WAY-204688 是一种选择性和口服活性的雌激素受体抑制剂,抑制 NF-Κb 转录活性(在 HAECT-1 细胞中 IC50 = 122 nM)。
产品描述
WAY-204688 is a selective and orally active estrogen receptor inhibitor of NF-κB transcriptional activity (IC50 = 122 nM in HAECT-1 cells).
体外活性
WAY-204688 displaces [3H]E2 from the ERα ligand-binding domain protein (C50=2.43 μM) and from the ERβ ligand-binding domain protein (IC50=1.5 μM)[1].
体内活性
WAY-204688 (5 mg/kg per day, p.o.) inhibits pro-inflammatory genes including MHI, VCAM-1, RANTES, and TNF-α and induces the gene products and uterine wet weight. WAY-204688 (0.3 mg/kg, p.o.) is active in the Lewis rat adjuvant-induced arthritis model [1].
Cas No.
796854-35-8
分子式
C34H31F3N2O2
分子量
556.62
别名
SIM688
储存和溶解度
DMSO:90 mg/mL (161.7 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years