Ca2+ channel agonist 1

Modify Date: 2024-01-05 17:28:35

Ca2+ channel agonist 1 Structure
Ca2+ channel agonist 1 structure
Common Name Ca2+ channel agonist 1
CAS Number 1402821-24-2 Molecular Weight 354.45
Density N/A Boiling Point N/A
Molecular Formula C19H26N6O Melting Point N/A
MSDS N/A Flash Point N/A

 Use of Ca2+ channel agonist 1


Ca2+ channel agonist 1 is an agonist of N-type Ca2+ channel and an inhibitor of Cdk2, with EC50s of 14.23 μM and 3.34 μM, respectively, and is used as a potential treatment for motor nerve terminal dysfunction.

 Names

Name Ca2+ channel agonist 1

 Ca2+ channel agonist 1 Biological Activity

Description Ca2+ channel agonist 1 is an agonist of N-type Ca2+ channel and an inhibitor of Cdk2, with EC50s of 14.23 μM and 3.34 μM, respectively, and is used as a potential treatment for motor nerve terminal dysfunction.
Related Catalog
Target

CDK2:3.34 μM (EC50)

N-Type Ca2+ Channel:14.23 μM (EC50)

In Vitro Ca2+ channel agonist 1 (Compound 13d) is an agonist of N-type Ca2+ channel and an inhibitor of Cdk2, with EC50s of 14.23 μM and 3.34 μM, respectively. Ca2+ channel agonist 1 exhibits a ca. 2-fold increased agonism and a 22-fold decreased cdk2 kinase activity versus the standard, (R)-roscovitine[1].
Cell Assay Briefly, the pipet solution consists of 70 nM Cs2SO4, 60 mM CsCl, 1 mM MgCl2, and 10 mM HEPES at pH 7.4. Cultured cells are bathed in a saline composed of 130 mM choline chloride (ChCl), 10 mM tetraethylammonium chloride (TEA-Cl), 2 mM CaCl2, 1 mM MgCl2, and 10 mM HEPES at pH 7.4. Patch pipettes are fabricated from borosilicate glass, and capacitive currents and passive membrane responses to voltage commands are subtracted. Currents are amplified by an amplifier, filtered at 5 kHz, and digitized at 10 kHz for subsequent analysis. A liquid junction potential of −11.3 mV is subtracted during recordings. To measure effects on calcium channel tail currents, the tail current integral is measured before and after application of a derivative (including Ca2+ channel agonist 1), with the integral of each trace being normalized to its peak.
References

[1]. Liang M, et al. Synthesis and biological evaluation of a selective N- and p/q-type calcium channel agonist. ACS Med Chem Lett. 2012 Oct 1;3(12):985-990.

 Chemical & Physical Properties

Molecular Formula C19H26N6O
Molecular Weight 354.45
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