Telmisartan-13C,d3(Synonyms: BIBR 277-13C,d3)

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Telmisartan-13C,d3 (Synonyms: BIBR 277-13C,d3)

Telmisartan-13C,d3 是一种 13C- 和氘代标记的 Telmisartan。Telmisartan 是一种有效的血管紧张素II 1型受体 (angiotensin II type 1 receptor) 拮抗剂，能够抑制其活性，IC50 值为 9.2 nM。

Telmisartan-13C,d3(Synonyms: BIBR 277-13C,d3)

Telmisartan-13C,d3 Chemical Structure

CAS No. : 1261396-33-1

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生物活性

Telmisartan-13C,d3 is the 13C- and deuterium labeled. Telmisartan is a potent, long lasting antagonist of angiotensin II type 1 receptor (AT1), selectively inhibiting the binding of 125I-AngII to AT1 receptors with IC50 of 9.2 nM.

体外研究
(In Vitro)

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[55].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

518.63

Formula

C3213CH27D3N4O2
CAS 号

1261396-33-1
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-223.

    [2]. Maillard MP, et al. In vitro and in vivo characterization of the activity of telmisartan: an insurmountable angiotensin II receptor antagonist. J Pharmacol Exp Ther. 2002 Sep;302(3):1089-95.

    [3]. Xuan H, et al. Inhibition or deletion of angiotensin II type 1 receptor suppresses elastase-induced experimental abdominal aortic aneurysms. J Vasc Surg. 2017 Apr 20. pii: S0741-5214(17)30100-3.

    [4]. Torika N, et al. Intranasal telmisartan ameliorates brain pathology in five familial Alzheimer’s disease mice. Brain Behav Immun. 2017 Apr 3.

    [5]. Aswar U, et al. Telmisartan attenuates diabetes induced depression in rats. Pharmacol Rep. 2017 Apr;69(2):358-364.

    [6]. Fujihara S, et al. The angiotensin II type 1 receptor antagonist telmisartan inhibits cell proliferation and tumor growth of esophageal adenocarcinoma via the AMPKα/mTOR pathway in vitro and in vivo. Oncotarget. 2017 Jan 31;8(5):8536-8549.

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