辛卡利特（胆囊收缩素八肽，CCK-8）作为一种新型心血管激素，对非梗死区心肌纤维化具有显着的抑制作用。 CCK-8 在对抗炎症、细胞凋亡和胶原蛋白沉积方面也发挥着积极作用。 CCK-8 部分通过激活 CCK1 受体和磷脂酰肌醇-3 激酶/蛋白激酶 B (PI3K/Akt) 信号通路来保护 H9c2 心肌细胞免受 Ang II 诱导的细胞凋亡[3]。细胞活力测定[3] 细胞系：H9c2 细胞 浓度：0.001、0.01、0.1、1、10 或 100 μmol/L 孵育时间：24 小时 结果：Ang II 诱导的 H9c2 细胞毒性减弱 细胞凋亡分析[3] 细胞细胞系：H9c2 细胞 浓度：0.001、0.01、0.1、1、10 或 100 μmol/L 孵育时间：24 小时 结果：凋亡细胞减少，并阻止 Ang II 诱导的涉及 PI3K/Akt 途径调节的细胞毒性。 Western Blot分析[3] 细胞系：H9c2细胞 浓度：0.001、0.01、0.1、1、10或100 μmol/L 孵育时间：24 h 结果：H9c2细胞表达CCK及其两种受体的蛋白和mRNA。 RT-PCR[3] 细胞系：H9c2 细胞 浓度：0.001、0.01、0.1、1、10 或 100 μmol/L 孵育时间：24 h 结果：CCK 蛋白和 mRNA 表达水平增加，CCK 1 受体表达减少Ang II 刺激后蛋白质和 mRNA 水平均显着升高。

辛卡利特（胆囊收缩素八肽，CCK-8）（腹腔注射；50 μg/kg/d；持续 4 周）可减轻 MI 大鼠模型中非梗塞区域的纤维化，并延缓左心室重构和心力衰竭的进展[4]。动物模型：MI大鼠模型[4] 剂量：50 μg/kg 给药方式：腹膜内注射； 50微克/公斤/天；连续4周 结果：对非梗塞区心肌纤维化有显着的抑制作用。

细胞系：H9c2 细胞
浓度：0.001、0.01、0.1、1、10 或 100 μmol/L
孵育时间：24 小时
结果：Ang II 诱导的 H9c2 细胞毒性减弱

MI rat model
50 μg/kg
i.p.; 50 μg/kg/d; for 4 weeks

Absorption, Distribution and Excretion
The intravenous (bolus) administration of sincalide causes a prompt contraction of the gallbladder that becomes maximal in 5 to 15 minutes, as compared with the stimulus of a fatty meal which causes a progressive contraction that becomes maximal after approximately 40 minutes.
Limited information is available on the route of elimination of sincalide
Limited information is available on the volume of distribution of sincalide.

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Metabolism / Metabolites
Limited information is available on the metabolism of sincalide.

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Biological Half-Life
Limited information is available on the half-life of sincalide.

Effects During Pregnancy and Lactation
◉ Summary of Use during Lactation
Sincalide is a synthetic octapeptide analogue of cholecystokinin. Because sincalide has a molecular weight of 1143, the amount in milk is likely to be very low and oral absorption by the infant is unlikely because it is probably destroyed in the infant's gastrointestinal tract. The serum half-life of sincalide is less than 2 minutes, indicating that withholding breastfeeding for 10 minutes after a dose should ensure that the infant is not exposed to the drug.
◉ Effects in Breastfed Infants
Relevant published information was not found as of the revision date.
◉ Effects on Lactation and Breastmilk
Relevant published information was not found as of the revision date.

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Protein Binding
Limited information is available on the protein binding of sincalide.

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

[2]. Sincalide: A Review of Clinical Utility, Proper Infusion Methodology, and Alternative Cholecystogogues. J Nucl Med Technol. 2019 Sep;47(3):210-212.

[3]. Protective effect of cholecystokinin octapeptide on angiotensin II-induced apoptosis in H9c2 cardiomyoblast cells. J Cell Biochem. 2020 Jul;121(7):3560-3569.

[4]. Cholecystokinin octapeptide reduces myocardial fibrosis and improves cardiac remodeling in post myocardial infarction rats. Int J Biochem Cell Biol. 2020 Aug;125:105793.

