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Eprosartan mesylate

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Chemical Structure| 144143-96-4 同义名 : SKF-108566J;Eprosartan (mesylate);SKF-108566;SK and F 108566;Regulaten;Navixen;Futuran;Teveten
CAS号 : 144143-96-4
货号 : A217175
分子式 : C24H28N2O7S2
纯度 : 99%
分子量 : 520.618
MDL号 : MFCD08141807
存储条件：

粉末 Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(96.04 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • AT1 receptor

    AT1 receptor, Kd:0.83 nM
描述 Angiotensin receptor is a G protein coupled receptor with angiotensin as ligand, which can trigger various signal cascades after being activated. Eprosartan mesylate (SKF-108566J) is a nonpeptide angiotensin receptor antagonist[3]. In rat and human adrenal cortical membranes, rat mesenteric artery membranes and human liver membranes, Eprosartan Mesylate specifically displaced angiotensin receptor ligand, [125I] angiotensin II (AII), with IC50 of 9.2, 3.9, 1.5 and 1.7 nM, respectively[3]. In rabbit aortic smooth muscle cells, Eprosartan Mesylate caused a concentration-dependent inhibition of AII-induced increases in intracellular Ca2+ levels[3]. In vivo assay, administration of Eprosartan mesylate (3-10 mg/kg) intraduodenally or intragastrically to conscious normotensive rats resulted in a dose-dependent inhibition of the pressor response to AII (250 ng/kg, i.v.). At 10 mg/kg, i.d., significant inhibition of the pressor response to AII was observed for 3 hr[3].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT01715584 Hypertension Phase 4 Recruiting December 31, 2019 Canada, Ontario ... 展开 >> London Health Sciences Centre - Victoria Campus Recruiting London, Ontario, Canada, N6A 5W9 Contact: Craig J Railton, MD, PhD    519 685 8500 ext 58525    Craig.Railton@lhsc.on.ca    Principal Investigator: Craig J Railton, MD, PhD          Sub-Investigator: Jonathan Fairbairn, BSc          Sub-Investigator: George Nicoloau, MD          Sub-Investigator: Robert Gros, PhD          Sub-Investigator: Jason Franklin, MD          Sub-Investigator: John Yoo, MD          Sub-Investigator: Kevin Fung, MD          Sub-Investigator: Anthony Nichols, MD          Sub-Investigator: Danielle McNeil, MD 收起 <<
NCT02024100 - Unknown December 2016 Korea, Republic of ... 展开 >> Seoul National University Bundang Hospital Recruiting Seongnam-si, Bundang-gu, Korea, Republic of, 463-717 Contact: Chang Hwan Yoon, MD          Principal Investigator: Chang Hwan Yoon, MD 收起 <<
NCT01753206 - Completed - Korea, Republic of ... 展开 >> Seoul National University Bundang Hospital Seongnam-si, Bundang-gu, Korea, Republic of, 463-717 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.92mL

0.38mL

0.19mL

9.60mL

1.92mL

0.96mL

19.21mL

3.84mL

1.92mL
参考文献

[1]Plosker GL, Foster RH. Eprosartan: a review of its use in the management of hypertension. Drugs. 2000 Jul;60(1):177-201.

[2]Ohlstein EH, Brooks DP, et al. Inhibition of sympathetic outflow by the angiotensin II receptor antagonist, eprosartan, but not by losartan, valsartan or irbesartan: relationship to differences in prejunctional angiotensin II receptor blockade. Pharmacology. 1997 Nov;55(5):244-51.

[3]Edwards RM, Aiyar N, et al. Pharmacological characterization of the nonpeptide angiotensin II receptor antagonist, SK&F 108566. J Pharmacol Exp Ther. 1992 Jan;260(1):175-81