1. GPCR/G Protein Neuronal Signaling Apoptosis PI3K/Akt/mTOR
  2. Cholecystokinin Receptor Apoptosis PI3K Akt
  3. Sincalide

Sincalide  (Synonyms: 辛卡利特; Cholecystokinin octapeptide; CCK-8; SQ19844)

目录号: HY-P0093 纯度: 99.51%
COA 产品使用指南 技术支持

Sincalide (Cholecystokinin octapeptide, CCK-8) 是一种速效胆囊收缩素 (CCK) 的氨基酸多肽激素类似物,在胆囊造影术中静脉使用。Sincalide 是 CCK 的一个主要生物活性片段,它保留了 CCK 的大部分生物活性。可通过注射促进胆囊收缩并帮助诊断胆囊和胰腺疾病。其增加胆汁的分泌,使胆囊收缩并使 Oddi 的括约肌松弛,从而使胆汁排入十二指肠。

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Custom Peptide Synthesis

Sincalide

Sincalide Chemical Structure

CAS No. : 25126-32-3

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Other Forms of Sincalide:

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Sincalide (Cholecystokinin octapeptide, CCK-8) is a rapid-acting amino acid polypeptide hormone analogue of cholecystokinin (CCK) for intravenous use in postevacuation cholecystography. Sincalide is a major bioactive segment of CCK that retains most of the biological activities of CCK. Sincalide can promote gallbladder contraction by injection and helps diagnose gallbladder and pancreas disorders. Sincalide can increase bile secretion, cause the gallbladder to contract and relax the sphincter of Oddi, resulting in bile drainage into the duodenum. Sincalide is a major bioactive segment of CCK that retains most of the biological activities of CCK[1][2][3].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
CHO IC50
1.2 x 10-10 M
Compound: CCK-8s
Displacement of [125I]CCK-8s from human recombinant CCK2 receptor expressed in CHO cells measured after 60 mins by scintillation counting method
Displacement of [125I]CCK-8s from human recombinant CCK2 receptor expressed in CHO cells measured after 60 mins by scintillation counting method
[PMID: 27876250]
CHO IC50
1.3 x 10-10 M
Compound: CCK-8s
Displacement of [125I]CCK-8s from human recombinant CCK1 receptor expressed in CHO cells measured after 60 mins by scintillation counting method
Displacement of [125I]CCK-8s from human recombinant CCK1 receptor expressed in CHO cells measured after 60 mins by scintillation counting method
[PMID: 27876250]
HEK293 EC50
27 nM
Compound: CCK-8, SO3
Antagonist activity at CCK2 receptor expressed in HEK293 cells assessed as accumulation of [3H]inositol phosphates by PI assay
Antagonist activity at CCK2 receptor expressed in HEK293 cells assessed as accumulation of [3H]inositol phosphates by PI assay
[PMID: 16686530]
HEK293 EC50
28 nM
Compound: CCK-8, SO3
Antagonist activity at CCK1 receptor expressed in HEK 293 cells assessed as accumulation of [3H]inositol phosphates by PI assay
Antagonist activity at CCK1 receptor expressed in HEK 293 cells assessed as accumulation of [3H]inositol phosphates by PI assay
[PMID: 16686530]
体外研究
(In Vitro)

Sincalide (Cholecystokinin octapeptide, CCK-8), as a novel cardiovascular hormone, has a significant inhibitory effect on myocardial fibrosis in noninfarcted areas. Sincalide also plays a positive role in fighting inflammation, apoptosis and collagen deposition. Sincalide 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].

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.
体内研究
(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].

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
分子量

1143.27

Formula

C49H62N10O16S3

CAS 号
性状

固体

颜色

White to off-white

Sequence

Asp-{SO3H-Tyr}-Met-Gly-Trp-Met-Asp-Phe-NH2

Sequence Shortening

D-{SO3H-Tyr}-MGWMDF-NH2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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)

溶解性数据
细胞实验: 

H2O 中的溶解度 : 50 mg/mL (43.73 mM; 超声助溶; 碱性条件溶解 (NH3·H2O 调节,pH≈11))

DMF 中的溶解度 : 50 mg/mL (43.73 mM; 超声助溶)

DMSO 中的溶解度 : 25 mg/mL (21.87 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 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
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

* 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物实验:

请根据您的 实验动物和给药方式 选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 方案 一

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (2.19 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中,混合均匀。

    2 g SBE-β-CD(磺丁基醚 β-环糊精)粉末定容于 10 mL 的生理盐水中,完全溶解至澄清透明。
  • 方案 二

    请依序添加每种溶剂: 10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (2.19 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液,此方案实验周期在半个月以上的动物实验酌情使用。

    1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
该产品水溶性佳,请具体参考实测 水 / PBS / Saline 中的溶解度数据。
您所需的储备液浓度超过该产品的实测溶解度,如有需要,请与 MCE 中国技术支持联系。
纯度 & 产品资料

纯度: 99.51%

参考文献

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO / H2O / DMF 1 mM 0.8747 mL 4.3734 mL 8.7468 mL 21.8671 mL
5 mM 0.1749 mL 0.8747 mL 1.7494 mL 4.3734 mL
10 mM 0.0875 mL 0.4373 mL 0.8747 mL 2.1867 mL
15 mM 0.0583 mL 0.2916 mL 0.5831 mL 1.4578 mL
20 mM 0.0437 mL 0.2187 mL 0.4373 mL 1.0934 mL
H2O / DMF 25 mM 0.0350 mL 0.1749 mL 0.3499 mL 0.8747 mL
30 mM 0.0292 mL 0.1458 mL 0.2916 mL 0.7289 mL
40 mM 0.0219 mL 0.1093 mL 0.2187 mL 0.5467 mL

* 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Sincalide
目录号:
HY-P0093
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