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Denufosol tetrasodium

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names：
Uridine 5'-(pentahydrogen tetraphosphate), P'''-5'-ester with 2'-deoxycytidine, tetrasodium salt
CAS號：
318250-11-2
MDL Number：
MF(分子式)： C18H23N5Na4O21P4 MW(分子量)： 861.2501
EINECS: Reaxys Number:
Pubchem ID: Brand:BIOFOUNT

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中文別名	Denufosol tetrasodium
英文別名	Denufosol tetrasodium; INS-37217; INS37217; INS 37217.
CAS號	318250-11-2
Inchi	InChI=1S/C18H27N5O21P4.4Na/c19-11-1-3-22(17(28)20-11)13-5-8(24)9(40-13)6-38-45(30,31)42-47(34,35)44-48(36,37)43-46(32,33)39-7-10-14(26)15(27)16(41-10)23-4-2-12(25)21-18(23)29;;;;/h1-4,8-10,13-16,24,26-27H,5-7H2,(H,30,31)(H,32,33)(H,34,35)(H,36,37)(H2,19,20,28)(H,21,25,29);;;;/q;4*+1/p-4/t8-,9+,10+,13+,14+,15+,16+;;;;/m0..../s1
InchiKey	PASYJVRFGUDDEW-WMUGRWSXSA-J
分子式 Formula	C18H23N5Na4O21P4
分子量 Molecular Weight	861.2501
溶解度Solubility
性狀	Solid powder
儲藏條件 Storage conditions	Dry, dark and store at 0-4℃ for short term (days to weeks) or -20℃ for long term (Store correctly 2-3years).

產品說明	Denufosol tetrasodium(CAS:318250-11-2 ):僅限應用于工業(yè)或者科學研究過程中非醫(yī)療目的，不應用于人類或動物的臨床診斷以及治過程療，該產品非藥用，非食用。
Introduction	Denufosol, also known as INS-37217, a P2Y2 agonist potentially for the treatment of cystic fibrosis. Cystic fibrosis is characterised by a defect of the chloride channel CFTR (cystic fibrosis transmembrane conductance regulator) on epithelial cells in the lungs. The CFTR regulates the components of sweat, digestive juices, and mucus. Defects lead to a viscous, dehydrated mucus, hindering mucociliary clearance. Denufosol is an agonist at the P2Y2 subtype of purinergic receptors, an alternative chloride channel. Activating this alternate chloride channel theoretically increases ion transport in cystic fibrosis patients which compensates the effects caused by the non-functioning CFTR.
Application1
Application2
Application3

警示圖
危險性	Warning
危險性警示
安全聲明
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備注

[1]Moss RB. Pitfalls of drug development: lessons learned from trials of denufosol in cystic fibrosis. J Pediatr. 2013 Apr;162(4):676-80. doi: 10.1016/j.jpeds.2012.11.034. Epub 2013 Jan 3. PubMed PMID: 23290508.

[2]Ratjen F, Durham T, Navratil T, Schaberg A, Accurso FJ, Wainwright C, Barnes M, Moss RB; TIGER-2 Study Investigator Group. Long term effects of denufosol tetrasodium in patients with cystic fibrosis. J Cyst Fibros. 2012 Dec;11(6):539-49. doi: 10.1016/j.jcf.2012.05.003. Epub 2012 Jun 8. PubMed PMID: 22682898.

[3] Accurso FJ, Moss RB, Wilmott RW, Anbar RD, Schaberg AE, Durham TA, Ramsey BW; TIGER-1 Investigator Study Group. Denufosol tetrasodium in patients with cystic fibrosis and normal to mildly impaired lung function. Am J Respir Crit Care Med. 2011 Mar 1;183(5):627-34. doi: 10.1164/rccm.201008-1267OC. Epub 2010 Dec 17. PubMed PMID: 21169471.

[4] Kellerman D, Rossi Mospan A, Engels J, Schaberg A, Gorden J, Smiley L. Denufosol: a review of studies with inhaled P2Y(2) agonists that led to Phase 3. Pulm Pharmacol Ther. 2008 Aug;21(4):600-7. doi: 10.1016/j.pupt.2007.12.003. Epub 2007 Dec 31. Review. PubMed PMID: 18276176.

[5] Goss CH, McKone EF, Mathews D, Kerr D, Wanger JS, Millard SP; Cystic Fibrosis Therapeutics Development Network. Experience using centralized spirometry in the phase 2 randomized, placebo-controlled, double-blind trial of denufosol in patients with mild to moderate cystic fibrosis. J Cyst Fibros. 2008 Mar;7(2):147-53. Epub 2007 Aug 28. PubMed PMID: 17728193.

6: Deterding RR, Lavange LM, Engels JM, Mathews DW, Coquillette SJ, Brody AS, Millard SP, Ramsey BW; Cystic Fibrosis Therapeutics Development Network and the Inspire 08-103 Working Group. Phase 2 randomized safety and efficacy trial of nebulized denufosol tetrasodium in cystic fibrosis. Am J Respir Crit Care Med. 2007 Aug 15;176(4):362-9. Epub 2007 Apr 19. PubMed PMID: 17446337.7: Deterding R, Retsch-Bogart G, Milgram L, Gibson R, Daines C, Zeitlin PL, Milla C, Marshall B, Lavange L, Engels J, Mathews D, Gorden J, Schaberg A, Williams J, Ramsey B; Cystic Fibrosis Foundation Therapeutics Development Network. Safety and tolerability of denufosol tetrasodium inhalation solution, a novel P2Y2 receptor agonist: results of a phase 1/phase 2 multicenter study in mild to moderate cystic fibrosis. Pediatr Pulmonol. 2005 Apr;39(4):339-48. PubMed PMID: 15704203.

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