Efonidipine

製品コードS4977 バッチS497702

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
* <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) is an L- and T-type calcium channel blocker leading to vasodilation and decreased automaticity of the heart. It also suppresses aldosterone secretion from the adrenal.
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^[1]. Efonidipine 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. Efonidipine also suppresses both Ang II- and K+-induced aldosterone secretion, but it blocks the latter at much lower concentrations than the former^[2].
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^[1].

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 Ca2+ channel blocker 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

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。

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