Search Result
Results for "
allosteric enhancer
" in MedChemExpress (MCE) Product Catalog:
2
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-Y1683
-
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Racementhol
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Environmental Pollutants
GABA Receptor
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Infection
Neurological Disease
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DL-Menthol (Racementhol) is an orally active, GABAaR positive allosteric modulator and UDP-glucuronosyltransferase (UGT) inhibitor that can cross the blood-brain barrier. DL-Menthol binds to GABAAR 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 .
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- HY-119339
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SX-682
Maximum Cited Publications
10 Publications Verification
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CXCR
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Inflammation/Immunology
Endocrinology
Cancer
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SX-682 is an orally bioavailable, potent allosteric inhibitor of CXCR1 and CXCR2. SX-682 can block tumor myeloid-derived suppressor cells (MDSCs) recruitment and enhance T cell activation and antitumor immunity .
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- HY-159641
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BAY-3605349
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Molecular Glues
Keap1-Nrf2
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Metabolic Disease
Inflammation/Immunology
Cancer
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VVD-130037 (BAY-3605349) is a covalent molecular glue and allosteric NRF2 degrader. VVD-130037 covalently binds to KEAP1 and allosterically enhances the affinity of KEAP1-CUL3, promotes the formation of the active KEAP1-CUL3 E3 ligase complex, and thereby enhances the ubiquitination and degradation of NRF2. VVD-130037 exhibits KEAP1 target-binding activity both in in vitro systems and mouse models, and it can be used in research related to NRF2-dependent cancers, solid tumors harboring KEAP1 nonsense mutations and frameshift mutations, as well as advanced solid tumors .
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- HY-154848
-
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PI3K
Akt
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Cardiovascular Disease
Neurological Disease
Cancer
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UCL-TRO-1938 is a potent small molecule allosteric activator of PI3Kα with an EC50 value of approximately 60 μM. UCL-TRO-1938 can induce cell proliferation and has cardioprotective effects from ischaemia reperfusion injury and enhances nerve regeneration following nerve crush .
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- HY-B1456A
-
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LILLY-53858
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COX
Melanocortin Receptor
ERK
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Inflammation/Immunology
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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 .
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- HY-13619
-
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RSR13
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Hemoglobin
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Infection
Cancer
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Efaproxiral (RSR13) is a haemoglobin (Hb) synthetic allosteric modifier. Efaproxiral decreases Hb-oxygen (O2) binding affinity and enhances oxygenation of hypoxic tumours during radiation therapy .
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- HY-15701B
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ADH-503
2 Publications Verification
(Z)-Leukadherin-1 choline
|
Complement System
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Cancer
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ADH-503 ((Z)-Leukadherin-1 choline) is an orally active and allosteric CD11b agonist. ADH-503 leads to the repolarization of tumor-associated macrophages, reduction in the number of tumor-infiltrating immunosuppressive myeloid cells, and enhances dendritic cell responses .
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- HY-19934
-
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TAS-117
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Akt
Apoptosis
Autophagy
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Cancer
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Pifusertib (TAS-117) is a potent, selective, orally active allosteric Akt inhibitor (with IC50s of 4.8, 1.6, and 44 nM for Akt1, 2, and 3, respectively). Pifusertib triggers anti-myeloma activities and enhances fatal endoplasmic reticulum (ER) stress induced by proteasome inhibition. Pifusertib induces apoptosis and autophagy .
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- HY-141510
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ITPP hexasodium
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HIF/HIF Prolyl-Hydroxylase
|
Cardiovascular Disease
Cancer
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myo-Inositol trispyrophosphate (ITPP) hexasodium is a salt form of inositol triphosphate (ITPP). myo-Inositol trispyrophosphate (ITPP) hexasodium is a membrane-permeant hemoglobin allosteric regulator. myo-Inositol trispyrophosphate (ITPP) hexasodium enhances the oxygen release capacity of red blood cells by reducing the affinity of hemoglobin to oxygen. myo-Inositol trispyrophosphate (ITPP) hexasodium can be used in the study of cardiovascular disease and cancer .
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- HY-13509
-
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RGS Protein
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Inflammation/Immunology
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CCG-50014 is the most potent against the regulator of G-protein signaling protein type 4 (RGS4) (IC50 =30 nM) and is >20-fold selective for RGS4 over other RGS proteins. CCG-50014 binds covalently to the RGS, forming an adduct on two cysteine residues located in an allosteric regulatory site . CCG50014, reduces nociceptive responses and enhances opioid-mediated analgesic effects in the mouse formalin test .
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- HY-156659
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Phosphatase
ERK
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Inflammation/Immunology
|
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NC1 is a selective non-competitive and allosteric lymphoid-specific tyrosine phosphatase (LYP) inhibitor, with a Ki value 4.3 μM. NC1 allosterically regulates LYP/PTPN22 activity by restricting WPD loop movement. NC1 inhibits LYP activity in lymphoid T cells and enhances T-cell receptor signaling. NC1 can be used for the research of autoimmune diseases .
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- HY-169329
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PINK1/Parkin
E1/E2/E3 Enzyme
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Neurological Disease
|
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BIO-2007817 is a Parkin positive allosteric modulators (PAMs). BIO-2007817 enhances the activity of wildtype Parkin. BIO-2007817 stimulates Parkin (an E3 ligase)autoubiquitination and induces the appearance of monoubiquitinated forms of Miro1 (EC50: 0.17 μM) .
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- HY-19934A
-
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TAS-117 hydrochloride
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Akt
Apoptosis
Autophagy
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Cancer
|
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Pifusertib (TAS-117) hydrochloride is a potent, selective, orally active allosteric Akt inhibitor (with IC50s of 4.8, 1.6, and 44 nM for Akt1, 2, and 3, respectively). Pifusertib hydrochloride triggers anti-myeloma activities and enhances fatal endoplasmic reticulum (ER) stress induced by proteasome inhibition. Pifusertib hydrochloride induces apoptosis and autophagy .
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- HY-139091
-
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Taste Receptor
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Others
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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 .
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- HY-106199
-
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Adenosine Receptor
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Neurological Disease
Inflammation/Immunology
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Adenosine A1 receptor activator T62 is an allosteric enhancer of adenosine A1 receptor. Adenosine A1 receptor activator T62 produces antinociception in animal models of acute pain and also reduces hypersensitivity in models of inflammatory and nerve-injury pain .
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- HY-103519
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-
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- HY-13619A
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RSR13 sodium
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Hemoglobin
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Infection
Cancer
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Efaproxiral (RSR13) sodium is a haemoglobin (Hb) synthetic allosteric modifier. Efaproxiral sodium decreases Hb-oxygen (O2) binding affinity and enhances oxygenation of hypoxic tumours during radiation therapy .
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- HY-139202
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Integrin
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Inflammation/Immunology
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XVA143, an α/β I-like allosteric antagonist, inhibits LFA-1 dependent firm adhesion, while at the same time it enhances adhesion in shear flow and rolling both in vitro and in vivo .
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- HY-174311
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Glycosidase
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Neurological Disease
Metabolic Disease
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GT-02216 can bind to GCase allosterically and enhance its activity. GT-02216 enhances the activity of GCase in primary human fibroblasts dose-dependently reduces the accumulation of its substrate, hexosylsphingosine (HexCer). GT-02216 reduces the Tau accumulation in mutant GBA1 fibroblasts. GT-02216 can be used for the study of Parkinson’s disease .
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- HY-156193
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PDHK
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Cardiovascular Disease
Metabolic Disease
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PF-07208254 is a selective, orally active allosteric inhibitor of branched-chain ketoacid dehydrogenase kinase (BDK) (IC50=110 nM, Ki=54 nM, KD=84 nM). PF-07208254 inhibits BDK-mediated BCKDH phosphorylation and enhances the catabolism of branched-chain amino acids (BCAAs) and branched-chain keto acids (BCKAs) by binding to the allosteric pocket of BDK, reducing BDK binding to BCKDH-E2 and promoting BDK degradation. PF-07208254 inhibits BDK activity in human skeletal muscle cells (IC50=540 nM) and has activity to improve cardiac function and metabolism. PF-07208254 can be used in the study of cardiometabolic diseases (e.g., heart failure, type 2 diabetes) .
