Minocycline

目录号: HY-17412A 纯度: 98.59%: Data Sheet SDS COA 产品使用指南
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Minocycline 是一种口服有效、能透过血脑屏障的半合成四环素类抗生素。Minocycline 是一种缺氧诱导因子 (HIF-1α) 抑制剂。Minocycline 具有抗癌(anti-cancer)，抗炎(anti-inflammatory) 和谷氨酸 (glutamate) 拮抗作用。Minocycline 降低谷氨酸神经传递，显示神经保护特性和抗抑郁作用。Minocycline 通过与细菌核糖体 30S 亚基结合，抑制细菌蛋白的合成，从而产生抑菌 (bacteriostatic) 作用。

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Minocycline Chemical Structure

CAS No. : 10118-90-8

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Customer Review

Other Forms of Minocycline:

MCE 顾客使用本产品发表的 52 篇科研文献

Proliferation Assay

: Minocycline purchased from MCE. Usage Cited in: J Neuroinflammation. 2018 Aug 30;15(1):245. [Abstract]; Immunostaining of the trigeminal nucleus caudalis (TNC) for Iba1 in the NTG group and the NTG+Minocycline (Mino) group on day 9.

: Minocycline purchased from MCE. Usage Cited in: Neurochem Res. 2017 Oct;42(10):2698-2711. [Abstract]; a Statistical analysis showing the prevention effect of minocycline pretreatment (40 mg/kg/day) on CUS-, CRS- or CSDS-induced decreases in hippocampal microglial numbers. b, c Statistical analysis showing the prevention effect of minocycline pretreatment (40 mg/kg/day) on CUS-, CRS- or CSDS-induced increases in the immobile time in the TST (b) and FST (c).

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生物活性
纯度 & 产品资料
参考文献

生物活性

Minocycline is an orally active, potent and BBB-penetrated semi-synthetic tetracycline antibiotic. Minocycline is a hypoxia-inducible factor (HIF)-1α inhibitor. Minocycline shows anti-cancer, anti-inflammatory, and glutamate antagonist effects. Minocycline reduces glutamate neurotransmission and shows neuroprotective properties and antidepressant effects. Minocycline inhibits bacterial protein synthesis through binding with the 30S subunit of the bacterial ribosome, resulting in a bacteriostatic effect^[1]^[2]^[3]^[4]^[5]^[6]^[7].

