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

L-365260 hemihydrate 

目录号: HY-106840A 纯度: 99.75%
COA 产品使用指南

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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5 mg ¥1860
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Other Forms of L-365260 hemihydrate:

MCE 顾客使用本产品发表的 1 篇科研文献

查看 Cholecystokinin Receptor 亚型特异性产品:

  • 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.

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)

溶解性数据
细胞实验: 

DMSO 中的溶解度 : 50 mg/mL (122.71 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.4542 mL 12.2708 mL 24.5417 mL
5 mM 0.4908 mL 2.4542 mL 4.9083 mL
查看完整储备液配制表

* 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
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

完整储备液配制表

* 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
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.4542 mL 12.2708 mL 24.5417 mL 61.3542 mL
5 mM 0.4908 mL 2.4542 mL 4.9083 mL 12.2708 mL
10 mM 0.2454 mL 1.2271 mL 2.4542 mL 6.1354 mL
15 mM 0.1636 mL 0.8181 mL 1.6361 mL 4.0903 mL
20 mM 0.1227 mL 0.6135 mL 1.2271 mL 3.0677 mL
25 mM 0.0982 mL 0.4908 mL 0.9817 mL 2.4542 mL
30 mM 0.0818 mL 0.4090 mL 0.8181 mL 2.0451 mL
40 mM 0.0614 mL 0.3068 mL 0.6135 mL 1.5339 mL
50 mM 0.0491 mL 0.2454 mL 0.4908 mL 1.2271 mL
60 mM 0.0409 mL 0.2045 mL 0.4090 mL 1.0226 mL
80 mM 0.0307 mL 0.1534 mL 0.3068 mL 0.7669 mL
100 mM 0.0245 mL 0.1227 mL 0.2454 mL 0.6135 mL
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.

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产品名称:
L-365260 hemihydrate
目录号:
HY-106840A
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