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  2. Anti-infection
  3. Bacterial Antibiotic
  4. Moxifloxacin

Moxifloxacin  (Synonyms: 莫西沙星; BAY 12-8039 free base)

目錄號: HY-66011A 純度: 99.47%
COA 產品使用指南

Moxifloxacin 是一種口服有效的 8-甲氧基喹諾酮類抗菌活性分子，用于急性細菌性鼻竇炎，慢性支氣管炎的急性細菌性加重和感染性肺炎的研究。

MCE 的所有產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品和服務

Moxifloxacin Chemical Structure

Moxifloxacin Chemical Structure

CAS No. : 151096-09-2

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規(guī)格 價格 是否有貨 數(shù)量
100 mg ￥500
In-stock
500 mg ￥1100
In-stock
1 g   詢價  
5 g   詢價  

* Please select Quantity before adding items.

  • 生物活性

  • 純度 & 產品資料

  • 參考文獻

生物活性

Moxifloxacin is an orally active 8-methoxyquinolone antimicrobial for use in the treatment of acute bacterial sinusitis, acute bacterial exacerbations of chronic bronchitis, and community-acquired pneumonia[1][2].

IC50 & Target

Quinolone

 

細胞效力
(Cellular Effect)
Cell Line Type Value Description References
CHO IC50
173 μM
Compound: moxifloxacin
Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits
Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits
[PMID: 23812503]
HEK293 IC50
168.9 μM
Compound: Moxifloxacin
Inhibition of L-type calcium channel measured using 2-electrode voltage-clamp in human embryonic kidney cells heterologically expressing alpha-1C subunit
Inhibition of L-type calcium channel measured using 2-electrode voltage-clamp in human embryonic kidney cells heterologically expressing alpha-1C subunit
[PMID: 22761000]
HeLa IC50
110 μg/mL
Compound: Moxifloxacin
Inhibition of metabolic activity in HeLa cells assessed as MTT reduction after 48 hrs
Inhibition of metabolic activity in HeLa cells assessed as MTT reduction after 48 hrs
[PMID: 17088489]
HeLa IC50
320 μg/mL
Compound: Moxifloxacin
Antiproliferative effect against HeLa cells after 48 hrs
Antiproliferative effect against HeLa cells after 48 hrs
[PMID: 17088489]
HeLa IC50
320 μM
Compound: Moxifloxacin
Inhibition of human HeLa cell proliferation assessed as bromodeoxyuridine incorporation during DNA synthesis after 48 hrs by ELISA
Inhibition of human HeLa cell proliferation assessed as bromodeoxyuridine incorporation during DNA synthesis after 48 hrs by ELISA
[PMID: 19595598]
HEp-2 CC50
> 100 μM
Compound: MXF
Cytotoxicity against human Hep2 cells after 72 hrs by alamar blue assay
Cytotoxicity against human Hep2 cells after 72 hrs by alamar blue assay
[PMID: 21425851]
HEp-2 CC50
> 100 μM
Compound: MXF
Cytotoxicity against human Hep2 cell line after 72 hrs
Cytotoxicity against human Hep2 cell line after 72 hrs
[PMID: 21443219]
HEp-2 CC50
> 100 μM
Compound: MXF
Cytotoxicity against human Hep2 cell line after 72 hrs
Cytotoxicity against human Hep2 cell line after 72 hrs
[PMID: 17228862]
Hepatocyte CC50
> 100 μM
Compound: MXF
Cytotoxicity against rat hepatocytes after 48 hrs
Cytotoxicity against rat hepatocytes after 48 hrs
[PMID: 17228862]
HepG2 EC50
> 100 μM
Compound: 2
Cytotoxicity against human HepG2 cells after 72 hrs by CellTiter Glo assay
Cytotoxicity against human HepG2 cells after 72 hrs by CellTiter Glo assay
[PMID: 33929852]
HepG2 CC50
> 100 μM
Compound: MXF
Cytotoxicity against human HepG2 cells after 72 hrs
Cytotoxicity against human HepG2 cells after 72 hrs
[PMID: 17228862]
HepG2 IC50
> 50 μM
Compound: Moxifloxacin
Cytotoxicity against human HepG2 cells assessed as reduction in cell viability by MTT assay
Cytotoxicity against human HepG2 cells assessed as reduction in cell viability by MTT assay
[PMID: 35500229]
J774.A1 IC50
14.56 μg/mL
Compound: MOX
Cytotoxicity against mouse J774.A1 cells assessed as reduction in cell viability incubated for 24 hrs by resazurin-dye based analysis
Cytotoxicity against mouse J774.A1 cells assessed as reduction in cell viability incubated for 24 hrs by resazurin-dye based analysis
[PMID: 35486992]
K562 EC50
> 100 μM
Compound: 2
Cytotoxicity against human K562 cells after 72 hrs by CellTiter Glo assay
Cytotoxicity against human K562 cells after 72 hrs by CellTiter Glo assay
[PMID: 33929852]
L6 IC50
5.7783 μM
Compound: Moxifloxacin
Cytotoxicity against rat L6 cells assessed as inhibition of cell viability incubated for 24 hrs by MTT assay
Cytotoxicity against rat L6 cells assessed as inhibition of cell viability incubated for 24 hrs by MTT assay
[PMID: 32623216]
MDCK CC50
161 μM
Compound: MXFX
Cytotoxicity against MDCK cells after 48 hrs by CPE assay
Cytotoxicity against MDCK cells after 48 hrs by CPE assay
[PMID: 21481984]
MG-63 IC50
170 μg/mL
Compound: Moxifloxacin
Inhibition of metabolic activity in MG63 cells assessed as MTT reduction after 48 hrs
Inhibition of metabolic activity in MG63 cells assessed as MTT reduction after 48 hrs
[PMID: 17088489]
MG-63 IC50
230 μg/mL
Compound: Moxifloxacin
Antiproliferative effect against MG63 cells assessed as BrdU incorporation into DNA after 48 hrs after 48 hrs
Antiproliferative effect against MG63 cells assessed as BrdU incorporation into DNA after 48 hrs after 48 hrs
[PMID: 17088489]
MG-63 IC50
230 μM
Compound: Moxifloxacin
Inhibition of human MG63 cell proliferation assessed as bromodeoxyuridine incorporation during DNA synthesis after 48 hrs by ELISA
Inhibition of human MG63 cell proliferation assessed as bromodeoxyuridine incorporation during DNA synthesis after 48 hrs by ELISA
[PMID: 19595598]
MRC5 IC50
> 100 μg/mL
Compound: MOX
Cytotoxicity against human MRC5 cells assessed as reduction in cell viability incubated for 24 hrs by resazurin-dye based analysis
Cytotoxicity against human MRC5 cells assessed as reduction in cell viability incubated for 24 hrs by resazurin-dye based analysis
[PMID: 35486992]
NIH3T3 IC50
379.82 μg/mL
Compound: Moxifloxacin
Cytotoxicity against mouse NIH/3T3 cells assessed as reduction in cell proliferation after 24 hrs by MTT assay
Cytotoxicity against mouse NIH/3T3 cells assessed as reduction in cell proliferation after 24 hrs by MTT assay
[PMID: 28174104]
Osteoblast IC50
> 400 μg/mL
Compound: Moxifloxacin
Inhibition of metabolic activity in primary human osteoblasts assessed as MTT reduction after 48 hrs
Inhibition of metabolic activity in primary human osteoblasts assessed as MTT reduction after 48 hrs
[PMID: 17088489]
Osteoblast IC50
160 μg/mL
Compound: Moxifloxacin
Antiproliferative effect against primary human osteoblasts assessed as BrdU incorporation into DNA after 48 hrs
Antiproliferative effect against primary human osteoblasts assessed as BrdU incorporation into DNA after 48 hrs
[PMID: 17088489]
Vero CC50
128 μg/mL
Compound: Moxifloxacin
Cytotoxicity against African green monkey Vero cells incubated for 72 hrs by MTT assay
Cytotoxicity against African green monkey Vero cells incubated for 72 hrs by MTT assay
[PMID: 31352245]
Vero CC50
128 μg/mL
Compound: MXF
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: 29227930]
體外研究
(In Vitro)

