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Cilastatin

Cat. No. M6090
Cilastatin Structure
Synonym:

MK0791

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mM*1mL in DMSO USD 45  USD45 In stock
10mg USD 55  USD55 In stock
50mg USD 95  USD95 In stock
100mg USD 150  USD150 In stock
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Quality Control
Biological Activity

Cilastatin attenuates VAN-induced acute renal failure in vitro by decreasing apoptosis without affecting antibacterial activity. This effect could be related, at least in part, to the reduction in accumulation of the drug in cells. Therefore, cilastatin could represent a novel therapeutic approach in reducing VAN-induced renal damage without compromising bactericidal efficacy.

Protocol
Cell Experiment
Cell lines Proximal Tubular Primary Cell
Preparation method Cells were pretreated with VAN (0.6, 3, and 6 mg/mL) alone or in combination with cilastatin (200 μg/mL) before being trypsinized, washed twice with PBS, and incubated for 30 min in the dark in 100 μL buffer containing 5 μL fluorescein isothiocyanate- (FITC-) labeled annexin V and 5 μL PI for flow cytometry.
Concentrations 200 μg/mL
Incubation time 24 h
Animal Experiment
Animal models
Formulation
Dosages
Administration
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 358.45
Formula C16H26N2O5S
CAS Number 82009-34-5
Purity 99.71%
Solubility DMSO ≥ 35 mg/mL
Storage at -20°C
References

[1] Humanes B, et al. Biomed Res Int. Protective Effects of Cilastatin against Vancomycin-Induced Nephrotoxicity.

[2] Ramirez J, et al. Antimicrob Agents Chemother. Randomized phase 2 trial to evaluate the clinical efficacy of two high-dosage tigecycline regimens versus imipenem-cilastatin for treatment of hospital-acquired pneumonia.

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