2. GPCR/G Protein Neuronal Signaling
  3. Cholecystokinin Receptor
  4. L-365260 hemihydrate

L-365260 hemihydrate 

目录号: HY-106840A 纯度: 99.75%
COA 产品使用指南

摩尔计算器

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 Kis 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。

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L-365260 hemihydrate Chemical Structure

L-365260 hemihydrate Chemical Structure

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规格 价格 是否有货 数量
5 mg ￥1860
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Customer Review

Other Forms of L-365260 hemihydrate:

L-365260 hemihydrate 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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 Kis 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[1][2][3].

IC50 & Target

Ki: 1.9 nM (gastrin); 2.0 nM (CCK-B)[1].
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[1].
L-365260 (1 μM) hemihydrate strongly attenuates the CCK8S- and CCK4-mediated depolarization in a different neuron[2].

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

L-365260 hemihydrate 相关抗体:
体内研究
(In Vivo)

L-365260 hemihydrate (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)[1].
L-365260 hemihydrate (0.01-10 mg/kg; s.c.) enhances analgesia induced by a submaximal dose of Morphine (4 mg/kg) in rats[3].
L-365260 hemihydrate (0.2 mg/kg; s.c. twice daily for 5 days) significantly prolongs the duration of Morphine analgesia in rats[3].

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

Animal Model: Male Sprague-Dawley rats (300-350 g; Morphine- injected)[3].
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.
分子量

407.47

Formula

C24H24N4O3
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

纯度 & 产品资料
参考文献

L-365260 hemihydrate 相关分类

  • 摩尔计算器

  • 稀释计算器

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

L-365260 hemihydrateCholecystokinin ReceptorCCK ReceptorgastrinbraincholecystokininCCK-BanalgesiaInhibitorinhibitorinhibit

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目录号：
HY-106840A
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