MK-0773

(Synonyms: PF-05314882)
目录号: PL01845 纯度: ≥98%
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。
CAS No. :606101-58-0
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中文名称
MK-0773
英文名称
MK-0773
英文别名
MK-0773;(1S,3aS,3bS,5aR,9aS,9bS,11aS)-8-fluoro-N-(1H-imidazo[4,5-b]pyridin-2-ylmethyl)-6,9a,11a-trimethyl-7-oxo-2,3,3a,3b,4,5,5a,9b,10,11-decahydro-1H-indeno[5,4-f]quinoline-1-carboxamide;MK 0773;N-(3H-Imidazo[4,5-b]pyridin-2-ylmethyl)-2-fluoro-4-methyl-3-oxo-4-aza-5alpha-androst-1-ene-17beta-carboxamide;PF 05314882;5730VNW22X;Q27261459
Cas No.
606101-58-0
分子式
C27H34FN5O2
分子量
479.59
包装储存
Powder -20°C 3 years;4°C 2 years
详情描述
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。
产品详情
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。
生物活性
MK-0773 is a selective androgen receptor modulators (SARMs) that binds to AR with an IC 50 of 6.6 nM.
性状
Solid
IC50 & Target[1][2]
IC50: 6.6 nM (AR)
体外研究(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). has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
ClinicalTrial
参考文献
[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
溶解度数据
In Vitro: DMSO : 33.33 mg/mL (69.50 mM; Need ultrasonic)配制储备液
搜索质检报告(COA)
[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

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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