Search Result

Results for "

centrally penetrant

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (1) Apoptosis (2) Btk (1) CXCR (1) DYRK (1) EGFR (2) GABA Receptor (1) GCGR (2) GHSR (3) GlyT (1) iGluR (1) mAChR (1) mGluR (1) Neurokinin Receptor (1) Neuropeptide Y Receptor (1) Opioid Receptor (1) Potassium Channel (1) ROCK (1) Somatostatin Receptor (2) TRP Channel (1)
By Research Areas:	Cancer (3) Endocrinology (2) Inflammation/Immunology (1) Metabolic Disease (5) Neurological Disease (15)

Inhibitors & Agonists

Screening Libraries

Peptides

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-15722

SB-222200 2 Publications Verification	Neurokinin Receptor	Neurological Disease Endocrinology
SB-222200 is a potent, selective, orally active and blood-brain barrier (BBB) penetrant NK-3 receptor antagonist. SB-222200 is developed for central nervous system (CNS) disorders .

HY-132308

DYRK1-IN-1 1 Publications Verification	DYRK	Neurological Disease
DYRK1-IN-1 is a highly selective and ligand-efficient DYRK1A inhibitor. DYRK1-IN-1 inhibits DYRK1A phosphorylation activity with an IC₅₀ value of 220 nM. DYRK1-IN-1 can be used for the research of central nervous system penetrant DYRK1A chemical probe .

HY-103530

CGP35348	GABA Receptor	Neurological Disease
CGP 35348 is a selective, brain penetrant, centrally active GABAB receptor antagonist with an EC₅₀ of 34 μM. CGP 35348 shows affinity for the GABAB receptor only . CGP 35348 has a potential to improve neuromuscular coordination and spatial learning in albino mouse following neonatal brain damage .

HY-19884

Relamorelin RM-131; BIM-28131	GHSR	Metabolic Disease
Relamorelin (RM-131), a pentapeptide ghrelin analog, is a selective ghrelin/growth hormone secretagogue receptor (GHSR) agonist with a K_i of 0.42 nM for GHS-1a receptor. Relamorelin is centrally penetrant. Relamorelin increases growth hormone levels and accelerates gastric emptying. Relamorelin has the potential for cachexia, gastroparesis, and gastric/intestinal dysmobility disorders research .

HY-19884A

Relamorelin acetate RM-131 acetate; BIM-28131 acetate	GHSR	Metabolic Disease
Relamorelin (RM-131) acetate, a pentapeptide ghrelin analog, is a selective ghrelin/growth hormone secretagogue receptor (GHSR) agonist with a K_i of 0.42 nM for GHS-1a receptor. Relamorelin acetate is centrally penetrant. Relamorelin acetate increases growth hormone levels and accelerates gastric emptying. Relamorelin acetate has the potential for cachexia, gastroparesis, and gastric/intestinal dysmobility disorders research .

HY-19884B

Relamorelin TFA RM-131 TFA; BIM-28131 TFA	GHSR	Metabolic Disease
Relamorelin (RM-131) TFA, a pentapeptide ghrelin analog, is a selective ghrelin/growth hormone secretagogue receptor (GHSR) agonist with a K_i of 0.42 nM for GHS-1a receptor. Relamorelin TFA is centrally penetrant. Relamorelin TFA increases growth hormone levels and accelerates gastric emptying. Relamorelin TFA has the potential for cachexia, gastroparesis, and gastric/intestinal dysmobility disorders research .

HY-101718

Aticaprant 4 Publications Verification CERC-501; LY-2456302	Opioid Receptor	Neurological Disease
Aticaprant (CERC-501) is a potent and centrally-penetrant kappa opioid receptor antagonist with a K_i of 0.807 nM.

HY-101022

CXCR2-IN-1

2 Publications Verification

CXCR Inflammation/Immunology Endocrinology

CXCR2-IN-1 is a central nervous system penetrant CXCR2 antagonist with a pIC₅₀ of 9.3.

CXCR2-IN-1 2 Publications Verification	CXCR	Inflammation/Immunology Endocrinology
CXCR2-IN-1 is a central nervous system penetrant CXCR2 antagonist with a pIC₅₀ of 9.3.

HY-17001

Flupirtine Maleate 1 Publications Verification	Potassium Channel iGluR	Neurological Disease
Flupirtine Maleate is a brain penetrant, and orally bioavailable, non-opioid and centrally acting analgesic agent. Flupirtine Maleate is an indirect N-methyl-D-aspartate receptor (NMDAR) antagonist. Neuroprotective properties .

HY-116524

PF-04781340	5-HT Receptor	Neurological Disease
PF-04781340 is a potent and selective 5-HT2C receptor agonist. PF-04781340 is orally available and have central nervous system penetrant profile .

HY-124382

AS1928370	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 treatment research .

HY-10716A

PF-03463275	GlyT	Neurological Disease
PF-03463275 is a centrally penetrant, orally available, selective, and competitive GlyT1 (glycine transporter-1) reversible inhibitor, with a K_i of 11.6 nM. PF-03463275 has the potential for Schizophrenia research .

