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リナクロチド

リナクロチド 化学構造式
851199-59-2
CAS番号.
851199-59-2
化学名:
リナクロチド
别名:
リナクロチド;リナクロチド (JAN)
英語化学名:
Linaclotide
英語别名:
CY-14;Linaelotide;Linaclotide;Linacllotide;Linaelotide Acetate
CBNumber:
CB82498818
化学式:
C59H79N15O21S6
分子量:
1526.73646
MOL File:
851199-59-2.mol

リナクロチド 物理性質

沸点 :
2045.0±65.0 °C(Predicted)
比重(密度) :
1.60
酸解離定数(Pka):
3.05±0.10(Predicted)

安全性情報

リナクロチド 価格 もっと(2)

メーカー 製品番号 製品説明 CAS番号 包装 価格 更新時間 購入
富士フイルム和光純薬株式会社(wako) W01TRCL465880 リナクロチド
Linaclotide
851199-59-2 10mg ¥43800 2018-12-26 購入
富士フイルム和光純薬株式会社(wako) W01TRCL465880 リナクロチド
Linaclotide
851199-59-2 100mg ¥350000 2018-12-26 購入

リナクロチド 化学特性,用途語,生産方法

効能

蠕動促進薬, エンテロトキシン受容体作動薬

商品名

リンゼス (アステラス製薬)

説明

In August 2012, the US FDA approved linaclotide (also referred to as MD-1100), a first-in-class, orally administered 14-amino acid peptide as a therapy for patients suffering from chronic idiopathic constipation (CIC) and irritable bowel syndrome with constipation (IBS-C). Linaclotide and its active metabolite MM-419447, which results from the cleavage of the C-terminal tyrosine residue by carboxypeptidase A, mimic the actions of the endogenous intestinal peptides guanylin (15 amino acids) and uroguanylin (16 amino acids) by activating guanylyl cyclase C (GC-C) on the intestinal epithelium. Activation of GC-C leads to increased intra- and extracellular levels of cGMP and activation of the CFTR ion channel, resulting in increased levels of HCO3-, Cl-, and water in the intestinal lumen and accelerated gastrointestinal transit. Based on an in vitro assaymeasuring the accumulation of cGMP in T84 cell exposed to an agonist, the EC50 of linaclotide at pH 7.0 was 99±17.5 nM. In preclinical studies in mice using the transit of activated charcoal as ameasure of efficacy, linaclotide at 100 μg/kg significantly accelerated transit compared to wild-type mice treated with charcoal only or GC-Cnullmice treatedwith and without linaclotide.118 Efficacy was also seen in rats treatedwith linaclotide atdoses of 5, 10, and 20 μg/kg. Linaclotide has been synthesized using conventional solid-phase peptide technology.

Originator

Ironwood Pharmaceuticals and Forest Pharmaceuticals (United States)

brand name

Linzess

リナクロチド 上流と下流の製品情報

原材料

準備製品


リナクロチド 生産企業

Global( 111)Suppliers
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