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Results for "

positive allosteric modulator

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (5) Adenosine Receptor (6) Apoptosis (1) Arrestin (1) Calcium Channel (1) Cannabinoid Receptor (7) CaSR (3) Cholinesterase (ChE) (2) Cytochrome P450 (2) Dopamine Receptor (4) EAAT (3) Endogenous Metabolite (6) Free Fatty Acid Receptor (2) GABA Receptor (42) GCGR (3) GLP Receptor (7) GPR68 (1) Guanylate Cyclase (1) Histone Methyltransferase (2) iGluR (27) Isotope-Labeled Compounds (4) Keap1-Nrf2 (1) Lipoxygenase (1) LXR (2) mAChR (28) Mas-related G-protein-coupled Receptor (MRGPR) (4) mGluR (67) nAChR (20) NAMPT (2) Neuropeptide Y Receptor (2) Opioid Receptor (5) P-glycoprotein (1) Parasite (2) PERK (1) Potassium Channel (2) Sigma Receptor (6) Sirtuin (1) Sodium Channel (1) Taste Receptor (1) TRP Channel (2) TSH Receptor (1)
By Research Areas:	Cancer (11) Cardiovascular Disease (4) Endocrinology (3) Infection (5) Inflammation/Immunology (10) Metabolic Disease (18) Neurological Disease (213)
Click Chemistry:	Alkynes (1)

276

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Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-122819

Calindol hydrochloride	CaSR	Cardiovascular Disease
Calindol hydrochloride is a positive allosteric modulator (PAM) of calcimimetic calcium-sensing receptor (CaSR) with an EC₅₀ of 132 nM .

HY-159826

Brexanolone caprilcerbate	GABA Receptor	Neurological Disease
Brexanolone caprilcerbate is a potent GABAA receptor positive allosteric modulator .

HY-116067

VU0404251	mGluR	Neurological Disease
VU0404251 is a highly potent positive allosteric modulator of mGlu for the study of psychosis .

HY-147530

mGluR2 modulator 4	mGluR	Neurological Disease
mGluR2 modulator 4 (compound 47) is a potent mGluR2 positive allosteric modulator with an EC₅₀ value of 0.8 μM. mGluR2 modulator 4 can be used for researching antipsychotic .

HY-147528

mGluR2 modulator 2	mGluR	Neurological Disease
mGluR2 modulator 2 (compound 2) is a potent, selective and orally bioavailable mGluR2 positive allosteric modulator with an EC₅₀ value of 0.13 μM. mGluR2 modulator 2 can be used for researching antipsychotic .

HY-162454

DA-023	EAAT	Neurological Disease
DA-023 (Compound 4) is a selective positive allosteric modulator (PAM) of EAAT2 with an EC₅₀ value of 1 nM .

HY-159829

Direclidine	mAChR	Neurological Disease
Direclidine is a muscarinic M4 receptor positive allosteric modulator .

HY-121806

VU0486846	mAChR	Neurological Disease
VU0486846 is an orally active and selective muscarinic acetylcholine receptor M1 positive allosteric modulator (PAM) .

HY-168025

VU6007496	Others	Neurological Disease
VU6007496 is a highly selective and CNS penetrant M1 positive allosteric modulator (PAM). VU6007496 shows excellent pharmacokinetics (PK) .

HY-107423

GNE 6901	iGluR	Neurological Disease
GNE 6901 (compound 40) is a potent GluN2A-selective NMDAR positive allosteric modulator (PAM) with an EC₅₀ of 382 nM .

HY-116855

TASP0433864	mGluR	Neurological Disease
TASP0433864 is a selective positive allosteric modulator (PAM) of metabotropic glutamate 2 (mGlu2) receptor with EC₅₀ values of 199 nM and 206 nM against human and rat mGlu2 receptors, respectively. TASP0433864 has antipsychotic activity .

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-119806

TMPPAA	5-HT Receptor	Neurological Disease
TMPPAA is an allosteric agonist and positive allosteric modulator of the 5-HT3 receptor. TMPPAA enhances 5-HT-mediated 5-HT3AR signaling .

