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

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

目录号: HY-66011A 纯度: 99.47%
COA 产品使用指南 技术支持

Moxifloxacin 是一种口服有效的 8-甲氧基喹诺酮类抗菌活性分子,用于急性细菌性鼻窦炎,慢性支气管炎的急性细菌性加重和感染性肺炎的研究。

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Moxifloxacin Chemical Structure

Moxifloxacin Chemical Structure

CAS No. : 151096-09-2

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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

 

细胞效力
(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]
体外研究
(In Vitro)

莫西沙星和阿莫西林的体外活性通过使用感染了L. monocytogenes EGDe的骨髓来源的小鼠巨噬细胞模型的时间杀菌曲线和抑制胞内生长实验进行了比较。莫西沙星的作用速度要快得多,从最初的3小时内就开始发挥作用,并在24小时的培养期内实现完全的肉汤灭菌。莫西沙星似乎对巨噬细胞溶解具有保护作用,因为在24小时的培养后,许多细胞仍然存活[3]

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

体内研究
(In Vivo)

Moxifloxacin (12 mg/kg;静脉注射;每天 1-3 次;持续 7 天;白色雄性 Wistar 大鼠) 每 8 小时处理一次可延长生存期。细菌攻击后 30 小时的组织培养显示,与盐水处理的动物相比,莫西沙星处理的脾脏和肺部的细菌过度生长要少得多,而且没有毒性[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 号
性状

固体

颜色

White to yellow

中文名称

莫西沙星

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
细胞实验: 

DMSO 中的溶解度 : 31.25 mg/mL (77.85 mM; 超声助溶 (<60°C); 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 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
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

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

质量
=
浓度
×
体积
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物实验:

请根据您的 实验动物和给药方式 选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 方案 一

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (6.23 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

    生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
  • 方案 二

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (6.23 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中,混合均匀。

    2 g SBE-β-CD(磺丁基醚 β-环糊精)粉末定容于 10 mL 的生理盐水中,完全溶解至澄清透明。
动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
请输入您的动物体内配方组成:
%
DMSO +
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。
您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
连续给药周期超过半月以上,请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
纯度 & 产品资料

纯度: 99.47%

参考文献

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 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
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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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HY-66011A
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