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CV-6209

Names

[ CAS No. ]:
100488-87-7

[ Name ]:
CV-6209

[Synonym ]:
2-{N-acetyl-N-[({2-methoxy-3-[(octadecylcarbamoyl)oxy]propoxy}carbonyl)amino]methyl}-1-ethylpyridinium chloride
2-{N-[1-(3,4-dihydroxyphenyl)ethyl]amino}acetaldehyde dimethyl acetal hydrochloride
1,2-Benzenediol,4-[1-[(2,2-dimethoxyethyl)amino]ethyl]-,hydrochloride
2-(2-ACETYL-6-METHOXY-3,9-DIOXO-4,8-DIOXA-2,10-DIAZAOCTACOS-1-YL)-1-ETHYL-PYRIDINIUM CHLORIDE

Biological Activity

[Description]:

CV-6209 is a potent antagonist of platelet activating factor (PAF). CV-6209 inhibits the PAF-induced aggregation of rabbit and human platelets, with IC50s of 75 nM and 170 nM, respectively. CV-6209 can inhibit PAF-induced hypotension in rats[1].

[Related Catalog]:

Research Areas >> Cardiovascular Disease
Signaling Pathways >> Others >> Others

[Target]

platelet activating factor (PAF)[1]


[In Vitro]

CV-6209 inhibits [3H]serotonin release from rabbit platelets stimulated with PAF (30 nM)[1]. CV-6209 has little action on platelet aggregation induced by arachidonic acid, ADP, or collagen[1]. CV-6209 (0.2-2 μM; pretreated for 30 min) inhibits PAF-induced MC degranulation in both LAD2 and hLMCs[1].

[In Vivo]

CV-6209 (i.v.) inhibits PAF (0.3 μg/kg; i.v.)-induced hypotension in rats (ED50=0.009 mg/kg) with no effect on the hypotension induced by arachidonic acid, histamine, bradykinin and isoproterenol[1]. CV-6209 (66 μg; i.v.) reduces asparaginase-induced hypersensitivity compared with nonpretreated, sensitized mice[3].

[References]

[1]. Terashita Z, et, al. CV-6209, a highly potent antagonist of platelet activating factor in vitro and in vivo. J Pharmacol Exp Ther. 1987 Jul;242(1):263-8.

[2]. Munoz-Cano R, et, al. Effects of Rupatadine on Platelet- Activating Factor-Induced Human Mast Cell Degranulation Compared With Desloratadine and Levocetirizine (The MASPAF Study). J Investig Allergol Clin Immunol. 2017;27(3):161-168.

[3]. Fernande CA, et, al. Effect of premedications in a murine model of asparaginase hypersensitivity. J Pharmacol Exp Ther. 2015 Mar;352(3):541-51.

Chemical & Physical Properties

[ Molecular Formula ]:
C34H60ClN3O6

[ Molecular Weight ]:
642.31

[ Exact Mass ]:
641.41700

[ PSA ]:
98.05000

[ LogP ]:
8.67470

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

DownStream

Related Compounds