HY-120023

VU0453595	mAChR	Neurological Disease
VU0453595 is a highly selective, systemically active M₁ positive allosteric modulator (PAM, EC₅₀=2140 nM) for the research of schizophrenia .

HY-103475

GS39783	GABA Receptor	Neurological Disease
GS39783 is a positive allosteric modulator (PAM) of GABA_BR. Positive modulation of the GABA_BR can be used for the research of Nicotine addiction .

HY-159177

M4 mAChR Modulator-1	mAChR	Neurological Disease
M4 mAChR Modulator-1 (compound 23i) is a M4 mAChR positive allosteric modulator (PAM). M4 mAChR Modulator-1 exhibits significantly greater cooperativity with ACh in β-arrestin recruitment over G protein activation. M4 mAChR Modulator-1 displays weak PAM effect in G protein-mediated responses, but strong PAM effect in β-arrestin recruitment .

HY-107682

TQS	nAChR	Neurological Disease Inflammation/Immunology
TQS is a α7 nicotinic acetylcholine receptor (nAChR) positive allosteric modulator. TQS can be used for the research of neuroinflammatory pain .

HY-143312

V-0219	GLP Receptor	Metabolic Disease
V-0219 (Compound 9) is an orally active, positive allosteric modulator (PAM) of the glucagon-like peptide-1 receptor (GLP-1R). V-0219 can be used for obesity-associated diabetes research .

HY-107504

VU0360172 hydrochloride	mGluR	Neurological Disease
VU0360172 hydrochloride is a potent and selective mGlu5 receptor positive allosteric modulator (PAM) with an EC₅₀ value of 16 nM and a K_i of 195 nM, respectively. VU0360172 hydrochloride stimulates polyphosphoinositide (PI) hydrolysis in vivo, which is abrogated in mGlu5 receptors gene deleted mice .

HY-10933

CX516 2 Publications Verification BDP 12	iGluR	Neurological Disease
CX516 (BDP 12) is an ampakine and acts as an AMPA receptor positive allosteric modulator for the research of Alzheimer's disease, schizophrenia and mild cognitive impairment (MCI) .

HY-120837

PZ-II-029	GABA Receptor	Neurological Disease
PZ-II-029 is a GABAA positive allosteric modulator that selectively binds with high affinity to α6β3γ2. PZ-II-029 shows anti-migraine effects .

HY-144291

LY3154885	Dopamine Receptor	Neurological Disease
LY3154885 is an orally active dopamine D1 receptor positive allosteric modulator (PAM). LY3154885 has an improved agent-agent interactions (DDI) risk profile .

HY-139091

FEMA 4774	Taste Receptor	Others
FEMA 4774 is a positive allosteric modulator of taste receptors T1R2 and T1R3, two subunits of the human sweet taste receptor. FEMA 4774 is also used as a sucrose sweetness enhancer .

HY-113689

GAT211	Cannabinoid Receptor	Neurological Disease
GAT211 is a cannabinoid 1 receptor (CB1R) positive allosteric modulator (PAM). GAT211 activates cAMP and β-arrestin2 with EC₅₀ values of 260 nM and 650 nM, respectively. GAT211 inhibits GAT211 can be used for neuropathic and/or inflammatory pain research .

HY-101165

Cyclothiazide	iGluR	Neurological Disease
Cyclothiazide, a positive allosteric modulator of AMPA receptors, is used frequently to block the desensitization of both native and heterologously expressed AMPA receptors. Cyclothiazide is known to produce a fast inhibition of AMPA receptor desensitization and a much slower potentiation of the AMPA current .

HY-A0106

Levamisole 4 Publications Verification (-)-Tetramisole	nAChR Parasite	Infection Inflammation/Immunology Cancer
Levamisole ((-)-Levamisole), an anthelmintic agent with immunomodulatory properties. Levamisole acts as a positive allosteric modulator (PAM) for the α3β2 (EC₅₀=300 μM) and α3β4 (EC₅₀=100 μM) subtype of nAChRs. Orally active .

