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CNS disorder

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (7) Adrenergic Receptor (2) Autophagy (2) Biochemical Assay Reagents (1) Cannabinoid Receptor (1) CDK (1) FAAH (2) GABA Receptor (1) Guanylate Cyclase (1) iGluR (2) LPL Receptor (1) Monoamine Oxidase (1) nAChR (1) Neurokinin Receptor (2) Opioid Receptor (5) Phosphodiesterase (PDE) (3) Potassium Channel (1) Thyroid Hormone Receptor (1) Vasopressin Receptor (1)
By Research Areas:	Cancer (6) Cardiovascular Disease (4) Endocrinology (4) Inflammation/Immunology (4) Metabolic Disease (3) Neurological Disease (27)

Inhibitors & Agonists

Screening Libraries

Biochemical Assay Reagents

Natural
Products

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-118158

FAAH/MAGL-IN-4	FAAH	Neurological Disease
FAAH/MAGL-IN-4 (Compound 13) is a potent fatty acid amide hydrolase (FAAH) and monoglyceride lipase (MGL) inhibitor with IC₅₀s of 9.1 nM and 7.9 μM, respectively. FAAH/MAGL-IN-4 can be used for the research of pain and CNS disorders .

HY-122697

ML418	Potassium Channel	Cardiovascular Disease Neurological Disease Endocrinology
ML418 is a potent, selective and CNS penetrating Kir7.1 potassium channel blocker. ML418 inhibits Kir7.1 with an IC₅₀ value of 0.31 μM. ML418 can be used for the research of neurological, cardiovascular, endocrine and muscle disorders.

HY-W105505

SAMe-1,4-Butanedisulfonate	Biochemical Assay Reagents	Neurological Disease Inflammation/Immunology
SAMe-1,4-Butanedisulfonate, a natural compound, is a methyl donor in the central nervous system. SAMe-1,4-Butanedisulfonate has antidepressant activity. SAMe-1,4-Butanedisulfonate can be used for research of CNS disorders .

HY-156533A

5-HT2 agonist-1 free base	5-HT Receptor	Neurological Disease Inflammation/Immunology Cancer
5-HT2 agonist-1 (Compound 24) free base is a 5-HT2A & 5-HT2B & 5-HT2C agonist, with IC₅₀s of 10 nM, 8.3, and 1.6 nM respectively. 5-HT2 agonist-1 free base can be used for research of depression, alcoholism, tobacco and cocaine addiction, inflammation, cluster headache, PTSD, seizure disorders and other CNS disorders .

HY-156533

5-HT2 agonist-1	5-HT Receptor	Cancer
5-HT2 agonist-1 (Compound 24) is a 5-HT2A & 5-HT2B & 5-HT2C agonist, with IC₅₀s of 10 nM, 8.3, and 1.6 nM respectively. 5-HT2 agonist-1 free base can be used for research of depression, alcoholism, tobacco and cocaine addiction, inflammation, cluster headache, PTSD, seizure disorders and other CNS disorders .

HY-156534

5-HT2A&5-HT2C agonist-1	5-HT Receptor	Neurological Disease Inflammation/Immunology Cancer
5-HT2A&5-HT2C agonist-1 (Example 2) is a 5-HT2A & 5-HT2C agonist, with IC₅₀s of 196 nM and 0.9 nM respectively. 5-HT2A&5-HT2C agonist-1 can be used for research of depression, alcoholism, tobacco and cocaine addiction, inflammation, cluster headache, PTSD, seizure disorders and other CNS disorders .

HY-144827

AM8936	Cannabinoid Receptor	Neurological Disease Metabolic Disease
AM8936 acts as a balanced and potent cannabinoid receptor type-1 (CB1) agonist in functional assays (EC₅₀s of 8.6 and 1.4 nM for rCB1 and hCB1, respectively). AM8936 exhibits high affinity for rat CB1 (rCB1) with K_i of 0.55 nM. AM8936 is a potent and efficacious CB1 agonist in vivo. AM8936 can be used for the research of CNS and metabolic disorders, pain, glaucoma, etc .

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-105685

SRX246	Vasopressin Receptor	Neurological Disease
SRX246 is a potent, CNS-penetrant, highly selective, orally bioavailable vasopressin 1a (V1a) receptor antagonist (K_i=0.3 nM for human V1a). SRX246 has no interaction at V1b and V2 receptors. SRX246 also displays negligible binding at 64 others receptors classes, including 35 G-proteincoupled receptors. SRX246 can be used for treatment of stress-related disorders .

HY-N2428

N-(3-Methoxybenzyl)Palmitamide	FAAH	Neurological Disease
N-(3-Methoxybenzyl)Palmitamide is a promising inhibitor of FAAH for the treatment of pain, inflammation and CNS degenerative disorders .