IC₅₀ & Target

L-type calcium channel

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
BV-2	IC₅₀	15 μM Compound: MINO	Antineuroinflammatory activity against mouse BV2 cells assessed as inhibition of LPS-induced NO production incubated for 20 hrs by Griess assay Antineuroinflammatory activity against mouse BV2 cells assessed as inhibition of LPS-induced NO production incubated for 20 hrs by Griess assay	[PMID: 33822610]
BV-2	IC₅₀	17.5 μM Compound: Minocycline	Ant-inflammatory LPS-induced mouse BV2 cells assessed as reduction in NO production after 24 hrs by Griess reagent based assay Ant-inflammatory LPS-induced mouse BV2 cells assessed as reduction in NO production after 24 hrs by Griess reagent based assay	[PMID: 32129063]
BV-2	IC₅₀	18.5 μM Compound: Minocycline	Antineuroinflammatory activity in mouse BV2 cells assessed as inhibition of LPS-induced NO production incubated for 24 hrs by Griess assay Antineuroinflammatory activity in mouse BV2 cells assessed as inhibition of LPS-induced NO production incubated for 24 hrs by Griess assay	[PMID: 32141299]
BV-2	IC₅₀	27.2 μM Compound: Minocycline	Antineuroinflammatory activity against mouse BV2 cells assessed as inhibition of LPS-induced NO production incubated for 24 hrs by Griess assay Antineuroinflammatory activity against mouse BV2 cells assessed as inhibition of LPS-induced NO production incubated for 24 hrs by Griess assay	[PMID: 31415170]
BV-2	IC₅₀	35.82 μM Compound: Minocycline	Antineuroinflammatory activity in mouse BV2 cells assessed as inhibition of LPS-induced NO production after 24 hrs in presence of LPS by Griess reaction based assay Antineuroinflammatory activity in mouse BV2 cells assessed as inhibition of LPS-induced NO production after 24 hrs in presence of LPS by Griess reaction based assay	[PMID: 27919656]
BV-2	IC₅₀	37.04 μM Compound: Minocycline	Antineuroinflammatory activity in human BV2 cells assessed as inhibition of LPS-induced NO production after 24 hrs in presence of LPS by Griess reaction Antineuroinflammatory activity in human BV2 cells assessed as inhibition of LPS-induced NO production after 24 hrs in presence of LPS by Griess reaction	[PMID: 27623545]
BV-2	IC₅₀	4.9 μM Compound: Minocycline	Antineuroinflammatory activity in mouse BV2 cells assessed as inhibition of LPS-induced nitric oxide production measured after 24 hrs by Griess assay Antineuroinflammatory activity in mouse BV2 cells assessed as inhibition of LPS-induced nitric oxide production measured after 24 hrs by Griess assay	[PMID: 30350995]
BV-2	IC₅₀	9.07 μM Compound: Minocycline	Antineuroinflammatory activity in mouse BV2 cells assessed as inhibition of LPS-induced NO production after 24 hrs in presence of LPS by Griess reaction based assay Antineuroinflammatory activity in mouse BV2 cells assessed as inhibition of LPS-induced NO production after 24 hrs in presence of LPS by Griess reaction based assay	[PMID: 28911817]
CCRF-CEM	CC₅₀	52.1 μM Compound: minocycline	Cytotoxicity against CEM cells after 5 days by MTT method Cytotoxicity against CEM cells after 5 days by MTT method	[PMID: 17376679]
N9	IC₅₀	19.89 μM Compound: Minocycline	Antineuroinflammatory activity in mouse N9 cells assessed as inhibition of LPS-induced nitric oxide production after 24 hrs by Griess assay Antineuroinflammatory activity in mouse N9 cells assessed as inhibition of LPS-induced nitric oxide production after 24 hrs by Griess assay	[PMID: 28073678]
RAW264.7	IC₅₀	31.28 μM Compound: Minocycline	Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS induced nitric oxide production preincubated for 2 hrs followed by LPS challenge measured after 24 hrs by Griess reagent based assay Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS induced nitric oxide production preincubated for 2 hrs followed by LPS challenge measured after 24 hrs by Griess reagent based assay	[PMID: 29853329]
RAW264.7	IC₅₀	34.81 μM Compound: MINO	Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production after 24 hrs Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production after 24 hrs	[PMID: 23391590]
RAW264.7	IC₅₀	34.85 μM Compound: MINO	Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production after 24 hrs by Griess method Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production after 24 hrs by Griess method	[PMID: 22264489]
RAW264.7	IC₅₀	55.1 μM Compound: Minocycline	Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production after 24 hrs by Griess assay Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production after 24 hrs by Griess assay	[PMID: 27765508]

体外研究
(In Vitro)

Minocycline (0-100 μM，24-72 小时) 可抑制卵巢癌细胞系 (OVCAR-3、SKOV-3 和 A2780) 的增殖和克隆形成活性^[3]。
Minocycline (0-100 μM，24-48 小时) 通过抑制细胞周期蛋白和抑制 DNA 掺入来阻滞细胞周期^[3]。
Minocycline (0-100 μM，72 小时) 可诱导卵巢癌细胞系细胞凋亡^[3]。
Minocycline 具有直接的神经元保护作用，这种保护模式可能是与线粒体完整性和细胞色素c的维持相关，进而抑制胱天蛋白酶依赖性和非胱天蛋白酶依赖性的细胞死亡^[2]。
Minocycline 可抑制缺氧诱导因子 (HIF)-1α，同时上调 p53 蛋白水平并失活 AKT/mTOR/p70S6K/4E-BP1 通路^[6]。

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

Cell Proliferation Assay^[3]

Cell Line:	Human ovarian cancer cell lines (OVCAR-3, SKOV-3 and A2780) and primary cells (HEK-293, HMEC, HUVEC, ATCC)
Concentration:	0, 1, 10, 50 and 100 μM
Incubation Time:	24, 48 or 72 h
Result:	Inhibited proliferation of OVCAR-3, SKOV-3 and A2780 cells in a concentration-dependent manner, with IC₅₀ values of 62.0, 56.1 and 59.5 μM, respectively. Had no effect on the viability of HEK-293 or HUVEC.

