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GPCR / G Protein

产品 101 到 150 共 860个

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  1. Ponesimod
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    Ponesimod

    Catalog No. A13307
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    S1P1 receptor modulator
    Ponesimod是一种口服活性，选择性鞘氨醇-1-磷酸受体1（S1P1）免疫调节剂，EC50为5.7 nM。 了解更多
  2. SKI-II
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    SKI-II

    Catalog No. A15988
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    SphK 抑制剂
    SKI-II是鞘氨醇激酶的选择性非脂质抑制剂（IC50 = 0.5 uM）。 了解更多
  3. KRP-203
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    KRP-203

    Catalog No. A13308
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    S1PR1 抑制剂
    KRP-203是选择性鞘氨醇-1-磷酸受体激动剂。它表明减少大鼠移植模型中外周淋巴细胞的浸润并延长生存期。 了解更多
  4. Fingolimod
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    Fingolimod

    Catalog No. A17798
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    S1P antagonist
    Fingolimod is a sphingosine 1-phosphate (S1P) antagonist with IC50 of 0.033 nM in K562 and NK cells. Fingolimod also is a pak1 activator, a immunosuppressant. 了解更多
  5. ASP1126
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    ASP1126

    Catalog No. A18432
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    S1P agonist
    ASP1126 is a selective and orally active sphingosine-1-phosphate (S1P) agonist, with EC50 values of 7.12 nM, 517 nM for hS1P1 and hS1P3, respectively. 了解更多
  6. K145
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    K145

    Catalog No. A16288
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    SphK2 抑制剂
    K145是一种选择性SphK2抑制剂，IC50为4.30±0.06μM，而在浓度不超过10 uM时，对SphK1无抑制作用。 了解更多
  7. K145 hydrochloride
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    K145 hydrochloride

    Catalog No. A16289
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    SphK2 抑制剂
    K145 hydrochloride是选择性鞘氨醇激酶2（SphK2）抑制剂和抗癌剂。 了解更多
  8. MP-A08
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    MP-A08

    Catalog No. A16290
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    ATP competitive SK 抑制剂
    MP-A08是一种高度选择性的ATP竞争性SK抑制剂，其靶向SK1和SK2的Kivalue分别为6.9±0.8 uM和27±3 uM。 了解更多
  9. VPC 23019
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    VPC 23019

    Catalog No. A20102
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    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). 了解更多
  10. TY-52156
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    TY-52156

    Catalog No. A12265
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    S1P3 receptor antagonist
    TY-52156 is a potent and selective S1P3 receptor antagonist with a Ki value of 110 nM. 了解更多
  11. Cenerimod
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    Cenerimod

    Catalog No. A20913
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    S1P1 agonist
    Cenerimod (ACT-334441) is a potent and orally available sphingosine 1-phosphate 1 receptor (S1P1) agonist extracted from patent WO 2016184939 A1 and WO 2011007324 A1, example 1, with an EC50 of 2.7 nM. 了解更多
  12. FTY720 (S)-Phosphate
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    FTY720 (S)-Phosphate

    Catalog No. A21324
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    S1PR1 agonist
    FTY720 (S)-Phosphate is an agonist of S1P receptor 1 (S1PR1), used in the research of acute inflammatory diseases such as acute lung injury. 了解更多
  13. PF429242 dihydrochloride
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    PF429242 dihydrochloride

    Catalog No. A21386
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    S1P inhibitor
    PF429242 dihydrochloride is a reversible and competitive S1P inhibitor with an IC50 of 175 nM. 了解更多
  14. Vorapaxar (SCH 530348)
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    Vorapaxar (SCH 530348)

    Catalog No. A12832
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    PAR-1 拮抗剂
    Vorapaxar (SCH 530348)是一种有效的口服活性凝血酶受体（PAR-1）拮抗剂，Ki为8.1 nM。 了解更多
  15. ML 161
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    ML 161

    Catalog No. A13495
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    PAR1 抑制剂
    ML-161是蛋白酶激活受体1（PAR1）介导的血小板活化的抑制剂（IC50 = 0.26μM，用于抑制人血小板上血小板P-选择素的表达）。 了解更多
  16. Aprepitant (MK-0869)
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    Aprepitant (MK-0869)

    Catalog No. A10083
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    neurokinin-1 receptor 拮抗剂
    Aprepitant (MK-0869)被归类为NK1拮抗剂。已经显示，阿瑞匹坦通过阻止P物质降落在大脑神经元受体上，从而抑制细胞毒性化疗药物引起的急性呕吐和延迟呕吐。还显示出它能增加5-HT3受体拮抗剂恩丹西酮和皮质类固醇地塞米松的活性，它们也可用于预防化学疗法引起的恶心和呕吐。 了解更多
  17. MK-0517 (Fosaprepitant)
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    MK-0517 (Fosaprepitant)

    Catalog No. A11756
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    neurokinin-1 receptor 拮抗剂
    MK-0517 (Fosaprepitant,L-758,298)是Aprepitant的水溶性磷酰基前药，它是NK1拮抗剂。 了解更多
  18. Vofopitant (GR 205171)
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    Vofopitant (GR 205171)

