Cilastatin

SKU: orb1223942

Description

A renal dehydropeptidase-I and leukotriene D4 dipeptidase inhibitor. Since the antibiotic, imipenem, is hydrolyzed by dehydropeptidase-I, which resides in the brush border of the renal tubule, cilastatin is administered with imipenem to increase its effectiveness. The drug also inhibits the metabolism of leukotriene D4 to leukotriene E4.(In Vitro):Cilastatin (200 μg/mL; 24 hours; RPTECs) treatment protects against Vancomycin-induced proximal tubule apoptosis and increases cell viability, without compromising the antimicrobial effect of Vancomycin.(In Vivo):In a mouse model (female mice, strain CD-1, 20 g) of systemic infection, Imipenem plus Cilastatin can protect mice from S. aureus, E. coli, and P. aeruginosa infection.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 82009-34-5
• MW: 358.45
• Purity: >98% (HPLC)
• Formula: C₁₆H₂₆N₂O₅S
• SMILES: CC1(C[C@H]1C(=O)N/C(=C\CCCCSC[C@H](C(=O)O)N)/C(=O)O)C
• Target: Proteasome
• Solubility: DMSO: 10 mM

Bioactivity

• In Vivo:
  In a mouse model (female mice, strain CD-1, 20 g) of systemic infection, Imipenem plus Cilastatin can protect mice from S. aureus, E. coli, and P. aeruginosa infection.
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• In Vitro:
  Cilastatin (200 μg/mL; 24 hours; RPTECs) treatment protects against Vancomycin-induced proximal tubule apoptosis and increases cell viability, without compromising the antimicrobial effect of Vancomycin. Apoptosis Analysis Cell line: Renal proximal tubular epithelial cells (RPTECs). Concentration: 200 μg/mL. Incubation time: 24 hours. Result: Significantly ameliorated Vancomycin-induced nuclear apoptosis.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

Proteasome