Allopurinol riboside 是别嘌醇的代谢产物,具有抗寄生虫作用。 Allopurinol riboside 竞争性抑制嘌呤核苷磷酸化酶对肌苷的作用,Ki 为 277 μM。
产品描述
Allopurinol riboside is a metabolite of allopurinol with potency against parasites. Allopurinol riboside competitively inhibits the action of purine nucleoside phosphorylase on inosine with a Ki of 277 μM.
体外活性
Allopurinol riboside is effective against parasites including leishmaniasis and American trypanosomiasis. Allopurinol riboside is selectively toxic because it is not metabolized by the corresponding enzymes in humans[1]. Humoral immunity is not suppressed by Allopurinol riboside. Lymphocyte blastogenesis induced by PHA and Con A is significantly suppressed by Allopurinol riboside in a concentration-dependent manner[2].
体内活性
Low levels of Allopurinol riboside in plasma are attributable to incomplete absorption and rapid renal clearance. Probenecid reduces the renal clearance of allopurinol riboside, extends the half-life of allopurinol riboside in plasma, and triples the levels of allopurinol riboside in plasma[3]. Allopurinol riboside peaks in plasma 1.6 hours after administration, has an elimination half-life of 3 h, and has steady-state concentrations in the therapeutic range[4].
Cas No.
16220-07-8
分子式
C10H12N4O5
分子量
268.23
储存和溶解度
DMSO:95 mg/mL (354.17 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years