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GPCR / G Protein

产品 1 到 50 共 385个

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  1. R-121919
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    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
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    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
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    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
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    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
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    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
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    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
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    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
  8. SBI-115
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    • 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
  9. NPS-2143 (SB-262470)
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    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
  10. NPS-2143 hydrochloride
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    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
  11. Loxiglumide (CR1505)
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    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
  12. Proglumide sodium salt
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    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
  13. Z-360 calcium salt (Nastorazepide calcium salt)
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    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
  14. Nastorazepide (Z-360)
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    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
  15. Proglumide
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    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
  16. Dexloxiglumide
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    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
  17. KU14R
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    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
  18. ESI-05
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    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
  19. GSK221149A (Retosiban)
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    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
  20. PF-3274167
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    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
  21. SHR1653
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    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
  22. L-371,257
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    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
  23. S1RA (E-52862)
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    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
  24. UMB24
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    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
  25. BD-1047 2HBr
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    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
  26. Sigma-1 receptor antagonist 2
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    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
  27. Sigma-1 receptor antagonist 3
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    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
  28. Tolvaptan
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    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
  29. OPC21268
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    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
  30. Vasopressin antagonist 1867
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    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
  31. Mozavaptan
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    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
  32. Lixivaptan
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    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
  33. RG7713
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    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
  34. MK 3207 HCl
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    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
  35. MK-0974 (Telcagepant)
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    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
  36. BMS-927711
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    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
  37. MK-3207
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    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
  38. CGRP 8-37 (human)
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    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
  39. Ubrogepant
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    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
  40. Olcegepant hydrochloride
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    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
  41. FTY720 (Fingolimod)
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    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
  42. 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
  43. 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
  44. 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
  45. 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
  46. 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
  47. 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
  48. 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
  49. 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
  50. 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

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