Minocycline HCl
(Synonyms: 盐酸米诺环素) 目录号 : GC11861
盐酸米诺环素（Minocycline HCl）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。
Cas No.:13614-98-7
Sample solution is provided at 25 µL, 10mM.
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Related Biological Data
Aucubin inhibit the inflammatory responses in microglia. BV2 cells were treated with Aucubin (25, 50, 100 µM) or minocycline (MINO; 50µM) for 12 h and were stimulated with 1 µg/mL LPS for another 24 h. (A, B, C) iNOS and COX-2 protein level were detected and quantified in microglia.
We also diluted tert-butyl hydroperoxide and minocycline (MINO; GLPBIO) in saline to stock concentrations of 100mM and 50 mM, respectively.
Int Immunopharmacol 111 (2022): 109163. PMID: 35994851 IF: 5.5999 -
Related Biological Data
Impairment of synaptic plasticity in hippocampus caused by chronic alcohol exposure were alleviated by administration of minocycline.(b) Confocal z stack and three-dimensional (3D) surface rendering showing the presence of PSD95 in microglia. Scale bar, 5 μm and 1 μm.
According to previous studies, the dose of minocycline (GLPBIO, Cat.NO. GC11861) was 30 mg/kg/day.Single daily injections of Mino (i.p.) were started 3 days prior to alcoholexposure and continued for 28 days.
Experimental Neurology (2022): 114061. PMID: 35367455 IF: 5.33 -
Related Biological Data
The NO inhibitory activity of clerodane diterpenoids from Tinospora sagittata. BV-2 cells were treated with each clerodane diterpenoid and the positive control Mino (with various concentrations) in the presence of 200 ng/mL LPS for 24 h, the supernatants were collected for measurement of NO production.
After incubation for 24 h, the normal control and LPS groups were treated with fresh medium, while the other groups were treated with compounds 2 and 12 and Mino (15 μM)(GLPBIO).
Phytochemistry, 2024, 218: 113932. PMID: 38056516 IF: 3.8001
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| Cell experiment [1]: | |
Cell lines | SH-SY5Y cells |
Preparation Method | SH-SY5Y cells were preincubated for 24h with various concentrations of Minocycline HCl (1, 10, and 50μM) prior to the exposure to the neurotoxin for 24h and 48h. |
Reaction Conditions | 1, 10, 50μM; 24h |
Applications | Minocycline HCl significantly prevented 6-hydroxydopamine (6-OHDA) induced cell death, and a significant protection was observed in the presence of 10μM of the drug. |
| Animal experiment [2]: | |
Animal models | Male CD‐1 mice |
Preparation Method | Mice were given either an intraperitoneal injection of saline or 50 mg/kg Minocycline HCl. This was followed 24 h later by a second injection of 50 mg/kg. Subsequently, treated mice were injected with a 25 mg/kg dose every 24 h for the next 5 days. All animals were killed at day 28 following Spinal cord injury (SCI). |
Dosage form | 25、50mg/kg; i.p. |
Applications | Minocycline HCl in a mouse model of SCI significantly preserves axonal integrity, prevents tissue loss and leads to motor behavioural improvements. |
References: [1] Ossola B, Lantto T A, Puttonen K A, et al. Minocycline protects SH‐SY5Y cells from 6‐hydroxydopamine by inhibiting both caspase‐dependent and‐independent programmed cell death[J]. Journal of neuroscience research, 2012, 90(3): 682-690. [2]Wells J E A, Hurlbert R J, Fehlings M G, et al. Neuroprotection by minocycline facilitates significant recovery from spinal cord injury in mice[J]. Brain, 2003, 126(7): 1628-1637. | |
Minocycline HCl is an orally effective, blood-brain barrier-permeable semisynthetic tetracycline antibiotic[1]. Minocycline HCl is a hypoxia-inducible factor (HIF-1α) inhibitor with anticancer, anti-inflammatory and glutamate antagonist effects, as well as neuroprotective and antidepressant properties[2]. Minocycline HCl inhibits bacterial protein synthesis by binding to the bacterial ribosome 30S subunit, thereby exerting an antibacterial effect[3].
In vitro, treatment of SH-SY5Y cells with Minocycline HCl (10μM) for 24 h significantly inhibited 6-hydroxydopamine (6-OHDA)-induced cell death, and inhibited cell DNA fragmentation and chromatin condensation[4]. Minocycline HCl (0-100μM) treatment of ovarian cancer cell lines (OVCAR-3, SKOV-3 and A2780 cells) for 24-72 h inhibited cell proliferation and colony formation, downregulated the expression of cyclins A, B and E, inhibited DNA synthesis, and also led to DNA laddering, caspase-3 activation and PARP-1 cleavage[5].
