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N-type calcium channel blocker-1

Catalog No. T12153Cas No. 241499-17-2

N-type calcium channel blocker-1 is an orally active analgesic agent with a high affinity for functionally blocking N-type calcium channels.

N-type calcium channel blocker-1

N-type calcium channel blocker-1

Catalog No. T12153Cas No. 241499-17-2
N-type calcium channel blocker-1 is an orally active analgesic agent with a high affinity for functionally blocking N-type calcium channels.
Pack SizePriceAvailabilityQuantity
25 mg$1,8208-10 weeks
50 mg$2,3808-10 weeks
100 mg$3,1008-10 weeks
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Product Introduction

Bioactivity
Description
N-type calcium channel blocker-1 is an orally active analgesic agent with a high affinity for functionally blocking N-type calcium channels.
Targets&IC50
Ca2+ channel, N-type:0.7 μM
In vitro
N-type calcium channel blocker-1, the most orally active compound in its series for analgesia, demonstrates significant activity in the IMR32 assay with an 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)
Chemical Properties
Molecular Weight461.73
FormulaC31H47N3
Cas No.241499-17-2
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

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