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Niflumic Acid

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Chemical Structure| 4394-00-7 同义名 : 尼氟酸 ;Actol;Nifluril;Niflumic Acid, Donalgin, Flunir, Niflactol, Niflugel, Nifluril;UP83;Donalgin
CAS号 : 4394-00-7
货号 : A207771
分子式 : C13H9F3N2O2
纯度 : 98%
分子量 : 282.218
MDL号 : MFCD00010569
存储条件：

粉末 Keep in dark place,Inert atmosphere,Room temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(372.05 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • COX-2

  • GABA receptor
描述 Niflumic acid, a drug used for joint and muscular pain, affected Ca²⁺ signaling in different models. In MG63 cells, niflumic acid induced [Ca²⁺]i rises by evoking PLC-dependent (phospholipase C) Ca²⁺ release from the endoplasmic reticulum, and Ca²⁺ entry via PKC-sensitive (protein kinase C) store-operated Ca²⁺ entry. Niflumic acid also induced Ca²⁺-independent cell death[3]. Niflumic acid (10 and 30 mM) also inhibited the noradrenaline-induced increase in perfusion pressure and 30 mM niflumic acid reduced the pressor response to 1 nmol noradrenaline by 34 +/- 6%. The increases in perfusion elicited by 5-HT (0.3 and 3 nmol) were reduced by niflumic acid (10 and 30 mM) in a concentration-dependent manner and 30 mM niflumic acid inhibited responses to 0.3 and 3 nmol 5-HT by, respectively, 49 +/- 8% and 50 +/- 7%. Niflumic acid selectively reduces a component of noradrenaline- and 5-HT-induced pressor responses by inhibiting a mechanism which leads to the opening of voltage-gated calcium channels[4]. Niflumic acid restored core and associated symptoms of peripheral neuropathy by suppressing oxidative-nitrosative stress, inflammatory cytokines (TNF-α, IL-1β) and TRPV1 level in stavudine-induced neuropathic pain in rats. Pharmacological efficacy of niflumic acid (20 mg/kg) was equivalent to pregabalin (30 mg/kg) [5].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.54mL

0.71mL

0.35mL

17.72mL

3.54mL

1.77mL

35.43mL

7.09mL

3.54mL
参考文献

[1]Gogelein H, Dahlem D, et al. Flufenamic acid, mefenamic acid and niflumic acid inhibit single nonselective cation channels in the rat exocrine pancreas. FEBS Lett. 1990 Jul 30;268(1):79-82.

[2]White MM, Aylwin M. Niflumic and flufenamic acids are potent reversible blockers of Ca2(+)-activated Cl- channels in Xenopus oocytes. Mol Pharmacol. 1990 May;37(5):720-4.

[3]Liao WC, Chou CT, Liang WZ, et al. Exploration of Niflumic Acid’s Action on Ca²⁺ Movement and Cell Viability in Human Osteosarcoma Cells. Chin J Physiol. 2018;61(6):341‐348

[4]Criddle DN, de Moura RS, Greenwood IA, Large WA. 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):813‐818

[5]Marwaha L, Bansal Y, Singh R, Saroj P, Sodhi RK, Kuhad A. Niflumic acid, a TRPV1 channel modulator, ameliorates stavudine-induced neuropathic pain. Inflammopharmacology. 2016;24(6):319‐334