GPCR/G Protein

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Product Citation
  1. A3 adenosine receptor agonist

    AB-MECA is a high affinity A3 adenosine receptor agonist, has high affinity for recombinant A1 and A3 receptors.
  2. 5-HT2c receptor agonist

    PRX933 hydrochloride is a 5-HT2c receptor agonist extracted from patent WO 2014140631 A1.
  3. human 5-HT1A receptor agonist

    AP521 is an agonist of human 5-HT1A receptor with an IC50 of 94 nM.
  4. 5-HT2C receptor agonist

    YM348 is a potent and orally active 5-HT2C receptor agonist, which shows a high affinity for cloned human 5-HT2C receptor (Ki: 0.89 nM).
  5. cannabinoid CB2 receptor inverse agonist

    CB2R-IN-1 is a potent cannabinoid CB2 receptor inverse agonist with a Ki of 0.9 nM.
  6. σ1 agonist

    4-IBP is a selective ς1 agonist with a high level of affinity for the ς1 receptor (Ki = 1.7 nM) and a moderate affinity for the ς2 receptor (Ki = 25.2 nM) .
  7. Dopamine D2 autoreceptor agonist

    NMI 8739 is a dopamine D2 autoreceptor agonist, which is an amine conjugate of the DHA carrier and the neurotransmitter dopamine.
  8. CB2 inverse agonist

    SR 144528 is a selective peripheral cannabinoid receptor inverse agonist that displays a Ki value of 0.6 nM for rat spleen and human recombinant CB2 receptors and a Ki value of 400 nM for rat brain and human recombinant CB1 receptors.
  9. GPR35/CXCR8 agonist

    GPR35 agonist 1 (compound 50) is a potent and specific G protein-coupled receptor-35 (GPR35)/CXCR8 agonist with an EC50 of 5.8 nM, displays good druggability.
  10. 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.
  11. 5-HT2C receptor agonist

    CP-809101 is a potent and selective 5-HT2C receptor agonist with pEC50 of 9.96/7.19/6.81 for human 5-HT2C/5-HT2B/5-HT2A receptors respectively.
  12. A2A adenosine agonist

    Regadenoson was selective agonist for the A2A adenosine receptor versus the A1, A2B, and A3 receptors in binding and functional studies. Regadenoson was also found to be a full and potent agonist to cause coronary vasodilation, a response that has a very large A2A receptor reserve?
  13. opioid κ-selective agonist

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

    Cebranopadol is a potent nociceptin/orphanin FQ peptide (NOP) and opioid receptor agonist
  15. TGR5 agonist

    SB756050 is a selective TGR5 agonist currently in phase 1clinical trials for the treatment of type 2 diabetes.
  16. β3-adrenergic receptor agonist

    β3-AR agonist 1 (compound 15) is a highly potent, selective, and orally available β3-adrenergic receptor (β3-AR) agonist (EC50=18 nM), being inactive to β1-, β2-, and α1A-AR (β1/β3, β2/β3, and α1A/β3>556-fold).
  17. beta2-adrenergic agonist

    Arformoterol tartrate is a beta2-adrenergic agonist
  18. 5-HT1A receptor agonist

    Lesopitron dihydrochloride is a full and selective 5-HT1A receptor agonist with IC50 of 125 nM in rat hippocampal membranes.
  19. GPR109A agonist

    MK-6892 is a potent, selective, and full agonist for the high affinity nicotinic acid (NA) receptor GPR109A.K i and GTPγS EC 50 of MK-6892 on the Human GPR109A is 4 nM and 16 nM, respectively.
  20. 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.
  21. FFA1/GPR40 Agonist

    TUG-770 is a Highly Potent Free Fatty Acid Receptor 1 (FFA1/GPR40) Agonist for Treatment of Type 2 Diabetes.
  22. α2 adrenergic agonist

    AGN 192836 is a potent and selective α2 adrenergic agonist with EC50s of 8.7, 41 and 6.6 nM for α2A, α2B and α2C receptor, respectively.
  23. Sigma-2 receptor agonist

