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positive modulator

" in MedChemExpress (MCE) Product Catalog:

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Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-A0106

Levamisole 10+ Cited Publications (-)-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-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-120645

BMS-986122 1 Publications Verification	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-101165

Cyclothiazide 2 Publications Verification	iGluR GABA Receptor	Neurological Disease
Cyclothiazide is a positive allosteric modulator of ionotropic AMPA-type glutamate receptors. Cyclothiazide inhibits GABA_A receptors. Cyclothiazide is frequently used to produce a fast inhibition of AMPA receptor desensitization and a much slower potentiation of the AMPA current. Cyclothiazide can potentiate responses to kainate in hippocampal neurons. Cyclothiazide has effects on glutamatergic neurotransmission. Cyclothiazide also induces epileptiform EEG activity accompanying behavioral seizures .

HY-108584

Flindokalner BMS-204352	Potassium Channel	Neurological Disease
Flindokalner (BMS-204352) is a potassium channel modulator. Flindokalner is a positive modulator of all neuronal Kv7 channel subtypes expressed in HEK293 cells. Flindokalner is also a large conductance calcium-activated K channel (BKca) positive modulator. Flindokalner shows a negative modulatory activity at Kv7.1 channels (K_i=3.7 μM), and acts as a negative modulator of GABAA receptors. Flindokalner shows anxiolytic efficacy in vivo .

HY-139580

Plazinemdor CAD-9303	iGluR	Neurological Disease
Plazinemdor (CAD-9303) is a positive allosteric modulator of N-methyl-D-aspartate (NMDA) receptors, which is used in the research of neurological diseases .

HY-159829

Direclidine NBI-1117568; HTL-0016878	mAChR	Neurological Disease
Direclidine (NBI-1117568, HTL-0016878) is a selective orthosteric agonist targeting the muscarinic acetylcholine M4 receptor, exhibiting very low affinity for M1, M2, M3, and M5 receptors. It binds to the orthosteric site of the M4 receptor in a non-covalent, competitive manner. Direclidine specifically activates the M4 receptor, inhibiting the release of acetylcholine from striatal cholinergic interneurons, thereby regulating the balance of the dopaminergic system and reducing psychiatric symptoms associated with excessive dopamine release. Direclidine can improve symptoms associated with neuropsychiatric disorders and is used in research on schizophrenia and other neuropsychiatric disorders .

HY-19559

JNJ-46778212 VU 0409551	mGluR	Neurological Disease
JNJ-46778212 (VU 0409551) is an mGlu5 positive allosteric modulator with an EC₅₀ of 260 nM.

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-116819

VU0453379	GCGR	Neurological Disease Metabolic Disease
VU0453379 is a blood-brain barrier permeable GLP-1R positive allosteric modulator (PAM) with an EC₅₀ value of 1.3 μM. VU0453379 potentiates the actions of endogenous GLP-1 and synthetic peptide agonists, and promotes GLP-1 receptor internalization. VU0453379 stimulates insulin secretion from primary mouse islets. VU0453379 enhances the function of endogenous GLP-1R and reverses catalepsy in animal models. VU0453379 is useful for research on Parkinson's disease and type 2 diabetes .

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-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.

HY-120023

VU0453595 2 Publications Verification	mAChR	Neurological Disease
VU0453595 is a highly selective, systemically active M₁ positive allosteric modulator (PAM, EC₅₀=2140 nM) for the research of schizophrenia .

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-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-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-177873

AMPA receptor modulator-10	iGluR	Neurological Disease
AMPA receptor modulator-10 (Compound 9a) is an orally active AMPA receptor (AMPAR) positive allosteric modulator. AMPA receptor modulator-10 exhibits potent activity (pEC₅₀ = 5.0) on the GluA2 subtype of AMPAR, significantly enhancing glutamate-induced calcium influx and current responses. AMPA receptor modulator-10 can reverse the memory impairment induced by Scopolamine (HY-N0296) and enhance cognitive function. AMPA receptor modulator-10 can be used for the research of neurological disease, such as schizophrenia .

HY-103668A

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

HY-105272

Loreclezole R 72063	GABA Receptor	Neurological Disease
Loreclezole, an antiepileptic compound, is a selective GABA_A receptor modulator and acts as a positive allosteric modulator of β2 or β3-subunit containing receptors .