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- HY-120327
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KY-226
2 Publications Verification
|
Phosphatase
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Neurological Disease
Metabolic Disease
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KY-226 is a potent, selective, orally active and allosteric protein tyrosine phosphatase 1B (PTP1B) inhibitor with an IC50 of 0.25 μM, and without PPARγ agonist activity. KY-226 exerts anti-diabetic and anti-obesity effects by enhancing insulin and leptin signaling, respectively. KY-226 also protects neurons from cerebral ischemic injury .
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- HY-10936
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iGluR
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Neurological Disease
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S 18986 is a selective, orally active, brain penetrant positive allosteric modulator of AMPA-type receptors. S 18986 shows cognitive enhancing properties in rodents. S 18986 activates the release of noradrenaline and acetylcholine in rat hippocampus and enhances rat memory in object-recognition tests .
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- HY-141840
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GCGR
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Metabolic Disease
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GLP-1R modulator C5 is an allosteric modulator enhancing GLP-1 binding to GLP-1R via a transmembrane site (EC50 1.59 ± 0.53 μM).
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- HY-176716
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Aldehyde Dehydrogenase (ALDH)
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Cardiovascular Disease
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ALDH2 activator 1 (Compound Z17) is an allosteric aldehyde dehydrogenase 2 (ALDH2) agonist. ALDH2 activator 1 enhances cardiac function and reduces myocardial necrosis in a mouse model of myocardial ischemia-reperfusion. ALDH2 activator 1 is promising for research of cardiovascular diseases such as myocardial infarction (MI) .
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- HY-158991
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CFTR
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Inflammation/Immunology
|
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I1421 is an activator of the cystic fibrosis transmembrane conductance regulator (CFTR) with an EC50 of 64 nM for WT CFTR currents. I1421 also allosterically activates multiple mutants causing cystic fibrosis (CF) with good in vivo potency, with an oral bioavailability of 60% in mice corresponding to a half-life of 75 min. I1421 synergizes with Elexacaftor (HY-111772) to enhance CFTR currents .
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- HY-141510A
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ITPP hexa-triethylamine
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Biochemical Assay Reagents
HIF/HIF Prolyl-Hydroxylase
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Cardiovascular Disease
Cancer
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myo-Inositol trispyrophosphate (ITPP) hexa-triethylamine is a salt form of inositol triphosphate (ITPP). myo-Inositol trispyrophosphate hexa-triethylamine is a membrane-permeant hemoglobin allosteric regulator. myo-Inositol trispyrophosphate hexa-triethylamine enhances the oxygen release capacity of red blood cells by reducing the affinity of hemoglobin to oxygen. myo-Inositol trispyrophosphate hexa-triethylamine can be used in the study of cardiovascular disease and cancer .
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- HY-177873
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iGluR
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Neurological Disease
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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 .
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- HY-107498
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iGluR
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Neurological Disease
|
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GNE-8324 is a selective GluN2A positive allosteric modulator. GNE-8324 selectively enhances NMDA receptor (NMDAR)-mediated synaptic responses in inhibitory but not excitatory neurons .
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- HY-141842
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GCGR
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Metabolic Disease
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GLP-1R modulator L7-028 is an allosteric modulator enhancing GLP-1 binding to GLP-1R via a transmembrane site (EC50 11.01 ± 2.73 μM).
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- HY-149453
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Guanylate Cyclase
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Cardiovascular Disease
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MCUF-651 is an orally active guanylyl cyclase A receptor (GC-A) positive allosteric modulator (PAM) (KD: 397 nM ). MCUF-651 binds to GC-A and selectively enhances the binding of atrial natriuretic peptide (ANP) to GC-A. MCUF-651 enhances ANP-mediated cGMP generation in human cardiac, renal, and fat cells. MCUF-651 inhibits cardiomyocyte hypertrophy .
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- HY-118140
-
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Cannabinoid Receptor
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Neurological Disease
Inflammation/Immunology
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ZCZ011 is a potent and brain-penetrant cannabinoid 1 (CB1) receptor positive allosteric modulator. ZCZ011 potentiates binding of CP55,940 to the CB1 receptor, enhances anandamide (AEA)-stimulated GTPγS binding in mouse brain membranes. ZCZ011 increases β-arrestin recruitment and ERK phosphorylation in hCB1 cells. ZCZ011 can be used for researching neuropathic and inflammatory pain .
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- HY-103520
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GABA Receptor
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Neurological Disease
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DS2 is a selective positive allosteric modulator of δ-GABAA 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 .
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- HY-174416
-
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E1/E2/E3 Enzyme
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Cardiovascular Disease
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Smurf1-IN-5 (Compound cpd-6) is an allosteric SMAD ubiquitin regulatory factor 1 (SMURF1) inhibitor. Smurf1-IN-5 leads to a reduction in the ubiquitylation of substrates such as BMPR2 (bone morphogenetic protein receptor 2) and SMAD1, enhancing the BMP (bone morphogenetic protein) signaling pathway. Smurf1-IN-5 is promising for research of pulmonary arterial hypertension (PAH) .
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- HY-116463
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- HY-115575
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Neuropeptide Y Receptor
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Metabolic Disease
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tBPC is a selective positive allosteric modulator for human Y4 receptor (Y4R), which enhances the activation of Y4R in G protein signaling and arrestin3 recruitment .
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- HY-141839
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GCGR
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Metabolic Disease
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GLP-1R modulator C16 is an allosteric modulator enhancing GLP-1 binding to GLP-1R via a transmembrane site (EC50 8.43 ± 3.82 μM).
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- HY-159527
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Glovadalen
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Dopamine Receptor
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Neurological Disease
|
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Glovadalenum (Glovadalen) is an orally active, selective, blood-brain barrier permeable positive allosteric modulator of dopamine D1 receptor. Glovadalenum selectively enhances the efficacy of dopamine in activating dopamine D1 receptor. Glovadalenum can be used for the research of Parkinson's disease .
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- HY-103502
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CGP7930
1 Publications Verification
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GABA Receptor
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Neurological Disease
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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 .
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- HY-163280
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NAMPT
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Neurological Disease
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JGB-1-155 is a positive allosteric modulators (N-PAMs), which enhances the activity of nicotinamide phosphoribosyltransferase NAMPT with EC50 of 3.29 μM. JGB-1-155 counteracts the oxidative stress, through upregulating the NAD + in THP-1 human monocytes. JGB-1-155 attenuates TNFα-induced ROS in HT-22 cells .
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- HY-139289S
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DNA/RNA Synthesis
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Cancer
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ART899 is a highly specific allosteric inhibitor of the Polθ DNA polymerase domain. ART899 can effectively enhance the radiosensitivity of tumor cells, shows good tolerance when combined with fractionated radiation, and significantly reduces tumor growth compared to radiation alone .
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- HY-178783
-
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Adenosine Receptor
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Metabolic Disease
Inflammation/Immunology
Cancer
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MRS8454 is a positive allosteric modulator (PAM) of the A3 adenosine receptor (A3AR). MRS8454 can significantly enhance the maximum effect of the standard agonist Cl-IB-MECA by approximately 286%-300%, and significantly reduce its EC50 value. MRS8454 effectively enhances the ability of A3AR agonists to inhibit the cAMP accumulation induced by Forskolin (HY-15371). MRS8454 can be used for the development of molecular probes .
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- HY-124985
-
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mGluR
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Neurological Disease
|
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VU6010608 is a blood-brain barrier-crossing mGlu7 negative allosteric modulator (IC50 = 0.76 μM). VU6010608 can block long-term enhancement (LTP) of SC-CA1 synapses in mouse brain slices induced by high-frequency stimulation. VU6010608 can be used for research on neurological diseases .
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- HY-162401
-
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RXFP Receptor
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Cardiovascular Disease
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AZ7976 (Compound 42) is a highly selective agonist for the Relaxin Family Peptide Receptor 1 (RXFP1) (pEC50 > 10.5). AZ7976 enhances RXFP1's cAMP signaling through an allosteric mechanism, thereby physiologically increasing heart rate. AZ7976 can be used in the field of cardiovascular disease research .
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- HY-15469
-
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P2X Receptor
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Neurological Disease
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GW791343 dihydrochloride is a potent human P2X7 receptor negative allosteric modulator (exhibits species-specific activity), produces a non-competitive antagonist effect on human P2X7 receptor, with a pIC50 of 6.9-7.2. GW791343 dihydrochloride can enhance ATP rhythm. GW791343 dihydrochloride can be used in study of neurological disease .
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- HY-15476
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- HY-107506
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mGluR
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Neurological Disease
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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 .
