方案
≥98% (HPLC)
表单
solid
药品控制
regulated under CDSA - not available from Sigma-Aldrich Canada
储存条件
desiccated
溶解性
DMSO: >20 mg/mL
创始人
Merck & Co., Inc., Kenilworth, NJ, U.S.
储存温度
−20°C
SMILES字符串
CN1C[C@H](NC(=O)Nc2cccc(C)c2)N=C(c3ccccc3)c4ccccc14
InChI
1S/C24H24N4O/c1-17-9-8-12-19(15-17)25-24(29)27-22-16-28(2)21-14-7-6-13-20(21)23(26-22)18-10-4-3-5-11-18/h3-15,22H,16H2,1-2H3,(H2,25,27,29)/t22-/m0/s1
InChI key
LIVVMCBMGZZRRY-QFIPXVFZSA-N
生化/生理作用
L-365260 is a CCK2 selective antagonist.
L-365260 is a CCK2 selective antagonist. Enhances amphetamine-induced stimulation of locomotor activity in rats (a model of drug abuse), inhibits thyroid carcinoma (TT)-cell proliferation (potential therapeutic implication for cancer treatment); bilateral injection into the medulla reverses both tactile allodynia and thermal hyperalgesia.
特点和优势
This compound is featured on the Cholecystokinin and Gastrin Receptors page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.
This compound was developed by Merck & Co., Inc., Kenilworth, NJ, U.S.. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.
警示用语：
Danger
危险声明
危险分类
Acute Tox. 3 Oral - Aquatic Acute 1
储存分类代码
6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
Jun Cao et al.
Zhonghua yi xue za zhi, 87(24), 1704-1708 (2007-09-11)
To explore the molecular mechanism of increasing the invasion of colon cancer cells by gastrin 17. The plasmid pCR 3.1/GR expressing the gastrin receptor cholecystokinin-2 receptor (CCK-2R) was transfected into colonic carcinoma cells of the line Colo320 by Lipofectamine 2000.
Kristiina Roots et al.
International journal of developmental neuroscience : the official journal of the International Society for Developmental Neuroscience, 24(6), 395-400 (2006-07-11)
This study provides the first evidence that CCK-8 (0.01 pM to 0.1 mM) stimulates Na,K-ATPase in the cortical membranes of wild-type and CCK(2) receptor-deficient mice. In each genotype, the maximal stimulation was about 40%. Homozygous mice revealed substantially lower EC50
Cheng Huang et al.
Brain research bulletin, 71(5), 447-451 (2007-01-30)
Cholecystokinin octapeptide (CCK-8) is a physiological antagonist of endogenous opioids in the central nervous system (CNS). Our previous work has shown that CCK-8 plays an important role in the development of tolerance to morphine analgesia and electroacupuncture (EA) analgesia in
O Kasimay et al.
Journal of physiology and pharmacology : an official journal of the Polish Physiological Society, 56(4), 543-553 (2006-01-05)
Pineal hormone melatonin is proposed as a potential treatment for severe sleep disturbances, and various gastrointestinal disorders. It was shown that melatonin increases intestinal motility and influences the activity of myoelectric complexes of the gut. The aim of the study
Hong-Gang Yu et al.
International journal of cancer, 119(12), 2724-2732 (2006-09-26)
Focal adhesion kinase (FAK) is suggested to be intimately involved in the progression of malignancies. Our previous research has demonstrated that activation of cholecystokinin-2 receptor (CCK2R) by gastrin stimulates a rapid activation of FAK pathway in human colon cancer cells.
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