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GPCR / G Protein

产品 1 到 50 共 86个

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  1. MK 0893
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    MK 0893

    Catalog No. A11495
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    GCGR 抑制剂
    MK 0893是胰高血糖素受体拮抗剂作为抗糖尿病药物，IC50 值为 6.6 nM。 了解更多
  2. ESI-09
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    ESI-09

    Catalog No. A14233
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    EPAC1/EPAC2 抑制剂
    ESI-09是一种直接由cAMP（EPAC）抑制剂激活的特异性交换蛋白，对于EPAC1和EPAC2，IC50为3.2 uM和1.4 uM。 了解更多
  3. HJC0350
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    HJC0350

    Catalog No. A14266
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    EPAC2 抑制剂
    HJC0350是一种有效的选择性EPAC2抑制剂，IC50为0.3μM，对Epac1无抑制作用。 了解更多
  4. SQ22536
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    SQ22536

    Catalog No. A16116
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    adenylyl cyclase 抑制剂
    SQ22536是腺苷酸环化酶的抑制剂，IC50为1.4 uM。它可以抑制完整人血小板中PGE1刺激的cAMP水平升高。 了解更多
  5. NS-2028
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    NS-2028

    Catalog No. A21643
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    sGC inhibitor
    NS-2028 is a highly selective soluble Guanylyl Cyclase (sGC) inhibitor with IC50 values of 30 nM and 200 nM for basal and NO-stimulated enzyme activity. 了解更多
  6. Atosiban
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    Atosiban

    Catalog No. A14334
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    peptide Oxytocin Receptor 抑制剂
    Atosiban是一种肽催产素受体抑制剂。 了解更多
  7. BAF312 (Siponimod)
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    BAF312 (Siponimod)

    Catalog No. A12906
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    S1PR1/S1PR5 抑制剂
    BAF312 (Siponimod)是下一代有效的1-磷酸鞘氨醇（S1P）受体激动剂，对S1P1和S1P5具有选择性。 了解更多
  8. PF-543
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    PF-543

    Catalog No. A13039
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    SphK1 抑制剂
    PF-543是一种新型选择性SK-1抑制剂，可与鞘氨醇竞争性抑制SK-1活性。 了解更多
  9. ABC294640
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    ABC294640

    Catalog No. A12614
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    SphK2 抑制剂
    ABC294640是一种口服的芳基金刚烷化合物，是鞘氨醇激酶2（SK2）的选择性抑制剂，Ki 为 9.8 μM，具有潜在的抗肿瘤活性。 了解更多
  10. PF-543 Citrate
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    PF-543 Citrate

    Catalog No. A15210
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    SphK1 抑制剂
    PF-543 Citrate是一种新型的SphK1细胞渗透抑制剂，K（i）为3.6 nM，PF-543具有鞘氨醇竞争性，对SphK1的选择性是SphK2同种型的100倍以上。 了解更多
  11. 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
  12. 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
  13. 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
  14. 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
  15. 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
  16. 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
  17. 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
  18. 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
  19. 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
  20. 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
  21. Reversine
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    Reversine

    Catalog No. A13250
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    human A3 adenosine receptor 拮抗剂 /Aurora 抑制剂
    Reversine是一种有效的人A3腺苷受体拮抗剂，Ki为0.66μM，是一种泛光A/B/C激酶抑制剂，IC50分别为12 nM/13 nM/20 nM。也用于干细胞去分化。 了解更多
  22. Pentostatin
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    Pentostatin

    Catalog No. A11534
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    Adenosine deaminase 抑制剂
    Pentostatin是腺苷脱氨酶的不可逆抑制剂(Ki = 2.5 pM)。 了解更多
  23. MT-DADMe-ImmA
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    MT-DADMe-ImmA

    Catalog No. A13651
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    human 5'-methylthioadenosine phosphorylase inhibitor
    MT-DADMe-ImmA is an inhibitor of human 5'-methylthioadenosine phosphorylase (MTAP) with a Ki of 90 pM. 了解更多
  24. EHNA hydrochloride
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    EHNA hydrochloride

    Catalog No. A21585
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    Adenosine deaminase inhibitor
    EHNA hydrochloride is a specific inhibitor of adenosine deaminase, prevents dAdo degradation and increases mitochondrial dATP levels in fibroblasts. 了解更多
  25. Laropiprant (MK0524)
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    Laropiprant (MK0524)

