
|
Monoamine Oxidase
|
Neurological Disease
|
hMAO-B-IN-2 (compound 6j) is an orally active, potent, selective and BBB penetrated and competitive reversible hMAO-B inhibitor, with an IC50 of 4 nM. hMAO-B-IN-2 shows low toxicity and good neuroprotective effects in SH-SY5Y cell. hMAO-B-IN-2 can be used for alzheimer’s disease research.
|
-
- HY-103164
-
-
- 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-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-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-147939
-
AChE/BuChE-IN-3
|
Cholinesterase (ChE)
Amyloid-β
|
Cancer
|
AChE/BuChE-IN-3 is a potent and blood-brain barrier (BBB) penetrant AChE and BuChE dual inhibitor with IC50s of 0.65 μM and 5.77 μM for AChE and BuChE. AChE/BuChE-IN-3 also inhibits Aβ1-42 aggregation. AChE/BuChE-IN-3 has effectively neuroprotective activities and nearly no toxicity on SH-SY5Y cells. AChE/BuChE-IN-3 can be used for researching Alzheimer's disease.
|
-
- HY-W040022
-
Cefcapene pivoxil hydrochloride hydrate
|
Bacterial
Antibiotic
|
Infection
|
Cefcapene pivoxil hydrochloride hydrate is a proagent and an orally active 3rd-generation cephalosporin with broad-spectrum of?anti-bacterial?activity. Cefcapene pivoxil hydrochloride hydrate is used for the study of palmoplantar pustulosis (PPP) and other?infectious diseases.
|
-
- HY-146356
-
-
- 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-145801
-
XT2
|
Others
|
Inflammation/Immunology
|
XT2 is a potent, orally active, and selective inhibitor of NF-κB-inducing kinase (NIK) with an IC50 of 9.1 nM. XT2 suppresses CCl4-induced upregulation of ALT, a key biomarker of acute liver injury. XT2 also decreases immune cell infiltration into the injured liver tissue. XT2 has the potential for the research of liver inflammatory diseases.
|
-
- HY-14759
-
Aleplasinin
PAZ-417
|
PAI-1
Amyloid-β
|
Neurological Disease
|
Aleplasinin is an orally active, potent, BBB-penetrated and selectiveSERPINE1 (PAI-1, Plasminogen activator inhibitor-1) inhibitor. Aleplasinin increases amyloid-β (Aβ) catabolism and ameliorates amyloid-related pathology. Aleplasinin improves memory deficiency. Aleplasinin can be used for Alzheimer's disease research.
|
-
- HY-151386
-
BChE-IN-13
|
Cholinesterase (ChE)
|
Neurological Disease
|
BChE-IN-13 (Compound 17c) is an orally active, potent and selective Butyrylcholinesterase (BChE) inhibitor with IC50s of 0.22 and 0.016 μM for eqBChE and hBChE, respectively. BChE-IN-13 can improve memory and cognitive impairments, and be used in Alzheimer’s disease (AD) research.
|
-
- HY-144429
-
TRPC5-IN-4
|
TRP Channel
|
Metabolic Disease
|
TRPC5-IN-4 is potent and safe TRPC inhibitor with IC50 value of 14.07 nM and 65 nM for TRPC5 and TRPC4, respectively. TRPC5-IN-4 shows no damage on the cellular component of liver and kidney. TRPC5-IN-4 can be used for the research of chronic kidney disease (CKD).
|
-
- HY-19285A
-
Sulfaclozine sodium
Sulfachloropyrazine sodium
|
Bacterial
Parasite
Antibiotic
|
Infection
|
Sulfaclozine sodium (Sulfachloropyrazine sodium) is an efficacious sulphonamide derivative with antibacterial and anticoccidial effects. Sulfaclozine sodium is commonly used for the treatment of various poultry diseases (particularly, collibacteriosis, fowl cholera and coccidiosis).
|
-
- HY-19285
-
Sulfaclozine
Sulfachloropyrazine
|
Bacterial
Parasite
Antibiotic
|
Infection
|
Sulfaclozine (Sulfachloropyrazine) is an efficacious sulphonamide derivative with antibacterial and anticoccidial effects. Sulfaclozine is commonly used for the treatment of various poultry diseases (particularly, collibacteriosis, fowl cholera and coccidiosis).
|
-
- HY-150076
-
BLU2864
|
Others
|
Cancer
Metabolic Disease
|
BLU2864 is an orally active, highly selective, ATP-competitive PRKACA inhibitor (IC50=0.3 nM). BLU2864 shows anti-tumor activity. BLU2864 can be used in cancer and polycystic kidney disease research.
|
-
- HY-136535
-
Anizatrectinib
hTrkA-IN-1
|
Trk Receptor
|
Inflammation/Immunology
|
Anizatrectinib (hTrkA-IN-1) is a potent and orally active inhibitor of TrkA kinase with an IC50 of 1.3 nM, compound 2 extracted from patent WO2015175788. Anizatrectinib can be used for the study of inflammatory disease, such as prostatitis, pelvic, et al.
|
-
- HY-126415
-
-
- HY-142936
-
RORγt modulator 3
|
ROR
|
Inflammation/Immunology
Cancer
Neurological Disease
|
RORγt modulator 3 (Compound 23) is a modulator of retinoid-related orphan receptor γt (RORγt). RORγt modulator 3 can be used for the research of RORyt mediated diseases such as, e.g., pain, inflammation, COPD, asthma, rheumatoid arthritis, colitis, multiple sclerosis, psoriasis, neurodegenerative diseases and cancer.
|
-
- HY-149279
-
JNK3 inhibitor-7
|
JNK
|
Neurological Disease
|
JNK3 inhibitor-7 is a potent, orally active and cross the blood-brain barrier JNK3 inhibitor with IC50 values of 53, 973, 1039 nM for JNK3, JNK2, JNK1, respectively. JNK3 inhibitor-7 shows significant neuroprotective effects. JNK3 inhibitor-7 has the potential for the research of Alzheimer’s disease (AD).
|
-
- HY-136780
-
SEN177
|
Amyloid-β
|
Neurological Disease
|
SEN177 is a potent glutaminyl cyclase (QPCT) inhibitor with an IC50 of 0.013μM for glutaminyl-peptide cyclotransferase-like (QPCTL). SEN177 has a Ki of 20 nM for human glutaminyl cyclase (hQC). SEN177 greatly reduces the early stages of mutant HTT oligomerisation and reduces the percentage of neurons with Q80 aggregates. SEN177 has the potential for Huntington’s disease research.
|
-
- HY-149280
-
JNK3 inhibitor-8
|
JNK
|
Neurological Disease
|
JNK3 inhibitor-8 is a potent, delective, orally active and cross the blood-brain barrier JNK3 inhibitor with IC50 values of 21, 2203, >10000 nM for JNK3, JNK2, JNK1, respectively. JNK3 inhibitor-8 shows significant neuroprotective effects. JNK3 inhibitor-8 has the potential for the research of Alzheimer’s disease (AD).
|
-
- HY-151878
-
CDK7-IN-20
|
CDK
GSK-3
|
Metabolic Disease
|
CDK7-IN-20 is a potent, selective and irreversible CDK7 (CDK) inhibitor with an IC50 value of 4 nM. CDK7-IN-20 displays >206-fold selectivity for CDK7 over CDK1, CDK2, CDK3, CDK5, CDK6, CDK9 and CDK12 . CDK7-IN-20 has the potential for autosomal dominant polycystic kidney disease (ADPKD) research.
|
-
- HY-B0558
-
Carbimazole
|
Others
|
Endocrinology
|
Carbimazole is an imidazole antithyroid agent and can be used for the research of Graves' disease. Carbimazole plays its role due to its rapid conversion to methylmercapto imidazole (MMI) in vivo and can be converted to methimazole in vitro.
