GPCR/G Protein

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  1. mGluR5 antagonist

    AZD 9272 is a brain penetrant mGluR5 antagonist.
  2. CGRP receptor antagonist

    CGRP antagonist 1 is a highly potent CGRP receptor antagonist with a Ki and IC50 of 35 and 57 nM, respectively.
  3. neuropeptide Y1 receptor antagonist

    Y1 receptor antagonist 1 (H 409-22 isomer) is a neuropeptide Y1 receptor antagonist.
  4. EP1 antagonist

    EP1-antanoist-1 is a EP1 antagonist with a pKi of 7.54 and an pIC50 of 8.5.
  5. NPY5-R antagonist

    L 152804 is an orally active and selective neuropeptide Y Y5 receptor (NPY5-R) antagonist, with a Ki of 26 nM for hY5. L 152804 causes weight loss in diet-induced obese mice by modulating food intake and energy expenditure.
  6. oxytocin receptor antagonist

    L-368,899 hydrochloride is a potent, selective, orally bioavailable, non-peptide oxytocin receptor antagonist, with IC50s of 8.9 nM and 26 nM for rat uterus and human uterus oxytocin receptor, respectively, used as a tocolytic agent.
  7. neuropeptide Y5 receptor antagonist

    CGP71683 hydrochloride is a competitive neuropeptide Y5 receptor antagonist with a Ki of 1.3 nM, and shows no obvious activity at Y1 receptor (Ki, >4000 nM) and Y2 receptor (Ki, 200 nM) in cell membranes.
  8. beta adrenergic receptor antagonist

    Ecastolol is a beta adrenergic receptor antagonist, with antianginal activities.
  9. α1 adrenergic receptor antagonist

    QF0301B is an α1 adrenergic receptor antagonist and a low α2 adrenoceptor, 5-HT2A, and histamine H1 receptor blocker.
  10. NK2 antagonist

    GR 159897 is a highly potent, selective, competitive, brain-penetrated non-peptide antagonist at tachykinin NK2 receptors, inhibits binding of [3H]GR100679 to hNK2-CHO cells and rat colon membranes with pKis of 9.51 and 10, respectively. Antagonizes bronchoconstriction, with anxiolytic-like activity.
  11. CysLT1 receptor antagonist

    LM-1484 is an antagonist of CysLT1 receptor and displays a higher affinity for 3H-LTC4 sites.
  12. peripheral adrenoceptor antagonist

    Deriglidole is a peripheral adrenoceptor antagonist with a high affinity for α2-adrenoceptors.
  13. PAF antagonist

    Apafant (WEB 2086), a potent platelet-activating factor (PAF) antagonist, inhibits PAF binding to human PAF receptors with a Ki of 9.9 nM.
  14. MCHR1 antagonist

    SNAP 94847 is a novel, high affinity selective melanin-concentrating hormonereceptor1 (MCHR1) antagonist with (Ki= 2.2 nM, Kd=530 pM), it displays >80-fold and >500-fold selectivity over MCHα1A and MCHD2 receptors respectively.
  15. peptidoleukotrienes antagonist

    RG-12525 is a a specific, competitive and orally effective antagonist of the peptidoleukotrienes, LTC4, LTD4 and LTE4, inhibiting LTC4-, LTD4- and LTE4-inducd guinea pig parenchymal strips contractions, with IC50s of 2.6 nM, 2.5 nM and 7 nM, respectively; RG-12525 is also a peroxisome proliferator-activated receptor gamma (PPAR-gamma) agonist with IC50 of appr 60 nM and a potent inhibitor of CYP3A4, with a Ki value of 0.5 ?M.
  16. PAF antagonist

    Setipafant is a platelet-activating factor (PAF) antagonist.
  17. Oxytocin antagonist

    OT antagonist 1 (Compound 4) is a potent, selective Oxytocin antagonist with a Ki of 50 nM.
  18. oxytocin (OT) antagonist

    OT antagonist 3 is an oxytocin (OT) antagonist extracted from patent WO2007017752A1.
  19. GPR35/CXCR8 antagonist

    ML 145 is a selective GPR35/CXCR8 antagonist with an IC50/EC50 of 20.1 nM, but not for the related GPR55 orphan receptor. GPR35 is expressed by various cells of the immune system and it may has potential as a therapeutic target in inflammatory disease.
  20. AT1 receptor antagonist

    ZD 7155 hydrochloride is an angiotensin II receptor type 1 (AT1 receptor) antagonist.
  21. CRTh2 receptor antagonist

    MK-8318 is a potent and selective CRTh2 receptor antagonist with a Ki of 5.0 nM.
  22. β adrenergic receptor antagonist

    Pargolol hydrochloride is a β adrenergic receptor antagonist.
  23. 5-HT1B receptor antagonist

    AR-A 2 is a selective 5-HT1B receptor antagonist.
  24. BRS-3 antagonist

    ML-18 is a non-peptide bombesin receptor subtype-3 (BRS-3) antagonist with an IC50 of 4.8 μM.
  25. histamine H3 receptor antagonist

