Search Result
Results for "
CNS penetrant
" in MedChemExpress (MCE) Product Catalog:
1
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-13030
-
-
-
- HY-P0201
-
-
-
- HY-13902
-
|
VE-822; VX-970; M6620
|
ATM/ATR
Apoptosis
STING
Caspase
|
Infection
Metabolic Disease
Cancer
|
|
Berzosertib (VE-822) is an orally active, CNS-penetrant, and selective ATR kinase inhibitor. Berzosertib blocks ATR kinase activity, abrogates G2/M cell cycle checkpoint, impairs DNA damage repair. Berzosertib induces apoptosis, inhibnits conlony migration, inhibits cell proliferation, and activates cGAS-STING axes in cancer cells. Berzosertib can be used for the research of cancers, such as head and neck squamous cell carcinoma, and colorectal cancer .
|
-
-
- HY-12768
-
|
BLZ945
|
c-Fms
|
Infection
Neurological Disease
Cancer
|
|
Sotuletinib (BLZ945) is a potent, selective, orally active and brain-penetrant CSF-1R (c-Fms) inhibitor with an IC50 of 1 nM, showing more than 1,000-fold selectivity against its closest receptor tyrosine kinase homologs. Sotuletinib can be used for microglia depletion, and for tumor and CNS-related disease research .
|
-
-
- HY-15136
-
|
Sch66336
|
Farnesyl Transferase
Ras
Autophagy
|
Infection
Neurological Disease
Cancer
|
|
Lonafarnib (Sch66336) is a potent and orally active, and CNS-penetrant farnesyl transferase (FTase) inhibitor. Lonafarnib inhibits the activities of H-ras, K-ras and N-ras with IC50 values of 1.9 nM, 5.2 nM and 2.8 nM, respectively. Lonafarnib also has anti-hepatitis delta virus (HDV) activities .
|
-
-
- HY-N2332A
-
|
MLA citrate
|
nAChR
|
Neurological Disease
|
|
Methyllycaconitine (MLA) citrate is a potent, selective, CNS-penetrant, competitive α7nAChR antagonist. Methyllycaconitine citrate alleviates amyloid-β peptides-induced cytotoxicity in SH-SY5Y cells. Methyllycaconitine citrate prevents methamphetamine-induced effects in mouse striatum. Methyllycaconitine citrate can be used for neurological disease research, such as Alzheimer’s disease .
|
-
-
- HY-12288
-
|
RPC-1063
|
LPL Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
Ozanimod (RPC-1063) is a CNS-penetrant sphingosine 1-phosphate (S1P) receptor modulator that binds with high affinity selectively to S1P receptor subtypes 1 (S1P1) and 5 (S1P5). Ozanimod has modulate effect for hS1P1 and hS1P5 receptor with EC50s of 1.03 nM and 8.6 nM, respectively. Ozanimod can be used for the research of relapsing multiple sclerosis (MS) .
|
-
-
- HY-156681
-
|
STX-478; STX-478-101; LY4064809
|
PI3K
|
Cancer
|
|
STX-478 (compound 80) is an oral CNS-penetrant allosteric mutant-selective PI3Kα inhibitor. STX-478 shows robust and durable tumor regression and can be used in cancer research .
|
-
-
- HY-12776
-
GSK805
5 Publications Verification
|
ROR
|
Inflammation/Immunology
|
|
GSK805 is an orally active and CNS penetrant RORγt inhibitor. GSK805 inhibits RORγ and Th17 cells differentiation with pIC50 values of 8.4 and >8.2. GSK805 inhibits the function of Th17 cells. GSK805 can be used for the research of immunity .
|
-
-
- HY-10342
-
-
-
- HY-12768A
-
|
BLZ945 hydrochloride
|
c-Fms
|
Cancer
|
|
Sotuletinib (BLZ945) hydrochloride is a potent, selective, orally active and brain-penetrant CSF-1R (c-Fms) inhibitor with an IC50 of 1 nM, showing more than 1,000-fold selectivity against its closest receptor tyrosine kinase homologs. Sotuletinib hydrochloride can be used for microglia depletion, and for tumor and CNS-related disease research. .
|
-
-
- HY-125021
-
2BAct
3 Publications Verification
|
Eukaryotic Initiation Factor (eIF)
|
Neurological Disease
|
|
2BAct is a highly selective, orally active, and CNS-penetrant eIF2B (eukaryotic initiation factor 2B) activator with an EC50 of 33 nM. 2BAct prevents neurological defects caused by a chronic integrated stress response. 2BAct displays improved solubility and pharmacokinetics relative to eIF2B activator ISRIB trans-isomer (HY-12495) .
|
-
-
- HY-17419
-
-
-
- HY-126358
-
|
|
Endogenous Metabolite
Mitochondrial Metabolism
|
Neurological Disease
Metabolic Disease
Cancer
|
|
Acetylcarnitine is a CNS-penetrant endogenous metabolite. Acetylcarnitine shuttling links mitochondrial metabolism to histone acetylation and lipogenesis. Acetylcarnitine attenuates oxidative stress and neuroinflammation. Acetylcarnitine can be used for fatigue-associated diseases research. Acetylcarnitine can be used as a candidate diagnostic and prognostic biomarker of hepatocellular carcinoma .
|
-
-
- HY-P10136
-
IA9
2 Publications Verification
human TREM-2 182-190
|
TREM receptor
|
Inflammation/Immunology
|
|
IA9 (human TREM-2 182-190) is a potent, CNS-penetrant TREM-2 inhibitor. IA9 can diminish the release of proinflammatory cytokines and suppress joint inflammation and damage in a Collagen (HY-P5003)-induced arthritis (CIA) mouse model. IA9 can be used for neuroinflammation PET imaging. IA9 can be used for Rheumatoid arthritis (RA) and neuroinflammation research .
|
-
-
- HY-13781
-
-
-
- HY-16975
-
-
-
- HY-101116
-
|
|
GCGR
|
Metabolic Disease
|
|
GLP-1R Antagonist 1 (compound 5d) is an orally active, CNS penetrant and non-competitive antagonist of glucagon-like peptide 1 receptor (GLP-1R), with an IC50 of 650 nM .
|
-
-
- HY-139279
-
|
TPX-0131
|
Anaplastic lymphoma kinase (ALK)
|
Cancer
|
|
Zotizalkib (TPX-0131) is a potent, selective, CNS-penetrant and orally active inhibitor of wild-type ALK (IC50 of 1.4 nM) and ALK-resistant mutation, e.g. G1202R (IC50 of 0.3 nM), L1196M (IC50 of 0.3 nM). Zotizalkib has strong antitumor activities .
