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Results for "

allosteric enhancer

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (1) Adenosine Receptor (3) Akt (2) Antibiotic (1) Apoptosis (2) Autophagy (2) Bacterial (1) Cannabinoid Receptor (2) CFTR (1) Cholinesterase (ChE) (1) Complement System (2) CXCR (1) E1/E2/E3 Enzyme (1) Endogenous Metabolite (1) GABA Receptor (5) GCGR (3) Guanylate Cyclase (1) HDAC (1) HIF/HIF Prolyl-Hydroxylase (2) iGluR (5) Integrin (1) Isotope-Labeled Compounds (1) Kinesin (1) mAChR (1) Melanocortin Receptor (3) mGluR (3) Microtubule/Tubulin (1) nAChR (2) NAMPT (2) Neurokinin Receptor (1) Neuropeptide Y Receptor (1) P2X Receptor (2) Parasite (1) Penicillin-binding protein (PBP) (1) Phosphatase (2) PINK1/Parkin (1) Prostaglandin Receptor (1) Ras (1) Reactive Oxygen Species (2) RGS Protein (1) RXFP Receptor (1) SHP2 (1) Sigma Receptor (1) Taste Receptor (1) TRP Channel (1)
By Research Areas:	Cancer (14) Cardiovascular Disease (5) Endocrinology (2) Infection (2) Inflammation/Immunology (12) Metabolic Disease (5) Neurological Disease (30)

By Targets:

5-HT Receptor (1)

Adenosine Receptor (3)

Akt (2)

Antibiotic (1)

Apoptosis (2)

Autophagy (2)

Bacterial (1)

Cannabinoid Receptor (2)

CFTR (1)

Cholinesterase (ChE) (1)

Complement System (2)

CXCR (1)

E1/E2/E3 Enzyme (1)

Endogenous Metabolite (1)

GABA Receptor (5)

GCGR (3)

Guanylate Cyclase (1)

HDAC (1)

HIF/HIF Prolyl-Hydroxylase (2)

iGluR (5)

Integrin (1)

Isotope-Labeled Compounds (1)

Kinesin (1)

mAChR (1)

Melanocortin Receptor (3)

mGluR (3)

Microtubule/Tubulin (1)

nAChR (2)

NAMPT (2)

Neurokinin Receptor (1)

Neuropeptide Y Receptor (1)

P2X Receptor (2)

Parasite (1)

Penicillin-binding protein (PBP) (1)

Phosphatase (2)

PINK1/Parkin (1)

Prostaglandin Receptor (1)

Ras (1)

Reactive Oxygen Species (2)

RGS Protein (1)

RXFP Receptor (1)

SHP2 (1)

Sigma Receptor (1)

Taste Receptor (1)

TRP Channel (1)

By Research Areas:

Cancer (14)

Cardiovascular Disease (5)

Endocrinology (2)

Infection (2)

Inflammation/Immunology (12)

Metabolic Disease (5)

Neurological Disease (30)

Inhibitors & Agonists

Peptides

Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

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-139091

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

HY-106199

Adenosine A1 receptor activator T62 1 Publications Verification	Adenosine Receptor	Neurological Disease Inflammation/Immunology
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 .

HY-B1456A

Fenoprofen 1 Publications Verification LILLY-53858	Melanocortin Receptor	Inflammation/Immunology
Fenoprofen (LILLY-53858) is a nonsteroidal anti-inflammatory agent (NSAID). Fenoprofen can be used to to relieve symptoms of arthritis (osteoarthritis and rheumatoid arthritis), such as inflammation, swelling, stiffness, and joint pain. Fenoprofen is an allosteric enhancer for melanocortin receptors. Fenoprofen also increases ERK1/2 activation .

HY-103519

rac-BHFF	GABA Receptor	Neurological Disease
rac-BHFF is a potent and orally active allosteric enhancer of GABA_B receptor .

HY-116463

E1R	Sigma Receptor	Neurological Disease
E1R is a positive allosteric modulator of sigma-1 receptors (Sig1R PAM) with cognition-enhancing activity .

HY-129274

RO4988546	mGluR	Neurological Disease
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 .

HY-B1456AR

Fenoprofen (Standard)	Melanocortin Receptor	Inflammation/Immunology
Fenoprofen (Standard) is the analytical standard of Fenoprofen. This product is intended for research and analytical applications. Fenoprofen (LILLY-53858) is a nonsteroidal anti-inflammatory agent (NSAID). Fenoprofen can be used to to relieve symptoms of arthritis (osteoarthritis and rheumatoid arthritis), such as inflammation, swelling, stiffness, and joint pain. Fenoprofen is an allosteric enhancer for melanocortin receptors. Fenoprofen also increases ERK1/2 activation .

HY-119806

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

HY-103497

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

HY-13619

Efaproxiral 1 Publications Verification RSR13	Reactive Oxygen Species	Cancer
Efaproxiral is a haemoglobin (Hb) synthetic allosteric modifier, decreases Hb-oxygen (O2) binding affinity and enhances oxygenation of hypoxic tumours during radiation therapy .

HY-13619A

Efaproxiral sodium 1 Publications Verification RSR13 sodium	Reactive Oxygen Species	Cancer
Efaproxiral sodium (RSR13 sodium) is a synthetic allosteric modifier of haemoglobin (Hb), decreases Hb-oxygen (O2) binding affinity and enhances oxygenation of hypoxic tumours during radiation therapy.

