MK-0773

MK-0773

MK-0773Musculoskeletal diseases
CAS: 606101-58-0
MF: C27H34FN5O2
MW: 479.59
适应症
Sarcopenia; Osteoporosis
作用靶点
AR
用途

A steroidal SARM, studied in sarcopenia and osteoporosis, has entered Phase II clinical trials.

规格标准
>99%
描述

概况

MK-0773 is a steroidal SARM with partial agonist activity, enhancing lean body mass and strength in sarcopenia while reducing prostate effects. It promotes bone formation and muscle recovery with limited virilization, though transaminase elevations noted. Ideal for osteoporosis and frailty research in elderly populations.

Synonyms: PF05314882; PF-05314882; MK0773; N-(3H-Imidazo[4,5-b]pyridin-2-ylmethyl)-2-fluoro-4-methyl-3-oxo-4-aza-5alpha-androst-1-ene-17beta-carboxamide; 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)-

Product Categories: SARM series; pharmaceutical original drug series

Mol File: 606101-58-0.mol

物化性质

Boiling point: 754.2±60.0°C(Predicted)

Density: 1.31±0.1g/cm3(Predicted)

Storage temp.: Store at -20°C

Solubility: DMSO: 33.33 mg/mL (69.50 mM; Need ultrasonic)

Form: Powder

Color: Light yellow to yellow

MSDS信息

实验数据

1.Cell Experiment

Solubility in DMSO: 33.33 mg/mL (69.50 mM; solubilized with ultrasound; the solubility of the product is significantly affected by hygroscopic DMSO, so please use freshly opened DMSO)

Preparing Stock Solutions:

image

Please choose a suitable solvent to prepare the stock solution based on the product's solubility in different solvents. Once the solution is prepared, aliquot and store it to avoid product degradation caused by repeated freeze-thaw cycles.

Storage conditions and shelf life of the stock solution: -80°C for 2 years; -20°C for 1 year. When stored at -80°C, use within 2 years; when stored at -20°C, use within 1 year.


2.Animal Experiment

Please choose an appropriate dissolution method based on your experimental animals and administration route.  

For all the following dissolution methods, please first prepare a clear stock solution according to the in vitro procedure, and then add solubilizing agents sequentially:  


— To ensure the reliability of experimental results, the clear stock solution can be stored appropriately depending on storage conditions; for in vivo experiments, it is recommended to prepare the working solution fresh and use it the same day.  

The percentages shown before the following solvents refer to the volume ratio of that solvent in your final prepared solution; if precipitation or crystallization occurs during preparation, solubilization can be aided by heating and/or ultrasonication.


Protocol 1

Please add each solvent in order: 10% DMSO, 40% PEG300, 5% Tween-80, 45% Saline

Solubility: ≥ 2.5 mg/mL (5.21 mM); clear solution

This protocol can achieve a clear solution of ≥ 2.5 mg/mL (saturation unknown).

For 1 mL of working solution as an example, take 100 μL of a 25.0 mg/mL clear DMSO stock solution and add it to 400 μL of PEG300, then mix well; next, add 50 μL of Tween-80 to the above mixture and mix thoroughly; then continue by adding 450 μL of saline and adjust the volume to 1 mL.

Preparation of saline: Dissolve 0.9 g of sodium chloride in ddH₂O and adjust the volume to 100 mL to obtain a clear, transparent saline solution.

Protocol 2

Please add each solvent in order: 10% DMSO, 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (5.21 mM); clear solution

This protocol can yield a clear solution with ≥ 2.5 mg/mL (saturation unknown).

For 1 mL of working solution, add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD saline solution and mix well.

Dissolve 2 g of SBE-β-CD (sulfobutyl ether β-cyclodextrin) powder in 10 mL of saline, fully dissolving to a clear and transparent solution.

Protocol 3

Please add each solvent in order: 10% DMSO, 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.21 mM); clear solution

This method can achieve a clear solution with ≥ 2.5 mg/mL (saturation unknown). For animal experiments lasting more than half a month, use this method as appropriate.

For 1 mL of working solution, take 100 μL of 25.0 mg/mL clear DMSO stock solution and add it to 900 μL of corn oil, then mix thoroughly.

Pharmacodynamics

Mechanism Of Action