GPCR/G Protein

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Catalog No.
Product Name
Application
Product Information
Citations
  1. angiotensin II receptor antagonist

    Valsartan (CGP-48933) is an angiotensin II receptor antagonist for the treatment of high blood pressure and heart failure.
  2. LTD4 receptor antagonist

    Zafirlukast is a potent orally active leukotriene D4 (LTD4) receptor antagonist.
  3. 5-HT (serotonin) and dopamine receptor antagonist

    Ziprasidone hydrochloride monohydrate (CP 88059 hydrochloride monohydrate) is a combined 5-HT (serotonin) and dopamine receptor antagonist which exhibits potent effects of antipsychotic activity.
  4. SMO Antagonist

    LY2940680 has been shown to affect a cancer cell signaling pathway initiated by the Hedgehog (Hh) protein.
  5. neurokinin-1 receptor antagonist

    Fosaprepitant is a selective neurokinin-1 (NK-1) receptor antagonist.
  6. Opioid Receptor agonist

    ADL5859 HCl is a highly potent and selective δ opioid receptor agonist with Ki value to be 0.84 nM and ED50 value to be 20 nM.
  7. ETAR/ETBR inhibitor

    Bosentan is a competitive antagonist of endothelin-1 at the endothelin-A (ET-A) and endothelin-B (ET-B) receptors.
  8. CXCR2 ligand

    SRT3109 is a CXCR2 ligand for use in the treatment of chemokine mediated diseases and conditions.
  9. 5-HT Receptor antagonist

    LY310762 is a 5-HT1D-preferring receptor antagonist (EC50 = 31 nM).
  10. Serotonin reuptake inhibitor

    Vilazodone acts as a serotonin reuptake inhibitor (IC50 = 0.5 nM) and 5-HT1A receptor partial agonist (IC50 = 0.2 nM; IA = ~60-70%).
  11. H3-receptor antagonist

    Ciproxifan maleate is a potent, selective H3 histamine receptor antagonist.
  12. Piribedil D8 is the deuterium labeled Piribedil, which is an antiparkinsonian agent.
  13. A3 adenosine receptor allosteric modulator

    LUF6000 is an allosteric modulator of the human A3 adenosine receptor (AR).
  14. Droxidopa(L-DOPS), the mixture of Droxidopa (w/w80%) and Pharmaceutical starch (w/w20%), acts as a prodrug to the neurotransmitters norepinephrine (noradrenaline) and epinephrine (adrenaline).
  15. NK1 receptor antagonist

    Vofopitant dihydrochloride (GR 205171A) is a potent, selective and orally available tachykinin neurokinin 1(NK1) receptor antagonist.
  16. vasopressor/antihypotensive agent

    Midodrine D6 hydrochloride is deuterium labeled Midodrine, which is a vasopressor/antihypotensive agent.
  17. CXCR3 antagonist

    SCH 546738 is a potent, orally active and non-competitive CXCR3 antagonist, the affinity constant (Ki) of SCH 546738 binding to human CXCR3 receptor is determined to be 0.4 nM in multiple experiments.
  18. CRHR1 antagonist

    DMP 696 is a selective corticotropin-releasing hormone receptor 1 (CRHR1) antagonist, used for the treatment of anxiety and depression.
  19. Alimemazine D6 is deuterium labeled Alimemazine, which is an antihistamine.
  20. Indoramin D5 is deuterium labeled Indoramin, which is a piperidine antiadrenergic agent.
  21. GPR3 inverse agonist

    AF64394 is a GPR3 inverse agonist, with a pIC50 of 7.3.
  22. angiotensin II receptor antagonist

    Losartan D4 Carboxylic Acid is the deuterium labeled Losartan(EXP-3174), which is an angiotensin II receptor antagonist.
  23. glucagon-like peptide-1 receptor agonist

    Exendin-4 (Exenatide), a 39 amino acid peptide, is a long-acting glucagon-like peptide-1 receptor agonist with an IC50 of 3.22 nM.
  24. Neurokinin-1 (NK-1) receptor antagonist

    Serlopitant is a selective Neurokinin-1 (NK-1) receptor antagonist.
  25. angiotensin II type 1 receptor antagonist

    Azilsartan D5 is the deuterium labeled Azilsartan(TAK-536), which is a specific and potent angiotensin II type 1 receptor antagonist.
  26. β1-selective adrenergic receptor agonist

    Norepinephrine hydrochloride (Levarterenol hydrochloride; L-Noradrenaline hydrochloride) is a β1-selective adrenergic receptor agonist with EC50 of 5.37 μM.
  27. PGD2 receptor type 2 (DP2) antagonist

    AM211 is a potent, selective and orally bioavailable prostaglandin D2 (PGD2) receptor type 2 (DP2) antagonist, with IC50s of 4.9 nM, 7.8 nM, 4.9 nM, 10.4 nM for human, mouse, guinea pig, and rat DP2, respectively.
  28. partial dopamine D2 and D3 receptor agonist

