检测方案
≥98% (HPLC)
形式
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. 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
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
法规信息
新产品
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
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.
Dan Li et al.
Ai zheng = Aizheng = Chinese journal of cancer, 27(1), 41-45 (2008-01-11)
Gastrin contributes to the growth and proliferation of gastric cancer cells and it is related to the effect of tyrosine kinase. This study was to investigate the effect of gastrin on tyrosine phosphorylation of focal adhesion kinase (FAK) in human
Jennifer M Mitchell et al.
Pharmacology, biochemistry, and behavior, 85(4), 787-795 (2007-01-02)
There is evidence that the neuropeptide cholecystokinin (CCK) is important for the rewarding effects of drugs of abuse. However, less is known regarding the role of CCK in drug seeking and craving. The present study investigated whether the CCK(B) antagonist
Mei Ming et al.
Zhonghua zhong liu za zhi [Chinese journal of oncology], 29(1), 4-8 (2007-06-20)
To study the effect of gastrin on the mRNA and protein expression of urokinase-type plasminogen activator (u-PA) in human colon cancer cells and detect the role of p38 MAPK in this process. Lipofectin method was used to transfect pCR3. 1/CCK2R
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