RN486

製品コードS7080 バッチS708001

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C35H35FN6O3
分子量 606.69 CAS No. 1242156-23-5
Solubility (25°C)* 体外 DMSO (warmed with 50ºC water bath) 62 mg/mL (102.19 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.
Clear solution
5%DMSO 30%PEG300 10%Tween80 55%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。

 5.000mg/ml (8.24mM) Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 300 μL of PEG300, mix evenly to clarify it; add 100 μL of Tween80 to the above system, mix evenly to make it clear; then continue to add 550 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 RN486 is a potent and selective BTK inhibitor with IC50 of 4 nM.
in vitro

RN486 not only potently and selectively inhibits the Btk enzyme, but also displays functional activities in human cell-based assays in multiple cell types, blocking Fcε receptor cross-linking-induced degranulation in mast cells (IC50 = 2.9 nM), Fcγ receptor engagement-mediated tumor necrosis factor α production in monocytes (IC50 = 7.0 nM), and B cell antigen receptor-induced expression of an activation marker, CD69, in B cells in whole blood (IC50 = 21.0 nM). This compound is able to block the signaling of BCR as demonstrated by a marked inhibition of phosphorylation of both Btk and PLCγ2 in B cells. It displays a selective B cell inhibitory profile in BioMAP Systems.[1]
in vivo

RN486 displays similar functional activities in rodent models, effectively preventing type I and type III hypersensitivity responses. More importantly, this compound produces robust anti-inflammatory and bone-protective effects in mouse CIA and rat adjuvant-induced arthritis (AIA) models.

プロトコル(参考用のみ)

キナーゼアッセイ Enzymatic Activity and Binding AssaysBtk Enzymatic Activity Assay.
A fluorescence-based kinase assay is used to measure Btk kinase activity and its inhibition by RN486. In the assay, this compound is incubated with a human recombinant Btk (10 nM), ATP (100 μM), and a fluorescent-labeled peptide substrate (15 μM) at 30°C for 15 min. The reaction is then stopped by the addition of a termination buffer, and reaction product is quantified by using a Desktop Profiler 4 sipper.

参考

  • https://pubmed.ncbi.nlm.nih.gov/22228807/

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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