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Results for "

negative allosteric modulator

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (1) Apoptosis (1) Cannabinoid Receptor (2) CaSR (2) CCR (1) Dopamine Receptor (1) GABA Receptor (5) GCGR (2) iGluR (6) Interleukin Related (1) LPL Receptor (1) mAChR (1) mGluR (27) P2X Receptor (2) Potassium Channel (2) Src (1) Wnt (1) β-catenin (1)
By Research Areas:	Cancer (4) Cardiovascular Disease (2) Inflammation/Immunology (2) Metabolic Disease (5) Neurological Disease (40)

Inhibitors & Agonists

Screening Libraries

Inhibitory Antibodies

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-103561

DCB	mGluR	Neurological Disease
DCB (3,3′-dichlorobenzaldazine) is an neutral allosteric modulator of themetabotropic glutamate receptor metabotropic glutamate receptor subtype 5 (mGluR5) . DCB blocks the positive allosteric regulation of mGluRs (mGluR5) with the help of 3,3′-difluorobenzaldazine (DFB). DCB shows the negative modulatory effect of 3,3′-dimethoxybenzaldazine (DMeOB) .

HY-119765

VU0366248

mGluR Neurological Disease

VU0366248 is a mGlu5 negative allosteric modulator .

VU0366248	mGluR	Neurological Disease
VU0366248 is a mGlu5 negative allosteric modulator .

HY-114863

PHCCC(4Me) THCCC	mGluR	Neurological Disease
PHCCC(4Me) (THCCC), a PHCCC analog, is a dual mGluR2 (IC₅₀ of 1.5 μM) negative allosteric modulator and mGluR3 (EC₅₀ of 8.9 μM) positive allosteric modulator .

HY-145585

Onfasprodil MIJ-821	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-103574

Raseglurant hydrochloride ADX-10059 hydrochloride	mGluR	Neurological Disease
Raseglurant hydrochloride is a negative allosteric modulator of mGluR5. Raseglurant hydrochloride can be used in study migraine .

HY-117959

TAK-615	LPL Receptor	Inflammation/Immunology
TAK-615 is a negative allosteric modulator (NAM) of the LPA1 receptor for the research of pulmonary fibrosis. TAK-615 binds the LPA1 receptor with high affinity (K_d high affinity of 1.7 nM and K_d low affinity of 14.5 nM) .

HY-12567

ML375 VU0483253	mAChR	Neurological Disease
ML375 (VU0483253) is a potent, highly selective, brain-penetrant and orally active M5 mAChR negative allosteric modulator (NAM) with IC₅₀s of 300 nM and 790 nM for human and rat M5, respectively. ML375 is inactive at human and rat M1-M4 .

HY-120428

VU0410425	mGluR	Neurological Disease
VU0410425 is an mGlu₁ negative allosteric modulator. VU0410425 exhibits potent inhibitory activity for rat mGlu₁ with an IC₅₀ value of 140 nM. VU0410425 can be used for the research of central nervous system disorders .

HY-16716

Basmisanil 1 Publications Verification RG1662; RO5186582	GABA Receptor	Neurological Disease
Basmisanil (RG1662) is a highly selective orally active α subunit-containing GABAA receptors (GABAAα5) negative allosteric modulator (NAMs). Basmisanil can inhibit GABAA-α5 with a K_i value of 5 nM and IC₅₀ value of 8 nM, respectively. Basmisanil can be used for the research of multiple cognitive and psychiatric disorders .

HY-116553

FzM1	Wnt β-catenin	Cancer
FzM1 is a negative allosteric modulator (NAM) of Frizzled receptor FZD4. FzM1 reduces WNT5A-dependent WNT responsive element (WRE) activity (log EC_50inh=−6.2). FzM1 binds to an allosteric binding site located in intracellular loop 3 (ICL3) of FZD4 and alters the conformation of the receptor, ultimately inhibiting the WNT/β-catenin cascade .

HY-147558

CB1R Allosteric modulator 1	Cannabinoid Receptor	Others
CB1R Allosteric modulator 1 (compound 11) is a potent CB1R allosteric modulator. CB1R Allosteric modulator 1 shows negatively affects the functional activity of orthosteric ligands (NAM) at CB1Rs .