HY-12439

ML380 1 Publications Verification	mAChR	Neurological Disease
ML380 is a potent, subtype-selective, and brain-penetrant positive allosteric modulator (PAM) of M5 mAChR, with EC₅₀s of 190 and 610 nM for human and rat M5, respectively. ML380 exhibits moderate selectivity versus the M1 and M3 mAChR subtypes. ML380 could increase the affinity of ACh for the M5 mAChR .

HY-120576

ML169 VU0405652	mAChR	Neurological Disease
ML169 (VU0405652) is a potent, selective and brain penetrant positive allosteric modulator (PAM) of M₁ mAChR, with an EC₅₀ of 1.38 µM. ML169 is a MLPCN probe and can be used for Alzheimer’s disease .

HY-117851

AC-265347	CaSR	Metabolic Disease Endocrinology
AC-265347 is a calcium-sensing receptor (CaSR) agonist and positive allosteric modulator (ago-PAM) with the functional affinity (pK_B) of 5.1. AC-265347 can be used for the research of hyperparathyroidism and related diseases .

HY-101165R

Cyclothiazide (Standard)	iGluR	Neurological Disease
Cyclothiazide (Standard) is the analytical standard of Cyclothiazide. This product is intended for research and analytical applications. Cyclothiazide, a positive allosteric modulator of AMPA receptors, is used frequently to block the desensitization of both native and heterologously expressed AMPA receptors. Cyclothiazide is known to produce a fast inhibition of AMPA receptor desensitization and a much slower potentiation of the AMPA current .

HY-A0106R

Levamisole (Standard)	nAChR Parasite	Infection Inflammation/Immunology Cancer
Levamisole (Standard) is the analytical standard of Levamisole. This product is intended for research and analytical applications. Levamisole ((-)-Levamisole), an anthelmintic agent with immunomodulatory properties. Levamisole acts as a positive allosteric modulator (PAM) for the α3β2 (EC₅₀=300 μM) and α3β4 (EC₅₀=100 μM) subtype of nAChRs. Orally active .

HY-130630

mGluR2 modulator 1	mGluR	Neurological Disease
mGluR2 modulator 1 (compound 95) is a potent and BBB-penetrated mGluR2 (metabotropic glutamate receptor-2) positive allosteric modulator, with an EC₅₀ of 0.03 μM. mGluR2 modulator 1 can be used for psychosis research .

HY-159624

KK-92A	GABA Receptor	Neurological Disease
KK-92A, a blood-brain barrier penetrated GABAB positive allosteric modulator (PAM), suppresses alcohol self-administration and cue-induced reinstatement of alcohol seeking in rats .

HY-144698

mGlu4 receptor agonist 1	mGluR	Neurological Disease
mGlu4 receptor agonist 1 (compound 62) is a potent mGlu4 receptor positive allosteric modulator, with an EC₅₀ of 308 nM. mGlu4 receptor agonist 1 shows significant anxiolytic- and antipsychotic-like effect .

HY-114978

VU0424465	mGluR PERK	Neurological Disease
VU0424465 is a potent and partial PAM (positive allosteric modulator)-agonist for mGlu₅ mediated iCa ²⁺ mobilization. VU0424465 exhibits high affinity at MPEP allosteric binding site, with a K_i value of 11.8 nM. VU0424465 is also a agonist for pERK1/2 in cortical neurons .

HY-120645

BMS-986122	Opioid Receptor	Neurological Disease
BMS-986122 is a selective, potent positive allosteric modulator of the mu-opioid receptor (μ-OR). BMS-986122 shows potentiation of orthosteric agonist-mediated β-arrestin recruitment, adenylyl cyclase inhibition, and G protein activation. BMS-986122 potentiates DAMGO-mediated [ ³⁵S]GTPγS binding in mouse brain membranes .

HY-128575

BNC375	nAChR	Neurological Disease
BNC375 is a potent, selective, and orally available type I positive allosteric modulator of α7 nAChRs with an EC₅₀ of 1.9 μM. BNC375 exhibits good CNS-agent like properties and clinical candidate potential. .

