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  1. Membrane Transporter/Ion Channel
  2. Chloride Channel
  3. Fenamic acid

Fenamic acid  (Synonyms: 芬那酸; N-Phenylanthranilic acid)

目錄號(hào): HY-W040265 純度: 98.19%
COA 產(chǎn)品使用指南

Fenamic acid (N-Phenylanthranilic acid, NPAA) 是一種具有口服活性的氯通道阻滯劑。Fenamic acid 是非甾體抗炎劑 (NSAIA) 的基本成分,可衍生甲芬那酸 (mefenamic),托芬那酸 (tofenacin),氟芬那酸 (flufenamic acid) 和 美洛芬酸 (melofenac acid)。Fenamic acid 也可作為抗菌和鎮(zhèn)痛劑。

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Fenamic acid Chemical Structure

Fenamic acid Chemical Structure

CAS No. : 91-40-7

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10 mM * 1 mL in DMSO ¥550
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Customer Review

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

Fenamic acid (N-Phenylanthranilic acid, NPAA) is an orally active chloride channel blocker. Fenamic acid is the basic constituent of non-steroidal anti-inflammatory agents (NSAIA), and derives into mefenamic, tofenacin, flufenac acid and melofenac acid. Fenamic acid also acts as antibacterial and analgesic agent[1]-[6].

IC50 & Target

Chloride Channel[1]

體外研究
(In Vitro)

Fenamic acid (N-Phenylanthranilic acid, NPAA) (2.5 mM; 3 h) inhibits Cl- transportation and blocks 36C1- uptake and efflux in endothelial cells[1][2].
Fenamic acid exhibits selectivity to AKR1B10 (the tumor-marker) over human AR, and inhibits AKR1B10 with IC50s of 0.76 μM (Flufenamic acid), 1.6 μM (Mefenamic acid), 9.89 μM (Meclofenamic acid), respectively[4].
Fenamic acid (4-16 μg/mL; 72 h) inhibits 50% of Neisseria gonorrhoeae with an MIC50 value from 4 to 16 μg/mL (tolfenamic acid, flufenamic acid, and meclofenamic acid) in a low frequency of resistance[5].
Fenamic acid (2-8 μg/mL; 8 h) reduces the expression of the porinflammatory cytokines (IL-8, IL-6 and IL-?) by infected endocervical cells without (>128 μg/mL; 24 h) inhibition towards commensal Lactobacillus spp. belonging healthy female genital microbiota[5].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

體內(nèi)研究
(In Vivo)

RPA-1 is a biomarker in the detection of collecting duct injury in papillary necrosis in male rats[3].
Fenamic acid (N-Phenylanthranilic acid, NPAA) (350-700 mg/kg/day; o.p.; 4 d, 8 d, and 15 d) causes renal papillary necrosis and increases urinary renal papillary antigen-1 (RPA-1) in rats[3].
Fenamic acid (20 g/0.2 mL; i.p.) shows inhibitory effect against the abdominal constriction induced by acetic acid in mice[6].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Wistar Hannover rats (8-10 weeks old; weighting 220-270 g)[3]
Dosage: 50, 350, or up to 700 mg/kg
Administration: Oral gavage; once daily; 7 days or 14 days
Result: Increased absolute paired kidney weights (13.8% at 350 mg/kg and 21.2% at 700/500 mg/kg) and relative to body weight (10.5% at 350 mg/kg/day and 20.3% at 700/500 mg/kg/day).
Caused minimal papillary necrosis of tip with necrosis, hemorrhage, and inflammation of collecting ducts.
Animal Model: Male NMRI mice (weighting 20-25 g); abdominal constriction model (writhing test), induced by acetic acid[6]
Dosage: 100 g/mL, each mice injected with 20 mL
Administration: Intraperitoneal injection; once
Result: Showed anti-nociceptive activity and inhibited the abdominal constriction with the maximal inhibition of 96.3% (Mefenamic acid).
分子量

213.23

Formula

C13H11NO2

CAS 號(hào)
性狀

固體

顏色

Yellow to khaki

中文名稱

芬那酸; N-苯基鄰氨基苯甲酸

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.

儲(chǔ)存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn): 

DMSO 中的溶解度 : 125 mg/mL (586.22 mM; 超聲助溶; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響,請(qǐng)使用新開(kāi)封的 DMSO)

H2O 中的溶解度 : < 0.1 mg/mL (insoluble)

配制儲(chǔ)備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 4.6898 mL 23.4489 mL 46.8977 mL
5 mM 0.9380 mL 4.6898 mL 9.3795 mL
查看完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液;一旦配成溶液,請(qǐng)分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C儲(chǔ)存時(shí),請(qǐng)?jiān)?個(gè)月內(nèi)使用,-20°C儲(chǔ)存時(shí),請(qǐng)?jiān)?個(gè)月內(nèi)使用。

  • 摩爾計(jì)算器

  • 稀釋計(jì)算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質(zhì)量
=
濃度
×
體積
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動(dòng)物實(shí)驗(yàn):

請(qǐng)根據(jù)您的 實(shí)驗(yàn)動(dòng)物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?