    Catalog No. A11483
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    DP1 抑制剂
    Laropiprant (MK0524)与烟酸合用可降低血液胆固醇。是一种有效的，选择性的 DP receptor 拮抗剂，Ki 值为 0.57 nM，对 TP 受体的 Ki 值为 2.95 nM。 了解更多
  26. Ozagrel hydrochloride
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    Ozagrel hydrochloride

    Catalog No. A11742
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    Thromboxane A2 synthesis 抑制剂
    Ozagrel hydrochloride是一种抗血小板剂，用作血栓烷a2合成抑制剂。 了解更多
  27. Benorylate
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    Benorylate

    Catalog No. A17501
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    Prostaglandin Receptor inhibitor
    Benorilate, also known as Win-11450, is an ester of aspirin and paracetamol with analgesic, antipyretic, and anti-inflammatory activity used in the treatment of rheumatoid diseases. Benorilate has less severe side effects than aspirin. 了解更多
  28. Dinoprost tromethamine
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    Dinoprost tromethamine

    Catalog No. A17505
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    Prostaglandin Receptor inhibitor
    Dinoprost Tromethamine, also known as Dinoprost Trometamol, is a naturally occurring prostaglandin used in medicine to induce labor and as an abortifacient. 了解更多
  29. Bosentan
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    Bosentan

    Catalog No. A11091
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    ETAR/ETBR 抑制剂
    Bosentan是内皮素-1（ET-A）和内皮素B（ET-B）受体的竞争性拮抗剂。 了解更多
  30. QS 11
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    QS 11

    Catalog No. A11228
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    ATPase and GTPase 抑制剂
    QS-11是ADP-核糖基化因子1（ARFGAP1）抑制剂的GTPase活化蛋白。 了解更多
  31. CASIN
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    CASIN

    Catalog No. A12912
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    Cdc42 GTPase 抑制剂
    CASIN是一种新型有效的Cdc42抑制剂。 了解更多
  32. CCG 50014
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    CCG 50014

    Catalog No. A16432
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    RGS4 抑制剂
    CCG 50014是RGS4的有效和选择性抑制剂，IC50为30 nM。 了解更多
  33. MSX-122
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    MSX-122

    Catalog No. A12596
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    CXCR4 抑制剂
    MSX-122是口服可生物利用的CXCR4抑制剂（IC50 =?10 nM），具有潜在的抗肿瘤和抗病毒活性。CXCR4抑制剂MSX-122与趋化因子受体CXCR4结合，阻止基质衍生因子-1（SDF-1）与CXCR4受体和受体激活结合，这可能导致肿瘤细胞增殖和迁移减少。 了解更多
  34. Reparixin
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    Reparixin

    Catalog No. A12383
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    CXCL8/CXCR1/2 抑制剂
    Reparixin是两种CXCL8受体CXCR1/2的有效抑制剂，它抑制CXCR2介导的细胞迁移（IC50 = 100 nM），而它强烈地阻断CXCR1介导的趋化性（IC50 = 1 nM）。 了解更多
  35. Reparixin L-lysine salt
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    Reparixin L-lysine salt

    Catalog No. A15219
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    CXCL8 receptor 抑制剂
    Reparixin L-lysine salt是CXCL8受体的抑制剂，也抑制CXCR1和CXCR2的活化，已显示在各种损伤模型中减弱了炎症反应。 了解更多
  36. LDE225 Diphosphate
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    LDE225 Diphosphate

    Catalog No. A12774
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    Smoothened 抑制剂
    LDE225 Diphosphate 是一种具有潜在抗肿瘤活性的口服生物利用小分子平滑（Smo）拮抗剂。抑制Hedgehog (Hh)信号通路，无细胞试验中IC50分别为1.3 nM (小鼠)和2.5 nM(人)。 了解更多
  37. PF-5274857
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    PF-5274857

    Catalog No. A12775
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    Smoothened 抑制剂
    PF-5274857是一种新型Smo拮抗剂，它以4.6±1.1 nmol/L的K（i）特异性结合Smo，并以2.7±1.4 nmol/L的IC（50）完全阻断下游基因Gli1的转录活性。在细胞中。 了解更多
  38. BMS-833923 (XL-139)
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    BMS-833923 (XL-139)

