Mercaptopurine is widely used to treat malignancies, rheumatic diseases, dermatologic conditions, inflammatory bowel disease, and solid organ transplant rejection. Mercaptopurine inhibits purine nucleotide synthesis and metabolism by inhibiting an enzyme called Phosphoribosyl pyrophosphate amidotransferase (PRPP Amidotransferase). PRPP Amidotransferase is the rate limiting enzyme of purine synthesis. It alters the synthesis and function of RNA and DNA. Mercaptopurine interferes with nucleotide interconversion and glycoprotein synthesis.
|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||100 mg/mL in DMSO|
Improving the dissolution and bioavailability of 6-mercaptopurine via co-crystallization with isonicotinamide.
Wang JR, et al. Bioorg Med Chem Lett. 2015 Mar 1;25(5):1036-9. PMID: 25630224.
|Related DNA/RNA Synthesis Products|
Vidarabine is an antiviral drug by interfering with the synthesis of viral DNA, used to treat herpes simplex and varicella zoster viruses.
Uridine is a nucleoside, contains a uracil attached to a ribose ring via a β-N1-glycosidic bond.
Rifampin is a DNA-dependent RNA polymerase inhibitor, used to treat a number of bacterial infections.
Mitomycin C is an antineoplastic antibiotic by inhibiting DNA synthesis, used to treat different cancers.
Mercaptopurine is a widely used antileukemic agent and immunosuppressive drug that inhibits de novo purine synthesis through incorporation of thiopurine methyltransferase metabolites into DNA and RNA.
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