MK-2866 (GTx-024) 化学構造
分子量: 389.33

高品質保証

Quality Control & MSDS

製品説明

  • Compare Androgen Receptor Inhibitors
    Androgen Receptor製品生物活性の比較
  • 研究分野

製品の説明

生物活性

製品説明 MK-2866 (GTx-024)は、口で生物が利用可能な非ステロイド性の選択的なアンドロゲン受容体モジュレータ(SARM)で、 Ki が3.8 nMになる。
ターゲット Androgen receptor (AR)
IC50 3.8 nM (Ki) [1]
In vitro試験 Ostarine at the concentration of 10 nM modulates the transcriptional activity of AR in CV-1 cells cotransfected with a human AR expression vector, a luciferase reporter vector, and a control β-galactosidase vector, with 94%-100% relative activity of the transcriptional activation observed for 1 nM DHT. [1] [2]
In vivo試験 After intravenous administration of Ostarine at a single dose of 10 mg/kg, plasma concentration of Ostarine declines slowly, exhibiting a longer terminal half-life of 6.0 hours, as compared to that of other related cyano/nitro group-substituted SARMs with terminal halflives of 2.6-4.0 hours. Ostarine exhibits significantly androgenic and anabolic activity by stimulating the growth of prostate, seminal vesicles, and levator ani muscle when administered in castrated male rats; Ostarine is more potent than other cyano/nitro group-substituted SARMs. Ostarine restores the weight of the prostate to 39.2%, and seminal vesicle 78.8%, and stimulates the growth of levator ani muscle to a greater extent of 141.9% as compared with that of androgenic organs. Ostarine exhibits the highest in vivo androgenic and anabolic activity of any AR nonsteroidal agonist examined to date, with ED50 values of 0.12, 0.39 and 0.03 mg/day in prostate, seminal vesicles, and levator ani muscle, respectively, being 4 times as potent as testosterone propionate (TP) in levator ani muscle. At low dose of 0.03 mg/day, Ostarine is sufficient to exert efficacious and selective activity in anabolic tissues. [1]
臨床試験 Currently under Phase III study to determine if the investigational drug Ostarine can help patients with non small cell lung cancer increase physical function and maintain or gain muscle.
特集 The most potent and tissue-selective in vivo activity of SARMs to date, with favorable pharmacokinetic properties.

プロトコル (参考用のみ)

キナーゼアッセイ: [1]

In vitro competitive radioligand binding assay The AR binding affinity of Ostarine is determined using an in vitro competitive radioligand binding assay with [3H]mibolerone (MIB). Briefly, increasing concentrations (0.01-5000 nM) of Ostarine are incubated with rat cytosol, a saturating concentration of [3H]-MIB (1 nM), and 1000 nM triamcinolone acetonide to prevent interaction of MIB with progesterone receptors at 4 °C for 18 hours. At the end of incubation, free and bound [3H]-MIB are separated using the hydroxyapatite method. IC50 value is determined by computer-fitting the data for each ligand by nonlinear regression analysi

動物実験: [1]

動物モデル Immature castrated male Sprague-Dawley rats
製剤 Dissolved in DMSO, and diluted in saline
投薬量 1 mg/day
投与方法 Subcutaneous injection

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDogMonkeyBaboon
Weight (kg)0.020.151.80.40.0810312
Body Surface Area (m2)0.0070.0250.150.050.020.50.240.6
Km factor361285201220
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

参考

化学情報

Download MK-2866 (GTx-024) SDF
分子量 389.33
化学式

C19H14F3N3O3

CAS No. 841205-47-8
保管 2年-20℃
6月-80℃in solvent
別名 Enobosarm
溶解度 (25°C) * In vitro DMSO 78 mg/mL (200.34 mM)
エタノール 78 mg/mL (200.34 mM)
<1 mg/mL (<1 mM)
In vivo 1% DMSO/30% polyethylene glycol/1% Tween 80 5 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
化学名 (S)-N-(4-cyano-3-(trifluoromethyl)phenyl)-3-(4-cyanophenoxy)-2-hydroxy-2-methylpropanamide

文献中の引用 (2)

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