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-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-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-110122

AZ 12216052 1 Publications Verification	mGluR	Neurological Disease
AZ 12216052 is a mGluR8 positive allosteric modulator, and helps mGluR8 modulate signaling inputing to retinal ganglion cells. AZ 12216052 exhibits antianxiety effect .

HY-10937

Farampator CX-691; Org24448	iGluR	Neurological Disease
Farampator (CX-691;Org24448) is an AMPA receptor positive modulator.

HY-121848

VU0155094 ML397	mGluR	Neurological Disease
VU0155094 is a positive allosteric modulator with differential activity at the various group III mGluRs .

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-177498

M1 mAChR modulator-1	mAChR	Neurological Disease
M1 mAChR modulator-1 (Example 66) is a muscarinic M1 receptor (mAChR1) positive allosteric modulator. M1 mAChR modulator-1 effectively promotes gastrointestinal motility and defecation in mouse models with low central permeability. M1 mAChR modulator-1 can be used for constipation research .

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-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-101216

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

HY-107457A

AZD-8529 mesylate 1 Publications Verification	mGluR	Neurological Disease
AZD-8529 mesylate 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 .

HY-121806

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

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-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-112567

TRR469	Adenosine Receptor	Neurological Disease
TRR469 is a positive allosteric modulator of the A₁ adenosine receptor (A₁AR). TRR469 significantly increases the affinity of 2-chloro N(6)-cyclopentyladenosine (CCPA) for A₁AR, increasing the number of receptors recognized by the agonist radioligand [³H]-CCPA. TRR469 shows significant effects in both anxiety and pain models. TRR469 can be used to study anxiety disorders and pain management .

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-107507

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

HY-15476

VU 0364439	mGluR	Neurological Disease
VU 0364439 is a mGlu4 positive allosteric modulator (PAM), with EC50 of 19.8 nM.

HY-118416

BMS-986124	Opioid Receptor	Neurological Disease
BMS-986124 is a μ-opioid receptor silent allosteric modulator (μ-SAMs). BMS-986124 antagonizes positive allosteric modulator effect of BMS-986122 (µ-OR PAM) .

HY-159826

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

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-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-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-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-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-179108

NMDAR modulator 1	iGluR	Neurological Disease
NMDAR modulator 1 (Compound 12) is a positive, allosteric GluN1/GluN2B receptor modulator. NMDAR modulator 1 enhances NMDAR current. NMDAR modulator 1 can be used in the research of psychiatric disorders .

HY-121393

Imidazenil	GABA Receptor	Neurological Disease
Imidazenil is a partial positive allosteric modulator of GABA_A receptors with anxiolytic, antipanic and anticonvulsant activities.

HY-123874

BMS-952048	mGluR	Neurological Disease
BMS-952048 is a positive allosteric modulator of mGluR5 with an EC₅₀ of 10 nM .

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 .

Cat. No.	Product Name

HY-L170

Allosteric Modulators (AMs) Compound Library

250 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 250 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-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-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-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-P11258

UPG-108	Urotensin Receptor	Cardiovascular Disease Metabolic Disease Inflammation/Immunology Cancer
UPG-108, a peptide compound, is a non-competitive allosteric modulator of Urotensin II receptors (UTR). UPG-108 significantly enhances the efficacy of UTR agonists but reduces the potency of UTR agonists. UPG-111 efficiently induces calcium release and does not cause contraction of rat aortic rings without endothelial denudation. UPG-111 can be used to study various diseases related to the angiotensinergic system .

Cat. No.	Product Name	Target	Research Area	Image

HY-P992360

GT-002	GABA Receptor	Neurological Disease Cancer
GT-002 is a partial positive allosteric modulator targeting the α3 subtype of GABAA receptors, as well as a specific binder of tumor-associated TF-glycosylated LYPD3. GT-002 mildly enhances GABA-induced chloride currents by binding to the benzodiazepine site of GABAA receptors, thereby alleviating prefrontal hypofunction and improving cognitive, memory and social interaction abilities. GT-002 can be used in research related to schizophrenia spectrum disorders, various squamous cell carcinomas, colorectal cancer, non-small cell lung cancer, and aromatic L-amino acid decarboxylase deficiency .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N6871

