SGLT


SGLT are a family of glucose transporter found in the intestinal mucosa (enterocytes) of the small intestine (SGLT1) and the proximal tubule of the nephron (SGLT2 in PCT and SGLT1 in PST). They contribute to renal glucose reabsorption. In the kidneys, 100% of the filtered glucose in the glomerulus has to be reabsorbed along the nephron (98% in PCT, via SGLT2). If the plasma glucose concentration is too high (hyperglycemia), glucose is excreted in urine (glucosuria) because SGLT are saturated with the filtered glucose. 
  • BMS-777607 EY0897

    BMS-777607是Met-相关抑制剂,对c-Met,Axl,Ron和Tyro3的IC50分别为3.9 nM,1.1 nM,1.8 nM和4.3 nM,比对Lck,VEGFR-2和TrkA/B的抑制性强40倍。

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  • Empagliflozin EY0853

    Empagliflozin (BI 10773)是一种有效的,选择性SGLT-2抑制剂,IC50为3.1 nM,比作用于SGLT-1, 4, 5和6选择性高300倍以上。

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  • BMS-794833 EY0835

    BMS-794833是Met/VEGFR2高效ATP竞争性抑制剂,IC50值为1.7/15 nM,还能抑制Ron, Axl和Flt3的活性,是BMS-817378的前体药物。

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  • MPEP EY0765

    MPEP is a selective mGlu5 receptor antagonist with IC50 of 36 nM, exhibits no appreciable activity at mGlu1b/2/3/4a/7b/8a/6 receptors.MPEP是mGlu5受体非竞争性拮抗剂,IC50为36 nM,还是mGlu4受体的正向变构调节剂。

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  • MK-2461 EY0673

    MK-2461是一种有效的,多靶点抑制剂,作用于c-Met(WT/mutants),IC50为0.4-2.5 nM,对Ron,和Flt1作用效果稍弱;作用于c-Met比作用于FGFR1, FGFR2, FGFR3, PDGFRβ, KDR, Flt3, Flt4, TrkA和TrkB选择性高8到30倍。Phase 1/2。

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  • BMS-777607 EY0897

    BMS-777607是Met-相关抑制剂,对c-Met,Axl,Ron和Tyro3的IC50分别为3.9 nM,1.1 nM,1.8 nM和4.3 nM,比对Lck,VEGFR-2和TrkA/B的抑制性强40倍。

    More
  • Empagliflozin EY0853

    Empagliflozin (BI 10773)是一种有效的,选择性SGLT-2抑制剂,IC50为3.1 nM,比作用于SGLT-1, 4, 5和6选择性高300倍以上。

    More
  • BMS-794833 EY0835

    BMS-794833是Met/VEGFR2高效ATP竞争性抑制剂,IC50值为1.7/15 nM,还能抑制Ron, Axl和Flt3的活性,是BMS-817378的前体药物。

    More
  • MPEP EY0765

    MPEP is a selective mGlu5 receptor antagonist with IC50 of 36 nM, exhibits no appreciable activity at mGlu1b/2/3/4a/7b/8a/6 receptors.MPEP是mGlu5受体非竞争性拮抗剂,IC50为36 nM,还是mGlu4受体的正向变构调节剂。

    More
  • MK-2461 EY0673

    MK-2461是一种有效的,多靶点抑制剂,作用于c-Met(WT/mutants),IC50为0.4-2.5 nM,对Ron,和Flt1作用效果稍弱;作用于c-Met比作用于FGFR1, FGFR2, FGFR3, PDGFRβ, KDR, Flt3, Flt4, TrkA和TrkB选择性高8到30倍。Phase 1/2。

    More
  • BMS-777607 EY0897

    BMS-777607是Met-相关抑制剂,对c-Met,Axl,Ron和Tyro3的IC50分别为3.9 nM,1.1 nM,1.8 nM和4.3 nM,比对Lck,VEGFR-2和TrkA/B的抑制性强40倍。

    More
  • Empagliflozin EY0853

    Empagliflozin (BI 10773)是一种有效的,选择性SGLT-2抑制剂,IC50为3.1 nM,比作用于SGLT-1, 4, 5和6选择性高300倍以上。

    More
  • BMS-794833 EY0835

    BMS-794833是Met/VEGFR2高效ATP竞争性抑制剂,IC50值为1.7/15 nM,还能抑制Ron, Axl和Flt3的活性,是BMS-817378的前体药物。

    More
  • MPEP EY0765

    MPEP is a selective mGlu5 receptor antagonist with IC50 of 36 nM, exhibits no appreciable activity at mGlu1b/2/3/4a/7b/8a/6 receptors.MPEP是mGlu5受体非竞争性拮抗剂,IC50为36 nM,还是mGlu4受体的正向变构调节剂。

    More
  • MK-2461 EY0673

    MK-2461是一种有效的,多靶点抑制剂,作用于c-Met(WT/mutants),IC50为0.4-2.5 nM,对Ron,和Flt1作用效果稍弱;作用于c-Met比作用于FGFR1, FGFR2, FGFR3, PDGFRβ, KDR, Flt3, Flt4, TrkA和TrkB选择性高8到30倍。Phase 1/2。

    More
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