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  2. Metabolic Enzyme/Protease Apoptosis Immunology/Inflammation NF-κB MAPK/ERK Pathway Cell Cycle/DNA Damage
  3. Xanthine Oxidase Apoptosis Interleukin Related Keap1-Nrf2 SOD Caspase Bcl-2 Family NF-κB JNK HSP
  4. Benzbromarone

Benzbromarone 是一種具有口服活性的抗痛風(fēng)劑。Benzbromarone 具有抗炎、抗氧化應(yīng)激和腎保護(hù)作用，可用于高尿酸血癥和痛風(fēng)的研究。

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Benzbromarone Chemical Structure

Benzbromarone Chemical Structure

CAS No. : 3562-84-3

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規(guī)格 價(jià)格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥550
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100 mg ￥500
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200 mg   詢價(jià)  
500 mg   詢價(jià)  

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Customer Review

Other Forms of Benzbromarone:

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

Benzbromarone is an orally active anti-gout agent. Benzbromarone has anti-infammatory, anti-oxidative stress and nephroprotective effects. Benzbromarone can be used for the research of hyperuricemia and gout[1][2][3][4].

IC50 & Target

IL-1β

 

IL-8

 

Caspase-8

 

Caspase 9

 

Caspase 3

 

Bcl-2

 

細(xì)胞效力
(Cellular Effect)
Cell Line Type Value Description References
HEK-293T IC50
0.12 μM
Compound: 2
Inhibition of human URAT1 expressed in HEK293T cells assessed as reduction in [14C]uric acid uptake measured after 5 mins by liquid scintillation counting method
Inhibition of human URAT1 expressed in HEK293T cells assessed as reduction in [14C]uric acid uptake measured after 5 mins by liquid scintillation counting method
[PMID: 28351592]
MDCK EC50
39 μM
Compound: 21
Antiviral activity against Influenza A virus A/PR/8/34 (H1N1) infected in MDCK cells assessed as reduction in plaque formation after 2 days by plaque reduction assay
Antiviral activity against Influenza A virus A/PR/8/34 (H1N1) infected in MDCK cells assessed as reduction in plaque formation after 2 days by plaque reduction assay
[PMID: 27046062]
MDCK EC50
39 μM
Compound: 3
Antiviral activity against Influenza A virus (A/PR/8/34) (H1N1) infected in MDCK cells assessed as reduction in plaque formation after 48 hrs by plaque reduction assay
Antiviral activity against Influenza A virus (A/PR/8/34) (H1N1) infected in MDCK cells assessed as reduction in plaque formation after 48 hrs by plaque reduction assay
[PMID: 25856229]
Sf9 IC50
4 μM
Compound: Benzbromarone
Inhibition of Homo sapiens (human) MRP1 expressed in Sf9 cell membranes assessed as decrease in N-ethyl-maleimide-glutathione-induced inorganic phosphate production by spectrophotometric analysis in presence of glutathione
Inhibition of Homo sapiens (human) MRP1 expressed in Sf9 cell membranes assessed as decrease in N-ethyl-maleimide-glutathione-induced inorganic phosphate production by spectrophotometric analysis in presence of glutathione
10.1007/s00044-012-9994-0
Sf9 IC50
4 μM
Compound: Benzbromarone
Inhibition of human MRP1 expressed in Spodoptera frugiperda Sf9 cells assessed as inhibition of NEM-GS-induced vanadate-sensitive ATPase activity measured by generation of inorganic phosphate by spectrophotometry in presence of glutathione
Inhibition of human MRP1 expressed in Spodoptera frugiperda Sf9 cells assessed as inhibition of NEM-GS-induced vanadate-sensitive ATPase activity measured by generation of inorganic phosphate by spectrophotometry in presence of glutathione
[PMID: 21530277]
體外研究
(In Vitro)

Benzbromarone (5-20 μM, 24 h) 保護(hù)人腦微血管內(nèi)皮細(xì)胞 (HBMVECs) 免受 propofol (HY-B0649) 誘導(dǎo)的細(xì)胞毒性[1]。
Benzbromarone (5-20 μM, 24 h) 減輕 propofol (HY-B0649) 誘導(dǎo)的氧化應(yīng)激并抑制人腦微血管內(nèi)皮細(xì)胞 (HBMVECs) 中促炎細(xì)胞因子和趨化因子的表達(dá)[1]。
Benzbromarone (1-100 μM, 2-24 h) 激活 HepG2 細(xì)胞中 NRF2 信號(hào)通路[2]。
Benzbromarone (1-30 μM, 24 h) 促進(jìn) HSP47 降解以改善人瘢痕疙瘩成纖維細(xì)胞中膠原過(guò)度生成[3]。

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

Cell Cytotoxicity Assay[1]

Cell Line: HBMVECs
Concentration: 5 μM, 10 μM, 20 μM
Incubation Time: 24 h
Result: Improved the viability reduced by propofol.

