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BMS-564929
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。
BMS-564929图片
CAS NO:627530-84-1
包装:50 mg
市场价:11672元

产品介绍

产品描述

BMS-564929 is an agonist of androgen receptor (AR, Ki of 2.11±0.16 nM).

体外活性

BMS-564929 is more than 1000-fold selective for AR vs. estrogen receptors (ER) α and β, glucocorticoid receptor (GR), and mineralocorticoid receptor (MR), and approximately 400-fold selective vs. BMS-564929 shows no measurable activity in functional transactivation assays with ERα/β, GR, MR, or PR at concentrations up to 30 μM[1]. BMS-564929 exhibits a potency (EC50, calculated as the concentration at which 50% of the maximum stimulatory effect of DHT is achieved) of 0.44±0.03 nM in the C2C12 myoblast cell line. In the PEC cell line, the EC50 for BMS-564929 is 8.66±0.22 nM. progesterone receptor (PR).

体内活性

BMS-564929 is more than 200 times more potent in stimulation of muscle and 80 times more selective for muscle vs. prostate, compared with T propionate (TP) in the same model[1]. BMS-564929 (p.o.) shows substantially more potent activity in the levator ani, exhibiting an ED50 of 0.0009 mg/kg in the levator ani and an ED50 of 0.14 mg/kg in the prostate; a net 160-fold selectivity for muscle vs. prostate, in sexually mature, castrated male rats, a well-characterized animal model. Approximately 100% muscle stimulation is achieved at 0.1 mg/kg, reaching greater than 125% stimulation at 0.3 and 1 mg/kg.

Cas No.

627530-84-1

分子式

C14H12ClN3O3

分子量

305.72

储存和溶解度

DMSO:50 mg/mL (163.55 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years