[CAS NO. 25126-32-3] Sincalide
PRODUCTS SPECIFICATIONS [25126-32-3]
DESCRIPTION [25126-32-3]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 1143.27 |
| Molecular Formula | C49H62N10O16S3 |
| SMILES | - |
3 Publications Citing Use of MCE
Summary
Sincalide (Cholecystokinin octapeptide, CCK‐8) is a rapid-acting amino acid polypeptide hormone analogue of cholecystokinin (CCK) for intravenous use in postevacuation cholecystography. CCK‐8 is a major bioactive segment of CCK that retains most of the biological activities of CCK. CCK‐8 can promote gallbladder contraction by injection and helps diagnose gallbladder and pancreas disorders. CCK‐8 can increase bile secretion, cause the gallbladder to contract and relax the sphincter of Oddi, resulting in bile drainage into the duodenum. CCK‐8 is a major bioactive segment of CCK that retains most of the biological activities of CCK [1] [2] [3] .
In Vitro
Sincalide (Cholecystokinin octapeptide, CCK‐8), as a novel cardiovascular hormone, has a significant inhibitory effect on myocardial fibrosis in noninfarcted areas. CCK‐8 also plays a positive role in fighting inflammation, apoptosis and collagen deposition. CCK‐8 protects H9c2 cardiomyoblasts from Ang II‐induced apoptosis partly via activation of the CCK1 receptor and the phosphatidyqinositol‐3 kinase/protein kinase B (PI3K/Akt) signaling pathway [3] .
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay [3]
| Cell Line: | H9c2 cells |
| Concentration: | 0.001, 0.01, 0.1, 1, 10, or 100 μmol/L |
| Incubation Time: | 24 h |
| Result: | Attenuated Ang II‐induced toxicity in H9c2 cells |
Apoptosis Analysis [3]
| Cell Line: | H9c2 cells |
| Concentration: | 0.001, 0.01, 0.1, 1, 10, or 100 μmol/L |
| Incubation Time: | 24 h |
| Result: | Decreased apoptotic cells, and prevented Ang II‐induced cytotoxicity that involves modulation of the PI3K/Akt pathway. |
Western Blot Analysis [3]
| Cell Line: | H9c2 cells |
| Concentration: | 0.001, 0.01, 0.1, 1, 10, or 100 μmol/L |
| Incubation Time: | 24 h |
| Result: | Expressed the protein and mRNAs of CCK and both its receptors in H9c2 cells. |
RT-PCR [3]
| Cell Line: | H9c2 cells |
| Concentration: | 0.001, 0.01, 0.1, 1, 10, or 100 μmol/L |
| Incubation Time: | 24 h |
| Result: | Increased the protein and mRNA expression levels of CCK and decreased CCK 1 receptor expression levels at both the protein and mRNA levels with Ang II stimulation markedly. |
In Vivo
Sincalide (Cholecystokinin octapeptide, CCK‐8) (i.p.; 50 μg/kg/d; for 4 weeks) alleviates fibrosis in the noninfarcted regions and delay the left ventricular remodeling and the progress of heart failure in a MI rat model [4] .
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | MI rat model [4] |
| Dosage: | 50 μg/kg |
| Administration: | i.p.; 50 μg/kg/d; for 4 weeks |
| Result: | Had significant inhibitory effect on myocardial fibrosis in noninfarcted areas. |
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT00004414 | University of Michigan|FDA Office of Orphan Products Development |
Cholestasis
|
September 1997 | Not Applicable |
| NCT00706381 | National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK)|National Institutes of Health Clinical Center (CC) |
Healthy Volunteers
|
June 23, 2008 | Phase 3 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
Sealed storage, away from moisture and light, under nitrogen
| Powder | -80°C | 2 years |
|---|---|---|
| -20°C | 1 year |
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen)
Solvent & Solubility
H 2 O : 50 mg/mL ( 43.73 mM ; ultrasonic and adjust pH to 11 with NH3·H2O)
DMF : 50 mg/mL ( 43.73 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 0.8747 mL | 4.3734 mL | 8.7468 mL |
| 5 mM | 0.1749 mL | 0.8747 mL | 1.7494 mL |
| 10 mM | 0.0875 mL | 0.4373 mL | 0.8747 mL |
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1.
Add each solvent one by one: 10% DMF >> 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (2.19 mM); Clear solution
References
- [1] Maher KA et al. Kinevac (sincalide for injection)/Squibb Diagnostics. Gastroenterol Nurs. 1991 Oct;14(2):98-100.
- [2] Ziessman HA. Sincalide: A Review of Clinical Utility, Proper Infusion Methodology, and Alternative Cholecystogogues. J Nucl Med Technol. 2019 Sep;47(3):210-212.
- [3] Can Wang, et al. Protective effect of cholecystokinin octapeptide on angiotensin II-induced apoptosis in H9c2 cardiomyoblast cells. J Cell Biochem. 2020 Jul;121(7):3560-3569.
- [4] Can Wang, et al. Cholecystokinin octapeptide reduces myocardial fibrosis and improves cardiac remodeling in post myocardial infarction rats. Int J Biochem Cell Biol. 2020 Aug;125:105793.