Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ripisartan (UP-269-6) 是一种强效的特异性血管紧张素 II 受体拮抗剂,对血管紧张素 II 介导的交感神经性心动过速反应有抑制作用。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 1,330 | 现货 | ||
5 mg | ¥ 3,310 | 现货 | ||
10 mg | ¥ 4,820 | 现货 | ||
25 mg | ¥ 7,580 | 现货 | ||
50 mg | ¥ 9,870 | 现货 | ||
100 mg | ¥ 13,800 | 现货 | ||
500 mg | ¥ 27,600 | 现货 |
产品描述 | Ripisartan (UP-269-6) is a potent and specific angiotensin II receptor antagonist that inhibits angiotensin II-mediated sympathetic tachycardia responses. |
靶点活性 | Adrenal membranes:35.8 nM, Smooth muscle cells (SMCs):23.8 nM |
体外活性 |
UP 269-6 bound selectively to AT1 receptors as evidenced by the inhibition of specific [125I] Sar1, Ile8-AII binding in rat adrenal membranes (IC50 = 35.8 nM) and in cultured vascular smooth muscle cells (IC50 = 23.8 nM). UP 269-6 displayed a very high selectivity for the AT1 compared to the AT2 receptor subtype (IC50 >10,000 nM). UP 269-6 inhibited the AII-induced contraction of isolated rabbit aortic strips.[4] UP 269-6 at low concentrations (10(-10), 3 x 10(-10), 10(-9) M) of UP 269-6 and insurmountable antagonism at higher concentrations (3 x 10(-9), 10(-8), 3 x 10(-8) M). Based on the calculated pA2 values, UP 269-6 (9.86 +/- 0.25) was an angiotensin II receptor antagonist as potent as L-158,809 (9.82 +/- 0.37) and much more potent than losartan (7.96 +/- 0.38). UP 269-6 was devoid of affinity (IC50 > 10,000 nM) for many other receptors, ion channels and uptake sites, demonstrating its high specificity for AII receptors. Furthermore, this compound did not affect the contractile response to KCl or phenylephrine in rabbit aorta and exhibited no effect on angiotensin-converting enzyme activity. These data demonstrate that UP 269-6 is a highly potent, selective, and specific AT1 receptor antagonist.[4] |
体内活性 |
UP 269-6 (0.03-1 mg/kg; i.v.; rats) shifted dose-dependently to the right of the dose-pressor response curve for angiotensin II and decreased the maximum response. UP 269-6 antagonized the angiotensin II sympathetic-mediated tachycardiac response.[1] UP 269-6 inhibited dose-dependently the pressor response to angiotensin II with an ID50 of 4.5 micrograms/kg, i.v. in conscious normotensive dogs.[1] UP 269-6 (0.1 to 30 mg/kg; Oral) resulted in a dose-dependent and long-lasting inhibition of the angiotensin II-induced pressor response in conscious normotensive rats and dogs.[1] UP 269-6 is a potent and specific angiotensin II receptor antagonist and does not possess agonistic properties. |
别名 | UP 269-6, UP-2696, UP 2696, UP-269-6, UP269-6 |
分子量 | 426.47 |
分子式 | C23H22N8O |
CAS No. | 148504-51-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 55 mg/mL (128.97 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.3448 mL | 11.7242 mL | 23.4483 mL | 58.6208 mL |
5 mM | 0.469 mL | 2.3448 mL | 4.6897 mL | 11.7242 mL | |
10 mM | 0.2345 mL | 1.1724 mL | 2.3448 mL | 5.8621 mL | |
20 mM | 0.1172 mL | 0.5862 mL | 1.1724 mL | 2.931 mL | |
50 mM | 0.0469 mL | 0.2345 mL | 0.469 mL | 1.1724 mL | |
100 mM | 0.0234 mL | 0.1172 mL | 0.2345 mL | 0.5862 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Ripisartan 148504-51-2 Endocrinology/Hormones RAAS UP 269-6 UP-2696 UP 2696 UP2696 UP-269-6 UP269-6 Inhibitor inhibitor inhibit