莫西沙星和阿莫西林的體外活性通過使用感染了L. monocytogenes EGDe的骨髓來源的小鼠巨噬細胞模型的時間殺菌曲線和抑制胞內生長實驗進行了比較。莫西沙星的作用速度要快得多，從最初的3小時內就開始發(fā)揮作用，并在24小時的培養(yǎng)期內實現(xiàn)完全的肉湯滅菌。莫西沙星似乎對巨噬細胞溶解具有保護作用，因為在24小時的培養(yǎng)后，許多細胞仍然存活[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
體內研究
(In Vivo)

Moxifloxacin (12 mg/kg；靜脈注射；每天 1-3 次；持續(xù) 7 天；白色雄性 Wistar 大鼠) 每 8 小時處理一次可延長生存期。細菌攻擊后 30 小時的組織培養(yǎng)顯示，與鹽水處理的動物相比，莫西沙星處理的脾臟和肺部的細菌過度生長要少得多，而且沒有毒性[4]。

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

Animal Model: 144 white male Wistar rats (18-22 weeks; 300-400 g) infected Stenotrophomonas maltophilia[4]
Dosage: 12 mg/kg
Administration: Intravenous injection; once per day, twice per day, three times per day; for 7 days
Result: Showed considerably less bacterial overgrowth in the spleens and lungs and without being toxic.
Clinical Trial
分子量

401.43

Formula

C21H24FN3O4
CAS 號
性狀

固體

顏色

White to yellow

中文名稱

莫西沙星
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 : 31.25 mg/mL (77.85 mM; 超聲助溶 (<60°C); 吸濕的 DMSO 對產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 質量 1 mg 5 mg 10 mg
1 mM 2.4911 mL 12.4555 mL 24.9109 mL
5 mM 0.4982 mL 2.4911 mL 4.9822 mL
查看完整儲備液配制表

* 請根據(jù)產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個月內使用，-20°C儲存時，請在1個月內使用。

  • 摩爾計算器

  • 稀釋計算器

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

質量
=
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: ≥ 2.5 mg/mL (6.23 mM); 澄清溶液

    此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液。

    以 1 mL 工作液為例，取 100 μL 25.0 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: ≥ 2.5 mg/mL (6.23 mM); 澄清溶液

    此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液。

    以 1 mL 工作液為例，取 100 μL 25.0 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。
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

只
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 中國技術支持聯(lián)系。
動物實驗體內工作液的配制方法 : 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 & 產品資料

純度: 99.47%

參考文獻

完整儲備液配制表

* 請根據(jù)產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個月內使用，-20°C儲存時，請在1個月內使用。

可選溶劑 濃度 溶劑體積 質量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.4911 mL 12.4555 mL 24.9109 mL 62.2774 mL
5 mM 0.4982 mL 2.4911 mL 4.9822 mL 12.4555 mL
10 mM 0.2491 mL 1.2455 mL 2.4911 mL 6.2277 mL
15 mM 0.1661 mL 0.8304 mL 1.6607 mL 4.1518 mL
20 mM 0.1246 mL 0.6228 mL 1.2455 mL 3.1139 mL
25 mM 0.0996 mL 0.4982 mL 0.9964 mL 2.4911 mL
30 mM 0.0830 mL 0.4152 mL 0.8304 mL 2.0759 mL
40 mM 0.0623 mL 0.3114 mL 0.6228 mL 1.5569 mL
50 mM 0.0498 mL 0.2491 mL 0.4982 mL 1.2455 mL
60 mM 0.0415 mL 0.2076 mL 0.4152 mL 1.0380 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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HY-66011A
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