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MedChemExpressModel Niflumic acid -4394-00-7

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Niflumic acid is a calcium-activated chloride channel blocker and COX-2 inhibitor with the IC50 value of 100 nM. Niflumic acid induces apoptosis through caspase-8/Bid/Bax pathway in lung cancer cells. Niflumic acide exhibits anti-tumor activity by affecting the expression of ERK1/2 and the activity of MMP2 and MMP9. Niflumic acid has orally bioactivity. Niflumic acid acts on rheumatoid arthritis[1][2][3][4][5][6][7][8].
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Niflumic acid

MCE China:Niflumic acid

Brand:MedChemExpress (MCE)

Cat. No.HY-B0493

CAS:4394-00-7

Purity:99.88%

Storage:Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year

Shipping:Room temperature in continental US; may vary elsewhere.

Description:Niflumic acid is a calcium-activated chloride channel blocker and COX-2 inhibitor with the IC50 value of 100 nM. Niflumic acid induces apoptosis through caspase-8/Bid/Bax pathway in lung cancer cells. Niflumic acide exhibits anti-tumor activity by affecting the expression of ERK1/2 and the activity of MMP2 and MMP9. Niflumic acid has orally bioactivity. Niflumic acid acts on rheumatoid arthritis.

In Vitro:Niflumic acid (100 and 200 μM; 48 h) combined with Ciglitazone (HY-W011220) exerts cytotoxic effect against A549, H460, and H1299 cells[5]. Niflumic acid (0-300 μM; 36 h) combined with Ciglitazone induces apoptosis in A549, H460, and H1299 cells[5]. Niflumic acid (100 μM; 30 h) combined with Ciglitazone induces activates caspase-8/Bid/Bax pathway in lung cancer cells[5].

In Vivo:Niflumic acid (30 mg/kg; inhalation; 2 times in 10 min) inhibits the secretory response of mucus granules in an pig asthma model [8].

IC50 & Target:COX-2 100 nM (IC50)

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References:

[1]. Criddle, D.N., et al., Inhibitory action of niflumic acid on noradrenaline- and 5-hydroxytryptamine-induced pressor responses in the isolated mesenteric vascular bed of the rat. Br J Pharmacol, 1997. 120(5): p. 813-8.  [Content Brief]

[2]. Jabeen, T., et al., Non-steroidal anti-inflammatory drugs as potent inhibitors of phospholipase A2: structure of the complex of phospholipase A2 with niflumic acid at 2.5 Angstroms resolution. Acta Crystallogr D Biol Crystallogr, 2005. 61(Pt 12): p. 1579-86.  [Content Brief]

[3]. Picollo, A., et al., Mechanism of interaction of niflumic acid with heterologously expressed kidney CLC-K chloride channels. J Membr Biol, 2007. 216(2-3): p. 73-82.  [Content Brief]

[4]. Yuliya V Kucherenko, et al. Niflumic Acid Affects Store-Operated Ca2+-Permeable (SOC) and Ca2+-Dependent K+ and Cl2 Ion Channels and Induces Apoptosis in K562 Cells. J Membr Biol. 2014 Jul;247(7):627-38.  [Content Brief]

[5]. Byeong Mo Kim, et al. Combined treatment with the Cox-2 inhibitor niflumic acid and PPARc ligand ciglitazone induces ER stress/caspase-8-mediated apoptosis in human lung cancer cells. Cancer Lett. 2011 Jan 28;300(2):134-44.  [Content Brief]

[6]. Shengqun Luo , et al. Niflumic acid exhibits anti-tumor activity in nasopharyngeal carcinoma cells through affecting the expression of ERK1/2 and the activity of MMP2 and MMP9. Int J Clin Exp Pathol  [Content Brief]

[7]. I Florentin , et al. MODULATION OF IMMUNE RESPONSES IN MICE BY ORAL ADMINISTRATION OF NIFLUMIC ACID. Int J Immunopharmacol. 1989;11(2):173-83.

[8]. Mitsuko Kondo , et al. Niflumic Acid Inhibits Goblet Cell Degranulation in a Guinea Pig Asthma Model. Allergol Int. 2012 Mar;61(1):133-42.  [Content Brief]

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