Ipragliflozin
(Synonyms: 伊格列净; ASP1941) 目录号 : GC16469
An SGLT2 inhibitor
Cas No.:761423-87-4
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Ipragliflozin is a selective inhibitor of sodium–glucose cotransporter 2 (SGLT2) with IC50 value of 7.38nM [1].
Ipragliflozin is a derivative of phlorizin. It shows inhibition activity for mouse, rat and human SGLT2 with IC50 values of 7.38nM, 6.73nM and 5.64nM, respectively. It is not effective for SGLT1 with IC50 value of 1876nM. In the radioligand binding and enzyme assays, lpragliflozin shows no interaction with other receptors, channels, and transporters like adrenergic, muscarinic and calcium channel, demonstrating a specific inhibition of SGLT2. As a glucitol compound, ipragliflozin is stable against glucosidases in mouse small intestine [1].
Since SGLT2 plays a critical role in renal glucose reabsorption, ipragliflozin is therapeutic potent to treat hyperglycemia in diabetes through increasing glucose excretion into urine. In STZ-induced type 1 diabetic rats and KK-Ay type 2 diabetic mice, the single administration of ipragliflozin significantly decreases the blood glucose levels [1].
References:
[1] Tahara A, Kurosaki E, Yokono M, Yamajuku D, Kihara R, Hayashizaki Y, Takasu T, Imamura M, Qun L, Tomiyama H, Kobayashi Y, Noda A, Sasamata M, Shibasaki M. Pharmacological profile of ipragliflozin (ASP1941), a novel selective SGLT2 inhibitor, in vitro and in vivo. Naunyn Schmiedebergs Arch Pharmacol. 2012 Apr;385(4):423-36.
| Cas No. | 761423-87-4 | SDF | |
| 别名 | 伊格列净; ASP1941 | ||
| 化学名 | (2S,3R,4R,5S,6R)-2-[3-(1-benzothiophen-2-ylmethyl)-4-fluorophenyl]-6-(hydroxymethyl)oxane-3,4,5-triol | ||
| Canonical SMILES | C1=CC=C2C(=C1)C=C(S2)CC3=C(C=CC(=C3)C4C(C(C(C(O4)CO)O)O)O)F | ||
| 分子式 | C21H21FO5S | 分子量 | 404.45 |
| 溶解度 | DMF: 30 mg/mL,DMSO: 30 mg/mL,Ethanol: 30 mg/mL,Ethanol:PBS (pH7.2) (1:7): 0.13 mg/mL | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.4725 mL | 12.3625 mL | 24.7249 mL |
| 5 mM | 0.4945 mL | 2.4725 mL | 4.945 mL |
| 10 mM | 0.2472 mL | 1.2362 mL | 2.4725 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。