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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.

• 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.

• 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)

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	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

• 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。

• 1. [1.61] Xin-Yi Liu et al."Trans-ε-viniferin as an inhibitor of TMEM16A preventing intestinal smooth muscle contraction."JOURNAL OF ASIAN NATURAL PRODUCTS RESEARCH.

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *