GPCR / G Protein

产品 1 到 50 共 385个

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  1. R-121919

    Catalog No. A13535
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    CRF1 receptor 拮抗剂
    R121919是有效的小分子CRF1受体拮抗剂。 了解更多
  2. Verucerfont

    Catalog No. A16950
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    CRF-1 拮抗剂
    Verucerfont,也称为GSK561679和NBI77860,是CRF-1拮抗剂。Verucerfont阻止CRH-1受体,因此减少了慢性应激后ACTH的释放。 了解更多
  3. Emicerfont

    Catalog No. A14047
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    CRF-1 拮抗剂
    Emicerfont,也称为GW876008,是一种CRF-1拮抗剂。Emicerfont阻止CRH-1受体,因此减少了ACTH的释放。 了解更多
  4. Pexacerfont

    Catalog No. A14105
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    CRF1 receptor antagonist
    Pexacerfont is a selective corticotropin-releasing factor (CRF1) receptor antagonist with IC50 of 6.1??0.6 nM for human CRF1 receptor. 了解更多
  5. NVS-CRF38

    Catalog No. A21770
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    CRF1 antagonist
    NVS-CRF38 is a novel corticotropin-releasing factor receptor 1 (CRF1) antagonist with low water solubility. 了解更多
  6. CP 376395

    Catalog No. A21973
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    CRF1 receptor antagonist
    CP 376395 is a potent and selective Corticotropin releasing factor 1 (CRF1) receptor antagonist. 了解更多
  7. CP 316311

    Catalog No. A21983
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    CRF1 receptor antagonist
    CP 316311 is a potent and selective CRF1 receptor antagonist with an IC50 value of 6.8 nM. 了解更多
    • 最新产品

    SBI-115

    Catalog No. A17235
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    GPCR19 antagonist
    SBI-115 is a TGR5 (GPCR19) antagonist. SBI-115 decreases hepatic cystogenesis with polycystic liver diseases via inhibiting TGR5. 了解更多
  8. NPS-2143 (SB-262470)

    Catalog No. A11140
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    CaSR 拮抗剂
    NPS-2143 (SB-262470)是一种选择性的Ca2+感应受体拮抗剂,显示可阻止HEK293细胞中表达的人Ca2+受体引起的细胞质Ca2+浓度增加,IC50为43 nM。 了解更多
  9. NPS-2143 hydrochloride

    Catalog No. A11505
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    CaSR antagonist
    NPS-2143 hydrochloride (SB-262470A hydrochloride), an orally active calcilytic agent, is a selective and potent calcium ion-sensing receptor (CaSR) antagonist. 了解更多
  10. Loxiglumide (CR1505)

    Catalog No. A11769
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    CCK-A receptor 拮抗剂
    Loxiglumide (CR1505)是一种胆囊收缩素拮抗剂。 了解更多
  11. Proglumide sodium salt

    Catalog No. A13713
    CCK 拮抗剂
    Proglumide sodium salt是一种非选择性胆囊收缩素(CCK)拮抗剂。它抑制CCK刺激的淀粉酶分泌,并防止CCK诱导的小鼠胰腺腺泡中的2-脱氧葡萄糖摄取。 了解更多
  12. Z-360 calcium salt (Nastorazepide calcium salt)

    Catalog No. A13671
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    CCK-2 receptor 拮抗剂
    Z-360 calcium salt (Nastorazepide calcium salt)是一种选择性口服可口服的1,5-苯并二氮杂卓衍生物胃泌素/胆囊收缩素2(CCK-2)受体拮抗剂,具有潜在的抗肿瘤活性。 了解更多
  13. Nastorazepide (Z-360)

    Catalog No. A15984
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    CCK-2 receptor 拮抗剂
    Nastorazepide (Z-360) 是一种选择性的,口服的1,5-苯二氮杂卓衍生物胃泌素/胆囊收缩素2(CCK-2)受体拮抗剂,具有潜在的抗肿瘤活性。 了解更多
  14. Proglumide

    Catalog No. A18171
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    CCK antagonist
    Proglumide is a drug that exerts an inhibitory effect on gastric secretion and reduces gastrointestinal motility. IProglumide is a known cholecystokinin (CCK) antagonist. 了解更多
  15. Dexloxiglumide

    Catalog No. A18541
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    CCKA receptor antagonist
    Dexloxiglumide is a selective cholecystokinin type A (CCKA) receptor antagonist. Dexloxiglumide, the active enantiomer of Loxiglumide, inhibits smooth muscle cell contractions induced by cholecystokinin-octapeptide (CCK-8). 了解更多
  16. KU14R

    Catalog No. A13987
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    I3 receptor 拮抗剂
    KU14R是胰腺β细胞非典型咪唑啉结合位点(可能的I3受体)的拮抗剂。KU14R也已显示出选择性阻断依法氧烷诱导的胰岛素分泌。 了解更多
  17. ESI-05

    Catalog No. A18644
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    EPAC2 antagonist
    ESI-05 (NSC 116966) is a specific antagonist of EPAC2 (exchange protein directly activated by cAMP 2), with an IC50 of 0.4 ?M. ESI-05 (NSC 116966) inhibits cAMP-mediated activation of EPAC2 as well as EAPC2 mediated Rap1 activation. 了解更多
  18. GSK221149A (Retosiban)

