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N-type calcium channel blocker-1

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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

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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 SizePriceUSA WarehouseGlobal WarehouseQuantity
25 mg$1,8208-10 weeks8-10 weeks
50 mg$2,3808-10 weeks8-10 weeks
100 mg$3,1008-10 weeks8-10 weeks
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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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
SmilesN(CC=C(C)C)(C1CCN(CC2=CC=C(N(C)C)C=C2)CC1)C3=CC=C(CCC(C)(C)C)C=C3
Relative Density.1.013 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
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2 Enter the in vivo formulation:
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%
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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

Keywords

N-type calcium channelsN-type calcium channel blocker-1Ntype calcium channel blocker1N type calcium channel blocker 1CalciumChannelCalcium Channel
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