GPCR / G Protein

产品 301 到 350 共 385个

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  1. 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
  2. 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
  3. 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
  4. 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
  5. 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
  6. 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
  7. 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
  8. 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
  9. 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
  10. 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
  11. 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
  12. 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
  13. 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
  14. 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
  15. 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
  16. 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
    • 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
  17. GSK1059865

    Catalog No. A12401
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    orexin 1 receptor antagonist
    GSK1059865 is a potent orexin 1 receptor antagonist. 了解更多
  18. 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
  19. 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
  20. 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
  21. 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
  22. 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
  23. Pavinetant

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

    Catalog No. A21473
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    NK1 receptor antagonist
    Maropitant is a neurokinin (NK1) receptor antagonist. 了解更多
  25. 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
  26. 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
  27. 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
  28. 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
  29. 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
  30. 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
  31. 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
  32. 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
  33. 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
  34. 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
  35. 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
  36. 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
  37. 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
  38. 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
  39. 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
  40. 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
  41. 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
  42. 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
  43. FTY720 (Fingolimod)

    Catalog No. A10408
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    S1P Receptor 拮抗剂
    FTY720 (Fingolimod)是ISP-1(肉豆蔻酸)的衍生物,ISP-1是中国草药Iscaria sinclarii的真菌代谢物,也是鞘氨醇的结构类似物。 了解更多
  44. 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
  45. CGRP 8-37 (human)

    Catalog No. A16949
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    CGRP receptor 拮抗剂
    CGRP 8-37 (human)是人降钙素基因相关肽(hCGRP)片段,也是CGRP受体的拮抗剂。序列:Val-Thr-His-Arg-Leu-Ala-Gly-Leu-Leu-Ser-Arg-Ser-Gly-Gly-Val-Val-Lys-Asn-Asn-Phe-Val-Pro-Thr-Asn- Val-Gly-Ser-Lys-Ala-Phe;VTHRLAGLLSRSGGVVKNNFVPTNVGSKAF。 了解更多
  46. Ubrogepant

    Catalog No. A21670
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    CGRP antagonist
    Ubrogepant (MK-1602) is a novel oral calcitonin gene-related peptide receptor (CGRP) antagonist in development for acute treatment of migraine. 了解更多
  47. Olcegepant hydrochloride

    Catalog No. A21900
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    CGRP1 receptor antagonist
    Olcegepant hydrochloride is the first potent and selective non-peptide antagonist of the calcitonin gene-related peptide 1 (CGRP1) receptor with IC50 of 0.03 nM and with a Ki of 14.4 pM for human CGRP. 了解更多
  48. MK 3207 HCl

    Catalog No. A10598
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    CGRP Receptor 拮抗剂
    MK 3207 hydrochloride是一种有效的CGRP受体拮抗剂,IC50为0.12 nM。 了解更多
  49. MK-0974 (Telcagepant)

    Catalog No. A11255
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    CGRP receptor 拮抗剂
    MK-0974 (Telcagepant)是人和恒河猴CGRP受体的有效和选择性拮抗剂。 了解更多

产品 301 到 350 共 385个

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