HY-147559

CB1R Allosteric modulator 2	Cannabinoid Receptor	Others
CB1R Allosteric modulator 2 (compound 18) is a potent CB1R allosteric modulator. CB1R Allosteric modulator 2 shows negatively affects the functional activity of orthosteric ligands (NAM) at CB1Rs .

HY-124803

GPCR modulator-1

GCGR Metabolic Disease

GPCR modulator-1 is a negative allosteric modulator of GLP receptor. GPCR modulator-1 has the potential for type 2 diabetes research .
HY-145370

GluN2B receptor modulator-1

iGluR Neurological Disease

GluN2B receptor modulator-1 is a selective GluN2B negative allosteric modulator with an IC₅₀ value of 31 nM.
HY-101845

FITM

1 Publications Verification

mGluR Cancer

FITM is a negative allosteric modulator of mGlu1 receptor with a K_i of 2.5 nM.
HY-112788

ONO-8590580

GABA Receptor Neurological Disease

ONO-8590580 is a GABA_A α5 negative allosteric modulator.
HY-103573

VU 0360223

mGluR Neurological Disease

VU 0360223 is a potent metabotropic glutamate receptors (mGluR) negative allosteric modulator with an IC₅₀ of 61 nM .
HY-16766

Decoglurant

RO4995819
mGluR Neurological Disease

Decoglurant (RO4995819) is a negative allosteric modulator of mGluR2 and mGluR3. Decoglurant is developed as an antidepressant .
HY-119941

VU0652835

mGluR Neurological Disease

VU0652835 is a metabotropic glutamate receptor subtype 5 (mGlu5) negative allosteric modulator with an IC₅₀ of 81 nM .
HY-110191

VU0469650

mGluR Neurological Disease Cancer

VU0469650 is a potent, selective and CNS-penetrated negative allosteric modulator of mGlu₁ receptor, with an IC₅₀ of 99 nM .

GPCR modulator-1	GCGR	Metabolic Disease
GPCR modulator-1 is a negative allosteric modulator of GLP receptor. GPCR modulator-1 has the potential for type 2 diabetes research .

GluN2B receptor modulator-1	iGluR	Neurological Disease
GluN2B receptor modulator-1 is a selective GluN2B negative allosteric modulator with an IC₅₀ value of 31 nM.

FITM 1 Publications Verification	mGluR	Cancer
FITM is a negative allosteric modulator of mGlu1 receptor with a K_i of 2.5 nM.

ONO-8590580	GABA Receptor	Neurological Disease
ONO-8590580 is a GABA_A α5 negative allosteric modulator.

VU 0360223	mGluR	Neurological Disease
VU 0360223 is a potent metabotropic glutamate receptors (mGluR) negative allosteric modulator with an IC₅₀ of 61 nM .

Decoglurant RO4995819	mGluR	Neurological Disease
Decoglurant (RO4995819) is a negative allosteric modulator of mGluR2 and mGluR3. Decoglurant is developed as an antidepressant .

VU0652835	mGluR	Neurological Disease
VU0652835 is a metabotropic glutamate receptor subtype 5 (mGlu5) negative allosteric modulator with an IC₅₀ of 81 nM .

VU0469650	mGluR	Neurological Disease Cancer
VU0469650 is a potent, selective and CNS-penetrated negative allosteric modulator of mGlu₁ receptor, with an IC₅₀ of 99 nM .

HY-147657

GABAA receptor modulator-2	GABA Receptor	Neurological Disease
GABAA receptor modulator-2 (Compound 20) is selective, orally active α5-GABA_AR negative allosteric modulator (NAM) with a K_i of 4.1 nM. GABAA receptor modulator-2 shows high-metabolic stability and good CNS safety .

HY-122138

VU6010572

mGluR Neurological Disease

VU6010572 is a potent and selective mGlu3 negative allosteric modulator with IC₅₀ of 245 nM. VU6010572 is highly CNS penetrant .
HY-120375

LUF7346

Potassium Channel Cardiovascular Disease

LUF7346 is a potent Kv11.1 (hERG) channel negative allosteric modulator, with an IC₅₀ of 35.6 ± 3.2 nM .

