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GPCR / G Protein

产品 51 到 86 共 86个

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  1. 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
  2. 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
  3. 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
  4. 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
  5. 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
  6. 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
  7. 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
  8. 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
  9. 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
  10. 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
  11. 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
  12. 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
  13. 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
  14. 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
  15. 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
  16. 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
  17. 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
  18. 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
  19. 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
  20. 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
  21. 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
  22. 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
  23. 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
  24. 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
  25. 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
  26. 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
  27. 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
  28. 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
  29. 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
  30. 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
  31. 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
  32. 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
  33. 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
  34. 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
  35. 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
  36. 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

产品 51 到 86 共 86个

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分类
  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)
  8. Platelet-Activating Factor (PAF) Receptors (2)
  9. Endothelin Receptors (1)
  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)
靶点
  1. A3 adenosine receptor (1)
  2. Aurora A (1)
  3. Aurora B (1)
  4. Aurora C (1)
  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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