GPCR/G Protein

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Catalog No.
Product Name
Application
Product Information
Product Citation
  1. EP2 receptor agonist

    Taprenepag isopropyl is a highly selective EP2 receptor agonist.
  2. mGluR5 agonist

    CHPG is a selective mGluR5 agonist, and attenuates SO2-induced oxidative stress and inflammation through TSG-6/NF-κB pathway in BV2 microglial cells.
  3. MC4R agonist

    Setmelanotide (RM-493; BIM-22493; IRC-022493) is a selective melanocortin 4 receptor (MC4R) agonist with EC50s of 0.27 nM and 0.28 nM for human and rat MC4R, respectively.
  4. 5-HT3 partial agonist

    Pumosetrag Hydrochloride (MKC-733; DDP-733) is an orally available 5-HT3 partial agonist developed for the treatment of irritable bowel syndrome and gastroesophageal reflux disease.
  5. dual FPR1/FPR2/ALX agonist

    FPR Agonist 43 (compound 43) is a dual formyl peptide receptor 1 (FPR1) and formyl peptide receptor 2 (FPR2)/ALX agonist.
  6. adenosine A1 receptor agonist

    GR79236 is a highly potent and selective adenosine A1 receptor agonist (Ki = 3.1 nM) that has analgesic and anti-inflammatory actions in humans and animals.
  7. S1P1/S1P5 receptor agonist

    GSK2018682 is an agonist for S1P1 and S1P5 receptor with pEC50s of 7.7 and 7.2, respectively, and has no agonist activity towards human S1P2, S1P3, or S1P4. GSK2018682 is used in the research of multiple sclerosis.
  8. dopamine D4 receptor agonist

    ABT-670 is a selective, oral bioavailable agonist of dopamine D4 receptor, with EC50 of 89 nM, 160 nM, and 93 nM for human?D4, ferret?D4, and rat?D4, respectively.
  9. β3-adrenergic receptor agonist

    Solabegron (GW 427353) is a selective β3-adrenergic receptor agonist, stimulating cAMP accumulation in Chinese hamster ovary cells expressing the human β3-AR, with an EC50 value of 22 nM.
  10. metabotropic receptor agonist

    trans-ACPD, a metabotropic receptor agonist, produces calcium mobilization and an inward current in cultured cerebellar Purkinje neurons.
  11. Prostanoid EP2 receptor agonist

    Aganepag is a potent Prostanoid EP2 receptor agonist, with an EC50 of 0.19 nM, and shows no activity at EP4 receptor. Aganepag can be used in the research of wound healing, scar reduction, scar prevention and wrinkle treatment and prevention.
  12. GPR40 agonist

    Setogepram sodium salt (PBI-4050 sodium salt) acts as an orally active agonist for GPR40 and as an antagonist or inverse agonist for GPR84.
  13. 5-HT1A receptor agonist

    F-15599 is a highly selective G-protein biased 5-HT1A receptor agonist, with Ki of 3.4 nM.
  14. 5-HT3 receptor selective agonist

    Phenylbiguanide is a 5-HT3 receptor selective agonist with an EC50 of 3.0±0.1 μM.
  15. vasopressin V2-receptor agonist

    WAY-151932 is a vasopressin V2-receptor agonist with IC50 of 80.3 nM and 778 nM in human-V2 binding and V1a binding assay.
  16. A3 adenosine receptor agonist

    APNEA (N6-[2-(4-Aminophenyl)ethyl]adenosine) is a potent, non-selective A3 adenosine receptor agonist.
  17. 5-HT1A/5-HT1B receptors agonist

    RU 24969 is a selective agonist at the 5-HT1A and 5-HT1B receptors.
  18. 5-HT1A/5-HT1B/5-HT1C agonist

    Eltoprazine(DU28853) is a serenic or antiaggressive agent which as an agonist at the 5-HT1A and 5-HT1B receptors and as an antagonist at the 5-HT2C receptor.
  19. β2-adrenergic receptor agonist

    Levosalbutamol tartrate(levalbuterol) is the R-enantiomer of the short-acting β2-adrenergic receptor agonist salbutamol.
  20. REV-ERBα/β agonist

    SR9009 is a REV-ERBα/β agonist with IC50s of 670 nM and 800 nM for REV-ERBα and REV-ERBβ, respectively.
  21. REV-ERBα/β agonist

    SR9011 is a REV-ERBα/β agonist with IC50s of 790 nM and 560 nM for REV-ERBα and REV-ERBβ, respectively.
  22. GPR119 receptors agonist

    PSN632408 is an optimized agonist of GPR119 receptors that shows similar potency to OEA at both recombinant mouse and human GPR119 receptors, exhibiting EC50 values of 5.6 and 7.9 uM, respectively.
  23. S1P1 agonist

    Cenerimod (ACT-334441) is a potent and orally available sphingosine 1-phosphate 1 receptor (S1P1) agonist extracted from patent WO 2016184939 A1 and WO 2011007324 A1, example 1, with an EC50 of 2.7 nM.
  24. angiotensin-(1-7) receptor agonist

    AVE 0991 is a nonpeptide and orally active angiotensin-(1-7) receptor agonist with an IC50 of 21 nM.
  25. group II (mGlu2/3) receptor agonist