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- HY-10915
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Adenosine Receptor
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Cardiovascular Disease
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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 .
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- HY-179240
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Dopamine Receptor
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Neurological Disease
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UNC9815 is a D1 dopamine receptor (D1R) orthosteric allosteric modulator (PAM). UNC9815 can dose-dependently enhance the functional efficacy of dopamine in β-inhibitory protein recruitment experiments and cAMP accumulation experiments. When used in combination with other PAMs, UNC9815 exhibits a significant synergistic enhancement effect. UNC9815 can be used to study neurological and psychiatric diseases such as Parkinson's disease and schizophrenia .
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- HY-118356
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Neurokinin Receptor
mAChR
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Neurological Disease
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WIN 62,577 is a rat-specific, but non-human, NK1 receptor antagonist. WIN 62,577 interacts with M1-M4 mAChRs and is an allosteric enhancer of acetylcholine affinity targeting the M3 receptor.
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- HY-179108
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iGluR
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Neurological Disease
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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 .
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- HY-129517
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iGluR
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Neurological Disease
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UBP714 exhibts agonistic activity for recombinant GluN1/GluN2 receptor by binding to the positive allosteric site (PAM) of NMDARs. UBP714 enhances NMDAR-mediated field excitatory postsynaptic potentials (f-EPSPs) in Xenopus oocytes .
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- HY-175366
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Opioid Receptor
Arrestin
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Neurological Disease
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DOR agonist 3 (Compound 10) is a δ-opioid receptor (DOR)-selective positive allosteric modulator. DOR agonist 3 enhances G protein signaling while reducing β-arrestin2 recruitment. DOR agonist 3 is promising for research of chronic pain and depression .
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- HY-W013376
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1-(Diphenylmethyl)piperazine; 1-Benzhydrylpiperazine
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Antibiotic
Bacterial
Penicillin-binding protein (PBP)
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Infection
Cancer
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Norcyclizine is a piperazine compound that can be used for the synthesis of antimicrobial agents. 1-Benzhydrylpiperazine derivatives have been found to enhance the antibacterial activity of β-lactam antibiotics (Oxacillin, HY-B0925A) against Methicillin (HY-121544)-resistant Staphylococcus aureus (MRSA). This enhancement is likely achieved by inhibiting the allosteric site of PBP2a. Additionally, 1-Benzhydrylpiperazine can also serve as a pharmacological scaffold for the synthesis of anticancer agents .
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- HY-15470
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P2X Receptor
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Neurological Disease
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GW791343 trihydrochloride is a potent human P2X7 receptor negative allosteric modulator (exhibits species-specific activity), produces a non-competitive antagonist effect on human P2X7 receptor, with a pIC50 of 6.9-7.2. GW791343 trihydrochloride can enhance ATP rhythm. GW791343 trihydrochloride can be used in study of neurological disease .
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- HY-176731
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P2X Receptor
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Neurological Disease
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MSK-9 is a positive allosteric modulator of the P2X4 receptor with dual activities of enhancing ion conductance and delaying receptor inactivation. MSK-9 stabilizes the open state of the P2X4 receptor through rigid 3-piperidinyl and hydrophobic menthyl substituents. MSK-9 can be used in the study of multiple sclerosis (MS) .
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- HY-W856819
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Opioid Receptor
Cholinesterase (ChE)
Drug Metabolite
nAChR
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Neurological Disease
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Eseroline is a potent μ-opioid receptor agonist, which is the hydrolytic metabolite of Physostigmine (HY-N6608). Eseroline is a selective and competitive acetylcholinesterase (AChE) inhibitor, with its Ki values for AChE and BuChE being 0.1 μM and 200 μM respectively. Eseroline has nicotinic acetylcholine receptor allosteric enhancing ligand (nAChR-APL) activity, meaning it does not activate the receptor but significantly enhances the signal transduction of Ach triggered by the receptor. Eseroline is neurotoxic, causing cell membrane damage (LDH leakage) and energy metabolism collapse (ATP depletion). Eseroline can be used for the study of Alzheimer's disease .
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- HY-169766
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Molecular Glues
Keap1-Nrf2
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Cancer
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VVD 065 is an orally active KEAP1-dependent NRF2 molecular glue degrader with a KEAP1 KD of 65 nM. VVD 065 covalently engages KEAP1 at Cys151, allosterically stabilizes KEAP1-CUL3 complex formation and enhances NRF2 polyubiquitination and proteasomal degradation. VVD 065 can be used for the research of esophageal squamous cell carcinoma, lung cancer, head-and-neck cancer, uterine cancers .
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- HY-129274
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mGluR
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Neurological Disease
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RO4988546 is a negative allosteric modulator (NAM) that targets metabotropic glutamate receptors 2 and 3 (mGlu2, mGlu3). RO4988546 can reduce the binding of [ 3h]-LY354740 at the positive binding site, while affecting the receptor's G protein coupling and intracellular signaling. RO4988546 can be used in the development of antidepressants and cognitive enhancers .
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- HY-119806
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5-HT Receptor
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Neurological Disease
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TMPPAA is an allosteric agonist and positive allosteric modulator of the 5-HT3 receptor. TMPPAA enhances 5-HT-mediated 5-HT3AR signaling .
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- HY-111332
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mGluR
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Others
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(E)-PHCCC is a positive allosteric modulator (PAM) for mGluR4, that enhances the activity of the receptor's endogenous ligand (glutamate), and exhibits activity in the calcium mobilization assay in CHO cells with an EC50 of 3.2 μM .
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- HY-15786
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iGluR
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Neurological Disease
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SGE-201 is an allosteric modulator of N-methyl-D-aspartate receptors (NMDARs), demonstrating significant neuroprotective effects by enhancing NMDAR-mediated responses while differing in action among various blockers in neuronal networks.
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- HY-116205
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iGluR
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Others
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UBP684 is a novel positive allosteric modulator of NMDA receptors (NMDARs) that enhances receptor function by stabilizing the ligand-binding domains in a closed conformation, resulting in potentiated whole-cell currents and increased mean open time.
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- HY-105567A
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GABA Receptor
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Neurological Disease
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Carbiphene hydrochloride is a GABAA receptor allosteric modulator. Carbiphene hydrochloride inhibits [ 35S] TBPS binding and enhances [ 3H] muscimol binding on rat forebrain membranes, acting on specific GABAA receptor subsets. Carbiphene hydrochloride can be used in research related to schizophrenia .
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- HY-119256
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GABA Receptor
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Neurological Disease
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COR627 is a GABA receptor positive allosteric modulator with the ability to enhance GABA activity. COR627 exhibits effects on GABA and baclofen stimulation in rat cortical membranes and can increase its affinity for GABA(B) receptors. In vivo experiments have shown that COR627 can enhance the sedative/hypnotic effects of baclofen at pretreatment ineffective doses .
|
-
- HY-119082A
-
|
|
mAChR
|
Others
|
|
VU0029767 is an allosteric enhancer of the M1 muscarinic receptor with the activity to modulate M1 receptor activity. VU0029767 can enhance M1 receptor activity by increasing agonist affinity, but exhibits different properties from other compounds under different experimental conditions, such as effects on mutant M1 receptors and effects on downstream signaling pathways.
|
-
- HY-169501
-
-
- HY-116149
-
|
|
nAChR
|
Others
|
|
A-424274 is a positive allosteric modulator of the α4β2 neuronal nicotinic acetylcholine receptor with activity to enhance the efficacy of analgesics. A-424274 selectively enhances the potency of a range of nicotinic acetylcholine receptor agonists at the α4β2 receptor and, in preclinical models, co-administration with an α4β2 PAM significantly enhances the analgesic efficacy of ABT-594 at clinically well-tolerated doses in humans.
|
-
- HY-15701A
-
|
ADH-503 free base
|
Complement System
|
Cancer
|
|
(Z)-Leukadherin-1 (ADH-503 free base) is an orally active and allosteric CD11b agonist. (Z)-Leukadherin-1 leads to the repolarization of tumor-associated macrophages, reduction in the number of tumor-infiltrating immunosuppressive myeloid cells, and enhances dendritic cell responses .
|
-
- HY-123904
-
|
|
iGluR
|
Neurological Disease
|
|
UoS12258 is a selective positive allosteric modulator of AMPA receptor. UoS12258 enhances AMPA receptor‐mediated synaptic transmission. UoS12258 improves performance in cognition rat models, including Scopolamine (HY-N0296)‐impaired rats and water maze learning and retention in aged rats .