HY-14550A

PDE10-IN-5

Phosphodiesterase (PDE) Others

PDE10-IN-5 is a phosphodiesterase 10 (PDE 10) inhibitor, can be used for researching certain central nervous system (CNS) disorders .

PDE10-IN-5	Phosphodiesterase (PDE)	Others
PDE10-IN-5 is a phosphodiesterase 10 (PDE 10) inhibitor, can be used for researching certain central nervous system (CNS) disorders .

HY-14758

Adipiplon NG2-73	GABA Receptor	Neurological Disease
Adipiplon (NG2-73) is a selective GABA_A receptor positive allosteric modulator. Adipiplon is particularly useful in the research of a variety of central nervous system (CNS) disorders.

HY-12813

PDE10-IN-1

Phosphodiesterase (PDE) Neurological Disease

PDE10-IN-1 is a potent PDE10-IN-1 inhibitor extracted from Patent WO 2013192273 A1, for treating CNS and metabolic disorders.

PDE10-IN-1	Phosphodiesterase (PDE)	Neurological Disease
PDE10-IN-1 is a potent PDE10-IN-1 inhibitor extracted from Patent WO 2013192273 A1, for treating CNS and metabolic disorders.

HY-160207

ABX-002 MA-JD21	Thyroid Hormone Receptor	Neurological Disease
ABX-002 (MA-JD21 )is a TR-β selective CNS-penetrant TR-β agonist prodrug and can be used for study of major depressive disorder (MDD) .

HY-145607

Zagociguat CY-6463; IW-6463	Guanylate Cyclase	Cardiovascular Disease
Zagociguat is the stimulator of soluble guanylate cyclase. Zagociguat increases nitric oxide (NO) signaling leading to an increase in cyclic guanosine monophosphate production. Zagociguat has the potential for the research of noncentral nervous system (CNS) disorders .

HY-145086

R-PSOP	Others	Metabolic Disease
R-PSOP is highly potent and selective nonpeptidic NMUR2 antagonist. R-PSOP binds to NMUR2 with the K_is of 52 and 32 nM for the human and rat NMUR2, respectively. R-PSOP shows moderate CNS penetration. R-PSOP can be used for the research of the eating disorders, obesity, pain, and stress-related disorders .

HY-109527

5-HT7 agonist 1	5-HT Receptor	Neurological Disease
5-HT7 agonist 1 is a selective 5-HT7 receptor agonist, with an IC₅₀ of 222.93 nM, can be used for the 5-HT7 receptor related disease, such as CNS disorders.

HY-153336

CDK-IN-12

CDK Cancer

CDK-IN-12 (Example 20) is a CDK Inhibitor. CDK-IN-12 Inhibits CDK4/6 with IC₅₀ values less than 20 nM .

CDK-IN-12	CDK	Cancer
CDK-IN-12 (Example 20) is a CDK Inhibitor. CDK-IN-12 Inhibits CDK4/6 with IC₅₀ values less than 20 nM .

HY-148115

S1p receptor agonist 2	LPL Receptor	Inflammation/Immunology
S1p receptor agonist 2 (compound 1) is an agonist of S1P5 receptor, exhibits selectivity over the S1P1 and/or S1P3 receptors. S1p receptor agonist 2 can be used for endogenous SIP signaling system research, and alleviating or preventing CNS disorders research, such as neurodegenerative disorders .

HY-155320

Mu opioid receptor antagonist 7	Opioid Receptor	Neurological Disease
Mu opioid receptor antagonist 7 (compound 24) is a potent and CNS permeable antagonist of µOR (µ-opioid receptor), with an IC₅₀ of 29 ± 3.0 nM. Mu opioid receptor antagonist 7 can be used for the research of pain and opioid use disorder .

HY-147399

5-HT7 agonist 2	5-HT Receptor	Neurological Disease
5-HT7 agonist 2 is a potent 5-HT₇ receptor agonist with an IC₅₀ value of 28.7 nM. 5-HT7 agonist 2 can be used for research of central nervous system (CNS) disorders .

HY-146101

NMDA receptor antagonist 5	iGluR	Neurological Disease
NMDA receptor antagonist 5 (Compound 10e) is a potent, brain permeable and non-toxic NMDA receptor antagonist. NMDA receptor antagonist 5 can be used for neurological disorder research .