    Catalog No. A12793
    NK1 receptor 拮抗剂
    Vofopitant (GR 205171)是选择性神经激肽1受体拮抗剂。 了解更多
  19. GW679769 (Casopitant)
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    GW679769 (Casopitant)

    Catalog No. A13103
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    NK1 receptor 拮抗剂
    GW679769 (Casopitant)是具有抗抑郁和止吐作用的中枢作用神经激肽1（NK1）受体拮抗剂的甲磺酸盐。 了解更多
  20. Ibodutant (MEN 15596)
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    Ibodutant (MEN 15596)

    Catalog No. A13104
    tachykinin NK2 receptor 拮抗剂
    Ibodutant (MEN 15596)是速激肽NK2受体拮抗剂，pKi 值为10.1，用于治疗腹泻型肠易激综合症（IBS-D）。 了解更多
  21. Fosaprepitant dimeglumine
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    Fosaprepitant dimeglumine

    Catalog No. A11069
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    neurokinin-1 receptor 拮抗剂
    Fosaprepitant是一种选择性的神经激肽-1（NK-1）受体拮抗剂。 了解更多
  22. Rolapitant
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    Rolapitant

    Catalog No. A13680
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    NK1 receptor 拮抗剂
    Rolapitant，也称为SCH-619734，是一种选择性的，可生物利用的CNS渗透性神经激肽NK1受体拮抗剂，在呕吐动物模型中显示出行为效应。 了解更多
  23. GR-203040
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    GR-203040

    Catalog No. A13861
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    NK1 receptor 拮抗剂
    GR203040是一种新型，有效且选择性的非肽速激肽NK1受体拮抗剂。 了解更多
  24. Netupitant
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    Netupitant

    Catalog No. A14428
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    NK1 receptor 拮抗剂
    Netupitant是一种选择性的神经激肽1（NK1）受体拮抗剂。它竞争性地结合并阻断中枢神经系统（CNS）中人类物质P/NK1受体的活性，从而抑制内源性速激肽神经肽物质P（SP）的NK1受体结合，这可能导致预防化疗引起的恶心和呕吐（CINV）。 了解更多
  25. NKP608
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    NKP608

    Catalog No. A15187
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    NK1 receptor 拮抗剂
    NKP608是4-氨基哌啶的非肽衍生物，在体外（IC50 = 2.6 nM）和体内均作为神经激肽-1（NK-1）受体的选择性，特异性和有效拮抗剂。 了解更多
  26. SB-222200
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    SB-222200

    Catalog No. A15230
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    NK3 receptor 拮抗剂
    SB 222200是人类NK-3受体（Ki = 4.4 nM）的选择性，可逆和竞争性拮抗剂，可有效穿越血脑屏障。 了解更多
  27. Talnetant
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    Talnetant

    Catalog No. A15254
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    NK3 receptor 拮抗剂
    Talnetant是一种有效且选择性的NK3受体拮抗剂（ki = 1.4 nM，hNK-3-CHO）；对hNK-3受体的选择性是对hNK-2受体的100倍，在浓度高达100 uM时，对hNK-1没有亲和力。 了解更多
  28. Talnetant hydrochloride
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    Talnetant hydrochloride

    Catalog No. A15255
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    NK3 receptor 拮抗剂
    Talnetant Hydrochloride是一种有效且选择性的NK3受体拮抗剂（ki = 1.4 nM，hNK-3-CHO）；对hNK-3受体的选择性是对hNK-2受体的100倍，在浓度高达100 uM时对hNK-1没有亲和力。 了解更多
  29. Senktide
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    Senktide

    Catalog No. A16945
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    NK3 receptor 激动剂
    Senktide是神经介素K3（NK3）受体的有效选择性激动剂（EC50 = 0.5-3 nM）。 了解更多
  30. Tradipitant
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    Tradipitant

    Catalog No. A16918
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    NK1 receptor 拮抗剂
    Tradipitant，也称为VLY-686和LY686017，是第二代神经激肽1受体拮抗剂，在临床前焦虑模型中表现出活性。 了解更多
  31. Befetupitant
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    Befetupitant

    Catalog No. A13149
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    NK1R antagonist
    Befetupitant is a high-affinity, nonpeptide, competitive tachykinin 1 receptor (NK1R) antagonist. 了解更多
  32. Pavinetant
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    Pavinetant

    Catalog No. A21174
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    NK3R antagonist
    Pavinetant (MLE-4901) is a neurokinin-3 receptor (NK3R) antagonist. 了解更多
  33. Maropitant
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    Maropitant

    Catalog No. A21473
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    NK1 receptor antagonist
    Maropitant is a neurokinin (NK1) receptor antagonist. 了解更多
  34. Vofopitant dihydrochloride
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    Vofopitant dihydrochloride