|
-
- HY-13619S
-
|
RSR13-d6
|
Isotope-Labeled Compounds
|
Cancer
|
|
Efaproxiral (RSR13)-d6 is the deuterium labeled Efaproxiral (HY-13619). Efaproxiral is a haemoglobin (Hb) synthetic allosteric modifier. Efaproxiral decreases Hb-oxygen (O2) binding affinity and enhances oxygenation of hypoxic tumours during radiation therapy .
|
-
- HY-151899
-
|
|
Adenosine Receptor
|
Inflammation/Immunology
|
|
A3AR modulator 1 (MRS8054) is an orally active A3 adenosine receptor (A3AR) (Adenosine Receptor) positive allosteric modulator (PAM). A3AR modulator 1 greatly enhances Cl-IB-MECA-stimulated [ 35S]GTPγS binding Emax .
|
-
- HY-13619AR
-
|
RSR13 sodium (Standard)
|
Reference Standards
|
Cancer
|
|
Efaproxiral (RSR13) sodium (Standard) is the analytical standard of Efaproxiral sodium (HY-13619A). This product is intended for research and analytical applications. Efaproxiral sodium is a haemoglobin (Hb) synthetic allosteric modifier. Efaproxiral sodium decreases Hb-oxygen (O2) binding affinity and enhances oxygenation of hypoxic tumours during radiation therapy .
|
-
- HY-13619R
-
|
RSR13 (Standard)
|
Reference Standards
|
Cancer
|
|
Efaproxiral (RSR13) (Standard) is the analytical standard of Efaproxiral (HY-13619). This product is intended for research and analytical applications. Efaproxiral is a haemoglobin (Hb) synthetic allosteric modifier. Efaproxiral decreases Hb-oxygen (O2) binding affinity and enhances oxygenation of hypoxic tumours during radiation therapy .
|
-
- HY-B1456AR
-
|
LILLY-53858 (Standard)
|
Reference Standards
COX
Melanocortin Receptor
ERK
|
Inflammation/Immunology
|
|
Fenoprofen (Standard) (LILLY-53858 (Standard)) is the analytical standard of Fenoprofen (HY-B1456A). This product is intended for research and analytical applications. Fenoprofenc 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-175508
-
|
|
iGluR
|
Neurological Disease
|
|
NMDA receptor modulator 9 is an orally active NMDA receptor positive allosteric modulator (PAM). NMDA receptor modulator 9 enhances GluN2A receptor activity. NMDA receptor modulator 9 demonstrates significant antidepressant-like effects in chronic restraint stress (CRS)-induced depression mice. NMDA receptor modulator 9 can be used for the study of depression .
|
-
- HY-123525
-
|
|
GABA Receptor
|
Neurological Disease
|
|
COR628 is a positive allosteric modulator of GABA(B) receptors with the activity of enhancing GABA-induced GTPγS stimulation. COR628 showed significant activity in in vitro studies but did not exhibit endogenous agonist activity. COR628 has shown efficacy in experiments in mice by enhancing the sedation/hypnosis induced by baclofen, shortening the onset time and extending the duration of loss of righting reflex when combined with non-sedating doses of baclofen . The cytotoxic effect of COR628 is comparable to or higher than that of GS39783 or BHF177 in concentration .
|
-
- HY-117440
-
|
|
Kinesin
|
Cancer
|
|
4'-Methoxy-S-trityl-L-cysteinol is an allosteric inhibitor of vertebrate Kinesin Spindle Protein (KSP). 4'-Methoxy-S-trityl-L-cysteinol significantly enhances its inhibitory activity against NCI60 tumor cells by modifying the trityl and cysteine groups. Its EC50 for bipolar spindle formation is 28 μM, showing stronger inhibitory potency than the parent molecule and monastrol.
|
-
- HY-120783
-
|
|
Endogenous Metabolite
|
Neurological Disease
|
|
Lu AF58801 is a potent, orally available, brain-penetrant positive allosteric modulator of α7 nicotinic acetylcholine receptors with efficacy in a novel object recognition task in mice. Lu AF58801 was shown to selectively enhance the activity of α7 nicotinic acetylcholine receptors. Lu AF58801 was able to improve cognitive function in mice treated with subchronic fluchlorothiazol (PCP) .
|
-
- HY-121600
-
|
|
Cannabinoid Receptor
|
|
|
GAT229 is a CB1 positive allosteric modulator (PAM) that effectively reduces intraocular pressure (IOP) in high IOP mouse models and enhances CB1 receptor-mediated IOP-lowering effects. A 0.2% GAT229 solution or 10 mg/kg of GAT229 alone significantly reduces IOP. GAT229 is promising for research related to glaucoma and elevated intraocular pressure .
|
-
- HY-117467
-
|
|
iGluR
|
Neurological Disease
|
|
BMT-108908 is a negative allosteric modulator with selective activity on the NR2B subtype of the NMDA receptor. BMT-108908 has been shown to damage cognition in research, affecting cognitive functions in multiple areas. BMT-108908 failed to show a significant impact on the γ wave power of the EEG in the experiment, but it had a significant inhibitory and enhancement effect on the β wave and δ wave power .
|
-
- HY-108204
-
|
THRX 918661
|
GABA Receptor
|
Others
|
|
AZD 3043 (THRX 918661) is a positive allosteric modulator of GABA(A) receptors with sedative and hypnotic activity. AZD 3043 can enhance GABA(A) receptor-mediated chloride currents in vitro and produce hypnotic and electroencephalographic inhibitory effects in vivo. Due to its esterase-dependent metabolic pathway, it has a short duration of action and can be quickly cleared even after long-term infusion, which may have clinical application potential.
|
-
- HY-12153
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
JNJ-1930942 is a selective and blood-brain barrier (BBB) penetrant α(7) nAChR positive allosteric modulator.JNJ-1930942 enhances the Choline (HY-B0282)-evoked rise in intracellular Ca 2+ levels and neurotransmission at hippocampal dentate gyrus synapses. JNJ-1930942 reverses the naturally occurring sensory gating deficit in DBA/2 mice .
|
-
- HY-129431
-
|
PNU-89843
|
GABA Receptor
|
Neurological Disease
|
|
U-89843A (PNU-89843) is a GABAA receptors positive allosteric modulator (PAM). U-89843A enhances GABA-induced Cl - currents in the α1β2γ2, α3β2γ2 and α6β2γ2 subtypes. U-89843A shows antioxidant and sedative effects .
|
-
- HY-103497
-
|
PNU-89843 hydrochloride
|
GABA Receptor
|
Neurological Disease
|
|
U-89843A (PNU-89843) hydrochloride is a GABAA receptors positive allosteric modulator (PAM). U-89843A hydrochloride enhances GABA-induced Cl - currents in the α1β2γ2, α3β2γ2 and α6β2γ2 subtypes. U-89843A hydrochloride shows antioxidant and sedative effects .
|
-
- HY-111161
-
|
|
nAChR
Parasite
|
Infection
|
|
GSK575594A is a modulator of the nicotinic acetylcholine receptor (nAChR) in Ascaris suum. GSK575594A enhances muscle contractions induced by acetylcholine (ACh) by binding to the allosteric binding site between subunits within the transmembrane domain of nAChR. At a concentration of 3 μM, GSK575594A significantly increased the contraction induced by ACh in Ascaris suum (Emax increased from 1.19 g to 1.51 g). GSK575594A may be used in research within the field of antiparasitic studies .
|
-
- HY-151464
-
|
|
SHP2
Phosphatase
HDAC
|
Inflammation/Immunology
Cancer
|
|
SHP2/HDAC-IN-1 is a dual allosteric SHP2/HDAC inhibitor with IC50 values of 20.4 nM (SHP2) and 25.3 nM (HDAC1) respectively. SHP2/HDAC-IN-1 triggers efficient antitumor immunity by activating T cells, enhancing the antigen presentation function and promoting cytokine secretion. SHP2/HDAC-IN-1 can be used in the research of cancer immunoresearch .
|
-
- HY-182631
-
|
|
iGluR
|
Neurological Disease
|
|
CX1763 is an AMPAR allosteric modulator. CX1763 allosterically potentiates glutamate-evoked currents, accelerates channel opening, and increases the surface levels of AMPAR containing Glur2 (R). CX1763 enhances synaptic transmission in the rat hippocampus. CX1763 improves attention in rats and attenuates amphetamine-induced hyperactivity in mice. CX1763 can be used in studies related to attention deficit hyperactivity disorder and opioid-induced respiratory depression .
