| 规格 | 价格 | 库存 | 数量 |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| Other Sizes |
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| 体外研究 (In Vitro) |
55 种临床美容痤疮菌株在棒培养基上的 MIC 值为 0.5~16 µg/ml，MIC50 为 0.5 µg/ml，MIC90 为 4 µg/ml [1]。药物 sarecycline 对大环内酯类生物体具有功效 [1]。降解性需氧革兰氏阴性细菌受盐酸沙雷环素影响不大[2]。
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| 体内研究 (In Vivo) |
在中性粒细胞减少小鼠感染范例中，盐酸血清霉素（0.33-9 mg/kg；静脉注射）已显示出对金黄色葡萄球菌的强大功效[1]。在 CD-1 小鼠腹部全身感染模型中，血清环素抑制金黄色葡萄球菌 (PD50=0.25 mg/kg) 的能力，但在最大浓度 (>40 mg/kg) 时不抑制大肠杆菌。影响是模糊的[6]。
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| 动物实验 |
Animal/Disease Models: Carrageenan-induced footpad edema male Sprague Dawley rat model [6]
Doses: 1 mg/kg, 5 mg/kg. kg; intraperitoneal; injection single dose) Anti-inflammatory in the Sprague Dawley rat model activity[6]. ,10 mg/kg, 25 mg/kg, 50 mg/kg, 75 mg/kg, 100 mg/kg, 150 mg/kg Route of Administration: intraperitoneal (ip) injection; single dose. Before injecting a sterile 1 mg/0.1 mL carrageenan solution into the plantar part of the right hind paw. Experimental Results: Compared to baseline, inflammation was diminished to 55.7% and 53.1% at the 75 mg/kg and 100 mg/kg doses, respectively. Animal/Disease Models: Male Sprague Dawley rat model of carrageenan-induced footpad edema [6] Doses: 0.33, 1, 3 or 9 mg/kg Route of Administration: intravenous (iv) (iv)injection Experimental Results: At one dose, thigh bacterial load was diminished 2-log10 is comparable to doxycycline, with ED50 of 8.23 and 8.32 mg/kg respectively. |
| 参考文献 |
[1]. Zhanel G, et al. Microbiological Profile of Sarecycline, a Novel Targeted Spectrum Tetracycline for the Treatment of Acne Vulgaris. Antimicrob Agents Chemother. 2018 Dec 21;63(1):e01297-18.
[2]. Moore AY, et al. Sarecycline: a narrow spectrum tetracycline for the treatment of moderate-to-severe acne vulgaris. Future Microbiol. 2019 Sep;14(14):1235-1242. [3]. Batool Z, et al. Sarecycline interferes with tRNA accommodation and tethers mRNA to the 70S ribosome. Proc Natl Acad Sci U S A. 2020 Aug 25;117(34):20530-20537. [4]. Butler MS, et al. Antibiotics in the clinical pipeline in 2013. J Antibiot (Tokyo). 2013 Oct;66(10):571-91. [5]. Bunick CG, et al. Antibacterial Mechanisms and Efficacy of Sarecycline in Animal Models of Infection and Inflammation. Antibiotics (Basel). 2021 Apr 15;10(4):439. |
| 分子式 |
C24H29N3O8
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|---|---|
| 分子量 |
487.51
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| CAS号 |
1035654-66-0
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| 相关CAS号 |
Sarecycline hydrochloride;1035979-44-2
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| SMILES |
O=C(C1=C(O)[C@@H](N(C)C)[C@@](C[C@@]2([H])C(C(C3=C(O)C=CC(CN(OC)C)=C3C2)=O)=C4O)([H])[C@@]4(O)C1=O)N
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| 化学名 |
(4S,4aS,5aR,12aS)-4-(dimethylamino)-3,10,12,12a-tetrahydroxy-7-((methoxy(methyl)amino)methyl)-1,11-dioxo-1,4,4a,5,5a,6,11,12a-octahydrotetracene-2-carboxamide
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| 别名 |
WC-3035; WC 3035; WC3035; P005672; P-005672; P 005672; P005672; trade name: Seysara
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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) |
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| 溶解度 (体内) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.13 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.13 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. 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 | 2.0512 mL | 10.2562 mL | 20.5124 mL | |
| 5 mM | 0.4102 mL | 2.0512 mL | 4.1025 mL | |
| 10 mM | 0.2051 mL | 1.0256 mL | 2.0512 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) 。
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