以下溶解方案都請(qǐng)先按照 In Vitro 方式配制澄清的儲(chǔ)備液,再依次添加助溶劑:
——為保證實(shí)驗(yàn)結(jié)果的可靠性,澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件,適當(dāng)保存;體內(nèi)實(shí)驗(yàn)的工作液,建議您現(xiàn)用現(xiàn)配,當(dāng)天使用;
以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比;如在配制過(guò)程中出現(xiàn)沉淀、析出現(xiàn)象,可以通過(guò)加熱和/或超聲的方式助溶

  • 方案 一

    請(qǐng)依序添加每種溶劑: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 4.17 mg/mL (19.56 mM); 澄清溶液

    此方案可獲得 ≥ 4.17 mg/mL(飽和度未知)的澄清溶液。

    1 mL 工作液為例,取 100 μL 41.7 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 400 μL PEG300 中,混合均勻;再向上述體系中加入 50 μL Tween-80,混合均勻;然后再繼續(xù)加入 450 μL 生理鹽水 定容至 1 mL。

    生理鹽水的配制:將 0.9 g 氯化鈉,溶解于 ddH?O 并定容至 100 mL,可以得到澄清透明的生理鹽水溶液。
動(dòng)物溶解方案計(jì)算器
請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息:

給藥劑量

mg/kg

動(dòng)物的平均體重

g

每只動(dòng)物的給藥體積

μL

動(dòng)物數(shù)量

由于實(shí)驗(yàn)過(guò)程有損耗,建議您多配一只動(dòng)物的量
請(qǐng)輸入您的動(dòng)物體內(nèi)配方組成:
%
DMSO +
+
%
Tween-80 +
%
Saline
如果您的動(dòng)物是免疫缺陷鼠或者體弱鼠,建議 DMSO 中的在最后工作液體系中的占比盡量不超過(guò) 2%。
方案所需 助溶劑 包括:DMSO, ,均可在 MCE 網(wǎng)站選購(gòu)。 Tween 80,均可在 MCE 網(wǎng)站選購(gòu)。
計(jì)算結(jié)果
工作液所需濃度 : mg/mL
儲(chǔ)備液配制方法 : mg 藥物溶于 μL  DMSO(母液濃度為 mg/mL)。

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

您所需的儲(chǔ)備液濃度超過(guò)該產(chǎn)品的實(shí)測(cè)溶解度,以下方案僅供參考,如有需要,請(qǐng)與 MCE 中國(guó)技術(shù)支持聯(lián)系。
動(dòng)物實(shí)驗(yàn)體內(nèi)工作液的配制方法 : 取 μL DMSO 儲(chǔ)備液,加入 μL 。 μL ,混合均勻至澄清,再加 μL Tween 80,混合均勻至澄清,再加 μL 生理鹽水。
連續(xù)給藥周期超過(guò)半月以上,請(qǐng)謹(jǐn)慎選擇該方案。
請(qǐng)確保第一步儲(chǔ)備液溶解至澄清狀態(tài),從左到右依次添加助溶劑。您可采用超聲加熱 (超聲清洗儀,建議頻次 20-40 kHz),渦旋吹打等方式輔助溶解。
純度 & 產(chǎn)品資料
參考文獻(xiàn)

完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液;一旦配成溶液,請(qǐng)分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C儲(chǔ)存時(shí),請(qǐng)?jiān)?個(gè)月內(nèi)使用,-20°C儲(chǔ)存時(shí),請(qǐng)?jiān)?個(gè)月內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 4.6898 mL 23.4489 mL 46.8977 mL 117.2443 mL
5 mM 0.9380 mL 4.6898 mL 9.3795 mL 23.4489 mL
10 mM 0.4690 mL 2.3449 mL 4.6898 mL 11.7244 mL
15 mM 0.3127 mL 1.5633 mL 3.1265 mL 7.8163 mL
20 mM 0.2345 mL 1.1724 mL 2.3449 mL 5.8622 mL
25 mM 0.1876 mL 0.9380 mL 1.8759 mL 4.6898 mL
30 mM 0.1563 mL 0.7816 mL 1.5633 mL 3.9081 mL
40 mM 0.1172 mL 0.5862 mL 1.1724 mL 2.9311 mL
50 mM 0.0938 mL 0.4690 mL 0.9380 mL 2.3449 mL
60 mM 0.0782 mL 0.3908 mL 0.7816 mL 1.9541 mL
80 mM 0.0586 mL 0.2931 mL 0.5862 mL 1.4656 mL
100 mM 0.0469 mL 0.2345 mL 0.4690 mL 1.1724 mL
Help & FAQs
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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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產(chǎn)品名稱:
Fenamic acid
目錄號(hào):
HY-W040265
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