|
-
-
- HY-15164A
-
|
BPI-2009
|
EGFR
|
Infection
Neurological Disease
Metabolic Disease
Cancer
|
|
Icotinib (BPI-2009) is a potent, CNS-penetrant and specific EGFR inhibitor with an IC50 of 5 nM; also inhibits mutant EGFR L858R, EGFR L858R/T790M, EGFR T790M and EGFR L861Q. Icotinib is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
-
- HY-122138
-
|
|
mGluR
|
Neurological Disease
|
|
VU6010572 is a potent, selective and brain-penetrant mGlu3 negative allosteric modulator with IC50 of 245 nM. VU6010572 is highly CNS penetrant .
|
-
-
- HY-15722
-
-
-
- HY-13593
-
|
CB-1348; WR-139013
|
DNA Alkylator/Crosslinker
|
Neurological Disease
Cancer
|
|
Chlorambucil (CB-1348), an orally active antineoplastic agent, is a CNS-penetrant bifunctional alkylating agent belonging to the nitrogen mustard group. Chlorambucil can be used for the research of lymphocytic leukemia, ovarian and breast carcinomas, and Hodgkin’s disease .
|
-
-
- HY-120111
-
|
MW01-18-150SRM
|
p38 MAPK
Autophagy
|
Neurological Disease
Inflammation/Immunology
|
|
MW150 (MW01-18-150SRM) is a selective, CNS penetrant, and orally active inhibitor of p38α MAPK with a Ki of 101 nM. MW-150 inhibits the ability of the endogenous p38α MAPK to phosphorylate an endogenous substrate MK2 in activated glia .
|
-
-
- HY-B0335
-
|
GEA 6414
|
COX
|
Infection
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Tolfenamic Acid (GEA 6414) is a CNS-penetrant non-steroidal anti-inflammatory and anti-cancer agent, selectively inhibits COX-2, with an IC50 of 13.49 μM (3.53 μg/mL) in LPS-treated (COX-2) canine DH82 monocyte/macrophage cells, but shows no effect on COX-1.
|
-
-
- HY-149555
-
|
|
Eukaryotic Initiation Factor (eIF)
|
Neurological Disease
|
|
DNL343 is a potent, selective, orally active and brain-penetrant activator of eukaryotic initiation factor eIF2B. DNL343 inhibits the activity of the integrated stress response (ISR) in the central nervous system (CNS) and reverses neurodegeneration and neuroinflammation. DNL343 also prevents motor dysfunction and premature death in eIF2B loss-of-function (LOF) mutant mice. DNL343 can be used in the study of neurodegenerative diseases .
|
-
-
- HY-172429
-
|
ORIC-114
|
EGFR
|
Neurological Disease
Cancer
|
|
Enozertinib (ORIC-114) is an orally active, CNS-penetrant, highly selective and irreversible dual EGFR/HER2 inhibitor that exhibits potent and targeted inhibition of exon 20 insertion mutations. Enozertinib exhibits high kinome selectivity for the EGFR family of receptors to reduce off-target kinase liabilities. Enozertinib induces tumor regression and demonstrates antitumor activity in central nervous system and non-small cell lung cancer (NSCLC) tumor models. Enozertinib can be used for the research of solid tumors and NSCLC .
|
-
-
- HY-B1904
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
Fluphenazine decanoate is a CNS-penetrant dopamine D2 receptor inhibitor, is a long-acting phenothiazine neuroleptic. Fluphenazine can be used for schizophrenia research .
|
-
-
- HY-108710
-
|
|
mGluR
|
Neurological Disease
|
|
VU0650786 is a potent and selective CNS penetrant negative allosteric modulator of metabotropic glutamate receptor subtype 3 (mGlu3 NAM), with an IC50 of 392 nM. VU0650786 has antidepressant and anxiolytic activity in rodents .
|
-
-
- HY-15180
-
-
-
- HY-15164
-
|
BPI-2009H
|
EGFR
|
Infection
Neurological Disease
Metabolic Disease
Cancer
|
|
Icotinib Hydrochloride (BPI-2009) is a potent, CNS-penetrant and specific EGFR inhibitor with an IC50 of 5 nM; also inhibits mutant EGFR L858R, EGFR L858R/T790M, EGFR T790M and EGFR L861Q. Icotinib (Hydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
-
- HY-119939
-
|
CHDI00390576
|
HDAC
|
Cancer
|
|
CHDI-390576, a potent, cell permeable and CNS penetrant class IIa histone deacetylase (HDAC) inhibitor with IC50s of 54 nM, 60 nM, 31 nM, 50 nM for class IIa HDAC4, HDAC5, HDAC7, HDAC9, respectively, shows >500-fold selectivity over class I HDACs (1, 2, 3) and ~150-fold selectivity over HDAC8 and the class IIb HDAC6 isoform .
|
-
-
- HY-156585
-
-
-
- HY-160207
-
-
-
- HY-119943
-
|
|
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-152107
-
|
|
LRRK2
|
Neurological Disease
|
|
LRRK2-IN-7 is a potent, selective, and CNS-penetrant LRRK2 kinase inhibitor with an IC50 of 0.9 nM. LRRK2-IN-7 shows >1000-fold selectivity over other kinases, ion channels, and CYP enzymes .
|
-
-
- HY-122635A
-
|
|
Histone Demethylase
|
Neurological Disease
|
|
T-448 is a specific, orally active, CNS-penetrant and irreversible inhibitor of lysine-specific demethylase 1 (LSD1, an H3K4 demethylase), with an IC50 of 22 nM. T-448 enhances H3K4 methylation in primary cultured rat neurons .
|
-
-
- HY-P10136A
-
IA9 TFA
2 Publications Verification
human TREM-2 182-190 TFA
|
TREM receptor
|
Inflammation/Immunology
|
|
IA9 TFA (human TREM-2 182-190 TFA) is a potent, CNS-penetrant TREM-2 inhibitor. IA9 TFA can diminish the release of proinflammatory cytokines and suppress joint inflammation and damage in a Collagen (HY-P5003)-induced arthritis (CIA) mouse model. IA9 TFA can be used for neuroinflammation PET imaging. IA9 TFA can be used for Rheumatoid arthritis (RA) and neuroinflammation research .
|
-
-
- HY-172429A
-
|
ORIC-114 hemihydrate
|
EGFR
|
Neurological Disease
Cancer
|
|
Enozertinib (ORIC-114) hemihydrate is an orally active, CNS-penetrant, highly selective and irreversible dual EGFR/HER2 inhibitor that exhibits potent and targeted inhibition of exon 20 insertion mutations. Enozertinib hemihydrate exhibits high kinome selectivity for the EGFR family of receptors to reduce off-target kinase liabilities. Enozertinib hemihydrate induces tumor regression and demonstrates antitumor activity in central nervous system and non-small cell lung cancer (NSCLC) tumor models. Enozertinib hemihydrate can be used for the research of solid tumors and NSCLC .