|
-
- HY-125990
-
SLC13A5-IN-1
|
Sodium Channel
|
Metabolic Disease
Cardiovascular Disease
|
SLC13A5-IN-1 is a selective sodium-citrate co-transporter (SLC13A5) inhibitor. SLC13A5-IN-1 completely blocks the uptake of 14C-citrate with an IC50 value of 0.022 μM in HepG2 cells. SLC13A5-IN-1 has the potential for the treatment of metabolic and/or cardiovascular diseases. SLC13A5-IN-1 is extracted from patent WO2018104220A1, Compound I-5.
|
-
- 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-120632
-
BMS-433771
|
RSV
|
Infection
|
BMS-433771 is a potent orally active inhibitor of respiratory syncytial virus (RSV). BMS-433771 is active against both A and B groups of RSV, with an average EC50 of 20 nM. BMS-433771 can be used for the research of respiratory tract disease.
|
-
- HY-120632A
-
BMS-433771 dihydrochloride hydrate
|
RSV
|
Infection
|
BMS-433771 dihydrochloride hydrate is a potent orally active inhibitor of respiratory syncytial virus (RSV). BMS-433771 dihydrochloride hydrate is active against both A and B groups of RSV, with an average EC50 of 20 nM. BMS-433771 dihydrochloride hydrate can be used for the research of respiratory tract disease.
|
-
- HY-113089A
-
Epsilon-(gamma-glutamyl)-lysine TFA
H-Glu(H-Lys-OH)-OH TFA; γ-Glu-ε-Lys TFA
|
Endogenous Metabolite
|
Metabolic Disease
|
Epsilon-(gamma-glutamyl)-lysine (H-Glu(H-Lys-OH)-OH) TFA is an N(6)-acyl-L-lysine derivative. The enzyme tissue transglutaminase (tTg) helps the formation of epsilon-(gamma-glutamyl)lysine bonds between ECM components in some disease, such as non-diabetic kidney, glaucoma filtration.
|
-
- HY-15283
-
Clopidogrel
|
P2Y Receptor
|
Cardiovascular Disease
|
Clopidogrel is an orally active platelet inhibitor that targets P2Y12 receptor. Clopidogrel is used to inhibit blood clots in coronary artery disease, peripheral vascular disease, and cerebrovascular disease.
|
-
- HY-18300A
-
Filgotinib maleate
GLPG0634 maleate
|
JAK
|
Inflammation/Immunology
|
Filgotinib (maleate) is a selective and orally active JAK1 inhibitor with IC50 of 10 nM, 28 nM, 810 nM and 116 nM for JAK1, JAK2, JAK3 and TYK2, respectively. Filgotinib (maleate) can be used for rheumatoid arthritis (RA) and Crohn's disease research.
|
-
- HY-142935
-
RORγt modulator 2
|
ROR
|
Inflammation/Immunology
Cancer
Neurological Disease
|
RORγt modulator 2 (Compound 21) is a modulator of retinoid-related orphan receptor γt (RORγt) with the IC50 of <50 nM. RORγt modulator 2 can be used for the research of RORyt mediated diseases such as, e.g., pain, inflammation, COPD, asthma, rheumatoid arthritis, colitis, multiple sclerosis, psoriasis, neurodegenerative diseases and cancer.
|
-
- HY-18054
-
BVT 2733
|
11β-HSD
|
Inflammation/Immunology
|
BVT 2733 is a potent, selective, and orally active non-steroidal 11β-hydroxydehydrogenase 1 (11β-HSD1) inhibitor. BVT 2733 is potently against the mouse enzyme (IC50=96 nM) over the human enzyme (IC50=3341 nM). BVT 2733 has the potential for the study of arthritis and obesity related disease.
|
-
- HY-P3528
-
GPR
|
Caspase
Apoptosis
|
Neurological Disease
|
GPR is a three amino acid peptide. GPR can rescue cultured rat hippocampal neurons from Aβ-induced neuronal death by inhibiting caspase-3/p53 dependent apoptosis. GPR can be used for the research of Alzheimer's disease (AD).
|
-
- HY-147683
-
FGFR-IN-3
|
FGFR
|
Neurological Disease
|
FGFR-IN-3 (compound 6) is an orally active, potent and BBB-penetrated FGFR (fibroblast growth factor receptor) modulator. FGFR-IN-3 shows neuroprotective activity. FGFR-IN-3 can be used for neurodegenerative diseases research.
|
-
- 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-50861
-
AZD3988
|
Acyltransferase
|
Metabolic Disease
|
AZD3988 is an orally active diacylglycerol acyl transferase-1 (DGAT-1) inhibitor. AZD3988 has excellent DGAT-1 (human) potency with an IC50 value of 0. 6 nM. AZD3988 can be used for the research of metabolic diseases such as diabetes, obesity.
|
-
- HY-108346
-
JX401
|
p38 MAPK
|
Inflammation/Immunology
|
JX401 is a potent inhibitor of p38alpha, containing a 4-benzylpiperidine motif. p38alpha is hyperactive in inflammatory diseases, and various indications suggest that its inhibition would reverse inflammation. JX401 has the potential for the research of inflammation.
|
-
- HY-107355
-
Letosteine
|
Others
|
Inflammation/Immunology
|
Letosteine is an orally active, potent and safe expectorant. Letosteine dissolves bronchial mucus and reduces respiratory inflammation symptoms, and restores gas exchanges and natural defense mechanisms in the lung. Letosteine can be used for acute or chronic respiratory diseases (such as bronchopneumopathies) research[1][2][3].
|
-
- HY-144882
-
-
- HY-153077
-
-
- HY-141645
-
IMM-H007
WS070117
|
AMPK
TGF-β Receptor
NF-κB
JNK
AP-1
|
Metabolic Disease
Inflammation/Immunology
Cardiovascular Disease
|
IMM-H007 (WS070117) is an orally active and potent AMPK (AMP-activated protein kinase) activator and TGFβ1 (transforming growth factor β1) antagonist. IMM-H007 has protective effects in cardiovascular diseases via activation of AMPK. IMM-H007 negatively regulates endothelium inflammation through inactivating NF-κB and JNK/AP1 signaling. IMM-H007 inhibits ABCA1 degradation. IMM-H007 resolves hepatic steatosis in HFD-fed hamsters by the regulation of lipid metabolism. IMM-H007 can be used for the research of nonalcoholic fatty liver disease (NAFLD) and inflammatory atherosclerosis.
|
-
- HY-19369
-
L-685458
L-685,458
|
γ-secretase
Apoptosis
|
Neurological Disease
Cancer
|
L-685458 is a potent transition state analog (TSA) γ-secretase inhibitor (GSI). L-685458 inhibits amyloid β-protein precursor γ-secretase activity with IC50 of 17 nM, shows greater than 50-100-fold selectivity over other aspartyl proteases tested. L685458 inhibits γ-secretase-mediated cleavage of APP-C99 and Notch-100 with IC50s of 301.3 nM and 351.3 nM, respectively. L-685458 can be used for the research of alzheimer’s disease (AD) and cancers.
|
-
- HY-P3340
-
Leptin (116-130)
|
iGluR
|
Neurological Disease
|
Leptin (116-130) is a bioactive leptin fragment. Leptin (116-130) promotes AMPA receptor trafficking to synapses and facilitate activity-dependent hippocampal synaptic plasticity. Leptin (116-130) prevents hippocampal synaptic disruption and neuronal cell death in models of amyloid toxicity. Leptin (116-130) has the potential for the research of Alzheimer's disease (AD).
|
-
- HY-N3680
-
-
- 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-152552
-
α-Synuclein inhibitor 8
|
α-synuclein
|
Neurological Disease
|
α-Synuclein inhibitor 8 is an active inhibitor of α-Synuclein with an IC50 value of 2.5 µM. α-Synuclein inhibitor 8 has highly inhibition on the aggregation and disaggregation of α-Synuclein fibers. α-Synuclein inhibitor 8 reduces the formation of inclusions in neurons that can repairs damage neurons and improves Parkinson’s disease (PD)-like symptoms. α-Synuclein inhibitor 8 has high antioxidant activity and low cytotoxicity.
