Cilastatin-15N-d3

Cilastatin-15N-d3 is intended for use as an internal standard for the quantification of cilastatin (Cay-23511) by GC- or LC-MS. Cilastatin is an inhibitor of dipeptidase (dehydropeptidase I), a renal dipeptidase. It inhibits human renal dipeptidase (Ki = 0.7 µM), porcine dipeptidase (IC50 = 0.11 µM), and bacterial metallo-beta-lactamase CphA from A. hydrophila (IC50 = 178 µM). Cilastatin (200 µg/ml) protects primary porcine renal proximal tubular epithelial cells from nephrotoxicity and apoptosis induced by vancomycin (Cay-15327). In a mouse model of systemic infection, cilastatin in combination with imipenem (Cay-16039) protects mice from S. aureus, E. coli, and P. aeruginosa infection. Cilastatin was designed to inhibit renal metabolism of imipenem and prolong its half-life. Formulations containing cilastatin in combination with imipenem have been used to treat susceptible bacterial infections.Formal Name: (Z)-7-((2-(amino-15N)-2-carboxyethyl-1,1,2-d3)thio)-2-((S)-2,2-dimethylcyclopropane-1-carboxamido)hept-2-enoic acid. CAS Number: 2738376-83-3. Molecular Formula: C16H23D3N[15N]O5S. Formula Weight: 362.5. Purity: >99% deuterated forms(d1-d3), =1% d0. Formulation: (Request formulation change), A solid. Solubility: DMSO: Soluble, Methanol: Soluble, Water: Soluble. SMILES: OC(C([15NH2])([2H])C([2H])([2H])SCCCC/C=C(C(O)=O)\NC([C@@H]1C(C)(C)C1)=O)=O. InChi Code: InChI=1S/C16H26N2O5S/c1-16(2)8-10(16)13(19)18-12(15(22)23)6-4-3-5-7-24-9-11(17)14(20)21/h6,10-11H,3-5,7-9,17H2,1-2H3,(H,18,19)(H,20,21)(H,22,23)/b12-6-/t10-,11+/m1/s1/i9D2,11D,17+1. InChi Key: DHSUYTOATWAVLW-MAVRWZHLSA-N.