MK-0773

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效的选择性雄激素受体调节剂 (SARM)，结合 IC50 为 6.6 nM。

A potent, selective androgen receptor modulator (SARM) with binding IC50 of 6.6 nM; displays no binding to other nuclear receptors ( GR, IC50> 2 uM) and 5α-reductase (IC50>10 uM); improves muscle function while minimizing effects on other tissues.Osteoporosis Phase 1 Clinical.

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).

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.

MK0773 | MK 0773 | PF 05314882 | PF-05314882 | PF05314882

Endocrinology/Hormones

Androgen Receptor (AR)

Androgen Receptor (AR)

Metabolic Disease

Osteoporosis

606101-58-0

479.5896

C27H34FN5O2

>98% (HPLC)

10 mM in DMSO

C[C@@]12[C@@H](C(NCC3=NC4=CC=CN=C4N3)=O)CC[C@@]1([H])[C@]5([H])CC[C@@]6([H])N(C)C(C(F)=C[C@]6(C)[C@@]5([H])CC2)=O

1H-Indeno[5,4-f]quinoline-7-carboxamide, 3-fluoro-2,4a,4b,5,6,6a,7,8,9,9a,9b,10,11,11a-tetradecahydro-N-(3H-imidazo[4,5-b]pyridin-2-ylmethyl)-1,4a,6a-trimethyl-2-oxo-, (4aS,4bS,6aS,7S,9aS,9bS,11aR)-

(-20℃)

With Ice Pack

≥ 2 years