Cilastatin-15N,d3(Synonyms: MK0791-15N,d3)

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Cilastatin-15N,d3 (Synonyms: MK0791-15N,d3)

Cilastatin-15N,d3 是一种 15N 标记和氘代标记的 Cilastatin。Cilastatin (MK0791) 是一种可逆的竞争性的肾脏脱氢肽酶 I (renal dehydropeptidase I) 抑制剂,IC50 为 0.1 μM。Cilastatin 抑制细菌金属叶内酰胺酶 CphAIC50 为 178 μM。Cilastatin 可用作抗菌辅助剂。

Cilastatin-15N,d3(Synonyms: MK0791-15N,d3)

Cilastatin-15N,d3 Chemical Structure

CAS No. : 2738376-83-3

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生物活性

Cilastatin-15N,d3 is a 15N-labeled and deuterium labeled Cilastatin (MK0791) is a reversible, competitive renal dehydropeptidase I inhibitor with an IC50 of 0.1 μM. Cilastatin inhibits the bacterial metallob-lactamase enzyme CphA with an IC50 of 178 μM. Cilastatin is an antibacterial adjunct[1][2][3].

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[5].

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

分子量

362.46

Formula

C16H23D3N15NO5S

CAS 号

2738376-83-3

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]. The renal membrane dipeptidase (dehydropeptidase I) inhibitor, cilastatin, inhibits the bacterialmetallo-beta-lactamase enzyme CphA. Antimicrob Agents Chemother. 1995 Jul;39(7):1629-31.

    [3]. Blanca Humanes, et al. Protective Effects of Cilastatin Against Vancomycin-Induced Nephrotoxicity. Biomed Res Int. 2015;2015:704382.

    [4]. P J Petersen, et al. In Vitro and in Vivo Activities of LJC10,627, a New Carbapenem With Stability to Dehydropeptidase I. Antimicrob Agents Chemother. 1991 Jan;35(1):203-7.

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