|
-
-
- HY-133554
-
-
-
- HY-P0201A
-
-
-
- HY-144372
-
|
|
TRP Channel
|
Neurological Disease
|
|
TRPV1 antagonist 3 (Compound 7q) is a potent TRPV1 antagonist with an IC50 of 2.66 nM against capsaicin. TRPV1 antagonist 3 is mode-selective, oral bioavailable (F = 60%) and CNS-penetrant .
|
-
-
- HY-150640
-
-
-
- HY-14418
-
|
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-128772
-
|
|
Sodium Channel
|
Neurological Disease
|
|
XPC-6444 is a highly potent, isoform-selective, and CNS-penetrant NaV1.6 inhibitor (IC50=41 nM for hNaV1.6). XPC-6444 also displays potent block of NaV1.2 (IC50=125 nM). XPC-6444 shows anticonvulsant activity .
|
-
-
- HY-19630
-
|
VU0463597
|
mGluR
|
Neurological Disease
|
|
ML289 (VU0463597) is a potent, selective, and CNS-penetrant mGlu3 (IC50=0.66 μM) negative allosteric modulator. ML289 displays >15-fold selectivity over mGlu2 and is inactive against mGlu5 . ML289 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
-
- HY-125339
-
|
|
COMT
Apoptosis
|
Neurological Disease
Cancer
|
|
Ro 41-0960 is a CNS-penetrant, orally active catechol-O-methyl transferase (COMT) inhibitor. Ro 41-0960 reduces dopamine catabolism, increases striatal dopamine and DOPAC levels, decreases striatal HVA levels, induces apoptosis, inhibits proliferation and extracellular matrix formation in uterine fibroid cells. Ro 41-0960 arrests or shrinks uterine fibroid lesions in rats. Ro 41-0960 can be used for the research of Parkinson’s disease, uterine leiomyomas, and breast cancer .
|
-
-
- HY-114403
-
|
|
mGluR
|
Neurological Disease
|
|
VU6012962 is an orally bioavailable and CNS-penetrant metabotropic glutamate receptor 7 negative allosteric modulator (mGlu7 NAM) with an IC50 of 347 nM .
|
-
-
- HY-132981
-
|
|
P2X Receptor
|
Neurological Disease
|
|
Lu AF27139 is a potent, selective, and orally active antagonist of P2X7 receptor (IC50s of 12 and 2.4 nM for human and rat, Kis of 22, 54, and 13 nM for mouse, human, and rat, respectively). Lu AF27139 has rodent-active and CNS-penetrant character. Lu AF27139 has the potential for the research of CNS diseases .
|
-
-
- HY-113616A
-
|
|
MARCKS
mAChR
|
Neurological Disease
|
|
VU0364572 TFA is an orally active and selective allosteric agonist of the M1 muscarinic receptor with an EC50 of 0.11 μM. VU0364572 TFA has neuroprotective potential for preventing memory impairments and reducing neuropathology in Alzheimer’s Disease. VU0364572 TFA is CNS penetrant .
|
-
- HY-144604
-
|
|
Formyl Peptide Receptor (FPR)
|
Infection
Neurological Disease
|
|
FPR2 agonist 2 is a potent and CNS-penetrant FPR2 agonist with an EC50 of 0.13 μM, 1.1 μM for FPR2 and FPR1, respectively. FPR2 agonist 2 inhibits the production of pro-inflammatory cytokines, counterbalances the changes in mitochondrial function, and inhibits caspase-3 activity .
|
-
- HY-148624
-
|
|
HDAC
|
Neurological Disease
|
|
CHDI-00484077 (Compound 12) is a CNS-penetrant class IIa HDAC inhibitor, with IC50s of 0.01 μM (HDAC4), 0.02 μM(HDAC5), 0.02 μM (HDAC7), 0.03 μM (HDAC9) respectively. CHDI-00484077 can be used for research of huntington’s disease .
|
-
- HY-179004
-
|
VU6022856
|
Potassium Channel
|
Neurological Disease
|
|
ONO-9517601 is a potent, orally active, selective and CNS
penetrant dual TREK-1/TREK-2 inhibitor (TREK-1 IC50= 0.067 μM, TREK-2 IC50= 0.23 μM). ONO-9517601 displays robust efficacy in an
MK-801 (HY-15084B) challenge rat novel object recognition (NOR) paradigm.
ONO-9517601 can be used for research on neurological and cognitive
disorders .
|
-
- HY-B1904A
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
Fluphenazine decanoate dihydrochloride is a CNS-penetrant dopamine D2 receptor inhibitor, is a long-acting phenothiazine neuroleptic. Fluphenazine can be used for schizophrenia research .
|
-
- HY-120004
-
|
|
mAChR
|
Infection
|
|
PF-06827443 is a potent, low-clearance, orally bioavailable, and CNS-penetrant M1-selective positive allosteric modulator (PAM) with minimal agonist activity. PF-06827443 induce cholinergic AEs and convulsion .
|
-
- HY-128879
-
|
|
Phosphodiesterase (PDE)
GSK-3
|
Neurological Disease
|
|
VP3.15 is a potent, orally bioavailable and CNS-penetrant dual phosphodiesterase (PDE)7- glycogen synthase kinase (GSK)3 inhibitor, with IC50s of 1.59 μM and 0.88 μM for PDE7 and GSK-3, respectively. VP3.15 has neuroprotective and neuroreparative activities, thus as potential combined anti-inflammatory and pro-remyelinating therapies for multiple sclerosis (MS) .
|
-
- HY-118098
-
-
- HY-179005
-
|
VU6024391
|
Potassium Channel
|
Neurological Disease
|
|
ONO-7927846 is a potent, orally active, selective and CNS penetrant dual TREK-1/TREK-2 inhibitor (TREK-1 IC50= 0.11 μM, TREK-2 IC50= 0.29 μM). ONO-7927846 displays robust efficacy in an MK-801 (HY-15084B) challenge rat novel object recognition (NOR) paradigm. ONO-7927846 can be used for research on neurological and cognitive disorders .
|
-
- HY-10869
-
|
|
FAAH
|
Metabolic Disease
|
|
OL-135 is a CNS penetrant, selective, and reversible of FAAH inhibitor. OL-135 exhibits analgesic activity .
|
-
- HY-137061
-
-
- HY-123481
-
|
|
P2X Receptor
|
Metabolic Disease
|
|
JNJ-42253432 is a CNS-penetrant, high-affinity and orally active P2X7 antagonist, with pKi values of 9.1 and 7.9 for rat and human P2X7 channels, respectively .
|
-
- HY-116819A
-
|
|
GCGR
|
Metabolic Disease
|
|
VU0453379 hydrochloride is a highly selective and central nervous system (CNS) penetrant positive allosteric modulator (PAM) of glucagon-like peptide-1R (GLP-1R) with an EC50 of 1.3 μM .
|
-
- HY-113616
-
|
|
mAChR
MARCKS
|
Neurological Disease
|
|
VU0364572 is a selective allosteric agonist of the M1 muscarinic receptor with an EC50 of 0.11 μM. VU0364572 has neuroprotective potential for preventing memory impairments and reducing neuropathology in Alzheimer’s Disease. VU0364572 is orally active and is CNS penetrant .
