Ceruletide(Synonyms: 雨蛙素 Caerulein Cerulein FI-6934)

Ceruletide;(Synonyms: 雨蛙素; Caerulein; Cerulein; FI-6934) 纯度: 99.84%

Ceruletide 是一种十肽,也是一种有效的胆囊收缩素受体 (cholecystokinin receptor) 激动剂。 Ceruletide 是一种安全有效的胆囊收缩剂,对胆囊肌肉和胆管有直接的痉挛性作用。

Ceruletideamp;;(Synonyms: 雨蛙素; Caerulein;  Cerulein;  FI-6934)

Ceruletide Chemical Structure

CAS No. : 17650-98-5

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生物活性

Ceruletide is a decapeptide and a potent cholecystokinin receptor agonist. Ceruletide is a safe and effective cholecystokinetic agent with a direct spasmogenic effect on the gallbladder muscle and bile ducts[1].

IC50 Target

Cholecystokinin receptor[4]

体外研究
(In Vitro)

Ceruletide is similar chemically and biologically to the human gastrointestinal hormones cholecystokinin-pancreozymin (CCK) and gastrin II. Ceruletide stimulates gallbladder contraction, pancreatic exocrine secretion, gastric secretion, and motility in the distal duodenum, jejunum, ileum and colon, while delaying gastric emptying and inhibiting motility in the proximal duodenum[1]. Ceruletide in supramaximal but not in physiological doses activates NF-kappaB/Rel in vitro. This activation may induce a self-defending genetic program before the onset of cellular injury, which may prevent higher degrees of damage of pancreatic acinar cells after secretagogue hyperstimulation[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Ceruletide (0.4-0.5 mcg/kg, i.v.; 3-4 mcg/kg, s.c.) results in emesis and evacuation of the bowel in the intact conscious dog, and recovery is complete 15-30 min after i. v. administration and 2-4 hr after s.c. administration. Ceruletide (5-15 ng/kg, i.v.) shows a marked spasmogenic effect on the pylorus of rats. Ceruletide also reduces blood pressure in anesthetized dogs[1]. Ceruletide serum bile acid (SBA) stimulation circumvents exogenous and endogenous influences associated with postprandial (PP) SBA stimulation. Ceruletide SBA stimulation may perform as well as PP SBA stimulation in dogs with portosystemic shunt (PSS) and be more sensitive for the detection of hepatic dysfunction in dogs with upper respiratory disease (URD)[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

1352.41

Formula

C58H73N13O21S2

CAS 号

17650-98-5

Sequence

{pGlu}-Gln-Asp-Tyr(SO3H)-Thr-Gly-Trp-Met-Asp-Phe-NH2

Sequence Shortening

{pGlu}-QD-Y(SO3H)-TGWMDF-NH2

中文名称

雨蛙素;蓝肽;硫酸化蓝肽;雨蛙肽

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -80deg;C 2 years
-20deg;C 1 year
In solvent -80deg;C 6 months
-20deg;C 1 month
溶解性数据
In Vitro:;

H2O : ≥ 100 mg/mL (73.94 mM)

DMSO : 100 mg/mL (73.94 mM; Need ultrasonic)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 0.7394 mL 3.6971 mL 7.3942 mL
5 mM 0.1479 mL 0.7394 mL 1.4788 mL
10 mM 0.0739 mL 0.3697 mL 0.7394 mL

*

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。-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。

In Vivo:

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

  • 1.

    请依序添加每种溶剂:;Saline

    Solubility: 12.5 mg/mL (9.24 mM); Clear solution; Need ultrasonic

  • 2.

    请依序添加每种溶剂:;10% DMSO ;; 40% PEG300 ;; 5% Tween-80 ;; 45% saline

    Solubility: ≥ 2.08 mg/mL (1.54 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (1.54 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 3.

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

    Solubility: ≥ 2.08 mg/mL (1.54 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (1.54 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 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。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 4.

    请依序添加每种溶剂:;10% DMSO ;; 90% corn oil

    Solubility: 2.08 mg/mL (1.54 mM); Clear solution; Need warming

    此方案可获得 2.08 mg/mL (1.54 mM) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 MCE 网站选购。
参考文献
  • [1]. Vincent ME, et al. Pharmacology, clinical uses, and adverse effects of ceruletide, a cholecystokinetic agent. Pharmacotherapy. 1982 Jul-Aug;2(4):223-34.

    [2]. Bridger N, et al. Comparison of postprandial and ceruletide serum bile acid stimulation in dogs. J Vet Intern Med. 2008 Jul-Aug;22(4):873-8.

    [3]. Steinle AU, et al. NF-kappaB/Rel activation in cerulein pancreatitis. Gastroenterology. 1999 Feb;116(2):420-30.

    [4]. Zarrindast MR, et al. Effects of cholecystokinin receptor agonist and antagonists on morphin dependence in mice. Pharmacol Toxicol. 1995 Dec;77(6):360-4.

Animal Administration
[3]

Dogs[3]
All dogs undergo serum bile acid (SBA) stimulation with food (<5 kg>5 kg BW 2 tablespoons) or 0.3 μg/kg BW Ceruletide IM, respectively, on consecutive days. A diet of moderate protein content and with an increased concentration of fiber is chosen to minimize metabolic complications such as hepatic encephalopathy. Before each test, the dogs are fasted for 12 hours. Blood samples are drawn at baseline, 60 and 120 minutes after feeding, and 20, 30, and 40 minutes postinjection, respectively. The blood samples are collected in plain tubes and left to clot; they are then centrifuged at 6,500 ×g for 1 minute, and the serum is used to measure SBA by a colorimetric test with endpoint determination[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献
  • [1]. Vincent ME, et al. Pharmacology, clinical uses, and adverse effects of ceruletide, a cholecystokinetic agent. Pharmacotherapy. 1982 Jul-Aug;2(4):223-34.

    [2]. Bridger N, et al. Comparison of postprandial and ceruletide serum bile acid stimulation in dogs. J Vet Intern Med. 2008 Jul-Aug;22(4):873-8.

    [3]. Steinle AU, et al. NF-kappaB/Rel activation in cerulein pancreatitis. Gastroenterology. 1999 Feb;116(2):420-30.

    [4]. Zarrindast MR, et al. Effects of cholecystokinin receptor agonist and antagonists on morphin dependence in mice. Pharmacol Toxicol. 1995 Dec;77(6):360-4.

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