Niflumic acid - Moligand™, 10mM in DMSO , Channel blocker of CaCC;Channel blocker of ClC-1;Activator of ClC-Ka;Channel blocker of ClC-Ka;Activator of ClC-Kb;Activator of K Na1.2;Activator of K v7.1;Activator of TRPA1;Channel blocker of TRPC4, CAS No.4394-, Channel blocker of CaCC;Channel blocker of ClC-1;Activator of ClC-Ka;Channel blocker of ClC-Ka;Activator of ClC-Kb;Activator of K Na1.2;Activator of K v7.1;Activator of TRPA1;Channel blocker of TRPC4

CAS: 4394-00-7 Cat. No.: N409062 Peso molecular: 282.22 Beilstein Registry Number: 22(5)13,598 Número EC: 224-516-2

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

2-(3-(trifluoromethyl)phenylamino)nicotinic acid

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Descripción general

Information

Niflumic acid is an inhibitor of cyclooxygenase-2 used for joint and muscular pain.
In vitro

Niflumic acid inhibits Ca²⁺-activated Cl- channels with inhibition constant of 17 mM. Niflumic acid also inhibits ICl(Ca) elicited by bath application of Ca²⁺ to oocytes permeabilized using the Ca²⁺ ionophore A23187, demonstrating that the inhibition of ICl(Ca) is due to a direct interaction with the Cl- channel, rather than by interference with Ca²⁺ entry through voltage-dependent Ca²⁺ channels. Niflumic acid blocks Ca²⁺-activated non-selective cation channels in inside-out patches from the basolateral membrane of rat exocrine pancreatic cells with IC50 of 50 μM. Niflumic acid dose-dependently and reversibly activates large conductance calcium-activated K+ (KCa) channels. Niflumic acid produces a concentration-dependent inhibition of spontaneous transient inward current (STIC, calcium-activated chloride current) amplitude. Niflumic acid inhibits noradrenaline- and caffeine-evoked IO(Ca) with an ICM50 of 6.6 μM, i.e.is less potent against evoked currents compared to spontaneous currents. Niflumic acid voltage-dependently inhibits spontaneous transient inward current (STIC) amplitude with IC50 of 2.3 μM and 1.1 μM at -50 and +50 mV respectively. Niflumic acid inhibits not only IL-13-induced goblet cell hyperplasia but also airway hyperresponsiveness and eosinophilic infiltration. Niflumic suppresses the eotaxin levels in bronchoalveolar lavage fluids and overexpression of the MUC5AC gene, a marker of goblet cell hyperplasia, in the lung after IL-13 instillation. Niflumic acid suppresses JAK2 activation, STAT6 activation, and eotaxin expression in epithelial cells.

In vivo

Cell Data

cell lines：

Concentrations：

Incubation Time：

Powder Purity:≥99%

Specifications

Sinónimos

2-(3-(trifluoromethyl)phenylamino)nicotinic acid

Especificaciones y pureza

Moligand™, 10mM in DMSO

Mecanismos bioquímicos y fisiológicos

Niflumic acid is an inhibitor of cyclooxygenase-2 used for joint and muscular pain.

Condiciones de almacenamiento de almacenamiento

Store at -80°C

Enviado en

Dry ice packs + Cold packs

Este producto requiere envío en cadena de frío. Los servicios terrestres y otros servicios económicos no están disponibles.

Grado

Moligand™

Tipo de acción

ACTIVATOR, CHANNEL BLOCKER

Mecanismo de acción

Channel blocker of CaCC;Channel blocker of ClC-1;Activator of ClC-Ka;Channel blocker of ClC-Ka;Activator of ClC-Kb;Activator of K Na1.2;Activator of K v7.1;Activator of TRPA1;Channel blocker of TRPC4

Nombres e identificadores

• Isómeros SMILES: C1=CC(=CC(=C1)NC2=C(C=CC=N2)C(=O)O)C(F)(F)F
• WGK Alemania: 3
• RTECS: QT2999100
• Peso molecular: 282.22
• Beilstein: 22(5)13,598
• Reaxy-Rn: 489360
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=489360&ln=

Objetivos asociados (humanos)

TRPA1 Tclin Transient receptor potential cation channel subfamily A member 1 (1 Activities)

Discover Target: TRPA1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

TTR Tclin Transthyretin (2 Activities)

Discover Target: TTR

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

PTGS2 Tclin Prostaglandin G/H synthase 2 (1 Activities)

Discover Target: PTGS2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

KCNT2 Tchem Potassium channel subfamily T member 2 (1 Activities)

Discover Target: KCNT2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Propiedades químicas y físicas

• Solubilidad: Solubility (25°C) In vitro DMSO: 66 mg/mL warmed with 50ºC Water: bath (197.54 mM); Ethanol: 20 mg/mL warmed with 50ºC Water: bath (59.86 mM); Water: Insoluble
• Punto de fusión (°C): 203-204 °C

Referencias

1. Shuai Liu, Keming Zheng, Yilin Jiang, Susu Gai, Bohan Li, Dehai Li, Shuang Yang, Zhihua Lv.  (2023)  Biotransformation of Penindolone, an Influenza A Virus Inhibitor.  MOLECULES,  28  (3): (1479).  [PMID:36771146] [10.3390/molecules28031479]

2. Linming Li, Ming Zhang, Dianlong Jia, Zhifang Liu, Ning Zhang, Bin Sun, Zhengping Wang, Min Liu, Qingpeng Wang.  (2022)  Multi-specific niflumic acid platinum(IV) complexes displaying potent antitumor activities by improving immunity and suppressing angiogenesis besides causing DNA damage.  DALTON TRANSACTIONS,  52  (1): (147-158).  [PMID:36472127] [10.1039/D2DT03246E]

3. Kai Ni, Bo Che, Rong Gu, Chunhong Wang, Hongyang Xu, Huiduo Li, Shiyan Cen, Mingzhi Luo, Linhong Deng.  (2024)  BitterDB database analysis plus cell stiffness screening identify flufenamic acid as the most potent TAS2R14-based relaxant of airway smooth muscle cells for therapeutic bronchodilation.  Theranostics,      [PMID:38389834] [10.7150/thno.92492]

4. Dao-Lai Zhang, Yu-Jing Sun, Ming-Liang Ma, Yi-jing Wang, Hui Lin, Rui-Rui Li, Zong-Lai Liang, Yuan Gao, Zhao Yang, Dong-Fang He, Amy Lin, Hui Mo, Yu-Jing Lu, Meng-Jing Li, Wei Kong, Ka Young Chung, Fan Yi, Jian-Yuan Li, Ying-Ying Qin, Jingxin Li, Alex R B Thomsen, Alem W Kahsai, Zi-Jiang Chen, Zhi-Gang Xu, Mingyao Liu, Dali Li, Xiao Yu, Jin-Peng Sun.  (2018)  Gq activity- and β-arrestin-1 scaffolding-mediated ADGRG2/CFTR coupling are required for male fertility.  eLife,      [PMID:29393851] [10.7554/eLife.33432]

5. Yuzhe Wang, Lu sheng, Lin Bu, Huijuan Li, Jianxin Wu, Qing Huang.  (2026)  A novel epidermal mimicking phospholipid vesicle-based permeation assay: EpiPVPA for in vitro permeation evaluation.  INTERNATIONAL JOURNAL OF PHARMACEUTICS,      [PMID:41558553] [10.1016/j.ijpharm.2026.126595]