|
-
- HY-122647
-
|
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-107128
-
|
TD-9855 hydrochloride
|
Serotonin Transporter
|
Neurological Disease
|
|
Ampreloxetine (TD-9855) hydrochloride is an orally active and CNS-penetrant inhibitor of Norepinephrine transporter (NET) and Serotonin 5-HT uptake transporter (SERT), but not Dopamine transporter (DAT). Ampreloxetine hydrochloride binds norepinephrine transporters (NET) and serotonin transporters (SERT) with EC50 values of 11.7 ng/mL and 50.8 ng/mL, respectively, in plasma .
|
-
- HY-120111A
-
|
MW01-18-150SRM hydrochloride
|
p38 MAPK
Autophagy
|
Neurological Disease
Inflammation/Immunology
|
|
MW-150 hydrochloride (MW01-18-150SRM hydrochloride) is a selective, CNS penetrant, and orally active inhibitor of p38α MAPK with a Ki of 101 nM. MW-150 hydrochloride (MW01-18-150SRM hydrochloride) inhibits the ability of the endogenous p38α MAPK to phosphorylate an endogenous substrate MK2 in activated glia .
|
-
- HY-12768B
-
|
BLZ945 dihydrochloride
|
c-Fms
|
Neurological Disease
Cancer
|
|
Sotuletinib (BLZ945) dihydrochloride is a potent, selective, orally active and brain-penetrant CSF-1R (c-Fms) inhibitor with an IC50 of 1 nM, showing more than 1,000-fold selectivity against its closest receptor tyrosine kinase homologs. Sotuletinib dihydrochloride can be used for microglia depletion, and for tumor and CNS-related disease research .
|
-
- HY-152107A
-
|
|
LRRK2
|
Neurological Disease
|
|
(R,R)-LRRK2-IN-7 is the isomer of LRRK2-IN-7 (HY-152107). LRRK2-IN-7 is a potent, selective, and CNS-penetrant LRRK2 kinase inhibitor with an IC50 of 0.9 nM. LRRK2-IN-7 shows >1000-fold selectivity over other kinases, ion channels, and CYP enzymes.
|
-
- HY-144607
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Mu opioid receptor antagonist 2 (compound 25) is a potent, selective and blood-brain barrier (BBB) penetrant μ opioid receptor (MOR) antagonist with a Ki of 0.37 nM and an EC50 of 0.44 nM. Mu opioid receptor antagonist 2 has remarkable CNS antagonism against morphine, and precipitated fewer withdrawal symptoms than Naloxone. Mu opioid receptor antagonist 2 can be used for researching opioid use disorders (OUD) .
|
-
- HY-168997
-
|
|
Cannabinoid Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
CB1R agonist 1 is a potent, CNS-penetrant, and selective Cannabinoid-1 receptor (CB1R) agonist with a Ki of 0.95 nM, modulating Gi/o signaling. CB1R agonist 1 exhibits high selectivity over CB2R and other off-target GPCRs, including GPR55, GPR18, and GPR119. CB1R agonist 1 induces analgesia and hypothermia, and potentiates opioid analgesia in mice. CB1R agonist 1 can be used for the research of pain .
|
-
- HY-154958
-
|
|
mTOR
|
Neurological Disease
|
|
mTOR inhibitor-12 (Compound 11) is a selective brain penetrant mTOR inhibitor without genotoxicity risk. mTOR inhibitor-12 can be used for the research of CNS diseases .
|
-
- HY-168025
-
|
|
nAChR
|
Neurological Disease
|
|
VU6007496 is a highly selective and CNS penetrant M1 positive allosteric modulator (PAM). VU6007496 shows excellent pharmacokinetics (PK) .
|
-
- HY-115726A
-
|
|
γ-secretase
|
Neurological Disease
|
|
(-)-FRM-024 is the (-)-isomer of FRM-024, a potent CNS-penetrant gamma secretase modulator that can be utilized in Alzheimer’s disease research .
|
-
- HY-112286
-
|
|
PI3K
|
Inflammation/Immunology
|
|
PI3Kγ inhibitor 2 (Compound 16) is an orally bioavailable, CNS-penetrant, isoform selective PI3Kγ inhibitor with a Ki of 4 nM .
|
-
- HY-124382
-
|
|
TRP Channel
|
Neurological Disease
|
|
AS1928370 is a novel and central nervous system (CNS) penetrant TRPV1 antagonist and can prevent ligand-induced activation in vivo. AS1928370 is a promising agent for neuropathic pain research .
|
-
- HY-120796
-
|
MW01-11-108SRM hydrochloride
|
p38 MAPK
|
Neurological Disease
|
|
MW108 (MW01-11-108SRM) hydrochloride is a selective and CNS-penetrant p38αMAPK inhibitor with a Ki of 114 nM. MW108 hydrochloride ameliorates beta-amyloid induced synaptic and cognitive dysfunction .
|
-
- HY-121313
-
|
BAY 10-6734
|
Angiotensin Receptor
|
Neurological Disease
Endocrinology
|
|
Embusartan (BAY 10-6734) is a brain-penetrant and effective AT1 receptor blocker. Embusartan inhibits Ang II binding to brain AT1 receptors in the nuclei of central nervous system (CNS) inside due to high lipophilic character. Embusartan is promising for research of sympathetic hyperactivity and hypertension .
|
-
- HY-150503
-
|
|
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-168240
-
|
|
iGluR
|
Neurological Disease
|
|
NMDAR antagonist 2 (compound 3I) is a CNS penetrant NMDAR antagonist with the IC50 of 4.42 μM and 214.75 μM for hGluN1/hGluN2A at −60 mV or 40 mV membrane potentials, respectively. NMDAR antagonist 2 can reduce hippocampal damage .
|
-
- HY-167893
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
AGH-107 is a high selective and brain-penetrant agonist of 5-HT7 receptor, with a Ki of 6 nM and EC50 of 19 nM. AGH-107 exhibits high selectivity over related CNS targets, high metabolic stability and low toxicity in HEK-293 and HepG2 cell cultures .
|
-
- HY-122635
-
|
|
Histone Demethylase
|
Neurological Disease
|
|
T-448 free base is a specific, orally active, CNS-penetrant and irreversible inhibitor of lysine-specific demethylase 1 (LSD1, an H3K4 demethylase), with an IC50 of 22 nM. T-448 free base enhances H3K4 methylation in primary cultured rat neurons .
|
-
- HY-154957
-
|
|
mTOR
|
Neurological Disease
|
|
mTOR inhibitor-11 (Compound 9) is a brain-penetrant mTOR inhibitor (IC50: 21 nM for pS6). mTOR inhibitor-11 also inhibits pCHK1 and PDE4D with IC50s of 17.2 and 17.0 μM. mTOR inhibitor-11 can be used for research of CNS disease .
