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Results for "

allosteric enhancer

" in MedChemExpress (MCE) Product Catalog:

46

Inhibitors & Agonists

2

Peptides

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-B1456A
    Fenoprofen

    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 .
    Fenoprofen
  • 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 .
    Fenoprofen (Standard)
  • HY-103519
    rac-BHFF

    		GABA Receptor Neurological Disease
    rac-BHFF is a potent and orally active allosteric enhancer of GABAB receptor .
    rac-BHFF
  • 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-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 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 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-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-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-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-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-119339
    SX-682
    5 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-13619S
    Efaproxiral-d6

    		Isotope-Labeled Compounds Reactive Oxygen Species 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[1][2].
    Efaproxiral-d6
  • 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-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-15701B
    ADH-503

    (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-15701A
    (Z)-Leukadherin-1

    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

    		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-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-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-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-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-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 .
    GW791343 dihydrochloride
  • 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].
    Fenoprofen-13C6(sodium salt hydrate)
  • 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 .
    GW791343 trihydrochloride
  • 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-120327
    KY-226
    1 Publications Verification

    		 Phosphatase Neurological Disease Metabolic Disease
    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 .
    KY-226
  • HY-103520
    DS2

    		GABA Receptor Neurological Disease
    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 .
    DS2
  • HY-118140
    ZCZ011

    		Cannabinoid Receptor Neurological Disease Inflammation/Immunology
    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 .
    ZCZ011
  • HY-13509
    CCG-50014
    1 Publications Verification

    		 RGS Protein Inflammation/Immunology
    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 .
    CCG-50014
  • HY-107506
    Ro 67-4853

    		mGluR Neurological Disease
    Ro 67-4853 is a positive allosteric modulator (PAM) of mGluR1 (pEC50=7.16 for rmGlu1a receptor). Ro67-4853 exhibits activity at all group I mGlu receptors including hmGlu1, rmGlu1, and rmGlu5. Ro 67-4853 enhances the potency of L-Glu by interacting with the transmembrane domain (TMD) of the receptor. Ro 67-4853 potentiates sensory synaptic responses to repetitive vibrissa stimulation .
    Ro 67-4853
  • HY-151464
    SHP2/HDAC-IN-1

    		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 .
    SHP2/HDAC-IN-1
  • 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 .
    PDC31
  • HY-136258
    nAChR agonist CMPI hydrochloride

    		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 .
    nAChR agonist CMPI hydrochloride
  • 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 .
    BRD9876
  • HY-156025
    HCAR2 agonist 1

    		Others 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 .
    HCAR2 agonist 1
  • HY-117734
    PYD-106

    		iGluR Neurological Disease
    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 .
    PYD-106
  • HY-136190
    TRPC6-PAM-C20

    		TRP Channel Neurological Disease
    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 .
    TRPC6-PAM-C20

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