HY-139897

CX 717	iGluR	Neurological Disease
CX 717 is a positive allosteric modulator of AMPA receptor. Antidepressant-like effect. CX 717 can be used for the research of adult attention deficit hyperactivity disorder (ADHD) .

HY-103520

DS2	GABA Receptor	Neurological Disease
DS2 is a selective positive allosteric modulator of δ-GABA_A receptor. DS2 selectively potentiates GABA responses mediated by α4β3δ receptor. DS2 does not enhance activity at α4β3γ2 and α1β3γ2 receptors. DS2 relieves pain and has the potential for sleep disorders research .

HY-141899

MK-6884	mAChR	Neurological Disease
MK-6884 is a M4 muscarinic receptor positive allosteric modulator (PAM) with a K_i value of 0.19 nM. MK-6884 can be used for the research of the neurodegenerative diseases. MK-6884 can be conveniently radiolabeled with carbon-11 and as a positron emission tomography (PET) imaging agent .

HY-107506

Ro 67-4853	mGluR	Neurological Disease
Ro 67-4853 is a positive allosteric modulator (PAM) of mGluR1 (pEC₅₀=7.16 for rmGlu1a receptor). Ro67-4853 exhibits activity at all group I mGlu receptors including hmGlu1, rmGlu1, and rmGlu5. Ro 67-4853 enhances the potency of L-Glu by interacting with the transmembrane domain (TMD) of the receptor. Ro 67-4853 potentiates sensory synaptic responses to repetitive vibrissa stimulation .

HY-120411

Sadopine	Calcium Channel	Others
Sadopine is an allosteric modulator for dihydropyridine receptor ((-)Sadopine as positive allosteric modulator and (+)Sadopine as negative allosteric modulator). Sadopine interacts with dihydropyridine (DHP)-sensitive L-type calcium channels .

HY-150056

CB1R Allosteric modulator 3	Cannabinoid Receptor Arrestin	Neurological Disease
CB1R Allosteric modulator 3 is a CB1R positive allosteric modulator. CB1R Allosteric modulator 3 has potent inhibition of cAMP and β-Arrestin with EC₅₀ values of 0.018 μM and 1.241 μM, respectively .

HY-147421

Xilmenolone	GABA Receptor	Neurological Disease
Xilmenolone is a GABAA receptor positive allosteric modulator .

HY-150057

CB1R Allosteric modulator 4	Cannabinoid Receptor	Others
CB1R Allosteric modulator 4 is a positive allosteric modulator of cannabinoid type-1 (CB1R) with good biological activity. CB1R Allosteric modulator 4 inhibits cAMP production and shows robust activity in β-arrestin-2 recruitment .

HY-101216

Org-26576	iGluR	Neurological Disease
Org-26576 is a AMPA receptor positive allosteric modulator.

HY-103668A

SSD114 hydrochloride	GABA Receptor	Neurological Disease
SSD114 hydrochloride is a novel GABA_B receptor positive allosteric modulator.

HY-155628

AMPA receptor modulator-6	iGluR	Others
AMPA receptor modulator-6 is an AMPA receptor positive allosteric modulator (PAM). AMPA receptor modulator-6 can be used in the study of neurological diseases .

HY-107507

Ro 01-6128 1 Publications Verification	mGluR	Neurological Disease
Ro 01-6128 is a positive allosteric modulator of mGluR1 .

HY-107457

AZD-8529 1 Publications Verification	mGluR	Neurological Disease
AZD-8529 is a potent, highly selective and orally bioavailable positive allosteric modulator of mGluR2, with an EC₅₀ of 285 nM, and shows no positive allosteric modulator responses at 20-25 M on the mGluR1, 3, 4, 5, 6, 7, and 8 subtypes.

