P005672 hydrochloride
(Synonyms: (4S,4AS,5AR,12AS)-4-(二甲基氨基)-1,4,4A,5,5A,6,11,12A-八氢-3,10,12,12A-四羟基-7-[(甲氧基甲基氨基)甲基]-1,11-二氧代-2-并四苯甲酰胺盐酸盐,Sarecycline hydrochloride) 目录号 : GC17232
P005672 hydrochloride是一种新型的窄谱四环素衍生物，用于治疗中度至重度炎性非结节性痤疮。
Cas No.:1035979-44-2
Sample solution is provided at 25 µL, 10mM.
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P005672 hydrochloride is a novel, narrow-spectrum tetracycline derivative for the treatment of moderate to severe inflammatory non-nodular acne[1].
In vitro, P005672 hydrochloride (100μM; 25min) reduces Staphylococcus aureus DNA and protein synthesis[2]. P005672 hydrochloride exhibited lower inhibitory activity against microbial species representing human gastrointestinal microbiota compared to minocycline[3].
In vivo, in a rat paw edema model, the anti-inflammatory activity of P005672 hydrochloride (1, 5, 10, 25, 50, 75, 100 and 125mg/kg; 3h; i.p.) was comparable to doxycycline and minocycline[2]. In a murine systemic (intraperitoneal) infection model, P005672 hydrochloride (0.25 mg/kg; 48h; s.c.) was effective in treating the systemic infection caused by Staphylococcus aureus, while P005672 hydrochloride (40 mg/kg; 48h; s.c.) did not demonstrate in vivo efficacy against the systemic infection caused by Escherichia coli PBS1478[4].
References:
[1] Kaul G, Saxena D, Dasgupta A, Chopra S. Sarecycline hydrochloride for the treatment of acne vulgaris. Drugs Today (Barc). 2019 Oct;55(10):615-625. doi: 10.1358/dot.2019.55.10.3045040. PMID: 31720559.
[2] Bunick CG, Keri J, Tanaka SK, Furey N, Damiani G, Johnson JL, Grada A. Antibacterial Mechanisms and Efficacy of Sarecycline in Animal Models of Infection and Inflammation. Antibiotics (Basel). 2021 Apr 15;10(4):439.
[3] Ghannoum MA, Long L, Bunick CG, Del Rosso JQ, Gamal A, Tyring SK, McCormick TS, Grada A. Sarecycline Demonstrated Reduced Activity Compared to Minocycline against Microbial Species Representing Human Gastrointestinal Microbiota. Antibiotics (Basel). 2022 Feb 28;11(3):324.
[4] Zhanel G, Critchley I, Lin LY, Alvandi N. 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.
P005672 hydrochloride是一种新型的窄谱四环素衍生物，用于治疗中度至重度炎性非结节性痤疮[1]。
体外研究显示，P005672 hydrochloride (100μM; 25min)可减少金黄色葡萄球菌的DNA和蛋白质合成[2]。与米诺环素相比，P005672 hydrochloride (0.016-8µg/mL; 48h)对代表人类胃肠道微生物群的微生物种类显示出更低的抑制活性[3]。
体内研究方面，在大鼠足趾水肿模型中，P005672 hydrochloride (1, 5, 10, 25, 50, 75, 100和125mg/kg; 3小时; 腹腔注射)的抗炎活性与多西环素和米诺环素相当[2]。在小鼠全身（腹腔）感染模型中，P005672 hydrochloride (0.25mg/kg; 48小时; 皮下注射)对由金黄色葡萄球菌引起的全身感染有效，而P005672 hydrochloride (40 mg/kg; 48小时; 皮下注射)未显示出对由大肠杆菌PBS1478引起的全身感染的体内疗效[4]。
| Cell experiment [1]: | |
Cell lines | Anaerobic Bacteria and Yeasts |
Preparation Method | 1. Anaerobic Bacteria |
Reaction Conditions | 0.016–8µg/mL or 0.125–64µg/mL; 48h or 24h |
Applications | P005672 hydrochloride exhibited lower inhibitory activity against microbial species representing human gastrointestinal microbiota compared to minocycline. |
| Animal experiment [2]: | |
Animal models | male Sprague Dawley rats |
Preparation Method | To determine whether P005672 hydrochloride decreased inflammation, male Sprague Dawley rats were intraperitoneally injected with saline, P005672 hydrochloride, or a positive control (either doxycycline or minocycline), followed by a subplantar injection of sterile 1mg/0.1mL carrageenan solution in the right hind paw. Paw surface volume was measured immediately after carrageenan injection using a digital water plethysmometer, and again 3h later. Rats were euthanized via CO₂ asphyxiation followed by cervical dislocation immediately after the second measurement. Percent inflammation was calculated as 100 × ((paw volume at 3h-paw volume at 0h)/paw volume at 0h). |
Dosage form | 1, 5, 10, 25, 50, 75, 100 and 125mg/kg; 3h; i.p |
Applications | In a rat paw edema model, the anti-inflammatory activity of P005672 hydrochloride was comparable to doxycycline and minocycline. |
References: | |
| Cas No. | 1035979-44-2 | SDF | |
| 别名 | (4S,4AS,5AR,12AS)-4-(二甲基氨基)-1,4,4A,5,5A,6,11,12A-八氢-3,10,12,12A-四羟基-7-[(甲氧基甲基氨基)甲基]-1,11-二氧代-2-并四苯甲酰胺盐酸盐,Sarecycline hydrochloride | ||
| 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-carbimidic acid hydrochloride | ||
| Canonical SMILES | CN([C@@]1([H])[C@]2([H])C[C@](C3=C(O)[C@]2(O)C(C(C(O)=N)=C1O)=O)([H])CC4=C(CN(OC)C)C=CC(O)=C4C3=O)C.Cl | ||
| 分子式 | C24H30ClN3O8 | 分子量 | 523.96 |
| 溶解度 | DMF: 0.25 mg/ml,DMSO: 0.25 mg/ml | 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 | 1.9085 mL | 9.5427 mL | 19.0854 mL |
| 5 mM | 0.3817 mL | 1.9085 mL | 3.8171 mL |
| 10 mM | 0.1909 mL | 0.9543 mL | 1.9085 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
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet