Lintitript (SR 27897) is a highly potent, selective, orally active, competitive and non-peptidecholecystokinin (CCK1) receptorantagonist with anEC₅₀of 6 nM and aK_iof 0.2 nM. Lintitript displays >33-fold selectivity more selective forCCK1than CCK2 receptors (EC₅₀value of 200 nM). Lintitript increases plasma concentration ofleptinand food intake as well as plasma concentration ofinsulin^[1][2][3].

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

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 (IC₅₀value of 0.58 nM) and also to CCK 2 sites in the guinea pig cortex (IC₂value 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 (K_d= 1.8 to 7.2 nM) without modifying the maximum number of receptors (B_max= 1800 to 1770 fmol/mg)^[1].

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].

411.86

Solid

C₂₀H₁₄ClN₃O₃S

136381-85-6

Room temperature in continental US; may vary elsewhere.

DMSO : 100 mg/mL(242.80 mM;Need ultrasonic)

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