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Diclofenac acyl glucuronide

Cat. No. M30413
Diclofenac acyl glucuronide Structure
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Biological Activity

Diclofenac acyl glucuronide (D-1-O-G) is a major bile metabolite directly involved in small intestinal ulceration in rats.

Chemical Information
Molecular Weight 472.27
Formula C20H19Cl2NO8
CAS Number 64118-81-6
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Conversion of different model animals based on BSA (PMID: 27057123)
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.

References

[1] Xiaokui Huo, et al. Br J Pharmacol. Protective effect of cilastatin against diclofenac-induced nephrotoxicity through interaction with diclofenac acyl glucuronide via organic anion transporters

[2] Atsushi Kawase, et al. Toxicol Mech Methods. Involvement of diclofenac acyl-β-d-glucuronide in diclofenac-induced cytotoxicity in glutathione-depleted isolated murine hepatocytes co-cultured with peritoneal macrophages

[3] Shingo Oda, et al. J Appl Toxicol. Toxicological role of an acyl glucuronide metabolite in diclofenac-induced acute liver injury in mice

[4] S Seitz, et al. Gastroenterology. Diclofenac acyl glucuronide, a major biliary metabolite, is directly involved in small intestinal injury in rats

[5] A Kretz-Rommel, et al. Toxicol Appl Pharmacol. Diclofenac covalent protein binding is dependent on acyl glucuronide formation and is inversely related to P450-mediated acute cell injury in cultured rat hepatocytes

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