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GPCR / G Protein

产品 151 到 200 共 860个

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  1. Orexin 2 Receptor Agonist
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    Orexin 2 Receptor Agonist

    Catalog No. A15982
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    Orexin 2 receptor 激动剂
    Orexin 2 Receptor Agonist一种有效的选择性Orexin2受体激动剂。 了解更多
  2. MK-1064
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    MK-1064

    Catalog No. A16360
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    OX2 拮抗剂
    MK-1064是一种有效的，选择性的，口服活性的Orexin OX2受体拮抗剂，可用于治疗失眠。 了解更多
  3. Alverine Citrate
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    Alverine Citrate

    Catalog No. A16396
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    Alverine Citrate是用于功能性胃肠道疾病的药物。 了解更多
  4. MK-6096 (Filorexant)
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    MK-6096 (Filorexant)

    Catalog No. A13168
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    Orexin receptor 拮抗剂
    MK-6096 (Filorexant)是目前正处于失眠临床开发中的口服生物利用型有效且选择性可逆的OX（1）R和OX（2）R拮抗剂。MK-6096表现出对人OX（1）R和OX（2）R的有效结合和拮抗作用（结合时<3 nM，FLIPR中为11 nM），对超过170个受体和 酶。 了解更多
  5. TCS-OX2-29 HCl
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    • 最新产品

    TCS-OX2-29 HCl

    Catalog No. A17136
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    OX2 receptor 拮抗剂
    TCS-OX2-29 HCl是一种选择性OX2受体拮抗剂，IC50值为40 nM。 了解更多
  6. GSK1059865
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    GSK1059865

    Catalog No. A12401
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    orexin 1 receptor antagonist
    GSK1059865 is a potent orexin 1 receptor antagonist. 了解更多
  7. Nemorexant
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    Nemorexant

    Catalog No. A12685
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    Orexin receptor antagonist
    Nemorexant (ACT-541468) is a potent orexin receptor antagonist extracted from patent WO2015083094A1, compound example 7, has IC50s of 2 nM and 3 nM for Ox1 receptor and Ox2 receptor, respectively. 了解更多
  8. SB-334867 free base
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    SB-334867 free base

    Catalog No. A16695
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    orexin OX1 receptor antagonist
    SB-334867 free base is a selective non-peptide orexin OX1 receptor antagonist with a pKb value of 7.2. 了解更多
  9. SR 48692
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    SR 48692

    Catalog No. A11770
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    NT 拮抗剂
    SR 48692代表NT受体的一种新型有效的非肽拮抗剂放射性配体，可区分激动剂和拮抗剂受体之间的相互作用。 了解更多
  10. ML314
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    ML314

    Catalog No. A13570
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    NTR1 激动剂
    ML-314是神经降压素NTR1受体的脑渗透性非肽β-arrestin偏向性激动剂，在主要试验中对NTR1（EC50 = 2.0μM）表现出完全的激动剂行为，对NTR2具有选择性。 了解更多
  11. JMV 390-1
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    JMV 390-1

    Catalog No. A16026
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    JMV 390-1是主要的神经降压素和神经调节素N降解酶的抑制剂（内肽酶24.15，内肽酶24.11，亮氨酸氨基肽酶和内肽酶24.16的IC50值分别为31、40、52和58 nM）。 了解更多
  12. SBI-553
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    SBI-553

    Catalog No. A18435
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    NTR1 allosteric modulator
    SBI-553 is a potent and brain penetrant NTR1 allosteric modulator. 了解更多
  13. UR-144
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    UR-144

    Catalog No. A11096
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    UR-144是有效的合成大麻素（CB），其优先结合周围的CB2受体（Ki = 1.8 nM）超过中央CB1受体（Ki = 150 nM）。 了解更多
  14. WIN 55,212-2 mesylate
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    WIN 55,212-2 mesylate

