SKF96365

製品コードS7999 バッチS799902

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

C22H26N2O3.HCl

分子量 402.91 CAS No. 130495-35-1
Solubility (25°C)* 体外 DMSO 80 mg/mL (198.55 mM)
Water 80 mg/mL (198.55 mM)
Ethanol 80 mg/mL (198.55 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。

4mg/ml (9.93mM) Taking the 1 mL working solution as an example, add 50 μL of 80 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.
Clear solution
5% DMSO 95% Corn oil

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。

0.57mg/ml (1.41mM) Taking the 1 mL working solution as an example, add 50 μL of 11.4 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. 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 SKF96365, originally identified as a blocker of receptor-mediated calcium entry, is widely used diagnostically, as a blocker of transient receptor potential canonical type (TRPC) channels.
in vitro SKF-96365 exhibits protective activity against MPP+ injury in PC12 cells and significantly inhibits apoptotic cell death in PC12 cells after MPP+ administration. SKF-96365 does not exert effects on necrotic cell death induced by MPP+ insult in PC12 cells. Because of its non-selective activity, SKF-96365 has been demonstrated to have effects on multiple other Ca2+ channels: it not only blocks high-voltage-activated (HVA) Ca2+ channels at typically utilized test concentrations, but also potently inhibits low-voltage -activated (LVA) T-type Ca2+ channels in HEK293 cells. The exact effect of SKF-96365 on intracellular calcium homeostasis might dependent on cell types and experimental models used[2].
in vivo SKF-96365 treatment inhibited the calcium/calmodulin-dependent protein kinase IIγ (CaMKIIγ)/AKT signaling cascade in vitro and in vivo[4].

プロトコル(参考用のみ)

細胞アッセイ 細胞株 PC12 cells
濃度 1 µM, 10 µM or 50 µM 
反応時間 30 min
実験の流れ

To investigate whether SKF-96365 could protect PC12 cells from injury induced by MPP+ insult, cultured PC12 cells are pretreated with SKF-96365 in different concentrations (1 µM, 10 µM or 50 µM) 30 min before MPP+ addition. The cells viability is measured 24 h after MPP+ insult by using the cell proliferation reagent WST-1.

動物実験 動物モデル C57BL/6N mice
投薬量 0.02 μmol & 0.2 μmol/2 μl/mouse
投与方法 intrastriatally

参考

  • https://pubmed.ncbi.nlm.nih.gov/20590636/
  • https://pubmed.ncbi.nlm.nih.gov/23383239/
  • https://pubmed.ncbi.nlm.nih.gov/19680266/
  • https://pubmed.ncbi.nlm.nih.gov/26803057/

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:

Store-operated Ca2+ entry contributes to the ASM phenotype transition in asthma [ Exp Lung Res, 2025, 51(1):23-37] PubMed: 40205756
Inhibition of Osteoclastogenesis by LY90009 through Notch Signaling Modulation in Osteolytic Disease Models [ J Vis Exp, 2025, (224)] PubMed: 41144506
STIM1/Orai1-mediated Ca 2+ influx contributes to the ASM phenotype modulation and ASM-related ECM deposition in asthma [ Research Square, 2024, 10.21203/rs.3.rs-3863076/v1] PubMed: none
TSPAN18 facilitates bone metastasis of prostate cancer by protecting STIM1 from TRIM32-mediated ubiquitination [ J Exp Clin Cancer Res, 2023, 42(1):195] PubMed: 37542345
TSPAN18 facilitates bone metastasis of prostate cancer by protecting STIM1 from TRIM32-mediated ubiquitination [ J Exp Clin Cancer Res, 2023, 42(1):195] PubMed: 37542345
EHD2 overexpression promotes tumorigenesis and metastasis in triple-negative breast cancer by regulating store-operated calcium entry [ Elife, 2023, 12e81288] PubMed: 36625722
Thalidomide Alleviates Apoptosis, Oxidative Damage and Inflammation Induced by Pemphigus Vulgaris IgG in HaCat Cells and Neonatal Mice Through MyD88 [ Drug Des Devel Ther, 2023, 17:2821-2839] PubMed: 37719363
Thalidomide Alleviates Apoptosis, Oxidative Damage and Inflammation Induced by Pemphigus Vulgaris IgG in HaCat Cells and Neonatal Mice Through MyD88 [ Drug Des Devel Ther, 2023, 17:2821-2839] PubMed: 37719363
How filopodia respond to calcium in the absence of a calcium-binding structural protein: non-channel functions of TRP [ Cell Commun Signal, 2022, 20(1):130] PubMed: 36028898
Role of TRPC6 in periodontal tissue reconstruction mediated by appropriate stress [ Stem Cell Res Ther, 2022, 13(1):401] PubMed: 35932080

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。