Cell Cycle Analysis^[3]

Cell Line:	OVCAR-3, SKOV-3 and A2780 cells
Concentration:	0, 10, 50 and 100 μM
Incubation Time:	24 or 48 h
Result:	Arrested cells in the G0-G1 phase in a concentration and time-dependent manner. Declined percentage of cells in the S and G2-M phases in excess of 80% each at 100 μM.

Western Blot Analysis^[3]

Cell Line:	OVCAR-3, SKOV-3 and A2780 cells
Concentration:	0, 10, 50 and 100 μM
Incubation Time:	72 h
Result:	Expressed lower levels of cyclins A, B and E. Increased caspase-3 levels by more than 3.0 fold in the 100 μM. Minocycline-activated caspase-3 in turn led to cleavage of PARP-1. Increased the degradation product p89 of PARP-1 by caspase-3.

体内研究
(In Vivo)

Minocycline (0-30 mg/kg，口服，每日一次，持续 4 周) 可抑制雌性裸鼠体内 OVCAR-3 肿瘤的生长^[3]。
Minocycline (腹腔注射) 在脑缺血动物模型中，以大剂量腹腔注射给药时，是一种有效的神经保护剂^[1]。
Minocycline (0-40 mg/kg，腹腔注射，一次) 可显著减弱METH诱导的小鼠运动亢进和行为敏化的发展^[2]。
Minocycline (3 和 10 mg/kg，静脉注射，一次) 可有效减少暂时性中梗死面积。脑动脉闭塞模型 (TMCAO)^[1]。
Minocycline 可减轻大鼠缺血诱发的室性心律失常。这种作用可能与 PI3K/Akt 信号通路、线粒体 KATP 通道和 L 型 Ca²⁺ 通道的激活有关^[7]。

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

Animal Model:	Female nude mice (6 weeks old, 9 per group, OVCAR-3 cells were injected s.c. into the left flank of each mouse)^[3]
Dosage:	10 or 30 mg/kg
Administration:	Administered orally in the drinking water, initiated on day 8 of cell inoculation, daily for 4 weeks
Result:	Suppressed OVCAR-3 tumor growth in these female nude mice, and reduced microvessel density.

Animal Model:	Male Balb/cAnNCrICrIj mice (8 weeks old, 23-30 g, methamphetamine (METH, 3 mg/kg) was injected subcutaneously (s.c.) in a volume of 10 ml/kg)^[2]
Dosage:	0, 10, 20, or 40 mg/kg
Administration:	IP, once, 30 min before the administration of METH
Result:	Significantly attenuated METH-induced hyperlocomotion and the development of behavioral sensitization in mice at 40 mg/kg. Did not exert any effect on the induction of METH-induced hyperthermia in mice. Significantly attenuated the reduction of DA and DOPAC in the striatum. Significantly attenuated the reduction of DAT-immunoreactivity in the mouse striatum. Significantly attenuated the increase in MAC1-immunoreactivity in the striatum after the administration of METH.

Animal Model:	Male Sprague-Dawley rats (270-330 g, TMCAO model)^[1]
Dosage:	3 mg/kg and 10 mg/kg
Administration:	IV, once, 4, 5, or 6 hours post TMCAO
Result:	Reduced infarct size by 42% while 10 mg/kg reduced infarct size by 56% at doses of 3 mg/kg; significantly reduced infarct size at 5 hours by 40% at doses of 10 mg/kg and the 3 mg/kg dose significantly reduced infarct size by 34%. With a 6 hour time window there was a non-significant trend in infarct reduction.

Animal Model:	Male Sprague-Dawley rats (270-330 g)^[1]
Dosage:	3, 10, or 20 mg/kg
Administration:	IV, once
Result:	Peak concentrations of serum levels of minocycline averaged 3.6, 13.0 and 28.8 mg/L with 3, 10 and 20 mg/kg doses respectively. The serum levels of minocycline at a 3 mg/kg dose (3.6 mg/L) were similar to that reported in humans after a standard 200 mg dose. Did not significantly affect hemodynamic and physiological variables.

