MK-3903

製品コードS8803 バッチS880301

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
化学式

C27H19ClN2O3
分子量 454.90 CAS No. 1219737-12-8
Solubility (25°C)* 体外 4-Methylpyridine (warmed with 50ºC water bath) 23 mg/mL (50.56 mM)
DMSO 5.6 mg/mL (12.31 mM)
Water Insoluble
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 MK-3903 is a potent and selective AMPK activator with an EC50 of 8 nM for α1 β1 γ1 subunit. It activates 10 of the 12 pAMPK complexes with EC50 values in the range of 8-40 nM and maximal activation >50%.
in vitro

MK-3903 activates 10 of the 12 pAMPK complexes with EC50 values in the range of 8-40 nM and maximal activation >50%. This compound partially activates pAMPK5 (36% max), which is only a minor component of human and mouse liver, and it does not activate pAMPK6, which is not detected in liver. It is a weak reversible inhibitor of CYP3A4 and 2D6 in human liver microsomes (apparent IC50 > 50 μM) and does not exhibit time-dependent inhibition of CYP3A4 activity. This chemical is not a potent PXR agonist[1].
in vivo

The pharmacokinetics of MK-3903 in C57BL/6 mice, Sprague–Dawley rats, and beagle dogs were characterized by moderate systemic plasma clearance (5.0–13 mL/min/kg), a volume of distribution at steady state of 0.6–1.1 L/kg, and a terminal half-life of ∼2 h. It has low oral bioavailability (8.4%) in C57BL/6 mice, but the oral exposure is later improved using other vehicles. Oral bioavailabilities in rats and dogs are improved (27-78%). Chronic oral administration of this compound robustly increased ACC phosphorylation in liver with more modest effects in skeletal muscle. Treatment of various mouse models with this chemical results in expected alterations in lipid metabolism and improvements in a measure of insulin sensitization[1].

プロトコル(参考用のみ)

動物実験 動物モデル lean C57BL/6 mice, Sprague-Dawley rats and beagle dogs
投薬量 for I.V., 2 mg/kg in mouse, 1 mg/kg in rat and 0.5 mg/kg in dog; for P.O., 10 mg/kg in mouse, 4 mg/kg in rat and 1 mg/kg in dog
投与方法 P.O. and I.V.

参考

  • https://pubmed.ncbi.nlm.nih.gov/29035567/

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

MK8722, an AMPK activator, inhibiting carcinoma proliferation, invasion and migration in human pancreatic cancer cells [ Biomed Pharmacother, 2021, 144:112325] PubMed: 34656065

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。