Zaldaride maleate
Based on 1 Customer Validation
Zaldaride maleate (CGS-9343B) is a potent, orally active and selective inhibitor of calmodulin. Zaldaride maleate inhibits CaM (calmodulin)-stimulated cAMP phosphodiesterase activity, with an IC50 of 3.3 nM. Zaldaride maleate 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.
- Purity : 99.7%
- CAS No.: 109826-27-9
- Formula: C30H32N4O6
- Molecular Weight:544.60
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Biological Activity
Description
IC50 & Target
In Vivo
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. 109826-27-9
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Appearance Solid
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Molecular Weight 544.60
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Formula C30H32N4O6
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Color White to off-white
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SMILES
O=C(O)/C=C\C(O)=O.CC1(C2=CC=CN2C3=CC=CC=C3CO1)CN4CCC(N5C6=C(C=CC=C6)NC5=O)CC4
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Synonyms
CGS-9343B; KW 5617
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Research Protocol for Endocrine Diseases
Endocrine diseases often arise from disrupted hormone production, hormone signaling, or target-tissue responsiveness; for diabetes-focused endocrine disease models, insulin signaling regulates glucose uptake, hepatic glucose output, lipid metabolism, and β-cell compensation. Type 2 diabetes develops through interacting defects in insulin resistance, β-cell dysfunction, adipose inflammation, hepatic glucose overproduction, altered incretin signaling, and ectopic lipid metabolism. A major unresolved question is whether endocrine dysfunction is driven primarily by target-tissue insulin resistance, intrinsic β-cell failure, immune/inflammatory stress, or combined multi-organ failure that differs by disease stage.
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Ca2+ Staining Technique
Ca2+ staining is an experimental technique that utilizes specific fluorescent probes (such as Fluo-4 AM, Fura-2, etc.) to qualitatively or quantitatively detect dynamic changes in intracellular Ca2+ concentrations; this is achieved by monitoring the changes in fluorescent signals generated when these probes bind to free intracellular calcium ions. The underlying principle relies primarily on the presence of chelating groups within the probe's molecular structure that possess high affinity for calcium ions.
Purity & Documentation
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Data Sheet (274 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
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)