MK-0773-PF-05314882-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEMK-0773Cat. No.: HY-11027CAS No.: 606101-58-0Synonyms: PF-05314882分式: CHFNO分量: 479.59作靶点: Androgen Receptor作通路: Others储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 33.33 mg/mL (69.50 mM;

2、Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.0851 mL 10.4256 mL 20.8511 mL5 mM 0.4170 mL 2.0851 mL 4.1702 mL10 mM 0.2085 mL 1.0426 mL 2.0851 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。体内实验请根据您的实验动物和给药式选择适当的溶解案，配制前请先配制澄清的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现现配，当天使；澄清的储备液可以根

3、据储存条件，适当保存；以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (5.21 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (5.21 mM); Clear solution3. 请依序添加每种溶剂： 10% DMSO 90% corn oil1/2 Master of Small Molecule

4、s 您边的抑制剂师www.MedChemESolubility: 2.5 mg/mL (5.21 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 MK-0773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。IC50 & Target IC50: 6.6 nM (AR)体外研究 The IC50 of MK-0773 binding to AR is increased 3.5-fold in the presence of 25% rat serum a

5、nd 13-fold in thepresence of 25% human serum, indicating that it binds to serum proteins. The affinity of MK-0773 for ARacross species is evaluated using COS cells transfected with AR, and IC50 values are very similar in fourspecies (rat, 0.50 nM; dog, 0.55 nM; rhesus, 0.45 nM; human, 0.65 nM) 1.体内研

6、究 MK-0773 (6 and 80 mg/kg, s.c.) produces exposure-related stimulatory effects on cortical BFR and LBM inthe OVX rat model. MK-0773 (5, 15, and 80 mg/kg, s.c.) increases seminal vesicle weights, and has reducedeffects on the prostate. The partial agonism and tissue selectivity of MK-0773 does not tr

7、anslate intodifferential effects on lipid metabolism in OVX rats 1.PROTOCOLAnimal Rats: Prostate and seminal vesicles are studied in 3-4-month-old 250-300-g rats after orchidectomy (ORX).Administration 1 Nine days after surgery, animals are injected (subcutaneously) daily with test compounds for 17

8、days, andthe weight of the seminal vesicles (SVs) is compared with ORX rats treated with vehicle or DHT as a positivecontrol.MCE has not independently confirmed the accuracy of these methods. They are for reference only.户使本产品发表的科研献 Eur J Mass Spectrom (Chichester). 2016;22(2):49-59.See more customer

9、 validations on HYPERLINK / www.MedChemEREFERENCES1. Schmidt A, et al. Discovery of the selective androgen receptor modulator MK-0773 using a rational development strategy based ondifferential transcriptional requirements for androgenic anabolism versus reproductive physiology. J Biol Chem. 2010 May 28;285McePdfHeightCaution: Product has not been fully validated for medic