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C1619

Sigma-Aldrich

CGS-9343B

≥98% (HPLC), powder

Sinónimos:

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

Fórmula empírica (notación de Hill):
C26H28N4O2 · C4H4O4
Número de CAS:
109826-27-9
Peso molecular:
544.60
MDL number:
MFCD04113002
UNSPSC Code:
12352200
PubChem Substance ID:
329774899
NACRES:
NA.77

Quality Level

100

assay

≥98% (HPLC)

form

powder

color

white to off-white

solubility

DMSO: >10 mg/mL

originator

Novartis

storage temp.

2-8°C

SMILES string

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-

InChI key

NGODOSILXOFQPH-BTJKTKAUSA-N

Biochem/physiol Actions

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.

Features and Benefits

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

Storage Class

11 - Combustible Solids

wgk_germany

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

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Certificados de análisis (COA)

Lot/Batch Number
021M4724V

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N Aikawa et al.
Japanese journal of pharmacology, 76(2), 199-206 (1998-04-16)
KW-5617 (zaldaride maleate), 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, is a selective calmodulin inhibitor. We studied the effects of KW-5617 on secretory diarrhea and gastrointestinal propulsion in rats, as compared with those of loperamide, a conventional anti-diarrheal drug. Diarrhea was induced in rats
P Yu et al.
The American journal of physiology, 275(2 Pt 1), G203-G211 (1998-08-04)
The signal transduction that mediates CCK-induced contraction of gallbladder muscle was investigated in the cat. Contraction was measured by scanning micrometry in single muscle cells isolated enzymatically with collagenase. Production of D-myo-inositol 1,4, 5-trisphosphate (IP3) and sn-1,2-diacylglycerol (DAG) was quantitated
R N Fedorak et al.
Journal of pediatric gastroenterology and nutrition, 8(2), 252-258 (1989-02-01)
In this study, the effect of CGS 9343B on cholera-toxin-stimulated intestinal secretion in rats was determined using in vivo isolated loops. This recently developed compound is a potent and specific inhibitor of calmodulin, but not of protein kinase C. At
J H Lin et al.
European journal of pharmacology, 397(1), 11-17 (2000-06-14)
The effects of CGS 9343B (zaldaride maleate), a calmodulin antagonist, on mechanosensitive channels were examined in crayfish slowly adapting sensory neurons using the two-electrode voltage clamp technique. In addition to its inhibition of voltage-gated Na(+) and K(+) currents, CGS 9343B
Z Li et al.
The Journal of biological chemistry, 276(20), 17354-17360 (2001-03-30)
The estrogen receptor mediates breast cell proliferation and is the principal target for chemotherapy of breast carcinoma. Previous studies have demonstrated that the estrogen receptor binds to calmodulin-Sepharose in vitro. However, the association of endogenous calmodulin with endogenous estrogen receptors
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