1. GPCR/G Protein Neuronal Signaling
  2. Cholecystokinin Receptor
  3. Lintitript

Lintitript  (Synonyms: SR 27897)

目录号: HY-101764 纯度: ≥99.0%
COA 产品使用指南

Lintitript (SR 27897) 是一种高效,选择性,口服活性,竞争性和非肽类 CCK1 受体拮抗剂,EC50 为 6 nM,Ki 为 0.2 nM。Lintitript 对 CCK1 的选择性比对 CCK2 受体的选择性高 33 倍以上 (EC50值为 200 nM)。Lintitript 增加瘦素的血浆浓度和食物摄入以及胰岛素的血浆浓度。

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Lintitript Chemical Structure

Lintitript Chemical Structure

CAS No. : 136381-85-6

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     可免费申领三个不同产品的试用装。

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥5500
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1 mg ¥1904
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5 mg ¥5000
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10 mg ¥8500
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100 mg   询价  

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Lintitript (SR 27897) is a highly potent, selective, orally active, competitive and non-peptide cholecystokinin (CCK1) receptor antagonist with an EC50 of 6 nM and a Ki of 0.2 nM. Lintitript displays > 33-fold selectivity more selective for CCK1 than CCK2 receptors (EC50 value of 200 nM). Lintitript increases plasma concentration of leptin and food intake as well as plasma concentration of insulin[1][2][3].

IC50 & Target

EC50: 6 nM (cholecystokinin (CCK1) receptor)[2]; Ki: 0.2 nM (cholecystokinin (CCK1) receptor)[1]

体外研究
(In Vitro)

In vitro, Lintitript (SR 27897) is a competitive antagonist of cholecystokinin (CCK)-stimulated amylase release in isolated rat pancreatic acini (pA2 = 7.50) and of CCK-induced guinea pig gall bladder contractions (pA2 = 9.57)[1].
Lintitript produces concentration dependent inhibition of [125I]CCK binding to CCK1 receptor sites in the rat pancreas (IC50 value of 0.58 nM) and also to CCK 2 sites in the guinea pig cortex (IC2 value of 479 nM). Lintitript inhibits [125I]gastrin binding to gastrin receptors. Lintitript (0.5 nM) increases the dissociation constant of CCK for the CCK A receptor (Kd = 1.8 to 7.2 nM) without modifying the maximum number of receptors (Bmax = 1800 to 1770 fmol/mg)[1].

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

体内研究
(In Vivo)

Lintitript (SR 27897; 1 mg/kg, i.v.) completely reverses the CCK-induced amylase secretion. Lintitript also inhibits CCK-induced gastric and gallbladder emptying in mice (ED50s = 3 and 72 μg/kg, respectively). Lintitript is also very active (ED50 = 27 μg/kg p.o.) in the gall bladder emptying protocol with egg yolk as an inducer of endogenous CCK release[1].

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

分子量

411.86

Formula

C20H14ClN3O3S

CAS 号
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
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO 中的溶解度 : 100 mg/mL (242.80 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 2.4280 mL 12.1400 mL 24.2801 mL
5 mM 0.4856 mL 2.4280 mL 4.8560 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。-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

纯度: 99.58%

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。-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 2.4280 mL 12.1400 mL 24.2801 mL 60.7002 mL
5 mM 0.4856 mL 2.4280 mL 4.8560 mL 12.1400 mL
10 mM 0.2428 mL 1.2140 mL 2.4280 mL 6.0700 mL
15 mM 0.1619 mL 0.8093 mL 1.6187 mL 4.0467 mL
20 mM 0.1214 mL 0.6070 mL 1.2140 mL 3.0350 mL
25 mM 0.0971 mL 0.4856 mL 0.9712 mL 2.4280 mL
30 mM 0.0809 mL 0.4047 mL 0.8093 mL 2.0233 mL
40 mM 0.0607 mL 0.3035 mL 0.6070 mL 1.5175 mL
50 mM 0.0486 mL 0.2428 mL 0.4856 mL 1.2140 mL
60 mM 0.0405 mL 0.2023 mL 0.4047 mL 1.0117 mL
80 mM 0.0304 mL 0.1518 mL 0.3035 mL 0.7588 mL
100 mM 0.0243 mL 0.1214 mL 0.2428 mL 0.6070 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:
Lintitript
目录号:
HY-101764
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