C1619
CGS-9343B
≥98% (HPLC), powder
동의어(들):
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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크기 선택
제품정보 (DICE 배송 시 비용 별도)
실험식(Hill 표기법):
C26H28N4O2 · C4H4O4
CAS 번호:
Molecular Weight:
544.60
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
12352200
MDL number:
InChI key
NGODOSILXOFQPH-BTJKTKAUSA-N
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-
assay
≥98% (HPLC)
form
powder
color
white to off-white
solubility
DMSO: >10 mg/mL
originator
Novartis
storage temp.
2-8°C
Quality Level
Biochem/physiol Actions
CGS-9343B is a calmodulin antagonist.
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.
저장 등급
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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
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
M Ashkenazy-Shahar et al.
Molecular genetics and metabolism, 65(3), 213-219 (1998-12-16)
We report here a novel mechanism of insulin action in cultures of NIH-3T3 fibroblasts. Our experiments revealed that in these cells, insulin induced a rapid and transient increase in cytoskeleton-bound phosphofructokinase (EC 2.7.1.11), the rate-limiting enzyme in glycolysis, with a
N Aikawa et al.
Japanese journal of pharmacology, 82(4), 350-352 (2000-06-30)
The effect of zaldaride, a calmodulin inhibitor, on fecal pellet output in rats was compared with that of loperamide, an antidiarrheal drug. 5-Hydroxytryptamine (10 mg/kg, s.c.), neostigmine (0.3 mg/kg, s.c.) and nicotine (1.0 mg/kg, s.c.) increased fecal pellet output. Zaldaride
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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