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MK-0773

CAS No. : 606101-58-0

MCE 国际站：MK-0773

产品活性：MK-0773 是一种选择性雄激素受体调节剂 (selective androgen receptor modulators)，与 AR 结合，IC₅₀ 值为 6.6 nM。

研究领域：Vitamin D Related/Nuclear Receptor

作用靶点：Androgen Receptor

In Vitro: The IC₅₀ of MK-0773 binding to AR is increased 3.5-fold in the presence of 25% rat serum and 13-fold in the presence of 25% human serum, indicating that it binds to serum proteins. The affinity of MK-0773 for AR across species is evaluated using COS cells transfected with AR, and IC₅₀ values are very similar in four species (rat, 0.50 nM; dog, 0.55 nM; rhesus, 0.45 nM; human, 0.65 nM).

In Vivo: MK-0773 (6 and 80 mg/kg, s.c.) produces exposure-related stimulatory effects on cortical BFR and LBM in the OVX rat model. MK-0773 (5, 15, and 80 mg/kg, s.c.) increases seminal vesicle weights, and has reduced effects on the prostate. The partial agonism and tissue selectivity of MK-0773 does not translate into differential effects on lipid metabolism in OVX rats.

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