A-83-01

製品コードS7692 バッチS769203

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

C25H19N5S
分子量 421.52 CAS No. 909910-43-6
Solubility (25°C)* 体外 DMSO 21 mg/mL (49.81 mM)
Water Insoluble
Ethanol 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 A-83-01 は、IC50 が 12 nM の強力な TGF-β タイプ I 受容体 (ALK5-TD) 阻害剤です。また、A-83-01 は、アクチビン/ノーダル タイプ I 受容体 (ALK4-TD) および ノーダル タイプ I 受容体 (ALK7-TD) によって誘導される転写を、それぞれ 45 nM および 7.5 nM の IC50 で阻害します。溶液は不安定なので、使用直前に調製してください。
in vitro

A-83-01 inhibits the transcriptional activity induced by TGF-β type I receptor ALK-5 and that by activin type IB receptor ALK-4 and nodal type I receptor ALK-7, the kinase domains of which are structurally highly related to those of ALK-5. This compound is potent in the inhibition of ALK5 and also prevents phosphorylation of Smad2/3 and the growth inhibition induced by TGF-β.
in vivo

A83-01 treatment significantly increases the number of Nkx2.5+ cardiomyoblasts at baseline and after myocardial injury, resulting in an increase in newly formed cardiomyocytes. This compound significantly improves ventricular elastance and stroke work, leading to improved contractility after injury.

プロトコル(参考用のみ)

細胞アッセイ 細胞株 Wild-type mink lung epithelial (Mv1Lu) cells, R mutant of Mv1Lu (R4-2) cells, HaCaT cells, C2C12 cells, NMuMG cells
濃度 1 μM
反応時間 1 h
実験の流れ

Cell proliferation assay: Mv1Lu cells are seeded in duplicate at a density of 2.5 × 104 cells/well in 24-well plates. The following day, cells are pretreated for 1 h with 1 μM A-83-01 and then cultured with TGF-β (1 ng/mL) for 24 h, 48 h, or 72 h. Cells are trypsinized and counted with a Coulter counter. To explore whether this compound reduces the growth-inhibitory effects of TGF-β in concentration-dependent fashion, Mv1Lu cells are seeded as above and pretreated for 1 h with various concentrations of this chemical. After pretreatment, cells are cultured with TGF-β (1 ng/mL) for 48 h and counted.
動物実験 動物モデル 8–10 week old Nkx2.5 enhancer-eGFP transgenic mice
投薬量 10 mg/kg
投与方法 IP

参考

  • https://pubmed.ncbi.nlm.nih.gov/16271073/
  • https://pubmed.ncbi.nlm.nih.gov/25362681/

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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。

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