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Results for "

orthosteric

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Adenosine Receptor (2) Antibiotic (1) Apoptosis (3) Cannabinoid Receptor (3) Endogenous Metabolite (1) JAK (1) LPL Receptor (1) mAChR (2) mGluR (6) nAChR (3) Opioid Receptor (1) PPAR (1) Prostaglandin Receptor (1) RAD51 (1) Raf (1) Ras (1)
By Research Areas:	Cancer (3) Cardiovascular Disease (3) Infection (3) Inflammation/Immunology (2) Metabolic Disease (1) Neurological Disease (10)

Inhibitors & Agonists

Screening Libraries

Peptides

Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-145299

nAChR modulator-1

nAChR Infection

nAChR modulator-1, a insecticide, is a insect nAChR orthosteric modulator .
HY-145300

nAChR modulator-2

nAChR Infection

nAChR modulator-2, a insecticide, is a insect nAChR orthosteric modulator .

nAChR modulator-1	nAChR	Infection
nAChR modulator-1, a insecticide, is a insect nAChR orthosteric modulator .

nAChR modulator-2	nAChR	Infection
nAChR modulator-2, a insecticide, is a insect nAChR orthosteric modulator .

HY-103549

Z-Cyclopentyl-AP4	mGluR	Neurological Disease
Z-Cyclopentyl-AP4 is a kainate-type glutamate receptor agonist (orthosteric agonist). Z-Cyclopentyl-AP4 is more selective for mGlu4 than mGlu8 .

HY-116569

VU0455691

mAChR Cardiovascular Disease

VU0455691 is a potent, selective orthosteric M₁ mAChR antagonist (pIC₅₀=6.64; IC₅₀=0.23 µM for hM1) .

VU0455691	mAChR	Cardiovascular Disease
VU0455691 is a potent, selective orthosteric M₁ mAChR antagonist (pIC₅₀=6.64; IC₅₀=0.23 µM for hM1) .

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-W011417

Cinnabarinic acid	mGluR Apoptosis	Others
Cinnabarinic acid is a specific orthosteric agonist of mGlu₄ by interacting with residues of the glutamate binding pocket of mGlu4, has no activity at other mGlu receptors. Cinnabarinic acid is an endogenous metabolite of the kynurenine pathway of tryptophan. Cinnabarinic acid induces cell apoptosis .

HY-13239

LY2979165

mGluR Neurological Disease

LY2979165 is the alanine proagent of 2812223, a selective and potent orthosteric mGlu2 receptor agonist .
HY-112247

SR 16832

PPAR Metabolic Disease

SR 16832 is a dual site covalent PPARγ inhibitor that acts at orthosteric and allosteric sites .
HY-138694

5-Benzyloxygramine

Antibiotic Infection

5-Benzyloxygramine is a N protein PPI orthosteric stabilizer that exhibits both antiviral and N-NTD protein-stabilizing activities .
HY-P10051

Cyclorasin 9A5

Ras Raf Cancer

Cyclorasin 9A5 is an 11-residue cell-permeable cyclic peptide that orthosterically inhibits the Ras-Raf protein interaction with an IC₅₀ of 120 nM .

LY2979165	mGluR	Neurological Disease
LY2979165 is the alanine proagent of 2812223, a selective and potent orthosteric mGlu2 receptor agonist .

SR 16832	PPAR	Metabolic Disease
SR 16832 is a dual site covalent PPARγ inhibitor that acts at orthosteric and allosteric sites .

5-Benzyloxygramine	Antibiotic	Infection
5-Benzyloxygramine is a N protein PPI orthosteric stabilizer that exhibits both antiviral and N-NTD protein-stabilizing activities .

Cyclorasin 9A5	Ras Raf	Cancer
Cyclorasin 9A5 is an 11-residue cell-permeable cyclic peptide that orthosterically inhibits the Ras-Raf protein interaction with an IC₅₀ of 120 nM .

HY-119943B

(R)-PF-06256142	Others	Neurological Disease
(R)-PF-06256142 is the R enantiomer of PF-06256142 with low active. PF-06256142 is a potent and selective orthosteric D1 receptor agonist that can reduce receptor desensitization relative to dopamine and other catechol-containing agonists .

HY-103551A

LY 541850	mGluR	Neurological Disease
LY 541850 is claimed from human ionotropic and metabotropic glutamate (mGlu) receptors expressed in non-neuronal cells. LY541850 is a selective orthosteric mGlu2 agonist and mGlu3 antagonist with IC₅₀ values of 0.161 μM and 0.038 μM, respectively .

HY-10915

LUF6096	Adenosine Receptor	Cardiovascular Disease
LUF6096, a potent allosteric enhancer of the adenosine A3 receptor, is able to allosterically enhance agonist binding. LUF6096 shows low orthosteric affinity for any of the adenosine receptors. LUF6096 shows protective effects in myocardial ischemia/reperfusion injury .

HY-142972

19(S)-HETE	Prostaglandin Receptor	Cardiovascular Disease
19(S)-HETE is an arachidonic acid metabolite produced by cytochrome P450 enzymes. 19(S)-HETE is a full orthosteric agonist of the prostacyclin (IP) receptor with an EC₅₀ value of 567 nM. 19(S)-HETE inhibits platelet activation and relaxation of vessels .

HY-150147

CAM833	RAD51 Apoptosis	Cancer
CAM833 is a potent orthosteric inhibitor of the interaction between BRCA2 and RAD51 with a K_d of 366 nM against the ChimRAD51 protein. CAM833 also inhibits RAD51 oligomerization. CAM833 increases the progression of G2/M-arrested cells into apoptosis .

