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Merck
CN

L4795

L-365260

≥98% (HPLC)

别名:

N-[(3R)-2,3-dihydro-1-methyl-2-oxo-5-phenyl-1H-1,4-benzodiazepin-3-yl]-N′-(3-methylphenyl)-urea

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关于此项目

经验公式(希尔记法):
C24H22N4O2
化学文摘社编号:
分子量:
398.46
UNSPSC Code:
12352202
PubChem Substance ID:
NACRES:
NA.77
Assay:
≥98% (HPLC)
Form:
solid
Storage condition:
desiccated
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assay

≥98% (HPLC)

form

solid

drug control

regulated under CDSA - not available from Sigma-Aldrich Canada

storage condition

desiccated

solubility

DMSO: >20 mg/mL

originator

Merck & Co., Inc., Kenilworth, NJ, U.S.

storage temp.

−20°C

SMILES string

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

Biochem/physiol Actions

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.

Features and Benefits

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.

pictograms

Skull and crossbonesEnvironment

signalword

Danger

hcodes

Hazard Classifications

Acute Tox. 3 Oral - Aquatic Acute 1

存储类别

6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

法规信息

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分析证书(COA)

Lot/Batch Number

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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
Yu-Mi Yang et al.
Life sciences, 79(18), 1702-1711 (2006-06-27)
The peptide cholecystokinin (CCK) is one of the major neurotransmitters modulating satiety, nociception, and anxiety behavior. Although many behavioral studies showing anti-analgesic and anxiogenic actions of CCK have been reported, less is known about its cellular action in the central

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