|
-
- HY-144389
-
hAChE/Aβ1-42-IN-1
|
Cholinesterase (ChE)
Amyloid-β
|
Neurological Disease
|
hAChE/Aβ1-42-IN-1 (Compound 16) is a potent inhibitor of hAChE and Aβ1-42 aggregation. hAChE/Aβ1-42-IN-1 shows acceptable relative safety upon hepG2 cell line and excellent BBB penetration with wide safety margin. hAChE/Aβ1-42-IN-1 has the potential for the research of Alzheimer disease (AD).
|
-
- HY-146619
-
RAGE/SERT-IN-1
|
Amyloid-β
Serotonin Transporter
|
Neurological Disease
|
RAGE/SERT-IN-1 is a potent and orally active advanced glycation end products (RAGE) and serotonin transporter (SERT) inhibitor with IC50s of 8.26 μM and 31.09 nM, respectively. RAGE/SERT-IN-1 exhibits significant neuroprotective effect against Aβ25-35-induced neuronal damage and alleviates depressive behavior of mice. RAGE/SERT-IN-1 can be used for researching the comorbidity of Alzheimer's disease and depression.
|
-
- HY-142934
-
RORγt inhibitor 2
|
ROR
|
Inflammation/Immunology
Cancer
|
RORγt inhibitor 2 (Compound 119) is a potent RORγt inhibitor with an IC50 of 9.2 nM. RORγt inhibitor 2 can be used for the research of cancer, inflammation or autoimmune diseases mediated by RORγt.
|
-
- HY-144204
-
Estrogen receptor antagonist 5
|
Estrogen Receptor/ERR
|
Cancer
Endocrinology
|
Estrogen receptor antagonist 5 is a potent antagonist of Estrogen receptor. The estrogen receptor is a ligand-activated transcriptional regulatory protein that mediates induction of a variety of biological effects through its interaction with endogenous estrogens. Estrogen receptor antagonist 5 has the potential for the research of metastatic disease (extracted from patent WO2017174757A1, compound 165).
|
-
- HY-144206
-
Estrogen receptor antagonist 6
|
Estrogen Receptor/ERR
|
Endocrinology
|
Estrogen receptor antagonist 6 is a potent antagonist of Estrogen receptor. The estrogen receptor is a ligand-activated transcriptional regulatory protein that mediates induction of a variety of biological effects through its interaction with endogenous estrogens. Estrogen receptor antagonist 6 has the potential for the research of metastatic disease (extracted from patent WO2017174757A1, compound 166).
|
-
- HY-148104
-
-
- 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-145240
-
eIF4E-IN-1
|
Eukaryotic Initiation Factor (eIF)
|
Cancer
Infection
|
eIF4E-IN-1 is a potent inhibitor of eIF4E. eIF4E-IN-1 inhibits immunosuppression components such as immune checkpoint proteins PD-1, PD-L1, LAG3, TIM3, and/or IDO, in order to inhibit or release immune suppression in certain diseases, such as cancer and infectious disease (extracted from patent WO2021003194A1, compound Y).
|
-
- HY-A0208
-
Rosoxacin
Acrosoxacin
|
Bacterial
Antibiotic
|
Infection
|
Rosoxacin (Acrosoxacin) is an orally active and broad-spectrum antibacterial quinolone antibiotic. Rosoxacin inhibits Gram-negative bacteria, including N. gonorrhoeae (MIC range=0.03-0.125 µg/mL).Rosoxacin can be used in studies of urinary tract infections and certain sexually transmitted diseases.
|
-
- HY-N1875
-
4-(Ethoxymethyl)phenol
p-Hydroxybenzyl Et ether
|
Others
|
Inflammation/Immunology
|
4-(Ethoxymethyl)phenol (p-Hydroxybenzyl Et ether) is a potent antioxidant from Amburana cearensis leaf extract, with in vitro cytogenotoxic properties. Amburana cearensis leaves can be used foe the research of respiratory diseases and inflammations.
|
-
- HY-P3779
-
Amyloid 17-42
Aβ(17-42)
|
Apoptosis
|
Neurological Disease
|
Amyloid 17-42 (Aβ(17-42)) is a major constituent of diffuse plaques in Alzheimer's disease and cerebellar pre-amyloid in Down's syndrome, derived by alpha- and gamma-secretase cleavage of the amyloid precursor protein (APP). Amyloid 17-42 can induce neuronal apoptosis via a Fas-like/caspase-8 activation pathway.
|
-
- HY-151885
-
Dual AChE-MAO B-IN-3
|
Cholinesterase (ChE)
Monoamine Oxidase
|
Neurological Disease
|
Dual AChE-MAO B-IN-3 (compound C10) is a potent dual AChE/MAO-B inhibitior, with IC50 values of 0.58 and 0.41 μM, respectively. Dual AChE-MAO B-IN-3 is a dual-binding inhibitor bound to both the catalytic anionic site and peripheral anionic site of AChE. Dual AChE-MAO B-IN-3 can be used for Alzheimer’s disease (AD) research.
|
-
- HY-116753
-
(-)Clausenamide
|
Amyloid-β
Tau Protein
|
Neurological Disease
|
(-)Clausenamide is an active alkaloid isolated from the leaves of Clausena lansium (Lour.) Skeels, and improves cognitive function in both normal physiological and pathological conditions. (-)Clausenamide inhibits β-amyloid (Aβ) toxicity, blocking neurofibrillary tangle formation by inhibiting the phosphorylation of tau protein. (-)Clausenamide exerts a significant neuroprotective activity against Aβ25-35. (-)Clausenamide can be used for researching Alzheimer's disease (AD).
|
-
- HY-B0124A
-
Zonisamide sodium
AD 810 sodium; CI 912 sodium
|
Carbonic Anhydrase
Apoptosis
|
Neurological Disease
Cardiovascular Disease
|
Zonisamide (AD 810) sodium is an orally active carbonic anhydrase inhibitor, with Kis of 35.2 and 20.6 nM for hCA II and hCA V, respectively. Zonisamide sodium exerts neuroprotective effects through anti-apoptosis and upregulating MnSOD levels. Zonisamide sodium also increases the expression of Hrd1, thereby improving cardiac function in AAC rats. Zonisamide sodium can be used in studies of seizure, parkinson’s disease and cardiac hypertrophy.
|
-
- HY-139290
-
RGLS4326
RG4326
|
Others
|
Cancer
Metabolic Disease
|
RGLS4326 (RG4326) is a first-in-class, short oligonucleotide inhibitor of microRNA-17 (miR-17). RGLS4326 can be used for the research of autosomal dominant polycystic kidney disease (ADPKD). RGLS4326 inhibits miR-17 function in HeLa cells with an EC50 value of 28.3 nM.
|
-
- HY-B0954A
-
Oxyphencyclimine
|
mAChR
|
Endocrinology
|
Oxyphencyclimine is an orally active muscarinic receptor (mAChR) antagonist. Oxyphencyclimine is effective in reducing ulceration index and increasing pepsin activity in rat gastric ulcer model. Oxyphencyclimine can be used in studies of peptic ulcer disease and gastrointestinal spasm.
|
-
- HY-101341
-
RS 67333 hydrochloride
|
5-HT Receptor
|
Neurological Disease
|
RS 67333 hydrochloride is a potent and selective 5-HT4 receptor (5-HT4R) partial agonist with a pKi of 8.7 in guinea-pig striatum. RS 67333 hydrochloride exhibits lower affinities at several other receptors including 5-HT1A, 5-HT1D, 5-HT2A, 5-HT2C, dopamine D1, D2 and muscarinic M1-M3 receptors. RS 67333 hydrochloride has neuroprotective effects, and can be used for Alzheimer's disease research.
|
-
- HY-152113
-
AChE/BChE/MAO-B-IN-3
|
Monoamine Oxidase
Cholinesterase (ChE)
|
Neurological Disease
|
AChE/BChE/MAO-B-IN-3, an indan-1-one derivative, is a potent MAO-B inhibitor with an IC50 of 0.0359 μM for human MAO-B. AChE/BChE/MAO-B-IN-3 is a potent AChE and BChE enzyme inhibitor, with IC50s of 0.0473 μM and 0.0782 μM for human AChE and BChE enzyme, respectively. AChE/BChE/MAO-B-IN-3 shows significant antioxidant activity and has the potential for Alzheimer's disease (AD) research.
