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Lintitript {[allProObj[0].p_purity_real_show]}

货号:A1209511 同义名: SR 27897

Lintitript是一种高效、选择性、口服活性的竞争性非肽类 CCK1 受体拮抗剂,具有极强的亲和力,EC50 为 6 nM,Ki 为 0.2 nM。其对 CCK1 受体的选择性比 CCK2 受体高 33 倍以上(EC50 为 200 nM)。Lintitript 能提高血浆中的瘦素水平,促进食物摄入,同时增加胰岛素的血浆浓度。

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There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.

Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
Limited Quantity USD 15-60
Inaccessible (Haz class 6.1), Domestic USD 80+
Inaccessible (Haz class 6.1), International USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic USD 100+
Accessible (Haz class 3, 4, 5 or 8), International USD 200+
Lintitript 化学结构 CAS号:136381-85-6
Lintitript 化学结构
CAS号:136381-85-6
Lintitript 3D分子结构
CAS号:136381-85-6
Lintitript 化学结构 CAS号:136381-85-6
Lintitript 3D分子结构 CAS号:136381-85-6
规格 价格 会员价 库存 数量
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Lintitript 纯度/质量文件 产品仅供科研

货号:A1209511 标准纯度: {[allProObj[0].p_purity_real_show]}
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Lintitript 生物活性

描述 Lintitript, also known as SR 27897, is a potent, selective, orally active, competitive non-peptide antagonist of the CCK1 receptor, with an EC50 of 6 nM and a Ki of 0.2 nM. Its selectivity for the CCK1 receptor is 33 times greater than that for the CCK2 receptor (EC50 of 200 nM). Lintitript increases plasma concentrations of leptin and food intake as well as insulin[1][2][3]. Lintitript antagonizes CCK-stimulated amylase release in isolated rat pancreatic acini (pA2 = 7.50) and CCK-induced contractions in guinea pig gall bladder (pA2 = 9.57). It inhibits the binding of [125I]CCK to CCK1 receptor sites in rat pancreas (IC50 = 0.58 nM) and to CCK2 sites in guinea pig cortex (IC50 = 479 nM) in a concentration-dependent manner. Lintitript also inhibits the binding of [125I]gastrin to gastrin receptors. At 0.5 nM, Lintitript increases the dissociation constant (Kd) for CCK from the CCK A receptor (Kd = 1.8 to 7.2 nM) without altering the maximum number of receptors (Bmax = 1800 to 1770 fmol/mg)[1].

Lintitript 动物研究

Animal study Administering Lintitript, i.v., at a dose of 1 mg/kg completely reverses CCK-induced amylase secretion. Lintitript also inhibits CCK-induced gastric and gallbladder emptying in mice, with ED50 values of 3 μg/kg and 72 μg/kg, respectively. Additionally, Lintitript is highly active in gall bladder emptying experiments using egg yolk as an endogenous inducer of CCK release, with an ED50 of 27 μg/kg, p.o.[1].

Lintitript 参考文献

[1]Gully D, et al. Peripheral biological activity of SR 27897: a new potent non-peptide antagonist of CCKA receptors. Eur J Pharmacol. 1993 Feb 23;232(1):13-9.

[2]Gouldson P, et al. Contrasting roles of leu(356) in the human CCK(1) receptor for antagonist SR 27897 and agonist SR 146131 binding. Eur J Pharmacol. 1999 Nov 3;383(3):339-46.

[3]Cano V, et al. Regulation of leptin distribution between plasma and cerebrospinal fluid by cholecystokinin receptors. Br J Pharmacol. 2003 Oct;140(4):647-52.

Lintitript 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.43mL

0.49mL

0.24mL

12.14mL

2.43mL

1.21mL

24.28mL

4.86mL

2.43mL

Lintitript 技术信息

CAS号136381-85-6
分子式C20H14ClN3O3S
分子量 411.861
别名 SR 27897
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,2-8°C

溶解度

DMSO: 105 mg/mL(254.94 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方
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