产品
编 号：F137955
分子式：C23H28ClN3O7
分子量：493.94
分子式：C23H28ClN3O7
分子量：493.94
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
50mg
360
In-stock
100mg
520
In-stock
结构图
CAS No: 13614-98-7
产品详情
生物活性：
Minocycline hydrochloride is an orally active, potent and BBB-penetrated semi-synthetic tetracycline antibiotic. Minocycline hydrochloride is a hypoxia-inducible factor (HIF)-1α inhibitor. Minocycline hydrochloride shows anti-cancer, anti-inflammatory, and glutamate antagonist effects. Minocycline hydrochloride reduces glutamate neurotransmission and shows neuroprotective properties and antidepressant effects. Minocycline hydrochloride inhibits bacterial protein synthesis through binding with the 30S subunit of the bacterial ribosome, resulting in a bacteriostatic effect.
体内研究：
Minocycline hydrochloride (0-30 mg/kg，口服，每日一次，持续 4 周) 抑制雌性裸鼠 OVCAR-3 肿瘤的生长。 Minocycline hydrochloride (IP) 是一种有效的药物当腹腔内给予高剂量时，脑缺血动物模型中的神经保护剂。Minocycline hydrochloride (0-40 mg/kg，IP，一次) 显著减弱 METH 诱导的过度运动和小鼠行为敏化的发展。Minocycline hydrochloride (3 和 10 mg/kg，IV，一次) 可有效减少临时大脑中动脉闭塞模型中的梗塞面积 (TMCAO)。Minocycline hydrochloride (3-10 mg/kg，IV，一次) 导致血清水平 (3 mg/kg) 与人类在标准 200 mg 剂量。Minocycline hydrochloride 可减轻大鼠缺血引起的室性心律失常。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。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)
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)
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)
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)
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.
体外研究：
Minocycline hydrochloride (0-100 μM，24-72 小时) 抑制卵巢癌细胞系 (OVCAR-3、SKOV-3 和 A2780) 的增殖和克隆形成活性。Minocycline hydrochloride (0-100 μM，24-48 h) 通过抑制细胞周期蛋白和抑制 DNA 掺入来抑制细胞周期。Minocycline hydrochloride (0-100 μM，72 h)) 在卵巢癌细胞系中诱导细胞凋亡。Minocycline hydrochloride 显示出直接的神经元保护作用，这种保护模式可能与线粒体完整性和细胞色素 c 的保护有关，随后抑制 caspase 依赖性和非 caspase 依赖性细胞死亡。Minocycline hydrochloride 导致缺氧诱导因子 (HIF)-1α 的抑制，并伴有 up-p53 蛋白水平的调节和 AKT/mTOR/p70S6K/4E-BP1 通路的失活。
Minocycline hydrochloride is an orally active, potent and BBB-penetrated semi-synthetic tetracycline antibiotic. Minocycline hydrochloride is a hypoxia-inducible factor (HIF)-1α inhibitor. Minocycline hydrochloride shows anti-cancer, anti-inflammatory, and glutamate antagonist effects. Minocycline hydrochloride reduces glutamate neurotransmission and shows neuroprotective properties and antidepressant effects. Minocycline hydrochloride inhibits bacterial protein synthesis through binding with the 30S subunit of the bacterial ribosome, resulting in a bacteriostatic effect.
体内研究：
Minocycline hydrochloride (0-30 mg/kg，口服，每日一次，持续 4 周) 抑制雌性裸鼠 OVCAR-3 肿瘤的生长。 Minocycline hydrochloride (IP) 是一种有效的药物当腹腔内给予高剂量时，脑缺血动物模型中的神经保护剂。Minocycline hydrochloride (0-40 mg/kg，IP，一次) 显著减弱 METH 诱导的过度运动和小鼠行为敏化的发展。Minocycline hydrochloride (3 和 10 mg/kg，IV，一次) 可有效减少临时大脑中动脉闭塞模型中的梗塞面积 (TMCAO)。Minocycline hydrochloride (3-10 mg/kg，IV，一次) 导致血清水平 (3 mg/kg) 与人类在标准 200 mg 剂量。Minocycline hydrochloride 可减轻大鼠缺血引起的室性心律失常。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。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)
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)
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)
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)
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.
体外研究：
Minocycline hydrochloride (0-100 μM，24-72 小时) 抑制卵巢癌细胞系 (OVCAR-3、SKOV-3 和 A2780) 的增殖和克隆形成活性。Minocycline hydrochloride (0-100 μM，24-48 h) 通过抑制细胞周期蛋白和抑制 DNA 掺入来抑制细胞周期。Minocycline hydrochloride (0-100 μM，72 h)) 在卵巢癌细胞系中诱导细胞凋亡。Minocycline hydrochloride 显示出直接的神经元保护作用，这种保护模式可能与线粒体完整性和细胞色素 c 的保护有关，随后抑制 caspase 依赖性和非 caspase 依赖性细胞死亡。Minocycline hydrochloride 导致缺氧诱导因子 (HIF)-1α 的抑制，并伴有 up-p53 蛋白水平的调节和 AKT/mTOR/p70S6K/4E-BP1 通路的失活。
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