HY-116819

VU0453379	GCGR	Metabolic Disease
VU0453379 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-116819A

VU0453379 hydrochloride	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-145778

AGI-41998	Somatostatin Receptor	Neurological Disease
AGI-41998 is a potent inhibitor of methionine adenosyltransferase 2A (MAT2A). AGI-41998 is a brain-penetrant compound. AGI-41998 has the potential for exploring the effects of SAM modulation in the central nervous system (CNS) and research of cancer disease .

HY-101839

ML381 VU0488130	mAChR	Neurological Disease
ML381 (VU0488130) is a highly selective, central nervous system penetrant mAChR M5 orthogonal antagonist (IC₅₀ = 450 nM; Ki = 340 nM). ML381 is unstable in rat plasma and can be mainly used as a molecular probe for in vitro and electrophysiological studies .

HY-145777

AGI-43192	Somatostatin Receptor	Neurological Disease Cancer
AGI-43192 is a potent inhibitor of methionine adenosyltransferase 2A (MAT2A). AGI-43192 is a potent, but limited brain-penetrant compound. AGI-43192 has the potential for exploring the effects of SAM modulation in the central nervous system (CNS) and research of cancer disease .

HY-150640

Rho-Kinase-IN-2	ROCK	Neurological Disease
Rho-Kinase-IN-2 (Compound 23) is an orally active, selective, and central nervous system (CNS)-penetrant Rho Kinase (ROCK) inhibitor (ROCK2 IC₅₀=3 nM). Rho-Kinase-IN-2 can be used in Huntington’s research .

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-107727

BMS-193885 L-Lactic acid	Neuropeptide Y Receptor	Neurological Disease
BMS-193885 (L-Lactic acid) is a potent, selective, and brain-penetrant neuropeptide Y1 receptor antagonist. BMS-193885 has a K_i value of 3.3 nM for the neuropeptide Y1 receptor, competitively acts on the neuropeptide Y binding site, and can reduce food intake and body weight through central Y1 inhibition .

HY-109192

Tolebrutinib 2 Publications Verification SAR442168; PRN2246	Btk	Neurological Disease
Tolebrutinib (SAR442168) is a potent, selective, orally active and brain-penetrant inhibitor of Bruton tyrosine kinase (BTK), with IC₅₀s of 0.4 and 0.7 nM in Ramos B cells and in HMC microglia cells, respectively. Tolebrutinib exhibits efficacy in central nervous system immunity. Tolebrutinib can be used for the research of multiple sclerosis (MS) .

HY-18750A

Zorifertinib hydrochloride AZD3759 hydrochloride	EGFR Apoptosis	Cancer
Zorifertinib (AZD3759) hydrochloride is a potent, orally active, central nervous system-penetrant, EGFR inhibitor (IC₅₀s: 0.3, 0.2, and 0.2 nM for EGFR ^wt, EGFR ^L858R, and EGFR ^{exon 19Del}, respectively). Zorifertinib hydrochloride induces cancer cell apoptosis. Zorifertinib hydrochloride has antitumor activity, and can be used for NSCLC, HCC etc. research .

HY-18750

Zorifertinib 5 Publications Verification AZD3759	EGFR Apoptosis	Cancer
Zorifertinib (AZD3759) is a potent, orally active, central nervous system-penetrant, EGFR inhibitor. At K_m ATP concentrations, the IC₅₀s are 0.3, 0.2, and 0.2 nM for EGFR ^wt, EGFR ^L858R, and EGFR ^{exon 19Del}, respectively. Zorifertinib induces cancer cell apoptosis. Zorifertinib has antitumor activity, and can be used for NSCLC, HCC etc. research .

CNS-Penetrant Compound Library	858 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 858 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.

Relamorelin TFA RM-131 TFA; BIM-28131 TFA	GHSR	Metabolic Disease
Relamorelin (RM-131) TFA, a pentapeptide ghrelin analog, is a selective ghrelin/growth hormone secretagogue receptor (GHSR) agonist with a K_i of 0.42 nM for GHS-1a receptor. Relamorelin TFA is centrally penetrant. Relamorelin TFA increases growth hormone levels and accelerates gastric emptying. Relamorelin TFA has the potential for cachexia, gastroparesis, and gastric/intestinal dysmobility disorders research .

Relamorelin RM-131; BIM-28131	GHSR	Metabolic Disease
Relamorelin (RM-131), a pentapeptide ghrelin analog, is a selective ghrelin/growth hormone secretagogue receptor (GHSR) agonist with a K_i of 0.42 nM for GHS-1a receptor. Relamorelin is centrally penetrant. Relamorelin increases growth hormone levels and accelerates gastric emptying. Relamorelin has the potential for cachexia, gastroparesis, and gastric/intestinal dysmobility disorders research .

Relamorelin acetate RM-131 acetate; BIM-28131 acetate	GHSR	Metabolic Disease
Relamorelin (RM-131) acetate, a pentapeptide ghrelin analog, is a selective ghrelin/growth hormone secretagogue receptor (GHSR) agonist with a K_i of 0.42 nM for GHS-1a receptor. Relamorelin acetate is centrally penetrant. Relamorelin acetate increases growth hormone levels and accelerates gastric emptying. Relamorelin acetate has the potential for cachexia, gastroparesis, and gastric/intestinal dysmobility disorders research .

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