规格 | 价格 | 库存 | 数量 |
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250mg |
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500mg |
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1g |
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2g |
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5g |
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Other Sizes |
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体外研究 (In Vitro) |
OVCAR-3、SKOV-3 和 A2780 珍珠棉系的增殖和克隆形成活性受到盐酸米诺环素(0-100 μM,24-72 小时)的抑制 [3]。米诺环素盐酸盐(0-100 μM,24-48 小时)。在示波器中,盐酸米诺环素(0-100 μM,72 小时))会引起细胞周期 [3]。除了抑制 caspase 依赖性和 caspase 非依赖性细胞死亡外,直接神经保护还可能与线粒体异常和细胞色素 c 保护有关 [2]。盐酸米诺环素诱导缺氧诱导因子(HIF)细胞增殖的检测[3]
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体内研究 (In Vivo) |
在雌性裸鼠中,每天一次静脉注射盐酸卵分泌素(0-30 mg/kg),持续四个星期,可抑制 OVCAR-3 肿瘤的生长[3]。在脑损伤动物模型中,盐酸米诺环素 (IP) 是一种强效药物,在腹腔内高剂量给药时表现出神经保护作用 [1]。盐酸米诺环素(0-40 mg/kg,IP,一次)可显着抑制 METH 诱导的小鼠过度运动和行为敏化 [2]。在暂时性大脑中动脉闭塞 (TMCAO) 模型中,盐酸米诺环素(静脉注射 3 和 10 mg/kg 一次)可有效减少梗塞面积 [1]。盐酸米诺环素(3-10 mg/kg,静脉注射一次)对血液的影响可能会因电位诱发的室性心律失常而减轻。标准 200 mg 剂量对人体的这种作用可能与线粒体 KATP 通道、PI3K/Akt 信号传导和 L 型水平 (3 mg/kg) 有关[1]。
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细胞实验 |
细胞增殖检测[3]
细胞类型:人卵巢癌细胞系(OVCAR-1α抑制,以及up-p53蛋白和AKT水平的调节/mTOR/p70S6K/4E-BP1失活染料 [6]。3. SKOV-3 和 A2780)和原代细胞(HEK-293、HMEC、HUVEC、ATCC) 测试浓度:0、1、10、50 和 100 μM 孵育时间:24、48或72小时 实验结果:抑制OVCAR-3、SKOV-3的增殖和A2780细胞呈浓度依赖性,IC50值分别为62.0、56.1和59.5 μM。对 HEK-293 或 HUVEC 的活力没有影响。 蛋白质印迹分析[3] 细胞类型: OVCAR-3、SKOV-3 和 A2780 细胞 测试浓度: 0、 10、50 和 100 μM 孵育时间:72 小时 实验结果: Cyclins A、B 和 E 低表达水平。 caspase- 增加 3 个水平,在 100 μM 时增加超过 3.0 倍。米诺环素激活的 caspase-3 进而导致 PARP-1 的裂解。 Caspase-3 增加 PARP-1、p89 的降解产物。 细胞周期分析[3] 细胞类型: OVCAR-3、SKOV-3 和 A2 |
动物实验 |
Animal/Disease Models: Female nude mice (6 weeks old, 9 mice per group, each mouse was injected with OVCAR-3 cells subcutaneously (sc) (sc) on the left side of the abdomen) [3]
Doses: 10 or 30 mg/kg Route of Administration: Orally in drinking water Administration, starting on day 8 of cell inoculation, one time/day for 4 weeks. Experimental Results: Inhibited OVCAR-3 tumor growth and diminished microvessel density in these female nude mice. Animal/Disease Models: Male Balb/cAnNCrICrIj mice (8 weeks old, 23-30 g, methamphetamine (METH, 3 mg/kg) subcutaneously (sc) (sc) (sc) in a volume of 10 ml/kg) [2] Doses: 0, 10 , 20 or 40 mg/kg Route of Administration: intraperitoneal (ip) injection, once, 30 minutes before METH administration Experimental Results: 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/Disease Models: Male Sprague-Dawley rats (270-330 g, TMCAO model)[1] Doses: 3 mg/kg and 10 mg/kg Route of Administration: IV, once, 4, 5, or 6 hours post TMCAO Experimental Results: 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/Disease Models: Male Sprague-Dawley rats (270-330 g)[1] Doses: 3, 10, or 20 mg/kg Route of Administration: IV, once Experimental Results: 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. |
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.
