"目录号: HY-13677
Cell Cycle/DNA DamageAutophagy-
Mercaptopurine (6-mercaptopurine; 6-MP)是免疫抑制剂。
Nucleoside Antimetabolite/AnalogAutophagy
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生物活性
Description
Mercaptopurine (6-mercaptopurine; 6-MP) is an immunosuppressive drug; is a thiopurine.IC50 Value: 149.5±124.9 nM (PBMC blastogenesis) [1]Target: Nucleoside antimetabolitein vitro: Both AZ and 6-MP dose-dependently suppressed PBMC blastogenesis. Mean +/- s.d. IC50 (concentration of drug that gave 50% inhibition) values for AZ and 6-MP were 230.4 +/- 231.3 and 149.5 +/- 124.9 nM, respectively [1]. After incubation of PBMCs with 100 microM AZ for 4 days, 35.3-92.5 microM 6-MP was liberated into the culture medium. in vivo: The conversion of 6-mercaptopurine to 6-thiouric acid was prevented when allopurinol or oxypurinol were added to the lumen. At a luminal drug concentration of 1 mmol/l, allopurinol increased the rate at which 6-mercaptopurine appeared in the serosal secretions by 90% compared with an increase of only 50% with oxypurinol [2]. Combined treatment with 150 R X-rays and 150 mg/kg 6-mercaptopurine gave an additive effect and demonstrated conclusively that the peak incidence of dead implants observed at 30.5 - 35.5 days can be attributed to cells treated [3].Clinical trial: Comparative Pharmacokinetics of a Compounded 6-mercaptopurine Liquid Formulation Preparation and Tablets. Phase not specified
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