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N-desmethyl Enzalutamide(N-desmethyl MDV 3100)
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
N-desmethyl Enzalutamide(N-desmethyl MDV 3100)图片
CAS NO:1242137-16-1
包装与价格：
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
N-desmethyl Enzalutamide (N-desmethyl MDV 3100) 是 Enzalutamide 的活性代谢物。N-desmethyl Enzalutamide (N-desmethyl MDV 3100) 是 Enzalutamide 的活性代谢物。 N-desmethyl Enzalutamide (N-desmethyl MDV 3100) 表现出与 Enzalutamide 相似效力的主要和次要药效学，并在与 enzalutamide 大致相同的血浆浓度下循环。
Cas No.1242137-16-1
别名4-[3-[4-氰基-3-(三氟甲基)苯基]-5,5-二甲基-4-氧代-2-硫代-1-咪唑烷基]-2-氟苯甲酰胺,N-desmethyl MDV 3100
Canonical SMILESS=C(N1C2=CC(F)=C(C(N)=O)C=C2)N(C3=CC=C(C(C(F)(F)F)=C3)C#N)C(C(C)1C)=O
分子式C20H14F4N4O2S
分子量450.41
溶解度DMSO : ≥ 48 mg/mL (106.57 mM)
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

N-desmethyl Enzalutamide is the active metabolite of Enzalutamide. Enzalutamide is an androgen-receptor (AR) antagonist with IC50 of 36 nM in LNCaP cells.

N-desmethyl Enzalutamide is an active metabolite that is thought to contribute to the clinical effects of Enzalutamide because it demonstrates primary and secondary pharmacodynamics of similar potency to Enzalutamide and circulates at approximately the same plasma concentrations as Enzalutamide. The carboxylic acid metabolite is pharmacologically inactive and circulates at approximately 25 % lower plasma concentrations than Enzalutamide[1].

[1]. Gibbons JA, et al. Pharmacokinetic Drug Interaction Studies with Enzalutamide. Clin Pharmacokinet. 2015 Oct;54(10):1057-69.