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CV-159

Names

[ CAS No. ]:
86384-98-7

[ Name ]:
CV-159

[Synonym ]:
3,5-Pyridinedicarboxylic acid,1,4-dihydro-2,6-dimethyl-4-(3-nitrophenyl)-,methyl 6-((5-phenyl-1H-pyrazol-3-yl)oxy)hexyl ester
CV-159
1,4-Dihydro-2,6-dimethyl-4-(3-nitrophenyl)-3,5-pyridinedicarboxylic acid methyl-6-(5-phenyl-3-pyrazolyloxy)hexyl ester
CV-159-6

Biological Activity

[Description]:

CV-159 is a unique dihydropyridine Ca2+ antagonist with an anti-calmodulin (CaM) action, and has antiinflammatory activities.

[Related Catalog]:

Signaling Pathways >> Membrane Transporter/Ion Channel >> Calcium Channel
Research Areas >> Inflammation/Immunology

[In Vitro]

CV-159 (0.1-10 μM) significantly inhibits TNF-α (10 ng/ml, 24 h)-induced VCAM-1 in SMCs in a concentrationdependent manner. CV-159 (10 μM, 30 min) significantly inhibits the TNF-induced ROS production[1]. CV-159 (10 μM) inhibits TNF (24 h)-induced expression of e-selectin but not vascular cell adhesion molecule-1 and intercellular adhesion molecule-1. CV-159 inhibits TNF (20 min)-induced phosphorylation of JNK, p38, and NF-κB p65 (Ser536)[2].

[In Vivo]

CV-159 (5 and 10 mg/kg, p.o.) gives significant protection against delayed neuronal death in the hippocampal CA1 region of the rats after 15-min transient forebrain ischemia. CV-159 also diminishes the size of the brain infarct after permanent middle cerebral artery (MCA) occlusion. CV-159 significantly reduces the increase in the water content of the infarcted cortex induced by MCA occlusion[3].

[References]

[1]. Usui T, et al. Mechanisms underlying the anti-inflammatory effects of the Ca2+/calmodulin antagonist CV-159 in cultured vascular smooth muscle cells. J Pharmacol Sci. 2010;113(3):214-23. Epub 2010 Jun 16.

[2]. Usui T, et al. CV-159, a unique dihydropyridine derivative, prevents TNF-induced inflammatory responses in human umbilical vein endothelial cells. J Pharmacol Sci. 2010;113(2):182-91. Epub 2010 May 19.

[3]. Miyazaki H, et al. Neuroprotective effects of a dihydropyridine derivative, 1,4-dihydro-2,6-dimethyl-4-(3-nitrophenyl)-3,5-pyridinedicarbox ylic acid methyl 6-(5-phenyl-3-pyrazolyloxy)hexyl ester (CV-159), on rat ischemic brain injury. Life Sci. 1999;64(10):869-78.


[Related Small Molecules]

Neomycin sulfate | Nifedipine | Acetylcholine chloride | Ionomycin | (S)-(-)-Bay K 8644 | Nimodipine | Mibefradil dihydrochloride | Levetiracetam | CDN 1163 | Dantrolene sodium | Thapsigargin | Flufenamic Acid | ABT 639 | Ranolazine dihydrochloride | Cromolyn (sodium)

Chemical & Physical Properties

[ Density]:
1.249g/cm3

[ Boiling Point ]:
755.5ºC at 760 mmHg

[ Molecular Formula ]:
C31H34N4O7

[ Molecular Weight ]:
574.62400

[ Flash Point ]:
410.7ºC

[ Exact Mass ]:
574.24300

[ PSA ]:
148.36000

[ LogP ]:
6.42730

[ Index of Refraction ]:
1.586

[ Storage condition ]:
2-8℃

Related Compounds