Flufenamic-acid _COX 抑制劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEFlufenamic acidCat. No.: HY-B1221CAS No.: 530-78-9分式: CHFNO分量: 281.23作靶點(diǎn): COX; AMPK; Potassium Channel; Chloride Channel; CalciumChannel作通路: Immunology/Inflammation; Epigenetics; PI3K/Akt/mTOR;Membrane Transporter/Ion Channel; N

2、euronal Signaling儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 300 mg/mL (1066.74 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 3.5558 mL 17.7790 mL 35.5581 mL5 mM 0.7112 mL 3.5558 mL 7.1116 mL10 mM 0.3556 mL 1.7779 mL 3.5558 mL請根據(jù)產(chǎn)品在

3、不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Flufenamic acid種甾體類抗炎劑，能夠抑制 COX 的活性，激活 AMPK 的活性，調(diào)節(jié)離通道，阻滯氯離通道 (chloride channel) 和 L-型鈣離通道 (L-type Ca2+ channel)，調(diào)節(jié)選擇性陽離通道，激活鉀離通道 (K+ channel) 等。IC50 & Target COX, Chloride Channel, Calcium Channel, Potassium Channel 1, AMPK 21/3 Master of

4、Small Molecules 您邊的抑制劑師www.MedChemE體外研究 Flufenamic acid is a non-steroidal anti-inflammatory agent, inhibits cyclooxygenase (COX), and alsomodulates ion channels, blocking chloride channels and L-type Ca2+ channels, modulating non-selectivecation channels (NSC), activating K+ channels. Flufenamic ac

5、id inhibits a wide spectrum of TRP channels,including: C3, C7, M2, M3, M4, M5, M7, M8, V1, V3, and V4 but activates at least two TRP channels (C6 andA1) 1. Flufenamic acid induces AMPK activation in T84 cells, and such an effect is via a direct stimulation ofcalcium/calmodulin-dependent protein kina

6、se kinase beta (CaMKK) activity 2. Moreover, Flufenamic acid(FFA; 5-50 M) dose-dependently inhibits cAMP-dependent Cl- secretion in intact T84 cells, suppressesCFTR-mediated apical ICl-, and blocks the Ca2+-dependent Cl- secretion in a dose-dependent manner withIC50 of appr 10 M and near complete in

7、hibition at 100 M in T84 cell monolayers, but shows no effect onNa+-K+ ATPase or NKCC in T84 cells 3.體內(nèi)研究 Flufenamic acid (50 mg/kg, i.p.) has anti-inflammatory effect in a mouse model of Vibrio cholerae El Torvariant (EL)-induced diarrhea and significantly abrogates EL-induced intestinal fluid secr

8、etion and barrierdisruption at 20 mg/kg. Furthermore, Flufenamic acid suppresses NF-B nuclear translocation andexpression of proinflammatory mediators and promotes AMPK phosphorylation in the EL-infected mouseintestine 2.PROTOCOLCell Assay 3 In brief, apical and basolateral chambers are filled symme

9、trically with Krebs solutions. Thereafter, DMSO orFlufenamic acid is added into the basolateral chamber followed by apical membrane permealization byamphotericin B. After the amphotericin B-elicited Isc is stabilized, ouabain is added into the basolateralchamber. The ouabain sensitive Isc is used as

10、 an indicator of Na+-K+ ATPase activity 3.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Rats 2Administration 2 Six-week-old male ICR outbred mice (weight 30-35 g) are fasted for 24 h before anesthesia using anintraperitoneal injection of nembut

11、al (60 mg/kg). Following abdominal incision, the ileum is ligated (appr 3-4cm long) and inoculated with 100 L of PBS or PBS containing V. cholerae (105 CFU/loop) with or without aconcomitant intraperitoneal injection of Flufenamic acid or metformin. Twelve hours post-inoculation, ilealloops are remo

12、ved for weight/length ratio measurement, biochemical analysis and ultrastructural evaluation2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.戶使本產(chǎn)品發(fā)表的科研獻(xiàn) Neurosci Lett. 2018 Dec.See more customer validations on HYPERLINK / www.MedChemEREFERENCES2/3 Mast

13、er of Small Molecules 您邊的抑制劑師www.MedChemE1. Guinamard R, et al. Flufenamic acid as an ion channel modulator. Pharmacol Ther. 2013 May;138(2):272-84.2. Pongkorpsakol P, et al. Flufenamic acid protects against intestinal fluid secretion and barrier leakage in a mouse model of Vibriocholerae infection through NF-B inhibition and AMPK activation. Eur J Pharmacol. 2017 Mar 5;798:94-104.3. Pongkorpsakol P, et al. Cellular mechanisms underlying the inhibitory effect of flufenamic acid on chloride secretion in human intestinalepithelial cells. J Pharmacol Sci. 2017 Jun;134(2):