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Vanoxerine dihydrochloride

Chemical Structure : Vanoxerine dihydrochloride

CAS No.: 67469-78-7

Vanoxerine dihydrochloride (Boxeprazine, GBR-12909, GBR12909;I893, I-893)

Catalog No.: PC-43399Not For Human Use, Lab Use Only.

Vanoxerine (GBR-12909, I-893, Boxeprazine) is a highly potent inhibitor of dopamine uptake in vitro in tissue slices obtained from rat neostriatum with IC50 of 40-50 nM, also inhibits norepinephrine uptake with IC50 of 560-2600 nM.

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Biological Activity

Vanoxerine (GBR-12909, I-893, Boxeprazine) is a highly potent inhibitor of dopamine uptake in vitro in tissue slices obtained from rat neostriatum with IC50 of 40-50 nM, also inhibits norepinephrine uptake with IC50 of 560-2600 nM.
Vanoxerine also is a potent hK(v)11.1 blocker, and at submicromolar concentrations.
Vanoxerine blocks Ca and Na currents in a strongly frequency-dependent manner possesses anticonvulsant activity in zebrafish and rodent models of generalized epilepsy but with cardiac ion channel effects.
Vanoxerine also is a cancer-specific downregulator of G9a expression, suppresses cancer stem cell functions in colon tumors.

Physicochemical Properties

M.Wt 450.5633
Formula C28H32F2N2O
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMSO: 9.4 mg/mL

Chemical Name/SMILES

Piperazine, 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)-, hydrochloride (1:2)

References

1. Teicher MH, et al. Brain Res. 1986 Nov;395(1):124-8.

2. Heikkila RE, et al. Eur J Pharmacol. 1984 Aug 17;103(3-4):241-8.

3. Lacerda AE, et al. J Cardiovasc Electrophysiol. 2010 Mar;21(3):301-10.

4. Goldsmith P, et al. Pharmacology. 2007;79(4):250-8.

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