GPCR/G Protein

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Catalog No.
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Product Citation
  1. GPR agonist

    TAK-875 is a potent, selective, and orally bioavailable GPR40 agonist.
  2. Opioid Receptor agonist

    ADL5859 HCl is a highly potent and selective δ opioid receptor agonist with Ki value to be 0.84 nM and ED50 value to be 20 nM.
  3. β1-selective adrenergic receptor agonist

    Norepinephrine (Levarterenol; L-Noradrenaline) is a β1-selective adrenergic receptor agonist with EC50 of 5.37 μM.
  4. Adenosine A2A Receptor Agonist

    CGS 21680 is a specific adenosine A2A subtype receptor agonist.
  5. CaSR agonist

    Strontium ranelate is an antiosteoporotic agent which both increases bone formation and reduces bone resorption, resulting in a rebalance of bone turnover in favor of bone formation. This is similar to the effects of choline stabilized orthosilicic acid.
  6. CB2 agonist

    JWH-133 is a potent selective CB2 receptor agonist, with a Ki of 3.4nM and selectivity of around 200x for CB2 over CB1 receptors.
  7. Sigma-2 receptor agonist

    Siramesine Hydrochloride is a selective sigma-2 receptor agonist, which has been shown to trigger cell death of cancer cells and to exhibit a potent anticancer activity in vivo.
  8. opioid κ-selective agonist

    Nalfurafine hydrochloride is a kappa-opioid receptor agonist
  9. Opioid Receptor Agonist

    Cebranopadol is a potent nociceptin/orphanin FQ peptide (NOP) and opioid receptor agonist
  10. sigma 1 receptor(σ1R) agonist

    SA4503 is a selective sigma 1 receptor(ς1R) agonist; high affinity for the sigma 1 receptor subtype labeled by (+)-[3H]pentazocine (IC50 = 17.4 +/- 1.9 nM); 100-fold less affinity for the sigma 2 receptor.
  11. mGlu2 receptor agonist

    LY 379268 is a highly selective group II mGlu receptor agonist (EC50 values are 2.69 and 4.48 nM for hmGlu2 and hmGlu3 respectively) that displays > 80-fold selectivity over group I and group III receptors.
  12. endothelin receptor agonist

    RO462005 is an endothelin receptor selective agonist.
  13. Adrenergic Receptor agonist

    Xylazine hydrochloride is an activator of α2A-AR, α2B-AR and α2C-AR.
  14. GPR40/FFA1 agonist

    AMG-837 calcium hydrate is a potent, orally bioavailable GPR40 agonist.
  15. 5-HT2C agonist

    S 32212 hydrochloride is an inverse agonist of 5-HT2C receptors (pKi = 8.18 at human 5-HT2C INI receptors).
  16. NTR1 agonist

    ML-314 is a brain penetrant nonpeptidic β-arrestin biased ggonist of the neurotensin NTR1 receptor, which exhibits full agonist behavior against NTR1 (EC50 = 2.0 μM) in the primary assay and selectivity against NTR2.
  17. EDG-1 (S1P1) agonist

    CYM 5442 HCl is a potent and selective EDG-1 (S1P1) agonist in vitro (EC50 = 1.35 nM).
  18. histamine H3 receptor agonist

    Immethridine hydrobromide is a strong and highly selective histamine H3 receptor agonist (pEC50 = 9.74) that displays 300-fold selectivity over the H4 receptor (pKi values are 9.07 and 6.61 respectively).
  19. β3 adrenergic agonist

    CL 316243 disodium salt, a beta-3 adrenergic agonist, was developed as an anti-obesity and diabetes drug, and causes rapid decreases in blood glucose levels in mice.
  20. β3-adrenergic receptors agonist

    BRL-37344 is a b3-AR (b 3-adrenoceptor) selective agonist with lipolytic activity.
  21. GLP-1 receptor agonist

    BETP is a selective positive allosteric modulator and partial agonist of the glucagon-like peptide 1 (GLP-1) receptor.
  22. NMDA& mGlu receptor agonist

    Ibotenic acid is a neuroexcitatory amino acid originally isolated from Amanita species that functions as a NMDA and metabotropic glutamate receptor agonist.
  23. GLP-1 receptor agonist

    ixisenatide inhibit glucagon release, markedly reduce postprandial glucago. have a promoting effct in diabetes mellitus (T2DM).
  24. cannabinoid agonist

    JWH 307 is a (1-naphthoyl)pyrrole cannabimimetic that potently activates both central cannabinoid (CB1) and peripheral cannabinoid (CB2) receptors (Ki values of 7.7 and 3.3 nM, respectively).
  25. κ1-opioid receptor agonist

    U-69593 is a potent, selective κ1-opioid receptor agonist (EC50 = 80-109 nM). Active in vivo. Antinociceptive.
  26. Adenosine A3-R agonist

    IB-MECA has been shown to act as a potent and selective Adenosine A3-R agonist with Ki values of 1.1, 54 and 56 nM for Adenosine A3-R, Adenosine A1-R and Adenosine A2A-R, respectively.
  27. Dopamine receptor agonist

