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产品描述： Linaclotide is a potent and selective guanylate cyclase C agonist; developed for the treatment of constipation-predominant irritable bowel syndrome (IBS-C) and chronic constipation. |
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靶点：
Guanylate Cyclase;Guanylatecyclase |
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 |
参考文献：
1. Bryant AP, et al. Linaclotide is a potent and selective guanylate cyclase C agonist that elicits pharmacological effects locally in the gastrointestinal tract. Life Sci. 2010 May 8;86(19-20):760-5. 2. Love BL, et al. Linaclotide: a novel agent for chronic constipation and irritable bowel syndrome. Am J Health Syst Pharm. 2014 Jul 1;71(13):1081-91. |
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溶解性：
DMSO : 50 mg/mL (32.75 mM; Need ultrasonic) H2O : 16.67 mg/mL (10.92 mM; ultrasonic and adjust pH to 2 with HCl) |
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保存条件：
-20℃ |
配置溶液浓度参考：
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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 |
| 50 mM |
0.013 ml |
0.065 ml |
0.131 ml |
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| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
北京