化学信息:
化学名
|
(2S,3R,4R,5S,6R)-2-[3-(1-benzothiophen-2-ylmethyl)-4-fluorophenyl]-6-(hydroxymethyl)oxane-3,4,5-triol
|
|
简称
|
Ipragliflozin
|
别名
|
ASP1941, ASP 1941, ASP-1941
|
中文名
|
N/A
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化学式
|
C21H21FO5S
|
分子量
|
404.45
|
CAS号
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761423-87-4
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纯度
|
98%
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溶剂/溶解度
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Water<1mg/ml; DMSO5mg/ml; Ethanol<1mg/ml
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溶液配制
|
5mg加入1.24ml DMSO,或者每4.04mg加入1ml DMSO,配制成10mM溶液。SF9015-10mM用DMSO配制。
|
生物信息:
产品描述
|
Ipragliflozin (ASP1941) is a highly potent and selective SGLT2 inhibitor with IC50 of 2.8nM; little and NO potency for SGLT1/3/4/5/6.
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信号通路
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Transmembrane Transporters
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靶点
|
SGLT2
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-
|
-
|
-
|
-
|
IC50
|
2.8nM
|
-
|
-
|
-
|
-
|
体外研究
|
Ipragliflozin potently and selectively inhibited human, rat, and mouse SGLT2 at nanomolar ranges and exhibited stability against intestinal glucosidases.
|
体内研究
|
Ipragliflozin showed good pharmacokinetic properties following oral dosing, and dose-dependently increased urinary glucose excretion, which lasted for over 12h in normal mice. Oral administration of ipragliflozin increased urinary glucose excretion in a dose-dependent manner, an effect which was significant at doses of 0.3mg/kg or higher and lasted over 12h. Single administration of ipragliflozin dose-dependently increased urinary glucose excretion, reduced blood glucose and plasma insulin levels, and improved glucose intolerance.
|
临床实验
|
N/A
|
特征
|
N/A
|
相关实验数据(此数据来自于公开文献,碧云天并不保证其有效性):
酶活性检测实验
|
方法
|
N/A
|
细胞实验
|
细胞系
|
N/A
|
浓度
|
N/A
|
处理时间
|
N/A
|
方法
|
N/A
|
动物实验
|
动物模型
|
N/A
|
配制
|
N/A
|
剂量
|
N/A
|
给药方式
|
N/A
|
参考文献:
1. Imamura M, et al. Bioorg Med Chem. 2012 May 15, 20(10), 3263-79.
2. Suzuki M, et al. J Pharmacol Exp Ther. 2012 Jun, 341(3), 692-701.
3. Tahara A, et al. Naunyn Schmiedebergs Arch Pharmacol. 2012 Apr, 385(4), 423-36.
4. Tahara A, et al. J Pharmacol Sci. 2012, 120(1), 36-44.
5. Tahara A, et al. Eur J Pharmacol. 2013 Sep 5, 715(1-3), 246-55.
包装清单:
产品编号
|
产品名称
|
包装
|
SF9015-10mM
|
Ipragliflozin (SGLT2抑制剂)
|
10mM×0.2ml
|
SF9015-5mg
|
Ipragliflozin (SGLT2抑制剂)
|
5mg
|
SF9015-25mg
|
Ipragliflozin (SGLT2抑制剂)
|
25mg
|
—
|
说明书
|
1份
|
保存条件:
-20℃保存,至少一年有效。5mg和25mg包装也可室温保存,至少6个月有效。如果溶于非DMSO溶剂,建议分装后-80℃保存,预计6个月内有效。
注意事项:
本产品仅限于专业人员的科学研究用,不得用于临床诊断或治疗,不得用于食品或药品,不得存放于普通住宅内。
为了您的安全和健康,请穿实验服并戴一次性手套操作。