Ipragliflozin is a selective inhibitor of SGLT2 with IC50 of 14 nM for hSGLT2.
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产品名称 | SGLT1 ↓ ↑ | SGLT2 ↓ ↑ | 其他靶点 | 纯度 | |||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Phloretin | ✔ | 98% | |||||||||||||||||
Canagliflozin |
+++
mSGLT2, IC50: 2 nM hSGLT2, IC50: 3.7 nM |
95% | |||||||||||||||||
Empagliflozin |
++
SGLT2, IC50: 3.1 nM |
98% | |||||||||||||||||
Dapagliflozin |
++++
hSGLT2, EC50: 1.1 nM |
97% | |||||||||||||||||
Tofogliflozin (hydrate) |
+++
hSGLT2, IC50: 2.9 nM |
99%+ | |||||||||||||||||
Sotagliflozin |
+
SGLT1, IC50: 36 nM |
++++
SGLT2, IC50: 1.8 nM |
98% | ||||||||||||||||
Ipragliflozin |
++
hSGLT2, IC50: 7.4 nM |
98% | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
靶点 |
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描述 | Ipragliflozin (ASP1941) is an orally active and selective inhibitor of SGLT2, with IC50s of 7.38 and 1876 nM for human SGLT2 and SGLT1, respectively. It serves as an antidiabetic agent[1]. |
Animal study | Ipragliflozin exhibits antihyperglycemic effects, with dose-dependent inhibition of increases in blood glucose levels. In both STZ-induced type 1 diabetic rats and KK-Ay type 2 diabetic mice, this effect is significant at various tested doses[1].In streptozotocin-induced type 1 diabetic rats, repeated administration of Ipragliflozin (0.3 and 1 mg/kg) demonstrates antidiabetic effects[1].In Streptozotocin (STZ; 50 mg/kg)-induced type 1 diabetic rats and KK-Ay type 2 diabetic mice, doses ranging from 0.1 to 1 mg/kg were orally administered once in the fed state. Blood glucose levels were then monitored for 8 hours under fasting conditions. The results indicated a dose-dependent reduction in blood glucose levels, which was statistically significant at all tested doses. This experiment utilized a repeated administration animal model[1].In Streptozotocin (STZ; 50 mg/kg)-induced type 1 diabetic rats, doses of 0.3 and 1 mg/kg were orally administered once daily at night for 4 weeks. The outcome revealed significant reductions in both HbA1c and blood glucose levels. Furthermore, pancreatic insulin content significantly increased at a dose of 1 mg/kg. Urinary glucose excretion exhibited a dose-dependent increase, reaching significance at the 1 mg/kg dose[1]. |
计算器 | ||||
存储液制备 | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
2.47mL 0.49mL 0.25mL |
12.36mL 2.47mL 1.24mL |
24.72mL 4.94mL 2.47mL |
CAS号 | 761423-87-4 |
分子式 | C21H21FO5S |
分子量 | 404.45 |
SMILES Code | O[C@H]1[C@H](C2=CC=C(F)C(CC3=CC4=CC=CC=C4S3)=C2)O[C@H](CO)[C@@H](O)[C@@H]1O |
MDL No. | MFCD19443744 |
别名 | ASP1941 |
运输 | 蓝冰 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Keep in dark place, sealed in dry, 2-8°C |
溶解方案 |
请根据您的动物给药指南选择适当的溶解方案。 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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