Azilsartan D5
(Synonyms: 阿齐沙坦D5; TAK-536-d5) 目录号 : GC35452
An internal standard for the quantification of azilsartan
Cas No.:1346599-45-8
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Azilsartan-d5 is intended for use as an internal standard for the quantification of azilsartan by GC- or LC-MS. Azilsartan is an antagonist of the angiotensin II type 1 receptor (AT1; IC50 = 0.42 ?M) and the active metabolite of azilsartan medoxomil .1,2 Azilsartan is formed from azilsartan medoxomil by hydrolysis in the gastrointestinal tract and liver.3 Azilsartan also acts as an inverse agonist, inhibiting angiotensin II-induced accumulation of inositol-1-phosphate in COS-7 cells expressing recombinant human AT1 (IC50 = 2.6 nM).2 It reduces the maximal contractile response induced by angiotensin II in isolated rabbit aortic strips (pD2 = 9.9).2 Azilsartan (100 ng/kg, i.v.) inhibits the angiotensin II-induced pressor response in conscious normotensive rats.1
1.Kohara, Y., Kubo, K., Imamiya, E., et al.Synthesis and angiotensin II receptor antagonistic activities of benzimidazole derivatives bearing acidic heterocycles as novel tetrazole bioisosteresJ. Med. Chem.39(26)5228-5235(1996) 2.Ojima, M., Igata, H., Tanaka, M., et al.In vitro antagonistic properties of a new angiotensin type 1 receptor blocker, azilsartan, in receptor binding and function studiesJ. Pharmacol. Exp. Ther.336(3)801-808(2011) 3.Clas, S.-D., Sanchez, R.I., and Nofsinger, R.Chemistry-enabled drug delivery (prodrugs): Recent progress and challengesDrug Discov. Today19(1)79-87(2014)
| Cas No. | 1346599-45-8 | SDF | |
| 别名 | 阿齐沙坦D5; TAK-536-d5 | ||
| Canonical SMILES | OC(C1=CC=CC2=C1N(C(OC(C([2H])([2H])[2H])([2H])[2H])=N2)CC(C=C3)=CC=C3C4=CC=CC=C4C5=NC(ON5)=O)=O | ||
| 分子式 | C25H15D5N4O5 | 分子量 | 461.48 |
| 溶解度 | DMSO : 100 mg/mL (216.69 mM; Need ultrasonic); DMSO : 100 mg/mL (216.69 mM; Need ultrasonic) | 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 | 2.1669 mL | 10.8347 mL | 21.6694 mL |
| 5 mM | 0.4334 mL | 2.1669 mL | 4.3339 mL |
| 10 mM | 0.2167 mL | 1.0835 mL | 2.1669 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。