    (+)-PD 128907 hydrochloride is a potent D3DR (dopamine receptor) agonist (Ki = 2.3 nM).
  28. μ-opioid receptor agonist

    Alvimopan dihydrate(LY 246736, ADL 8-2698) is a peripherally acting mu-opioid receptor (PAM-OR, IC50= 1.7 nM) antagonist for accelerating gastrointestinal recovery after surgery.
  29. μ-opioid receptor agonist

    Alvimopan monohydrate is a peripherally acting mu-opioid receptor (PAM-OR, IC50= 1.7 nM) antagonist for accelerating gastrointestinal recovery after surgery.
  30. LPA2 agonist

    GRI 977143, selective lysophosphatidic acid 2 (LPA2) receptor non-lipid agonist (EC50 = 3.3 uM).
  31. EP2 Agonist

    C-544326 is a potent and selective prostaglandin E2 receptor agonist with EC50 value of 2.8 nM.
  32. 5HT(1A) receptor agonist

    Eptapirone is a potent, selective, high efficacy 5-HT1A receptor agonist with marked anxiolytic and antidepressant potential.
  33. Orexin 2 receptor agonist

    A potent and selective Orexin2 receptor agonist.
  34. dopamine D2 receptor agonist

    UNC 9994 hydrochloride, unique, beta-arrestin-biased functionally selective dopamine D2 receptor (D2R) agonist (Ki value 30 nM; EC50 value 50 nM in ??-arrestin-2 recruitment assay) that exhibits antipsychotic activity in vivo. UNC9994 markedly inhibited PCP-induced hyperlocomotion in wild-type mice, which effect was completely abolished in ??-arrestin-2 knockout mice.
  35. GLP-1 receptor agonist

    Liraglutide is a long-acting glucagon-like peptide-1(GLP-1) receptor agonist.
  36. REV-ERBα/β agonist

    SR9011 is the agonist for REV-ERB-α with IC50 of 670 nM and REV-ERB-β with IC50 of 800 nM.
  37. CXCR4 agonist

    ATI-2341, pepducin targeting the C-X-C chemokine receptor type 4 (CXCR4) (EC50 = 194 nM, is an allosteric agonist activating the inhibitory heterotrimeric G protein (Gi) to promote inhibition of cAMP production and induce calcium mobilization.
  38. β-adrenoceptor agonist

    Indacaterol (QAB149) maleate is an ultra-long-acting β-adrenoceptor agonist.
  39. GLP-1 agonist

    Albiglutide is a glucagon-like peptide-1 agonist (GLP-1 agonist).
  40. Endogenous galanin receptor agonist

    Galanin (1-30) (human) is an endogenous peptide with multiple endocrine, metabolic and behavioral effects
  41. NK3 receptor agonist

    Senktide is a potent, selective agonist of the neuromedin K3 (NK3) receptor (EC50 = 0.5-3 nM).
  42. CNS penetrant mGlu7/8 receptor agonist

    VU6005649 is a CNS penetrant mGlu7/8 receptor agonist with EC50s of 0.65 μM and 2.6 μM for mGlu7 receptor and mGlu8 receptor, respectively.
  43. GPR39 agonist

    TM N1324 is an agonist of G-Protein-Coupled Receptor 39 (GPR39) with EC50s of 9 nM/5 nM in the presence of Zn2+, and 280 nM/180 nM in the absence of Zn2+ for human/murine GPR39.
  44. 5-HT(2A) receptor agonist

    Temanogrel, also known as APD791, is a highly selective 5-hydroxytryptamine2A receptor inverse agonist under development for the treatment of arterial thrombosis.
  45. beta-adrenergic agonist

    Nylidrin hydrochloride is a beta-adrenergic agonist. Nylidrin hydrochloride is shown to be an effective inhibitor of IgE-mediated release of histamine from human basophils, and thus can be used as antiallergic agent.
  46. Somatostatin Receptor agonist

    Pasireotide(SOM 230) is a stable cyclohexapeptide somatostatin mimic that exhibits unique high-affinity binding to human somatostatin receptors (subtypes sst1/2/3/4/5, pKi=8.2/9.0/9.1/<7.0/9.9 respectively).
  47. Rev-Erbα/β agonist

    SR10067 is a potent, selective and brain penetrant Rev-Erbα/β agonist, with IC50 values are 160 and 170 nM for Rev-Erbβ and Rev-Erbα, respectively. SR10067 has anxiolytic activity.
  48. angiotensin 1 (AT1) and AT2 receptor agonist

    Angiotensin III is an angiotensin 1 (AT1) and AT2 receptor agonist.
  49. β3-adrenoceptor agonist

    Amibegron hydrochloride is a selective β3-adrenoceptor agonist, with an EC50 of 3.5 nM for β-adrenoceptor in rat colon; Amibegron hydrochloride has anxiolytic and antidepressant activity.
  50. Adenosine receptor agonist

    N6-Ethyladenosine is an adenosine derivative, acts as a Adenosine receptor agonist, with Kis of 4.9 and 4.7 nM for hA1AR and hA3AR, respectively.

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