MedChemExpress - Model Azelnidipine - 123524-52-7
Azelnidipine (CS 905) is a dihydropyridine calcium channel blocker that is effective orally. Azelnidipine inhibits the intracellular calcium ion flow and lower blood pressure by selectively blocking L-type calcium channel on the membrane of vascular smooth muscle. Azelnidipine inhibits esophageal squamous cell carcinoma proliferation by targeting MEK1/2. Azelnidipine also has anti-inflammatory, antioxidant and neuroprotective effects [1] [2] [3].MCE products for research use only. We do not sell to patients.
Azelnidipine
MCE China：Azelnidipine
Brand：MedChemExpress (MCE)
Cat. No.HY-B0023
CAS：123524-52-7
Synonyms：CS 905
Purity：99.66%
Storage：Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Shipping：Room temperature in continental US; may vary elsewhere.
Description：Azelnidipine (CS 905) is a dihydropyridine calcium channel blocker that is effective orally. Azelnidipine inhibits the intracellular calcium ion flow and lower blood pressure by selectively blocking L-type calcium channel on the membrane of vascular smooth muscle. Azelnidipine inhibits esophageal squamous cell carcinoma proliferation by targeting MEK1/2. Azelnidipine also has anti-inflammatory, antioxidant and neuroprotective effects .
In Vitro：Azelnidipine (0-10 μM; 96 h) inhibits esophageal squamous cell carcinoma proliferation by targeting MEK1/2 [2].
In Vivo：Azelnidipine (3 mg/kg/day; Oral gavage; 7 days) plays a protective role in rat models of cerebral ischemia-reperfusion [3]. Azelnidipine (0-3 mg/kg; Oral administration/Intravenous injection; 0-24 h) reduces blood pressure in hypertensive rat models. Oral efficacy is more than three times of Nicardipine (HY-12515). Intravenous injection is three times less effective than Nicardipine (HY-12515) [4].
IC50 & Target：L-type calcium channel MEK1 MEK2
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References：
[1]. Ram CVS. Therapeutic Usefulness of a Novel Calcium Channel Blocker Azelnidipine in the Treatment of Hypertension: A Narrative Review. Cardiol Ther. 2022 Dec;11(4):473-489. [Content Brief]
[2]. Zhao L, et al. Azelnidipine inhibits esophageal squamous cell carcinoma proliferation in vivo and in vitro by targeting MEK1/2. Mol Ther Oncolytics. 2022 Sep 26;27:61-72. [Content Brief]
[3]. Fakharaldeen Z, et al. Potential protective effects of Azelnidipine against cerebral ischemia-reperfusion injury in male rats. J Med Life. 2022 Nov;15(11):1384-1391. [Content Brief]
[4]. Oizumi K, et al. Antihypertensive effects of CS-905, a novel dihydropyridine Ca ++ channel blocker. Jpn J Pharmacol. 1989 Sep;51(1):57-64. [Content Brief]
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