|
-
- HY-120060
-
GNF6702
|
Parasite
|
Infection
|
GNF6702 is a selective inhibitor of the kinetoplastid proteasome. GNF6702 clears parasites in murine models of leishmaniasis, Chagas disease, and human African trypanosomiasis.
|
-
- HY-10664
-
-
- HY-139572
-
-
- HY-108557
-
-
- HY-B0051
-
-
- HY-103314
-
-
- HY-108599A
-
DCPLA-ME
DCPLA methyl ester
|
PKC
|
Neurological Disease
|
DCPLA-ME, the methyl ester form of DCPLA, is a potent PKCε activator for use in the treatment of neurodegenerative diseases.
|
-
- HY-N5078
-
-
- HY-151430
-
-
- HY-149087
-
-
- HY-124832
-
δ-Secretase inhibitor 11
|
Caspase
Amyloid-β
|
Neurological Disease
|
δ-Secretase inhibitor 11 (compound 11) is an orally active, potent, BBB-penetrated, non-toxic, selective and specific δ-secretase inhibitor, with an IC50 of 0.7 μM. δ-Secretase inhibitor 11 interacts with both the active site and allosteric site of δ-secretase. δ-Secretase inhibitor 11 attenuates tau and APP (amyloid precursor protein) cleavage. δ-Secretase inhibitor 11 ameliorates synaptic dysfunction and cognitive impairments in tau P301S and 5XFAD transgenic mouse models. δ-Secretase inhibitor 11 can be used for Alzheimer's disease research.
|
-
- HY-13995B
-
Sevelamer carbonate
|
Others
|
Metabolic Disease
|
Sevelamer carbonate is an orally active and non-calcium-based phosphate binding agent and used for the hyperphosphatemia of chronic kidney disease (CKD)research. Sevelamer carbonate effectively lowers serum phosphorus levels hile having minimal effect on serum calcium or serum chloride levels in vivo. Sevelamer carbonate is considered as an improved, buffered form of sevelamer (HY-13995).
|
-
- HY-142834
-
-
- HY-N11366
-
Hadogenes Troglodytes Venom
South African Rock Scorpion Venom
|
Others
|
Infection
|
Hadogenes Troglodytes Venom (South African Rock Scorpion Venom) is venom that can be obtained from Hadogenes troglodytes. Hadogenes Troglodytes Venom can be used for the research of ion channel-associated diseases, and infections.
|
-
- HY-N2905
-
Aurantiamide acetate
Asperglaucide
|
Cathepsin
|
Inflammation/Immunology
|
Aurantiamide acetate (TMC-58A) is a selective and orally active cathepsin inhibitor isolated from Portulaca oleracea L. Aurantiamide acetate has anti-inflammatory activities and can be used for the study of inflammatory diseases.
|
-
- HY-149060
-
Neuraminidase-IN-15
|
Influenza Virus
|
Infection
|
Neuraminidase-IN-15 is an inhibitor of neuraminidase. Neuraminidase-IN-15 inhibits the activity of La Sota Clone 30 NDV-HN with an IC50 value of 0.06 µM. Neuraminidase-IN-15 can be used for the study of Newcastle disease virus (NDV) .
|
-
- HY-151193
-
NNMT-IN-3
|
Others
|
Cancer
Metabolic Disease
|
NNMT-IN-3 (compound 14) is a potent and selective nicotinamide N-methyltransferase NNMT inhibitor with IC50 values of 1.1 nM and 0.4 μM in cell-free and cell-based assays, respectively. NNMT-IN-3 can be used to research obesity, type 2 diabetes, alcohol-related liver disease, cancer, sarcopenia and so on.
|
-
- 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-P1053
-
-
- HY-132830
-
-
- HY-P0265A
-
-
- HY-134238
-
-
- HY-121577
-
-
- HY-B0124
-
Zonisamide
AD 810; CI 912
|
Carbonic Anhydrase
Apoptosis
|
Neurological Disease
|
Zonisamide (AD 810) is an orally active carbonic anhydrase inhibitor, with Kis of 35.2 and 20.6 nM for hCA II and hCA V, respectively. Zonisamide exerts neuroprotective effects through anti-apoptosis and upregulating MnSOD levels. Zonisamide also increases the expression of Hrd1, thereby improving cardiac function in AAC rats. Zonisamide can be used in studies of seizure, parkinson’s disease and cardiac hypertrophy.
|
-
- HY-100794
-
GR127935 hydrochloride
|
5-HT Receptor
|
Neurological Disease
|
GR127935 hydrochloride is a potent and orally active 5-HT1D and 5-HT1B receptor antagonist with pKis of 8.5 for both isoforms. GR127935 hydrochloride has 100-fold selectivity for 5-HT1B/1D receptors over 5-HT1A, 5-HT2A, and 5-HT2C receptors. GR127935 hydrochloride can be used in neurological disease research.
|
-
- HY-151562
-
AChE/BuChE/MAO-B-IN-1
|
Cholinesterase (ChE)
Monoamine Oxidase
|
Neurological Disease
|
AChE/BuChE/MAO-B-IN-1 (compound 19) is an inhibitor of human acetyl- (hAChE), butyrylcholinesterase (hBuChE) and monoamine oxidase-B (hMAO-B) with IC50s of 4.8 μM, 13.7 μM, and 1.11 μM, respectively. AChE/BuChE/MAO-B-IN-1 also exhibits high affinity to both the σ1 and σ2 receptors with Ki values of 42.8 nM (human σ1 receptor) and 191 nM (rat σ2 receptor), respectively. AChE/BuChE/MAO-B-IN-1 can be used for Alzheimer’s disease research.
|
-
- HY-146669
-
-
- HY-P9956
-
Siltuximab
CNTO-328
|
Interleukin Related
|
Cancer
|
Siltuximab is an anti-IL-6 (interleukin-6) monoclonal antibody, and shows antitumor activity. Siltuximab can be used in Multicentric Castleman's Disease (MCD) and COVID-19 research.
|
-
- HY-118795
-
SC-22716
|
Aminopeptidase
|
Inflammation/Immunology
|
SC-22716 is a potent, competitive, reversible inhibitor of human LTA4 hydrolase, with an IC50 of 0.20 µM. SC-22716 has potential for the research of inflammatory bowel disease (IBD) and psoriasis.
|
-
- HY-P99050
-
-
- HY-144029
-
RET-IN-13
|
RET
|
Cancer
|
RET-IN-13 (compound 1), a quinoline compound, is a potent RET inhibitor with IC50s of 0.5 nM, 0.9 nM for RET (WT) and RET (V804M), respectively. RET-IN-13 has the potential for tumors or intestinal diseases related to abnormal activation of RET research.
|
-
- HY-111547
-
M1001
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
M1001 is a weak hypoxia-inducible factor-2α (HIF-2α) agonist. M1001 can bind to the HIF-2α PAS-B domain, with a Kd of 667 nM. M1001 can be used in chronic kidney disease research.
|
-
- HY-145062
-
Enpp-1-IN-4
|
Phosphodiesterase (PDE)
|
Cancer
|
Enpp-1-IN-4 is a potent inhibitor of ectonucleotide pyrophosphatase-phosphodiesterase 1 (enpp-1). Enpp-1-IN-4 has the potential for the research of cancer diseases (extracted from patent WO2019177971A1, compound 1).
|
-
- HY-13499
-
CCR2 antagonist 5
|
CCR
|
Inflammation/Immunology
|
CCR2 antagonist 5 is a selective, orally active hCCR2 inhibitor with good binding affinity (IC50=37 nM) and potent functional antagonism (chemotaxis IC50=30 nM). CCR2 antagonist 5 displays a Ki of 9.6 µM for mCCR2 binding. CCR2 antagonist 5 can be used in the research of inflammatory disease.