|
-
- HY-120111B
-
|
MW01-18-150SRM dihydrochloride dihydrate
|
p38 MAPK
Autophagy
|
Neurological Disease
Inflammation/Immunology
|
|
MW-150 dihydrochloride dihydrate (MW01-18-150SRM dihydrochloride dihydrate) is a selective, CNS penetrant, and orally active inhibitor of p38α MAPK with a Ki of 101 nM. MW-150 dihydrochloride dihydrate (MW01-18-150SRM dihydrochloride dihydrate) inhibits the ability of the endogenous p38α MAPK to phosphorylate an endogenous substrate MK2 in activated glia .
|
-
- HY-123934
-
|
|
P-glycoprotein
|
Neurological Disease
|
|
VU6007477 is a brain-penetrant, selective M1 positive allosteric modulator (PAM) with an EC50 value of 230 nM. VU6007477 is also a human P-glycoprotein (P-gp) substrate with moderate permeability. VU6007477 displays improved central nervous system (CNS) penetration over the hydroxylated congeners. VU6007477 a pyranyl amide derivative, which is promising for research of robust cholinergic seizure activity .
|
-
- HY-137055
-
|
|
Others
|
Others
|
|
PF-3774076 is a highly central nervous system (CNS) penetrant, potent, and selective human α1A-adrenoceptor partial agonist. It exhibits good potency and selectivity in multiple binding and functional assays. PF-3774076 increases peak urethral pressure in anesthetized female dogs in a dose-dependent manner via a central mechanism. PF-3774076 affects both the proximal and distal portions of the urethra in vivo. These properties suggest that PF-3774076 may have significant benefit in the treatment of stress urinary incontinence (SUI) as a CNS-penetrant α1A receptor partial agonist. However, despite its partial agonism and selectivity for α1A receptors, PF-3774076 failed to provide adequate safety differences in in vivo models of cardiovascular function. This may be due to the simultaneous activation of both peripheral and central α1A receptors. These data suggest that while central α1A partial agonists may have significant benefit in the treatment of SUI, this class of agents may have difficulty achieving the desired urethral selectivity without affecting cardiovascular function.
|
-
- HY-164504
-
|
|
MMP
|
Neurological Disease
|
|
NRMA-10, an amide prodrug, is a brain-penetrant nuclear receptor modulator. NRMA-10 increases brain expression of Adam10. NRMA-10 preferres distribution to the CNS compared to the periphery. NRMA-10 can be used for the study of central nervous system (CNS) disorders .
|
-
- HY-180421
-
|
|
mAChR
|
Neurological Disease
|
|
VU6009048 is a CNS-penetrant human M4 muscarinic acetylcholine receptor (mAChR4) positive allosteric modulator. VU6009048 can be used for the research of parkinson’s disease, huntington’s disease, schizophrenia .
|
-
- HY-122561
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
MK-1925 is an orally active, CNS-penetrant ORL1 receptor antagonist with an IC50 of 8.2 nM. MK-1925 selectively inhibits the ORL1 receptor and shows no significant activity against other opioid receptors or the hERG potassium channel .
|
-
- HY-105704
-
|
NSC 170955; WA 335
|
5-HT Receptor
|
Neurological Disease
|
|
Danitracen (NSC 170955) is an orally active, CNS penetrant serotonin antagonist with antidepressant activity. Danitracen reduces serotonin levels in the cerebrum, cerebellum, medulla and the whole brain. Danitracen exhibits anticataleptic effects in rat catalepsy models. Danitracen can be used for catalepsy and depression research .
|
-
- HY-183269
-
|
|
Serotonin Transporter
|
Neurological Disease
|
|
SERT-IN-5 is a potent, selective, and CNS-penetrant serotonin transporter (SERT) inhibitor with a Ki of 0.3 nM. SERT-IN-5 blocks serotonin reuptake to increase synaptic serotonin levels. SERT-IN-5 exhibits anti-anxiety effects in mice. SERT-IN-5 can be used for the research of anxiety, depression .
|
-
- HY-108710R
-
|
|
Reference Standards
mGluR
|
Neurological Disease
|
|
VU0650786 (Standard) is the analytical standard of VU0650786 (HY-108710). This product is intended for research and analytical applications. VU0650786 is a potent and selective CNS penetrant negative allosteric modulator of metabotropic glutamate receptor subtype 3 (mGlu3 NAM), with an IC50 of 392 nM. VU0650786 has antidepressant and anxiolytic activity in rodents .
|
-
- HY-N2332
-
|
MLA
|
nAChR
|
Neurological Disease
|
|
Methyllycaconitine (MLA) is a potent, selective, CNS-penetrant, competitive α7nAChR antagonist. Methyllycaconitine alleviates amyloid-β peptides-induced cytotoxicity in SH-SY5Y cells. Methyllycaconitine prevents methamphetamine-induced effects in mouse striatum. Methyllycaconitine can be used for neurological disease research, such as Alzheimer’s disease .
|
-
- HY-123778
-
|
|
mAChR
|
Neurological Disease
|
|
VU6007678 is a CNS-penetrant muscarinic acetylcholine receptor (mAChR) modulator. VU6007678 potentiates acetylcholine-mediated signaling at human M1, M3, M5 and rat M1, M3, M4, M5 muscarinic acetylcholine receptors. VU6007678 is applicable to research related to Alzheimer's disease, schizophrenia, and ischemic stroke .
|
-
- HY-176995
-
|
|
GHSR
|
Metabolic Disease
|
|
AZ-GHS-38 (compound 38) is an orally active CNS-penetrant inverse agonist of growth hormone secretagogue receptor (GHS-R1a) with an IC50 of 6.7 nM. AZ-GHS-38 results in acute reduction of food intake in wild-type mice. AZ-GHS-38 can be used for anti-obesity research .
|
-
- HY-153922
-
|
|
Glycosidase
|
Neurological Disease
|
|
N-Octyl-α-4-epivalienamine is an orally active and CNS-penetrant molecular chaperone that induces high expression of the deficient β-galactosidase activity. N-Octyl-α-4-epivalienamine ameliorates symptoms and increase survival rate in a mouse model of GM1-gangliosidosis. N-Octyl-α-4-epivalienamine can be used for neurogenetic disease research .
|
-
- HY-182943
-
|
|
Btk
Fc Receptor (FcR)
|
Neurological Disease
Inflammation/Immunology
|
|
BTK-IN-49 is a selective, orally active and brain-penetrant BTK inhibitor with an IC50 of 0.14 nM. BTK-IN-49 binds to BTK and blocks B-cell receptor and Fcγ receptor signaling. BTK-IN-49 inhibits the proliferation of CNS-compartmentalized B-cells and FcγR-induced microglial proliferation in a BTK-dependent manner. BTK-IN-49 can be used for the study of multiple sclerosis .