HY-W011417R

Cinnabarinic acid (Standard)	Endogenous Metabolite mGluR Apoptosis	Others
Cinnabarinic acid (Standard) is the analytical standard of Cinnabarinic acid. This product is intended for research and analytical applications. Cinnabarinic acid is a specific orthosteric agonist of mGlu₄ by interacting with residues of the glutamate binding pocket of mGlu4, has no activity at other mGlu receptors. Cinnabarinic acid is an endogenous metabolite of the kynurenine pathway of tryptophan. Cinnabarinic acid induces cell apoptosis .

HY-12150

CCMI AVL-3288; UCI-4083	nAChR	Neurological Disease
CCMI (AVL-3288) is a potent and selective α7 nAChR-positive allosteric modulator, does not bind to or activate α7 nAChRs via the orthosteric site, and causes significant positive modulation of agonist-induced currents at α7 nAChRs. CCMI has potential in CNS diseases with cognitive dysfunction .

HY-117764

LSP4-2022	mGluR	Neurological Disease
LSP4-2022 is a potent and brain-penetrant mGlu4-selective orthosteric agonist, with an EC₅₀ of 0.11 μM. LSP4-2022 inhibits neurotransmission in cerebellar slices from wild-type but not mGlu4 receptor-knockout mice. LSP4-2022 shows pro-depressant activity .

HY-117444

ONO-9780307

LPL Receptor Cancer

ONO-9780307 is a specific synthetic LPA1 (lysophosphatidic acid receptor 1) antagonist with an IC₅₀ value of 2.7 nM .

ONO-9780307	LPL Receptor	Cancer
ONO-9780307 is a specific synthetic LPA1 (lysophosphatidic acid receptor 1) antagonist with an IC₅₀ value of 2.7 nM .

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-124634

PZ-2891 1 Publications Verification	Others	Neurological Disease
PZ-2891 is an orally bioavailable, brain penetrant pantothenate kinase (PANK) modulator. PZ-2891 act as an orthosteric inhibitor at high concentrations and an allosteric activator at lower sub-saturating concentrations. PZ-2891 inhibits human pantothenate kinases PANK1β, PANK2, and PANK3 with IC₅₀s of 40.2 nM, 0.7 nM and 1.3 nM, respectively .

HY-131032

KI-7	Adenosine Receptor	Others
KI-7 is an A2B adenosine receptor positive allosteric modulator. KI-7 potentiates the cAMP accumulation induced by the non-selective A2B adenosine receptor agonist NECA (EC₅₀=445.8 nM). KI-7 also potentiates the cAMP accumulation induced by the selective A2B adenosine receptor agonist BAY 60-6583 as well as by adenosine with EC₅₀s of 2390 nM and 2550 nM, respectively .

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-148502

VU6019650	mAChR	Neurological Disease
VU6019650 is a potent and selective orthosteric antagonist of M5 mAChR (IC₅₀=36 nM), can be used for opioid use disorder (OUD) relief. VU6019650 can cross blood brain barrier, potentially modulates the mesolimbic dopaminergic reward circuitry. VU6019650 blocks Oxotremorine M iodide (HY-101372A) induced increases of neuronal firing rates of midbrain dopamine neurons in the ventral tegmental area (VTA) .

HY-156025

HCAR2 agonist 1	Others	Inflammation/Immunology
HCAR2 agonist 1 (Compound 9n) is a G_i protein-biased allosteric modulator of HCAR2. HCAR2 agonist 1 activates the G_i protein signaling pathway. HCAR2 agonist 1 shows anti-inflammatory effect, and reduces mRNA level of pro-inflammatory cytokine (TNF-α, IL-1β, IL-6, and MCP-1). HCAR2 agonist 1 enhances anti-inflammatory effects of orthosteric agonists in the mouse model of colitis .

HY-126242S

Tyk2-IN-7	JAK	Inflammation/Immunology
Tyk2-IN-7 is a TYK2 JH2 inhibitor, binds to TYK2 JH2 domain with IC50 and Ki.app of 0.00053 μM and 0.00007 μM, respectively. Tyk2-IN-7 provides a highly selective alternative to conventional TYK2 orthosteric inhibitors, inhibits TYK2/JAK1/JAK2 kinase domain. Tyk2-IN-7 provides robust inhibition in a mouse IL-12-induced IFNγ pharmacodynamic model as well as efficacy in an IL-23 and IL-12-dependent mouse colitis model[1].

Allosteric Modulators (AMs) Compound Library	174 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 174 small allosteric modulators. It is a good tool to be used for research on metabolize, cancer and other diseases.

Cyclorasin 9A5	Ras Raf	Cancer
Cyclorasin 9A5 is an 11-residue cell-permeable cyclic peptide that orthosterically inhibits the Ras-Raf protein interaction with an IC₅₀ of 120 nM .

LPPM-8	Peptides	Others
LPPM-8 is a ligand of Med25 and an inhibitor of Med25 protein-protein interactions (PPIs). LPPM-8 engages Med25 through interaction with the H2 face of its Activator Interaction Domain and stabilizes full-length protein in the cellular proteome. LPPM-8 is an orthosteric inhibitor of H2-binding transcriptional activators (such as ATF6a). LPPM-8 can be used for studying Med25 and Mediator complex biology .

Tyk2-IN-7
Tyk2-IN-7 is a TYK2 JH2 inhibitor, binds to TYK2 JH2 domain with IC50 and Ki.app of 0.00053 μM and 0.00007 μM, respectively. Tyk2-IN-7 provides a highly selective alternative to conventional TYK2 orthosteric inhibitors, inhibits TYK2/JAK1/JAK2 kinase domain. Tyk2-IN-7 provides robust inhibition in a mouse IL-12-induced IFNγ pharmacodynamic model as well as efficacy in an IL-23 and IL-12-dependent mouse colitis model[1].

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