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|
GC7 Sulfate is a deoxyhypusine synthase (DHPS) inhibitor.
|Pyridostatin Trifluoroacetate Salt
Pyridostatin Trifluoroacetate Salt is a G-quadruplexe stabilizer, with a Kd of 490 nM.
Chebulinic acid is a potent natural inhibitor of M. tuberculosis DNA gyrase, also can inhibit SMAD-3 phosphorylation, inhibit H+ K+-ATPase activity.
TAS-102 is an orally administered combination of a thymidine-based nucleic acid analogue, trifluridine, and a thymidine phosphorylase inhibitor, tipiracil hydrochloride.
6-Thio-2′-deoxyguanosine (6-thio-dG) is a nucleoside analog and telomerase substrate that is incorporated into de novo–synthesized telomeres.
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