In vivo, Minocycline HCl (25, 50mg/kg) was treated by intraperitoneal injection in spinal cord injury model mice for 28 days, which significantly protected axonal integrity, prevented tissue loss and improved motor behavior[6]. Minocycline HCl (3, 10mg/kg) was injected into the jugular vein in rats with transient middle cerebral artery occlusion (TMCAO) model, which effectively reduced the infarct area and significantly improved neurological deficits[7].
References:
[1] Zhou J, Yang J, Dai M, et al. A combination of inhibiting microglia activity and remodeling gut microenvironment suppresses the development and progression of experimental autoimmune uveitis[J]. Biochemical Pharmacology, 2020, 180: 114108.
[2] Pajarillo E, Nyarko-Danquah I, Digman A, et al. Mechanisms of manganese-induced neurotoxicity and the pursuit of neurotherapeutic strategies[J]. Frontiers in Pharmacology, 2022, 13: 1011947.
[3] Singh S, Khanna D, Kalra S. Minocycline and doxycycline: more than antibiotics[J]. Current Molecular Pharmacology, 2021, 14(6): 1046-1065.
[4] Ossola B, Lantto T A, Puttonen K A, et al. Minocycline protects SH‐SY5Y cells from 6‐hydroxydopamine by inhibiting both caspase‐dependent and‐independent programmed cell death[J]. Journal of neuroscience research, 2012, 90(3): 682-690.
[5] Pourgholami M H, Mekkawy A H, Badar S, et al. Minocycline inhibits growth of epithelial ovarian cancer[J]. Gynecologic oncology, 2012, 125(2): 433-440.
[6] Wells J E A, Hurlbert R J, Fehlings M G, et al. Neuroprotection by minocycline facilitates significant recovery from spinal cord injury in mice[J]. Brain, 2003, 126(7): 1628-1637.
[7] Xu L, Fagan S C, Waller J L, et al. Low dose intravenous minocycline is neuroprotective after middle cerebral artery occlusion-reperfusion in rats[J]. BMC neurology, 2004, 4: 1-7.
盐酸米诺环素（Minocycline HCl）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[1]。Minocycline HCl是一种缺氧诱导因子（HIF-1α）抑制剂，具有抗癌、抗炎和谷氨酸拮抗作用，还具有神经保护特性和抗抑郁作用[2]。Minocycline HCl通过与细菌核糖体30S亚基结合，抑制细菌蛋白的合成，从而产生抑菌作用[3]。
在体外，Minocycline HCl（10μM）处理SH-SY5Y细胞24h，显著抑制了6-羟基多巴胺（6-OHDA）诱导的细胞死亡，抑制了细胞DNA断裂和染色质浓缩[4]。Minocycline HCl（0-100μM）处理卵巢癌细胞系 （OVCAR-3、SKOV-3和A2780细胞）24-72h，抑制了细胞增殖和集落形成，下调了细胞周期蛋白A、B和E的表达，抑制了DNA合成，还导致了DNA梯状化、caspase-3活化和PARP-1裂解[5]。
在体内，Minocycline HCl（25、50mg/kg）通过腹腔注射治疗脊髓损伤模型小鼠28天，显著保护了轴突完整性、防止了组织损失并改善了运动行为[6]。Minocycline HCl（3、10mg/kg）通过颈静脉注射暂时性大脑中动脉闭塞（TMCAO）模型大鼠，可有效减少梗死面积，显著改善神经功能缺损[7]。
| Cas No. | 13614-98-7 | SDF | |
| 别名 | 盐酸米诺环素 | ||
| 化学名 | (4S,4aS,5aR,12aR)-4,7-bis(dimethylamino)-1,10,11,12a-tetrahydroxy-3,12-dioxo-4a,5,5a,6-tetrahydro-4H-tetracene-2-carboxamide;hydrochloride | ||
| Canonical SMILES | CN(C)C1C2CC3CC4=C(C=CC(=C4C(=C3C(=O)C2(C(=C(C1=O)C(=O)N)O)O)O)O)N(C)C.Cl | ||
| 分子式 | C23H28ClN3O7 | 分子量 | 493.94 |
| 溶解度 | ≥ 60.7 mg/mL in DMSO with gentle warming, ≥ 7.86 mg/mL in Water with gentle warming | 储存条件 | Store at 2-8°C |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
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，
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 saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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