AZ876

製品コードS6427 バッチS642701

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

C24H29N3O3S
分子量 439.57 CAS No. 898800-26-5
Solubility (25°C)* 体外 DMSO 88 mg/mL (200.19 mM)
 
 
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.
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O

この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。

 4.400mg/ml (10.01mM) Taking the 1 mL working solution as an example, add 50 μL of 88 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <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 AZ876 is a novel high-affinity Liver X Receptor (LXR) agonist with Ki values of 0.007 μM and 0.011 μM for human LXRα and LXRβ respectively.
in vitro

In binding assays, AZ876 is 25-fold and 2.5-fold more potent than GW3965 on human (h)LXRα and hLXRβ respectively. In reporter transactivation assays, this compound is 196-fold and fivefold more potent than GW3965 on hLXRα and hLXRβ respectively. It is also more potent than GW3965 on mouse (m)LXRα (248-fold) and mLXRβ (10.5-fold). This chemical is four- to sevenfold more potent than GW3965 on the expression of ABCA1 mRNA in hamster and human blood PMN cells. It is highly selective with respect to other nuclear hormone receptors, including retinoid X receptor, farnesoid X receptor, thyroid hormone receptor (TR)α or TRβ, when tested in agonist mode in fluorescence resonance energy transfer assays[1].
in vivo

AZ876 is a dual partial LXR agonist that has been shown to reduce atherosclerosis in mice without affecting liver or plasma triglyceride levels when administered in low dose. Chronic administration of this compound attenuates pathological cardiac hypertrophy in a murine model of chronic pressure overload without altering systemic blood pressure, implicating heart-specific effects. This compound treatment diminishes myocardial fibrosis and suppresses induction of profibrotic gene expression[2].

プロトコル(参考用のみ)

参考

  • https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3057293/
  • https://pubmed.ncbi.nlm.nih.gov/25684370/

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：

PTEN-induced partial epithelial-mesenchymal transition drives diabetic kidney disease. [ J Clin Invest, 2019, 129(3):1129-1151] PubMed: 30741721

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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