|
-
- HY-124073
-
-
- HY-N6617
-
-
- HY-108680
-
-
- HY-12381
-
ML224
NCGC00242364; ANTAG3
|
TSH Receptor
|
Endocrinology
|
ML224 (NCGC00242364) is a selective TSHR antagonist with an IC50 value of 2.1 µM. ML224 can be used in the study of Graves' disease and other thyroid disorders.
|
-
- HY-148093
-
PM-81I
|
STAT
|
Cancer
Inflammation/Immunology
|
PM-81I is a potent STAT6 inhibitor (targeting the SH2 structural domain) that effectively reduces STAT6 phosphorylation levels. PM-81I can be used in studies of allergic lung disease, allergic rhinitis, chronic obstructive pulmonary disease or cancer[1].
|
-
- HY-142701
-
SSTR4 agonist 4
|
Somatostatin Receptor
|
Neurological Disease
|
SSTR4 agonist 4 is a potent agonist of SSTR4. SSTR4 is expressed at relatively high levels in the hippocampus and neocortex, memory and learning regions, and Alzheimer's disease pathology. SSTR4 agonists are potent in rodent models of pain associated with acute and chronic associated anti-peripheral nociceptive and anti-inflammatory activity. SSTR4 agonist 4 has the potential for the research of pain (extracted from patent WO2021233428A1, compound 14).
|
-
- HY-106224B
-
Orexin A (human, rat, mouse) (acetate)
Hypocretin-1 (human, rat, mouse) (acetate)
|
Orexin Receptor (OX Receptor)
|
Neurological Disease
|
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.
|
-
- HY-142700
-
SSTR4 agonist 3
|
Somatostatin Receptor
|
Neurological Disease
|
SSTR4 agonist 3 is a potent agonist of SSTR4. SSTR4 is expressed at relatively high levels in the hippocampus and neocortex, memory and learning regions, and Alzheimer's disease pathology. SSTR4 agonists are potent in rodent models of pain associated with acute and chronic associated anti-peripheral nociceptive and anti-inflammatory activity. SSTR4 agonist 3 has the potential for the research of pain (extracted from patent WO2021233427A1, compound 14).
|
-
- 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-N2099
-
Onjisaponin B
|
Autophagy
|
Neurological Disease
|
Onjisaponin B is a natural product derived from Polygala tenuifolia. Onjisaponin B enhances autophagy and accelerates the degradation of mutant α-synuclein and huntingtin in PC-12 cells, and exbibits potential therapeutic effects on Parkinson disease and Huntington disease.
|
-
- HY-137315
-
TML-6
|
Amyloid-β
NF-κB
mTOR
Keap1-Nrf2
|
Neurological Disease
|
TML-6, an orally active curcumin derivative, inhibits the synthesis of the β-amyloid precursor protein and β-amyloid (Aβ). TML-6 can upregulate Apo E, suppress NF-κB and mTOR, and increase the activity of the anti-oxidative Nrf2 gene. TML-6 has the potential for Alzheimer’s disease (AD) research.
|
-
- HY-131592
-
-
- HY-107337S
-
-
- HY-103391
-
Qc1
|
Others
|
Metabolic Disease
|
Qc1 is a reversible and noncompetitive threonine dehydrogenase (TDH) inhibitor. Qc1 can be used for the research of Metabolic disease.
|
-
- HY-B1096
-
Etamivan
Ethamivan; N,N-Diethylvanillamide
|
Others
|
Neurological Disease
|
Etamivan (Ethamivan), an orally active respiratory stimulant, is mainly used in the research of barbiturate overdose and chronic obstructive pulmonary disease.
|
-
- HY-103372
-
-
- 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-W181102
-
NFAT Inhibitor-2
|
Others
|
Inflammation/Immunology
Neurological Disease
Cardiovascular Disease
|
NFAT Inhibitor-2 is a potent inhibitor of calcineurin NFAT signalling. Calcineurin is a serine/threonine protein phosphatase regulated by Ca2+ and calmodulin. NFAT Inhibitor-2 has the potential for the research of inflammatory disease, an autoimmune disorder, a cardiovascular disease, a neurodegenerative disease, a disease occurring with uncontrolled cell proliferation and/or differentiation, an angiogenesis-related disease, an allergy, anaphylaxis and alopecia (extracted from patent WO2016207212A1, compound 17).
|
-
- HY-W268334
-
-
- HY-109086
-
Edicotinib
JNJ-40346527; JNJ-527
|
c-Fms
|
Inflammation/Immunology
Neurological Disease
|
Edicotinib (JNJ-40346527) is a potent, selective, brain penetrant and orally active colony-stimulating factor-1 receptor (CSF-1R) inhibitor with an IC50 of 3.2 nM. Edicotinib exhibits less inhibitory effects on KIT and FLT3 with IC50 values of 20 nM and 190 nM, respectively. Edicotinib limits microglial expansion and attenuates microglial proliferation and neurodegeneration in mice. Edicotinib has the potential for Alzheimer’s disease and rheumatoid arthritis research.
|
-
- 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-33169
-
-
- HY-10388
-
-
- HY-19344
-
Lifitegrast
SAR 1118; SHP-606
|
Integrin
|
Inflammation/Immunology
|
Lifitegrast (SAR 1118) is a potent integrin antagonist. Lifitegrast blocks the binding of intercellular adhesion molecule 1 (ICAM-1) to lymphocyte function-associated antigen 1 (LFA-1), interrupting the T cell-mediated inflammatory cycle. Lifitegrast inhibits Jurkat T cell attachment to ICAM-1 with an IC50 of 2.98 nM. Lifitegrast can be used for researching dry eye disease.
|
-
- HY-19344A
-
Lifitegrast sodium
SAR 1118 sodium; SHP-606 sodium
|
Integrin
|
Inflammation/Immunology
|
Lifitegrast (SAR 1118) sodium is a potent integrin antagonist. Lifitegrast sodium blocks the binding of intercellular adhesion molecule 1 (ICAM-1) to lymphocyte function-associated antigen 1 (LFA-1), interrupting the T cell-mediated inflammatory cycle. Lifitegrast sodium inhibits Jurkat T cell attachment to ICAM-1 with an IC50 of 2.98 nM. Lifitegrast sodium can be used for researching dry eye disease.
|
-
- HY-P99563
-
Tibulizumab
LY 3090106; LY-3090106; LY3090106
|
TNF Receptor
Interleukin Related
|
Inflammation/Immunology
|
Tibulizumab (LY 3090106) is a tetravalent bispecific monoclonal antibody targeting B-cell activating factor (BAFF) and IL-17A with Kd values of 60 pM and 14 pM, respectively. Tibulizumab can be used for autoimmune disease research.
|
-
- HY-121390
-
Lasiocarpine
|
Endogenous Metabolite
|
Cancer
|
Lasiocarpine, a hepatotoxic pyrrolizidine alkaloid (PA), causes fatal liver veno-occlusive disease in vivo. Lasiocarpine is toxic only after its metabolic conversion to the toxic intermediate, including dehydrolasiocarpine and N-oxide.
|
-
- HY-146398
-
AMPK activator 6
|
AMPK
|
Metabolic Disease
|
AMPK activator 6 (Compound GC) reduces lipid content and activates the AMPK pathway in HepG2 and 3T3-L1 cells. AMPK activator 6 significantly suppresses the increase in triglyceride (TG) , total cholesterol (TC), low-density lipoprotein-C (LDL-C), and other biochemical indices in blood serum. AMPK activator 6 can be used for the research of non-alcoholic fatty liver disease (NAFLD) and metabolic syndrome.
|
-
- HY-115876
-
-
- HY-151201
-
Steroid sulfatase/17β-HSD1-IN-3
|
Others
|
Cancer
|
Steroid sulfatase/17β-HSD1-IN-3 (compound 19) is a dual inhibitor of steroid sulfatase (STS) and 17β-hydroxysteroid dehydrogenase type 1 (17β HSD1). Steroid sulfatase/17β-HSD1-IN-3 irreversibly inhibits hSTS activity with anIC50 value of 27 nM. Steroid sulfatase/17β-HSD1-IN-3 can be used in the study of endometriosis and other estrogen-dependent diseases.