    Pardoprunox hydrochloride is a novel partial dopamine D2 and D3 receptor agonist and serotonin 5-HT1A receptor agonist, D2 (pKi = 8.1) and D3 receptor (pKi = 8.6) partial agonist and 5-HT1A receptor (pKi = 8.5) full agonist.
  29. TSHR inverse agonist

    ML224(NCGC00242364; ANTAG3) is a selective TSHR inverse agonist; inhibits TSH-stimulated cAMP production with an IC50 = 2.3 μM.
  30. GPR40 activator

    GPR40 Activator 2 is a potent GPR40 activator from patents WO 2012147516 A1, WO 2012046869A1 and WO 2011078371 A1.
  31. sGC inhibitor

    NS-2028 is a highly selective soluble Guanylyl Cyclase (sGC) inhibitor with IC50 values of 30 nM and 200 nM for basal and NO-stimulated enzyme activity.
  32. OT-R antagonist

    OT-R antagonist 2 is a nonpeptide low molecular weight OT-R antagonist. OT-R antagonist 2 inhibitis IP3-Synthesis, rat OT-R (IC50 = 0.33 μM).
  33. adenosine A1 receptor antagonist

    Rolofylline (KW-3902) is a potent, selective adenosine A1 receptor antagonist that is under development for the treatment of patients with acute congestive heart failure and renal impairment.
  34. mGlu2 agonist/mGlu3 antagonist

    LY541850 is a selective orthosteric mGlu2 agonist and mGlu3 antagonist with IC50 values of 0.161 μM and 0.038 μM, respectively.
  35. GPR88 receptor agonist

    (1R,2R)-2-PCCA hydrochloride is a diastereomer of 2-PCCA, and acts as a potent GPR88 receptor agonist, with an EC50 of 3 nM in cell-free assay, and 603 nM in cell assay.
  36. CGRP antagonist

    Ubrogepant (MK-1602) is a novel oral calcitonin gene-related peptide receptor (CGRP) antagonist in development for acute treatment of migraine.
  37. Smo receptor agonist

    SAG (hydrochloride) is a potent Smo receptor agonist, and activates the Hedgehog signaling pathway, with a Kd of 59 nM.
  38. triple reuptake inhibitor

    Dasotraline hydrochloride (SEP-225289 hydrochloride) is a triple reuptake inhibitor that blocks dopamine, norepinephrine, and serotonin transporters with IC50 values of 4, 6, and 11 nM, respectively.
  39. AT2R antagonist

    Olodanrigan (EMA401) is a highly selective, orally active, peripherally restricted angiotensin II type 2 receptor (AT2R) antagonist.
  40. CB1 antagonist/inverse agonist

    Taranabant racemate is an antagonist and/or inverse agonist of the Cannabinoid-1 (CB1) receptor extracted from patent WO 2004048317 A1.
  41. CB1 receptor inverse agonist

    Taranabant (1R,2R)stereoisomer is the R-enantiomer of Taranabant. Taranabant is a highly potent and selective cannabinoid 1 (CB1) receptor inverse agonist.
  42. 5-HT2C receptor antagonist

    SB 242084 is a 5-HT2C receptor antagonist(pKi=9.0) that displays 158- and 100-fold selectivity over 5-HT2A and 5-HT2B receptors respectively.
  43. nociceptin receptor agonist

    MCOPPB 3Hcl is a nociceptin receptor agonist with pKi of 10.07; weaker activity at other opioid receptors.
  44. 5-HT1F receptor agonist

    LY 344864 S-enantiomer is the S-enantiomer of LY344864. LY344864 is a 5-HT1F receptor agonist.
  45. 5-HT1F agonist

    LY 344864 hydrochloride is a selective 5-HT1F agonist with a Ki of 6 nM.
  46. SSTR5 antagonist

    SSTR5 Antagonist 1 (compound 10) is a highly potent, oral active and selective somatostatin (receptor) subtype 5 (SSTR5) antagonist and has potential to treat type 2 diabetes mellitus (T2DM).
  47. D1/D5 receptor full agonist

    SKF-82958 hydrobromide is a D1/D5 receptor full agonist.
  48. CRF1 antagonist

    NVS-CRF38 is a novel corticotropin-releasing factor receptor 1 (CRF1) antagonist with low water solubility.
  49. GPR40 agonist

    AM-4668 is a GPR40 agonist for type 2 diabetes. EC50s of 3.6 nM and 36 nM for GPR40 in A9 cells (GPR40 IP3 assay) and CHO cells (GPR40 aequorin assay), respectively.
  50. ghrelin receptor inverse agonist

    PF-5190457 is a potent and selective ghrelin receptor inverse agonist with a pKi of 8.36.

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