    Cipralisant is a potent and selective histamine H3 receptor antagonist in vivo, and an agonist in vitro, with a pKi of 9.9 for histamine H3 receptor and a Ki of 0.47 nM for rat histamine H3 receptor; Cipralisant has entered in clinical trials for the treatment of attention-deficit hyperactivity disorder.
  26. NK2 receptor antagonist

    Saredutant is a selective NK2 receptor antagonist.
  27. S1P antagonist

    VPC 23019, an aryl amide-containing Sphingosine 1-phosphate (S1P) analog, is a competitive antagonist at the S1P1 and S1P3 receptors (pKi= 7.86 and 5.93, respectively) and an agonist at the S1P4 and S1P5 receptors (pEC50= 6.58 and 7.07, respectively).
  28. A2B adenosine receptor antagonist

    BAY-545 is a potent and selective A2B adenosine receptor antagonist, with an IC50 of 59 nM.
  29. Dopamine D4 receptor antagonist

    NRA-0160 is a selective dopamine D4 receptor antagonist, with a Ki value of 0.48 nM and with negligible affinity for dopamine D2 receptor (Ki: >10000 nM), D3 receptor (Ki: 39 nM), rat 5-HT2A receptor (Ki: 180 nM) and rat α1 adrenoceptor (Ki: 237 nM).
  30. PAF antagonist

    YM-264 is a selective, potent and orally active platelet-activating factor (PAF) antagonist with a pKi value of 8.85 for rabbit platelet membranes.
  31. 5-HT3 /5-HT4 receptor dual antagonist

    FK1052 hydrochloride is a potent 5-HT3 and 5-HT4 receptor dual antagonist.
  32. H1 receptor antagonist

    Wy 49051 is a potent, orally active H1 receptor antagonist, with IC50 of 44 nM.
  33. serotonin 5-HT2 antagonist

    Irindalone is a novel serotonin 5-HT2 antagonist.
  34. adenosine receptor antagonist

    Taminadenant is an antagonist of adenosine receptor.
  35. NK-1 receptor antagonist

    NK-1 Antagonist 1 (Rolapitant intermediate) is an antagonist of NK-1 receptor, used in the research of NK-1 related diseases and conditions such as cough, overactive bladder, alcohol dependency and depression.
  36. PAR2 antagonist

    AZ3451 is a potent protease-activated receptor-2 (PAR2) antagonist with IC50 of 23 nM.
  37. MCH1 receptor antagonist

    ALB-127158(a) is a potent and selective melanin concentrating hormone 1 (MCH1) receptor antagonist.
  38. SSTR5 antagonist

    SSTR5 antagonist 1 is a potent, selective, and orally available somatostatin receptor subtype 5 (SSTR5) antagonist with IC50s of 9.6 and 57 nM for hSSTR5 and mSSTR5, respectively. (Compound 25a).
  39. 5-HT6 receptor antagonist

    Masupirdine free base (SUVN-502 free base) is a potent, selective, orally bioavailable, and brain penetrant 5-HT6 receptor antagonist (Ki of 2.04 nM for human 5-HT6 receptor).
  40. β adrenergic receptor antagonist

    Spirendolol is a β adrenergic receptor antagonist.
  41. 5-HT2A/α1-adrenergic receptor antagonist

    Lidanserin is a drug which acts as a combined 5-HT2A and α1-adrenergic receptor antagonist.
  42. 5-HT2A/dopamine D2 antagonist

    Abaperidone is a potent antagonist of 5-HT2A?receptor and dopamine D2 receptor with IC50s of 6.2 and 17 nM.
  43. angiotensin AT1 receptor antagonist

    L162389 is a potent antagonist of angiotensin AT1 receptor with Ki of 28 nM.
  44. histamine H1 receptor antagonist

    Pirolate is a histamine H1 receptor antagonist.

  45. mGluR5 antagonist

    Fenobam is a selective, orally active, and non-competitive mGluR5 antagonist acting at an allosteric modulatory site (Kd values are 54 and 31 nM for rat and human recombinant mGlu5 receptors, respectively).
  46. AA3R antagonist

    Adenosine antagonist-1 is an adenosine A3 receptor (AA3R) antagonist.
  47. LPA1 antagonist

    BMS-986020 is a high-affinity lysophosphatidic acid receptor 1 (LPA1) antagonist.
  48. FPR1 antagonist

    HCH6-1 is a competitive antagonist of Formyl peptide receptor 1 (FPR1), an emerging therapeutic target for the discovery of drugs to treat neutrophilic inflammatory diseases.
  49. CXCR4 antagonist

    IT1t is a potent CXCR4 antagonist; inhibits CXCL12/CXCR4 interaction with an IC50 of 2.1 nM.
  50. dopamine autoreceptor antagonist

    CGP 25454A is a novel and selective presynaptic dopamine autoreceptor antagonist.

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