Abietic acid 3 Publications Verification	Infection Colophony Classification of Application Fields Pinaceae Ketones, Aldehydes, Acids Metabolic Disease Plants Inflammation/Immunology Disease Research Fields	Bacterial IKK Ferroptosis
Abietic acid, an orally active diterpene isolated from Colophony, displays significant anti-proliferative, anti-inflammatory, anti-obesity effect, bacteriostatic, cell cycle arresting and pro-apoptotic activities. Abietic acid inhibits lipoxygenase activity for allergy. Abietic acid enhances cell migration and tube formation in HUVECs. Abietic acid induces significant angiogenic potential, which is associated with upregulation of extracellular signal-regulated kinase (ERK) and p38 expression. Abietic acid attenuates sepsis-induced lung injury by inhibiting nuclear factor kappa-light-chain-enhancer of activated B cells (NF-κB) pathway to inhibit M1 macrophage polarization. Abietic acid exhibits a positive effect against liver injury by attenuating inflammation and ferroptosis. Abietic acid shows accelerated wound closure in a mouse model of cutaneous wounds. Abietic acid significantly reduces the proliferation and growth of NSCLC cells by IKKβ inhibition.Additionally, Abietic acid ameliorates psoriasis-like inflammation and modulates gut microbiota in mice. Abietic acid is promising for research in non-small-cell lung cancer (NSCLC), liver injury-related deseases and psoriasis .

HY-16940

24(S)-Hydroxycholesterol 24S-OHC; 24S-HC; Cerebrosterol	Classification of Application Fields Disease markers Metabolic Disease Nervous System Disorder Endogenous metabolite Disease Research Fields Steroids Source Classification	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 .

HY-Y1683

DL-Menthol Racementhol	Structural Classification Natural Products Classification of Application Fields Leguminosae Labiatae Other Diseases Erythrina poeppigiana Plants Glycyrrhiza uralensis Fisch. Disease Research Fields Source Classification	Environmental Pollutants GABA Receptor
DL-Menthol (Racementhol) is an orally active, GABA_aR positive allosteric modulator and UDP-glucuronosyltransferase (UGT) inhibitor that can cross the blood-brain barrier. DL-Menthol binds to GABA_AR and exhibits an allosteric activation effect, enhancing GABA-mediated chloride influx and inhibiting neuronal excitability. DL-Menthol can induce surgical anesthesia in fish and inhibit the metabolic detoxification of tobacco carcinogens by human liver and intestinal UGT enzymes, resulting in reduced NNAL-N-Gluc production .

HY-112171

γ-L-Glutamyl-L-alanine 1 Publications Verification γ-Glu-Ala	Natural Products Human Gut Microbiota Metabolites Classification of Application Fields Other Diseases Endogenous metabolite Disease Research Fields Source Classification	Endogenous Metabolite CaSR
γ-L-Glutamyl-L-alanine (γ-Glu-Ala), composed of gamma-glutamate and alanine, is a proteolytic breakdown product of larger proteins. γ-L-Glutamyl-L-alanine is a natural substrate of the γ-Glutamylcyclotransferase. γ-L-Glutamyl-L-alanine is a positive modulator of calcium-sensing receptor (CaR) function .

HY-N2370

24-Hydroxycholesterol 3 Publications Verification	Animals Steroids Source Classification	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	Microorganisms Endogenous metabolite Steroids Source Classification	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	Flavonoids Humulus lupulus L. Flavonones Phenols Polyphenols Plants Moraceae Source Classification	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-N6084

Humulone α-Lupulic acid	Cardiovascular Disease Classification of Application Fields Ketones, Aldehydes, Acids Humulus lupulus L. Plants Moraceae Disease Research Fields Source Classification	COX GABA Receptor Apoptosis
Humulone (α-Lupulic acid), a prenylated phloroglucinol derivative, is a potent cyclooxygenase-2 (COX-2) inhibitor. Humulone acts as a positive modulator of GABA_A receptor at low micromolar concentrations. Humulone is an inhibitor of bone resorption. Humulone possesses antioxidant, anti-angiogenic and apoptosis-inducing properties .

HY-113346

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

HY-N2370R

24-Hydroxycholesterol (Standard)	Structural Classification Animals Steroids Source Classification	Reference Standards 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-N15339

Convolamine	Alkaloids Convolvulus krauseanus Regel & Schmalh. Quinoline Alkaloids Plants Convolvulaceae Source Classification	Sigma Receptor
Convolamine is an alkaloid found in Convolvulus pluricaulis and an effective positive modulator of the sigma-1 receptor (IC₅₀ = 289 nM), exhibiting cognitive and neuroprotective properties .