    Catalog No. A11932
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    CB receptor 激动剂
    WIN 55,212-2 mesylate是一种有效的cannabinoid receptor激动剂，在神经性疼痛的大鼠模型中具有有效的镇痛作用。它通过受体介导的信号激活p42和p44 MAP激酶。 了解更多
  15. BML-190
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    BML-190

    Catalog No. A11938
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    CB2 receptor ligand
    BML-190是CB2受体的选择性反向激动剂。 了解更多
  16. MDA 19
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    MDA 19

    Catalog No. A11939
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    CB2 激动剂
    MDA 19是CB2的有效选择性激动剂，对精神活性CB1受体具有合理的选择性。 了解更多
  17. CP 945598 HCl (Otenabant HCl)
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    CP 945598 HCl (Otenabant HCl)

    Catalog No. A11942
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    CB1 拮抗剂
    CP 945598 HCl (Otenabant HCl)是一种有效且高度选择性的CB1拮抗剂。 了解更多
  18. GW842166X
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    GW842166X

    Catalog No. A11253
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    CB2 receptor 激动剂
    GW842166X是一种选择性的非大麻类CB2受体激动剂，EC50为63 nM，对CB1受体没有显著的活性。 了解更多
  19. Rimonabant (SR141716)
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    Rimonabant (SR141716)

    Catalog No. A11547
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    Rimonabant是CB1的选择性拮抗剂，在hCB1转染的HEK 293膜中的IC50为13.6 nM，EC50为17.3 nM。 了解更多
  20. Org 27569
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    Org 27569

    Catalog No. A11513
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    CB1 modulator?
    Org 27569是一种强效CB1受体变构调节剂(PEC50 = 8.24)。 了解更多
  21. AM251
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    AM251

    Catalog No. A12914
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    CB1 receptor 拮抗剂
    AM251是有效的CB1受体拮抗剂（IC50 = 8 nM，Ki = 7.49 nM），其选择性是CB2受体的306倍。 了解更多
  22. AM 2201
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    AM 2201

    Catalog No. A14174
    Cannabinoid 抑制剂
    AM2201是有效的合成大麻素（CB），对于CB1和CB2受体的Ki值分别为1.0和2.6 nM。 了解更多
  23. Tedalinab
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    Tedalinab

    Catalog No. A14189
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    CB2 receptor 激动剂
    Tedalinab (GRC-10693)是开发用于治疗骨关节炎和神经性疼痛的药物，它可作为有效的选择性大麻素CB2受体激动剂。与相关的CB1受体相比，它对CB2的选择性为4700x，具有很高的口服生物利用度，并在早期临床试验中显示出令人鼓舞的安全性结果以及有效的镇痛和抗炎作用。 了解更多
  24. Otenabant
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    Otenabant

    Catalog No. A15200
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    CB1 receptor 拮抗剂
    Otenabant是最近发现的选择性，高亲和力，竞争性CB1受体拮抗剂，Ki为0.7 nM。 了解更多
  25. AM630
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    AM630

    Catalog No. A14993
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    CB2 拮抗剂
    AM630是一种选择性CB2拮抗剂，Ki为31.2 nM，选择性是CB1受体的150倍以上。 了解更多
  26. Bay 59-3074
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    Bay 59-3074

    Catalog No. A16328
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    CB1/CB2 receptor 激动剂
    Bay 59-3074是一种新型的选择性CB1/CB2受体部分激动剂，对人CB1和CB2受体的Ki值分别为48.3和45.5 nM。 了解更多
  27. AM1241
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    AM1241

    Catalog No. A16397
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    CB2 receptor 激动剂
    AM1241是选择性的大麻素CB2受体激动剂，Ki为3.4 nM，相对于CB1受体具有82倍的选择性。 了解更多
  28. Rimonabant hydrochloride
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    Rimonabant hydrochloride

    Catalog No. A11548
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    CB1 receptor inverse 激动剂
    Rimonabant hydrochloride是CB1受体反向激动剂。 了解更多
  29. SR 144528
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    SR 144528

