Zaldaride
Zaldaride (CGS-9343B free base) is a potent, orally active and selective inhibitor of calmodulin. Zaldaride inhibits CaM (calmodulin)-stimulated cAMP phosphodiesterase activity, with an IC50 of 3.3 nM. Zaldaride prevents estrogen-induced transcription activation by ER, reversibly blocks voltage-activated Na+, Ca2+ and K+ currents in PC12 cells and inhibits nAChR.
For research use only. We do not sell to patients.
- CAS No.: 109826-26-8
- Formula: C26H28N4O2
- Molecular Weight:428.53
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Sprague-dawley rats neighing 193-265 g[4].
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Dosage:3-100 mg/kg.
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Administration:P.O..
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Result:Ameliorated the DMPGE-induced diarrhea.
Delayed the onset of diarrhe and reduced or abolished the incidence of diarrhea.
Chemical Information
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CAS No. 109826-26-8
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Molecular Weight 428.53
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Formula C26H28N4O2
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SMILES
O=C1NC2=C(N1C3CCN(CC4(C)OCC5=C(N6C=CC=C64)C=CC=C5)CC3)C=CC=C2
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Synonyms
CGS-9343B free base; KW 5617 free base
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
[4]. Aikawa N, et al. Effects of KW-5617 (zaldaride maleate), a potent and selective calmodulin inhibitor, on secretory diarrhea and on gastrointestinal propulsion in rats. Jpn J Pharmacol. 1998 Feb;76(2):199-206. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)