|
-
- HY-105567
-
|
|
GABA Receptor
|
Neurological Disease
|
|
Carbiphene is a GABAA receptor allosteric modulator. Carbiphene inhibits [ 35S] TBPS binding and enhances [ 3H] muscimol binding on rat forebrain membranes, acting on specific GABAA receptor subsets. Carbiphene can be used in research related to schizophrenia .
|
-
- HY-182062
-
|
|
NAMPT
E1/E2/E3 Enzyme
|
Neurological Disease
|
|
NAMPT activator-9 (Compound DIPM) is an allosteric, non-competitive NAMPT activator, with an EC50 of 3.366 μM against hNAMPT. NAMPT activator-9 enhances the enzymatic activity of NAMPT via an allosteric, non-competitive mechanism. NAMPT activator-9 increases intracellular NAD + levels. NAMPT activator-9 restores myotube diameter and reduces the expression of atrophy markers Atrogin-1 and MuRF1. NAMPT activator-9 is applicable to research related to muscle atrophy .
|
-
- HY-119082
-
|
|
mAChR
|
Others
|
|
(E/Z)-VU0029767 is an allosteric enhancer of M1 muscarinic receptors with the activity to modulate M1 receptor activity. (E/Z)-VU0029767 can enhance M1 receptor activity by increasing agonist affinity, but exhibits different properties from other compounds under different experimental conditions, such as effects on mutant M1 receptors and effects on downstream signaling pathways.
|
-
- HY-182437
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
ASP4345 free base is a blood-brain barrier-permeable dopamine D1 receptor modulator. ASP4345 free base binds to the allosteric site of the dopamine D1 receptor, thereby enhancing dopamine activity. ASP4345 free base can be used in the research of schizophrenia and Parkinson's disease .
|
-
- HY-107498R
-
|
|
Reference Standards
iGluR
|
Neurological Disease
|
|
GNE-8324 (Standard) is the analytical standard of GNE-8324 (HY-107498). This product is intended for research and analytical applications. GNE-8324 is a selective GluN2A positive allosteric modulator. GNE-8324 selectively enhances NMDA receptor (NMDAR)-mediated synaptic responses in inhibitory but not excitatory neurons .
|
-
- HY-122222
-
|
|
PPAR
|
Others
|
|
MRL20 is a PPARγ constitutive and allosteric agonist. MRL20 enhances the interaction between PPARγ and the co-activating peptide of TRAP220, with its EC50 being 10 nM. Even after being covalently blocked in the constitutive pocket by GW9662 (HY-16578) or T0070907 (HY-13202), MRL20 can still strengthen the interaction between PPARγ and TRAP220, with EC50 values of 176 and 440 nM respectively. MRL20 fails to completely inhibit its cell activation effect. MRL20 can be used to study the allosteric regulatory mechanism of PPARγ .
|
-
- HY-183101
-
|
|
iGluR
NADPH Oxidase
|
Neurological Disease
|
|
AMPAR modulator-12 is a blood-brain barrier-permeable AMPAR positive allosteric modulator. AMPAR modulator-12 reduces NOX-1 expression, enhances AMPAR-mediated currents, promotes excitatory postsynaptic transmission and restores AMPAR function. AMPAR modulator-12 enhances excitatory and inhibitory synaptic transmission, reduces burst firing in the lateral habenula after withdrawal, and produces rapid and sustained antidepressant-like effects. AMPAR modulator-12 is applicable for the research of depression .
|
-
- HY-P11258
-
|
|
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 .
|
-
- HY-182941
-
|
|
EAAT
|
Neurological Disease
|
|
Parawixin10 (Compound 2) is an N-acylpolyamine. Parawixin10 fails to enhance glutamate uptake in radioligand uptake assays of EAAT1, EAAT2 or EAAT3. Parawixin10 exhibits no positive allosteric modulatory activity in radioligand uptake assays of EAAT1−EAAT3, nor can it improve neuronal survival rates in mice in a dose-dependent and statistically significant manner. Parawixin10 has no neuroprotective activity .
|
-
- HY-180554
-
|
|
Synaptic Vesicle Proteins
|
Neurological Disease
|
|
UCB1244283 is a synaptic vesicle glycoprotein 2A (SV2A) allosteric modulator. UCB1244283 binds to a secondary ligand-binding site in SV2A and enhances orthosteric ligand engagement when the orthosteric site is occupied, by stabilizing the occluded state and slowing ligand dissociation. UCB1244283 shows a clear protective effect against both tonic and clonic convulsions in sound-sensitive mice. UCB1244283 can be used for epilepsy research .
|
-
- HY-183588
-
|
|
EAAT
Reactive Oxygen Species (ROS)
|
Neurological Disease
|
|
HCM-01 is an Excitatory amino acid transporter 2 (EAAT2) activator with oral effectiveness and blood-brain barrier penetration.HCM-01 binds to the allosteric site of EAAT2, increases EAAT2 expression in astrocytes, enhances glutamate-handling capacity, and modulates glutamate homeostasis.HCM-01 acts as an antioxidant, improves oxidative/antioxidative balance and increases total antioxidant capacity. HCM-01 can be used for the research of Alzheimer's disease .
|
-
- HY-179625
-
|
|
Aminopeptidase
|
Inflammation/Immunology
Cancer
|
|
GSK235 is an orally active, selective and allosteric endoplasmic reticulum aminopeptidase 1 (ERAP1) inhibitor with pIC50 values of 8.45 and 7.59 for human and mouse ERAP1, respectively. GSK235 exhibits over 1000-fold selectivity for the two most homologous enzymes, ERAP2 and IRAP. GSK235 can regulate the immunopeptidome of cancer cells and enhance cancer cell antigenicity. GSK235 can be used for the study of colorectal cancer and arthritis .
|
-
- HY-182723
-
|
|
GPR84
|
Cancer
|
|
PSB-16671 is an allosteric agonist of GPR84. PSB-16671 recruits β-arrestins and couples to Gi, enhances the Gi activation potency of orthosteric agonists, and exerts a synergistic effect with orthosteric agonists. PSB-16671 promotes G protein activation and partial chemotaxis independent of GPR84 in mouse neutrophils, maintains the phagocytic function of macrophages against cancer cells without inducing receptor desensitization. PSB-16671 can be used in cancer-related research .
|
-
- HY-P4160
-
|
THG113.31; ILGHXDYK
|
Prostaglandin Receptor
|
Endocrinology
|
|
PDC31 (THG113.31; ILGHXDYK) is an allosteric and non-competitive inhibitor of FP Prostaglandin Receptor. PDC31 is the D-amino acid-based oligopeptide, is used for smooth muscle contractile agent. PDC31 decreases the strength and duration of uterine contractions in vivo, which can be used for research of preterm labor and primary dysmenorrhea (PD). PDC31 also enhances Ca 2+-dependent large-conductance K +-channel in human myometrial cells .
|
-
- HY-143312A
-
|
|
GLP Receptor
|
Metabolic Disease
Inflammation/Immunology
|
|
V-0219 hydrochloride is an orally active glucagon-like peptide-1 receptor (GLP-1R) positive allosteric modulator. V-0219 hydrochloride potentiates GLP-1R stimulation, and enhances GLP-1-induced cAMP production and insulin secretion. V-0219 hydrochloride potentiates glucose-dependent insulin secretion. V-0219 hydrochloride improves glucose handling in normal and diabetic rodents. V-0219 hydrochloride can be used for the research of obesity-associated diabetes .
|
-
- HY-143312
-
|
|
GLP Receptor
|
Metabolic Disease
Inflammation/Immunology
|
|
V-0219 is an orally active glucagon-like peptide-1 receptor (GLP-1R) positive allosteric modulator. V-0219 potentiates GLP-1R stimulation, and enhances GLP-1-induced cAMP production and insulin secretion. V-0219 potentiates glucose-dependent insulin secretion. V-0219 improves glucose handling in normal and diabetic rodents. V-0219 can be used for the research of obesity-associated diabetes .
|
-
- HY-136258
-
|
|
nAChR
|
Neurological Disease
|
|
nAChR agonist CMPI hydrochloride is a potent and selective positive allosteric modulator (PAM) of nAChR containing a α4:α4 subunit interface. nAChR agonist CMPI hydrochloride enhances the response of (α4)3(β2)2 nAChR to ACh (10 µM) with an EC50 of 0.26 µM. nAChR agonist CMPI hydrochloride has potential for the research of nicotine dependence and many neuropsychiatric conditions associated with decreased brain cholinergic activity .
