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.
|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.|
|Incubation time||24 h|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.
|Solubility||10 mM in DMSO|
Protective Effects of Cilastatin against Vancomycin-Induced Nephrotoxicity.
Humanes B, et al. Biomed Res Int. 2015;2015:704382. PMID: 26504822.
Randomized phase 2 trial to evaluate the clinical efficacy of two high-dosage tigecycline regimens versus imipenem-cilastatin for treatment of hospital-acquired pneumonia.
Ramirez J, et al. Antimicrob Agents Chemother. 2013 Apr;57(4):1756-62. PMID: 23357775.
Corn oil, extracted from the germ of corn, can be used as a carrier for drug molecules and has anti-tumor activity.
Palosuran, also known as ACT-058362, is a Urotensin-II receptor antagonist with an IC50 of 3.6±0.2 nM.
Dithiothreitol (DTT) is the common name for a small-molecule redox reagent known as Cleland's reagent; as a reducing or "deprotecting" agent for thiolated DNA.
SAR7334 is a novel, highly potent and bioavailable inhibitor of TRPC6 channels.
FICZ is a potent aryl hydrogen receptor (AhR) agonist.
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