VU6010572	mGluR	Neurological Disease
VU6010572 is a potent and selective mGlu3 negative allosteric modulator with IC₅₀ of 245 nM. VU6010572 is highly CNS penetrant .

LUF7346	Potassium Channel	Cardiovascular Disease
LUF7346 is a potent Kv11.1 (hERG) channel negative allosteric modulator, with an IC₅₀ of 35.6 ± 3.2 nM .

HY-114403

VU6012962	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-124622

NNC-0640

GCGR Metabolic Disease

NNC-0640 is a potent human G-protein-coupled glucagon receptor (GCGR) negative allosteric modulator (NAM) with an IC₅₀ of 69.2 nM .

NNC-0640	GCGR	Metabolic Disease
NNC-0640 is a potent human G-protein-coupled glucagon receptor (GCGR) negative allosteric modulator (NAM) with an IC₅₀ of 69.2 nM .

HY-100667

UBP608	iGluR	Neurological Disease
UBP608 is a potent N-Methyl-D-aspartate receptors (NMDARs) negative allosteric modulator. UBP608 has the potential for the research of neurological disorders .

HY-155088

MK-8768	mGluR	Metabolic Disease
MK-8768 is a highly potent, orally bioavailable and selective class of mGluR2 **negative allosteric** modulator (IC₅₀ of 9 .6nM) with excellent brain permeability.

HY-129946

Dopamine D2 receptor antagonist-1	Dopamine Receptor	Neurological Disease
Dopamine D2 receptor antagonist-1 is a negative allosteric modulator (NAM) of the dopamine D2 receptor (D2R) with sub-mM affinity .

HY-133555

mGluR2 antagonist 1	mGluR	Neurological Disease
mGluR2 antagonist 1 is a highly potent, orally bioavailable and selective class of mGluR2 negative allosteric modulator (IC₅₀ of 9 nM) with excellent brain permeability .

HY-110278

ADX71743	mGluR	Neurological Disease
ADX71743 is a highly selective, noncompetitive and brain-penetrant metabotropic glutamate receptor 7 negative allosteric modulator (mGlu7 NAM). ADX71743 has anxiolytic-like activity .

HY-108710

VU0650786	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-124569

NAB-14	iGluR	Neurological Disease
NAB-14 is a potent, selective, orally active and non-competitive GluN2C/2D antagonists with an IC₅₀ of 580 nM for GluN1/GluN2D. NAB-14 shows >800-fold selective for recombinant GluN2C and GluN2D over GluN2A and GluN2B. NAB-14 can cross the blood-brain-barrier .

HY-107774

BMS-986163	iGluR	Neurological Disease
BMS-986163 is a negative allosteric modulator of GluN2B. The proagent BMS-986163 rapidly converts to its active parent molecule BMS-986169 (K_i=4 nM, IC₅₀=24 nM).

HY-101281

VU 6008667

VU 6008667 is a selective negative allosteric modulator of M5 NAM with IC₅₀s of 1.2 μM and 1.6 μM for human M5 and rat M5, respectively. High CNS penetration .

VU 6008667
VU 6008667 is a selective negative allosteric modulator of M5 NAM with IC₅₀s of 1.2 μM and 1.6 μM for human M5 and rat M5, respectively. High CNS penetration .

HY-135891

AZD2423	CCR	Neurological Disease
AZD2423 is a potent, selective, orally bioavailable, and non-competitive CCR2 chemokine receptor negative allosteric modulator. AZD2423 has an IC₅₀ of 1.2 nM for CCR2 Ca ²⁺ flux .

HY-103572

MNI137	mGluR	Neurological Disease
MNI137 is a potent and selective negative allosteric modulator for group II mGluRs. MNI137 has IC₅₀s values of 8.3 and 12.6 nM for human and rat mGlu2 inhibition of glutamate-induced calcium mobilization .

HY-110180

VU0409106	mGluR	Neurological Disease
VU0409106 is a potent and selective mGlu₅ negative allosteric modulator (NAM) with an IC₅₀ of 24 nM. VU0409106 shows anxiolytic effects in rat models in a concentration-dependent manner. VU0409106 also penetrates the blood-brain barrier (BBB) .