Sincalide is an oligopeptide.
Sincalide is a medication given by injection to assist in the diagnosis of gallbladder and pancreas disorders. It is identified as the 8-amino acid C-terminal segment of cholecystokinin and is also known as CCK-8. Naturally occurring cholecystokinin is a gastrointestinal peptide hormone normally essential for stimulating protein and fat digestion in the body. When injected intravenously, sincalide produces a substantial reduction in gallbladder size by causing this organ to contract. The evacuation of bile that results is similar to that which occurs physiologically in response to endogenous cholecystokinin. Furthermore, sincalide stimulates the pancreatic secretion of bicarbonate and enzymes. As the product Kinevac (FDA), sincalide is used to stimulate the duodenum, pancreas, and small bowel for cholesterol analysis, enzymatic activity analysis, and x-ray examination respectively.
Sincalide is a Cholecystokinin Analog.
Sincalide is a synthetic C-terminal octapeptide identical to the sequences of the endogenous cholecystokinin hormone. Mimic action of cholecystokinin, sincalide induces gallbladder smooth muscle contraction directly, thereby reducing gallbladder size, inducing bile evacuation, and secretion of pancreatic enzymes. In addition, this agent decreases esophageal sphincter tone and delays gastric emptying via cholinergic signaling.
An octapeptide hormone present in the intestine and brain. When secreted from the gastric mucosa, it stimulates the release of bile from the gallbladder and digestive enzymes from the pancreas.

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Drug Indication
As the product Kinevac (FDA), sincalide is used for the following indications: 1) to stimulate gallbladder contraction, as may be assessed by various methods of diagnostic imaging, or to obtain by duodenal aspiration a sample of concentrated bile for analysis of cholesterol, bile salts, phospholipids, and crystals; (2) to stimulate pancreatic secretion in combination with secretin prior to obtaining a duodenal aspirate for analysis of enzyme activity, composition, and cytology; (3) to accelerate the transit of a barium meal through the small bowel, thereby decreasing the time and extent of radiation associated with fluoroscopy and x-ray examination of the intestinal tract.
FDA Label

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Mechanism of Action
When injected intravenously, sincalide produces a substantial reduction in gallbladder size by causing this organ to contract. The evacuation of bile that results is similar to that which occurs physiologically in response to endogenous cholecystokinin. Like cholecystokinin, sincalide stimulates pancreatic secretion; concurrent administration with secretin increases both the volume of pancreatic secretion and the output of bicarbonate and protein (enzymes) by the gland. This combined effect of secretin and sincalide permits the assessment of specific pancreatic function through measurement and analysis of the duodenal aspirate.

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Pharmacodynamics
Following an intravenous (bolus) injection of 0.02 mcg/kg of sincalide, maximal contraction of the gallbladder occurred in 5 to 15 minutes. Sincalide reduced gallbladder radiographic size by at least 40%, generally considered satisfactory contraction.

C49H62N10O16S3

1143.26898

1142.35

C, 51.48; H, 5.47; N, 12.25; O, 22.39; S, 8.41

25126-32-3

Sincalide ammonium; 70706-98-8

9833444

White to off-white solid powder

1.4±0.1 g/cm3

1.643

2.25

485.78

13

19

33

78

2180

7

CSCC[C@H](NC([C@@H](NC([C@@H](N)CC(O)=O)=O)CC1=CC=C(OS(=O)(O)=O)C=C1)=O)C(NCC(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N)=O)CC2=CC=CC=C2)=O)CC(O)=O)=O)CCSC)=O)CC3=CNC4=CC=CC=C34)=O)=O

IZTQOLKUZKXIRV-YRVFCXMDSA-N

InChI=1S/C49H62N10O16S3/c1-76-18-16-34(55-47(69)37(58-44(66)32(50)23-41(61)62)21-28-12-14-30(15-13-28)75-78(72,73)74)45(67)53-26-40(60)54-38(22-29-25-52-33-11-7-6-10-31(29)33)48(70)56-35(17-19-77-2)46(68)59-39(24-42(63)64)49(71)57-36(43(51)65)20-27-8-4-3-5-9-27/h3-15,25,32,34-39,52H,16-24,26,50H2,1-2H3,(H2,51,65)(H,53,67)(H,54,60)(H,55,69)(H,56,70)(H,57,71)(H,58,66)(H,59,68)(H,61,62)(H,63,64)(H,72,73,74)/t32-,34-,35-,36-,37-,38-,39-/m0/s1

(3S)-3-amino-4-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-4-methylsulfanyl-1-oxobutan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-4-methylsulfanyl-1-oxobutan-2-yl]amino]-1-oxo-3-(4-sulfooxyphenyl)propan-2-yl]amino]-4-oxobutanoic acid

CCK-8S; CCK 8S; CCK8S; Kinevac; CCK-8; CCK 8; CCK8

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

注意： 请将本产品存放在密封且受保护的环境中（例如氮气保护），避免吸湿/受潮和光照。

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

H2O: ~50 mg/mL (~43.7 mM)
DMF: ~50 mg/mL (~43.7 mM)

配方 1 中的溶解度: ≥ 2.5 mg/mL (2.19 mM) (饱和度未知) in 10% DMF 90% Corn Oil (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。

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请根据您的实验动物和给药方式选择适当的溶解配方/方案：
1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液));
2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方):
10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline);
假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL；
3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例;
4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶;
5、为保证最佳实验结果，工作液请现配现用！
6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们;
7、 以上所有助溶剂都可在 Invivochem.cn网站购买。