Plecanatide
(Synonyms: 普卡那肽) 目录号 : GC61194
A peptide agonist of the guanylate cyclase C receptor
Cas No.:467426-54-6
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Plecanatide is a peptide agonist of the guanylate cyclase C receptor.1 It stimulates cGMP production in T84 colon cancer cells (EC50 = 170 nM). Plecanatide (10 ppm in the diet) reduces increases in the number of neoplastic colon epithelial cells expressing Ki-67, a marker of cell proliferation, induced by dextran sulfate in cancer-prone Apc+/Min-FCCC mice.2 It suppresses trinitrobenzenesulfonic acid-induced increases in abdominal contractions in a rat model of visceral hypersensitivity when administered at doses of 0.01 and 0.05 mg/kg.3 Formulations containing plecanatide have been used in the treatment of chronic idiopathic constipation.
1.Shailubhai, K., Palejwala, V., Arjunan, K.P., et al.Plecanatide and dolcanatide, novel guanylate cyclase-C agonists, ameliorate gastrointestinal inflammation in experimental models of murine colitisWorld J. Gastrointest. Pharmacol. Ther.6(4)213-222(2015) 2.Chang, W.-C.L., Masih, S., Thadi, A., et al.Plecanatide-mediated activation of guanylate cyclase-C suppresses inflammation-induced colorectal carcinogenesis in Apc+/Min-FCCC miceWorld J. Gastrointest. Pharmacol. Ther.8(1)47-59(2017) 3.Boulete, I.-M., Thai, A., Beaufrand, C., et al.Oral treatment with plecanatide or dolcanatide attenuates visceral hypersensitivity via activation of guanylate cyclase-C in rat modelsWorld J. Gastroenterol.24(17)1888-1900(2018)
| Cas No. | 467426-54-6 | SDF | |
| 别名 | 普卡那肽 | ||
| 分子式 | C65H104N18O26S4 | 分子量 | 1681.89 |
| 溶解度 | 储存条件 | Store at -20°C | |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 0.5946 mL | 2.9728 mL | 5.9457 mL |
| 5 mM | 0.1189 mL | 0.5946 mL | 1.1891 mL |
| 10 mM | 0.0595 mL | 0.2973 mL | 0.5946 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Plecanatide: First Global Approval
Drugs 2017 Apr;77(5):593-598.PMID:28255961DOI:10.1007/s40265-017-0718-0.
Plecanatide (TrulanceTM) is an oral guanylate cyclase-C agonist that is being developed by Synergy Pharmaceuticals for the treatment of gastrointestinal disorders, such as chronic idiopathic constipation (CIC) and irritable bowel syndrome with constipation (IBS-C). It is a synthetic analogue of human uroguanylin, a 16 amino acid peptide that regulates ion and fluid transport in the gastrointestinal tract. In January 2017, Plecanatide received its first global approval in the USA for the treatment of adult patients with CIC. Plecanatide is undergoing phase III investigation in IBS-C. This article summarizes the milestones in the development of Plecanatide leading to this first approval in CIC.
Plecanatide for Treatment of Chronic Constipation and Irritable Bowel Syndrome
Am J Med 2019 May;132(5):572-575.PMID:30550753DOI:10.1016/j.amjmed.2018.11.027.
Chronic idiopathic constipation and irritable bowel syndrome with constipation are commonly encountered in ambulatory patients, but limited options exist for patients with persistent or severe symptoms following treatment with nonprescription products. Plecanatide (Trulance, Synergy Pharmaceuticals, New York, NY) is a 16-amino acid peptide analog of uroguanylin that stimulates guanylate cyclase-C receptors to increase chloride and bicarbonate secretion into the intestine and prevents the absorption of sodium ions, thereby increasing the secretion of water into the lumen. The influx of additional fluid accelerates intestinal transit, softens the stool, and facilitates easier defecation. Plecanatide is the second guanylate cyclase-C receptor agonist to be approved by the US Food and Drug Administration for chronic idiopathic constipation and irritable bowel syndrome, but Plecanatide is unique because its effects are limited to the proximal small bowel.
Plecanatide: a new guanylate cyclase agonist for the treatment of chronic idiopathic constipation
Therap Adv Gastroenterol 2018 Jun 8;11:1756284818777945.PMID:29942351DOI:10.1177/1756284818777945.
