GPCR/G Protein

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  1. mGlu5 receptor antagonist

    MPEP is a potent, highly selective non-competitive antagonist at the mGlu5a receptor subtype (IC50 = 36 nM) while having no agonist or antagonist activities at the mGlu1b receptor at concentrations up to 30 uM.
  2. prostaglandin (PG) antagonist

    Aligeron is a non-selective prostaglandin (PG) antagonist, and has vasodilatory properties.
  3. 5-HT2B receptor antagonist

    PRX-08066, a Novel 5-Hydroxytryptamine Receptor 2B Antagonist, reduced monocrotaline-induced pulmonary arterial hypertension and right ventricular hypertrophy in rats.
  4. 5-HT Receptor antagonist

    Tandospirone is a partial agonist at 5HT1A receptors. It significantly reduces haloperidol-induced bradykinesia in a dose-dependent manner.
  5. Urotensin-II receptor antagonist

    Palosuran is a new potent and specific antagonist of the human UT receptor with an IC50 of 3.6??0.2 nM.
  6. AT1 receptor antagonist

    Eprosartan is an angiotensin II receptor antagonist used for the treatment of high blood pressure.
  7. CaSR antagonist

    NPS-2143 is a selective Ca2+-sensing receptor antagonist, shown to block increases in cytoplasmic Ca2+ concentrations elicited by human Ca2+ receptors expressed in HEK293 cells with an IC50 of 43 nM.
  8. 5-HT1D receptor antagonist

    BRL-15572 is a selective h5-HT1D antagonist, displaying 60-fold selectivity over h5-HT1B, and exhibiting little or no affinity for a range of other receptor types.

  9. 5-HT3 antagonist

    Tropisetron is a serotonin 5-HT3 receptor antagonist used mainly as an antiemetic to treat nausea and vomiting following chemotherapy.
  10. CGRP receptor antagonist

    MK-0974 (Telcagepant) is a potent and selective antagonist of the human and rhesus CGRP receptors.
  11. Opioid antagonist

    Alvimopan behaves as a peripherally acting μ-opioid antagonist. Alvimopan competitively binds to mu-opioid receptor in the gastrointestinal tract.
  12. D2 receptor antagonist

    Adoprazine is part of the Antidepressant Agent group
  13. Endothelin antagonist

    Avosentan (SPP301) is a potent and highly selective ETA receptor blocker.
  14. Serotonin 5HT3-receptor antagonist

    Alosetron Hydrochloride(1:X) (GR 68755 Hydrochloride(1:X)) is a Serotonin 5HT3-receptor antagonist that is used in treatment of irritable bowel syndrome.
  15. 5-HT3 antagonist

    Alosetron is a 5-HT3 antagonist that an antagonist action on the 5-HT3 receptors of the enteric nervous system of the gastrointestinal tract.
  16. NOP antagonist

    BAN ORL 24 is a potent and selective NOP receptor antagonist.
  17. mGluR5 antagonists

    Dipraglurant (ADX 48621) is a mGluR5 antagonists with IC50 of 0.021 μM.
  18. glucagon receptor antagonist

    Glucagon receptor antagonists-1 is a highly potent glucagon receptor antagonist.
  19. Glucagon receptor antagonist

    Glucagon receptor antagonists-2 is a highly potent glucagon receptor antagonist.
  20. Glucagon receptor antagonist

    Glucagon receptor antagonists-3 is a highly potent glucagon receptor antagonist.
  21. GPR40 antagonist

    GW-1100 is a selective GPR40 antagonist with a pIC50 of 6.9.
  22. κ-opioid receptor antagonist

    JDTic is a highly selective antagonist for the κ-opioid receptor; without affecting the μ- or δ-opioid receptors.
  23. KOR antagonist

    JDTic (dihydrochloride) is a potent antagonist of kappa-opioid receptors (KOR), blocking the κ-agonist U50, 488-induced antinociception.
  24. mGluR-2 antagonist

    LY 341495 has been shown to be a highly potent and selective group II metabotropic glutamate receptor (mGluR-2) antagonist with Ki / IC50 values are 2.3, 1.3, 173, 990, 6800, 8200 and 22000 nM for human mGluR-2, mGluR-3, mGluR-8 , mGluR-7a, mGluR-1a, mGluR-5a and mGluR-4a.
  25. CysLT1 receptor antagonist

    Montelukast (sodium) (MK0476) is a potent, selective CysLT1 receptor antagonist.
  26. Endothelin receptor antagonist

    Macitentan is an orally active, non-peptide dual endothelin ETA and ETB receptor antagonist for the potential treatment of idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH).
  27. EP4 receptor antagonist

    MK-2894 is a highly potent and selective second generation EP4 antagonist.
  28. EP4 antagonist

    MK-2894 sodium salt is a highly potent and selective second generation EP4 antagonist.
  29. CaSR antagonist

    NPS-2143 hydrochloride (SB-262470A hydrochloride), an orally active calcilytic agent, is a selective and potent calcium ion-sensing receptor (CaSR) antagonist.
  30. EP4 antagonist

    ONO-AE3-208 is an EP4 antagonist, and suppresses cell invasion, migration, and metastasis of prostate cancer.
  31. dopamine D3 receptor antagonist

    SB-277011 is a drug which acts as a potent and selective dopamine D3 receptor antagonist which is around 80-100x selective for D3 over D2 and lacks any partial agonist activity.
  32. A2a receptor antagonist

    SYN115 is an orally administered, potent and selective inhibitor of the adenosine 2a (A2a) receptor that is being developed initially for the treatment of Parkinson?€?s disease, but may also have utility in other CNS disorders.
  33. ETA receptor antagonist

    Sitaxentan sodium (TBC-11251) is a selective endothelin receptor-A antagonist with IC50 and Ki of 1.4 nM and 0.43 nM, respectively.
  34. ETA receptor antagonist

    Sitaxsentan (IPI 1040; TBC-11251) is a selective endothelin A (ETA) receptor antagonist. Antihypertensive. Sitaxsentan is used in treatment of chronic heart failure.
  35. OX Receptor Antagonist

    SB-408124 is a selective non-peptide orexin OX1 receptor antagonist (Kb values are 21.7 and 1405 nM for human OX1 and OX2 receptors respectively). Blocks orexin-A induced grooming following oral administration in vivo.
  36. 5-HT6 receptor antagonist

    SB271046 Hydrochloride is a potent, selective and orally active 5-HT6 receptor antagonist with pKi of 8.9.
  37. vasopressin receptor 2 antagonist

    Tolvaptan is a selective, competitive arginine vasopressin receptor 2 antagonist with an IC50 of 1.28μM.
  38. LTD4 receptor antagonist

    Verlukast (MK-0679) is a potent leukotriene D4 antagonist
  39. histamine receptor antagonist

    Cyproheptadine hydrochloride is a histamine receptor antagonist for 5-HT2 receptor with IC50 of 0.6 nM.
  40. NMDA receptor antagonist

    Orphenadrine citrate is a NMDA receptor antagonist with Ki of 6.0 +/- 0.7 μM, HERG potassium channel blocker.
  41. H2 receptor antagonist

    Lafutidine is a second generation H2 receptor antagonist having multimodal mechanism of action.
  42. 5-HT antagonist

    Tegaserod functions as a motility stimulant, achieving its desired therapeutic effects through activation of the 5-HT4 receptors of the enteric nervous system in the gastrointestinal tract. It also stimulates gastrointestinal motility and the peristaltic reflex, and allegedly reduces abdominal pain. Additionally, tegaserod is a 5-HT2B receptor antagonist.
  43. neurokinin-1 receptor antagonist

    Fosaprepitant (MK-0517, L-758,298) is a water-soluble phosphoryl prodrug for Aprepitant which is a NK1 antagonist.
  44. Prostaglandin D2 receptor CRTH2 antagonist

    CAY10471 Racemate (TM30089 Racemate) is a potent and highly selective prostaglandin D2 receptor CRTH2 antagonist.
  45. CCK-A receptor antagonist

    Loxiglumide (CR1505) is a cholecystokinin antagonist
  46. NT Antagonist

    SR 48692 represents a new, potent, nonpeptide antagonist radioligand of the NT receptor that differentiates between agonist- and antagonist-receptor interactions.
  47. D2/5-HT2 receptor antagonist

    Blonanserin is a D2/5-HT2 receptor antagonist; atypical antipsychotic.
  48. Leukotriene receptor antagonist

    Pranlukast is a selective cysteinyl leukotriene receptor antagonist.
  49. 5-HT7 receptor antagonist

    SB269970 is a potent and selective 5-HT7 receptor antagonist.
  50. CB1 antagonist

    CP 945598 is a potent and highly selective CB1 antagonist.

Items 101-150 of 627

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