YM-58483 (BTP2)

製品コードS8380 バッチS838001

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

C15H9F6N5OS
分子量 421.32 CAS No. 223499-30-7
Solubility (25°C)* 体外 DMSO 84 mg/mL (199.37 mM)
Ethanol 42 mg/mL (99.68 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 YM-58483/BTP2 is a blocker of store-operated Ca2+ entry (SOCE), which regulates the activation of non-excitable cells such as lymphocytes.
in vitro YM-58483 (also known as BTP2) is a selective SOCE blocker that inhibits anti-CD3 antibody-induced sustained Ca2+ influx in Jurkat T cells. YM-58483 does not cross-react with voltage-operated Ca2+ entry, K+ channels, or Cl− channels. It suppresses the CRAC, TRPC3, and TRPC5 channels, and also facilitates the TRPM4 channel. YM-58483 suppresses cytokine production (IL-2, IL-4, IL-5, IFN-γ, etc.) and proliferation in T cells in vitro. YM-58483 inhibits the spleen cell proliferation associated with MLR by suppressing NF-AT activation via sustained influx of extracellular Ca2+[1]. YM-58483 potently inhibits IL-2 production and NF-AT-driven promoter activity, but not AP-1-driven promoter activity in Jurkat cells[2].
in vivo YM-58483 exhibits inhibitory effects on several types of allergic asthma models, such as airway hyperresponsiveness, early and late bronchoconstriction, and antigen-induced airway eosinophilia, with the reduction of IL-4 and leukotriene levels in the airways of rats and guinea pigs. YM-58483 also inhibits the anti-host CTL response, donor T cell expansion, and IFN-γ production in GVHD mice. YM-58483 selectively inhibits storeoperated Ca2+ influx, it does not affect baseline intracellular Ca2+ levels. YM-58483 caused no apparent change in general activity in mice at doses up to 30 mg/kg, p. o[1].

プロトコル(参考用のみ)

細胞アッセイ 細胞株 Jurkat cells
濃度 0.03-3 μM
反応時間 30 min
実験の流れ

Jurkat cells (1×107 cells/ml) were tested with varying concentration of compounds for 30 min at 37°C. The cells were stimulated with 1 μM ionomycin for 30 min at 37°C. After stimulation, the cells were centrifuged at 200×g for 2 min, and were solubilized in 100 μl of Triton X-100 lysis buffer. The cell lysate was centrifuged at 15,000×g for 20 min; the clarified lysate was subjected to SDS-PAGE; and NF-ATc2 was detected by Western blotting with anti-NF-ATc2 mAb.
動物実験 動物モデル Male C57BL/6, BDF1((C57BL/6×DBA2)F1), DBA2 and Balb/c mice
投薬量 1-30 mg/kg
投与方法 p.o.

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：

Lysosomal Ca2+ as a mediator of palmitate-induced lipotoxicity [ Cell Death Discov, 2023, 9(1):100] PubMed: 36944629
Sensing plasma membrane pore formation induces chemokine production in survivors of regulated necrosis [ Dev Cell, 2022, S1534-5807(21)01035-2] PubMed: 35016014
Mannan-Binding Lectin Reduces Epithelial-Mesenchymal Transition in Pulmonary Fibrosis via Inactivating the Store-Operated Calcium Entry Machinery [ J Innate Immun, 2022, 1-13] PubMed: 35671705
Ang II Promotes Cardiac Autophagy and Hypertrophy via Orai1/STIM1 [ Front Pharmacol, 2021, 12:622774] PubMed: 34079454
Epithelial Sodium Channel Regulates Adult Neural Stem Cell Proliferation in a Flow-Dependent Manner. [ Cell Stem Cell, 2018, 22(6):865-878] PubMed: 29779889

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。