HY-124754

Navacaprant BTRX-335140; CYM-53093	Opioid Receptor	Neurological Disease Metabolic Disease
Navacaprant (BTRX-335140) is a selective and orally active κ opioid receptor (KOR) antagonist, has antagonist activity for κOR, μOR and δOR with IC₅₀ values of 0.8 nM, 110 nM, and 6500 nM, respectively. Navacaprant endows with favorable in vitro ADMET and in vivo pharmacokinetic profiles and medication-like duration of action in rats. Navacaprant distributes well into the CNS and can be used for the research of neuropathy .

HY-144608

Mu opioid receptor antagonist 3	Opioid Receptor	Neurological Disease
Mu opioid receptor antagonist 3 (compound 26) is a potent and selective μ opioid receptor (MOR) antagonist with a K_i of 0.24 nM and an EC₅₀ of 0.54 nM. Mu opioid receptor antagonist 3 has remarkable CNS antagonism against morphine, and precipitated fewer withdrawal symptoms than Naloxone. Mu opioid receptor antagonist 3 can be used for researching opioid use disorders (OUD) .

HY-138879B

CP-601932 (1S,5R)-CP-601927	nAChR	Neurological Disease
CP-601932 ((1S,5R)-CP-601927) is a high-affinity partial agonist at α3β4 nAChR (K_i=21 nM; EC₅₀=~ 3 μM). CP-601932 has the same high-binding affinity at α4β2 nAChR (K_i=21 nM) and an order of magnitude lower affinity for α6 and α7 nAChR subtypes. CP-601932 selectively decreases ethanol but not sucrose consumption and operant self-administration following long-term exposure. CP-601932 can penetrate the CNS .

HY-144609

Mu opioid receptor antagonist 4	Opioid Receptor	Neurological Disease
Mu opioid receptor antagonist 4 (compound 31) is a potent and selective μ opioid receptor (MOR) antagonist with a K_i of 0.38 nM and an EC₅₀ of 1.07 nM. Mu opioid receptor antagonist 4 has remarkable CNS antagonism against morphine, and precipitated fewer withdrawal symptoms than Naloxone. Mu opioid receptor antagonist 4 Mu opioid receptor antagonist 4 can be used for researching opioid use disorders (OUD) .

HY-144607

Mu opioid receptor antagonist 2	Opioid Receptor	Neurological Disease
Mu opioid receptor antagonist 2 (compound 25) is a potent, selective and blood-brain barrier (BBB) penetrant μ opioid receptor (MOR) antagonist with a K_i 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-B0193A

Prazosin hydrochloride Maximum Cited Publications 8 Publications Verification	Adrenergic Receptor Autophagy	Cardiovascular Disease Endocrinology Cancer
Prazosin hydrochloride is a well-tolerated, CNS-active α1-adrenergic receptor antagonist for the research of high blood pressure and alcohol use disorders . Prazosin hydrochloride potently inhibits Norepinephrine (NE)-stimulated 45Ca efflux with an IC₅₀ of 0.15 nM .Prazosin hydrochloride inhibits organic cation transporters OCT-1 and OCT-3 with IC₅₀s of 1.8, and 13 μM, respectively .

HY-112831

Osoresnontrine 1 Publications Verification BI-409306	Phosphodiesterase (PDE)	Neurological Disease
Osoresnontrine (BI-409306) is a potent and selective PDE9A inhibitor, with an IC₅₀ of 52 nM, and shows weak activity against other PDEs, such as PDE1A (IC₅₀, 1.4 µM), PDE1C (IC₅₀, 1.0 µM), PDE2A, PDE3A, PDE4B, PDE5A, PDE6AB, PDE7A, and PDE10A (IC₅₀ all > 10 μM); Osoresnontrine can be used in the research of memory enhancement in CNS disorders.

HY-14558

Tandospirone 2 Publications Verification SM-3997	5-HT Receptor	Neurological Disease
Tandospirone (SM-3997) is a potent and selective 5-HT_1A receptor partial agonist, with a K_i of 27 nM. Tandospirone has anxiolytic and antidepressant activities. Tandospirone can be used for the research of the central nervous system disorders and the underlying mechanisms .

HY-110053

Tandospirone hydrochloride SM-3997 hydrochloride	5-HT Receptor	Neurological Disease
Tandospirone (SM-3997) hydrochloride is a potent and selective 5-HT_1A receptor partial agonist, with a K_i of 27 nM. Tandospirone hydrochloride has anxiolytic and antidepressant activities. Tandospirone hydrochloride can be used for the research of the central nervous system disorders and the underlying mechanisms .