    Catalog No. A13106
    Oxytocin Receptor 拮抗剂
    GSK221149A (Retosiban)是一种口服药物,可作为选择性纳摩尔(Ki = 0.65 nM)催产素受体拮抗剂,其选择性是相关血管加压素受体的> 1400倍。 了解更多
  19. PF-3274167

    Catalog No. A13754
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    Oxytocin 拮抗剂
    PF-3274167是一种高亲和力非肽催产素受体(OTR)拮抗剂,Ki为9.5 nM。 了解更多
  20. SHR1653

    Catalog No. A18575
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    Oxytocin receptor antagonist
    SHR1653 is a highly potent, selective and brain penetrated oxytocin receptor (OTR) antagonist, with an IC50 of 15 nM for hOTR. 了解更多
  21. L-371,257

    Catalog No. A21219
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    oxytocin receptor antagonist
    L-371,257 is an orally bioavailable, non-blood-brain barrier penetrant, selective and competitive antagonist of oxytocin receptor (pA2=8.4) with high affinity at both the oxytocin receptor (Ki=19 nM) and vasopressin V1a receptor (Ki=3.7 nM). 了解更多
  22. S1RA (E-52862)

    Catalog No. A12504
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    sigma-1 receptor 拮抗剂
    S1RA是一种选择性sigma-1受体拮抗剂,据报道其结合亲和力为Ki = 17.0±7.0 nM,对sigma-2受体具有选择性,并且对其他170种受体,酶,转运蛋白和离子通道具有选择性。 了解更多
  23. UMB24

    Catalog No. A13513
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    Sigma2 拮抗剂
    UMB24是推定的sigma2优选拮抗剂。 了解更多
  24. BD-1047 2HBr

    Catalog No. A13196
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    Sigma-1 拮抗剂
    BD-1047 2HBr是sigma受体的选择性功能拮抗剂,在动物模型中显示出抗精神病活性,可预测精神分裂症的疗效。 了解更多
  25. Sigma-1 receptor antagonist 2

    Catalog No. A18504
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    sigma 1 receptor antagonist
    Sigma-1 receptor antagonist 2 is a potent and selective sigma 1 receptor (??1 R) antagonist with Kis of 3.88 and 1288 nM for ??1 and ??2 receptor, respectively. 了解更多
  26. Sigma-1 receptor antagonist 3

    Catalog No. A18501
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    Sigma-1 receptor antagonist
    Sigma-1 receptor antagonist 3 (compound135) is a potent and selective Sigma-1 (??1) receptor antagonist with a Ki of 1.14 nM. 了解更多
  27. Tolvaptan

    Catalog No. A11594
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    vasopressin receptor 2 拮抗剂
    Tolvaptan是一种选择性的竞争性精氨酸加压素受体2拮抗剂,IC50为1.28μM。 了解更多
  28. OPC21268

    Catalog No. A15784
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    vasopressin V1 拮抗剂
    OPC21268是一种非肽AVP受体V(Vasopressin Receptor)拮抗剂,对V1受体的选择性是V2受体的1000倍。 了解更多
  29. Vasopressin antagonist 1867

    Catalog No. A16188
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    V1b receptor 拮抗剂
    Vasopressin antagonist 1867,可口服和选择性V1b受体拮抗剂(hV1b抑制作用的IC50值为3 nM,相对于hV1a,hV2和hOT表现出> 1000倍的选择性)。 了解更多
  30. Mozavaptan

    Catalog No. A16622
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    nonpeptide vasopressin V2 receptor antagonist
    Mozavaptan (OPC31260) is a orally effective, nonpeptide vasopressin V2 receptor antagonist with an IC50 of 14 nM. 了解更多
  31. Lixivaptan

    Catalog No. A21279
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    vasopressin receptor V2 antagonist
    Lixivaptan (VPA-985, WAY-VPA 985) is an orally active and selective vasopressin receptor V2 antagonist, with IC50 values of 1.2 and 2.3 nM for human and rat V2, respectively. 了解更多
  32. RG7713

    Catalog No. A21380
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    Brain-Penetrant Vasopressin 1a (V1a) receptor antagonist
    RG7713 (RO5028442) is a highly potent and selective Brain-Penetrant Vasopressin 1a (V1a) receptor antagonist with Kis of 1 nM (hV1a) and 39 nM (mV1a). 了解更多
  33. 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
  34. 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
  35. BMS-927711

    Catalog No. A13102
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    CGRP receptor 拮抗剂
    BMS-927711是一种有效的,选择性的,竞争性的人降钙素基因相关肽(CGRP)受体拮抗剂,已显示出体内功效,而没有血管收缩作用。 了解更多
  36. MK-3207

    Catalog No. A15165
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    CGRP Receptor 拮抗剂
    MK-3207是一种有效且口服可生物利用的CGRP受体拮抗剂(IC50 = 0.12 nM;Ki = 0.024 nM);对人类AM1,AM2,CTR和AMY3具有高度选择性。 了解更多
  37. 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
  38. 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
  39. 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
  40. 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
  41. 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
  42. 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
  43. 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
  44. 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
  45. 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
  46. 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
  47. 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
  48. 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
  49. 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

产品 1 到 50 共 385个

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