    Catalog No. A21543
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    NK1 receptor antagonist
    Vofopitant dihydrochloride (GR 205171A) is a potent, selective and orally available tachykinin neurokinin 1(NK1) receptor antagonist. 了解更多
  35. Serlopitant
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    Serlopitant

    Catalog No. A21582
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    Neurokinin-1 (NK-1) receptor antagonist
    Serlopitant is a selective Neurokinin-1 (NK-1) receptor antagonist. 了解更多
  36. Octreotide Acetate
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    Octreotide Acetate

    Catalog No. A12782
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    somatostatin receptor 拮抗剂
    Octreotide是sst2，sst3和sst5生长抑素受体的肽激动剂。克隆的人类生长抑素受体的IC50/Kd值（nM）为：290-1140（sst1），0.4-2.1（sst2），4.4-34.5（sst3），> 1000（sst4）和5.6-32（sst5）。 了解更多
  37. CYN-154806
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    CYN-154806

    Catalog No. A13714
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    somatostatin receptor 2 拮抗剂
    CYN-154806是一种有效的选择性生长抑素受体2（sst2）拮抗剂。 了解更多
  38. Somatostatin
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    Somatostatin

    Catalog No. A13453
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    Somatostatin是一种抑制生长激素、胰岛素和胰高血糖素释放的内源性肽。 了解更多
  39. MK-4305 (Suvorexant)
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    MK-4305 (Suvorexant)

    Catalog No. A11500
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    OX receptor 拮抗剂
    Suvorexant (MK-4305)是OX1R和OX2R的有效，选择性和口服可生物利用的拮抗剂，目前正在临床研究中作为失眠的新疗法。 了解更多
  40. SB-408124
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    SB-408124

    Catalog No. A11567
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    OX Receptor 拮抗剂
    SB-408124是一种选择性的非肽orexin OX1受体拮抗剂(人OX1和OX2受体的Kb值分别为21.7和1405 nM)。体内口服后阻断orexin-A诱导的修饰。 了解更多
  41. SB-649868
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    SB-649868

    Catalog No. A12651
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    Orexin 拮抗剂
    SB-649868是葛兰素史克（GlaxoSmithKline）开发的一种食欲素OX1和OX 2受体拮抗剂 (作用于 OX1 和 OX2 受体，pKi 分别为 9.4 和 9.5)。。 了解更多
  42. SB 334867
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    SB 334867

    Catalog No. A12786
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    OX1 receptor 拮抗剂
    SB 334867是一种选择性的非肽orexin OX1受体拮抗剂。对于分别表达人OX1和OX2受体的CHO细胞中的细胞内Ca2 +释放抑制，pKb值为7.2和<5。体内全身给药后，阻断orexin-A诱导的美容和进食。 了解更多
  43. TCS 1102
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    TCS 1102

    Catalog No. A13439
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    Dual orexin receptor 拮抗剂
    TCS 1102是一种有效的双重食欲素受体拮抗剂（OX2和OX1受体的Ki值分别为0.2和3 nM）。 了解更多
  44. Almorexant
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    Almorexant

    Catalog No. A12503
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    OX 拮抗剂
    Almorexant (ACT078573)是一种有效的竞争性双重食欲素1受体(OX1)/orexin 2受体（OX2）拮抗剂，对于OX1和OX2的Ki值分别为1.3和0.17 nM。 了解更多
  45. MK-3697
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    MK-3697

    Catalog No. A12633
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    OX2 拮抗剂
    MK-3697是一种高效的，口服生物利用的选择性orexin 2受体拮抗剂，Ki值为0.95nM。 了解更多
  46. JNJ-10397049
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    JNJ-10397049

    Catalog No. A14104
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    OX2 receptor 拮抗剂
    JNJ-10397049是orexin-2受体（OX2R）的有效，选择性且可生物利用的拮抗剂（OX2R的KB = 4.5 nM，OX1R的1.1μM）。 了解更多
  47. Almorexant HCl
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    Almorexant HCl

    Catalog No. A14286
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    OX1/OX2 拮抗剂
    Almorexant HCl是一种活性双重食欲素受体拮抗剂，对OX1和OX2受体3的IC50为6.6 nM和3.4 nM。 了解更多
  48. ACT-335827
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    ACT-335827

    Catalog No. A13778
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    OX1 拮抗剂
    ACT-335827是选择性orexin受体1拮抗剂。 了解更多
  49. SB-408124 HCl
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    SB-408124 HCl

    Catalog No. A15231
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    OX Receptor 拮抗剂
    SB408124 Hydrochloride是OX1受体的非肽拮抗剂，全细胞和膜的Ki分别为57 nM和27 nM。表现出比OX2受体高50倍的选择性。 了解更多
  50. SB-674042
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    SB-674042

    Catalog No. A15233
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    OX1 receptor 拮抗剂
    SB-674042是有效的选择性非肽orexin OX1受体拮抗剂（Kd = 3.76 nM），对OX1的选择性比OX2受体高100倍。 了解更多

产品 101 到 150 共 860个

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  1. 5-HT Receptors (143)
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