|
-
- HY-178153
-
|
|
iGluR
|
Neurological Disease
|
|
BPAM363 is an orally active, selective positive allosteric modulator (PAM) of AMPARs with blood-brain barrier penetration. BPAM363 selectively potentiates AMPAR activity in human and rat models, with an EC2x value of 0.96 μM in rat embryonic cortex primary neurons. BPAM363 upregulates BDNF protein expression in rat primary cortical neuronal cultures. BPAM363 enhances AMPA-mediated excitatory postsynaptic responses in rat and mice. BPAM363 can be used for the study of cognitive disorders .
|
-
- HY-110208
-
BRD9876
1 Publications Verification
|
Kinesin
Microtubule/Tubulin
|
Cancer
|
|
BRD9876 is the “rigor” inhibitor that locks kinesin-5 (Eg5) in a state with enhanced microtubules (MTs) binding, leading to bundling and stabilization of MTs. BRD9876 interacts with the tyrosine 104 residue that is part of the α4-α6 allosteric binding pocket. BRD9876 specifically targets microtubule-bound Eg5 and selectively inhibits myeloma over CD34 cells. BRD9876 has the potential for multiple myeloma (MM) research .
|
-
- HY-156025
-
|
|
Hydroxycarboxylic Acid Receptor (HCAR)
|
Inflammation/Immunology
|
|
HCAR2 agonist 1 (Compound 9n) is a Gi protein-biased allosteric modulator of HCAR2. HCAR2 agonist 1 activates the Gi 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-14562
-
|
|
mAChR
Amyloid-β
|
Neurological Disease
Inflammation/Immunology
|
|
TBPB (tert-butyl peroxybenzoate) is a highly selective, blood-brain-permeable M1 mAChR allosteric agonist (EC50=289 nM) with anti-schizophrenia and anti-inflammatory activities. TBPB can enhance the sensitivity of M1 receptors to acetylcholine, activate downstream signaling pathways, and inhibit the release of pro-inflammatory cytokines (TNF-α, IL-6). TBPB can regulate the processing of amyloid and can be used in the study of neurodegenerative diseases (such as Alzheimer's disease) and inflammation-related diseases (such as sepsis) .
|
-
- HY-124057
-
|
|
nAChR
|
Neurological Disease
|
|
RO5126946 is a selective, orally active α7 nAChR allosteric potentiator with EC50 values of 0.06 μM (hα7 nAChR) and 770 nM (α7 nAChR), and it crosses the blood-brain barrier. RO5126946 enhances synaptic transmission and positively modulates GABA-ergic responses by increasing peak current, slowing current decay, and elevating the frequency of spontaneous inhibitory postsynaptic currents, without affecting the recovery of receptors from the desensitized state. RO5126946 not only enhances subthreshold nicotine effects and improves associative learning, but also does not interfere with the original pro-cognitive effects of nicotine. RO5126946 can be used to study cognitive impairments associated with diseases such as Alzheimer's disease and schizophrenia .
|
-
- HY-156505A
-
|
|
iGluR
|
Neurological Disease
|
|
R-(+)-EU-1180-453 is a positive allosteric modulator targeting NMDA receptors containing GluN2C and GluN2D subunits, with a pEC50 value of 5.5 for both rat receptor subtypes, and it can cross the blood-brain barrier. R-(+)-EU-1180-453 increases the potency of glutamate, enhances receptor responses to maximally effective concentrations of agonists, and acts only on receptors bound to both co-agonists. R-(+)-EU-1180-453 is applicable to research related to Alzheimer's disease, Parkinson's disease, epilepsy, and neuropathic pain .
|
-
- HY-W001692
-
|
DOV 273547
|
GABA Receptor
|
Neurological Disease
|
|
Ocinaplon (DOV 273547) is an orally active positive allosteric modulator of GABAA receptor, with an EC50 ranging from 3.07 μM (α1β2γ2 subtype) to 10.03 μM (α1β2γ3 subtype). Ocinaplon enhances GABA-stimulated chloride currents across multiple GABAA receptor subtypes, with varying potency between different subtypes. Ocinaplon exerts anxiolytic and anticonvulsant effects, and causes motor impairment at high doses. Ocinaplon can be used for research on generalized anxiety disorder .
|
-
- HY-180802
-
|
|
Mas-related G-protein-coupled Receptor (MRGPR)
|
Neurological Disease
|
|
BCFTP is a potent, orally active and selective human Mas-related G protein-coupled receptor X1 (MrgprX1)-positive allosteric modulator. BCFTP selectively potentiates MrgprX1 signaling in HEK293 cells. BCFTP alleviates specific neuropathic pain-related behaviors in a humanized MrgprX1 mouse model of chronic constrictive injury (CCI) in a MrgprX1-dependent manner. BCFTP synergistically enhances psychoactive substances analgesia in CCI MrgprX1 mice. BCFTP can be used for neuropathic pain research .
|
-
- HY-W677042
-
|
5α-Androst-16-en-3α-ol
|
GABA Receptor
|
Neurological Disease
|
|
α-Androstenol (5α-Androst-16-en-3α-ol) is a steroid pheromone that has been found in boar testes and male axillary sweat. α-Androstenol is also a positive allosteric modulator of GABAA receptors, which enhances GABA-activated currents in primary mouse cerebellar granule cells (EC50 of 0.4 μM). α-Androstenol produces anxiolytic-like, antidepressant-like, and anticonvulsant effects in mice. α-Androstenol can be used for the research of seizures .
|
-
- HY-13509R
-
|
|
RGS Protein
|
Inflammation/Immunology
|
|
CCG-50014 (Standard) is the analytical standard of CCG-50014. This product is intended for research and analytical applications. CCG-50014 is the most potent against the regulator of G-protein signaling protein type 4 (RGS4) (IC50 =30 nM) and is >20-fold selective for RGS4 over other RGS proteins. CCG-50014 binds covalently to the RGS, forming an adduct on two cysteine residues located in an allosteric regulatory site . CCG50014, reduces nociceptive responses and enhances opioid-mediated analgesic effects in the mouse formalin test .
|
-
- HY-162809
-
|
|
Ras
|
Cancer
|
|
XMU-MP-9 is a bifunctional compound that binds to the C2 domain of Nedd4-1 and the allosteric site of K-Ras. XMU-MP-9 enhances the interaction between Nedd4-1 and K-Ras, induces conformational changes in the Nedd4-1/K-Ras complex, promotes the ubiquitination and degradation of multiple K-Ras mutants, and inhibits the proliferation of cells carrying K-Ras mutants. XMU-MP-9 can be used for the study of colon, lung and pancreatic cancer .
|
-
- HY-116819
-
|
|
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-115860
-
|
|
iGluR
|
Neurological Disease
|
|
TAS-4 is a potent and selective mGluR4 positive allosteric modulator with significant anti-Parkinson's disease activity. TAS-4 is able to show efficacy when used alone or in combination with l-DOPA. TAS-4 is able to reverse haloperidol-induced spasticity when administered alone. TAS-4 enhances the contralateral rotation behavior induced by l-DOPA in a dose-dependent manner. TAS-4 combined with low-dose l-DOPA shows anti-Parkinson's effects similar to full-dose l-DOPA without exacerbating abnormal motor side effects .
|
-
- HY-131196
-
|
|
mAChR
|
Neurological Disease
|
|
M3 mAChR agonist 1 is an M3-preferring M3/M5 mAChR dual positive allosteric modulators (PAM). M3 mAChR agonist 1 shows excellent subtype selectivity over other subtypes of mAChRs including M1, M2, and M4 mAChRs. M3 mAChR agonist 1 increases the contraction of isolated rat bladder strips by modulating the M3 muscarinic acetylcholine receptor, leading to enhanced signaling pathways. M3 mAChR agonist 1 can be used for the research of endocrinology .
|
-
- HY-117734
-
|
|
iGluR
|
Neurological Disease
|
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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 .
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- HY-P992360
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GABA Receptor
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Neurological Disease
Cancer
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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 .