|
-
- HY-101116R
-
|
|
GCGR
Reference Standards
|
Metabolic Disease
|
|
GLP-1R Antagonist 1 (Standard) is the analytical standard of GLP-1R Antagonist 1 (HY-101116). This product is intended for research and analytical applications. GLP-1R Antagonist 1 (compound 5d) is an orally active, CNS penetrant and non-competitive antagonist of glucagon-like peptide 1 receptor (GLP-1R), with an IC50 of 650 nM .
|
-
- HY-107128R
-
|
TD-9855 hydrochloride (Standard)
|
Reference Standards
Serotonin Transporter
|
Neurological Disease
|
|
Ampreloxetine hydrochloride (Standard) (TD-9855 hydrochloride (Standard)) is the analytical standard of Ampreloxetine (hydrochloride) (HY-107128). This product is intended for research and analytical applications. Ampreloxetine (TD-9855) hydrochloride is an orally active and CNS-penetrant inhibitor of Norepinephrine transporter (NET) and Serotonin 5-HT uptake transporter (SERT), but not Dopamine transporter (DAT). Ampreloxetine hydrochloride binds norepinephrine transporters (NET) and serotonin transporters (SERT) with EC50 values of 11.7 ng/mL and 50.8 ng/mL, respectively, in plasma .
|
-
- HY-13902A
-
|
VE-822 hydrochloride; VX-970 hydrochloride; M6620 hydrochloride
|
ATM/ATR
Apoptosis
STING
Caspase
|
Neurological Disease
Cancer
|
|
Berzosertib (VE-822) hydrochloride is an orally active, CNS-penetrant, and selective ATR kinase inhibitor. Berzosertib hydrochloride blocks ATR kinase activity, abrogates G2/M cell cycle checkpoint, impairs DNA damage repair. Berzosertib hydrochloride induces apoptosis, inhibnits conlony migration, inhibits cell proliferation, and activates cGAS-STING axes in cancer cells. Berzosertib hydrochloride can be used for the research of cancers, such as head and neck squamous cell carcinoma, and colorectal cancer .
|
-
- HY-180807
-
|
|
p38 MAPK
Reactive Oxygen Species (ROS)
Mitochondrial Metabolism
ERK
JNK
|
Cardiovascular Disease
Neurological Disease
|
|
MAPK-IN-6 (compound 116B) is a CNS-penetrant compound that inhibits the MAPK signaling pathway. MAPK-IN-6 reduces oxidative stress in SH-SY5Y neuronal cells by reducing ROS, restoring mitochondrial function, and inhibiting MAPK-driven inflammation. MAPK-IN-6 demonstrates profound neuroprotective efficacy in a rat tBCCAO/R model via ERK-P38-JNK signaling. MAPK-IN-6 can be used as a neuroprotective agent in ischemic stroke research .
|
-
- HY-109061R
-
|
YH25448 (Standard); GNS-1480 (Standard)
|
Apoptosis
Akt
TRP Channel
EGFR
ERK
Reference Standards
|
Infection
Neurological Disease
Metabolic Disease
Cancer
|
|
Lazertinib (Standard) is the analytical standard of Lazertinib (HY-109061). This product is intended for research and analytical applications. Lazertinib (YH25448) is a potent, selective, CNS-penetrant, orally available and irreversible EGFR tyrosine Kinase inhibitor, exhibiting high selectivity for activating (EGFRm) and T790M resistance mutations. Lazertinib inhibits phosphorylation of EGFR, AKT and ERK, leading to apoptosis and suppression of tumor growth in mouse H1975-luc brain metastasis xenograft models. Lazertinib can be used in the study of non-small cell lung cancer .
|
-
- HY-135629
-
|
|
Casein Kinase
|
Neurological Disease
|
|
PF-5236216 is a brain-penetrant CK1δ/CK1ε inhibitor with IC50 values of 8 and 36 nM. PF-5236216 inhibits CK1δ and CK1ε-mediated PER3 nuclear translocation. PF-5236216 forms an H-bond with the backbone NH of Leu85, hydrophobic stacking with Met82, and a water-mediated H-bond with Lys38 of CK1δ. PF-5236216 can be used as a tool ligand for CNS PET studies .
|
-
- HY-109061BR
-
|
YH25448 mesylate (Standard); GNS-1480 mesylate (Standard)
|
Reference Standards
|
Cancer
|
|
Lazertinib mesylate (Standard) is the analytical standard of Lazertinib (mesylate) (HY-109061B). This product is intended for research and analytical applications. Lazertinib (YH25448) mesylate is a potent, selective, CNS-penetrant, orally available and irreversible EGFR tyrosine Kinase inhibitor, exhibiting high selectivity for activating (EGFRm) and T790M resistance mutations. Lazertinib mesylate inhibits phosphorylation of EGFR, AKT and ERK, leading to apoptosis and suppression of tumor growth in mouse H1975-luc brain metastasis xenograft models. Lazertinib mesylate can be used in the study of non-small cell lung cancer .
|
-
- HY-172182
-
|
VU6011887
|
Potassium Channel
|
Neurological Disease
|
|
ONO-2920632 is an orally active and central nervous system (CNS)-penetrant TREK activator, with EC50 values of 0.3 µM and 2.8 μM for TREK-1 and TREK-2, respectively. ONO-2920632 exhibits selectivity for other K2P channels (>91-fold selective versus TASK1, TASK2, TASK3, TRAAK, and TWIK2; 31-fold selective versus TRESK). ONO-2920632 possesses analgesic effects and can be used in research on pain, migraine, and neurological disorders.
|
-
- HY-156438
-
|
NT-0796
|
NOD-like Receptor (NLR)
Interleukin Related
|
Neurological Disease
|
|
Ruvonoflast (NT-0796) is an orally active, selective and CNS-penetrant NLRP3 inflammasome inhibitor. Ruvonoflast inhibits IL-1β release in human PBMC cells with an IC50 value of 0.32 nM. Ruvonoflast is an isopropyl ester that undergoes intracellular conversion to Ruvonoflast, the carboxylic acid active species. Ruvonoflast reverses high fat diet-induced obesity, systemic inflammation and astrogliosis in the diet-induced obesity mouse model. Ruvonoflast is promising for research of neurodegenerative disorders, including Alzheimer’s disease, Parkinson’s disease, multiple sclerosis, and amyotrophic lateral sclerosis .
|
-
- HY-176942
-
|
ROS1-IN-3
|
ROS Kinase
Trk Receptor
|
Cancer
|
|
YP0322 (ROS1-IN-3) is a potent orally active, selective, and CNS-penetrant ROS1 inhibitor. JYP0322 selectively inhibits human wild-type ROS1 and human ROS1 G2032R with IC50s of 0.37 and 0.3 nM, respectively, showing 6-130-fold selectivity over TRKA, TRKB, and TRKC. JYP0322 inhibits proliferation of ROS1 fusion-expressing cells, and inhibits tumor growth in mouse xenograft models. JYP0322 can be used for the research of non-small cell lung cancer (NSCLC) .
