Cilastatin-¹⁵N,d₃  (Synonyms: 西司他丁-¹⁵N,d₃; MK0791-¹⁵N,d₃)

Cilastatin-¹⁵N,d₃ is a ¹⁵N-labeled and deuterium labeled Cilastatin. 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].

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

362.46

C₁₆H₂₃D₃N¹⁵NO₅S

2738376-83-3

固体

White to off-white

西司他丁-¹⁵N,d₃

Room temperature in continental US; may vary elsewhere.

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

  [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.  [Content Brief]

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

  [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.  [Content Brief]