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 is a potent inhibitor of TGF-β type I receptor (ALK5-TD) with IC50 of 12 nM. A-83-01 also inhibits the transcription induced by activin/nodal type I receptor (ALK4-TD) and nodal type I receptor (ALK7-TD) with IC50 of 45 nM and 7.5 nM, respectively.Solutions are unstable and should be fresh-prepared.
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.[1]
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.[2]

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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