Cicletanine 

Cicletanine is a voltage-dependent Ca²⁺ channel inhibitor. Cicletanine inhibits α-adrenoceptor-mediated Ca²⁺ release pathway, and shows vasodilatory effects on isolated vascular smooth muscle. Cicletanine directly stimulates lysosomal and cytoplasmic cholesteryl ester hydrolase activity. Cicletanine can be used for the research of hypertension^[1][2].

Cicletanine (10-300 μM; 20 min) concentration-dependently inhibits high K⁺-, NE-, and PGF₂α-induced sustained contractions in isolated rat aortic preparations, with 300 μM causing the greatest inhibition of low-intensity stimulant-induced contractions^[1].
Cicletanine (100-300 μM; 5-10 min) inhibits sustained high K⁺- and NE-induced increases in [Ca²⁺]ᵢ and muscle tension in fura-PE3-loaded rat aortic strips, and does not alter the [Ca²⁺]ᵢ/tension relationship for either stimulant^[1].
Cicletanine (300 μM; 15 min) inhibits NE-induced transient increases in both [Ca²⁺]ᵢ and muscle tension^[1].
Cicletanine (300 μM; 1 h) does not affect resting or SNP-stimulated cGMP content in isolated rat aortic rings^[1].
Cicletanine (1.7 mM; 2 h) stimulates PGI₂ production 2-3 fold, activates lysosomal and cytoplasmic cholesteryl ester hydrolases, and modestly inhibits cholesteryl ester synthesis in cultured arterial smooth muscle cells without increasing cyclic AMP levels or causing cellular toxicity^[2].
Cicletanine (1.7 mM; 2 h) has no effect on blood-derived monocyte adhesion to endothelial cells in vitro^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

261.70

C₁₄H₁₂ClNO₂

89943-82-8

ClC1=CC=C(C2OCC3=C(C(C)=NC=C32)O)C=C1

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Izumi M, et al. Cicletanine-induced decreases in cytosolic Ca2+ level and contraction in vascular smooth muscle. Jpn J Pharmacol. 1998;76(1):57-63.

  [2]. Hajjar DP, et al. Cicletanine stimulates cholesteryl ester hydrolase activities and prostacyclin production in arterial smooth muscle cells. Arch Mal Coeur Vaiss. 1989;82 Spec No 4:79-84.