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 K_i 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.

Solid

EC50: 6 nM (cholecystokinin (CCK1) receptor); Ki: 0.2 nM (cholecystokinin (CCK1) receptor)

体外研究, 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).
Lintitript produces concentration dependent inhibition of [I]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 [I]gastrin binding to gastrin receptors. Lintitript (0.5 nM) increases the dissociation constant of CCK for the CCK A receptor (K_d = 1.8 to 7.2 nM) without modifying the maximum number of receptors (B_max = 1800 to 1770 fmol/mg).

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

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.

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

Room temperature or refrigerated transportation.

• [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.  [Information]

  [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.  [Information]

  [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.  [Information]

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，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，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。