GlpBio

P005672 hydrochloride

目录号: GC17232纯度: >98%同义词: (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
COASDSData Sheet
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。
P005672 hydrochloride
Cas No.: 1035979-44-2
规格价格库存数量操作
10mg¥819.00现货
1
50mg¥2,730.00现货
1
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产品描述 Description

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]。

实验参考方法 Experimental Reference Method

Cell experiment [1]:

Cell lines

Anaerobic Bacteria and Yeasts

Preparation Method

1. Anaerobic Bacteria
Minimum inhibitory concentration (MIC) testing was performed for anaerobic bacteria using a modified Clinical Laboratory Standards Institute (CLSI) M11-A7 agar dilution method in an anaerobic chamber. Bacteria were grown on Brucella Blood Agar plates supplemented with hemin and vitamin K, and infused with various concentrations of P005672 hydrochloride or minocycline (0.016-8µg/mL). Infused agar was inoculated with 2µL of 1 to 2 × 10⁸ colony forming units (CFUs)/mL and incubated at 37°C for 48h in an anaerobic atmosphere. The lowest concentration of the antimicrobial agent that resulted in a visually evaluated inhibition of growth was recorded and MIC evaluated.
2. Yeasts
Candida isolates were tested using a modified CLSI M27-A4 broth microdilution method at a range of 0.125–64µg/mL. RPMI 1640 broth was inoculated with 0.5 to 2.5 × 10³ CFUs/mL, and incubated at 37°C for 24h. The lowest concentration of the antimicrobial agent that resulted in 50% growth inhibition when compared to the untreated growth control was recorded.

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:
[1] 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.
[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.

产品文档 Product Documents

Purity:>98%
COASDSData Sheet

化学性质Chemical Properties

CAS 号
1035979-44-2
同义词
(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
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 g/mol
溶解性
DMF: 0.25 mg/ml,DMSO: 0.25 mg/ml
保存条件
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°C，然后在超声波浴中震荡一段时间。
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。

计算工具摩尔浓度 / 稀释 / 分子量 / 单位换算 / 体内配方 / 溶解度

g/mol