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  1. 誘導疾病模型產(chǎn)品 Anti-infection
  2. 內(nèi)分泌與代謝疾病模型 Bacterial Antibiotic
  3. 高尿酸模型
  4. Ethambutol

Ethambutol  (Synonyms: 乙胺丁醇)

目錄號: HY-B0535 純度: ≥98.0%
COA 產(chǎn)品使用指南 技術(shù)支持

Ethambutol是抗分枝桿菌化合物,能通過抑制阿拉伯糖基轉(zhuǎn)移酶活性阻止細胞壁的形成。

MCE 的所有產(chǎn)品僅用作科學研究或藥證申報,我們不為任何個人用途提供產(chǎn)品和服務

Ethambutol Chemical Structure

Ethambutol Chemical Structure

CAS No. : 74-55-5

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10 mM * 1 mL in DMSO ¥440
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10 mg ¥680
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Other Forms of Ethambutol:

MCE 顧客使用本產(chǎn)品發(fā)表的 1 篇科研文獻

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻

生物活性

Ethambutol is a bacteriostatic antimycobacterial agent, which obstructs the formation of cell wall by inhibiting arabinosyl transferases. Target: Antibacterial Ethambutol directly affects two polymers, arabinogalactan (AG) and lipoarabinomannan (LAM) in Mycobacterium smegmatis. In M. smegmatis, Ethambutol inhibits synthesis of arabinan completely and inhibits AG synthesis most likely as a consequence of this; more than 50% of the cell arabinan is released from the bacteria following Ethambutol treatment, whereas no galactan is released. Ethambutol main targets against embB gene product in M. avium. Ethambutol induces 60% changes in the embB gene in M. tuberculosis resistant mutants [1]. Ethambutol is effective against actively growing microorganisms of the genus Mycobacterium, including M. tuberculosis. Nearly all strains of M. tuberculosis and M. kansasii as well as a number of strains of the M. aviumcomplex (MAC) are sensitive to Ethambutol. [1] Ethambutol is potency against M. tuberculosis (H37Rv) with MIC of 0.5 μg/mL in vitro [2]. Ethambutol is efficient on treatment of mycobacterial-infected macrophages. When M. tuberculosis infected macrophages are treated with 6 μg/mL Ethambutol, the log CFUs following treatment for 3 days is 4.17, while value in control group is 4.8. The MICs for M. avium (MTCC 1723) and M. smegmatis (MTCC 6) are 15 μg/mL and 0.18 μg/mL, respectively. Ethambutol is efficient in animal model. 100 mg/kg Ethambutol given orally 15 days post i.v. infection 1 ×/week for 5 weeks, induces a lower log CFU compared with untreatment (4.59 vs 5.07) [3].