HY-N4157

Isopteropodine	Uncaria rhynchophylla (Miq.) Miq. ex Havil. Structural Classification Iridoids Terpenoids Rubiaceae Plants Source Classification	mAChR 5-HT Receptor Bacterial
Isopteropodine is a positive modulator that selectively acts on muscarinic M₁ and 5-HT₂ receptors. Isopteropodine has an EC₅₀ of 9.92 μM for acetylcholine and 14.5 μM for 5-HT. Isopteropodine also has antibacterial activity against Gram-positive bacteria, with MICs of 150 μg/mL and 250 μg/mL for Staphylococcus aureus and Bacillus subtilis, respectively. Isopteropodine enhances receptor function by increasing the affinity of agonists for receptors and can also inhibit the growth of specific Gram-positive bacteria, and can be used in cognitive impairment and antibacterial research .

HY-112171R

γ-L-Glutamyl-L-alanine (Standard) γ-Glu-Ala (Standard)	Structural Classification Natural Products Human Gut Microbiota Metabolites Endogenous metabolite Source Classification	Endogenous Metabolite CaSR Reference Standards
γ-L-Glutamyl-L-alanine (Standard) is the analytical standard of γ-L-Glutamyl-L-alanine. This product is intended for research and analytical applications. γ-L-Glutamyl-L-alanine, composed of gamma-glutamate and alanine, is a proteolytic breakdown product of larger proteins. γ-L-Glutamyl-L-alanine is a natural substrate of the γ-Glutamylcyclotransferase. γ-L-Glutamyl-L-alanine is a positive modulator of calcium-sensing receptor (CaR) function .

HY-N4157R

Isopteropodine (Standard)	Uncaria rhynchophylla (Miq.) Miq. ex Havil. Structural Classification Iridoids Terpenoids Rubiaceae Plants Source Classification	Reference Standards mAChR 5-HT Receptor Bacterial
Isopteropodine (Standard) is the analytical standard of Isopteropodine (HY-N4157). This product is intended for research and analytical applications. Isopteropodine is a positive modulator that selectively acts on muscarinic M₁ and 5-HT₂ receptors. Isopteropodine has an EC₅₀ of 9.92 μM for acetylcholine and 14.5 μM for 5-HT. Isopteropodine also has antibacterial activity against Gram-positive bacteria, with MICs of 150 μg/mL and 250 μg/mL for Staphylococcus aureus and Bacillus subtilis, respectively. Isopteropodine enhances receptor function by increasing the affinity of agonists for receptors and can also inhibit the growth of specific Gram-positive bacteria, and can be used in cognitive impairment and antibacterial research .

HY-N15339A

Convolamine hydrochloride	Structural Classification Alkaloids Microorganisms Tropane Alkaloids Source Classification	Sigma Receptor
Convolamine hydrochloride is a tropane alkaloid and a potent Sigma-1 receptor positive allosteric modulator with an IC₅₀ value of 289 nM. Convolamine hydrochloride can be extracted from Convolvulus plauricalis. Convolamine hydrochloride exhibits cognitive-improving and neuroprotective properties. Convolamine hydrochloride can be used in research related to Wolfram syndrome and Alzheimer's disease .

HY-W097625R

6-Methoxyflavone (Standard)	Structural Classification Flavonoids Flavones Thymelaeaceae Plants Pimelea simplex F.Muell. Source Classification	Toll-like Receptor (TLR) MyD88 p38 MAPK NF-κB Heme Oxygenase (HO) Reference Standards PERK
6-Methoxyflavone (Standard) is the analytical standard of 6-Methoxyflavone (HY-W097625). This product is intended for research and analytical applications. 6-Methoxyflavone is an orally active methoxyflavone. 6-Methoxyflavone suppresses neuroinflammation in microglia through the inhibition of TLR4/MyD88/p38 MAPK/NF-κB dependent pathways and the activation of HO-1/NQO-1 signaling. 6-Methoxyflavone induces S-phase arrest through the CCNA2/CDK2/p21CIP1 signaling pathway and activates the PERK/EIF2a/ATF4/CHOP pathway in HeLa cells. 6-Methoxyflavone acts as a Flumazenil (HY-B0009)-insensitive positive allosteric modulator at human recombinant α1β2γ2L and α2β2γ2L GABAα receptors. 6-Methoxyflavone inhibits NFAT Translocation into the nucleus and suppresses T cell activation. 6-Methoxyflavone partially restores chronic ethanol-induced behavioral deficits in mice. 6-Methoxyflavone antagonizes chronic constriction injury and diabetes associated neuropathic nociception expression. 6-Methoxyflavone can be used for the study of cancer, inflammation and neurological diseases .

