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Allosteric modulator

" in MedChemExpress (MCE) Product Catalog:

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322

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Cat. No.	Product Name	Target	Research Areas	Chemical Structure

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-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-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-103503

CGP13501

GABA Receptor Neurological Disease

CGP13501 is a positive allosteric modulator of GABAB receptor. CGP13501 is a structural analogue of propofol .
HY-119765

VU0366248

mGluR Neurological Disease

VU0366248 is a mGlu5 negative allosteric modulator .
HY-116067

VU0404251

mGluR Neurological Disease

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

CGP13501	GABA Receptor	Neurological Disease
CGP13501 is a positive allosteric modulator of GABAB receptor. CGP13501 is a structural analogue of propofol .

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

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-103497

U-89843A

GABA Receptor Neurological Disease

U-89843A is an allosteric modulator of GABAA receptor. U-89843A enhances GABA-induced Cl ^- currents .

U-89843A	GABA Receptor	Neurological Disease
U-89843A is an allosteric modulator of GABAA receptor. U-89843A enhances GABA-induced Cl ^- currents .

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-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-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 .

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-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-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-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 .

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-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-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 .

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-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-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-100605

VU0483605	mGluR	Others
VU0483605 is a potent and brain-penetrated mGlu₁ receptor positive allosteric modulator (PAM). VU0483605 shows excellent mGlu₁ PAM activity at both human and rat, with EC₅₀ values of 390 and 356 nM, respectively .

HY-10933

CX516 1 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-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-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-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-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-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-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-147260B

(Rac)-Dalzanemdor (Rac)-SAGE-718	TRP Channel	Neurological Disease
(Rac)-Dalzanemdor ((Rac)-SAGE-718) is an isomer of Dalzanemdor (HY-147260). Dalzanemdor is an orally active and highly intrinsically active N-methyl-d-aspartate receptor (NMDAR)-positive allosteric modulator (PAM). Dalzanemdor can be used in the research of Huntington's disease .

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-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-118301

ADX71441	GABA Receptor	Neurological Disease
ADX71441 is a potent and selective positive allosteric modulator of the GABA_B receptor. ADX71441 is bioavailable after oral administration and is brain penetrant. ADX71441 has the potential for research of anxiety, pain and spasticity .

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-121736

AGI-12026 AGI-026	Isocitrate Dehydrogenase (IDH)	Neurological Disease
AGI-12026 is brain-penetrant dual inhibitor of mutant IDH1 and 2. AGI-12026 shows partial inhibition of the IDH1-R132H homodimer as allosteric modulators. AGI-12026 has the potential for research of glioma .

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-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-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-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-117734

PYD-106	iGluR	Neurological Disease
PYD-106 is a stereoselective pyrrolidinone (PYD) positive allosteric modulator for GluN2C-containing NMDA receptors. PYD-106 increases opening frequency and open time of single channel currents activated by maximally effective concentrations of agonist but only has modest effects on glutamate and glycine EC₅₀. PYD-106 selectively enhances the responses of diheteromeric GluN1/GluN2C receptors but not triheteromeric GluN1/GluN2A/GluN2C receptors .

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-144705

GAT564	Cannabinoid Receptor	Neurological Disease
GAT564 (Compound 15d) is a potent allosteric modulator of cannabinoid 1 receptor (CB1R) with EC₅₀s of 87 and 320 nM respectively for cAMP and β-arrestin2. GAT564 markedly promotes orthosteric ligand binding to hCB1R. GAT564 is efficacious as a topical agent that significantly reduces intraocular pressure (IOP) in the ocular normotensive murine model of glaucoma .

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-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-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-114314

BA-53038B	HBV	Infection
BA-53038B is a *HBV core protein allosteric* modulator (CpAM)*, binding to the HAP pocket and modulating* HBV capsid assembly. BA-53038B has antiviral activity for hepatitis B virus (HBV) with an EC₅₀ value of 3.32 μM. BA-53038B can be used for the research of chronic hepatitis B .

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-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-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 .

Cat. No.	Product Name	Target	Research Area

HY-107663A

MIF-1 TFA Pro-Leu-Gly-NH2 TFA; Melanostatin TFA	Dopamine Receptor	Neurological Disease
MIF-1 TFA (Melanostatin), an endogenous brain peptide, is a potent dopamine receptor allosteric modulator. MIF-1 TFA inhibits melanin formation. MIF-1 TFA blocks the effects of opioid receptor activation to modulate the analgesic effects. MIF-1 TFA accesses from the blood to the CNS by directly crossing the blood-brain barrier (BBB) .

HY-P5860

MmTx1 toxin Micrurotoxin 1	GABA Receptor	Neurological Disease
MmTx1 toxin (Micrurotoxin 1) is an allosteric GABA_A receptor modulator that increases GABA_A receptor susceptibility to agonist .

HY-107663

MIF-1 Pro-Leu-Gly-NH2; Melanostatin	Dopamine Receptor	Neurological Disease
MIF-1 (Melanostatin), an endogenous brain peptide, is a potent dopamine receptor allosteric modulator. MIF-1 inhibits melanin formation. MIF-1 blocks the effects of opioid receptor activation to modulate the analgesic effects. MIF-1 accesses from the blood to the CNS by directly crossing the blood-brain barrier (BBB) .

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-103502

CGP7930	GABA Receptor	Neurological Disease
CGP7930 (3-(3’,5’-Di-tert-butyl-4’-hydroxy) phenyl-2, 2-dimethylpropanol) is a positive metabotropic GABAB receptor allosteric modulator. CGP7930 enhances the inhibitory effect of l-baclofen on the oscillatory activity of cultured cortical neurons .

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 .

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
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-P5839

α-Conotoxin MrIC	nAChR	Neurological Disease
α-Conotoxin MrIC is an α7nAChR biased agonist. α-Conotoxin MrIC exclusively activates α7nAChR regulated by type II positive allosteric modulators, including PNU120596. α-Conotoxin MrIC can be used to study neurological diseases and also to probe the pharmacological properties of α7nAChR .

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	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 .

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-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-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-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].

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Allosteric modulator

Inhibitors & Agonists

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