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Cat. No.: HY-100310

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N-type calcium channel blocker-1

N-type calcium channel blocker-1 is an orally active compound which shows high affinity to functionally block N-type calcium channels with an IC₅₀ of 0.7 μM in the IMR32 assay.

For research use only. We do not sell to patients.

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

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (274 KB)

N-type calcium channel blocker-1 Chemical Structure

CAS No.: 241499-17-2

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
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Biological Activity

Description

N-type calcium channel blocker-1 is an orally active compound which shows high affinity to functionally block N-type calcium channels with an IC₅₀ of 0.7 μM in the IMR32 assay.

IC₅₀ & Target

IC50: 0.7 μM (N-type calcium channels)^[1]

All Calcium Channel Isoforms :

In Vitro

N-type calcium channel blocker-1 shows good activities in the IMR32 assay (IC₅₀=0.7 μM). N-type calcium channel blocker-1 is the most orally active N-type calcium channel blocker for analgesia found in a series of compounds^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

N-type calcium channel blocker-1 shows good activities in the acetic acid anti-writhing model (ED₅₀=4 mg/kg, iv). N-type calcium channel blocker-1 exhibits oral activity (ED₅₀=12 mg/kg, po). 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)^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

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

C/C(C)=C\CN(C1=CC=C(CCC(C)(C)C)C=C1)C2CCN(CC3=CC=C(N(C)C)C=C3)CC2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (274 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

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. [Content Brief]

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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