CGS 9343B

Names

[ Name ]:
CGS 9343B

Biological Activity

[Description]:

Zaldaride maleate (CGS-9343B) is a potent and selective inhibitor of calmodulin. Zaldaride maleate (CGS-9343B) inhibits CaM (calmodulin)-stimulated cAMP phosphodiesterase activity, with an IC50 of 3.3 nM[1][2]. Zaldaride maleate (CGS-9343B) prevents estrogen-induced transcription activation by ER, reversibly blocks voltage-activated Na+, Ca2+ and K+ currents in PC12 cells and inhibits nAChR[3].

[Related Catalog]:

Signaling Pathways >> Membrane Transporter/Ion Channel >> nAChR

Signaling Pathways >> Neuronal Signaling >> nAChR

Research Areas >> Neurological Disease

[Target]

IC50: 3.3 nM (calmodulin)[1][2].

[References]

[1]. Norman JA, et al. CGS 9343B, a novel, potent, and selective inhibitor of calmodulin activity. Mol Pharmacol. 1987 May;31(5):535-40.

[2]. Neuhaus R, et al. Inhibition of membrane currents and rises of intracellular Ca2+ in PC12 cells by CGS 9343B, a calmodulin inhibitor. Eur J Pharmacol. 1992 Jun 5;226(2):183-5.

[3]. Li L, et al. Calmodulin regulates the transcriptional activity of estrogen receptors. Selective inhibition of calmodulin function in subcellular compartments. J Biol Chem. 2003 Jan 10;278(2):1195-200.

Chemical & Physical Properties

[ Density]:
1.31g/cm3

[ Boiling Point ]:
778ºC at 760 mmHg

[ Molecular Formula ]:
C₃₀H₃₂N₄O₆

[ Molecular Weight ]:
544.60

[ Flash Point ]:
424.3ºC

[ Exact Mass ]:
544.23200

[ PSA ]:
129.79000

[ LogP ]:
3.85250

[ Vapour Pressure ]:
1.78E-25mmHg at 25°C

MSDS

Click to get detail MSDS

Safety Information

[ Hazard Codes ]:
Xi

[ RIDADR ]:
NONH for all modes of transport

Articles

Calcium Signaling Is Required for Erythroid Enucleation.

PLoS ONE 11 , e0146201, (2016)

Although erythroid enucleation, the property of erythroblasts to expel their nucleus, has been known for 7ore than a century, surprisingly little is known regarding the molecular mechanisms governing ...

The calmodulin inhibitor CGS 9343B inhibits voltage-dependent K(+) channels in rabbit coronary arterial smooth muscle cells.

Toxicol. Appl. Pharmacol. 285 , 207-13, (2015)

We investigated the effects of the calmodulin inhibitor CGS 9343B on voltage-dependent K(+) (Kv) channels using whole-cell patch clamp technique in freshly isolated rabbit coronary arterial smooth mus...

ATP hydrolysis is critically required for function of CaV1.3 channels in cochlear inner hair cells via fueling Ca2+ clearance.

J. Neurosci. 34(20) , 6843-8, (2014)

Sound encoding is mediated by Ca(2+) influx-evoked release of glutamate at the ribbon synapse of inner hair cells. Here we studied the role of ATP in this process focusing on Ca(2+) current through Ca...

Related Compounds

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