Linaclotide
Linaclotide
CAS: 851199-59-2
Molecular Formula: C59H79N15O21S6
Linaclotide - Names and Identifiers
| Name | Linaclotide |
| Synonyms | CY-14 Argpessin Liclotide Linaelotide Linaclotide Linacllotide Linaelotide Acetate Rinalodipine Acetate |
| CAS | 851199-59-2 |
Linaclotide - Physico-chemical Properties
| Molecular Formula | C59H79N15O21S6 |
| Molar Mass | 1526.74 |
| Density | 1.60 |
| Boling Point | 2045.0±65.0 °C(Predicted) |
| Storage Condition | -20℃ |
| Physical and Chemical Properties | Linaclotide is a white to off-white amorphous powder; Slightly soluble in water and aqueous sodium chloride (0.9%). |
Linaclotide - Synthesis method of linaclotide
from Baidu library
patent type:
patent for invention
application (patent) number:
CN202010688097.5
date of application:
20200716
public/announcement number:
CN111732632A
date of publication/announcement:
20201002
Applicant (patentee):
Taizhou Jinuo Biotechnology Co., Ltd.
Inventor:
Wang Fengjian ,< a href = "https://xueshu.baidu.com/s?wd=author: (pull and Kumar Tar) & tn = SE_baiduxueshu_c1gjeupa & ie = utf-8 & SC _f_para = SC _hilight = person" target = "_blank"> pull and Kumar Tar
national and provincial code:
CN331022
Summary:
The invention discloses a synthesis method of linaclotide, which belongs to the technical field of drug synthesis. The synthesis method includes: solid phase synthesis of linaclotide resin, wherein the C- terminal cysteine containing OPfp ester is used for solid phase synthesis, and then the protective group and the resin solid phase carrier are removed to obtain linear linaclotide; The linear linaclotide is dissolved in an aqueous solution of dimethyl sulfoxide with a mass percentage concentration of 2-10% to obtain a mixed solution with a linear linaclotide concentration of 1-5 mg/mL, then ammonium sulfate, ammonium hydroxide or ammonium carbonate equivalent to 10-15 times of linear linaclotide is added, the pH value is controlled at 8.0±0.3, and three pairs of disulfide bonds are formed by random oxidation to obtain crude linaclotide. after purification, linaclotide with purity of 99.5% and impurities <0.1% is prepared. The synthesis method provided by the invention is simple to operate, and the correct disulfide bond pair can be formed in one step, which greatly improves the production efficiency and reduces the manufacturing cost.
Last Update：2024-01-02 23:10:35
Linaclotide - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 0.655 ml | 3.275 ml | 6.55 ml |
| 5 mM | 0.131 ml | 0.655 ml | 1.31 ml |
| 10 mM | 0.065 ml | 0.327 ml | 0.655 ml |
| 5 mM | 0.013 ml | 0.065 ml | 0.131 ml |
Last Update：2024-01-02 23:10:35
Linaclotide - A novel, oral intestinal epithelial cell guanylate cyclase C agonist-linaclotide
From Wanfang Medicine
Author:
Summary:
irritable bowel syndrome (IBS) is a common clinical functional gastrointestinal disease, and its prevalence rate is increasing year by year. Constipation-predominant irritable bowel syndrome (IBS-C) is a common type of IBS, which may be related to abnormal intestinal contraction, high sensitivity of visceral nerves and brain-gut axis dysfunction. At present, IBS-C treatment has limited improvement in patients' quality of life. Rinaclotide is a polypeptide containing 14 amino acids. It is the first oral intestinal epithelial cell guanylate cyclase C(GC-C) agonist in China. Its mechanism of action is different from the existing IBS-C therapeutic drugs and can effectively improve the symptoms of patients. In addition, the degradation products of linaclotide are mainly distributed in the gastrointestinal tract, so it rarely causes kidney and liver damage, and the efficacy is not affected by liver and kidney functions. The results of a number of randomized, double-blind clinical trials have shown that linaclotide treatment can significantly improve the symptoms of IBS-C patients such as abdominal pain, abdominal discomfort and constipation, and improve the quality of life of patients.
expand
keywords:
linaclotide constipation irritable bowel syndrome constipation abdominal pain
DOI:
10.19577/j.1007-4406.2019.04.012
Year:
2019
Last Update：2023-08-16 22:23:51
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