Fuzapladib

    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 573364

CAS#: 141283-87-6

Description: Fuzapladib, also known as IS 741, is a phospholipase A2 inhibitor. IS-741 attenuates local migration of monocytes and subsequent pancreatic fibrosis in experimental chronic pancreatitis induced by dibutyltin dichloride in rats. IS-741 blocked the adhesion of inflammatory cells to microvascular endothelial cells both in vivo and in vitro. IS-741 suppressed the spontaneous colitis that developed in HLA-B27 rats. Some of the actions of IS-741 may be associated with its inhibitory effects on the adhesion of neutrophils to endothelial cells.

Chemical Structure

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Fuzapladib
CAS# 141283-87-6
Instruction

Theoretical Analysis

MedKoo Cat#: 573364
Name: Fuzapladib
CAS#: 141283-87-6
Chemical Formula: C15H20F3N3O3S
Exact Mass: 379.12
Molecular Weight: 379.400
Elemental Analysis: C, 47.49; H, 5.31; F, 15.02; N, 11.08; O, 12.65; S, 8.45

Price and Availability

This product is not in stock, which may be available by custom synthesis. For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge). Quote less than 1g will not be provided. To request quote, please email to sales @medkoo.com or click below button.
Note: Price will be listed if it is available in the future.

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Synonym: Fuzapladib; IS 741; IS-741; IS741;

IUPAC/Chemical Name: N-[2-(ethanesulfonamido)-5-(trifluoromethyl)pyridin- 3-yl]cyclohexanecarboxamide

InChi Key: TUWCZRFHNIOVTC-UHFFFAOYSA-N

InChi Code: InChI=1S/C15H20F3N3O3S/c1-2-25(23,24)21-13-12(8-11(9-19-13)15(16,17)18)20-14(22)10-6-4-3-5-7-10/h8-10H,2-7H2,1H3,(H,19,21)(H,20,22)

SMILES Code: O=C(C1CCCCC1)NC2=CC(C(F)(F)F)=CN=C2NS(=O)(CC)=O

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >3 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 379.40 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
In vitro protocol:
In vivo protocol:

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1: DeYonker NJ. What a difference a decade has not made: the murky electronic structure of iron monocyanide (FeCN) and iron monoisocyanide (FeNC). J Phys Chem A. 2015 Jan 8;119(1):215-23. doi: 10.1021/jp5110906. Epub 2014 Dec 26. Erratum in: J Phys Chem A. 2015 Jan 29;119(4):815. PMID: 25495149.


2: Liu D, Guo HY, Tang WQ, Yang JQ. Comparative evolution of S7 Intron 1 and ribosomal internal transcribed spacer in Coilia nasus (Clupeiformes: Engraulidae). Int J Mol Sci. 2012;13(3):3085-3100. doi: 10.3390/ijms13033085. Epub 2012 Mar 7. PMID: 22489143; PMCID: PMC3317704.


3: Shimaoka Y, Tajima S, Fujimori F, Yamabayashi C, Moriyama H, Terada M, Takada T, Suzuki E, Bando M, Sugiyama Y, Narita I. Effects of IS-741, a synthetic anti- inflammatory agent, on bleomycin-induced lung injury in mice. Lung. 2009 Sep- Oct;187(5):331-9. doi: 10.1007/s00408-009-9162-6. Epub 2009 Aug 13. PMID: 19672658.


4: Nagashio Y, Otsuki M. Action of antiproteases on fibrosis in experimental chronic pancreatitis. JOP. 2007 Jul 9;8(4 Suppl):495-500. PMID: 17625306.


5: Kaku T, Oono T, Zhao H, Gibo J, Kawabe K, Ito T, Takayanagi R. IS-741 attenuates local migration of monocytes and subsequent pancreatic fibrosis in experimental chronic pancreatitis induced by dibutyltin dichloride in rats. Pancreas. 2007 Apr;34(3):299-309. doi: 10.1097/MPA.0b013e31802fc1fa. PMID: 17414052.


6: Takase K, Ueda T, Kuroda Y. [New aspects of pharmaco-therapy for acute pancreatitis]. Nihon Rinsho. 2004 Nov;62(11):2074-8. Japanese. PMID: 15552891.


7: Fukunaga T, Tsujikawa T, Sasaki M, Fujiyama Y, Bamba T, Fujimiya M. A novel diamino-pyridine derivative (IS-741) attenuates rat ileitis induced by trinitrobenzene sulfonic acid. J Gastroenterol. 2003;38(5):451-9. doi: 10.1007/s00535-002-1081-8. PMID: 12768387.