    Catalog No. A13204
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    Smoothened 抑制剂
    BMS-833923 (XL-139)是一种生物可利用的小分子SMO(平滑)抑制剂，具有潜在的抗肿瘤活性。 了解更多
  39. Glasdegib (PF-04449913)
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    Glasdegib (PF-04449913)

    Catalog No. A13881
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    Smoothened 抑制剂
    PF-04449913是有效且口服可生物利用的平滑化抑制剂。 了解更多
  40. Jervine
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    Jervine

    Catalog No. A16221
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    SMO 抑制剂
    Jervine是天然存在的甾体生物碱，可通过阻断声波刺猬（Shh）信号传导而引起Cyclopia。抑制Smo。 了解更多
  41. Saridegib
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    Saridegib

    Catalog No. A12966
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    Smo inhibitor
    Saridegib is a potent and specific inhibitor of Smoothened (Smo), a key signaling transmembrane protein in the Hedgehog (Hh) pathway. 了解更多
  42. LEQ506
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    LEQ506

    Catalog No. A20941
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    Smo inhibitor
    LEQ506 is a second-generation inhibitor of smoothened (Smo) with IC50s of 2 and 4 nM in human and mouse, respectively. 了解更多
  43. (-)-Huperzine A
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    (-)-Huperzine A

    Catalog No. A10006
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    GluR 抑制剂
    (-)-Huperzine A是一种天然存在的倍半萜生物碱化合物，存在于石楠石杉中。 了解更多
  44. Vanoxerine 2HCl (GBR-12909)
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    Vanoxerine 2HCl (GBR-12909)

    Catalog No. A10725
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    dopamine re-uptake 抑制剂
    Vanoxerine 2HCl (GBR-12909)是哌嗪衍生物，是一种有效的、选择性的多巴胺摄取（dopamine uptake）抑制剂。 了解更多
  45. Lurasidone (SM13496)
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    Lurasidone (SM13496)

    Catalog No. A11214
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    Dopamine D2 抑制剂
    Lurasidone (SM-13496)是dopamine D2和5-HT7的拮抗剂，IC50 值分别为 1.68 和 0.495 nM。Lurasidone (SM-13496) 也是 5-HT1A 受体的部分激动剂。 了解更多
  46. GBR-12935 2HCl
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    GBR-12935 2HCl

    Catalog No. A11937
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    DAT and SLC6A2 抑制剂
    GBR-12935 dihydrochloride是一种有效的选择性多巴胺再摄取抑制剂。 了解更多
  47. Haloperidol (Haldol)
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    Haloperidol (Haldol)

    Catalog No. A10446
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    CYP2D6 抑制剂
    Haloperidol (Haldol)是一种抗精神病药和丁二酮。 了解更多
  48. GBR 12783 dihydrochloride
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    GBR 12783 dihydrochloride

    Catalog No. A13128
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    dopamine uptake 抑制剂
    GBR 12783 dihydrochloride是一种非常有效的选择性多巴胺摄取抑制剂（抑制大鼠纹状体突触体中[3H]-多巴胺摄取的IC50为1.8 nM）。 了解更多
  49. Bupropion
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    Bupropion

    Catalog No. A15850
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    NDR 抑制剂
    Bupropion是主要用作抗抑郁药和戒烟辅助药的药物。 了解更多
  50. Nepicastat (free base) (SYN-117)
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    Nepicastat (free base) (SYN-117)

    Catalog No. A10637
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    dopamine beta-hydroxylase 抑制剂
    Nepicastat (free base) (SYN-117)是多巴胺β-羟化酶的抑制剂，该酶催化多巴胺向去甲肾上腺素的转化。 了解更多

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  1. 5-HT Receptors (16)
  2. Adrenergic Receptors (7)
  3. Histamine Receptors (6)
  4. Metabotropic glutamate receptors (mGluR) (1)
  5. Smoothened Receptors (7)
  6. CXCR (3)
  7. G Protein (3)
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  10. Prostanoid Receptors (4)
  11. Adenosine Receptors (5)
  12. Cannabinoid Receptors (2)
  13. Protease-Activated Receptors (PAR) (1)
  14. S1P Receptor (10)
  15. Guanylate Cyclase (1)
  16. cAMP (3)
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  2. Aurora A (1)
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  5. COX-1 (1)
  6. COX-2 (1)
  7. CXCL8 (2)
  8. CXCR1 (2)
  9. CXCR2 (2)
  10. CXCR4 (1)
  11. Histamine H1 receptor (1)
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