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CGP-53153  

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包装规格：1mg in glass bottle
产品描述：基本信息 产品编号： C11224 产品名称： CGP-53153 CAS: 149281-19-6   储存条件 粉末 -20℃ 四年     分子式： C23H33N3O2 溶于液体     分子量 383.53     化学名：  (1S,3aS,3bS,5aR,9aR,9bS,11aS)-N-(2-cyanopropan-2-yl)-9a,11a-dimethyl-7-oxo-1,2,3,3a,3b,4,5,5a,6,9b,10,11-dodecahydroindeno[5,4-f]quinoline-1-carboxamide   生物活性 产品描述 一种甾体类的5alphareductase抑制剂，在大鼠和人前列腺组织中的IC50值分别为36nM。 靶点 IC50: 36nM (rat 5 alpha reductase), 262nM (human 5 alpha reductase) 体外研究 CGP-53153 competitively inhibits rat microsomal 5 alpha reductase from prostate with an IC50 of 36nM compared to the reference compound finasteride (IC50=11nM). CGP 53153 is approximately one order of magnitude more potent in inhibiting rat compared to human 5 alpha reductase, with IC50 values of 36 and 262nM, respectively 体内研究 CGP-53153 can significantly reduce T-propionate-mediated prostate growth at oral doses of 0.01mg/kg. CGP-53153 significantly reduces prostate weight at 3 and 10mg/kg by 31% and 37%, respectively. Treatment for 12 weeks with both CGP-53153 reduces prostate volume by more than 70% in individual dogs. Neither body weight nor the weight of any organ tested is affected by CGP-53153   推荐实验方法(仅供参考) Animal Administration Rats: Adult male rats weighing 160-180 g at the start of the study are treated orally once daily for 14 consecutive days either with increasing doses of CGP-53153 (1, 3 and 10mg/kg) or with 10mg/kg finasteride in 20% HCD. Control rats are given 20% HCD. On the 14th treatment day, 4 h after the last application, the animals are randomized and rapidly killed. Trunk blood is collected in polystyrene tubes and serum obtained by centrifugation is stored at -20°C for hormone (T, DHT and rat-LH) determination at a later date. After decapitation, the following organs are excised and weighed after removal of adhering fat and connective tissue: ventral prostate, seminal vesicles, levator ani and bulbocavernosus muscle, testes, pituitary, adrenals, thyroid, thymus and liver
保存条件：-20℃

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