Cilastatin-15N,d3

Modify Date: 2022-09-02 12:08:50

Cilastatin-15N,d3 Structure
Cilastatin-15N,d3 structure
Common Name Cilastatin-15N,d3
CAS Number 2738376-83-3 Molecular Weight 362.46
Density N/A Boiling Point N/A
Molecular Formula C16H23D3N15NO5S Melting Point N/A
MSDS N/A Flash Point N/A

 Use of Cilastatin-15N,d3


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].

 Names

Name Cilastatin-15N,d3

 Cilastatin-15N,d3 Biological Activity

Description 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].
Related Catalog
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].
References

[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.

 Chemical & Physical Properties

Molecular Formula C16H23D3N15NO5S
Molecular Weight 362.46