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CAS No.: 144143-96-4

Eprosartan mesylate/依普罗沙坦甲磺酸盐 Catalog No. CSN10923

Synonyms: SKF-108566J;Eprosartan (mesylate);Eprosartan Mesylate

Eprosartan Mesylate is a reversible and competitive angiotensin II receptor inhibitor.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 Angiotensin Receptor

IC50:3.9nM Angiotensin Receptor (rat)

IC50:9.2nM
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 ... more >> 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 Collapse <<
NCT02024100	-	-	Unknown	December 2016	Korea, Republic of ... more >> 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 Collapse <<
NCT01753206	-	-	Completed	-	Korea, Republic of ... more >> Seoul National University Bundang Hospital Seongnam-si, Bundang-gu, Korea, Republic of, 463-717 Collapse <<

更多
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

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.9208 mL
- 9.6040 mL
- 19.2079 mL
- 5 mM
- 0.3842 mL
- 1.9208 mL
- 3.8416 mL
- 10 mM
- 0.1921 mL
- 0.9604 mL
- 1.9208 mL

技术信息

CAS号

144143-96-4

储存条件

粉末: Sealed in dry,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C24H28N2O7S2

运输

蓝冰

分子量

520.62

别名

SKF-108566J;Eprosartan (mesylate);Eprosartan Mesylate;Teveten;Futuran;Navixen;Regulaten;SK and F 108566;SKF-108566

溶解度

DMSO	104.0 mg/mL (199.8 mM)
Water	Insoluble
Ethanol	4.0 mg/mL (7.7 mM)

动物实验配方

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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 ... more >> 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 Collapse <<
NCT02024100	-	-	Unknown	December 2016	Korea, Republic of ... more >> 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 Collapse <<
NCT01753206	-	-	Completed	-	Korea, Republic of ... more >> Seoul National University Bundang Hospital Seongnam-si, Bundang-gu, Korea, Republic of, 463-717 Collapse <<
NCT01087749	Kidney Disease	Phase 1	Completed	-	United States, California ... more >> Clinical Reserach Center, UCSF San Francisco,, California, United States, 94143 Collapse <<
NCT01631227	-	-	Completed	-	-
NCT01631227	Essential Hypertension	Phase 3	Completed	-	Germany ... more >> Site Reference ID/Investigator# 74062 Berlin, Germany, 12627 Site Reference ID/Investigator# 74066 Bochum, Germany, 44787 Site Reference ID/Investigator# 74065 Dresden, Germany, 01067 Site Reference ID/Investigator# 93513 Dresden, Germany, 01307 Site Reference ID/Investigator# 93495 Essen, Germany, 45355 Site Reference ID/Investigator# 93515 Frankfurt, Germany, 60594 Site Reference ID/Investigator# 74060 Frankfurt, Germany, 60596 Site Reference ID/Investigator# 74063 Goerlitz, Germany, 02826 Site Reference ID/Investigator# 93494 Hamburg, Germany, 22143 Site Reference ID/Investigator# 93493 Karlsruhe, Germany, 76199 Site Reference ID/Investigator# 74061 Leipzig, Germany, 04103 Site Reference ID/Investigator# 74064 Magdeburg, Germany, 39104 Site Reference ID/Investigator# 93514 Nuremberg, Germany, 90402 Russian Federation Site reference ID/Investigator # 82515 Barnaul, Russian Federation, 656055 Site reference ID/Investigator # 82520 Kazan, Russian Federation, 420012 Site reference ID/Investigator # 82493 Kemerovo, Russian Federation, 650002 Site reference ID/Investigator # 82516 Kemerovo, Russian Federation, 650055 Site refernce ID/Investigator # 82521 Krasnodar, Russian Federation, 350086 Site reference ID/Investigator # 82495 Novosibirsk, Russian Federation, 630008 Site reference ID/Investigator # 82494 Novosibirsk, Russian Federation, 630047 Site reference ID/Investigator # 82525 Novosibirsk, Russian Federation, 630068 Site reference ID/Investigator # 82522 St. Petersburg, Russian Federation, 192283 Site reference ID/Investigator # 82517 St. Petersburg, Russian Federation, 194044 Site reference ID/Investigator # 82524 St. Petersburg, Russian Federation, 197022 Site reference ID/Investiragor # 82523 St. Petersburg, Russian Federation, 197022 Site reference ID/Investigator # 82519 St. Petersburg, Russian Federation, 198205 Site reference ID/Investigator # 82518 St. Petersburg, Russian Federation, 198260 Site reference ID/Investigator # 82527 St. Petersburg, Russian Federation, 199106 United Kingdom Site Reference ID/Investigator# 74057 Birmingham, United Kingdom, B15 2SQ Site Reference ID/Investigator# 74059 Cardiff, United Kingdom, CF14 5GJ Site Reference ID/Investigator# 74056 Chorley, United Kingdom, PR7 7NA Site Reference ID/Investigator# 74054 Glasgow, United Kingdom, G20 0SP Site reference ID/Investigator # 95456 Glasgow, United Kingdom, G45 9AW Site Reference ID/Investigator# 74053 Liverpool, United Kingdom, L22 0LG Site reference ID/Investigator # 95457 London, United Kingdom, EC1M 6BQ Site Reference ID/Investigator# 74055 Manchester, United Kingdom, M16 6SX Site reference ID/Investigator # 95455 Northwood, United Kingdom, HA6 2RN Site Reference ID/Investigator# 74058 Reading, United Kingdom, RG2 0TG Collapse <<

靶点	Description	IC50
Angiotensin Receptor		IC50:3.9nM
Angiotensin Receptor (rat)		IC50:9.2nM

Eprosartan mesylate/依普罗沙坦甲磺酸盐 Catalog No. CSN10923

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