|
-
- HY-16561
-
-
- HY-103586
-
|
|
DNA/RNA Synthesis
SARS-CoV
|
Infection
|
|
GS-441524 is a potent, orally active and CNS-penetrant viral RNA-dependent RNA polymerase inhibitor. GS-441524 competes with natural nucleosides to block viral RNA transcription as an alternative substrate and RNA chain terminator. GS-441524 inhibits the replication of feline infectious peritonitis virus, African swine fever virus, and severe acute respiratory syndrome coronavirus 2. GS-441524 reduces viral RNA levels in cats. GS-441524 can be used in research related to feline infectious peritonitis, African swine fever, and coronavirus disease 2019 (COVID-19) .
|
-
- HY-103586A
-
|
|
DNA/RNA Synthesis
SARS-CoV
|
Infection
|
|
GS-441524 hydrochloride is a potent, orally active and CNS-penetrant viral RNA-dependent RNA polymerase inhibitor. GS-441524 hydrochloride competes with natural nucleosides to block viral RNA transcription as an alternative substrate and RNA chain terminator. GS-441524 hydrochloride inhibits the replication of feline infectious peritonitis virus, African swine fever virus, and severe acute respiratory syndrome coronavirus 2. GS-441524 hydrochloride reduces viral RNA levels in cats. GS-441524 hydrochloride can be used in research related to feline infectious peritonitis, African swine fever, and coronavirus disease 2019 (COVID-19) .
|
-
- HY-N17383
-
|
|
Toll-like Receptor (TLR)
NF-κB
Collagen
Interleukin Related
Cadherin
NOD-like Receptor (NLR)
TGF-β Receptor
FXR
Apoptosis
|
Metabolic Disease
Inflammation/Immunology
|
|
Ligusticum cycloprolactam is a potent, orally active, and CNS-penetrant TLR4/NF-κB inhibitor, exhibiting anti-inflammatory and neuroprotective activity. Ligusticum cycloprolactam reduces FPR1 expression, inhibits NLRP3 inflammasome, TLR4/NF-κB, hepatic MAPK and TGF-β signaling, and selectively activates hepatic FXR. Ligusticum cycloprolactam attenuates pro-inflammatory mediator production, enhances anti-inflammatory cytokine secretion, regulates renal uric acid transporters, and preserves intestinal microbiota composition. Ligusticum cycloprolactam can be used for the research of ischemic stroke, hyperuricemic nephropathy, neuroinflammation, and metabolic dysfunction-associated fatty liver disease .
|
-
- HY-159838
-
|
EI‐1071
|
c-Fms
Amyloid-β
|
Neurological Disease
Cancer
|
|
Enrupatinib (EI‐1071) is a potent, orally active, CNS-penetrant and selective CSF1R inhibitor. Enrupatinib inhibits macrophage proliferation and osteoclast differentiation in vitro. Enrupatinib preserves microglia distal to Aβ plaques. Enrupatinib mitigates Alzheimer's disease (AD)-related pathologies by reducing neuroinflammation, preserving neuronal integrity, lowering disease-associated microglia gene expression, and enhancing cognitive function in 5xFAD and J20 mouse models. Enrupatinib reduces tumor-associated macrophage infiltration and enhances antitumor activity of anti-PD-1 antibody in murine colorectal cancer and breast cancer models. Enrupatinib can be used for the research of AD, colorectal cancer, and breast cancer .
|
-
- HY-180400
-
|
|
nAChR
Calcium Channel
|
Neurological Disease
|
|
PAM-2 is a potent, orally active, CNS-penetrant selective α7 nAChR positive allosteric modulator (human α7 nAChR EC50: 39 μM, rat α7 nAChR EC50: 12 μM) with anti-nociceptive and anti-inflammatory activity. PAM-2 exhibits selectivity over α9α10 nAChR (IC50 = 174 μM) and CaV2.2 channel (IC50 = 89 μM). PAM-2 decreases Streptozotocin (STZ) (HY-13753)- and Oxaliplatin (HY-17371)-inducned nuroparhic pain in mice by α7 nAChR potentiation. PAM-2 can be used for the research of neuropathic pain .
|
-
- HY-103586R
-
|
|
Reference Standards
DNA/RNA Synthesis
SARS-CoV
|
Infection
|
|
GS-441524 (Standard) is the analytical standard of GS-441524 (HY-103586). GS-441524 is a potent, orally active and CNS-penetrant viral RNA-dependent RNA polymerase inhibitor. GS-441524 competes with natural nucleosides to block viral RNA transcription as an alternative substrate and RNA chain terminator. GS-441524 inhibits the replication of feline infectious peritonitis virus, African swine fever virus, and severe acute respiratory syndrome coronavirus 2. GS-441524 reduces viral RNA levels in cats. GS-441524 can be used in research related to feline infectious peritonitis, African swine fever, and coronavirus disease 2019 (COVID-19) .
|
-
- HY-103586S2
-
|
|
Isotope-Labeled Compounds
DNA/RNA Synthesis
SARS-CoV
|
Infection
|
|
GS-441524-d is the deuterium labeled GS-441524 (HY-103586). GS-441524 is a potent, orally active and CNS-penetrant viral RNA-dependent RNA polymerase inhibitor. GS-441524 competes with natural nucleosides to block viral RNA transcription as an alternative substrate and RNA chain terminator. GS-441524 inhibits the replication of feline infectious peritonitis virus, African swine fever virus, and severe acute respiratory syndrome coronavirus 2. GS-441524 reduces viral RNA levels in cats. GS-441524 can be used in research related to feline infectious peritonitis, African swine fever, and coronavirus disease 2019 (COVID-19) .
|
-
- HY-128879A
-
|
|
Phosphodiesterase (PDE)
GSK-3
Tau Protein
|
Cardiovascular Disease
Neurological Disease
Inflammation/Immunology
|
|
VP3.15 dihydrobromide is a highly potent, orally bioavailable, and CNS-penetrant PDE7-GSK3 dual inhibitor, with IC50 values of 1.59 μM and 0.88 μM against PDE7 and GSK3, respectively . VP3.15 dihydrobromide elevates intracellular cAMP levels, suppresses immune responses, enhances remyelination, limits excessive tau phosphorylation, and alleviates neuroinflammation and neuronal loss. VP3.15 dihydrobromide promotes oligodendrocyte precursor cell differentiation, improves in vivo remyelination, inhibits autoimmune encephalomyelitis, and mitigates germinal matrix-intraventricular hemorrhage-related brain injury, cerebral atrophy, ventricular enlargement, and cognitive impairment. VP3.15 dihydrobromide can be used in research related to multiple sclerosis and germinal matrix-intraventricular hemorrhage .
