L-365260 hemihydrate||-陌孚医药/Medlife

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L-365260 hemihydrate

目录号: PL01579 纯度: ≥99%

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中文名称	L-365260 hemihydrate
英文名称	L-365260 hemihydrate
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情	L-365260 hemihydrate 是一种口服有效的和选择性的非肽胃泌素和脑胆囊收缩素受体 (CCK-B) 拮抗剂，其 K_is 值分别为 1.9 nM 和 2.0 nM。L-365260 hemihydrate 以立体选择性和竞争性方式与豚鼠胃胃泌素和脑 CCK 受体相互作用。L-365260 hemihydrate 可增强 Morphine 缓解疼痛的活性，并防止 Morphine 耐受。
生物活性	L-365260 hemihydrate is an orally active and selective antagonist of non-peptide gastrin and brain cholecystokinin receptor (CCK-B), with K i s of 1.9 nM and 2.0 nM, respectively. L-365260 hemihydrate interacts in a stereoselective and competitive manner with guinea pig stomach gastrin and brain CCK receptors.
性状	Solid
IC50 & Target[1][2]	Ki: 1.9 nM (gastrin); 2.0 nM (CCK-B).
体外研究(In Vitro)	L-365260 hemihydrate 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. L-365260 (1 μM) hemihydrate strongly attenuates the CCK8S- and CCK4-mediated depolarization in a different neuron. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)	L-365260 hemihydrate (0.1-30 mg/kg; p.o.) antagonizes gastrin-stimulated acid secretion in mice (ED 50 =0.03 mg/kg), rats (ED 50 =0.9 mg/kg) and guinea pigs (ED 50 =5.1 mg/kg). L-365260 hemihydrate (0.01-10 mg/kg; s.c.) enhances analgesia induced by a submaximal dose of Morphine (4 mg/kg) in rats. L-365260 hemihydrate (0.2 mg/kg; s.c. twice daily for 5 days) significantly prolongs the duration of Morphine analgesia in rats. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Powder -20°C 3 years；4°C 2 years
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. [2]. 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.

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1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

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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