|
-
- HY-151202
-
Steroid sulfatase/17β-HSD1-IN-4
|
Others
|
Cancer
|
Steroid sulfatase/17β-HSD1-IN-4 (compound 37) is a dual inhibitor of steroid sulfatase (STS) and 17β-hydroxysteroid dehydrogenase type 1 (17β HSD1). Steroid sulfatase/17β-HSD1-IN-4 irreversibly inhibits hSTS activity with anIC50 value of 63 nM. Steroid sulfatase/17β-HSD1-IN-4 can be used in the study of endometriosis and other estrogen-dependent diseases.
|
-
- HY-N0611
-
alpha-Boswellic acid
α-Boswellic acid
|
Others
|
Inflammation/Immunology
|
alpha-Boswellic acid (α-Boswellic acid) is a pentacyclic triterpene compound from extracts of Frankincense, has anticonvulsant and anti-cancer properties. alpha-Boswellic acid prevents and decreases the progression of Alzheimer’s hallmarks in vivo and can be used for Alzheimer’s disease research.
|
-
- HY-152114
-
AChE/BChE/MAO-B-IN-4
|
Monoamine Oxidase
Cholinesterase (ChE)
|
Neurological Disease
|
AChE/BChE/MAO-B-IN-4, an indan-1-one derivative, is a potent MAO-B inhibitor with an IC50 of 0.0393 μM for human MAO-B. AChE/BChE/MAO-B-IN-4 is a potent AChE and BChE enzyme inhibitor, with IC50s of 0.0458 μM and 0.075 μM for human AChE and BChE enzyme, respectively. AChE/BChE/MAO-B-IN-4 shows significant antioxidant activity and prevent β-amyloid plaque aggregation. AChE/BChE/MAO-B-IN-4 has the potential for Alzheimer's disease (AD) research.
|
-
- HY-105697
-
Protoveratrine A
NSC 7526; Protalba; Protoveratrin
|
Others
|
Cardiovascular Disease
|
Protoveratrine A (NSC 7526; Protalba; Protoveratrin) is an alkaloid with strong cardiostimulant and vasoconstrictive effects, which can be used in the study of hypertension and other cardiovascular diseases.
|
-
- HY-N4305
-
-
- HY-N4173
-
-
- HY-40161
-
-
- HY-134879
-
-
- HY-147195
-
-
- HY-117983
-
RU-505
|
Amyloid-β
|
Neurological Disease
|
RU-505 is an effective β-amyloid (Aβ)-fibrinogen interaction inhibitor with IC50s of 5.00 and 2.72 μM in fluorescence polarization (FP) and AlphaLISA assays, respectively. RU-505 is highly permeable to the BBB. RU-505 reduces cerebral amyloid angiopathy (CAA). RU-505 can be used for the research of Alzheimer’s disease (AD).
|
-
- HY-120785
-
SR1555
|
ROR
|
Inflammation/Immunology
|
SR1555 is a specific retinoic acid receptor-related orphan nuclear receptor γ (RORγ) inverse agonist with an IC50 value of 1 μM. SR1555 not only inhibits TH17 cell development and function but also increases the frequency of T regulatory cells, as well as inhibits the expression of IL-17. SR1555 can be used for researching autoimmune diseases.
|
-
- HY-100007A
-
Vonoprazan hydrochloride
TAK-438 hydrochloride
|
Proton Pump
Bacterial
|
Infection
Endocrinology
|
Vonoprazan hydrochloride, a proton pump inhibitor (PPI), is a potent and orally active potassium-competitive acid blocker (P-CAB), with antisecretory activity. Vonoprazan hydrochloride inhibits H +,K +-ATPase activity in porcine gastric microsomes with an IC50 of 19 nM at pH 6.5. Vonoprazan hydrochloride is developed for the research of acid-related diseases, such as gastroesophageal reflux disease and peptic ulcer disease. Vonoprazan hydrochloride can be used for eradication of Helicobacter pylori.
|
-
- HY-N2913
-
-
- HY-E70005
-
Collagenase
|
Biochemical Assay Reagents
|
Others
|
Collagenase is a proteolytic enzyme, which breaks the peptide bonds in collagen. Collagenase has good research potential in disc herniation, keloid, cellulite, lipoma, as well as peyronie's disease and dupuytren fracture.
|
-
- HY-115987
-
MAO-B-IN-6
|
Monoamine Oxidase
|
Neurological Disease
|
MAO-B-IN-6 is a potent, selective and orally active MAO-B inhibitor with an IC50 of 0.019 µM. MAO-B-IN-6 shows more efficacious than Safinamide in vitro and in vivo. MAO-B-IN-6 has the potential for the research of parkinson's disease (PD).
|
-
- HY-115977
-
Aldose reductase-IN-3
|
Aldose Reductase
|
Inflammation/Immunology
|
Aldose reductase-IN-3 (Compound 5) is a potent and moderately selective inhibitor of aldose reductase (AR) with an IC50 of 3.99 μM. Aldose reductase has recently emerged as a molecular target that is involved in various inflammatory diseases, including sepsis. Aldose reductase-IN-3 has the potential for the research of sepsis.
|
-
- HY-147060
-
Dyrk1A-IN-3
|
DYRK
|
Neurological Disease
|
Dyrk1A-IN-3 (Compound 8b), a highly selective dual-specificity tyrosine-regulated kinase 1A (DYRK1A) inhibitor, maintains high levels of DYRK1A binding affinity (IC50=76 nM). Dyrk1A-IN-3 can be used for the research of neurodegenerative disorders such as Alzheimer’s Disease, Huntington’s Disease, and Parkinson’s Disease.
|
-
- HY-P9953
-
Certolizumab pegol
Certolizumab; CDP870
|
TNF Receptor
|
Inflammation/Immunology
|
Certolizumab pegol (Certolizumab) is a recombinant, polyethylene glycolylated, antigen-binding fragment of a humanized monoclonal antibody that selectively targets and neutralizes tumour necrosis factor-α (TNF-α). Certolizumab pegol can be used for rheumatoid arthritis and Crohn disease research.
|
-
- HY-15781
-
Morinidazole
|
Bacterial
|
Infection
|
Morinidazole is an orally active and 5-nitroimidazole antimicrobial agent that undergoes extensive metabolism in humans via N +-glucuronidation and sulfation. Morinidazole can be used for bacterial infections research including appendicitis and pelvic inflammatory disease (PID) caused by anaerobic bacteria.
|
-
- HY-103190
-
MRS1220
|
Adenosine Receptor
|
Cancer
Neurological Disease
|
MRS1220, a highly potent and selective human A3 adenosine receptor (hA3AR) antagonist with a Ki of 0.59 nM, has therapeutic potential for the research of diseases of the central nervous system. MRS1220 reduces glioblastoma tumor size and blood vessel formation in vivo.
|
-
- HY-101367A
-
-
- HY-17623S
-
-
- HY-10043A
-
-
- HY-120475A
-
PBT434 methanesulfonate
|
α-synuclein
|
Neurological Disease
|
PBT434 methanesulfonate is a potent, orally active and cross the blood-brain barrier α-synuclein aggregation inhibitor. PBT434 methanesulfonate can be used as a iron chelator and modulates transcellular iron trafficking. PBT434 methanesulfonate inhibits iron-mediated redox activity and iron-mediated aggregation of α-synuclein. PBT434 methanesulfonate prevents the loss of substantia nigra pars compacta neurons (SNpc). PBT434 methanesulfonate has the potential for the research of Parkinson’s disease (PD).
|
-
- HY-148325
-
α7 Nicotinic receptor agonist-1
|
nAChR
|
Neurological Disease
|
α7 Nicotinic receptor agonist-1 (Preparation 5) is an α7 nAChR agonist. α7 Nicotinic receptor agonist-1 can be used in studies of psychiatric disorders (such as schizophrenia, manic or hypomanic depression and anxiety disorders) and intellectual disorders (such as alzheimer's disease, learning deficits, cognitive deficits, attention deficits, memory loss, lewy body dementia and attention deficit hyperactivity disorder).
