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.
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]。
| 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. | |
| 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。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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- Purity: >98.00%
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