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- HY-15618
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M1 receptor modulator
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mAChR
Calcium Channel
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Neurological Disease
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MK-7622 (M1 receptor modulator) is an orally active positive allosteric modulator of muscarinic M1 acetylcholine receptors (mAChRs). MK-7622 enhances ACh-induced calcium flux in CHO cells expressing human M1 receptors (EC50 = 21 nM) and shows robust agonist activity in rat M1-expressing CHO cells, increasing intracellular calcium. MK-7622 reverses Scopolamine (HY-N0296)-induced cognitive deficits in rhesus macaques in an object retrieval detour task. MK-7622 can be used for the study of Alzheimer's disease (AD) .
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- HY-107111
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mAChR
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Neurological Disease
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GSK1034702 is an orally active and allosteric agonist of M1 mAChR (pEC50=8.1) that can cross the blood-brain barrier. GSK1034702 activates the Gq/11 protein-mediated signaling pathway, enhancing neuronal firing and long-term potentiation (LTP) in the CA1 region of the hippocampus. GSK1034702 can modulate hippocampal function, improve memory encoding in the nicotine withdrawal cognitive dysfunction model, and show pro-cognitive effects in rodents. GSK1034702 can be used for the study of the mechanisms of cognitive impairment diseases such as Alzheimer's disease, and has certain peripheral M receptor activation-related side effects (such as gastrointestinal reactions) .
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- HY-107111A
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Cholinesterase (ChE)
mAChR
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Neurological Disease
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GSK1034702 hydrochloride is an orally active and allosteric agonist of M1 mAChR (pEC50=8.1) that can cross the blood-brain barrier. GSK1034702 hydrochloride activates the Gq/11 protein-mediated signaling pathway, enhancing neuronal firing and long-term potentiation (LTP) in the CA1 region of the hippocampus. GSK1034702 hydrochloride can modulate hippocampal function, improve memory encoding in the nicotine withdrawal cognitive dysfunction model, and show pro-cognitive effects in rodents. GSK1034702 hydrochloride can be used for the study of the mechanisms of cognitive impairment diseases such as Alzheimer's disease, and has certain peripheral M receptor activation-related side effects (such as gastrointestinal reactions) .
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- HY-182850
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CXCR
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Metabolic Disease
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UCUF-965 is a CXCR4 positive allosteric modulator. UCUF-965 potentiates CXCL12-induced β-arrestin recruitment and cAMP signaling, activates lymphoblast migration, induces calcium flux, and does not bind CXCR4’s orthosteric CXCL12 site. UCUF-965 reduces miR-15b and miR-29a levels, increases miR-146a levels in fibroblasts. UCUF-965 enhances angiogenesis and reduces wound healing time in diabetic mice. UCUF-965 can be used for the research of diabetic wound healing impairment .
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- HY-175670
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GABA Receptor
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Neurological Disease
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GABAA receptor modulator-10 is an orally active, potent positive allosteric modulator (PAM) of the α1β2γ2 GABAA receptor with favorable blood-brain barrier (BBB) penetration. GABAA receptor modulator-10 enhances α1β2γ2 GABAA receptor function and potentiates GABA-evoked currents. GABAA receptor modulator-10 demonstrates potent antiepileptic efficacy in both the Pentetrazol (PTZ)- and Kainic Acid (KA) (HY-N2309)-induced mice epilepsy models. GABAA receptor modulator-10 can be used for the study of epilepsy .
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- HY-16639
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GPR35
Neurotensin Receptor
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Neurological Disease
Endocrinology
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ML314 is a potent, BBB-penetrant and β-arrestin biased molecule agonist of NTR1 (EC50 = 1.9 μM). ML314 shows good selectivity against NTR2 and GPR35, but does not stimulate Ca2+ mobilization. ML314 can attenuate amphetamine-like hyperlocomotion in dopamine transporter knockout mice. ML314 attenuates methamphetamine-associated hyperlocomotion and potentiates the psychostimulant inhibitory effects of a ghrelin antagonist in wild type mouse model. ML314 also acts as an allosteric enhancer of endogenous neurotensin. ML314 antagonizes G protein signaling. ML314 can be studied in research for methamphetamine abuse conditions .
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- HY-18654A
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mGluR
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Neurological Disease
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ADX88178 TFA is an orally active, blood-brain barrier-penetrant, selective positive allosteric modulator of mGluR4, with an EC50 of 3.5 nM against hmGluR4. ADX88178 TFA modulates mGlu4 activity, enhances glutamate-mediated receptor activation, and increases the apparent affinity of glutamate for the receptor. ADX88178 TFA reverses haloperidol-induced catalepsy, potentiates the effects of levodopa (L-DOPA) and quinpirole, but fails to alleviate established abnormal involuntary movements, does not exacerbate L-DOPA-induced dyskinesia, and does not affect forelimb akinesia when administered alone. ADX88178 TFA can be used in research related to L-DOPA-induced dyskinesia and Parkinson's disease .
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- HY-12316
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20α-Hydroxycholesterol
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Smo
Endogenous Metabolite
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Cardiovascular Disease
Metabolic Disease
Cancer
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20(S)-Hydroxycholesterol (20α-Hydroxycholesterol) is an allosteric activator that selectively targets the Smoothened (Smo) of the Hedgehog pathway with an EC50 of ~30 μM (Hedgehog). 20(S)-Hydroxycholesterol binds to the extracellular cysteine-rich domain (CRD) of Smo in a stereoselective manner, activating downstream Gli transcription factors (without inducing transcription of receptor genes in the Wnt pathway). 20(S)-Hydroxycholesterol enhances osteogenic differentiation of bone marrow stromal cells and synergistically activates the Raf/MEK/ERK pathway with Simvastatin (HY-17502) to promote bone regeneration. 20(S)-Hydroxycholesterol can be used to study the mechanisms of developmental biology, oncology, bone, and angiogenesis .
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- HY-136190
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TRP Channel
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Neurological Disease
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TRPC6-PAM-C20 is a selective positive allosteric modulator (PAM) of TRPC6 channels. TRPC6-PAM-C20 is a potent enhancer of channel activation, enabling low basal concentrations of DAG to induce activation of the ion channel. TRPC6-PAM-C20 induces increases in intracellular Ca 2+ concentrations ([Ca 2+]i) in TRPC6-expressing HEK293 cells with an EC50 of 2.37 μM. TRPC6-PAM-C20 can be used as a valuable tool to selectively exaggerate TRPC6-dependent signals .
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- HY-183324
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iGluR
Dopamine Transporter
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Neurological Disease
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AMPA receptor modulator-12 is an orally acrive AMPA receptor positive allosteric modulator. AMPA receptor modulator-12 also exhibits moderate binding affinity for the human dopamine transporter with a Kd of 1.57 μM. AMPA receptor modulator-12 enhances AMPA receptor-mediated ion currents, delays channel deactivation. AMPA receptor modulator-12 prolongs sleep latency, reduces sleep duration, extends forced swimming time, improves rotarod endurance, and alleviates acute sleep deprivation-related behavioral deficits. AMPA receptor modulator-12 does not increase spontaneous locomotion. AMPA receptor modulator-12 can be used for the research of narcolepsy and fatigue-related conditions .
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- HY-155811
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iGluR
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Neurological Disease
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DQP-997-74 (compound 2i) is a selective negative allosteric modulator of N-methyl-d-aspartate receptor (NMDAR), specifically targeting GluN2C/D (IC50: 0.069 μM and 0.035 μM), with blood-brain barrier penetrability. Where DQP refers to dihydroquinoline-pyrazoline. DQP-997-74 acts synergistically with the agonist glutamate to exhibit time-dependent enhanced potency in inhibiting hypersynchronous activity driven by high-frequency excitatory synaptic transmission. DQP-997-74 reduces the number of epileptogenesis in a murine model of tuberous sclerosis complex (TSC)-induced epilepsy. DQP-997-74 can be used for research on NMDAR-related neurological diseases .
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- HY-107111R
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Reference Standards
mAChR
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Neurological Disease
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GSK1034702 (Standard) is the analytical standard of GSK1034702 (HY-107111). This product is intended for research and analytical applications. GSK1034702 is an orally active and allosteric agonist of M1 mAChR (pEC50=8.1) that can cross the blood-brain barrier. GSK1034702 activates the Gq/11 protein-mediated signaling pathway, enhancing neuronal firing and long-term potentiation (LTP) in the CA1 region of the hippocampus. GSK1034702 can modulate hippocampal function, improve memory encoding in the nicotine withdrawal cognitive dysfunction model, and show pro-cognitive effects in rodents. GSK1034702 can be used for the study of the mechanisms of cognitive impairment diseases such as Alzheimer's disease, and has certain peripheral M receptor activation-related side effects (such as gastrointestinal reactions) .
