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MK-0773
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
MK-0773图片
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品介绍
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。

Animal experiment:

Rats: Prostate and seminal vesicles are studied in 3-4-month-old 250-300-g rats after orchidectomy (ORX). Nine days after surgery, animals are injected (subcutaneously) daily with test compounds for 17 days, and the weight of the seminal vesicles (SVs) is compared with ORX rats treated with vehicle or DHT as a positive control.

产品描述

MK-0773 is a selective androgen receptor modulators (SARMs) that binds to AR with an IC50 of 6.6 nM. IC50: 6.6 nM (AR)

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)[1].

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[1].

[1]. Schmidt A, et al. Discovery of the selective androgen receptor modulator MK-0773 using a rational development strategy based on differential transcriptional requirements for androgenic anabolism versus reproductive physiology. J Biol Chem. 2010 May 28;285