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Molecular Formula :C11H17N3O8
Molecular Weight : 319.28
CAS No: 4368-28-9
Chemical Name :
Octahydro-12-(hydroxymethyl)-2-imino-5,9:7,10a-dimethano-10aH-\[1,3]dioxocino
\[6,5-d]pyrimidine-4,7,10,11,12-pentol
Melting Point :
does not melt at 200??C, darkens and black with increasing temperature.
Solubility in :
dilute acetic acid, dilute sulfuric acid, ethanol, or citrate buffer ( pH 4.8-4.9 );
slightly in water, dry alcohol and ether; insoluble in organic solvent.
Purity min. :
99% ( HPLC, TLC-FID, IR, NMR ).
Physical Form :
white crystal powder.
Biological Activity :
KD( cardiac myocytes in rats ) :0.8 nM(2)10-8 M block nervous system; * 10-5 M block heart muscle. The binding to Na+ channel is reversible.
ED50 = 3.7 nM.
Toxicity
( LD50) : mice ( i.v.) : 8.4 mg / kg. ;
mice ( i.p.) : 8.1 mg / kg. ;
mice ( s.c.) : 10.8 mg / kg.
Storage recommendations :
stable at room temperature, store preferably at
4C. Solid and solutions can be kept in deep
freeze for a long time without any change in their activity. Solution for use: reconstitute in
citrate or acetate buffer, pH 4.8-4.9 . Safety recommendations: highly toxic.
Merck Index 12th Ed. : 9382
References :
1.Biochem. Biophys. Res. Commun. 138, 1250-1256 (1986).
2.Biochemistry 20,1279-1285(1981).
3.Exp. Neurol. 99, 118 (1988).
4.J. Pharmacol. Exp. Ther. 251, 1166-1173 (1989).
5.Proc.Natl. Acad. Sci.
U.S.A. 88, 5379-5382 (1991).
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