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.
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- CAS. Nr.: 89943-82-8
- Formel: C14H12ClNO2
- Molecular Weight:261.70
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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.
Chemical Information
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CAS. Nr. 89943-82-8
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Molecular Weight 261.70
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Formel C14H12ClNO2
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SMILES
ClC1=CC=C(C2OCC3=C(C(C)=NC=C32)O)C=C1
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
[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. [Content Brief]
[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. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
- Cicletanine
- 89943-82-8
- Calcium Channel
- α-adrenoceptor-mediated Ca2+ release pathway
- prostacyclin
- cytoplasmic cholesteryl ester hydrolase
- voltage-dependent Ca2+ channel
- cholesteryl ester synthase
- lysosomal cholesteryl ester hydrolase
- arterial smooth muscle cells
- rat aorta
- vascular smooth muscle
- rabbit mesenteric artery
- Inhibitor
- inhibitor
- inhibit