HY-129636A

GABAB receptor antagonist 1	GABA Receptor	Neurological Disease
GABAB receptor antagonist 1 (compound 14) is a selective and negative allosteric modulator of GABAB (γ-Aminobutyric acid) receptors. (E)-GABAB receptor antagonist 1 decreases GABA-induced IP3 (inositol trisphosphate) production with IC₅₀ of 37.9 μM .

HY-15446

Basimglurant 1 Publications Verification RG7090; CTEP Derivative	mGluR	Neurological Disease
Basimglurant (RG7090) is a potent, selective and orally available mGlu5 negative allosteric modulator with a K_d of 1.1 nM . Basimglurant 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-155810

DQP-26	iGluR	Neurological Disease
DQP-26 is a potent NMDAR negative allosteric modulator with IC₅₀ values of 0.77 μM and 0.44 μM for GluN2C and GluN2D, respectively. DQP-26 has the potential for NMDAR-associated neurological disease research .

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-103575A

MFZ 10-7 hydrochloride	mGluR	Neurological Disease
MFZ 10-7 hydrochloride is a highly potent and selective mGluR5 NAM (negative allosteric modulator), with a K_i of 0.67 nM for rat mGluR5 . MFZ 10-7 (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-120717

VU6001966	mGluR	Others
VU6001966 (compound 15m) is a potent and cross the blood-brain barrier mGlu2 (metabotropic glutamate receptor 2) negative allosteric modulator with IC₅₀s of 78 nM and >30 µM for mGlu2 and mGlu3, respectively. VU6001966 can serve as an mGlu2 PET tracer .

HY-103575

MFZ 10-7	mGluR	Neurological Disease
MFZ 10-7 is a highly potent and selective mGluR5 NAM (negative allosteric modulator), with a K_i of 0.67 nM for rat mGluR5 . MFZ 10-7 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-19888

GSK-1482160
GSK-1482160 is an orally available negative allosteric modulator of the P2X7 receptor. P2X7 receptors are involved in the production of pro-inflammatory cytokines, such as Il-1β, by central and peripheral immune cells. GSK-1482160 has the potential for the research of inflammation diseases .

HY-129636

(E)-GABAB receptor antagonist 1	GABA Receptor	Neurological Disease
(E)-GABAB receptor antagonist 1 is a trans-GABAB receptor antagonist 1. GABAB receptor antagonist 1 (compound 14) is a selective and negative allosteric modulator of GABAB (γ-Aminobutyric acid) receptors. (E)-GABAB receptor antagonist 1 decreases GABA-induced IP3 (inositol trisphosphate) production with IC₅₀ of 37.9 μM .

HY-103320A

Calhex 231 hydrochloride 3 Publications Verification	CaSR	Metabolic Disease
Calhex 231 hydrochloride is a potent negative allosteric modulator that blocks (IC₅₀ = 0.39 μM) increases in [ ³H]inositol phosphates elicited by activating the human wild-type CaSR transiently Ca ²⁺-sensing receptor. Calhex 231 hydrochloride can be used in the study of traumatic hemorrhagic shock (THS) and diabetic cardiomyopathy (DCM) .

HY-131019

JF-NP-26	mGluR	Neurological Disease
JF-NP-26, an inactive photocaged derivative of raseglurant, is the first caged mGlu5 receptor negative allosteric modulator. Uncaging of JF-NP-26 is elicited with light pulses in the visible spectrum (405 nm). JF-NP-26 induces light-dependent analgesia in models of inflammatory and neuropathic pain in freely behaving animals .

HY-103320

Calhex 231	CaSR	Metabolic Disease
Calhex 231 is a potent negative allosteric modulator that blocks (IC₅₀ = 0.39 μM) increases in [ ³H]inositol phosphates elicited by activating the human wild-type CaSR transiently Ca ²⁺-sensing receptor. Calhex 231 can be used in the study of traumatic hemorrhagic shock (THS) and diabetic cardiomyopathy (DCM) .

HY-16636

ML337	mGluR	Neurological Disease
ML337 is a selective and brain-penetrant negative allosteric modulator of mGlu3, with an IC₅₀ of 593 nM. ML337 possesses a favorable dystrophia myotonica protein kinase (DMPK) and ancillary pharmacology profile . ML337 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

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