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Results for "

allosteric enhancer

" in MedChemExpress (MCE) Product Catalog:

81

Inhibitors & Agonists

1

Peptides

2

Natural
Products

2

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 .
    LUF6096
  • 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 .
    FEMA 4774
  • 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 .
    Adenosine A1 receptor activator T62
  • HY-103519
    rac-BHFF

    		GABA Receptor Neurological Disease
    rac-BHFF is a potent and orally active allosteric enhancer of GABAB receptor .
    rac-BHFF
  • HY-116463
    E1R

    		Sigma Receptor Neurological Disease
    E1R is a positive allosteric modulator of sigma-1 receptors (Sig1R PAM) with cognition-enhancing activity .
    E1R
  • HY-13619
    Efaproxiral
    1 Publications Verification

    RSR13

    		 Reactive Oxygen Species (ROS) Cancer
    Efaproxiral is a haemoglobin (Hb) synthetic allosteric modifier, decreases Hb-oxygen (O2) binding affinity and enhances oxygenation of hypoxic tumours during radiation therapy .
    Efaproxiral
  • HY-13619A
    Efaproxiral sodium
    1 Publications Verification

    RSR13 sodium

    		 Reactive Oxygen Species (ROS) 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.
    Efaproxiral sodium
  • 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 .
    RO4988546
  • HY-119806
    TMPPAA

    		5-HT Receptor Neurological Disease
    TMPPAA is an allosteric agonist and positive allosteric modulator of the 5-HT3 receptor. TMPPAA enhances 5-HT-mediated 5-HT3AR signaling .
    TMPPAA
  • 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 .
    U-89843A hydrochloride
  • 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 .
    GNE-8324
  • 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 .
    tBPC
  • 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 .
    S 18986
  • 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 .
    (E)-PHCCC
  • HY-15786
    SGE-201

    		iGluR 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.
    SGE-201
  • HY-116205
    UBP684

    		iGluR 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.
    UBP684
  • 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 .
    XVA143
  • 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 .
    Nampt activator-4
  • 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).
    GLP-1R modulator C5
  • 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).
    GLP-1R modulator C16
  • HY-Y1683
    DL-Menthol

    Racementhol

    		 GABA Receptor Neurological Disease
    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 .
    DL-Menthol
  • HY-13619S
    Efaproxiral-d6

    		Isotope-Labeled Compounds Reactive Oxygen Species (ROS) Cancer
    Efaproxiral-d6 is the deuterium labeled Efaproxiral. Efaproxiral (RSR13) is a haemoglobin (Hb) synthetic allosteric modifier, decreases Hb-oxygen (O2) binding affinity and enhances oxygenation of hypoxic tumours during radiation therapy .
    Efaproxiral-d6
  • HY-119339
    SX-682
    Maximum Cited Publications
    7 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 .
    SX-682
  • 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).
    GLP-1R modulator L7-028
  • 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.
    WIN 62,577
  • HY-119256
    COR627

    		GABA Receptor 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 .
    COR627
  • HY-119082A
    VU0029767

    		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.
    VU0029767
  • HY-169501
    WIN 62577

    		Neurokinin Receptor mAChR SARS-CoV Infection Neurological Disease
    WIN 62577 is a species-selective tachykinin NK1 receptor antagonist. WIN 62577 is also an allosteric enhancer with micromolar potency at M3 receptors. WIN 62577 exhibits potent antiviral activity against SARS-CoV-2 .
    WIN 62577
  • HY-149453
    MCUF-651

    		Guanylate Cyclase Cardiovascular Disease
    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 .
    MCUF-651
  • 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 .
    UBP714
  • HY-139289S
    ART899

    		DNA/RNA Synthesis Cancer
    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 .
    ART899
  • HY-116149
    A-424274

    		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.
    A-424274
  • 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 .
    ADH-503
  • 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) .
    BIO-2007817
  • HY-119082
    (E/Z)-VU0029767

    		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.
    (E/Z)-VU0029767
  • 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 .
    (Z)-Leukadherin-1
  • 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 .
    CGP7930
  • 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 .
    UoS12258
  • 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 Emax .
    A3AR modulator 1
  • 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 .
    Norcyclizine
  • 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 .
    Pifusertib
  • 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 .
    Pifusertib hydrochloride
  • HY-154848
    UCL-TRO-1938
    1 Publications Verification

    		 PI3K Akt Cardiovascular Disease Neurological Disease Cancer
    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 .
    UCL-TRO-1938
  • 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 .
    AZ7976
  • HY-123525
    COR628

    		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 .
    COR628
  • HY-117440
    4'-Methoxy-S-trityl-L-cysteinol

    		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.
    4'-Methoxy-S-trityl-L-cysteinol
  • 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 .
    JGB-1-155
  • 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) .
    Lu AF58801
  • 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 .
    I1421
  • HY-121600
    GAT229

    		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 .
    GAT229

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