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N-type calcium channel blocker-1

Catalog No. T12153 CAS 241499-17-2

N-type calcium channel blocker-1 is an orally active analgesic agent,shows high affinity to functionally block N-type calcium channels.

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N-type calcium channel blocker-1 Chemical Structure

N-type calcium channel blocker-1, CAS 241499-17-2

Pack Size	Availability	Price/USD
25 mg	8-10 weeks	$ 1,820.00
50 mg	8-10 weeks	$ 2,380.00
100 mg	8-10 weeks	$ 3,100.00

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This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.

Biological Description

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Description	N-type calcium channel blocker-1 is an orally active analgesic agent,shows high affinity to functionally block N-type calcium channels.
Targets&IC50	Ca2+ channel, N-type:0.7 μM
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)

Molecular Weight	461.73
Formula	C31H47N3
CAS No.	241499-17-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

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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Keywords

N-type calcium channel blocker-1 241499-17-2 Membrane transporter/Ion channel Metabolism Calcium Channel N type calcium channel blocker 1 Ntype calcium channel blocker1 inhibitor inhibit

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