HY-107498

GNE-8324	iGluR	Neurological Disease
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-115575

tBPC	Neuropeptide Y Receptor	Metabolic Disease
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 .

HY-111332

(E)-PHCCC	mGluR	Others
(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 .

HY-10936

S 18986	iGluR	Neurological Disease
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 .

HY-116205

UBP684	Others	Others
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.

HY-15786

SGE-201	Others	Neurological Disease
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.

HY-139202

XVA143	Integrin	Inflammation/Immunology
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 .

HY-157421

Nampt activator-4	NAMPT	Others
Nampt activator-4 is a positive allosteric modulator (N-PAM) of nicotinamide phosphoribosyltransferase (NAMPT) with an EC₅₀ of 0.058 μM. Nampt activator-4 can enhance the nicotinamide adenine dinucleotide (NAD ⁺) in cells .

HY-141839

GLP-1R modulator C16	GCGR	Metabolic Disease
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).

HY-141840

GLP-1R modulator C5	GCGR	Metabolic Disease
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).

HY-119339

SX-682 Maximum Cited Publications 6 Publications Verification	CXCR	Inflammation/Immunology Endocrinology Cancer
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 .

HY-141842

GLP-1R modulator L7-028	GCGR	Metabolic Disease
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).

HY-118356

WIN 62,577	Neurokinin Receptor mAChR	Neurological Disease
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.

HY-119082A

VU0029767	Others	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-119256

COR627	Others	Neurological Disease
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-129517

UBP714	iGluR	Neurological Disease
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 .

HY-149453

MCUF-651	Guanylate Cyclase	Cardiovascular Disease
MCUF-651 is an orally active guanylyl cyclase A receptor (GC-A) positive allosteric modulator (PAM) (K_D: 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 .

HY-15701B

ADH-503 1 Publications Verification (Z)-Leukadherin-1 choline	Complement System	Cancer
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 .

HY-169329

BIO-2007817	PINK1/Parkin E1/E2/E3 Enzyme	Neurological Disease
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) .

HY-116149

A-424274	Others	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

(Z)-Leukadherin-1 1 Publications Verification 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-119082

(E/Z)-VU0029767	Others	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-103502

CGP7930 1 Publications Verification	GABA Receptor	Neurological Disease
CGP7930 (3-(3’,5’-Di-tert-butyl-4’-hydroxy) phenyl-2, 2-dimethylpropanol) is a positive metabotropic GABAB receptor allosteric modulator. CGP7930 enhances the inhibitory effect of l-baclofen on the oscillatory activity of cultured cortical neurons .

HY-123904

UoS12258	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-151899

A3AR modulator 1	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 E_max .

HY-W013376

Norcyclizine 1-(Diphenylmethyl)piperazine; 1-Benzhydrylpiperazine	Antibiotic Bacterial Penicillin-binding protein (PBP)	Infection Cancer
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 .

HY-19934A

Pifusertib hydrochloride TAS-117 hydrochloride	Akt Apoptosis Autophagy	Cancer
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 .

HY-19934

Pifusertib TAS-117	Akt Apoptosis Autophagy	Cancer
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 .

HY-162401

AZ7976	RXFP Receptor	Cardiovascular Disease
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 .

HY-123525

COR628	Others	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-15469

GW791343 dihydrochloride	P2X Receptor	Neurological Disease
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 .

HY-B1456AS

Fenoprofen-13C6(sodium salt hydrate)	Isotope-Labeled Compounds Melanocortin Receptor	Inflammation/Immunology
Fenoprofen- ¹³C₆ (sodium hydrate) is the ¹³C labeled Fenoprofen (HY-B1456A). Fenoprofen is a nonsteroidal anti-inflammatory agent (NSAID). Fenoprofen can be used to to relieve symptoms of arthritis (osteoarthritis and rheumatoid arthritis), such as inflammation, swelling, stiffness, and joint pain. Fenoprofen is an allosteric enhancer for melanocortin receptors. Fenoprofen also increases ERK1/2 activation[1][2][3].

HY-15470

GW791343 trihydrochloride	P2X Receptor	Neurological Disease
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 .

HY-141510

myo-Inositol trispyrophosphate hexasodium ITPP hexasodium	HIF/HIF Prolyl-Hydroxylase	Cardiovascular Disease Cancer
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 .

HY-163280

JGB-1-155	NAMPT	Neurological Disease
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 .

HY-158991

I1421	CFTR	Inflammation/Immunology
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 .

HY-117440

4'-Methoxy-S-trityl-L-cysteinol	Others	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

Lu AF58801	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) .

Cat. No.	Product Name	Target	Research Area

HY-P4160

PDC31 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 .

Cat. No.	Product Name	Chemical Structure

HY-B1456AS

Fenoprofen-13C6(sodium salt hydrate)

Fenoprofen- ¹³C₆ (sodium hydrate) is the ¹³C labeled Fenoprofen (HY-B1456A). Fenoprofen is a nonsteroidal anti-inflammatory agent (NSAID). Fenoprofen can be used to to relieve symptoms of arthritis (osteoarthritis and rheumatoid arthritis), such as inflammation, swelling, stiffness, and joint pain. Fenoprofen is an allosteric enhancer for melanocortin receptors. Fenoprofen also increases ERK1/2 activation[1][2][3].

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