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  • Ipragliflozin
    货号: abs817510
    CAS号: 761423-87-4
    分子式: C21H21FO5S
    分子量: 404.45
    产品说明书
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    货号-规格 货期 价格 数量
    abs817510-5mg 1-2周 ¥1152.00
    - +
    abs817510-10mg 1-2周 ¥1794.00
    - +
    abs817510-50mg 1-2周 ¥5362.00
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    abs817510-100mg 1-2周 ¥8637.00
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    大包装询价
    产品描述
    描述
    Ipragliflozin (ASP1941) is a highly potent and selective SGLT2 inhibitor with IC50 of 2.8 nM; little and NO potency for SGLT1/3/4/5/6.
    纯度
    99%
    储存/保存方法
    Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
    基本信息
    可溶性/溶解性
    10 mM in DMSO
    生物活性
    靶点
    mouse SGLT2 ,rat SGLT2 ,hSGLT2
    In vitro(体外研究)
    Ipragliflozin concentration-dependently inhibits mouse, rat, and human SGLT2 activity at nanomolar concentrations. Furthermore, ipragliflozin does not potently inhibit human SGLT4 and SGLT5 isoforms (IC50>1,000 nM). In addition, ipragliflozin does not inhibit several glucose transporter (GLUT) isoforms, including GLUT1 and GLUT4, in mouse 3T3-L1, rat L6, human Caco-2, and HepG2 cells (IC50>1,000 nM). Ipragliflozin does not interact with various receptors, ion channels, and transporters such as adrenergic (α1, α2, and β), muscarinic (M1, M2, and non-selective), angiotensin(AT1 and AT2), calcium channel (L-type and N-type), potassium channel (KATP and SKCa), sodium channel (site 2), cholecystokinin (CCKA and CCKB), dopamine (D1, D2, and transporter), endothelin (ETA and ETB), gamma-aminobutyric acid (GABAA and GABAB), glutamate (AMPA, kainate, and NMDA), serotonin (5-HT1, 5HT2B, and transporter), histamine (H1, H2, and H3), and neurokinin (NK1, NK2, and NK3), exhibiting IC50 values >3,000 nM. Ipragliflozi is stable against mouse intestinal glucosidases.
    In vivo(体内研究)
    Single oral doses (0.01-10 mg/kg) of ipragliflozin induces urinary glucose excretion in a dose-dependent manner in both normal and in KK-Ay mice, a type 2 diabetes model. Single administrations of ipragliflozin (0.1, 0.3 and 1 mg/kg) dose-dependently reduces blood glucose level in both KK-Ay mice and STZ rats. Administration of a single 0.3 mg/kg dose intravenously and a single 1 mg/kg dose orally to rats reveal that ipragliflozin has good bioavailability with a value of 71.7%. Ipragliflozin shows good pharmacokinetic properties following oral dosing, and dose-dependently increased urinary glucose excretion, which lasts for over 12 h in normal mice. Single administration of ipragliflozin results in dose-dependent and sustained antihyperglycemic effects in both diabetic models. It has a low risk of hypoglycemia. After oral administration of ipragliflozin (3 mg/kg) to normal mice, plasma concentrations of ipragliflozin reach a maximum at 1 h and then gradually decrease. Obvious plasma concentrations are detected even 8 h after administration. In the pharmacokinetic studies in mice, ipragliflozin shows good oral bioavailability and exhibits high drug concentrations for long periods. The absolute bioavailabilities of ipragliflozin are 71.7-90.7% and 74.5-75.3% in rats and monkeys, respectively .
    参考文献
    参考文献
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    • 实验方法 实验条件
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