Chronic constipation affects millions of Americans, consumes significant healthcare resources, and significantly affects quality of life (QOL). Recently, several new treatment options have become available for the treatment of constipation, including intestinal secretagogues such as lubiprotone, and linaclotide, prokinetics such as prucalopride, and bile acid transporter antagonists. Plecanatide is the newest of the secretagogue class of compounds that has been approved by the US Food and Drug Administration for the treatment of adults with chronic idiopathic constipation (CIC) in the USA. It is a guanylate cyclase agonist, and a 16 amino acid synthetic peptide that is a structural analog of human uroguanylin. Two large randomized, double-blind, placebo-controlled studies assessed the efficacy and safety of Plecanatide in CIC patients (Rome III). Both doses of Plecanatide, 3 mg and 6 mg resulted in a significantly greater percentage of patients who were durable overall complete spontaneous bowel movement (CSBM) responders (primary endpoint) compared with those who received placebo (Plecanatide 3 mg, 21.0%; Plecanatide 6 mg, 19.5%; placebo, 10.2%; p < 0.001 for each drug dose versus placebo). Plecanatide treatment also significantly reduced the severity of other CIC symptoms (straining effort, stool consistency, bloating). Also, plecanatide-treated patients reported high levels of satisfaction and improved QOL and desire to continue treatment. The rate of treatment-emergent adverse events with Plecanatide was low, including rates of diarrhea (5%). Plecanatide is a luminally acting secretagogue that is efficacious and safe for the treatment of CIC. This article provides an overview of Plecanatide in the management of adults with CIC.
Plecanatide for the treatment of chronic idiopathic constipation in adult patients
Expert Rev Clin Pharmacol 2019 Nov;12(11):1019-1026.PMID:31575291DOI:10.1080/17512433.2019.1670057.
Introduction. Chronic idiopathic constipation (CIC) is a functional gastrointestinal disorder that is associated with an increased healthcare cost and an abnormally poor quality of life. Plecanatide is a natural analog to the peptide agonist of the guanylate cyclase-C (GC-C) receptor, uroguanylin. The conversion of guanosine 5-triphosphate to cyclic guanosine monophosphate results in an increased bowel fluid secretion. Plecanatide is a promising new agent for CIC unresponsive to current therapeutic regimes.Areas covered. A comprehensive online search of Medline and the Science Citation Index was made using the keywords 'Plecanatide', 'guanylate cyclase-C agonists', and 'constipation', in various combinations. We reviewed the pharmacodynamics, pharmacokinetics, and metabolism of this agent, and the most significant studies regarding the clinical efficacy and safety of Plecanatide in CIC therapy.Expert opinion. Experimental studies showed that Plecanatide was significantly better than placebo in reducing CIC severity, straining, stool consistency, bowel movements and quality of life. Apart from limited cases of diarrhea, no serious adverse events were reported. However, few data are available on its long-term safety. Furthermore, patients' affordability of Plecanatide can be limited by its costs. Finally, this new agent with a different way of action can be proposed in patients refractory to common therapy.
Plecanatide for the treatment of constipation-predominant irritable bowel syndrome
Expert Rev Gastroenterol Hepatol 2020 Feb;14(2):71-84.PMID:31985305DOI:10.1080/17474124.2020.1722101.
Introduction: As an analogue of uroguanylin Plecanatide binds to the Guanylate Cyclase-C receptor activating fluid and ion secretion in the small intestine with the same pH-dependent binding kinetics as the natural ligand. Plecanatide has been FDA approved as safe and effective for the indications of Chronic Idiopathic Constipation (CIC) and Irritable Bowel Syndrome with Constipation (IBS-C).Areas covered: All clinical trial results supporting approval of Plecanatide in IBS-C are reported, evaluated and interpreted in the context of the complex pathophysiology of functional diseases and the barriers that must be overcome for appropriate protocol design and conduct.Expert opinion: The Expert Opinion section discusses safety and efficacy of Plecanatide for IBS-C. Broader consideration of some of the inherent challenges in understanding and treating functional gastrointestinal disorders includes: 1. the difficulty of understanding diseases with complex pathophysiology that clinically present with a few simple symptoms, 2. exploring the pathophysiology of functional diseases using pharmacophysiology, 3. value of 'Set Theory' in the evaluation of complex clinical data and 4. physiologic and pathophysiologic insight gained by evaluation 'physiologic redundancy' and 'conservation of function'.