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GPCR / G Protein

产品 151 到 200 共 385个

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  1. Atrasentan
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    Atrasentan

    Catalog No. A13779
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    ETA 拮抗剂
    Atrasentan是一种实验药物，正在研究中，用于治疗各种类型的癌症，包括非小细胞肺癌。它是对A型亚型（ETA）有选择性的内皮素受体拮抗剂,对ETA的IC50为0.0551 nM。 了解更多
  2. Atrasentan HCl
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    Atrasentan HCl

    Catalog No. A15007
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    Endothelin 拮抗剂 receptor
    Atrasentan hydrochloride是一种开发用于治疗前列腺癌的内皮素拮抗剂受体（IC50 = 0.0551 nM，ETA）。 了解更多
  3. BQ-123
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    BQ-123

    Catalog No. A15912
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    ETA receptor 拮抗剂
    BQ-123是一种选择性内皮素A受体（ETA）拮抗剂，IC50为7.3 nM。 了解更多
  4. Bosentan Hydrate
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    Bosentan Hydrate

    Catalog No. A14944
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    ET-A and ET-B 拮抗剂
    Bosentan Hydrate是ET-A和ET-B的内皮素（ET）受体拮抗剂，Ki分别为4.7 nM和95 nM。 了解更多
  5. IRL-2500
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    IRL-2500

    Catalog No. A13638
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    ETBR 拮抗剂
    IRL-2500是一种有效的选择性ETBR拮抗剂。它显示了对ETB受体的一些选择性（对于ETB和ETA受体，IC50值分别为1.3和94 nM）。 了解更多
  6. Macitentan
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    Macitentan

    Catalog No. A11492
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    Endothelin receptor 拮抗剂
    Macitentan是一种口服活性非肽双重ETA/ETB(内皮素) receptor双重拮抗剂，IC50为0.5 nM/391 nM。用于治疗特发性肺纤维化(IPF)和肺动脉高压(PAH)。 了解更多
  7. PD-159020
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    PD-159020

    Catalog No. A13499
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    ETA/ETB antagonist
    PD-159020 is a non-selective ETA/ETB antagonist, with IC50s of 30 and 50 nM for hETA and hETB, respectively. 了解更多
  8. Sparsentan
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    Sparsentan

    Catalog No. A20879
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    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. 了解更多
  9. Tezosentan
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    Tezosentan

    Catalog No. A21118
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    endothelin (ET) receptor antagonist
    Tezosentan (RO 610612) is an endothelin (ET) receptor antagonist, with pA2s of 9.5, 7.7 for ETA and ETB receptors, respectively. 了解更多
  10. Darusentan
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    Darusentan

    Catalog No. A21280
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    endothelin A (ETA) receptor antagonist
    Darusentan is a selective endothelin A (ETA) receptor antagonist. 了解更多
  11. Macitentan (n-butyl analogue)
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    Macitentan (n-butyl analogue)

    Catalog No. A21845
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    endothelin ETA and ETB receptor antagonist
    Macitentan n-butyl analogue is a n-butyl analogue of Macitentan. 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). 了解更多
  12. Aprocitentan
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    Aprocitentan

    Catalog No. A21999
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    dual ETA/ETB antagonist
    Aprocitentan (ACT-132577) is the major and pharmacologically active metabolite of Macitentan. Aprocitentan is dual ETA/ETB antagonist with IC50s of 3.4 nM and 987 nM, and pA2 valus of 6.7 and 5.5, respectively. 了解更多
  13. Ginkgolide B
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    Ginkgolide B

    Catalog No. A10429
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    PAFR 拮抗剂
    Ginkgolide B (BN 52021)是一种PAFR拮抗剂，IC50为3.6 μM。 了解更多
  14. Etizolam
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    Etizolam

    Catalog No. A14257
    PAFR 拮抗剂
    Etizolam是一种具有抗焦虑活性的特异性血小板活化因子（PAF）拮抗剂。 了解更多
  15. YM-264
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    YM-264

    Catalog No. A20139
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    PAF 拮抗剂
    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. 了解更多
  16. 48740 RP
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    48740 RP

    Catalog No. A12339
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    PAF 拮抗剂
    48740 RP (RP-55778) is a platelet-activating factor (PAF) antagonist. 了解更多
  17. Aglafoline
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    Aglafoline

    Catalog No. A12257
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    PAF antagonist
    Aglafoline is an effective PAF antagonist not only in vitro, but also in vivo. 了解更多
  18. Foropafant
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    Foropafant

    Catalog No. A13388
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    PAF receptor antagonist
    Foropafant (SR27417) highly potent, competitive, selective and orally active antagonist of platelet-activating factor (PAF) receptor. 了解更多
  19. CP-96486
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    CP-96486

