500794-88-7
中文名稱(chēng)
500794-88-7
英文名稱(chēng)
TR antagonist 1
CAS
500794-88-7
分子式
C25H23Br2NO4
分子量
561.26
MOL 文件
500794-88-7.mol
500794-88-7 結(jié)構(gòu)式
基本信息
中文別名
化合物 T13435 英文別名
TR antagonist 1Benzenepropanoic acid, 3,5-dibromo-4-[4-hydroxy-3-(1-methylethyl)-5-[(1E)-2-(4-pyridinyl)ethenyl]phenoxy]-
物理化學(xué)性質(zhì)
沸點(diǎn)636.5±55.0 °C(Predicted)
密度1.553±0.06 g/cm3(Predicted)
儲(chǔ)存條件4°C, protect from light
溶解度DMSO : ≥ 83.3 mg/mL (148.42 mM)
酸度系數(shù)(pKa)4.51±0.10(Predicted)
形態(tài)Solid
顏色Light yellow to yellow
常見(jiàn)問(wèn)題列表
生物活性
TR antagonist 1是高親和力的甲狀腺激素受體 (thyroid hormone receptor (TR)) 拮抗劑，對(duì) TRα 和 TRβ 的IC50 值分別為 36 和 22 nM。靶點(diǎn)
IC50: 36 nM (Thyroid hormone α), 22 nM (Thyroid hormone α)
體外研究
TR antagonist 1 displays high affinity for both thyroid hormone TRα and TRβ (IC 50 =36 and 22 nM, respectively). TR antagonist 1 acts as a full antagonist in the TRAFR cell assay and the IC 50 32 nM for both TRAFα1 and TRAFβ1.
體內(nèi)研究
TR antagonist 1 treatment lowers heart rate and shows a possible trend toward an increase of low-density lipoprotein cholesterol (LDL-C) in the cholesterol fed rat model.