細胞效力
(Cellular Effect)
Cell Line Type Value Description References
BMDM CC50
100 μg/mL
Compound: Ethambutol
Cytotoxicity against Swiss mouse BMDM assessed as reduction in cell viability after 24 hrs by MTS assay
Cytotoxicity against Swiss mouse BMDM assessed as reduction in cell viability after 24 hrs by MTS assay
[PMID: 28712709]
HepG2 CC50
> 400 μg/mL
Compound: EMB
Cytotoxicity against human HepG2 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Cytotoxicity against human HepG2 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
[PMID: 33940463]
MRC5 CC50
> 10 μg/mL
Compound: EMB
Cytotoxicity against human MRC5 cells after 24 hrs
Cytotoxicity against human MRC5 cells after 24 hrs
[PMID: 26254828]
RAW264.7 CC50
≥ 400 μg/mL
Compound: EMB
Cytotoxicity against mouse RAW264.7 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Cytotoxicity against mouse RAW264.7 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
[PMID: 33940463]
THP-1 EC50
5.38 mg/L
Compound: Ethambutol
Antimycobacterial activity against Mycobacterium avium ATCC 700898 infected in human THP1 cells assessed as extracellular bacterial killing after 7 days
Antimycobacterial activity against Mycobacterium avium ATCC 700898 infected in human THP1 cells assessed as extracellular bacterial killing after 7 days
[PMID: 20231389]
THP-1 EC50
7.93 mg/L
Compound: Ethambutol
Antimycobacterial activity against Mycobacterium avium ATCC 700898 infected in human THP1 cells assessed as intracellular bacterial killing after 7 days
Antimycobacterial activity against Mycobacterium avium ATCC 700898 infected in human THP1 cells assessed as intracellular bacterial killing after 7 days
[PMID: 20231389]
Vero IC50
> 150 μg/mL
Compound: ethambutol
Cytotoxicity against Vero cells after 48 hrs by XTT method
Cytotoxicity against Vero cells after 48 hrs by XTT method
[PMID: 17888665]
Vero CC50
> 188.5 μM
Compound: Ethambutol
Cytotoxicity against Chlorocebus aethiops (African green monkey) Vero cells assessed as cell viability after 72 hr by MTT assay
Cytotoxicity against Chlorocebus aethiops (African green monkey) Vero cells assessed as cell viability after 72 hr by MTT assay
10.1007/s00044-011-9638-9
Vero IC50
> 200 μg/mL
Compound: EMB
Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability after 72 hrs by MTT assay
Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability after 72 hrs by MTT assay
[PMID: 30145051]
Vero IC50
> 305.9 μM
Compound: Ethambutol
Cytotoxicity against african green monkey Vero cells after 72 hrs by MTT assay
Cytotoxicity against african green monkey Vero cells after 72 hrs by MTT assay
[PMID: 19942326]
Vero IC50
> 305.9 μM
Compound: ethambutol
Cytotoxicity against Vero cells after 72 hrs by MTT assay
Cytotoxicity against Vero cells after 72 hrs by MTT assay
[PMID: 17276683]
Vero IC50
> 50 μg/mL
Compound: Ethambutol
Cytotoxicity against African green monkey Vero cells assessed as cell viability after 72 hrs by MTT assay
Cytotoxicity against African green monkey Vero cells assessed as cell viability after 72 hrs by MTT assay
[PMID: 24044875]
Vero CC50
> 500 μM
Compound: EMB
Cytotoxicity against african green monkey Vero cells after 48 hrs by MTT assay
Cytotoxicity against african green monkey Vero cells after 48 hrs by MTT assay
[PMID: 22626551]
Vero IC50
> 6.25 μg/mL
Compound: Ethambutol
Cytotoxicity against monkey Vero cells assessed as decrease in cell viability after 72 hrs by MTT assay
Cytotoxicity against monkey Vero cells assessed as decrease in cell viability after 72 hrs by MTT assay
[PMID: 28552337]
Vero IC50
> 62.5 μg/mL
Compound: Ethambutol
Cytotoxicity against African green monkey Vero cells assessed as cell viability after 72 hrs by MTT assay
Cytotoxicity against African green monkey Vero cells assessed as cell viability after 72 hrs by MTT assay
[PMID: 24721315]
Vero IC50
> 62.5 μg/mL
Compound: Ethambutol
Cytotoxicity against african green monkey Vero cells after 72 hrs by MTT assay
Cytotoxicity against african green monkey Vero cells after 72 hrs by MTT assay
[PMID: 23352268]
Vero CC50
1470 μM
Compound: EMB
Cytotoxicity against african green monkey Vero cells after 72 hrs by MTT assay
Cytotoxicity against african green monkey Vero cells after 72 hrs by MTT assay
[PMID: 21376586]
Vero CC50
38.51 μg/mL
Compound: A, ETB
Cytotoxicity against african green monkey Vero cells after 72 hrs by resazurin assay
Cytotoxicity against african green monkey Vero cells after 72 hrs by resazurin assay
[PMID: 23474387]
Vero IC50
390.93 μg/mL
Compound: EMB
Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability incubated for 24 hrs by trypan blue staining based assay
Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability incubated for 24 hrs by trypan blue staining based assay
[PMID: 28844400]
體內(nèi)研究
(In Vivo)

誘導高尿酸血癥[5]

致病原理
尿酸水平升高可導致晶體沉積,并可能導致痛風、尿石癥和尿酸鹽腎病。Ethambutol 可通過降低腎臟尿酸清除率而導致尿酸增高,最后形成高尿酸血癥[4][5]。
具體造模方法
Rat[4]: male • Wistar rats • SPF • 200-220 g
Administrtion: 250 mg/kg • intragastric administration • once daily for 23 days
Note
1. Ethambutol 誘導高尿酸模型宜與腺嘌呤 (HY-B0152) 聯(lián)用 (100 mg/kg;灌胃),模型構(gòu)建效果更好[4]。
2. 部分化合物可協(xié)同促進尿酸生成,如:Ethanol 和 Vitamin B12 (HY-B0315)[5]。3. Ethambutol 誘導的高尿酸模型可被黃嘌呤氧化酶抑制劑控制。
造模成功指標
病理變化:胸腺和脾臟出現(xiàn)病理性損傷和炎癥反應;胸腺萎縮、皮質(zhì)髓質(zhì)融合;脾竇充血,有鐵血黃色沉積。
生理指標變化:血清尿酸水平↑;細胞稀疏、組織細胞數(shù)量↑、淋巴細胞數(shù)量↓。
分子層面變化:腎臟勻漿中 URAT1 水平↑,OAT1 水平↓。
拮抗產(chǎn)品 Xanthine Oxidase Inhibitors

誘導視神經(jīng)病變

致病原理
Ethambutol 在一定劑量和時間范圍內(nèi)治療可引起雙眼中毒。目前尚無明確的治療方法可以預防 Ethambutol 誘導視神經(jīng)病變 (EON) 病例中視網(wǎng)膜神經(jīng)元細胞的損傷。
具體造模方法
Rat[6]: Wistar rats • Administration: 35 mg/kg/day &bull po for 30 days
Note
/
造模成功指標
分子變化:Bcl-2、Caspase-3 表達水平↑。
病理指標:神經(jīng)節(jié)細胞損傷,視網(wǎng)膜神經(jīng)節(jié)細胞 (RGC) 密度增加;由于神經(jīng)節(jié)細胞胞漿中形成空泡,RGC 細胞層增厚。
拮抗產(chǎn)品 Citicoline (HY-B0739)

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

Clinical Trial
分子量

204.31

Formula

C10H24N2O2

CAS 號
性狀

固體

顏色

White to off-white

中文名稱

乙胺丁醇;乙二胺二丁醇;乙二胺丁醇

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 6 months
-20°C 1 month
溶解性數(shù)據(jù)
細胞實驗: 

DMSO 中的溶解度 : 100 mg/mL (489.45 mM; 超聲助溶; 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)

配制儲備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 4.8945 mL 24.4726 mL 48.9452 mL
5 mM 0.9789 mL 4.8945 mL 9.7890 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, 6 months; -20°C, 1 month。-80°C儲存時,請在6個月內(nèi)使用,-20°C儲存時,請在1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
計算結(jié)果
工作液所需濃度 : mg/mL
純度 & 產(chǎn)品資料
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, 6 months; -20°C, 1 month。-80°C儲存時,請在6個月內(nèi)使用,-20°C儲存時,請在1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 4.8945 mL 24.4726 mL 48.9452 mL 122.3631 mL
5 mM 0.9789 mL 4.8945 mL 9.7890 mL 24.4726 mL
10 mM 0.4895 mL 2.4473 mL 4.8945 mL 12.2363 mL
15 mM 0.3263 mL 1.6315 mL 3.2630 mL 8.1575 mL
20 mM 0.2447 mL 1.2236 mL 2.4473 mL 6.1182 mL
25 mM 0.1958 mL 0.9789 mL 1.9578 mL 4.8945 mL
30 mM 0.1632 mL 0.8158 mL 1.6315 mL 4.0788 mL
40 mM 0.1224 mL 0.6118 mL 1.2236 mL 3.0591 mL
50 mM 0.0979 mL 0.4895 mL 0.9789 mL 2.4473 mL
60 mM 0.0816 mL 0.4079 mL 0.8158 mL 2.0394 mL
80 mM 0.0612 mL 0.3059 mL 0.6118 mL 1.5295 mL
100 mM 0.0489 mL 0.2447 mL 0.4895 mL 1.2236 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:
Ethambutol
目錄號:
HY-B0535
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