Omadacycline hydrochloride (PTK0796 hydrochloride)
(Synonyms: PTK0796 hydrochloride; Amadacycline hydrochloride) 目录号 : GC32064
Omadacycline hydrochloride (PTK0796 hydrochloride)是一种氨甲基环素类四环素抗生素。
Cas No.:1196800-39-1
Sample solution is provided at 25 µL, 10mM.
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Omadacycline hydrochloride (PTK0796 hydrochloride) is an aminomethylcycline tetracycline antibiotic[1]. Omadacycline hydrochloride inhibits bacterial protein synthesis by binding the primary tetracycline binding site on the 30S subunit of the bacterial ribosome [2]. Omadacycline hydrochloride overcomes common tetracycline resistance mechanisms and has been widely used to inhibit drug-resistant Gram-positive pathogens, including methicillin-resistant Staphylococcus aureus (MRSA), penicillin-resistant and macrolide-resistant Streptococcus pneumoniae, vancomycin-resistant Enterococci (VRE), and Clostridium difficile [3].
In vitro, Omadacycline hydrochloride treatment significantly inhibited the activity of P. falciparum strain 3D7 with an IC50 value of 8.443±0.618µM at 3 days and 0.248±0.109µM at 6 days[4]. Treatment of THP-1-derived macrophages with Omadacycline hydrochloride (100µg/ml) 30 minutes before lipopolysaccharide (LPS) stimulation resulted in a significant decrease in IL-6, CXCL-1, and MMP-9 expression and inhibited IL-8-induced neutrophil chemotaxis[5].
In vivo, Omadacycline hydrochloride treatment via intraperitoneal injection at a dose of 20mg/kg/day for 3 days decreased the parasite load and increased the survival of P. berghei infectious murine model[6]. Omadacycline hydrochloride (5mg/kg) administered intraperitoneally every 12 hours for 6 days inhibited the production of multiple proinflammatory cytokines and reduced neutrophil infiltration in the lungs, improving survival in a mouse model of post-influenza MRSA [7].
References:
[1] Karlowsky J A, Steenbergen J, Zhanel G G. Microbiology and preclinical review of omadacycline[J]. Clinical Infectious Diseases, 2019, 69(Supplement_1): S6-S15.
[2] Zhanel G G, Esquivel J, Zelenitsky S, et al. Omadacycline: a novel oral and intravenous aminomethylcycline antibiotic agent[J]. Drugs, 2020, 80(3): 285.
[3] Burgos R M, Rodvold K A. Omadacycline: a novel aminomethylcycline[J]. Infection and Drug Resistance, 2019: 1895-1915.
[4] de Carvalho L P, Groeger-Otero S, Kreidenweiss A, et al. Boromycin has rapid-onset antibiotic activity against asexual and sexual blood stages of Plasmodium falciparum[J]. Frontiers in Cellular and Infection Microbiology, 2022, 11: 802294.
[5] Sanders M, Beringer P. Immunomodulatory activity of omadacycline in vitro and in a murine model of acute lung injury[J]. mSphere, 2024, 9(11): e00671-24.
[6] Madejczyk M S, Leed S E, Kudyba K, et al. In vitro activity and in vivo efficacy of omadacycline against Plasmodium species[J]. Malaria Journal, 2025, 24(1): 194.
[7] Gomi S, Price E, Burgoyne H, et al. Omadacycline exhibits anti-inflammatory properties and improves survival in a murine model of post-influenza MRSA pneumonia[J]. Antimicrobial Agents and Chemotherapy, 2025, 69(9): e00469-25.
Omadacycline hydrochloride (PTK0796 hydrochloride)是一种氨甲基环素类四环素抗生素[1]。Omadacycline hydrochloride通过结合细菌核糖体30S亚基上的主要四环素结合位点抑制细菌蛋白质合成[2]。Omadacycline hydrochloride能够克服常见的四环素耐药机制，已广泛应用于抑制耐药革兰氏阳性病原体，包括耐甲氧西林金黄色葡萄球菌（MRSA）、耐青霉素和耐大环内酯类肺炎链球菌、耐万古霉素肠球菌（VRE）以及艰难梭菌[3]。
在体外，Omadacycline hydrochloride处理3天和6天可分别抑制恶性疟原虫3D7株活性，IC50值为8.443±0.618µM和0.248±0.109µM[4]。脂多糖（LPS）刺激前30分钟用100µg/ml的Omadacycline hydrochloride预处理THP-1来源的巨噬细胞能显著降低IL-6、CXCL-1和MMP-9表达，并抑制IL-8诱导的中性粒细胞趋化[5]。
在体内，伯氏疟原虫感染小鼠模型每日腹腔注射Omadacycline hydrochloride（20mg/kg/天；持续3天）可降低寄生虫负荷并提高生存率[6]。流感后MRSA肺炎小鼠模型每12小时腹腔注射5mg/kg剂量的Omadacycline hydrochloride（持续6天）能抑制多种促炎细胞因子产生并减少肺部中性粒细胞浸润，提高生存率[7]。
| Cell experiment [1]: | |
Cell lines | THP-1 cells |
Preparation Method | THP-1 cells were seeded in six-well culture plates at a density of 2×106 cells/well in triplicate per well in RPMI 1640 complete medium containing 10% FBS. THP-1 cells were preincubated with vehicle, dexamethasone (1µM), or Omadacycline hydrochloride (20, 40, 60, 80, or 100µg/ml) for 30min at 37°C and subsequently stimulated with LPS (100ng/mL) for 24h. Cell supernatants were collected and cytokine/chemokine levels were analyzed by ELISA. |
Reaction Conditions | 20, 40, 60, 80, or 100µg/ml; 30min |
Applications | Omadacycline hydrochloride treatment resulted in significant, dose-dependent reductions in IL-6, CXCL-1, and MMP-9 expression. |
| Animal experiment [2]: | |
Animal models | Female albino C57BL/6 mice |
Preparation Method | Female albino C57BL/6 mice weighing 18-22g were acclimated for 7 days. Mice were housed in designated rooms with ad libitum access to food and water and followed a 12:12h light/dark cycle. On day 0, mice were infected with 104 luciferase-expressing Plasmodia burgdorferi sporozoites (ANKA strain) by tail vein injection. Omadacycline hydrochloride 20mg/kg/day was administered intraperitoneally (i.p.) for three days, after which mice were subjected to in vivo bioluminescence imaging analysis. |
Dosage form | 20mg/kg/day for 3 days; i.p. |
Applications | Omadacycline hydrochloride treatment decreased bioluminescent signal and increase the survival of mice. |
References: | |
| Cas No. | 1196800-39-1 | SDF | |
| 别名 | PTK0796 hydrochloride; Amadacycline hydrochloride | ||
| Canonical SMILES | O=C(C1=C(O)[C@@H](N(C)C)[C@@](C[C@@]2([H])C(C(C3=C(O)C(CNCC(C)(C)C)=CC(N(C)C)=C3C2)=O)=C4O)([H])[C@@]4(O)C1=O)N.Cl | ||
| 分子式 | C29H40N4O7.HCl | 分子量 | 593.11 |
| 溶解度 | Water : ≥ 50 mg/mL (84.30 mM) | 储存条件 | Store at -20°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 | 1.686 mL | 8.4301 mL | 16.8603 mL |
| 5 mM | 337.2 μL | 1.686 mL | 3.3721 mL |
| 10 mM | 168.6 μL | 843 μL | 1.686 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: >99.00%
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