Chemical Structure : Vatinoxan hydrochloride
CAS No.:
130466-38-5
Vatinoxan hydrochloride
(MK-467, L-659066)
Catalog No.: PC-25616Not For Human Use, Lab Use Only.
Vatinoxan hydrochloride (MK-467, L-659066) is a potent and selective alpha-2 adrenoceptor (α2A adrenoceptor, α2AR) antagonist with IC50 of 3 nM against the binding of [3H]rauwolscine to rat cerebrocortical membranes, selective over alpha-1 adrenoceptors.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
Vatinoxan hydrochloride (MK-467, L-659066) is a potent and selective alpha-2 adrenoceptor (α2A adrenoceptor, α2AR) antagonist with IC50 of 3 nM against the binding of [3H]rauwolscine to rat cerebrocortical membranes, selective over alpha-1 adrenoceptors.
Vatinoxan has a pA2 of 8.44 at alpha-2 adrenoceptors in the isolated rat vas deferens.
Vatinoxan inhibits the predominately peripherally mediated inhibition of colonic propulsion caused by clonidine in vivo.
Vatinoxan increases sympathetically mediated NE release and catecholamine turnover due to inhibition of presynaptic alpha 2-receptors as well as due to reflexive sympathetic activation related to blockade of alpha 2-receptors on arterial smooth muscle cells.
Physicochemical Properties
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M.Wt
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454.97
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Formula
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C20H27ClN4O4S
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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Methanesulfonamide,N-[2-[(2R,12bS)-1,3,4,6,7,12b-hexahydro-2'-oxospiro[2H-benzofuro[2,3-a]quinolizine-2,4'-imidazolidin]-3'-yl]ethyl]-,hydrochloride (1:1)
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References
1. Clineschmidt BV, et al. J Pharmacol Exp Ther. 1988 Apr;245(1):32-40.
2. Szemeredi K, et al. Eur J Pharmacol. 1989 Oct 24;170(1-2):53-9.
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