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Merck
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Key Documents

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C1619

Sigma-Aldrich

CGS-9343B

≥98% (HPLC), powder

Sinonimo/i:

1,3-Dihydro-1-[1-[(4-methyl-4H,6H-pyrrolo[1,2-a][4,1]- benzoxazepin-4-yl)methyl]-4-piperidinyl]-2H-benzimidazol-2-one maleate, CGS9343B, KW-5617, Zaldaride maleate

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About This Item

Formula empirica (notazione di Hill):
C26H28N4O2 · C4H4O4
Numero CAS:
109826-27-9
Peso molecolare:
544.60
Numero MDL:
MFCD04113002
Codice UNSPSC:
12352200
ID PubChem:
329774899
NACRES:
NA.77

Saggio

≥98% (HPLC)

Forma fisica

powder

Colore

white to off-white

Solubilità

DMSO: >10 mg/mL

Ideatore

Novartis

Temperatura di conservazione

2-8°C

Stringa SMILE

OC(=O)\C=C/C(O)=O.CC4(CN1CCC(CC1)N2C(=O)Nc3ccccc23)OCc5ccccc5-n6cccc46

InChI

1S/C26H28N4O2.C4H4O4/c1-26(24-11-6-14-29(24)22-9-4-2-7-19(22)17-32-26)18-28-15-12-20(13-16-28)30-23-10-5-3-8-21(23)27-25(30)31;5-3(6)1-2-4(7)8/h2-11,14,20H,12-13,15-18H2,1H3,(H,27,31);1-2H,(H,5,6)(H,7,8)/b;2-1-
NGODOSILXOFQPH-BTJKTKAUSA-N

Azioni biochim/fisiol

CGS-9343B is a selective calmodulin antagonist with minimal protein kinase C or antidopaminergic activity. CGS-9343B is a potent inhibitor of calmodulin-activated (Type I) phosphodiesterase activity with IC50 in the nanomolar range.

Caratteristiche e vantaggi

This compound was developed by Novartis. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.

Codice della classe di stoccaggio

11 - Combustible Solids

Classe di pericolosità dell'acqua (WGK)

WGK 3

Punto d’infiammabilità (°F)

Not applicable

Punto d’infiammabilità (°C)

Not applicable

Certificati d'analisi (COA)

Cerca il Certificati d'analisi (COA) digitando il numero di lotto/batch corrispondente. I numeri di lotto o di batch sono stampati sull'etichetta dei prodotti dopo la parola ‘Lotto’ o ‘Batch’.

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N Aikawa et al.
Japanese journal of pharmacology, 83(3), 269-272 (2000-08-22)
The effect of zaldaride, a calmodulin inhibitor, on 16,16-dimethyl prostaglandin E2 (dmPGE2)-induced intestinal ion secretion was investigated in rats. Zaldaride inhibited the dmPGE2-induced increase in water content in the colon, but not that in the small intestine. In the colonic
Lu Li et al.
The Journal of biological chemistry, 278(2), 1195-1200 (2002-11-07)
The steroid hormone estrogen elicits biological effects in cells by binding to and activating the estrogen receptor (ER). Estrogen binding induces a conformational change in the receptor, inducing nuclear translocation and transcriptional activation of ER. The ubiquitous Ca(2+)-binding protein calmodulin
L Glass-Marmor et al.
European journal of pharmacology, 328(2-3), 241-248 (1997-06-11)
Glycolysis, which is the primary energy source in cancer cells, is known to be controlled by allosteric regulators, as well as by reversible binding of glycolytic enzymes to cytoskeleton. We have previously found that different calmodulin antagonists decrease the levels
N Aikawa et al.
Japanese journal of pharmacology, 81(4), 397-400 (2000-02-11)
The antidiarrheal action of zaldaride maleate (ZAL) after oral, intravenous and subcutaneous administration was examined to determine whether ZAL acts systemically or locally in the intestine of rats. Oral administration of ZAL inhibited castor oil- and 16,16-dimethyl prostaglandin E2-induced diarrhea;
N Aikawa et al.
Japanese journal of pharmacology, 83(1), 86-88 (2000-07-11)
The effect of zaldaride maleate (ZAL) on intracellular Ca2+-mediated short-circuit current (Isc) response in rat colonic mucosa was investigated. The Isc response to acetylcholine was partially reduced by the neuronal blocker tetrodotoxin. The tetrodotoxin-sensitive Isc response to acetylcholine was inhibited
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