Lubiprostone Inhibitor CAS No. 136790-76-6

Cat. No.	Name	Size	Price
KI0904	Lubiprostone	2 mg	$272
	Lubiprostone	5 mg	$432
	Lubiprostone	10 mg	$752

Chemical Characteristic

Product Name	Lubiprostone
Synonyms	Amitiza, SPI-0211, RU-0211
CAS No.	136790-76-6
Molecular Weight	390.46
Formula	C₂₀H₃₂F₂O₅
Chemical Structure

Biological activities

Lubiprostone is a selective type 2 chloride channel (ClC-2) activator. Lubiprostone is also a member of a new class of bicyclic fatty acid compounds called prostones, which are derived from a metabolite of prostaglandin E1. Lubiprostone is efficacious in the treatment of chronic idiopathic constipation. Lubiprostone induces intestinal secretion and relieves constipation. Lubiprostone accelerates small bowel and colonic transit in healthy subjects.^[1] Lubiprostone enhances intestinal Cl^- and fluid secretion via prostanoid receptor signaling, triggering activation of CFTR.^[2]The EC50 for lubiprostone mediated CFTR activation is 10 nM.^[3]Lubiprostone reduces mucosal-to-serosal fluxes of ³H-mannitol and ¹⁴C-inulin.^[4]In rats, lubiprostone contracts stomach longitudinal muscle and inhibits neuronally mediated contractions of colon circular muscle.^[5]n a mouse model of the genetic disease cystic fibrosis, administration of lubiprostone results in greater mucus accumulation in the small intestine.^[6]

References

[1] Camilleri M, et al. Effect of a selective chloride channel activator, lubiprostone, on gastrointestinal transit, gastric sensory, and motor functions in healthy volunteers. Am J Physiol Gastrointest Liver Physiol. 2006, 290(5): G942-947. 閵嗏偓閵嗏偓 [2] Bijvelds MJ, et al. Activation of intestinal Cl- secretion by lubiprostone requires the cystic fibrosis transmembrane conductance regulator. Gastroenterology. 2009, 137(3): 976-985. 閵嗏偓閵嗏偓 [3] Norimatsu Y, et al. Lubiprostone activates CFTR, but not ClC-2, via the prostaglandin receptor (EP (4)). Biochem Biophys Res Commun. 2012, 426(3): 374-379. 閵嗏偓閵嗏偓 [4] Adam J Moeser, et al. Comparison of the chloride channel activator lubiprostone and the oral laxative Polyethylene Glycol 3350 on mucosal barrier repair in ischemic-injured porcine intestine. World J Gastroenterol. 2008, 14(39): 6012閳?017. 閵嗏偓閵嗏偓 [5] Moeser AJ, et al. Recovery of mucosal barrier function in ischemic porcine ileum and colon is stimulated by a novel agonist of the ClC-2 chloride channel, lubiprostone. Am J Physiol Gastrointest Liver Physiol. 2007, 292(2): G647-656. 閵嗏偓閵嗏偓 [6] De Lisle RC, et al. Lubiprostone stimulates small intestinal mucin release. BMC Gastroenterol. 2012, 12:156. 閵嗏偓閵嗏偓

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