8: Manabe T. Current aspects of the pathophysiology of acute pancreatitis and therapeutic effects of an inflammatory cell infiltration inhibitor. J Gastroenterol. 2003;38(3):305-7. doi: 10.1007/s005350300055. PMID: 12693385.


9: Imamura T, Niikawa J, Kitamura K, Takahashi A, Ikegami A, Yoshida H, Tanaka S, Mitamura K. Effect of IS-741 on ethionine-induced acute pancreatitis in rats: relation to pancreatic acinar cell regeneration. J Gastroenterol. 2003;38(3):260-7. doi: 10.1007/s005350300045. PMID: 12673449.


10: Makino J, Andoh A, Hata K, Yotsuya S, Shikama H, Imamura M, Fujiyama Y, Bamba T. Inhibitory effects of the new anti-inflammatory agent, IS-741, on spontaneous colitis in HLA-B27/beta2-microglobulin transgenic rats. J Gastroenterol Hepatol. 2002 Aug;17(8):854-60. doi: 10.1046/j.1440-1746.2002.02815.x. PMID: 12164961.


11: Makino J, Andoh A, Hata K, Yotsuya S, Shikama H, Araki Y, Fujiyama Y, Bamba T. Suppressive effects of a new anti-inflammatory agent, IS-741, on dextran sulfate sodium-induced experimental colitis in rats. Int J Mol Med. 2002 Apr;9(4):391-6. PMID: 11891534.


12: Xie MJ, Motoo Y, Su SB, Iovanna JL, Sawabu N. Effect of carboxamide derivative IS-741 on rat spontaneous chronic pancreatitis. Dig Dis Sci. 2002 Jan;47(1):139-47. doi: 10.1023/a:1013232024148. PMID: 11837714.


13: Yotsuya S, Shikama H, Imamura M. Efficacy of the inflammatory cell infiltration inhibitor IS-741 on colitis induced by dextran sulfate sodium in the rat. Jpn J Pharmacol. 2001 Oct;87(2):151-7. doi: 10.1254/jjp.87.151. PMID: 11700014.


14: Bassi C. IS-741 (Ishihara Sangyo). Curr Opin Investig Drugs. 2001 Apr;2(4):510-2. PMID: 11566008.


15: Ogura Y, Matsuda S, Ito M, Niimi R, Sumitomo M, Kawarada Y. Chemoprevention of biliary carcinogenesis in syrian hamsters by the novel carboxamide derivative IS-741 after initiation with N-nitrosobis(2-oxopropyl)amine (BOP). Carcinogenesis. 2000 Aug;21(8):1469-75. PMID: 10910946.


16: Sunamura M, Shibuya K, Yamauchi J, Matsuno S. [Microcirculatory derangement and ischemia of the pancreas]. Nihon Geka Gakkai Zasshi. 1999 May;100(5):342-6. Japanese. PMID: 10412154.


17: Shikama H, Yotsuya S, Satake S, Sugi H, Kato M. Effect of IS-741 on cell adhesion between human umbilical vein endothelial cells and HL-60 cells. Biol Pharm Bull. 1999 Feb;22(2):127-31. doi: 10.1248/bpb.22.127. PMID: 10077429.


18: Liang J, Yamaguchi Y, Matsumura F, Okabe K, Akizuki E, Matsuda T, Ohshiro H, Nakano S, Ishihara K, Ogawa M. Novel carboxamide derivative (IS-741) attenuates lung injury in rats with cerulein-induced pancreatitis complicated by endotoxemia. Dig Dis Sci. 1999 Feb;44(2):341-9. doi: 10.1023/a:1026610702676. PMID: 10063921.


19: Yamaguchi Y, Okabe K, Liang J, Matsumura F, Akizuki E, Matsuda T, Ohshiro H, Nakano S, Ishihara K, Ogawa M. The novel carboxamide derivative IS-741 reduces neutrophil chemoattractant production by bronchoalveolar macrophages in rats with cerulein-induced pancreatitis complicated by sepsis. Digestion. 1999;60 Suppl 1:52-6. doi: 10.1159/000051454. PMID: 10026432.


20: Isaji S, Hayashi J, Higashiguchi T, Yokoi H, Ogura Y, Noguchi T, Kawarada Y. Effect of IS-741 (a new synthetic antiinflammatory agent) on acute necrotizing pancreatitis in dogs. Significance of its inhibitory effect on cytosolic phospholipase A2. Digestion. 1999;60 Suppl 1:47-51. doi: 10.1159/000051453. PMID: 10026431.