[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. [3]. Pourgholami MH, et al. Minocycline inhibits growth of epithelial ovarian cancer. Gynecol Oncol. 2012 May;125(2):433-40. [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. [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. [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. [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. |
分子式 |
C23H28CLN3O7
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分子量 |
493.9373
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CAS号 |
13614-98-7
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相关CAS号 |
Minocycline;10118-90-8
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SMILES |
O=C([C@@]1(O)[C@@](C[C@]2([H])C(C1=O)=C(O)C3=C(O)C=CC(N(C)C)=C3C2)([H])[C@@H]4N(C)C)/C(C4=O)=C(N)/O.[H]Cl
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InChi Key |
KDLQIOPKJDNQIM-YKWOUSISSA-N
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InChi Code |
InChI=1S/C23H27N3O7.ClH/c1-25(2)12-5-6-13(27)15-10(12)7-9-8-11-17(26(3)4)19(29)16(22(24)32)21(31)23(11,33)20(30)14(9)18(15)28;/h5-6,9,11,17,27-28,32-33H,7-8,24H2,1-4H3;1H/b22-16+;/t9-,11-,17+,23-;/m1./s1
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化学名 |
(4S,4aR,5aS,12aR,E)-2-(amino(hydroxy)methylene)-4,7-bis(dimethylamino)-10,11,12a-trihydroxy-4a,5a,6,12a-tetrahydrotetracene-1,3,12(2H,4H,5H)-trione hydrochloride
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别名 |
NSC 141993; Minocycline HCl; NSC 141993; Mynocine hydrochloride; NSC141993; NSC-141993; Periocline; Klinomycin; Minocin; Solodyn; Mynocine; Tri-mino; Vectrin; Ximino; Minomax; Minomycin chloride; Mynocine hydrochloride
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存储方式 |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
运输条件 |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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溶解度 (体外) |
DMSO : ~19.23 mg/mL (~38.93 mM)
H2O : ~9.09 mg/mL (~18.40 mM) |
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溶解度 (体内) |
Solubility in Formulation 1: 7.69 mg/mL (15.57 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
请根据您的实验动物和给药方式选择适当的溶解配方/方案: 1、请先配制澄清的储备液(如:用DMSO配置50 或 100 mg/mL母液(储备液)); 2、取适量母液,按从左到右的顺序依次添加助溶剂,澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明,并不一定代表此产品 的实际溶解配方): 10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline); 假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀/澄清;向上述体系中加入50 μL Tween-80,混合均匀/澄清;然后继续加入450 μL ddH2O (或 saline)定容至 1 mL; 3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例; 4、 如产品在配制过程中出现沉淀/析出,可通过加热(≤50℃)或超声的方式助溶; 5、为保证最佳实验结果,工作液请现配现用! 6、如不确定怎么将母液配置成体内动物实验的工作液,请查看说明书或联系我们; 7、 以上所有助溶剂都可在 Invivochem.cn网站购买。 |
制备储备液 | 1 mg | 5 mg | 10 mg | |
1 mM | 2.0245 mL | 10.1227 mL | 20.2454 mL | |
5 mM | 0.4049 mL | 2.0245 mL | 4.0491 mL | |
10 mM | 0.2025 mL | 1.0123 mL | 2.0245 mL |
1、根据实验需要选择合适的溶剂配制储备液 (母液):对于大多数产品,InvivoChem推荐用DMSO配置母液 (比如:5、10、20mM或者10、20、50 mg/mL浓度),个别水溶性高的产品可直接溶于水。产品在DMSO 、水或其他溶剂中的具体溶解度详见上”溶解度 (体外)”部分;
2、如果您找不到您想要的溶解度信息,或者很难将产品溶解在溶液中,请联系我们;
3、建议使用下列计算器进行相关计算(摩尔浓度计算器、稀释计算器、分子量计算器、重组计算器等);
4、母液配好之后,将其分装到常规用量,并储存在-20°C或-80°C,尽量减少反复冻融循环。
计算结果:
工作液浓度: mg/mL;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL)。如该浓度超过该批次药物DMSO溶解度,请首先与我们联系。
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL ddH2O,混匀澄清。
(1) 请确保溶液澄清之后,再加入下一种溶剂 (助溶剂) 。可利用涡旋、超声或水浴加热等方法助溶;
(2) 一定要按顺序加入溶剂 (助溶剂) 。