Remibrutinib

製品コードS9660 バッチS966001

印刷

化学情報

Chemical Structure Synonyms LOU064 Storage
(From the date of receipt)		 3 years -20°C powder
化学式

C27H27F2N5O3
分子量 507.53 CAS No. 1787294-07-8
Solubility (25°C)* 体外 DMSO 100 mg/mL (197.03 mM)
Ethanol 4 mg/mL (7.88 mM)
Water Insoluble
* <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 Remibrutinib is a potent, highly selective covalent inhibitor of bruton tyrosine kinase (BTK) with IC50 of 1.3 nM, 2.5 nM and 18 nM for BTK, FcγR-induced IL8 and anti-IgM/IL4-induced CD69, respectively. Remibrutinib (LOU064) exhibits an exquisite kinase selectivity due to binding to an inactive conformation of BTK and has the potential for the treatment of autoimmune diseases.
in vitro

LOU064 exhibits an exquisite kinase selectivity due to binding to an inactive conformation of BTK and has the potential for a best-in-class covalent BTK inhibitor for the treatment of autoimmune diseases.[1]
in vivo

LOU064 demonstrates potent in vivo target occupancy with an EC90 of 1.6 mg/kg and dose-dependent efficacy in rat collagen-induced arthritis.[1]

プロトコル(参考用のみ)

細胞アッセイ 細胞株 human monocytic cell line THP1, Human Blood B cell and Basophil.
濃度 3 nM, 10 nM, 30 nM, 100 nM, 300 nM
反応時間 25 min, 50 min, 75 min, 100 min
実験の流れ

The effects of LOU064 on signaling from the activating FcγR are assessed in the human monocytic cell line THP1 (ATCC, TIB-202). The THP1 cell line expresses the two activating FcγRs CD32a (FcγRII2) and CD64 (FcγRI) that signal through BTK. Briefly, 384 well culture plates are coated with pooled non-specific human IgG fraction. Serial compound dilutions are dispensed into the IgG-coated plates containing a small volume of tissue culture medium. Then THP1 cells that are pre-differentiated by vitamin D3 treatment for 5 days are added to each well. Twenty-four hours later the secretion of IL-8 in the supernatant of these culture wells is assessed by a homogenous immunoassay.
動物実験 動物モデル Female Lewis rats, female C57BL/6 mice, male beagle dog.
投薬量 1 mg/kg, 3 mg/kg
投与方法 IV, Oral gavage

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。