GPCR/G Protein

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Product Name
Application
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Product Citation
  1. PPARγ and CB2 receptor dual agonist

    VCE-004.8, a semi-synthetic multitarget cannabinoquinoid, is a specific PPARγ and CB2 receptor dual agonist with potent anti-inflammatory activity.
  2. LPA2 agonist

    Radioprotectin-1 is a potent and specific nonlipid agonist of lysophosphatidic acid receptor 2 (LPA2), with an EC50 value of 25 nM for murine LPA2 subtype.
  3. 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.
  4. β2 adrenergic receptor agonist

    BI-167107 is a high affinity, full agonist that binds to the β2 adrenergic receptor (β2AR) with a dissociation constant Kd of 84 pM.
  5. non-peptide PAR2 agonist

    GB110 is a Novel potent non-peptide PAR2 agonist. GB-110 selectively induces PAR2-mediated intracellular Ca2+ release in HT29 cells with an EC50 of 0.28 μM.
  6. GPRC6A agonist

    DJ-V-159 is an agonist for G protein-coupled receptor family C group 6 member A (GPRC6A).
  7. non-peptide MAS agonist

    AR234960, a non-peptide MAS (a G protein-coupled receptor) agonist, increases both mRNA and protein levels of CTGF via ERK1/2 signaling in HEK293-MAS cells and adult human cardiac fibroblasts.
  8. D1 receptor agonist

    PF-06256142 is a potent and selective orthosteric agonist of the D1 receptor, with D1 EC50=30 nM and D1 binding Ki = 12 nM.
  9. GLP-1 receptor agonist

    Semaglutide, a long-acting GLP-1 analogue, is a glucagon-like peptide-1 (GLP-1) receptor agonist that can be used in the treatment of type 2 diabetes.
  10. TSHR agonist

    ML-109 is a potent and full thyroid stimulating hormone receptor (TSHR) agonist, with an EC50 of 40 nM.
  11. histamine H4 receptor inverse agonist

    H4 Receptor antagonist 1 is a potent and selective histamine H4 receptor inverse agonist, with an IC50 of 19 nM.
  12. angiotensin 1 (AT1) and AT2 receptor agonist

    Angiotensin III is an angiotensin 1 (AT1) and AT2 receptor agonist.
  13. mGlu3 receptor agonist

    LY2794193 is a highly potent and selective mGlu3 receptor agonist (hmGlu3 Ki=0.927 nM??EC50=0.47 nM; hmGlu2 Ki=412 nM??EC50=47.5 nM).
  14. GPR40 full agonist

    GPR40 agonist 1 is a potent and novel GPR40 full agonist with an EC50 of 2 nM and 17 nM for hGPR40 and rGPR40, respectively.
  15. GPR120 agonist

    GPR120 Agonist 2 is a GPR120 agonist extracted from patent US 20110313003 A1, example 209.
  16. 5-HT agonist

    8-OH-DPAT is a potent and selective 5-HT agonist, with a pIC50 of 8.19 for 5-HT1A and a Ki of 466 nM for 5-HT7; 8-OH-DPAT weakly binds to 5-HT1B (pIC50, 5.42), 5-HT (pIC50 <5).
  17. β-adrenergic agonist

    Imoxiterol (RP 58802B) is a β-adrenergic agonist.
  18. 5-HT2C receptor-selective agonist

    Vabicaserin hydrochloride is a 5-hydroxytryptamine 2C (5-HT2C) receptor-selective agonist with an EC50 of 8 nM.
  19. Human CXCR3 agonist

    PS372424, a three amino-acid fragment of CXCL10, is a specific human CXCR3 agonist with anti-inflammatory activity, which inhibits the binding of CXCR3 ligand CXCL10 to CXCR3 receptor with IC50 of 42 nM.
  20. CB2 agonist

    Olorinab (APD 371) is a highly potent, selective and fully efficacious cannabinoid receptor type 2 (CB2) agonist, with an EC50 of 6.2 nM for hCB2.
  21. 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.
  22. S1P1 and S1P5 agonist

    ASP-4058 is a next-generation, selective and oral bioactive agonist for Sphingosine 1-Phosphate receptors 1 and 5 (S1P1 and S1P5), ameliorates rodent experimental autoimmune encephalomyelitis with a favorable safety profile.
  23. Adenosine A1 receptor agonist

    N6-Cyclopentyladenosine (CPA) is a selective Adenosine A1 receptor agonist, with Ki values of 2.3 nM, 790 nM and 43 nM for human A1, A2A and A3 receptors, respectively.
  24. 5-HT6 agonist

    EMDT oxalate is a selective 5-HT6 agonist, and has antidepressant effects.
  25. GPR120 agonist

    GPR120 Agonist 1 is a potent and selective GPR120 agonist, and possesses promising antidiabetic effect and good safety profile to be a development candidate.
  26. GLP-1R agonist

