P005672 hydrochloride|1035979-44-2|(P-005672 hydrochloride)-陌孚医药/Medlife

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P005672 hydrochloride (Synonyms: P-005672 hydrochloride)

目录号: PC11736 纯度: ≥98%

CAS No. :1035979-44-2

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中文名称	P005672 hydrochloride
中文别名	(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;P005672 HCl 抑制剂;P005672盐酸盐;P005672(Sarecycline hcl)
英文名称	P005672 hydrochloride
英文别名	P005672 HCl;WC3035;Sarecycline Hydrochloride [USAN];(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-octahydro-naphthacene-2-carboxylic acid amide mono hydrochloride;(4S,4aS,5aR,12aS)-4-(dimethylamino)-3,10,12,12a-tetrahydroxy-7-((methoxymethylamino)methyl)-1,11-dioxo-1,4,4a,5,5a,6,11,12a-octahydrotetracene-2-carboxamide monohydrochloride;Sarecycline Hydrochloride;cc-302;2-Naphthacenecarboxamide, 4-(dimethylamino)-1,4,4a,5,5a,6,11,12a-octahydro-3,10,12,12a-tetrahydroxy-7-((methoxymethylamino)methyl)-1,11-dioxo-, hydrochloride (1:1), (4S,4aS,5aR,12aS)-;(4S,4aS,5aR,12aR)-4-(dimethylamino)-1,10,11,12a-tetrahydroxy-7-[[methoxy(methyl)amino]methyl]-3,12-dioxo-4a,5,5a,6-tetrahydro-4H-tetracene-2-carboxamide,hydrochloride;(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;Sarecycline;(4S,4aS,5aR,12aR)-4-(dimethylamino)-1,10,11,12a-tetrahydroxy-7-[[methoxy(methyl)amino]methyl]-3,12-dioxo-4a,5,5a,6-tetrahydro-4H-tetracene-2-carboxamide;hydrochloride;Sarecycline HCl;P005672 (hydrochloride);Sarecycline (hydrochloride);P005672 HCl (Sarecycline HCl);(4S,4AS,5aR,12aS)-4-(dimethylamino)-3,10,12,12a-tetrahydroxy-7-((methoxy(methyl)amino)methyl)-;(4S,4aS,5aR,12aS)-4-(DiMethylaMino)-1,4,4a,5,5a,6,11,12a-octahydro-3,10,12,12a-tetrahydroxy-7-[(MethoxyMethylaMino)Methyl]-1,11-dioxo-2-naphthacenecarboxaMide hydrochloride;4S,4aS,5aR,12aS)-4-(Dimethylamino)-1,4,4a,5,5a,6,11,12a-octahydro-3,10,12,12a-tetrahydroxy-7-[(methoxymethylamino)methyl]-1,11-dioxo-2-naphthacenecarboxamide hydrochloride P005672 HCl;94O110CX2E;Sarecycline [USAN:INN];Sarecycline (USAN/INN);P005672;BCP24790;DB12035;D10666
Cas No.	1035979-44-2
分子式	C₂₄H₂₉N₃O₈
分子量	487.50
包装储存	4°C, stored under nitrogen *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

生物活性

Sarecycline hydrochloride is a narrow-spectrum tetracycline-class antibiotic. Sarecycline hydrochloride possesses anti-inflammatory properties and potent activity against Gram-positive bacteria, including activity against multiple strains of Cutibacterium acnes. Sarecycline hydrochloride interferes with tRNA accommodation and tethers mRNA to the 70S ribosome.

性状

Solid

IC50 & Target[1][2]

Tetracycline

体外研究(In Vitro)

Sarecycline inhibits 55 clinical isolates of C. acnes, and the MIC values for Sarecycline ranged from 0.5 to 16?μg/ml; the MIC₅₀ was 0.5 μg/ml, and the MIC₉₀ was 4?μg/ml. Sarecycline, exhibits activity against the macrolide-resistant organisms.
Sarecycline hydrochloride exhibits minimal activity against enteric aerobic Gram-negative bacteria.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

Sarecycline hydrochloride (0.33-9?mg/kg; i.v.) show potent activity against S. aureus in a murine neutropenic thigh infection model.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Female SD-1 mice (A murine neutropenic thigh wound infection model)
Dosage:	0.33, 1, 3, or 9?mg/kg
Administration:	Intravenously
Result:	Achieved a 2-log10 reduction in the bacterial burden in the thigh at a dose comparable to that of doxycycline, with ED50s of 8.23 and 8.32?mg/kg, respectively.

运输条件

Room temperature or refrigerated transportation.

储存方式

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

ClinicalTrial

参考文献

[1]. 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;63(1):e01297-18. Published 2018 Dec 21. [Information]

[2]. Moore AY, Charles JEM, Moore S. Sarecycline: a narrow spectrum tetracycline for the treatment of moderate-to-severe acne vulgaris. Future Microbiol. 2019;14(14):1235-1242. [Information]

[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;117(34):20530-20537. [Information]

溶解度数据

体外研究:

DMSO : 100 mg/mL (190.85 mM; Need ultrasonic)

配制储备溶液

浓度溶剂体积质量	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

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，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, 6 months; -20°C, 1 month (stored under nitrogen)。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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