L-365260 ≥98%
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| 包装规格: | 1mg 5mg 10mg 25mg in glass bottle |
| 产品描述: | 基本信息 产品编号: L60016 产品名称: L-365260 CAS: 118101-09-0 储存条件 粉末 -20℃ 四年 分子式: C24H22N4O2 溶于液体 -80℃ 二年 分子量: 398.46 化学名: N-[(3R)-2,3-Dihydro-1-methyl-2-oxo-5-phenyl-1H-1,4-benzodiazepin-3-yl]-N'-(3-methylphenyl)urea Solubility (25°C): 体外: DMSO Ethanol Water 体内(现配现用): <1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;⼀旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 生物活性 产品描述 一种有效和选择性的非肽胃泌素和脑胆囊收缩素受体 (CCK-B) 拮抗剂。 靶点 Ki:1.9nM (gastrin);2.0nM (CCK-B) 体外研究 L-365260 (1μM) 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=20-40nM) receptors in dog tissues. 体内研究 L-365260 (0.01-10mg/kg;s.c.) enhances analgesia induced by a submaximal dose of Morphine (4mg/kg) in rats.L-365260 (0.2mg/kg;s.c.twice daily for 5 days) significantly prolongs the duration of Morphine analgesia in rats.L-365260 (0.1-30mg/kg;p.o.) antagonizes gastrin-stimulated acid secretion in mice (ED50=0.03mg/kg),rats (ED50=0.9mg/kg) and guinea pigs (ED50=5.1mg/kg). Animal Model: Male Sprague-Dawley rats (300-350g) were injected with Morphine. Dosage: 0.01,0.05,0.1,0.2,0.75,1.0,10.0mg/kg Administration: S.c.10 min prior to i.p.injection of 4mg/kg Morphine Result: Enhanced morphine analgesia. |
| 保存条件: | -20℃ |
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