118101-09-0|L-365,260，≥98%|Medlife|Medlife为MCE，Selleck，麦克林，阿拉丁试剂，罗恩试剂，Sigma，安耐吉试剂，泰坦等同类产品品牌，上海现货，高性价比小分子化合物

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L-365,260

胆囊收缩素受体2（CCK2）拮抗剂,A potent, selective, orally active cholecystokinin receptor 2 (CCK2) antagonist with IC50 of 2 nM

目录号: PC11278 纯度: ≥98%

CAS No. :118101-09-0

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中文名称

L-365,260

英文名称

L-365,260

英文别名

Urea,N-[(3R)-2,3-dihydro-1-methyl-2-oxo-5-phenyl-1H-1,4-benzodiazepin-3-yl]-N'-(3-methylphenyl)-;L 365260;N-[(3R)-2,3-dihydro-1-methyl-2-oxo-5-phenyl-1H-1,4-benzodiazepin-3-yl]-N′-(3-methylphenyl)-urea;Urea,N-[(3R)-2,3-dihydro-1-methyl-2-oxo-5-phenyl-1H-1,4-benzodiazepin-3-yl]-N'-(3-methylphenyl...;L-365,260,N-[(3R)-2,3-Dihydro-1-methyl-2-oxo-5-phenyl-1H-1,4-benzodiazepin-3-yl]-N'-(3-methylphenyl)urea;N-[(3R)-2,3-Dihydro-1-Methyl-2-oxo-5-phenyl-1H-1,4-benzodiazepin-3-yl]-N'-(3-Methylphenyl)urea;MSD-365260;(3R)-1-Methyl-3-[3-(3-methylphenyl)ureido]-5-phenyl-1H-1,4-benzodiazepin-2(3H)-one;1-[[(3R)-2,3-Dihydro-1-methyl-2-oxo-5-phenyl-1H-1,4-benzodiazepin]-3-yl]-3-(3-methylphenyl)urea;(+)-1-[[(3R)-2,3-Dihydro-1-methyl-2-oxo-5-phenyl-1H-1,4-benzodiazepin]-3-yl]-3-(3-methylphenyl)urea;(+)-N-[[(3R)-2,3-Dihydro-1-methyl-2-oxo-5-phenyl-1H-1,4-benzodiazepin]-3-yl]-N'-(3-methylphenyl)urea;370JHF4586;N-((3R)-2,3-dihydro-1-methyl-2-oxo-5-phenyl-1H-1,4-benzodiazepin-3-yl)-N'-(3-methylphenyl)urea;L365260;BDBM81962;PDSP1_000921;PDSP2_000907;1-[(3R)-1-methyl-2-oxo-5-phenyl-3H-1,4-benzodiazepin-3-yl]-3-(3-methylphenyl)urea;B7181;C15026

Cas No.

118101-09-0

分子式

C₂₄H₂₂N₄O₂

分子量

398.46

包装储存

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

生物活性

L-365260 is an orally active and selective antagonist of non-peptide gastrin and brain cholecystokinin receptor (CCK-B), with K_is of 1.9 nM and 2.0 nM, respectively. L-365260 interacts in a stereoselective and competitive manner with guinea pig stomach gastrin and brain CCK receptors. L-365260 can enhance Morphine analgesia and prevents Morphine tolerance.

性状

Solid

IC50 & Target[1][2]

CCKBR

体外研究(In Vitro)

L-365260 (1 μM) strongly attenuates the CCK8S- and CCK4-mediated depolarization in a different neuron.
L-365260 exhibits a similar high affinity for brain CCK-B receptors of rats, mice and man, and a lower affinity for gastrin and brain CCK-B (IC₅₀=20-40 nM) receptors in dog tissues.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

L-365260 (0.01-10 mg/kg; s.c.) enhances analgesia induced by a submaximal dose of Morphine (4 mg/kg) in rats.
L-365260 (0.2 mg/kg; s.c. twice daily for 5 days) significantly prolongs the duration of Morphine analgesia in rats.
L-365260 (0.1-30 mg/kg; p.o.) antagonizes gastrin-stimulated acid secretion in mice (ED₅₀=0.03 mg/kg), rats (ED₅₀=0.9 mg/kg) and guinea pigs (ED₅₀=5.1 mg/kg).

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Male Sprague-Dawley rats (300-350 g) were injected with Morphine
Dosage:	0.01, 0.05, 0.1, 0.2, 0.75, 1.0, 10.0 mg/kg
Administration:	S.c. 10 min prior to i.p. injection of 4 mg/kg Morphine
Result:	Enhanced morphine analgesia.

运输条件

Room temperature or refrigerated transportation.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

参考文献

[1]. Lotti VJ, et, al. A new potent and selective non-peptide gastrin antagonist and brain cholecystokinin receptor (CCK-B) ligand: L-365,260. Eur J Pharmacol. 1989 Mar 21;162(2):273-80. [Information]

[2]. Chung L, et, al. Cholecystokinin action on layer 6b neurons in somatosensory cortex. Brain Res. 2009 Jul 28;1282:10-9. [Information]

[3]. Dourish CT, et, al. The selective CCK-B receptor antagonist L-365,260 enhances morphine analgesia and prevents morphine tolerance in the rat. Eur J Pharmacol. 1990 Jan 25;176(1):35-44. [Information]

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Data Sheet

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2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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