    Anti-cancer agent siramesine is a lysosomotropic detergent that induces cytoprotective autophagosome accumulation.
  24. Adrenergic Receptor agonist

    Tetrahydrozoline Hydrochloride is an alpha agonist which causes constriction of conjunctival blood vessels.
  25. D2 agonist

    Naxagolide is a dopamine D2-receptor agonist which is used for the treatment of extrapyramidal disorders.
  26. dopamine D2-receptor agonist

    ent Naxagolide Hydrochloride is a dopamine D2-receptor agonist which is used for the treatment of extrapyramidal disorders. This compound is an antiparkinsonian drug.
  27. 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.
  28. ultra-long-acting β??? adrenoreceptor agonist

    Vilanterol is a novel and selective agonist of Beta2-AR with a PEC50 value of 10.37??0.05.
  29. 5-HT1B/1D receptors agonist

    Donitriptan is a potent, high efficacy agonist at 5-HT1B/1D receptors with pKis of 9.4 and 9.3, respectively.
  30. PAR2 agonist

    AC-264613 is a potent and selective protease-activated receptor 2 (PAR2) agonist (pEC50 = 7.5).
  31. endothelin receptor agonist

    RO462005 is an endothelin receptor selective agonist.
  32. A1 adenosine receptor agonist

    Tecadenoson (CVT-510) is a selective A1 adenosine receptor agonist.
  33. β-adrenergic receptors agonist

    Cimaterol is a potent agonist of β-adrenergic receptors (pEC50 = 8.13, 8.78, and 6.62 for human β1, β2, and β3, respectively).
  34. α2- adrenoceptor antagonist / I2 imidazoline receptor agonist

    Idazoxan hydrochloride is an α2-AR adrenoceptor antagonist and potential I2 imidazoline receptor agonist. Also displays I1 imidazoline receptor antagonist activity. (pKi values are 5.90, 7.22, 8.01, 7.43, and 7.7 for I1, I2, α 2A, α2B, and α 2C receptors respectively).
  35. imidazoline receptor 1 agonist

    Moxonidine hydrochloride is a centrally acting antihypertensive agent.
  36. Adrenergic Receptor agonist

    Tulobuterol is a beta-adrenergic receptor agonist that is related structurally to Terbutaline.
  37. Adrenoceptors agonist

    UK 14,304 tartrate is a water-soluble form UK 14,304. It is a full α2 adrenergic agonist.
  38. Adrenergic Receptor agonist

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

    AMG-837 calcium hydrate is a potent, orally bioavailable GPR40 agonist.
  40. δ opioid receptor agonist

    ADL5747 is a selective, nonpeptidic δ opioid receptor agonist.
  41. Kainate receptor agonist

    Kainate class of ionotropic glutamate receptor agonist. Has been shown to induce seizures and neurodegeneration in vivo and has also been used to induce experimental epilepsy in rodents and to examine excitation-induced neuronal apoptosis mechanisms.
  42. prostanoid DP-receptor (DP1) agonist

    BW 245C is a prostanoid DP-receptor (DP1) agonist, used to treat stroke.
  43. 5-HT2C agonist

    S 32212 hydrochloride is an inverse agonist of 5-HT2C receptors (pKi = 8.18 at human 5-HT2C INI receptors).
  44. D2 dopamine partial agonist

    Brexpiprazole is a novel D2 dopamine partial agonist investigational product currently in clinical trials for the treatment of depression, schizophrenia, and attention deficit hyperactivity disorder (ADHD).
  45. 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.
  46. SMO agonist

    SAG is a chlorobenzothiophene-containing compound which acts as a SMO agonist (EC50 = 3 nM) but inhibits hedgehog signaling at high concentrations (>1 uM).
  47. 2A-AR adrenergic agonist

    Guanabenz acetate is an a2A-AR adrenergic agonist and IGRS (imidazoline I2 binding site) selective ligand.
  48. EDG-1 (S1P1) agonist

    CYM 5442 HCl is a potent and selective EDG-1 (S1P1) agonist in vitro (EC50 = 1.35 nM).
  49. 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).
  50. 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.

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