产品信息
抗原名称
Guanylate Cyclase
商品描述
Linaclotide is a peptide agonist of the guanylate cyclase 2C.
分子量
1526.7531
纯度
>98%
可溶性
10 mM in DMSO
In vitro(体外研究)
Linaclotide inhibits in vitro -STa binding to intestinal mucosal membranes from wt mice in a concentration-dependent manner. In contrast, -STa binding to these membranes from GC-C null mice is significantly decreased. After incubation in vitro in jejunal fluid for 30 min, linaclotide is completely degraded. Linaclotide acts on guanylate cyclase-C receptors on the luminal membrane to increase chloride and bicarbonate secretions into the intestine and inhibit the absorption of sodium ions, thus increasing the secretion of water into the lumen and improving defecation; the drug is minimally absorbed into the systemic circulation.
In vivo(体内研究)
Pharmacokinetic analysis shows very low oral bioavailability (0.10%). In intestinal secretion and transit models, linaclotide exhibits significant pharmacological effects in wt, but not in GC-C null mice: induction of increased fluid secretion into surgically ligated jejunal loops is accompanied by the secretion of elevated levels of cyclic guanosine-3',5-monophosphate and accelerated gastrointestinal transit. Linaclotide significantly increases weekly spontaneous bowel movements and complete spontaneous bowel movements (CSBMs) while reducing abdominal pain in patients with chronic constipation.
背景
分子式
C59H79N15O21S6
CAS号
851199-59-2
制备和贮存
保存方式
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
参考图片
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