Cat. No.	Product Name

HY-L170

Allosteric Modulators (AMs) Compound Library

190 compounds

An emerging drug design method is based on the secondary binding site effect, where small molecule drugs are designed to bind to secondary binding sites on target biomolecules rather than primary orthomorphic sites. Successful potential drugs (known as allosteric modulators) will be able to bind to allosteric sites and remotely alter (or modify) the conformation of the main orthosteric binding sites of biological targets. Allosteric modulators (AMs) are ligands of proteins that act through binding sites different from natural (orthosteric) ligand sites. AMs are relatively small, more lipophilic, and more rigid compounds. The binding efficacy of AMs with their targets is often slightly lower. AMs are divided into positive AMs (PAMs) and negative AMs (NAMs). AMs are ideal drug targets because they can fine-tune receptor activity while preserving the spatial and temporal signal transduction characteristics of endogenous ligands, resulting in fewer targeted side effects, improved subtype selectivity, and better promotion of biased signal transduction than normal ligands.

MCE designs a unique collection of 190 small allosteric modulators. It is a good tool to be used for research on metabolize, cancer and other diseases.

Cat. No.	Product Name	Target	Research Area

HY-126327A

UNC4976 TFA	Histone Methyltransferase	Cancer
UNC4976 TFA is a positive allosteric modulator (PAM) peptidomimetic of CBX7 chromodomain binding to nucleic acids. UNC4976 TFA simultaneously antagonizes H3K27me3-specific recruitment of CBX7 to target genes while increasing non-specific binding to DNA and RNA .

HY-P1397A

RVD-Hpα TFA	Cannabinoid Receptor	Cardiovascular Disease
RVD-Hpα TFA is the N-terminally extended form of human hemopressin that acts as a selective CB1 receptor agonist. RVD-Hpα TFA increases intracellular Ca ²⁺ levels in cells expressing CB1 receptors in vitro. RVD-Hpα TFA also high affinity CB2 positive allosteric modulator (K_i=50 nM).

HY-P1397

RVD-Hpα	Cannabinoid Receptor	Neurological Disease
RVD-Hpα, an α-hemoglobin-derived peptide containing three additional amino acids, is a CB1 cannabinoid receptor agonist. RVD-Hpα is a positive allosteric modulator of cannabinoid receptor 2 .

HY-126327

UNC4976	Histone Methyltransferase	Cancer
UNC4976 is a positive allosteric modulator (PAM) peptidomimetic of CBX7 chromodomain binding to nucleic acids. UNC4976 simultaneously antagonizes H3K27me3-specific recruitment of CBX7 to target genes while increasing non-specific binding to DNA and RNA .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-113346

Tetrahydrodeoxycorticosterone Tetrahydro-11-deoxycorticosterone	Structural Classification Neurological Disease Classification of Application Fields Source classification Endogenous metabolite Disease Research Fields Steroids	GABA Receptor Endogenous Metabolite
Tetrahydrodeoxycorticosterone, an neurosteroid, is a potent positive allosteric modulator (PAM) of GABA_A receptor. Tetrahydrodeoxycorticosterone has potent neuroinhibitory properties .

HY-N2370

24-Hydroxycholesterol 1 Publications Verification	Structural Classification Animals Source classification Steroids	iGluR LXR
24-Hydroxycholesterol is a natural sterol, which serves as a positive allosteric modulator of N-Methyl-d-Aspartate (NMDA) receptorsR, and a potent activator of the transcription factors LXR.

HY-113320

Etiocholanolone 5β-Androsterone	Structural Classification Microorganisms Source classification Endogenous metabolite Steroids	GABA Receptor Endogenous Metabolite
Etiocholanolone (5β-Androsterone) is the excreted metabolite of testosterone and has anticonvulsant activity . Etiocholanolone is a less potent?neurosteroid positive allosteric modulator?(PAM) of the GABA_A?receptor than its?enantiomer form .

HY-107198

(2S)-6-Prenylnaringenin 1 Publications Verification	Structural Classification Flavonoids Humulus lupulus L. Flavonones Source classification Phenols Polyphenols Plants Moraceae	GABA Receptor
(2S)-6-Prenylnaringenin is the most efficient compound in forebrain. (2S)-6-Prenylnaringenin acts as a GABA_A positive allosteric modulator at α+β- binding interface .