    Catalog No. A12376
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    CB2 inverse 激动剂
    SR 144528是一种选择性的外周大麻素受体反向激动剂，对大鼠脾脏和人重组CB2受体的Ki值为0.6 nM，对大鼠脑和人重组CB1受体的Ki值为400 nM。 了解更多
  30. VCE-004.8
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    VCE-004.8

    Catalog No. A18549
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    PPARγ and CB2 receptor dual agonist
    VCE-004.8, a semi-synthetic multitarget cannabinoquinoid, is a specific PPARγ and CB2 receptor dual agonist with potent anti-inflammatory activity. 了解更多
  31. GNE-049
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    GNE-049

    Catalog No. A20206
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    CBP inhibitor
    GNE-049 is a highly potent and selective CBP inhibitor with an IC50 of 1.1 nM in TR-FRET assay. GNE-049 also inhibits BRET and BRD4(1) with IC50s of 12 nM and 4200 nM, respectively. 了解更多
  32. CB1 antagonist 2
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    CB1 antagonist 2

    Catalog No. A18810
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    CB1 antagonist
    CB1 antagonist 2 is caimabinoid 1 (CB1) antagonist extracted from patent WO2016184310A1, compound 3, inhibits CB1 in vivo with an IC50 of 25.5 nM. 了解更多
  33. CB2R-IN-1
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    CB2R-IN-1

    Catalog No. A12306
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    cannabinoid CB2 receptor inverse agonist
    CB2R-IN-1 is a potent cannabinoid CB2 receptor inverse agonist with a Ki of 0.9 nM. 了解更多
  34. Taranabant
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    Taranabant

    Catalog No. A11578
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    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. 了解更多
  35. JD-5037
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    JD-5037

    Catalog No. A20837
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    CB1R antagonist
    JD-5037 is a novel, peripherally restricted CB1R antagonist with an IC50 of 1.5 nM. 了解更多
  36. (±)-Ibipinabant
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    (±)-Ibipinabant

    Catalog No. A21439
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    CB-1 receptor antagonist
    (±)-Ibipinabant ((±)-SLV319) is the racemate of SLV319. (±)-Ibipinabant ((±)-SLV319) is a potent and selective cannabinoid-1 (CB-1) receptor antagonist with an IC50 of 22 nM. 了解更多
  37. Taranabant racemate
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    Taranabant racemate

    Catalog No. A21699
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    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. 了解更多
  38. Taranabant ((1R,2R)stereoisomer)
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    Taranabant ((1R,2R)stereoisomer)

    Catalog No. A21705
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    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. 了解更多
  39. Istradefylline (KW-6002)
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    Istradefylline (KW-6002)

    Catalog No. A11451
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    A2A 拮抗剂
    Istradefylline (KW-6002)是A2A受体的选择性拮抗剂。 了解更多
  40. SYN-115 (Tozadenant)
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    SYN-115 (Tozadenant)

    Catalog No. A11560
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    A2a receptor 拮抗剂
    SYN115是口服，有效和选择性的腺苷2a（A2a）受体抑制剂，作用于人类和恒河猴的 adenosine A2A 受体，Ki 值分别为 11.5 nM 和 6 nM。 了解更多
  41. CGS 21680 HCl Hydrate
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    CGS 21680 HCl Hydrate

    Catalog No. A11619
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    Adenosine A2A Receptor 激动剂
    CGS 21680 HCl是一种特定的腺苷A2A亚型受体激动剂。 了解更多
  42. Adenosine
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    Adenosine

    Catalog No. A10040
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    Adenosine在生化过程中起着重要作用，例如能量转移（如三磷酸腺苷（ATP）和二磷酸腺苷(ADP)）以及信号传导中的环状单磷酸腺苷cAMP。 它也是一种抑制性神经递质。 了解更多
  43. Aminophylline
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    Aminophylline