    Catalog No. A12471
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    LTD4/PAF receptor antagonist
    CP-96486 is a potent and orally active leukotriene D4 (LTD4)/platelet activating factor (PAF) receptor antagonist with Kis of 20 and 24 nM, respectively. 了解更多
  20. CID16020046
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    CID16020046

    Catalog No. A16818
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    GPR55 拮抗剂
    CID16020046是一种选择性的GPR55拮抗剂，在酵母中抑制GPR55的组成活性，IC50为150 nM。它对其他广谱GPCRs、离子通道、激酶和核受体表现出弱活性。 了解更多
  21. GW-1100
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    GW-1100

    Catalog No. A11445
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    GPR40 antagonist
    GW-1100 is a selective GPR40 antagonist with a pIC50 of 6.9. 了解更多
  22. GPR4 antagonist 1
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    GPR4 antagonist 1

    Catalog No. A12340
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    GPR4 antagonist
    GPR4 antagonist 1 is a GPR4 antagonist, with an IC50 of 189 nM. 了解更多
  23. G15
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    G15

    Catalog No. A13675
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    GPER/GPR30 antagonist
    G15 is a high affinity and selective G-protein-coupled estrogen receptor (GPER/GPR30) antagonist with a Ki of 20 nM. 了解更多
  24. GLPG0974
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    GLPG0974

    Catalog No. A21466
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    FFA2/GPR43 antagonist
    GLPG0974 is a free fatty acid receptor-2 (FFA2/GPR43) antagonist with an IC50 of 9 nM. 了解更多
  25. Plerixafor 8HCl (DB06809)
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    Plerixafor 8HCl (DB06809)

    Catalog No. A10913
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    CXCR4 拮抗剂
    Plerixafor 8HCl (DB06809)是CXCR4趋化因子受体拮抗剂，作用于CXCR4和CXCL12介导调节的趋化性， IC50分别为44 nM和5.7 nM。 了解更多
  26. AMD 070
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    AMD 070

    Catalog No. A11315
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    CXCR4 拮抗剂
    AMD 070是CXCR4趋化因子受体拮抗剂。 了解更多
  27. AMD 3465 Hexahydrobromide
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    AMD 3465 Hexahydrobromide

    Catalog No. A11953
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    CXCR4 拮抗剂
    AMD 3465 Hexahydrobromide是一种有效的选择性CXCR4拮抗剂。 了解更多
  28. WZ811
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    WZ811

    Catalog No. A12588
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    CXCR4 拮抗剂
    WZ811是4型C-X-C趋化因子受体（CXCR4）拮抗剂（EC50 = 0.3 nM）。在体外抑制CXCR4/基质细胞衍生因子1（SDF-1）介导的cAMP调节（EC50 = 1.2 nM）。 了解更多
  29. AMD3100 (Plerixafor)
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    AMD3100 (Plerixafor)

    Catalog No. A13074
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    CXCR4 拮抗剂
    AMD3100 (Plerixafor)是用于增殖造血干细胞的免疫刺激剂，并且是用于动员造血干细胞进行移植的趋化因子受体-4拮抗剂。 了解更多
  30. SCH-527123 (Navarixin)
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    SCH-527123 (Navarixin)

    Catalog No. A11555
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    CXCR1/CXCR2 拮抗剂
    SCH-527123 (Navarixin)是人CXCR1和CXCR2受体的强效选择性拮抗剂，IC50分别为42 nM和3 nM。 了解更多
  31. SB265610
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    SB265610

    Catalog No. A14195
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    CXCR2 拮抗剂
    SB265610是CXCR2 (Kd = 2.51 nM)的非肽变构反向激动剂，通过与不同于激动剂结合位点的区域结合来防止受体活化。它不与相关CXCR1受体结合。在体外和高氧诱导肺损伤的大鼠模型中，它已被证明能防止中性粒细胞趋化性。 了解更多
  32. SB225002
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    SB225002

    Catalog No. A14209
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    CXCR2 拮抗剂
    SB225002是一种有效的选择性CXCR2拮抗剂，IC50为22 nM，可抑制白介素IL-8与CXCR2的结合，选择性是其他测试的7-TMR的150倍以上。 了解更多
  33. AMD-070 HCl
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    AMD-070 HCl

    Catalog No. A14997
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    CXCR4 拮抗剂
    在CXCR4 125I-SDF抑制结合试验中，AMD-070 HCl是一种有效的选择性CXCR4拮抗剂，IC50值为13 nM，抑制T-4型HIV-1（NL4.3株）在MT-4细胞中的复制和PBMC。 了解更多
  34. UNBS5162
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    UNBS5162

    Catalog No. A15439
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    CXCL chemokines 拮抗剂
    UNBS5162是一种新型萘二甲酰亚胺，可降低实验性前列腺癌中CXCL趋化因子的表达。9种癌细胞系的平均抗增殖活性IC50值为17.9 uM；UNBS3157的水解产物。 了解更多
  35. MSX-130
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    MSX-130

    Catalog No. A17150
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    CXCR4 拮抗剂
    MSX-130是CXCR4拮抗剂。 了解更多
  36. USL311
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    USL311

    Catalog No. A18778
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    CXCR4 拮抗剂
    USL311 is a CXCR4 receptor antagonist which prevents the binding of stromal-cell derived factor-1 (SDF-1 or CXCL12) to CXCR4. 了解更多
  37. CXCR2-IN-1
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    CXCR2-IN-1

    Catalog No. A12649
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    CXCR2 激动剂
    CXCR2-IN-1 is a central nervous system penetrant CXCR2 antagonists with a pIC50 of 9.3. 了解更多
  38. SCH 563705
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    SCH 563705

    Catalog No. A15234
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    CXCR2/CXCR1 拮抗剂
    SCH 563705是有效的双重CXCR2（IC50 = 1.3 nM)/CXCR1（IC50 = 7.3 nM）拮抗剂。 了解更多
  39. AZD-5069
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    AZD-5069

    Catalog No. A15941
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    CXCR2 拮抗剂
    AZD-5069是一种有效的选择性CXCR2拮抗剂，具有抑制COPD患者中性粒细胞向气管迁移的潜能。 了解更多
  40. AMG 487
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    AMG 487

    Catalog No. A21162
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    CXCR3 antagonist
    AMG 487 is an orally active and selective antagonist of CXC chemokine receptor 3 (CXCR3) which inhibits the binding of CXCL10 and CXCL11 to CXCR3 with IC50s of 8.0 and 8.2 nM, respectively. 了解更多
  41. SCH 546738
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    SCH 546738

    Catalog No. A21554
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    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. 了解更多
  42. AMG 487 S-enantiomer
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    AMG 487 S-enantiomer

    Catalog No. A21874
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    CXCR3 antagonist
    AMG 487 S-enantiomer is the S enantiomer of AMG 487. AMG 487 is an antagonist of the chemokine receptor CXCR3. 了解更多
  43. NBI-74330
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    NBI-74330

    Catalog No. A21158
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    CXCR3 antagonist
    NBI-74330 is a potent antagonist for CXCR3, and exhibits potent inhibition of (125I)CXCL10 and (125I)CXCL11 specific binding with Ki of 1.5 and 3.2 nM, respectively. 了解更多
  44. LDE225 (NVP-LDE225, Sonidegib)
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    LDE225 (NVP-LDE225, Sonidegib)

    Catalog No. A10520
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    Smo 拮抗剂
    LDE225 (NVP-LDE225)是一种强效、选择性和口服生物可利用的平滑(SMO)拮抗剂，通过平滑受体(SMO)的拮抗作用抑制hedgehog (Hh)信号通路。 了解更多
  45. LY2940680 (Taladegib)
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    LY2940680 (Taladegib)

    Catalog No. A11048
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    SMO 拮抗剂
    LY2940680 (Taladegib)已显示可影响由Hedgehog（Hh）蛋白引发的癌细胞信号通路。 了解更多
  46. ALLO-2
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    ALLO-2

    Catalog No. A18698
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    Smo mutant antagonist
    ALLO-2 is a potent drug-resistant Smoothened (Smo) mutant antagonist that inhibits Smo agonist Hh-Ag1.5-induced luciferase expression in TM3-Gli-Luc cells with IC50 of 6 nM. 了解更多
  47. MRT-83
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    MRT-83

    Catalog No. A21020
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    Smo antagonist
    MRT-83 is a potent antagonist of Smo, with an IC50 in the nanomolar range. MRT-83 also blocks Hedgehog (Hh) signaling. 了解更多
  48. MPEP
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    MPEP

    Catalog No. A12589
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    mGlu5 receptor 拮抗剂
    MPEP是mGlu5受体亚型（IC50 = 36 nM）的有效且高度选择性的非竞争性拮抗剂，并且是mGlu4受体的正构构调节剂。 了解更多
  49. PHCCC
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    PHCCC

    Catalog No. A12705
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    mGluR 拮抗剂
    PHCCC是I组代谢型谷氨酸受体拮抗剂（IC50?3μM）。 了解更多
  50. SIB 1893
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    SIB 1893

    Catalog No. A13759
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    mGluR 拮抗剂
    SIB 1893是代谢型谷氨酸mGlu5受体亚型的高度选择性非竞争性拮抗剂。 了解更多

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