Flufenamic acid

製品コードS4268 バッチS426801

印刷

化学情報

Synonyms

N/A

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₁₄H₁₀F₃NO₂

分子量

281.23

CAS No.

530-78-9

Solubility (25°C)*

体外

DMSO

56 mg/mL (199.12 mM)

Ethanol

56 mg/mL (199.12 mM)

Water

Insoluble

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	8%DMSO 1 92%Corn oil この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	4.000mg/ml (14.22mM)	Taking the 1 mL working solution as an example, add 80 μL of 50 mg/ml clear DMSO stock solution to 920 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Flufenamic acidは抗炎症薬であり、イオンチャネル修飾因子としても機能します。
in vitro	Flufenamic acid reversibly inhibits ICl(Ca) in Xenopus oocytes with IC50 of 28 mM, elicit in response to depolarizing voltage steps, in a dose-dependent manner, with no effect on the shape of the current-voltage curve. This compound blocks Ca2(+)-activated non-selective cation channels in inside-out patches from the basolateral membrane of rat exocrine pancreatic cells with IC50 of 10 μM. It binds with high affinity and negative cooperativity (pH 7.6) to wild-type (KD1=30 nM, KD2=255 nM), V30M (KD1=41 nM, KD2=320 nM) and L55P transthyretin (KD1=74 nM, KD2=682 nM), completely inhibiting amyloid fibril formation at a concentration of 10.8 μM, 3× the physiological concentration of transthyretin (3.6 μM), under conditions where transthyretin amyloid fibril formation is maximal (pH 4.4). This compound (viz 200 μM) produces a near complete collapse of the holding current at −50 mV, mirroring the effect of removal of extracellular Ca2+. It inhibits recombinant human TRPM2 (hTRPM2) as well as currents activated by intracellular ADP-ribose in the CRI-G1 rat insulinoma cell line. It antagonises ADP-ribose activated currents in the rat insulinoma cell line CRI-G1 in concentration- and pH-dependent kinetics manner. It reversibly inhibits (IC50 = 13.8 μM) DAPs and phasic firing with a similar time course in rat supraoptic neurones, but has no significant effects (P > 0.05) on membrane potential, spike threshold and input resistance, nor on the frequency and amplitude of spontaneous synaptic potentials.

製品説明

Flufenamic acidは抗炎症薬であり、イオンチャネル修飾因子としても機能します。

in vitro

Flufenamic acid reversibly inhibits ICl(Ca) in Xenopus oocytes with IC50 of 28 mM, elicit in response to depolarizing voltage steps, in a dose-dependent manner, with no effect on the shape of the current-voltage curve. This compound blocks Ca2(+)-activated non-selective cation channels in inside-out patches from the basolateral membrane of rat exocrine pancreatic cells with IC50 of 10 μM. It binds with high affinity and negative cooperativity (pH 7.6) to wild-type (KD1=30 nM, KD2=255 nM), V30M (KD1=41 nM, KD2=320 nM) and L55P transthyretin (KD1=74 nM, KD2=682 nM), completely inhibiting amyloid fibril formation at a concentration of 10.8 μM, 3× the physiological concentration of transthyretin (3.6 μM), under conditions where transthyretin amyloid fibril formation is maximal (pH 4.4). This compound (viz 200 μM) produces a near complete collapse of the holding current at −50 mV, mirroring the effect of removal of extracellular Ca2+. It inhibits recombinant human TRPM2 (hTRPM2) as well as currents activated by intracellular ADP-ribose in the CRI-G1 rat insulinoma cell line. It antagonises ADP-ribose activated currents in the rat insulinoma cell line CRI-G1 in concentration- and pH-dependent kinetics manner. It reversibly inhibits (IC50 = 13.8 μM) DAPs and phasic firing with a similar time course in rat supraoptic neurones, but has no significant effects (P > 0.05) on membrane potential, spike threshold and input resistance, nor on the frequency and amplitude of spontaneous synaptic potentials.

プロトコル(参考用のみ)

参考

https://pubmed.ncbi.nlm.nih.gov/1692608/
https://pubmed.ncbi.nlm.nih.gov/1696554/
https://pubmed.ncbi.nlm.nih.gov/10465408/

https://pubmed.ncbi.nlm.nih.gov/15275834/
https://pubmed.ncbi.nlm.nih.gov/12456832/

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長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。