|
-
- HY-111573
-
|
C286
|
RAR/RXR
|
Others
Neurological Disease
Inflammation/Immunology
|
|
KCL-286 (C286) is an orally active and brain-penetrant retinoic acid receptor (RAR) β2 agonist (EC50 = 1.9 nM). KCL-286 targets RARβ2 with good selectivity over RAR α (EC50 = 26 nM) and RAR γ (EC50 = 11 nM). KCL-286 activates RARβ2 in the injured neurons. KCL-286 induces axonal regeneration of both spinal and sensory nerves through the inhibitory environment of the CNS, modulates neuroinflammation and extracellular matrix molecules. KCL-286 can modulate the expression of CSPGs by neuronal secretion of decorin which promotes myelination and aids axonal growth. KCL-286 can be studied in research for area such as spinal cord injury and traumatic nerve injury .
|
-
-
-
HY-L028
-
|
|
1,096 compounds
|
|
The blood-brain barrier (BBB) is the complex network of brain microvessels. It protects the brain from the external bloodstream environment and supplies the brain with the required nutrients for normal function. However, blood-brain barrier is also the obstacle to deliver beneficial drugs to treat CNS (central nervous system) diseases or brain tumors, as it has the least permeable capillaries in the entire body due to physical barriers (tight junctions). Therefore, it is crucial to discover drugs which can cross this barrier for the treatment of brain-based diseases, such as Alzheimer’s disease (AD), Parkinson’s disease (PD) and epilepsy.
MCE offers a unique collection of 1,096 compounds with confirmed CNS-Penetrant property. It’s a useful tool for the discovery of drugs used for brain diseases, such as brain tumors, mental disorders, and neurodegenerative diseases.
|
-
-
HY-L093
-
|
|
454 compounds
|
|
Food additives are substances added to food to maintain or improve its safety, freshness, taste, texture, or appearance. All food additives used in food undergo a safety assessment, which includes rigorous testing, before they are approved, so all food additives are generally recognized as safe substances.
MCE supplies 454 approved food additives which are safe substances and can be used for drug discovery and other research.
|
-
-
HY-L061
-
|
|
5,259 compounds
|
|
Most of the drugs that are available in the marketplace are administered via the oral route, which is a convenient and cost effective route of administration. Thus, oral bioavailability is one of the key considerations in drug design and development. A high oral bioavailability reduces the amount of an administered drug necessary to achieve a desired pharmacological effect and therefore could reduce the risk of side-effects and toxicity. A poor oral bioavailability can result in low efficacy and higher inter-individual variability and therefore can lead to unpredictable response to a drug. Low oral bioavailability in clinical trials is a major reason for drug candidates failing to reach the market.
MCE offers a unique collection of 5,259 compounds with confirmed high oral bioavailability. MCE Orally Active Compound Library is a useful tool for discovering new drugs with oral bioavailability.
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P0201
-
-
- HY-P10136
-
IA9
2 Publications Verification
human TREM-2 182-190
|
TREM receptor
|
Inflammation/Immunology
|
|
IA9 (human TREM-2 182-190) is a potent, CNS-penetrant TREM-2 inhibitor. IA9 can diminish the release of proinflammatory cytokines and suppress joint inflammation and damage in a Collagen (HY-P5003)-induced arthritis (CIA) mouse model. IA9 can be used for neuroinflammation PET imaging. IA9 can be used for Rheumatoid arthritis (RA) and neuroinflammation research .
|
-
- HY-P10136A
-
IA9 TFA
2 Publications Verification
human TREM-2 182-190 TFA
|
TREM receptor
|
Inflammation/Immunology
|
|
IA9 TFA (human TREM-2 182-190 TFA) is a potent, CNS-penetrant TREM-2 inhibitor. IA9 TFA can diminish the release of proinflammatory cytokines and suppress joint inflammation and damage in a Collagen (HY-P5003)-induced arthritis (CIA) mouse model. IA9 TFA can be used for neuroinflammation PET imaging. IA9 TFA can be used for Rheumatoid arthritis (RA) and neuroinflammation research .
|
-
- HY-P0201A
-
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-16561
-
-
-
- HY-P0201
-
-
-
- HY-126358
-
-
-
- HY-N2332
-
-
-
- HY-N17383
-
|
|
Structural Classification
Natural Products
Umbelliferae
Plants
Echinacea angustifolia DC.
Source Classification
|
Toll-like Receptor (TLR)
NF-κB
Collagen
Interleukin Related
Cadherin
NOD-like Receptor (NLR)
TGF-β Receptor
FXR
Apoptosis
|
|
Ligusticum cycloprolactam is a potent, orally active, and CNS-penetrant TLR4/NF-κB inhibitor, exhibiting anti-inflammatory and neuroprotective activity. Ligusticum cycloprolactam reduces FPR1 expression, inhibits NLRP3 inflammasome, TLR4/NF-κB, hepatic MAPK and TGF-β signaling, and selectively activates hepatic FXR. Ligusticum cycloprolactam attenuates pro-inflammatory mediator production, enhances anti-inflammatory cytokine secretion, regulates renal uric acid transporters, and preserves intestinal microbiota composition. Ligusticum cycloprolactam can be used for the research of ischemic stroke, hyperuricemic nephropathy, neuroinflammation, and metabolic dysfunction-associated fatty liver disease .
|
-
| Cat. No. |
Product Name |
Chemical Structure |
-
- HY-103586S2
-
|
|
|
GS-441524-d is the deuterium labeled GS-441524 (HY-103586). GS-441524 is a potent, orally active and CNS-penetrant viral RNA-dependent RNA polymerase inhibitor. GS-441524 competes with natural nucleosides to block viral RNA transcription as an alternative substrate and RNA chain terminator. GS-441524 inhibits the replication of feline infectious peritonitis virus, African swine fever virus, and severe acute respiratory syndrome coronavirus 2. GS-441524 reduces viral RNA levels in cats. GS-441524 can be used in research related to feline infectious peritonitis, African swine fever, and coronavirus disease 2019 (COVID-19) .
|
-
| Cat. No. |
Product Name |
|
Classification |
-
- HY-15164A
-
|
BPI-2009
|
|
Alkynes
|
|
Icotinib (BPI-2009) is a potent, CNS-penetrant and specific EGFR inhibitor with an IC50 of 5 nM; also inhibits mutant EGFR L858R, EGFR L858R/T790M, EGFR T790M and EGFR L861Q. Icotinib is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-15164
-
|
BPI-2009H
|
|
Alkynes
|
|
Icotinib Hydrochloride (BPI-2009) is a potent, CNS-penetrant and specific EGFR inhibitor with an IC50 of 5 nM; also inhibits mutant EGFR L858R, EGFR L858R/T790M, EGFR T790M and EGFR L861Q. Icotinib (Hydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
Your information is safe with us. * Required Fields.
Inquiry Information
- Product Name:
- Cat. No.:
- Quantity:
- MCE Japan Authorized Agent: