GPCR/G Protein

Items 251-300 of 6977

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  1. 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.
  2. CaSR activator

    AMG-073 (Cinacalcet) represents a new class of compounds for the treatment of hyperparathyroidism.
  3. NOP antagonist

    BAN ORL 24 is a potent and selective NOP receptor antagonist.
  4. D2 receptor agonist

    B-HT 920 is a dopamine agonist that has been proposed as an antiparkinsonian agent. It also has α1-adrenergic and α2-adrenergic agonist activity.
  5. adenosine A2A receptor agonist

    CGS 21680 is a selective adenosine A2A receptor agonist, with a Ki of 27 nM.
  6. RGS4 inhibitor

    CCG-63802 is a reversible inhibitor of regulator of G-protein signaling (RGS) proteins. Selective amongst RGS proteins, with greatest potency at RGS4.

  7. RGS inhibitor

    CCG-63808 is a reversible inhibitor of regulator of G-protein signaling (RGS) proteins.
  8. mGluR5 antagonists

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

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

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

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

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

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

    JDTic (dihydrochloride) is a potent antagonist of kappa-opioid receptors (KOR), blocking the κ-agonist U50, 488-induced antinociception.
  15. DP1 inhibitor

    Laropiprant is used in combination with niacin to reduce blood cholesterol. Laropiprant acts as a DP1 antagonist, reducing the vasodilation.
  16. 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.
  17. mGlu2 agonist

    LY2979165 is a mGlu2 agonist.
  18. CysLT1 receptor antagonist

    Montelukast (sodium) (MK0476) is a potent, selective CysLT1 receptor antagonist.
  19. 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).
  20. α2-adrenoceptor agonist

    Medetomidine(Domtor) is a potent, highly selective α2-adrenoceptor agonist (Ki values are 1.08 and 1750 nM for α2- and α1-adrenoceptors respectively).
  21. GCGR inhibitor

    MK 0893 is glucagon receptor antagonist as antidiabetic agents.
  22. EP4 receptor antagonist

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

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

    NPS-2143 hydrochloride (SB-262470A hydrochloride), an orally active calcilytic agent, is a selective and potent calcium ion-sensing receptor (CaSR) antagonist.
  25. CGRP1 receptor

    Olcegepant is a potent and selective non-peptide antagonist of the calcitonin gene-related peptide 1 (CGRP1) receptor with IC50 of 0.03 nM and Ki of 14.4 pM for human CGRP.
  26. CB1 modulator?€?

    Org 27569 is a potent CB1 receptor allosteric modulator (pEC50 = 8.24).
  27. EP4 antagonist

    ONO-AE3-208 is an EP4 antagonist, and suppresses cell invasion, migration, and metastasis of prostate cancer.
  28. nonimidazole inverse agonist

    Pitolisant is a potent and selective nonimidazole inverse agonist at the recombinant human histamine H3 receptor (Ki=0.16 nM).
  29. Pardoprunox is an antiparkinsonian drug currently under development by Solvay for the treatment of Parkinson's disease.
  30. CB1 receptor inverse agonist

    Rimonabant hydrochloride is a CB1 receptor inverse agonist.
  31. sGC stimulator

    Riociguat (BAY 63-2521; BAY 632521) is a stimulator of soluble guanylate cyclase (sGC).
  32. Dopamine agonist

    Rotigotine is dopamine D2 and D3 receptor agonist. Ki values are 13 and 0.71 nM for D2 and D3 respectively.
  33. 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.
  34. 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.
  35. 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.
  36. 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.
  37. 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.
  38. Dopamine receptor ligand

    ST-836 is a dopamine receptor ligand; Antiparkinsonian agent.
  39. 5-HT6 receptor antagonist

    SB271046 Hydrochloride is a potent, selective and orally active 5-HT6 receptor antagonist with pKi of 8.9.
  40. SIRT1 activator

    SRT3190 is a potent CXCR2 ligand.
  41. CB1 receptor inverse agonist

    Taranabant is a highly potent and selective cannabinoid 1 (CB1) receptor inverse agonist that inhibits the binding and functional activity of various agonists, with a binding Ki of 0.13 nM for the human CB1R in vitro.
  42. vasopressin receptor 2 antagonist

    Tolvaptan is a selective, competitive arginine vasopressin receptor 2 antagonist with an IC50 of 1.28μM.
  43. serotonin transporter (SER) inhibitor

    Vilazodone Hydrochloride (EMD 68843 Hydrochloride) is a serotonin transporter (SER) inhibitor and 5-HT1A receptor partial agonist.
  44. LTD4 receptor antagonist

    Verlukast (MK-0679) is a potent leukotriene D4 antagonist
  45. DL-Adrenaline is a hormone and a neurotransmitter secreted by the medulla of the adrenal glands. DL-Adrenaline is found in small amounts in the body and is essential for maintaining cardiovascular homeostasis because of its ability to divert blood to tissues under stress.
  46. Noradrenaline bitartrate monohydrate (Levophed) is a direct alpha-adrenergic receptors stimulator.
  47. CaSR agonist

    Strontium ranelate is an antiosteoporotic agent which both increases bone formation and reduces bone resorption, resulting in a rebalance of bone turnover in favor of bone formation. This is similar to the effects of choline stabilized orthosilicic acid.
  48. Brompheniramine maleate is a first-generation antihistamine. Brompheniramine works by acting as an antagonist of histamine H1 receptors. It also functions as a moderately effective anticholinergic agent, and is likely an antimuscarinic agent similar to other common antihistamines such as diphenhydramine.

  49. Ondansetron is a serotonin 5-HT3 receptor antagonist used mainly as an antiemetic (to treat nausea and vomiting). Ondansetron reduces the activity of the vagus nerve, which deactivates the vomiting center in the medulla oblongata, and also blocks serotonin receptors in the chemoreceptor trigger zone.
  50. Mirtazapine is a noradrenergic and specific serotonergic antidepressant (NaSSA) . Structurally, mirtazapine can also be classified as a tetracyclic antidepressant (TeCA).

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