WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H526070
CAS#: 66898-62-2
Description: Talniflumate is a novel potent and selective inhibitor of core mucin-synthesizing enzyme GCNT3 (core 2b-1,6 N-acetylglucosaminyltrans-ferase).
Hodoodo Cat#: H526070
Name: Talniflumate
CAS#: 66898-62-2
Chemical Formula: C21H13F3N2O4
Exact Mass: 414.08
Molecular Weight: 414.340
Elemental Analysis: C, 60.88; H, 3.16; F, 13.76; N, 6.76; O, 15.45
Synonym: Talniflumate
IUPAC/Chemical Name: 2-[[3-(Trifluoromethyl)phenyl]amino]-3-pyridinecarboxylic acid 1,3-dihydro-3-oxo-1-isobenzofuranyl ester
InChi Key: ANMLJLFWUCQGKZ-UHFFFAOYSA-N
InChi Code: InChI=1S/C21H13F3N2O4/c22-21(23,24)12-5-3-6-13(11-12)26-17-16(9-4-10-25-17)19(28)30-20-15-8-2-1-7-14(15)18(27)29-20/h1-11,20H,(H,25,26)
SMILES Code: O=C(C1=CC=CN=C1NC2=CC=CC(C(F)(F)F)=C2)OC3OC(C4=C3C=CC=C4)=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: >2 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: |
The following data is based on the product molecular weight 414.34 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.
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: |
1: Kim Y, Yim S, Kim BH, Lee S. Pharmacokinetic comparison of two formulations of talniflumate 370 mg tablets in healthy Korean volunteers. Int J Clin Pharmacol Ther. 2017 Jan;55(1):102-108. doi: 10.5414/CP202707. PubMed PMID: 27879193.
2: Rao CV, Janakiram NB, Madka V, Kumar G, Scott EJ, Pathuri G, Bryant T, Kutche H, Zhang Y, Biddick L, Gali H, Zhao YD, Lightfoot S, Mohammed A. Small-Molecule Inhibition of GCNT3 Disrupts Mucin Biosynthesis and Malignant Cellular Behaviors in Pancreatic Cancer. Cancer Res. 2016 Apr 1;76(7):1965-74. doi: 10.1158/0008-5472.CAN-15-2820. Epub 2016 Feb 15. PubMed PMID: 26880801.
3: Kang HA, Lee SM, Park C, Kim DS. Prevalence and predictors of non-steroidal anti-inflammatory drug/analgesic therapeutic duplication in the South Korean ambulatory care setting. Eur J Clin Pharmacol. 2016 Jan;72(1):109-16. PubMed PMID: 26490355.
4: Kim E, Kang W. Contribution of pH to systemic exposure of niflumic acid following oral administration of talniflumate. Eur J Clin Pharmacol. 2011 Apr;67(4):425-428. doi: 10.1007/s00228-010-0980-5. Epub 2011 Feb 17. PubMed PMID: 21327911.
5: Kang W, Kim K. Determination of talniflumate and niflumic acid in human plasma by liquid chromatography-tandem mass spectrometry. Anal Sci. 2009 Apr;25(4):571-4. PubMed PMID: 19359802.
6: Park EJ, Na DH, Shin YH, Lee KC. Liquid chromatography-mass spectrometric method for the sensitive determination of niflumic acid in human plasma and its application to pharmacokinetic study of talniflumate tablet. J Chromatogr B Analyt Technol Biomed Life Sci. 2008 Dec 15;876(2):159-62. doi: 10.1016/j.jchromb.2008.10.010. Epub 2008 Oct 14. PubMed PMID: 19010744.
7: Kang W, Kim K, Kim EY, Kwon KI, Bang JS, Yoon YR. Effect of food on systemic exposure to niflumic acid following postprandial administration of talniflumate. Eur J Clin Pharmacol. 2008 Oct;64(10):1027-30. doi: 10.1007/s00228-008-0524-4. Epub 2008 Jul 8. PubMed PMID: 18607579.
8: Walker NM, Simpson JE, Levitt RC, Boyle KT, Clarke LL. Talniflumate increases survival in a cystic fibrosis mouse model of distal intestinal obstructive syndrome. J Pharmacol Exp Ther. 2006 Apr;317(1):275-83. Epub 2005 Dec 14. PubMed PMID: 16354791.
9: Jung YS, Kim MK, Um YJ, Park HS, Lee EW, Kang JW. The effects on postoperative oral surgery pain by varying NSAID administration times: comparison on effect of preemptive analgesia. Oral Surg Oral Med Oral Pathol Oral Radiol Endod. 2005 Nov;100(5):559-63. PubMed PMID: 16243240.
10: Lee HW, Won KJ, Cho SH, Ha YH, Park WS, Yim HT, Baek M, Rew JH, Yoon SH, Yim SV, Chung JH, Lee KT. Quantitation of niflumic acid in human plasma by high-performance liquid chromatography with ultraviolet absorbance detection and its application to a bioequivalence study of talniflumate tablets. J Chromatogr B Analyt Technol Biomed Life Sci. 2005 Jul 25;821(2):215-20. PubMed PMID: 15921965.
11: Jang DJ, Park JS, Ko HR, Jee JP, Kim JK, Kim ST, Kim CK. Simultaneous determination of niflumic acid and its prodrug, talniflumate in human plasma by high performance liquid chromatography. Biomed Chromatogr. 2005 Jan;19(1):32-5. PubMed PMID: 15470687.
12: Knight D. Talniflumate (Genaera). Curr Opin Investig Drugs. 2004 May;5(5):557-62. Review. PubMed PMID: 15202731.
13: Choi NK, Kim Y, Lee SM, Park BJ. Nonsteroidal Anti-inflammatory Drugs Utilization Patterns among the Elderly with Osteoarthritis at Primary Ambulatory Care Units in Busan Metropolitan City, Korea. J Prev Med Public Health. 2004 May;37(2):150-6. PubMed PMID: 25178446.
14: Donnelly LE, Rogers DF. Therapy for chronic obstructive pulmonary disease in the 21st century. Drugs. 2003;63(19):1973-98. Review. PubMed PMID: 12962514.
15: Los M, Boned JE, Piccinali C. [New esters of substituted anilinonicotinic and phenylanthranilic acids]. Farmaco Sci. 1981 May;36(5):372-85. Spanish. PubMed PMID: 7238853.