Losartan Carboxylic Acid
(Synonyms: 氯沙坦羧酸,E-3174,EXP-3174) 目录号 : GC12512
An active metabolite of losartan
Cas No.:124750-92-1
Sample solution is provided at 25 µL, 10mM.
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Ki = 5-20 nM
Losartan Carboxylic Acid, also named E-3174, a physiologically active metabolite of losartan, is a non-peptide, potent angiotensin II (AII) receptor, type 1 (AT1) antagonist, which inhibits the AII induced cellular responses. AII is the primary mediator of the reninangiotensin system, which regulates the blood pressure and body-fluid balance and may be associated with the development of cardiovascular diseases via increasing contractility and cell growth in vascular smooth muscle cells (VSMC).
In vitro: E-3174 potently blocked the specific binding of [125I]-AII to VSMC isolated from rat aorta. E-3174 was able to dampen the platelet-derived growth factor-induced increase in cell DNA synthesis and protein, which led to the blockade of the AII-induced increase in cell protein [1].
In vivo: Rats were administrated E-3174 intravenously at a dose of l.0 mg/kg. After 6 hours, E-3174 markedly attenuated the cardiovascular effects of AII in rats. E-3174 induced a progressive fall in mean arterial pressure and a marked increase in renal flow only [2].
References:
[1]. Li, X. & Widdop, R. Angiotensin Type I Receptor Antagonists CY-11974 and EXP 3174 Cause Selective Renal Vasodilatation in Conscious Spontaneously Hypertensive Rats. Clinical Science, 1996; 91(2): 147-154.
[2]. Sachinidis, A., Ko, Y., Weisser, P., zu BricBkwedde, M., Dsing, R., & Christian, R. et al. EXP3174, a metabolite of losartan (MK954, DuP753) is more potent than losartan in blocking the angiotensin ll-induced responses in vascular smooth muscle cells. Journal of Hypertension. 1993; 11(2): 155-162.
| Cas No. | 124750-92-1 | SDF | |
| 别名 | 氯沙坦羧酸,E-3174,EXP-3174 | ||
| 化学名 | 2-butyl-4-chloro-1-[[2'-(2H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl]-1H-imidazole-5-carboxylic acid | ||
| Canonical SMILES | [H]N1N=NN=C1C2=CC=CC=C2C3=CC=C(CN4C(C(O)=O)=C(Cl)N=C4CCCC)C=C3 | ||
| 分子式 | C22H21ClN6O2 | 分子量 | 436.9 |
| 溶解度 | ≤30mg/ml in ethanol;30mg/ml in DMSO;30mg/ml in dimethyl formamide | 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 | 2.2889 mL | 11.4443 mL | 22.8885 mL |
| 5 mM | 0.4578 mL | 2.2889 mL | 4.5777 mL |
| 10 mM | 0.2289 mL | 1.1444 mL | 2.2889 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。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet