ACP-105 是选择性的、可口服的雄激素受体调节剂 , 能够作用于野生型 AR (pEC50:9.0)和 T877A 突变型 AR (pEC50:9.3)。
产品描述
ACP-105 is a novel and potent nonsteroidal selective androgen receptor modulator (SARM) with partial agonist activity relative to the natural androgen testosterone.
体外活性
ACP-105 is an orally available, selective amd potent androgen receptor modulator (SARM), with pEC50s of 9.0 and 9.3 for AR wild type and T877A mutant, respectively. The half-lives of ACP-105 (compound 1) in human hepatocytes is measured and found to be 5.0 h[1].
体内活性
Irradiation impaired sensorimotor function in vehicle-treated mice but not in ACP-105-treated mice. Irradiation impaired cued fear conditioning and ACP-105 enhanced fear conditioning in sham-irradiated and irradiated mice. There are relatively early radiation-induced behavioral changes in female mice and reduced MAP-2 levels in the sensorimotor cortex following ACP-105 treatment might contribute to enhanced rotorod performance[2].
Cas No.
899821-23-9
分子式
C16H19ClN2O
分子量
290.79
储存和溶解度
DMSO:60 mg/mL (206.33 mM)
Ethanol:60 mg/mL(206.33 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years