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1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemELoxiglumideCat. No.: HY-B2154CAS No.: 107097-80-3Synonyms: CR-1505分式: CHClNO分量: 461.38作靶點: Cholecystokinin Receptor作通路: GPCR/G Protein; Neuronal Signaling儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)
2、據(jù)體外實驗 DMSO : 150 mg/mL (325.11 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 2.1674 mL 10.8371 mL 21.6741 mL5 mM 0.4335 mL 2.1674 mL 4.3348 mL10 mM 0.2167 mL 1.0837 mL 2.1674 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度,選擇合適的溶劑配制儲備液,并請注意儲備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Loxiglum
3、ide是縮膽囊素 (CCK-1) 受體拮抗劑。IC50 & Target CCK-1 receptor 1體內(nèi)研究The effects of pancreatic rest by oral administration of CCK-1 receptor antagonist Loxiglumide and pancreas1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEstimulation are investigated via endogenous CCK release induced by po protease inhibito
4、r camostat on therecovery of pancreatic secretory function, and biochemical and histological changes of the pancreas afteracute hemorrhagic pancreatitis. Oral administration of CCK-1 receptor antagonist Loxiglumide with a dose of50 mg/kg body weight inhibits pancreatic exocrine secretion for more th
5、an 12 h. Thus, every 12-hadministration of Loxiglumide might have completely blocks the effect of endogenously released CCK on thepancreas (pancreatic rest) 1.PROTOCOLAnimal Rats 1Administration 1 At 24 h after induction of acute hemorrhagic pancreatitis, rats are divided into four different treatme
6、nt groups:standard rat chow (AP-C); standard rat chow with pancreatic rest (AP-R); standard rat chow with pancreaticstimulation (AP-S); and standard rat chow with pancreatic rest, followed by pancreatic stimulation (AP-R/S).Rats in the AP-C group receive 2 mL/kg body weight saline orally (po) via an
7、 orogastric tube twice daily(09:00 and 21:00 h) for 10 d; the AP-R group receive 50 mg/kg body weight of CCK-1 receptor antagonistLoxiglumide dissolved in 2 mL distilled water po twice daily for 10 d; the AP-S group receive 25 mg/kg bodyweight protease inhibitor Camostat, which is known to stimulate
8、 endogenous CCK release, dissolved in 2 mLdistilled water po twice daily for 10 d; and the AP-R/S group receive 50 mg/kg body weight Loxiglumide twicedaily for the first 5 d followed by 25 mg/kg body weight camostat twice daily for the next 5 d. Rats are fed adlibitum. On day 12 at 24 h after the la
9、st treatment and overnight fasting, pancreatic exocrine function andhistological examination of the pancreas are performed.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Jia D, et al. Effect of endogenous cholecystokinin on the course of acute pancreatitis in rats. World J Gastroenterol. 2015 Jul7;21(25):7742-53.McePdfHeightCaution: Product has not been fully validated for m
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