    Catalog No. A10066
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    Adenosine receptor 拮抗剂
    Aminophylline是一种非选择性的腺苷受体拮抗剂和磷酸二酯酶抑制剂，能够逆转局部缺血引起的bradyasystole。 了解更多
  44. Dyphylline
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    Dyphylline

    Catalog No. A10339
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    Adenosine receptor 拮抗剂
    Dyphylline是黄嘌呤衍生物，具有支气管扩张药和血管扩张药的作用。 它充当腺苷受体拮抗剂和磷酸二酯酶抑制剂。 了解更多
  45. SCH 442416
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    SCH 442416

    Catalog No. A12695
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    A2A Receptor 拮抗剂
    SCH 442416是一种选择性的腺苷A2A受体拮抗剂。以高亲和力结合人和大鼠A2A受体（Ki值分别为0.048和0.5 nM）。在体外对hA2A的选择性比hA1高> 23000倍，并且对hA2B和hA3受体的亲和力最小（IC50> 10μM）。 了解更多
  46. Tamsulosin hydrochloride
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    Tamsulosin hydrochloride

    Catalog No. A12846
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    Tamsulosin hydrochloride是前列腺素α1A肾上腺素受体的拮抗剂。 了解更多
  47. CVT 6883
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    CVT 6883

    Catalog No. A13745
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    adenosine A2B receptors 拮抗剂
    CVT-6883是一种选择性的A2B腺苷拮抗剂，代表了一种治疗心肺疾病的新型潜在方法。 了解更多
  48. Capadenoson
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    Capadenoson

    Catalog No. A14159
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    Adenosine Receptor 激动剂
    Capadenoson是腺苷A1受体的选择性激动剂。 了解更多
  49. 5-Iodotubercidin
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    5-Iodotubercidin

    Catalog No. A13948
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    Adenosine kinase 抑制剂
    5-Iodotubercidin是一种有效的腺苷激酶抑制剂，IC50为26 nM。 了解更多
  50. CF-102
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    CF-102

    Catalog No. A14402
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    Adenosine A3 receptor 激动剂
    CF-102是具有潜在抗肿瘤活性生物利用的，合成的，高度选择性的腺苷A3受体（A3AR）激动剂。 了解更多

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  1. 5-HT Receptors (143)
  2. Adrenergic Receptors (110)
  3. Histamine Receptors (62)
  4. Opioid Receptors (28)
  5. Metabotropic glutamate receptors (mGluR) (50)
  6. Melatonin Receptors (4)
  7. Peptide Receptors (6)
  8. Smoothened Receptors (14)
  9. CXCR (30)
  10. G Protein (26)
  11. Platelet-Activating Factor (PAF) Receptors (10)
  12. Endothelin Receptors (21)
  13. LPA Receptor (13)
  14. Prostanoid Receptors (28)
  15. Adenosine Receptors (48)
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  28. Bombesin Receptors (1)
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  30. CCK (6)
  31. GLP-1 receptors (8)
  32. Calcium-Sensing Receptor (6)
  33. GPCR19 (5)
  34. CRFR (7)
作用机制
  1. Inhibitor (抑制剂) (86)
  2. Agonist (激动剂) (229)
  3. Antagonist (拮抗剂) (385)
  4. Activator (激活剂) (12)
  5. Modulator (调节剂) (28)
  6. Blocker (阻断剂) (12)
  7. Stabilizer (稳定剂) (1)
  8. Stimulator (刺激物) (4)
靶点
  1. A1 adenosine receptor (1)
  2. A3 adenosine receptor (1)
  3. Aurora A (1)
  4. Aurora B (1)
  5. Aurora C (1)
  6. COX-1 (1)
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  8. CXCL12 (1)
  9. CXCL8 (2)
  10. CXCR1 (4)
  11. CXCR2 (9)
  12. CXCR4 (11)
  13. Histamine H1 receptor (1)
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