    GLP-1 receptor agonist 2 is a glucagon-like peptide-1 receptor (GLP-1R) agonist.
  27. CaSR agonist

    GSK3004774 is a potent, nonabsorbable agonist of CaSR, with an pEC50 of 7.3, 6.6 and 6.5 for human, mouse and rat CaSR, respectively. GSK3004774 shows an EC50 of 50 nM for human CaSR.
  28. GLP-1 receptor agonist

    GLP-1 receptor agonist 1 is a glucagon-like peptide-1 (GLP-1) receptor agonist extracted from patent WO2018056453A1, Compound 67.
  29. CB1 agonist

    Leelamine hydrochloride is a tricyclic diterpene molecule that is extracted from the bark of pine trees. Leelamine hydrochloride is a cannabinoid receptor type 1 (CB1) agonist and a inhibitor of SREBP1-regulated fatty acid/lipid synthesis in prostate cancer cells that is not affected by androgen receptor status.
  30. 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.
  31. GPR35/CXCR8 agonist

    Kynurenic acid sodium, an endogenous tryptophan metabolite, is a broad-spectrum antagonist targeting NMDA, glutamate, α7 nicotinic acetylcholine receptor. Kynurenic acid sodium is also an agonist of GPR35/CXCR8.
  32. NOP agonist

    MT-7716 hydrochloride (W-212393 hydrochloride) is a selective non-peptide nociceptin receptor (NOP) agonist and promising potential treatment drug for alcohol abuse and relapse prevention.
  33. A1 adenosine receptor agonist

    N6-(2-Phenylethyl)adenosine is a selective A1 adenosine receptor agonist.
  34. EP4 partial agonist

    GSK726701A is a novel prostaglandin E2 receptor 4 (EP4) partial agonist with a pEC50 of 7.4.
  35. GPR40/FFAR1 agonist

    GPR40/FFAR1 modulator 1 is an agonist and an allosteric modulator for Gq-coupled free fatty acid receptor 1 (GPR40/FFAR1).
  36. 5-HT7 receptor agonist

    5-HT7 agonist 1 is a selective 5-HT7 receptor agonist, with an IC50 of 222.93 nM, can be used for the 5-HT7 receptor related disease, such as CNS disorders.
  37. dopamine receptor agonist

    Foslevodopa is a dopamine receptor agonist.
  38. dopamine receptor agonist

    Foscarbidopa (Carbidopa 4??-monophosphate) is a prodrug of Carbidopa, acts as a dopamine receptor agonist.
  39. Gpr120 agonist

    GPR120-IN-1 is a selective Gpr120 agonist with a logEC50 of ?7.62.
  40. dopamine D1 receptor agonist

    (+)-Dihydrexidine hydrochloride ((+)-DAR-0100 hydrochloride) is a dopamine D1 receptor agonist with an EC50 of 72± 21 nM.
  41. A2A adenosine agonist

    PD 117519 (CI947) is an A2A adenosine agonist which has shown oral antihypertensive activity in pharmacological animal models.
  42. LHCGR/TSHR agonist

    Org41841 is a partial agonist of both luteinizing hormone/chorionic gonadotropin receptor (LHCGR) and thyroid-stimulating hormone receptor (TSHR) with EC50s of 0.2 and 7.7 μM, respectively.
  43. GPBAR1 agonist

    BAR501 is a potent and selective agonist of GPBAR1 with an EC50 of 1 μM.
  44. dual FXR and GPBAR1 agonist

    BAR502 is a dual FXR and GPBAR1 agonist with IC50 values of 2 μM and 0.4 μM, respectively.
  45. S1P receptor agonist

    S1p receptor agonist 1 is an S1P receptor agonist extracted from patent WO 2015039587 A1, compound example 2.
  46. histamine H4 receptor agonist

    VUF10460 is a non-imidazole histamine H4 receptor agonist; binds to rat H4 receptor with a pKi of 7.46.
  47. S1P3 receptor agonist

    CYM-5541 (ML249) is an selective and allosteric S1P3 receptor agonist with an EC50 between 72 and 132 nM.
  48. mGluR agonist

    L-Cysteinesulfinic acid is a potent agonist at several rat metabotropic glutamate receptors (mGluRs) with pEC50s of 3.92±0.03, 4.6±0.2, 3.9±0.2, 2.7±0.2, 4.0±0.2, and 3.94±0.08 for mGluR1, mGluR5, mGluR2, mGluR4, mGluR6, and mGluR8, respectively.
  49. μ opioid receptor agonist

    PZM21 is a potent and selective μ opioid receptor agonist with an EC50 of 1.8 nM.
  50. EP2 receptor agonist

    Taprenepag isopropyl is a highly selective EP2 receptor agonist.

Items 201-250 of 364

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