    Eglumegad (LY354740) is a highly potent and selective group II (mGlu2/3) receptor agonist with IC50s of 5 and 24 nM on transfected human mGlu2 and mGlu3 receptors, respectively.
  26. A1 receptor agonist

    N6-Cyclohexyladenosine is a selective A1 receptor agonist (EC50 = 8.2 nM).
  27. DP1/EP2 agonist

    Treprostinil sodium is a potent DP1 and EP2 agonist with EC50 values of 0.6??0.1 and 6.2??1.2 nM, respectively.
  28. A2AR/ENT1 agonist

    A2AR-agonist-1 is a potent A2AR and ENT1 agonist with Ki of 4.39 and 3.47 for A2AR and ENT1.
  29. endothelin receptor type B (ETB) agonist

    IRL-1620 is a potent and selective endothelin receptor type B (ETB) agonist with a Ki of 16 pM.
  30. Sigma-1 receptor agonist/muscarinic M1 agonist

    Blarcamesine, also known as AVex-73 and AE-37, is a muscarinic M1 agonist potentially for the treatment of Alzheimer's disease. It is an ς receptor ligand.
  31. mGlu2 receptor agonist

    LY2812223 is a highly potent, functionally selective mGlu2 receptor agonist with mGlu2 binding affinity for mGlu2 and mGlu3 (Ki=144 nM and 156 nM, respectively).
  32. sigma 1 receptor agonist

    Cutamesine (SA4503; AGY-94806) is a selective sigma 1 receptor(??1R) 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.
  33. group III mGluR receptors agonist

    O-Phospho-L-serine is the immediate precursor to L-serine in the serine synthesis pathway, and an agonist at the group III mGluR receptors (mGluR4, mGluR6, mGluR7, and mGluR8); O-Phospho-L-serine also acts as a weak antagonist for mGluR1 and a potent antagonist for mGluR2.
  34. FFAR1/GPR40 agonist

    AMG 837 is a potent GPR40 agonist (EC50=13 nM) with a superior pharmacokinetic profile and robust glucose-dependent stimulation of insulin secretion in rodents.

  35. TGR5 agonist

    INT-777 is a potent TGR5 agonist with an EC50 of 0.82 μM.
  36. 5-HT1A receptor agonist

    Befiradol (NLX-112) is a selective 5-HT1A receptor agonist.
  37. D3 receptor and D2 receptor partial agonist

    Cariprazine is a novel antipsychotic drug candidate that exhibits high affinity for the D3 (Ki=0.085 nM) and D2 (Ki=0.49 nM) receptors, and moderate affinity for the 5-HT1A receptor (Ki=2.6 nM).
  38. PAR2 agonist

    AC-55541 is a highly selective protease-activated receptor 2 (PAR2) agonist (pEC50=6.7), displays no activity at other PAR subtypes or at over 30 other receptors involved in nociception and inflammation.
  39. BRS-3 agonist

    MK-5046 is a novel BRS-3 agonist, binds to BRS-3 with high affinity (mouse Ki = 1.6 nM, human Ki = 25 nM).
  40. GHSR agonist

    Capromorelin Tartrate is an orally active, potent growth hormone secretagogue receptor (GHSR) agonist, with Ki of 7 nM for hGHS-R1a.
  41. Sigma receptor agonist

    Ditolylguanidine (1,3-Di-o-tolylguanidine) is an agonist of sigma receptor (??1/??2 receptor).
  42. prostaglandin EP2 agonist

    AGN 210676 is a selective prostaglandin EP2 agonist extracted from patent US20070203222A1, Compound example 23, has an EC50 of 5 nM.
  43. 5-HT(2C) receptor agonist

    WAY 163909 is a potent and selective 5-HT(2C) receptor agonist with a Ki of 10.5??1.1 nM.
  44. V2R agonist

    Fedovapagon is a selective vasopressin V2 receptor (V2R) agonist with an EC50 of 24 nM, which is being developed for the treatment of nocturia.
  45. S1PR1 agonist

    FTY720 (S)-Phosphate is an agonist of S1P receptor 1 (S1PR1), used in the research of acute inflammatory diseases such as acute lung injury.
  46. mu-opioid receptor agonist

    CYT-1010 hydrochloride is a mu-opioid receptor agonist extracted from patent WO2013173730A2, with EC50s of 13.1 nM and 0.0053 nM on beta-arrestin recruitment and inhibition of cAMP production, respectively.
  47. glucagon-like peptide-1 receptor agonist

    Exendin-4 Acetate (Exenatide acetate), a 39 amino acid peptide, is a long-acting glucagon-like peptide-1 receptor agonist with an IC50 of 3.22 nM.
  48. MC4R agonist

    PF-00446687 is a potent, selective melanocortin-4 receptor (MC4R) agonist with EC50 of 12????1 nM. Pf-446687 is brain penetrant.
  49. muscarinic receptor antagonist and β2-adrenoceptor agonist

    Batefenterol (GSK961081;TD-5959) is a novel muscarinic receptor antagonist and β2-adrenoceptor agonist; displays high affinity for hM2, hM3 muscarinic and hβ2-adrenoceptor with Ki values of 1.4, 1.3 and 3.7 nM, respectively.
  50. nonpeptide cholecystokinin 1 receptor agonist

    SR 146131 is a potent, orally available, and selective nonpeptide (cholecystokinin 1) receptor agonist.

Items 251-300 of 366

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