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- HY-117106
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GABA Receptor
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Others
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PNU-107484A is a GABAA receptor ligand that exhibits target activity mechanisms dependent on α isoforms. In the α1β2γ2 subtype, PNU-107484A acts as a positive allosteric modulator, enhancing GABA-induced Cl - currents, while it inhibits the currents in the α3β2γ2 and α6β2γ2 subtypes. The half-maximal concentrations for the α1β2γ2, α3β2γ2, and α6β2γ2 subtypes are 3.1, 4.2, and 3.5 μM, respectively. PNU-107484A can be used as a probe to investigate the physiological roles of different α isoform subtypes .
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- HY-P5542
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SB-01; Peniel 2000
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Factor Xa
TGF-beta/Smad
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Inflammation/Immunology
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Vicatertide (SB-01, Peniel 2000) is a polypeptide with both competitive inhibitory activity against TGF-β1 and selective inhibitory activity against human factor XIa (hFXIa, with a Ka of 80 nM for hFXIa). Vicatertide binds allosterically to the two binding sites of dimeric hFXI/hFXIa, while directly binding to activated TGF-β1, selectively blocking the Smad1/5/8 pathway and maintaining low-level activation of the Smad2 pathway to enhance the synthesis of type Ⅱ collagen and aggrecan. Vicatertide inhibits thrombus formation in arteriovenous thrombosis models, and also reduces thrombus weight and thrombus incidence in mouse lung cancer models. Vicatertide can be used for research on degenerative disc disease and thrombosis-related diseases .
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- HY-147105
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Orphan Nuclear Receptor
Interleukin Related
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Inflammation/Immunology
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LRH-1 agonist-2 (Compound 6N) is a selective, full LRH-1 agonist with an EC50 of 15.7 nM. LRH-1 agonist-2 directly interacts with the Thr352 and His390 residues in the LRH-1 binding pocket, promotes allosteric signaling to the activation function surface (AFS), stabilizes the AFS and enhances coactivator recruitment. LRH-1 agonist-2 induces the anti-inflammatory cytokine IL-10, and reduces the pro-inflammatory cytokines IL-1β and TNFα. LRH-1 modulator-1 exerts anti-inflammatory effects in intestinal organoids. LRH-1 modulator-1 can be used in studies related to inflammatory bowel disease .
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- HY-182707
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nAChR
Interleukin Related
TNF Receptor
NF-κB
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Neurological Disease
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JWX-A0108 is a selective human α7 nAChR positive allosteric modulator with an EC50 of 4.35 μM. JWX-A0108 potentiates α7 nAChR currents only in the presence of acetylcholine, with no direct activating effect or alteration of desensitization. JWX-A0108 enhances hippocampal GABAergic synaptic transmission by increasing spontaneous inhibitory postsynaptic currents. JWX-A0108 reduces the brain expression levels of IL-1β, TNF-α, and IL-6 by blocking the NF-κB signaling pathway, and reduces microglial activation by downregulating Iba1. JWX-A0108 effectively improves cognitive deficits, neuroinflammation, and hippocampal neuronal damage in mouse models of schizophrenia and Alzheimer's disease. JWX-A0108 can be used for research related to schizophrenia and Alzheimer's disease .
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- HY-139997
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PROTACs
EGFR
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Cancer
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DDC-01-163 is an allosteric PROTAC degrader targeting EGFR. DDC-01-163 is dependent on the ubiquitin–proteasome system. DDC-01-163 can selectively inhibit the proliferation of L858R/T790M (L/T) mutant Ba/F3 cells. DDC-01-163 is effective against Osimertinib (HY-15772)-resistant cells with L/T/C797S and L/T/L718Q EGFR mutations. DDC-01-163 exhibits enhanced anti-proliferative activity against L858R/T790M EGFR-Ba/F3 cells when combined with the ATP-site EGFR inhibitor Osimertinib. DDC-01-163 can be used for the study of non-small cell lung cancer .
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| Cat. No. |
Product Name |
Target |
Research Area |
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- HY-P5542
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SB-01; Peniel 2000
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Factor Xa
TGF-beta/Smad
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Inflammation/Immunology
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Vicatertide (SB-01, Peniel 2000) is a polypeptide with both competitive inhibitory activity against TGF-β1 and selective inhibitory activity against human factor XIa (hFXIa, with a Ka of 80 nM for hFXIa). Vicatertide binds allosterically to the two binding sites of dimeric hFXI/hFXIa, while directly binding to activated TGF-β1, selectively blocking the Smad1/5/8 pathway and maintaining low-level activation of the Smad2 pathway to enhance the synthesis of type Ⅱ collagen and aggrecan. Vicatertide inhibits thrombus formation in arteriovenous thrombosis models, and also reduces thrombus weight and thrombus incidence in mouse lung cancer models. Vicatertide can be used for research on degenerative disc disease and thrombosis-related diseases .
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- HY-P4160
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THG113.31; ILGHXDYK
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Prostaglandin Receptor
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Endocrinology
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PDC31 (THG113.31; ILGHXDYK) is an allosteric and non-competitive inhibitor of FP Prostaglandin Receptor. PDC31 is the D-amino acid-based oligopeptide, is used for smooth muscle contractile agent. PDC31 decreases the strength and duration of uterine contractions in vivo, which can be used for research of preterm labor and primary dysmenorrhea (PD). PDC31 also enhances Ca 2+-dependent large-conductance K +-channel in human myometrial cells .
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- HY-P11258
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Urotensin Receptor
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Cardiovascular Disease
Metabolic Disease
Inflammation/Immunology
Cancer
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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 .
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| Cat. No. |
Product Name |
Target |
Research Area |
Image |
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- HY-P992360
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GABA Receptor
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Neurological Disease
Cancer
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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 .
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(5)
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
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- HY-Y1683
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- HY-12316
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20α-Hydroxycholesterol
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Classification of Application Fields
Endogenous metabolite
Disease Research Fields
Steroids
Source Classification
Cancer
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Smo
Endogenous Metabolite
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20(S)-Hydroxycholesterol (20α-Hydroxycholesterol) is an allosteric activator that selectively targets the Smoothened (Smo) of the Hedgehog pathway with an EC50 of ~30 μM (Hedgehog). 20(S)-Hydroxycholesterol binds to the extracellular cysteine-rich domain (CRD) of Smo in a stereoselective manner, activating downstream Gli transcription factors (without inducing transcription of receptor genes in the Wnt pathway). 20(S)-Hydroxycholesterol enhances osteogenic differentiation of bone marrow stromal cells and synergistically activates the Raf/MEK/ERK pathway with Simvastatin (HY-17502) to promote bone regeneration. 20(S)-Hydroxycholesterol can be used to study the mechanisms of developmental biology, oncology, bone, and angiogenesis .
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- HY-156193
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Cardiovascular Disease
Classification of Application Fields
Ketones, Aldehydes, Acids
Endogenous metabolite
Disease Research Fields
Source Classification
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PDHK
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PF-07208254 is a selective, orally active allosteric inhibitor of branched-chain ketoacid dehydrogenase kinase (BDK) (IC50=110 nM, Ki=54 nM, KD=84 nM). PF-07208254 inhibits BDK-mediated BCKDH phosphorylation and enhances the catabolism of branched-chain amino acids (BCAAs) and branched-chain keto acids (BCKAs) by binding to the allosteric pocket of BDK, reducing BDK binding to BCKDH-E2 and promoting BDK degradation. PF-07208254 inhibits BDK activity in human skeletal muscle cells (IC50=540 nM) and has activity to improve cardiac function and metabolism. PF-07208254 can be used in the study of cardiometabolic diseases (e.g., heart failure, type 2 diabetes) .
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| Cat. No. |
Product Name |
Chemical Structure |
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- HY-139289S
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ART899 is a highly specific allosteric inhibitor of the Polθ DNA polymerase domain. ART899 can effectively enhance the radiosensitivity of tumor cells, shows good tolerance when combined with fractionated radiation, and significantly reduces tumor growth compared to radiation alone .
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- HY-13619S
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Efaproxiral (RSR13)-d6 is the deuterium labeled Efaproxiral (HY-13619). Efaproxiral is a haemoglobin (Hb) synthetic allosteric modifier. Efaproxiral decreases Hb-oxygen (O2) binding affinity and enhances oxygenation of hypoxic tumours during radiation therapy .
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