Western Blot Analysis[2]

Cell Line: HepG2 cells
Concentration: 1 μM, 2 μM, 5 μM, 10 μM, 20 μM, 50 μM, 100 μM
Incubation Time: 2 h, 6 h, 24 h
Result: Increased NRF2 protein expression in HepG2 cells exposed for 2 h, 6 h and 24 h at any concentration.
Significantly accumulated the protein of NRF2 in the nuclear fraction after exposure to 100 μM at any time point.
Caused an increase in the protein expression of TRX1 and TRX2.
Significantly increased the ratio of oxidized TRX2 to reduced TRX2 at a concentration of 100 μM.
體內(nèi)研究
(In Vivo)

Benzbromarone (25-50 mg/kg，灌胃，一天一次，連續(xù) 4 周) 可加重高脂飲食 (HFD) 誘導(dǎo)的肥胖 (DIO)小鼠的肝臟脂肪變性[3]。
Benzbromarone (10 mg/kg，灌胃，一天一次，連續(xù) 14 天) 可減輕 cisplatin(HY-17394) 所致大鼠腎毒性[4]。

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

Animal Model: High fat diet (HFD)-induced obese (DIO) mice[3]
Dosage: 25 mg/kg, 50 mg/kg
Administration: Intragastric (i.g.)
Result: Aggravated lipid accumulation in the liver of DIO mice.
Significantly increased triglyceride accumulation and AST, ALT levels.
Regulated multiple lipid metabolism genes and the expression of protein markers associated with apoptosis, endoplasmic reticulum stress, and inflammation in the liver of DIO mice.
Animal Model: Cisplatin treated rats[2]
Dosage: 10 mg/kg
Administration: Oral gavage (p.o.)
Result: Ameliorated the elevation in serum creatinine and blood urea nitrogen (BUN) levels induced by cisplatin.
Counteracted oxidative stress induced by cisplatin and enhances anti-oxidant defenses in kidney.
Alleviated the inflammatory events of nephrotoxicity induced by cisplatin.
Attenuated cisplatin-induced apoptosis.
Clinical Trial
分子量

424.08

Formula

C17H12Br2O3
CAS 號(hào)
性狀

固體

顏色

White to off-white

中文名稱

苯溴馬?。槐戒羼R龍；本補(bǔ)麻隆
運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.
儲(chǔ)存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 1 year
-20°C 6 months
溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn)： 

DMSO 中的溶解度 : ≥ 100 mg/mL (235.80 mM; 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)

* "≥" means soluble, but saturation unknown.

配制儲(chǔ)備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 2.3580 mL 11.7902 mL 23.5805 mL
5 mM 0.4716 mL 2.3580 mL 4.7161 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, 1 year; -20°C, 6 months。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(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: ≥ 2.08 mg/mL (4.90 mM); 澄清溶液

    此方案可獲得 ≥ 2.08 mg/mL（飽和度未知）的澄清溶液。

    以 1 mL 工作液為例，取 100 μL 20.8 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。
  • 方案 二

    請(qǐng)依序添加每種溶劑： 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 2.08 mg/mL (4.90 mM); 懸濁液; 超聲助溶

    此方案可獲得 2.08 mg/mL的均勻懸濁液，懸濁液可用于口服和腹腔注射。

    以 1 mL 工作液為例，取 100 μL 20.8 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液 中，混合均勻。

    2 g SBE-β-CD（磺丁基醚 β-環(huán)糊精）粉末定容于 10 mL 的生理鹽水中，完全溶解至澄清透明。

以下溶解方案，請(qǐng)直接配制工作液。建議現(xiàn)用現(xiàn)配，在短期內(nèi)盡快用完。 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： 15% Cremophor EL    85% Saline

    Solubility: 2.5 mg/mL (5.90 mM); 澄清溶液; 超聲助溶 (<60°C)

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

只
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）。
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

純度: 99.81%

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, 1 year; -20°C, 6 months。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(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 2.3580 mL 11.7902 mL 23.5805 mL 58.9511 mL
5 mM 0.4716 mL 2.3580 mL 4.7161 mL 11.7902 mL
10 mM 0.2358 mL 1.1790 mL 2.3580 mL 5.8951 mL
15 mM 0.1572 mL 0.7860 mL 1.5720 mL 3.9301 mL
20 mM 0.1179 mL 0.5895 mL 1.1790 mL 2.9476 mL
25 mM 0.0943 mL 0.4716 mL 0.9432 mL 2.3580 mL
30 mM 0.0786 mL 0.3930 mL 0.7860 mL 1.9650 mL
40 mM 0.0590 mL 0.2948 mL 0.5895 mL 1.4738 mL
50 mM 0.0472 mL 0.2358 mL 0.4716 mL 1.1790 mL
60 mM 0.0393 mL 0.1965 mL 0.3930 mL 0.9825 mL
80 mM 0.0295 mL 0.1474 mL 0.2948 mL 0.7369 mL
100 mM 0.0236 mL 0.1179 mL 0.2358 mL 0.5895 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    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：
Benzbromarone
目錄號(hào)：
HY-B1135
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