GPCR/G Protein

Items 1051-1100 of 5455

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Product Name
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  1. dopamine D2 receptor antagonist

    Sultopride (LIN-1418) is a selective antagonist of dopamine D2 receptor.
  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. mGluR1 antagonist

    FPTQ is mGluR1 antagonist with IC50 of 6 nM and 1.4 nM for human and mouse mGluR1 respectively.
  4. glucagon-like peptide 1 receptor antagonist

    GLP-1R Antagonist 1 (compound 5d) is an orally active, CNS penetrant and non-competitive antagonist of glucagon-like peptide 1 receptor (GLP-1R), with an IC50 of 650 nM.
  5. 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.
  6. 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.
  7. Angiotensin Receptor antagonist

    Elisartan is an orally active non-peptide pro-drug of angiotensin II AT1 receptor antagonist HN-12206, and shows anti-hypertension activities.
  8. Leukotriene B4 Receptor antagonist

    CP-105696 is a potent and selective Leukotriene B4 Receptor antagonist, with an IC50 of 8.42 nM.
  9. nonpeptide angiotensin II receptor antagonist

    L-159282 is a highly potent, orally active, nonpeptide angiotensin II receptor antagonist, with anti-hypertensive activity.
  10. triple tachykinin receptor antagonist

    CS-003 Free base (CS-003), a triple tachykinin receptor antagonist, shows high affinities for human (Neurokinin) NK1, NK2 and NK3 receptors with Ki values of 2.3 nM, 0.54 nM and 0.74 nM, respectively.
  11. thromboxane A2 synthase inhibitor

    Terbogrel is an orally available thromboxane A2 receptor antagonist and a thromboxane A2 synthase inhibitor, with both IC50s of about 10 nM.
  12. NK3R antagonist

    Fezolinetant is an antagonist of the neurokinin 3 receptor (NK3R), used for the treatment of menopausal hot flushes.
  13. 5-HT3 antagonist

    RG-12915 is a selective 5-HT3 antagonist, with IC50 value of 0.16 nM.
  14. PAF antagonist

    Ro 24-4736 is a potent, selective, p.o.-active platelet-activating factor (PAF) antagonist with a long duration of action.
  15. thromboxane synthesis inhibitor

    Ro-24-0238 is an antagonist of platelet activating factor (PAF) and inhibitor of thromboxane synthesis, used for lessening the inflammation and damage resulting from a local release of PAF.
  16. 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.
  17. histamine H2-receptor antagonist

    CP-66948 is a histamine H2-receptor antagonist with gastric antisecretory activity and mucosal protective properties.
  18. mGlu5 modulator

    JNJ-46778212 (VU 0409551) is an mGlu5 positive allosteric modulator with an EC50 of 260 nM.
  19. GRK2 inhibitor

    GSK180736A is a G protein-coupled receptor kinase 2 (GRK2) inhibitor with an IC50 of 0.77 μM.
  20. 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.
  21. 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.
  22. EP2 receptor antagonist

    TG4-155 is a potent, brain-permeant and selective EP2 receptor antagonist with a Ki of 9.9 nM.
  23. prostaglandin D2 antagonist

    AMG-009 is a potent antagonist of prostaglandin D2, with IC50 of 3 nM and 12 nM for CRTH2 and DP receptors, respectively.
  24. 5-HT1B receptor antagonist

    SB-616234A is a selective and orally bioavailable 5-HT1B receptor antagonist, with anxiolytic and antidepressant activity.
  25. 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.
  26. 5-HT2/sigma 2 receptor antagonist

    Roluperidone, also known as MIN-101, CYR-101, and MT-210, is a 5-HT2A and sigma 2 receptor antagonist potentially for the treatment of schizophrenia.
  27. neurokinin receptors antagonist

    SSR-241586 is an antagonist of neurokinin receptors. SSR-241586 is shown to be active in the treatment of depression, schizophrenia, urinary trouble, emesis, and irritable bowel syndrome (IBS).
  28. 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.
  29. metabotropic receptor agonist

    trans-ACPD, a metabotropic receptor agonist, produces calcium mobilization and an inward current in cultured cerebellar Purkinje neurons.
  30. CXCR2 antagonist

    Danirixin is a selective, and reversible CXCR2 antagonist, with IC50?of?12.5 nM for CXCL8.
  31. 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.
  32. 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.
  33. dual dopamine and serotonin receptor antagonist

    Deschloroclozapine is a dual dopamine and serotonin receptor antagonist with Kis of 200, 2500, 420, 39, 84, 40 nM for dopamine D1, D2,D4, and serotonin S2A, S2C, S3, respectively.
  34. 5-HT1A receptor agonist

    F-15599 is a highly selective G-protein biased 5-HT1A receptor agonist, with Ki of 3.4 nM.
  35. group I/group II mGluR antagonist

    E4CPG is a novel group I/group II metabotropic glutamate receptor antagonist, more potent than (RS)-MCPG .
  36. histamine H2 receptor antagonist

    BMY-25271 is a histamine H2 receptor antagonist.
  37. 5-HT3 receptor selective agonist

    Phenylbiguanide is a 5-HT3 receptor selective agonist with an EC50 of 3.0±0.1 μM.
  38. group I/group II mGluR antagonist

    (RS)-MCPG is a non-selective group I/group II metabotropic glutamate receptor antagonist.
  39. 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.
  40. CB1R antagonist

    JD-5037 is a novel, peripherally restricted CB1R antagonist with an IC50 of 1.5 nM.
  41. A3 adenosine receptor agonist

    APNEA (N6-[2-(4-Aminophenyl)ethyl]adenosine) is a potent, non-selective A3 adenosine receptor agonist.
  42. 5-HT1A/5-HT1B receptors agonist

    RU 24969 is a selective agonist at the 5-HT1A and 5-HT1B receptors.
  43. angiotensin II receptor type 1 antagonist

    Azilsartan medoxomil monopotassium is an orally administered angiotensin II receptor type 1 antagonist with IC50 of 0.62 nM, which used in the treatment of adults with essential hypertension.
  44. 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.
  45. β2-adrenergic receptor agonist

    Levosalbutamol tartrate(levalbuterol) is the R-enantiomer of the short-acting β2-adrenergic receptor agonist salbutamol.
  46. leukotriene A4 hydrolase inhibitor

    Acebilustat (CTX-4430) is a leukotriene A4 hydrolase inhibitor, used for an oral antiinflammatory drug.
  47. angiotensin II and endothelin A receptor antagonist

    Sparsentan (RE-021) is a highly potent dual angiotensin II and endothelin A receptor antagonist with Kis of 0.8 and 9.3 nM, respectively.
  48. thromboxane-prostaglandin receptor antagonist

    Terutroban is a thromboxane-prostaglandin receptor antagonist.
  49. 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.
  50. 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.

Items 1051-1100 of 5455

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