N-type calcium channel blocker-1 Bioactivity,Chemical Properties,Storage & Solubility Information Pathways-PeptideDB

Description	N-type calcium channel blocker-1 is an orally active analgesic agent,shows high affinity to functionally block N-type calcium channels.
In vitro	N-type calcium channel blocker-1 is the most orally active blocker of N-type calcium channel for analgesia found in a series of compounds.N-type calcium channel blocker-1 shows good activities in the IMR32 assay with IC50 of 0.7 μM[1].
In vivo	A time course study of N-type calcium channel blocker-1 in the anti-writhing model indicates that the CF-1 mice have maximal effect at 120 min after oral dosing at 60 mg/kg.?Further evaluation of N-type calcium channel blocker-1 demonstrates several important and advantageous features: the pharmacokinetic profile of N-type calcium channel blocker-1 is improved (Versus of 5.9 L/kg and CL of 26 mL/min/kg) and the logPn of 26 is favorable for CNS agent (logPn measured to be 3.20)
Target activity	Ca2+ channel, N-type:0.7 μM
molecular weight	461.73
Molecular formula	C31H47N3
CAS	241499-17-2
Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year
References	1. Hu LY, et al. The discovery of [1-(4-dimethylamino-benzyl)-piperidin-4-yl]-[4-(3,3-dimethylbutyl)-phen yl]-(3-methyl-but-2-enyl)-amine, an N-type Ca+2 channel blocker with oral activity for analgesia. Bioorg Med Chem. 2000 Jun;8(6):1203-12.

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