CILASTATIN SODIUM
Cilastatin sodium inhibits renal dehydropeptidase‑I, preventing imipenem degradation and improving its antibacterial activity. Side effects include nausea, rash, and rare seizures.
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Product Description
Mechanism of Action
Cilastatin sodium is a dehydropeptidase‑I (DHP‑1) inhibitor that prevents renal breakdown of imipenem. It binds the active site of DHP‑1 on proximal tubular brush‑border membranes, blocking enzymatic hydrolysis of the β‑lactam ring. This increases imipenem half‑life and prevents formation of nephrotoxic metabolites.
Benefits and Advantages
Used in β‑lactam stability research, renal‑enzyme inhibition studies, PK/PD modelling of carbapenems, combination‑therapy optimisation and nephrotoxicity‑prevention research. Essential in studying kidney enzyme–drug interactions.
Side Effects and Risks
Risks include GI upset, headache, hepatic enzyme elevation and rare hypersensitivity reactions. Handle with enzyme‑inhibitor precautions.
Datasheet
| Molecular Formula | C16H23N2NaO5S |
|---|---|
| Molecular Weight | 380.4 g/mol |
| CAS Number | 81129-83-1 |
| Storage Condition | Store in a cool, dry place. Keep container tightly closed. Protect from moisture and light. |
| Solubility | 1.00e-01 g/L |
| Purity | Purity information is available upon request (COA). |
| Synonym | Cilastatin sodium; 81129-83-1; Cilastatin sodium salt; DTXSID2046915; DTXCID0026915 |
| IUPAC/Chemical Name | sodium (Z)-7-[(2R)-2-amino-2-carboxyethyl]sulfanyl-2-[[(1S)-2,2-dimethylcyclopropanecarbonyl]amino]hept-2-enoate |
| InChl Key | QXPBTTUOVWMPJN-QBNHLFMHSA-M |
| InChl Code | InChI=1S/C16H26N2O5S.Na/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);/q;+1/p-1/b12-6-;/t10-,11+;/m1./s1 |
| References | PubChem; ChemBL; FDA; |
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