HY-B0193AR

Prazosin hydrochloride (Standard)	Adrenergic Receptor Autophagy	Cardiovascular Disease Endocrinology Cancer
Prazosin (hydrochloride) (Standard) is the analytical standard of Prazosin (hydrochloride). This product is intended for research and analytical applications. Prazosin hydrochloride is a well-tolerated, CNS-active α1-adrenergic receptor antagonist for the research of high blood pressure and alcohol use disorders . Prazosin hydrochloride potently inhibits Norepinephrine (NE)-stimulated 45Ca efflux with an IC₅₀ of 0.15 nM .Prazosin hydrochloride inhibits organic cation transporters OCT-1 and OCT-3 with IC₅₀s of 1.8, and 13 μM, respectively .

HY-122347A

Orvepitant maleate GW823296 maleate	Neurokinin Receptor	Neurological Disease
Orvepitant maleate (GW823296 maleate) is potent, selective, orally active and well-tolerated neurokinin-1 receptor (NK-1) antagonist with a pK_i of 10.2 for human neurokinin-1 receptor. Orvepitant maleate can across the blood-brain barrier. Orvepitant maleate has the potential for depressive disorder and chronic refractory cough (CRC) treatment .

HY-151094

FTEAA	Monoamine Oxidase	Neurological Disease
FTEAA is a 4-styrylpiperidine inhibitor. FTEAA exhibits potent inhibitory effect towards both monoamine oxidase with IC₅₀s of 0.52 μM (MAO-A), 1.02 μM (MAO-B), respectively. MAO inhibitors can be used for cardiovascular, neurological and oncological disorders research .

Cat. No.	Product Name

HY-L028

CNS-Penetrant Compound Library	856 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 856 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.

CNS-Penetrant Compound Library

856 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 856 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-L013

Neuronal Signaling Compound Library	2542 compounds
Neuronal Signaling is involved in the regulation of the mechanisms of the central nervous system (CNS) such as its structure, function, genetics and physiology as well as how this can be applied to understand diseases of the nervous system. Every information processing system in the CNS is composed of neurons and glia, neurons have evolved unique capabilities for intracellular signaling (communication within the cell) and intercellular signaling (communication between cells). G protein-coupled receptors (GPCRs), including 5-HT receptor, histamine receptor, opioid receptor, etc. are the largest class of sensory proteins and are important therapeutic targets in Neuronal Signaling. Besides, Notch signaling, such as β- and γ-secretase, also plays multiple roles in the development of the CNS including regulating neural stem cell (NSC) proliferation, survival, self-renewal and differentiation. GPCR dysfunction caused by receptor mutations and environmental challenges contributes to many neurological diseases. Notch signaling in neurons, glia, and NSCs is also involved in pathological changes that occur in disorders such as stroke, Alzheimer's disease and CNS tumors. Thus, targeting Neuronal Signaling, such as notch signaling and GPCRs, can be used as therapeutic interventions for several different CNS disorders. MCE designs a unique collection of 2542 Neuronal Signaling-related compounds that act as a useful tool for the research of neuronal regulation and neuronal diseases.

Neuronal Signaling Compound Library

2542 compounds

Neuronal Signaling is involved in the regulation of the mechanisms of the central nervous system (CNS) such as its structure, function, genetics and physiology as well as how this can be applied to understand diseases of the nervous system. Every information processing system in the CNS is composed of neurons and glia, neurons have evolved unique capabilities for intracellular signaling (communication within the cell) and intercellular signaling (communication between cells). G protein-coupled receptors (GPCRs), including 5-HT receptor, histamine receptor, opioid receptor, etc. are the largest class of sensory proteins and are important therapeutic targets in Neuronal Signaling. Besides, Notch signaling, such as β- and γ-secretase, also plays multiple roles in the development of the CNS including regulating neural stem cell (NSC) proliferation, survival, self-renewal and differentiation. GPCR dysfunction caused by receptor mutations and environmental challenges contributes to many neurological diseases. Notch signaling in neurons, glia, and NSCs is also involved in pathological changes that occur in disorders such as stroke, Alzheimer's disease and CNS tumors. Thus, targeting Neuronal Signaling, such as notch signaling and GPCRs, can be used as therapeutic interventions for several different CNS disorders.

MCE designs a unique collection of 2542 Neuronal Signaling-related compounds that act as a useful tool for the research of neuronal regulation and neuronal diseases.

SAMe-1,4-Butanedisulfonate	Biochemical Assay Reagents
SAMe-1,4-Butanedisulfonate, a natural compound, is a methyl donor in the central nervous system. SAMe-1,4-Butanedisulfonate has antidepressant activity. SAMe-1,4-Butanedisulfonate can be used for research of CNS disorders .

N-(3-Methoxybenzyl)Palmitamide	Natural Products other families Source classification Plants	FAAH
N-(3-Methoxybenzyl)Palmitamide is a promising inhibitor of FAAH for the treatment of pain, inflammation and CNS degenerative disorders .

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