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 .

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-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-113320S

Etiocholanolone-d5
Etiocholanolone-d₅ is the deuterium labeled Etiocholanolone. 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 GABAA?receptor than its?enantiomer form .

HY-W777503

Calindol hydrochloride-13C,D2
Calindol hydrochloride- ¹³C,d₂ is the deuterium and ¹³C labeled Calindol hydrochloride (HY-122819). Calindol hydrochloride is a positive allosteric modulator (PAM) of calcimimetic calcium-sensing receptor (CaSR) with an EC₅₀ of 132 nM .

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) .

HY-113320S1

Etiocholanolone-d2
Etiocholanolone-d₂ is the deuterium labeled Etiocholanolone. 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 GABAA?receptor than its?enantiomer form .

HY-W725476

Bifenazate-d5
Bifenazate-d₅ is the deuterium labeled Bifenazate (HY-119687). Bifenazate is a carbazate acaricide that control 100% of mites at a concentration of 25 ppm . Bifenazate is a positive allosteric modulator of GABA receptor . Bifenazate is the inhibitor for the mitochondrial electron transport chain complex III .

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 .

HY-173251S

ENX-101
ENX-101 is an orally active (GABA_A) receptor partial positive allosteric modulator (PAM). ENX-101 is selective to α2β2γ2L (EC₅₀ = 0.76 nM), α2β3γ2L (EC₅₀ = 0.61 nM), α3 (EC₅₀ = 1.97 nM), α5 (EC₅₀ = 0.85 nM) subunits of GABA receptor. ENX-101 possesses antiseizure activity in several animal models .

HY-B1456AS

Fenoprofen-13C6 sodium hydrate

Fenoprofen- ¹³C₆ (LILLY-53858- ¹³C₆) sodium hydrate is the ¹³C labeled Fenoprofen (HY-B1456A).Fenoprofen (LILLY-53858) is a nonsteroidal anti-inflammatory agent (NSAID) and inhibits cyclooxygenase (COX). Fenoprofen is a melanocortin receptors (MCRs) positive allosteric modulator (PAM). Fenoprofen also increases ERK1/2 activation in HEK293T cells. Fenoprofen has anti-arthritic activities and can be used for the study of rheumatoid arthritis and osteoarthritis .

HY-167922S

Heptadecanoyl L-carnitine-d3 HCl

Heptadecanoyl L-carnitine-d₃ HCl is the deuterium labeled (R,R,S)-GAT107 (HY-167922). (R,R,S)-GAT107 is a fully agonistic positive modulator of α7 nicotinic receptors with significant biological activity. Its activity is entirely present in its (+)-isomer 1b, while (-)-isomer 1a does not affect its activity when used together. Studies have shown that (R,R,S)-GAT107 is the most potent ago-PAM for α7 nicotinic receptors currently known and has the potential for further in vivo evaluation .

HY-123489S

3α,21-Dihydroxy-5α-pregnan-20-one-d3
3α,21-Dihydroxy-5α-pregnan-20-one-d₃ is the deuterium labeled 3α,21-Dihydroxy-5α-pregnan-20-one. 3α,21-Dihydroxy-5α-pregnan-20-one (THDOC), an endogenous neurosteroid, is a positive modulator of GABAA receptors. 3α,21-Dihydroxy-5α-pregnan-20-one potentiates neuronal response to low concentrations of GABA at α4β1δ GABAA receptors in vitro.

HY-110168S

NS 9283-d4
NS 9283-d₄ is the deuterium labeled NS 9283 (HY-110168). NS 9283 is a positive positive allosteric modulator of (α4)₃(β2)₂ nicotinic ACh receptors. NS 9283 can be used in a series of neurological conditions such as attention deficit hyperactivity disorder (ADHD), schizophrenia, Parkinson's disease and Alzheimer's disease .

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 .

HY-171333

TMEM16A modulator-1		Alkynes
TMEM16A modulator-1 (compound 36) is a positive modulator of the calcium-activated chloride channel (CaCC) TMEM16A. TMEM16A modulator-1 can be used for TMEM16A-related diseases research, particularly respiratory diseases and conditions .

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