Sincalide

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Chemical Structure| 25126-32-3 同义名 : CCK八肽硫酸盐 ;CCK-8; Cholecystokinin octapeptide; Kinevac; Cholecystokinin (26-33); CCK-8S; CCK Octapeptide (sulfated); CCK Octapeptide; SQ19844
CAS号 : 25126-32-3
货号 : A627742
分子式 : C49H62N10O16S3
纯度 : 98%
分子量 : 1143.27
MDL号 : MFCD00079849
存储条件:

Pure form Keep in dark place, sealed in dry, store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月

溶解度 :

H2O: 50 mg/mL(43.73 mM),配合低频超声,并调节pH至11

DMF: 50 mg/mL(43.73 mM),配合低频超声助溶

动物实验配方:
生物活性
描述 Sincalide is a rapid-acting, synthetic analog of cholecystokinin for intravenous use in postevacuation cholecystography[3]. Sincalide-stimulated cholescintigraphy is performed to quantify gallbladder contraction and emptying[4]. Sincalide antagonized the effect of morphine which inhibited the potentiation of ACh (Acetylcholine) on jejunal activities in vitro. The antagonistic effect of sincalide on morphine was mainly mediated by CCK-A receptor[5]. Sincalide (CCK-8) evoked guinea pig isolated ileum contraction at 10(-5)-10(-1) mumol/L in a concentration-dependent manner, EC50 being 207 pmol/L. It delayed the gastric emptying as well. The rate of inhibition of gastric emptying was 71 +/- 12% at 100 mg/kg by ip[6].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00737295 Biliary Dyskinesia Not Applicable Terminated(PI left institution... 展开 >>, study interest wained-so stopped.) 收起 << - United States, Texas ... 展开 >> Texas Tech University Health Sciences Center Lubbock, Texas, United States, 79430 收起 <<
NCT01656057 To Assess the Impact of Bile A... 展开 >>cids on Human Glukagon-like-peptide-1 Secretion 收起 << Not Applicable Completed - Denmark ... 展开 >> University Hospital of Copenhagen, Gentofte Hospital, Diabetic Research Division Copenhagen, Hellerup, Denmark, 2900 收起 <<
NCT02496221 Diabetes Mellitus, Type 2 Phase 4 Completed - United States, Maryland ... 展开 >> GSK Investigational Site Baltimore, Maryland, United States, 21225 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

0.87mL

0.17mL

0.09mL

4.37mL

0.87mL

0.44mL

8.75mL

1.75mL

0.87mL

参考文献

[1]Maher KA. Kinevac (sincalide for injection)/Squibb Diagnostics. Gastroenterol Nurs. 1991 Oct;14(2):98-100.

[2]Gaw AJ, Hills DM, et al. Characterization of the receptors and mechanisms involved in the cardiovascular actions of sCCK-8 in the pithed rat. Br J Pharmacol. 1995 Jun;115(4):660-4.

[3]Maher KA. Kinevac (sincalide for injection)/Squibb Diagnostics. Gastroenterol Nurs. 1991 Oct;14(2):98-100

[4]Ziessman HA, Tulchinsky M, Lavely WC, Gaughan JP, Allen TW, Maru A, Parkman HP, Maurer AH. Sincalide-stimulated cholescintigraphy: a multicenter investigation to determine optimal infusion methodology and gallbladder ejection fraction normal values. J Nucl Med. 2010 Feb;51(2):277-81

[5]Xu MY, Yang XP, Jin HB, Yang CX, Yang LZ. Devazepide reversed effect of sincalide against morphine on rat jejunal activities. Zhongguo Yao Li Xue Bao. 1999 May;20(5):419-22

[6]Wang SX. [Effect of cholecystokinin and its antagonists lorglumide, devazepide, and L-365,260 on gastrointestinal motility in rats]. Zhongguo Yao Li Xue Bao. 1993 Sep;14(5):443-6. Chinese