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  3. Benzbromarone

Benzbromarone  (Synonyms: 苯溴馬隆)

目錄號: HY-B1135 純度: 99.81%
COA 產(chǎn)品使用指南

Benzbromarone 是一種具有口服活性的抗痛風劑。Benzbromarone 具有抗炎、抗氧化應激和腎保護作用,可用于高尿酸血癥和痛風的研究。

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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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500 mg   詢價  

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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

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

固體

顏色

White to off-white

中文名稱

苯溴馬??;苯溴馬龍;本補麻隆

運輸條件

Room temperature in continental US; may vary elsewhere.

儲存方式
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)
細胞實驗: 

DMSO 中的溶解度 : ≥ 100 mg/mL (235.80 mM; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響,請使用新開封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制儲備液
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
查看完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限:-80°C, 1 year; -20°C, 6 months。-80°C儲存時,請在1年內(nèi)使用, -20°C儲存時,請在6個月內(nèi)使用。

  • 摩爾計算器

  • 稀釋計算器

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

動物實驗:

請根據(jù)您的 實驗動物和給藥方式 選擇適當?shù)娜芙夥桨浮?

以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液,再依次添加助溶劑:
——為保證實驗結(jié)果的可靠性,澄清的儲備液可以根據(jù)儲存條件,適當保存;體內(nèi)實驗的工作液,建議您現(xiàn)用現(xiàn)配,當天使用;
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;如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象,可以通過加熱和/或超聲的方式助溶

  • 方案 一

    請依序添加每種溶劑: 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。

    1 mL 工作液為例,取 100 μL 20.8 mg/mL 的澄清 DMSO 儲備液加到 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。

    1 mL 工作液為例,取 100 μL 20.8 mg/mL 的澄清 DMSO 儲備液加到 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; 如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象,可以通過加熱和/或超聲的方式助溶。

  • 方案 一

    請依序添加每種溶劑: 15% Cremophor EL    85% Saline

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

動物溶解方案計算器
請輸入動物實驗的基本信息:

給藥劑量

mg/kg

動物的平均體重

g

每只動物的給藥體積

μL

動物數(shù)量

由于實驗過程有損耗,建議您多配一只動物的量
請輸入您的動物體內(nèi)配方組成:
%
DMSO +
+
%
Tween-80 +
%
Saline
如果您的動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 2%。
方案所需 助溶劑 包括:DMSO, ,均可在 MCE 網(wǎng)站選購。 ,Tween 80,均可在 MCE 網(wǎng)站選購。
計算結(jié)果
工作液所需濃度 : mg/mL
儲備液配制方法 : mg 藥物溶于 μL  DMSO(母液濃度為 mg/mL)。
您所需的儲備液濃度超過該產(chǎn)品的實測溶解度,以下方案僅供參考,如有需要,請與 MCE 中國技術(shù)支持聯(lián)系。
動物實驗體內(nèi)工作液的配制方法 : 取 μL DMSO 儲備液,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)給藥周期超過半月以上,請謹慎選擇該方案。
請確保第一步儲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

完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復凍融造成的產(chǎn)品失效
儲備液的保存方式和期限:-80°C, 1 year; -20°C, 6 months。-80°C儲存時,請在1年內(nèi)使用, -20°C儲存時,請在6個月內(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
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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:
Benzbromarone
目錄號:
HY-B1135
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