|
-
- HY-W091734
-
-
- HY-151431
-
Nrf2/HO-1 activator 2
|
Keap1-Nrf2
Reactive Oxygen Species
ERK
Akt
JNK
|
Neurological Disease
|
Nrf2/HO-1 activator 2 (compound 13m), difluoro-substituted derivative, is a potent Nrf2/HO-1 activator. Nrf2/HO-1 activator 2 has neuroprotective and antioxidant effects through the Nrf2/HO-1 pathway mediated by phosphorylation of ERK1/2, JNK, or Akt in PC12 cells. Nrf2/HO-1 activator 2 can be used in the research of Parkinson's disease (PD).
|
-
- HY-151369
-
-
- 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-P99755
-
-
- HY-B0232
-
-
- HY-113344
-
-
- HY-P1440
-
-
- HY-112070
-
-
- HY-N10579
-
Chrexanthomycin C
|
DNA/RNA Synthesis
|
Neurological Disease
|
Chrexanthomycin C is an orally active marine natural product with remarkable bioactivities. Chrexanthomycin C has binding affinity for DNA (G4C2) 4 G4 with a Kd value of 2.8 mM. Chrexanthomycin C can be used for the research of neurodegenerative disease such as amyotrophic lateral sclerosis (ALS).
|
-
- HY-W028142
-
Quipazine
|
5-HT Receptor
SARS-CoV
|
Neurological Disease
|
Quipazine is a 5-HT agonist with a Ki value of 1.4 nM for displaces [3H]GR65630 from 5-HT3R in rat. Quipazine shows antiviral activity against SARS-CoV-2 with an EC50 of 31.64 μM. Quipazine behaves as a 5-HT3R agonist in peripheral models. Quipazine can be used for neurological disease research.
|
-
- HY-W008614
-
Lansoprazole sulfone
AG-1813
|
Proton Pump
|
Metabolic Disease
|
Lansoprazole sulfone (AG-1813) is an orally active and selective inhibitor of H +, K +-ATPase. Lansoprazole sulfone can significantly stimulates gastric acid secretion by inhibiting H +, K +-ATPase. Lansoprazole sulfone has potential applications in duodenal ulcer, gastric ulcer, gastroesophageal reflux disease and Zolinger Ellison disease.
|
-
- HY-110168
-
NS 9283
|
nAChR
|
Neurological Disease
|
NS9283 is a positive positive allosteric modulator of (α4)3(β2)2 nicotinic ACh receptors. NS9283 can be used in a series of neurological conditions such as attention deficit hyperactivity disorder (ADHD), schizophrenia, Parkinson's disease and Alzheimer's disease.
|
-
- HY-N11416
-
-
- HY-122094
-
-
- HY-15781A
-
(R)-Morinidazole
|
Bacterial
|
Infection
|
(R)-Morinidazole is an orally active and 5-nitroimidazole antimicrobial agent that undergoes extensive metabolism in humans via N +-glucuronidation and sulfation. (R)-Morinidazole can be used for bacterial infections research including appendicitis and pelvic inflammatory disease (PID) caused by anaerobic bacteria.
|
-
- HY-145721
-
Mongersen
GED-0301
|
TGF-beta/Smad
|
Inflammation/Immunology
|
Mongersen (GED-0301) is a specific and orally active SMAD7 antisense oligonucleotide. Mongersen restores TGF-β1 activity leading to inhibition of inflammatory signals. Mongersen can attenuate Crohn's disease-like experimental colitis in mice.
|
-
- HY-131062
-
yGsy2p-IN-1
|
Others
|
Metabolic Disease
|
yGsy2p-IN-1 is a potent inhibitor for yeast glycogen synthase 2 (yGsy2p). yGsy2p-IN-1 is a competitive human glycogen synthase 1 (hGYS1) inhibitor with an IC50 of 2.75 µM and a Ki of 1.31 µM for wild-type hGYS1. yGsy2p-IN-H23 a pyrazole inhibitor, is used for glycogen storage diseases (GSDs).
|
-
- HY-107529
-
TC-G 24
|
GSK-3
|
Metabolic Disease
Neurological Disease
|
TC-G 24 (Compound 24) is a potent, selective glycogen synthase kinase-3β (GSK-3β) inhibitor with an IC50 of 17.1 nM. TC-G 24 can cross the BBB and can be used for studying many diseases such as type 2 diabetes mellitus, stroke, Alzheimer, and other related diseases.
|
-
- HY-W040146S
-
-
- HY-148689
-
SPC4061
|
Ser/Thr Protease
|
Metabolic Disease
|
SPC4061 an antisense nucleotide, is a potent PCSK9 inhibitor. SPC4061 targets the lock-in nucleic acid (LNA) of PCSK9 for the study of hypercholesterolemia and related diseases.
|
-
- HY-132812
-
Emraclidine
CVL-231
|
mAChR
|
Neurological Disease
|
Emraclidine (CVL-231) is a muscarinic M4 receptor positive allosteric modulator (WO2018002760, compound 11). Emraclidine can be used for the research of neurological diseases.
|
-
- HY-134880
-
-
- HY-P99317
-
Solanezumab
Immunoglobulin G1, anti-(human β-amyloid) (human-mouse monoclonAnti-Human Abeta Recombinant Antibody
|
Amyloid-β
|
Neurological Disease
|
Solanezumab is a humanized monoclonal IgG1 antibody directed against the mid-domain of the amyloid-β (Aβ) peptide. Solanezumab has the potential for the research of Alzheimer’s disease.
|
-
- HY-N7506
-
13-Hydroxyisobakuchiol
Delta3,2-Hydroxylbakuchiol
|
Monoamine Transporter
Dopamine Transporter
|
Neurological Disease
|
Hydroxyisobakuchiol (Delta3,2-Hydroxylbakuchiol), an analog of Bakuchiol (HY-N0235) isolated from Psoralea corylifolia (L.), is a potent monoamine transporter inhibitor. 13-Hydroxyisobakuchiol is more selective for the dopamine transporter (DAT) (IC50=0.58 μM) and norepinephrine transporter (NET) (IC50=0.69 μM) than for the serotonin transporter (SERT) (IC50=312.02 μM). 13-Hydroxyisobakuchiol has the potential for the research of disorders such as Parkinson's disease and depression.
|
-
- HY-19999A
-
PF-CBP1 hydrochloride
|
Epigenetic Reader Domain
Histone Acetyltransferase
|
Neurological Disease
|
PF-CBP1 hydrochloride is a highly selective inhibitor of the CREB binding protein bromodomain (CBP BRD). PF-CBP1 inhibits CREBBP and EP300 bromodomains with IC50 of 125 nM and 363 nM respectively. PF-CBP1 hydrochloride reduces LPS-induced inflammatory cytokines expression (IL-1β, IL-6 and IFN-β) in primary macrophages. PF-CBP1 hydrochloride also downregulates RGS4 expression cortical neurons and can be used for the research of neurological disorders, including epilepsy and parkinson's disease, et al.
|
-
- 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-112726
-
-
- HY-100007
-
Vonoprazan
TAK-438 free base
|
Proton Pump
Bacterial
|
Endocrinology
|
Vonoprazan (TAK-438 free base), a proton pump inhibitor (PPI), is a potent and orally active potassium-competitive acid blocker (P-CAB), with antisecretory activity. Vonoprazan inhibits H +,K +-ATPase activity in porcine gastric microsomes with an IC50 of 19 nM at pH 6.5. Vonoprazan is developed for the research of acid-related diseases, such as gastroesophageal reflux disease and peptic ulcer disease. Vonoprazan can be used for eradication of Helicobacter pylori.
|
-
- HY-P1267
-
α-Conotoxin PnIA
|
nAChR
|
Neurological Disease
|
α-Conotoxin PnIA, a potent and selective antagonist of the mammalian α7 nAChR, has the potential for the research of neurological conditions such as neuropathic pain and Alzheimer’s disease.
