C1619
CGS-9343B
≥98% (HPLC), powder
别名:
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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所有图片(1)
About This Item
经验公式（希尔记法）:
C26H28N4O2 · C4H4O4
CAS号:
分子量:
544.60
MDL號碼:
分類程式碼代碼:
12352200
PubChem物質ID:
NACRES:
NA.77
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品質等級
化驗
≥98% (HPLC)
形狀
powder
顏色
white to off-white
溶解度
DMSO: >10 mg/mL
起源
Novartis
儲存溫度
2-8°C
SMILES 字串
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 密鑰
NGODOSILXOFQPH-BTJKTKAUSA-N
生化／生理作用
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.
特點和優勢
This compound was developed by Novartis. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.
儲存類別代碼
11 - Combustible Solids
水污染物質分類（WGK）
WGK 3
閃點（°F）
Not applicable
閃點（°C）
Not applicable
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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