Efonidipine

製品コードS4977 バッチS497702

印刷

化学情報

Synonyms

NZ-105

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₃₄H₃₈N₃O₇P

分子量

631.66

CAS No.

111011-63-3

Solubility (25°C)*

体外

DMSO

100 mg/mL (158.31 mM)

Ethanol

6 mg/mL (9.49 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	5%DMSO 1 40%PEG300 2 5%Tween80 3 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。	5.000mg/ml (7.92mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 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.

* <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	Efonidipine (NZ-105)は、血管拡張と心臓の自動能低下につながるL型およびT型カルシウムチャネルブロッカーです。また、副腎からのアルドステロン分泌を抑制します。
in vitro	Although efonidipine is not a specific T-type calcium channe (TTCC) blocker as it could also block L-type calcium channe (LTCC), its efficacy in blocking TTCC is much greater than that of LTCC. This compound exerts an inhibitory effect on aldosterone synthesis and secretion in a human adrenocortical cell line (H295R), an effect that is mediated, at least in part, by suppression of 11-β-hydroxylase and aldosterone synthase expression. It also suppresses both Ang II- and K+-induced aldosterone secretion, but it blocks the latter at much lower concentrations than the former.
in vivo	Efonidipine could provide broader beneficial effects including the heart, liver, and plasma, and antioxidant in iron-overload condition in both WT(muβ^+⁄+) and HT(muβ^{th-3 ⁄+},) mice.

プロトコル(参考用のみ)

細胞アッセイ	細胞株	The NCI-H295R human adrenocortical cell line (H295)
	濃度	0.3 μM and 3 μM
	反応時間	24 h
	実験の流れ	H295R cells are plated to a density of 0.2 × 10⁶ in 6-well plates and incubated for 48 hours, after which the medium is replaced with low-serum medium containing 0.2% UltroserSF, and the cells are then treated with Ang II (100 nmol/L) or KCl (10 mmol/L) with or without the indicated concentration of this compound for 24 hours. The cells are then harvested, and the total cellular RNA is extracted using the isothiocyanate-acid phenol chloroform method. After quantifying the extracted RNA based on absorbance at 260 nm, 500-ng aliquots are reverse transcribed.
動物実験	動物モデル	adult C57/BL6 mice (3-6 months old, heterozygous β^KO type) with FE diet (0.2% ferrocene w⁄w)
	投薬量	4 mg⁄kg
	投与方法	i.p.

参考

https://pubmed.ncbi.nlm.nih.gov/22404220/
https://pubmed.ncbi.nlm.nih.gov/16424797/

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：

Efonidipine Inhibits JNK and NF-κB Pathway to Attenuate Inflammation and Cell Migration Induced by Lipopolysaccharide in Microglial Cells [ Biomol Ther (Seoul), 2022, 30(5):455-464]	PubMed: 35993250

Efonidipine Inhibits JNK and NF-κB Pathway to Attenuate Inflammation and Cell Migration Induced by Lipopolysaccharide in Microglial Cells [ Biomol Ther (Seoul), 2022, 30(5):455-464]

PubMed: 35993250

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。