|
-
- HY-P2562
-
-
- HY-108017
-
Ferric maltol
|
Others
|
Metabolic Disease
|
Ferric maltol is an orally active complex of a single ferric ion (Fe 3+). Ferric maltol has tha potential for iron deficiency anemia treatment in inflammatory bowel disease.
|
-
- HY-N7480A
-
-
- HY-W029659
-
-
- HY-N1362
-
Salvianolic acid B
Lithospermic acid B
|
Autophagy
|
Cardiovascular Disease
|
Salvianolic acid B is an active ingredient of Salvia miltiorrhiza, which has been widely applied in China for the management of various microcirculation-related disorders, such as cardiovascular disease, cerebrovascular disease, and diabetic vascular complication.
|
-
- HY-108411
-
Emedastine
|
Histamine Receptor
|
Inflammation/Immunology
|
Emedastine is an orally active, selective and high affinity histamine H1 receptor antagonist with a Ki value of 1.3 nM. Emedastine is a benzimidazole derivative with potent antiallergic properties and used for allergic rhinitis, allergic skin diseases and allergic conjunctivitis.
|
-
- HY-108464A
-
Phenamil methanesulfonate
|
Sodium Channel
TRP Channel
|
Metabolic Disease
Inflammation/Immunology
|
Phenamil methanesulfonate, an analog of Amiloride (HY-B0285), is a more potent and less reversible epithelial sodium channel (ENaC) blocker with an IC50 of 400 nM. Phenamil methanesulfonate is also a competive inhibitor of TRPP3 and inhibits TRPP3-mediated Ca 2+ transport with an IC50 of 140 nM in a Ca 2+ uptake assay. Phenamil methanesulfonate is an intriguing small molecule to promote bone repair by strongly activating BMP signaling pathway. Phenamil methanesulfonate is used for the research of cystic fibrosis lung disease.
|
-
- HY-101046
-
Quipazine dimaleate
|
5-HT Receptor
SARS-CoV
|
Neurological Disease
|
Quipazine dimaleate is a 5-HT agonist with a Ki value of 1.4 nM for displaces [3H]GR65630 from 5-HT3R in rat. Quipazine dimaleate shows antiviral activity against SARS-CoV-2 with an EC50 of 31.64 μM. Quipazine dimaleate behaves as a 5-HT3R antagonist in peripheral models. Quipazine dimaleate can be used for neurological disease research.
|
-
- HY-152028
-
-
- HY-152027
-
-
- HY-113110
-
-
- HY-W016443
-
-
- HY-139908
-
MERS-CoV-IN-1
|
SARS-CoV
|
Infection
|
MERS-CoV-IN-1 exhibits excellent inhibitory activity against coronavirus. MERS-CoV-IN-1 is useful as a pharmaceutical composition for preventing coronavirus-induced diseases (MERS-CoV and SARS) (extracted from patent WO2018174442A1, compound 1).
|
-
- HY-107935
-
6α-Fluoroprednisolone
Fluprednisolone
|
Others
|
Inflammation/Immunology
|
6α-Fluoroprednisolone (Fluprednisolone) is an internal standard for methylprednisolone, prednisolone and prednisone. 6α-Fluoroprednisolone is an anti-inflammatory agent. 6α-Fluoroprednisolone can be used for congenital adrenal virilism and Addison's disease research.
|
-
- HY-P1267A
-
α-Conotoxin PnIA TFA
|
nAChR
|
Neurological Disease
|
α-Conotoxin PnIA TFA, a potent and selective antagonist of the mammalian α7 nAChR, has the potential for the research of neurological conditions such as neuropathic pain and Alzheimer’s disease.
|
-
- HY-125967
-
AM 374
|
FAAH
|
Neurological Disease
|
AM 374 is an fatty acid amide hydrolase (FAAH) inhibitor. AM 374 inhibits amidase activity with an IC50 value of 13 nM. AM 374 can be used for the research of neurological disease.
|
-
- HY-W013372
-
-
- HY-116459
-
trans-Cevimeline hydrochloride
AF102A hydrochloride
|
mAChR
|
Neurological Disease
|
Trans-Cevimeline (AF102A) (hydrochloride), as a trans-isomer of AF102B, is a M1 selective cholinergic agonist. Trans-Cevimeline (AF102A) (hydrochloride) can be used for the research of Alzheimer's disease.
|
-
- HY-103479
-
GOAT-IN-1
|
Acyltransferase
|
Cancer
Metabolic Disease
Neurological Disease
Cardiovascular Disease
|
GOAT-IN-1 is an inhibitor of ghrelin O-acyltransferase (GOAT), which could be useful for the prophylaxis or treatment of obesity, diabetes, hyperlipidemia, metabolic, non-alcoholic fatty liver, steatohepatitis, sarcopenia, appetite control, alcohol/narcotic dependence, Alzheimer’s disease, Parkinson’s disease, cerebrovascular dementia, cerebral apoplexy, cerebral infarction, cardic disease, some kind of tumors.
|
-
- HY-Y0055
-
-
- 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-B0520
-
Benztropine
Benzatropine; Benzotropine
|
Dopamine Receptor
mAChR
Histamine Receptor
|
|
Benztropine (Benzatropine; Benzotropine) is an orally active centrally acting anticholinergic agent that can be used for Parkinson's disease research. Benztropine is an anti-histamine agent and a dopamine re-uptake inhibitor. Benztropine is also a human D2 dopamine receptor allosteric antagonist. Benztropine mesylate also has anti-CSCs (cancer stem cells) effects.
|
-
- HY-142703
-
RORγt inverse agonist 28
|
ROR
|
Inflammation/Immunology
|
RORγt inverse agonist 28 is a potent reverse agonist of RORγt. RORγt inverse agonist 28 regulates the differentiation of Th17 cells and inhibits the production of IL-17. RORγt inverse agonist 28 has the potential for the research of inflammation and autoimmune diseases (extracted from patent WO2021228215A1, compound 6) .
|
-
- HY-142806
-
RORγt inverse agonist 26
|
ROR
|
Inflammation/Immunology
|
RORγt inverse agonist 26 is a potent reverse agonist of RORγt. RORγt inverse agonist 26 regulates the differentiation of Th17 cells and inhibits the production of IL-17. RORγt inverse agonist 26 has the potential for the research of inflammation and autoimmune diseases (extracted from patent WO2021228215A1, compound 1) .
|
-
- HY-148322
-
Sirtuin modulator 5
|
Sirtuin
|
Cancer
Infection
Metabolic Disease
Inflammation/Immunology
Neurological Disease
|
Sirtuin modulator 5 is a sirtuin modulating agent. Sirtuin modulator 5 can activate SIRT1 with a DC50 value of <50 μM. Sirtuin modulator 5 can be used for increasing the lifespan of a cell and used for the research of variety of diseases including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benfit from increased mitochondrial activity.
|
-
- HY-101283
-
HCH6-1
|
Formyl Peptide Receptor (FPR)
|
Inflammation/Immunology
|
HCH6-1 is a potent and competitive dipeptide antagonist of Formyl peptide receptor 1 (FPR1). HCH6-1 inhibits chemotaxis, superoxide anion generation, and elastase release in human neutrophils specifically activated by fMLF (an FPR1 agonist). HCH6-1 has protective effects against acute lung injury (ALI) in vivo and can be used for the research of FPR1-involved inflammatory lung diseases.
|
-
- HY-P3977
-
ACTH (3-24) (human, bovine, mouse, ovine, porcine, rabbit, rat)
|
Melanocortin Receptor
|
Cancer
Inflammation/Immunology
Cardiovascular Disease
|
ACTH (3-24) (human, bovine, mouse, ovine, porcine, rabbit, rat) is the 3-24 fragment of adrenocorticotropic hormone (ACTH). ACTH (3-24) (human, bovine, mouse, ovine, porcine, rabbit, rat) can be used for research of a variety of diseases, including cancer, immune diseases, cardiovascular disease.
|
-