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Ripisartan

Ripisartan

产品编号 T28540   CAS 148504-51-2
别名: UP 269-6, UP-2696, UP 2696, UP-269-6, UP269-6

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。

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Ripisartan Chemical Structure
Ripisartan, CAS 148504-51-2
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
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产品目录号及名称: Ripisartan (T28540)
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纯度: 98.24%
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参考文献
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

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 55 mg/mL (128.97 mM)

溶液配制表

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

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TargetMol Library Books参考文献

1. Cazes M, et al. In vivo pharmacological characterization of UP 269-6, a novel nonpeptide angiotensin II receptor antagonist. Eur J Pharmacol. 1995;284(1-2):157-170. 2. Virone-Oddos A, et al. In vitro and in vivo effects of UP 269-6, a new potent orally active nonpeptide angiotensin II receptor antagonist, on vascular smooth muscle cell proliferation. Br J Pharmacol. 1997;120(3):488-494. 3. McIntyre M, et al. Comparison of the oral angiotensin II receptor antagonist UP 269-6 or enalapril 20 mg on blood pressure and neurohormonal effects in salt-deplete man. J Cardiovasc Pharmacol. 1995;25(6):994-1000. 4. Caussade F, et al. In vitro pharmacological characterization of UP 269-6, a novel nonpeptide angiotensin II receptor antagonist. Fundam Clin Pharmacol. 1995;9(2):119-128.
DX600 TFA Candesartan Cilexetil Plantainoside D YS-49 ANGIOTENSIN IV TFA(12676-15-2(free base)) Valsartan Methyl Ester Fimasartan Aliskiren D6 hemifumarate

相关化合物库

该产品包含在如下化合物库中:
膜蛋白靶向化合物库 已知活性化合物库 经典已知活性库

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Keywords

Ripisartan 148504-51-2 Endocrinology/Hormones RAAS UP 269-6 UP-2696 UP 2696 UP2696 UP-269-6 UP269-6 Inhibitor inhibitor inhibit

 

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