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Eprosartan

Catalog No. T2531L CAS 133040-01-4

Synonyms: KF-108566J free base, Teveten

Eprosartan (SKF-108566J free base) is a selective and competitive nonpeptide angiotensin II receptor antagonist with high affinity for AT1 receptor subtypes and can be used as an antihypertensive agent.Eprosartan has an inhibitory effect on angiotensin II receptor, with IC50 values of 9.2 nM and 3.9 nM in rat and human adrenocortical membranes, respectively. The IC50 values of Eprosartan in rat and human adrenocortical membranes were 9.2 nM and 3.9 nM, respectively.

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Eprosartan, CAS 133040-01-4

Pack Size	Availability	Price/USD
5 mg	In stock	$ 39.00
10 mg	In stock	$ 64.00
25 mg	In stock	$ 105.00
50 mg	In stock	$ 153.00
100 mg	In stock	$ 229.00
1 mL * 10 mM (in DMSO)	In stock	$ 70.00

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Purity: 100%

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Description	Eprosartan (SKF-108566J free base) is a selective and competitive nonpeptide angiotensin II receptor antagonist with high affinity for AT1 receptor subtypes and can be used as an antihypertensive agent.Eprosartan has an inhibitory effect on angiotensin II receptor, with IC50 values of 9.2 nM and 3.9 nM in rat and human adrenocortical membranes, respectively. The IC50 values of Eprosartan in rat and human adrenocortical membranes were 9.2 nM and 3.9 nM, respectively.
Targets&IC50	Mesenteric artery membranes (rat):1.5 nM, [125I] bnding to human liver membranes:1.7 nM
In vitro	Eprosartan (SKF-108566J) inhibits [125I]AII binding to human liver membranes with an IC50 of 1.7 nM and to rat mesenteric artery membranes with an IC50 of 1.5 nM. In rabbit aortic smooth muscle cells, Eprosartan causes a concentration-dependent inhibition of AII-induced increases in intracellular Ca2+ levels[1]
In vivo	In conscious normotensive rats, intravenous administration of Eprosartan (0.01-0.3 mg/kg) produced dose-dependent parallel shifts in the AII pressor dose-response curve. Intragastric or intraduodenal administration of Eprosartan (3-10 mg/kg) to conscious normotensive rats resulted in a dose-dependent inhibition of the pressor response to AII (250 ng/kg, i.v.). Significant inhibition of the pressor response to AII was observed for 3 hours at a dose of 10 mg/kg, intraduodenally[1].

Synonyms	KF-108566J free base, Teveten
Molecular Weight	424.51
Formula	C23H24N2O4S
CAS No.	133040-01-4

Storage

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

Solubility Information

DMSO: Soluble

References and Literature

1. R M Edwards, et al. Pharmacological characterization of the nonpeptide angiotensin II receptor antagonist, SK&F 108566. J Pharmacol Exp Ther. 1992 Jan;260(1):175-81. 2. Yang R, Luo Z, Liu Y, Sun M, Zheng L, Chen Y, Li Y, Wang H, Chen L, Wu M, Zhao H. Drug Interactions with Angiotensin Receptor Blockers: Role of Human Cytochromes P450. Curr Drug Metab. 2016;17(7):681-91. Review. PubMed PMID: 27216792. 3. Castilla-Guerra L, Fernandez-Moreno Mdel C. Chronic Management of Hypertension after Stroke: The Role of Ambulatory Blood Pressure Monitoring. J Stroke. 2016 Jan;18(1):31-7. doi: 10.5853/jos.2015.01102. Epub 2015 Dec 17. Review. PubMed PMID: 26687120; PubMed Central PMCID: PMC4747066. 4. Zaiken K, Hudd TR, Cheng JW. A review of the use of angiotensin receptor blockers for the prevention of cardiovascular events in patients with essential hypertension without compelling indications. Ann Pharmacother. 2013 May;47(5):686-93. doi: 10.1345/aph.1R273. Epub 2013 Apr 12. Review. PubMed PMID: 23585649.

Related compound libraries

This product is contained In the following compound libraries：

Drug Repurposing Compound Library EMA Approved Drug Library FDA-Approved & Pharmacopeia Drug Library Approved Drug Library Bioactive Compounds Library Max FDA-Approved Drug Library Bioactive Compound Library

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Keywords

Eprosartan 133040-01-4 Endocrinology/Hormones RAAS KF-108566J KF-108566J free base Teveten inhibitor inhibit

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