Senicapoc (ICA-17043)

製品コードE0501 バッチE050101

印刷

化学情報

Synonyms

Storage
(From the date of receipt)

3 years -20°C powder

化学式

C₂₀H₁₅F₂NO

分子量

323.34

CAS No.

289656-45-7

Solubility (25°C)*

体外

DMSO

65 mg/mL (201.02 mM)

Ethanol

6 mg/mL (18.55 mM)

Water

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	2%DMSO 1 40%PEG300 2 5%Tween80 3 53%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。	1.000mg/ml (3.09mM)	Taking the 1 mL working solution as an example, add 20 μL of 50 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 530 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	Senicapoc (ICA-17043) is a Gardos channel(Ca2⁺-activated K⁺ channel; KCa3.1) blocker with an IC50 of 11 nM and produces dose-dependent increases in hemoglobin and decreases in markers of hemolysis. Senicapoc blocks Ca2⁺-induced rubidium flux from human RBCs with an IC50 value of 11 nM and inhibits RBC dehydration with IC50 of 30 nM.
in vitro	Senicapoc (ICA-17043) is shown to block the Gardos channel of mouse (C57 Black) RBCs with an IC₅₀ of 50±6 nM. This compound also blocks the increase in cellular hemoglobin concentration in human RBCs in a concentration-dependent fashion.^[1]
in vivo	Administration of Senicapoc (ICA-17043) produces a significant decrease in Gardos channel activity measured at day 11 and 21 and is associated with a corresponding increase in red cell K+ content without changes in Na+ content. This compound (10 mg/kg, twice a day) induces a significant increase in Hct after 11 days of dosing in the SAD mouse.^[1]

プロトコル(参考用のみ)

細胞アッセイ	細胞株	Human RBCs
	濃度	1 nM-10 mM, 10 μM
	反応時間	10 min
	実験の流れ	Heparinized human blood is centrifuged at 2000 rpm, and the resulting pellet is washed 3 times with MFB as described previously. The RBC pellet is resuspended in MFB. Senicapoc (ICA-17043), at increasing concentrations, is incubated with an aliquot of cells for 10 minutes at room temperature.
動物実験	動物モデル	SAD mouse, Transgenic Hbb SAD1 mice
	投薬量	10 mg/kg
	投与方法	p.o.

参考

https://pubmed.ncbi.nlm.nih.gov/12433690/

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：

Phospholipid scrambling induced by an ion channel/metabolite transporter complex [ Nat Commun, 2024, 15(1):7566]	PubMed: 39217145

Phospholipid scrambling induced by an ion channel/metabolite transporter complex [ Nat Commun, 2024, 15(1):7566]

PubMed: 39217145

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。