HY-16940

24(S)-Hydroxycholesterol 24S-OHC; 24S-HC; Cerebrosterol	Structural Classification Classification of Application Fields Source classification Disease markers Metabolic Disease Nervous System Disorder Endogenous metabolite Disease Research Fields Steroids	LXR iGluR Endogenous Metabolite
24(S)-Hydroxycholesterol (24S-OHC), the major brain cholesterol metabolite, plays an important role to maintain homeostasis of cholesterol in the brain. 24(S)-Hydroxycholesterol (24S-OHC) is one of the most efficient endogenous LXR agonist known and is present in the brain and in the circulation at relatively high levels. 24(S)-Hydroxycholesterol (24S-OHC) is a very potent, direct, and selective positive allosteric modulator of NMDARs with a mechanism that does not overlapthat of other allosteric modulators .

Cat. No.	Product Name	Chemical Structure

HY-113346S

Tetrahydrodeoxycorticosterone-d3 1 Publications Verification
Tetrahydrodeoxycorticosterone-d₃ is the deuterium labeled Tetrahydrodeoxycorticosterone. Tetrahydrodeoxycorticosterone, an neurosteroid, is a potent positive allosteric modulator (PAM) of GABAA receptor. Tetrahydrodeoxycorticosterone has potent neuroinhibitory properties[1][2][3].

HY-113320S

Etiocholanolone-d5
Etiocholanolone-d₅ is the deuterium labeled Etiocholanolone. Etiocholanolone (5β-Androsterone) is the excreted metabolite of testosterone and has anticonvulsant activity[1]. Etiocholanolone is a less potent neurosteroid positive allosteric modulator (PAM) of the GABAA receptor than its enantiomer form[2].

HY-15831

L-838417-d9
L-838417-d₉ is the deuterium labeled L-838417. L-838417 is a subtype-selective GABAA positive allosteric modulator, acting as a partial agonist at α2, α3 and α5 subtypes[1].

HY-14774S

(Rac)-Monepantel-d5
(Rac)-Monepantel-d₅ is deuterium labeled Monepantel. Monepantel is organic anthelmintic, and acts as a positive allosteric modulator of a nematode-specific clade of nicotinic acetylcholine receptor (nAChR) subunits.

HY-14774S1

(Rac)-Monepantel sulfone-d5
(Rac)-Monepantel sulfone-d₅ is deuterium labeled Monepantel. Monepantel is organic anthelmintic, and acts as a positive allosteric modulator of a nematode-specific clade of nicotinic acetylcholine receptor (nAChR) subunits.

HY-10933S

CX516-d10
CX516-d₁₀ is the deuterium labeled CX516. CX516 (BDP 12) is an ampakine and acts as an AMPA receptor positive allosteric modulator for the research of Alzheimer's disease, schizophrenia and mild cognitive impairment (MCI)[1].

HY-113320S1

Etiocholanolone-d2
Etiocholanolone-d₂ is the deuterium labeled Etiocholanolone. Etiocholanolone (5β-Androsterone) is the excreted metabolite of testosterone and has anticonvulsant activity[1]. Etiocholanolone is a less potent neurosteroid positive allosteric modulator (PAM) of the GABAA receptor than its enantiomer form[2][3].

HY-16579AS2

Etifoxine-d5
Etifoxine-d₅ is the deuterium labeled Etifoxine. Etifoxine, a non-benzodiazepine GABAergic compound, is a positive allosteric modulator of α1β2γ2 and α1β3γ2 subunit-containing GABAA receptors. Etifoxine reveals anxiolytic and anticonvulsant properties in rodents[1][2][3].

Cat. No.	Product Name		Classification

HY-118022

VU0361747		Alkynes
VU0361747 is a potent and selective positive allosteric modulator of metabotropic glutamate receptor 4 (mGluR4?PAM). VU0361737 has neuroprotective effect. VU0361737 significantly reverses Amphetamine-induced hyperlocomotion in vivo .

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