Clinical Trial

分子量

457.48

Formula

C₂₃H₂₇N₃O₇

CAS 号

10118-90-8

性状

固体

颜色

Light yellow to yellow

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据

细胞实验：

DMSO 中的溶解度 : 25 mg/mL (54.65 mM; 超声助溶; 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	2.1859 mL	10.9294 mL	21.8589 mL
5 mM	0.4372 mL	2.1859 mL	4.3718 mL
10 mM	0.2186 mL	1.0929 mL	2.1859 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 (protect from light)。-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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

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 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.46 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。
以 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

每只动物的给药体积

μL

动物数量

只

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）。

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

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: 98.59%

选择批次：

Data Sheet (661 KB) SDS (393 KB)

COA (291 KB) HNMR (296 KB) RP-HPLC (264 KB) LCMS (95 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Xu L, et al. Low dose intravenous minocycline is neuroprotective after middle cerebral artery occlusion-reperfusion in rats. BMC Neurol. 2004 Apr 26;4:7. [Content Brief]

[2]. Zhang L, et al. Protective effects of minocycline on behavioral changes and neurotoxicity in mice after administration of methamphetamine. Prog Neuropsychopharmacol Biol Psychiatry. 2006 Dec 30;30(8):1381-93. [Content Brief]

[3]. Pourgholami MH, et al. Minocycline inhibits growth of epithelial ovarian cancer. Gynecol Oncol. 2012 May;125(2):433-40. [Content Brief]

[4]. Molina-Hernández M, et al. Antidepressant-like actions of minocycline combined with several glutamate antagonists. Prog Neuropsychopharmacol Biol Psychiatry. 2008 Feb 15;32(2):380-6. [Content Brief]

[5]. Ritchie DJ, et al. A review of intravenous minocycline for treatment of multidrug-resistant Acinetobacter infections. Clin Infect Dis. 2014 Dec 1;59 Suppl 6:S374-80. [Content Brief]

[6]. Ataie-Kachoie P, et al. Minocycline attenuates hypoxia-inducible factor-1α expression correlated with modulation of p53 and AKT/mTOR/p70S6K/4E-BP1 pathway in ovarian cancer: in vitro and in vivo studies. Am J Cancer Res. 2015 Jan 15;5(2):575-88. [Content Brief]

[7]. Hu X, Wu B, Wang X, Xu C, He B, Cui B, Lu Z, Jiang H. Minocycline attenuates ischemia-induced ventricular arrhythmias in rats. Eur J Pharmacol. 2011 Mar 11;654(3):274-9. [Content Brief]

Minocycline 相关分类

Neurological Disease Metabolic Disease Inflammation/Immunology Infection Cardiovascular Disease Cancer

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.1859 mL	10.9294 mL	21.8589 mL	54.6472 mL
	5 mM	0.4372 mL	2.1859 mL	4.3718 mL	10.9294 mL
	10 mM	0.2186 mL	1.0929 mL	2.1859 mL	5.4647 mL
	15 mM	0.1457 mL	0.7286 mL	1.4573 mL	3.6431 mL
	20 mM	0.1093 mL	0.5465 mL	1.0929 mL	2.7324 mL
	25 mM	0.0874 mL	0.4372 mL	0.8744 mL	2.1859 mL
	30 mM	0.0729 mL	0.3643 mL	0.7286 mL	1.8216 mL
	40 mM	0.0546 mL	0.2732 mL	0.5465 mL	1.3662 mL
	50 mM	0.0437 mL	0.2186 mL	0.4372 mL	1.0929 mL

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Minocycline

Customer Review

Other Forms of Minocycline:

MCE 顾客使用本产品发表的 52 篇科研文献

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Minocycline

Customer Review

Other Forms of Minocycline:

Minocycline 相关抗体

MCE 顾客使用本产品发表的 52 篇科研文献

Minocycline 相关产品

•相关化合物库:

•同靶点产品:

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查看 Antibiotic 亚型特异性产品:

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生物活性

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参考文献

Minocycline 相关抗体:

摩尔计算器

稀释计算器

Minocycline 相关分类

完整储备液配制表

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