Azithromycin

別名: XZ-450,CP-62993 中文名稱：阿奇霉素,阿齊紅霉

目錄號(hào)：S1835 Purity: 97%

Azithromycin是一種抑制蛋白合成的抗生素，用于細(xì)菌感染的治療。

Azithromycin Chemical Structure

CAS: 83905-01-5

規(guī)格	價(jià)格	庫(kù)存
10mM (1mL in DMSO)	1066.32	現(xiàn)貨
25mg	784.33	現(xiàn)貨
200mg	3017.23	現(xiàn)貨
1g	7944.3	現(xiàn)貨
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產(chǎn)品質(zhì)控

批次：純度： >97%

Azithromycin相關(guān)產(chǎn)品

相關(guān)化合物庫(kù)	激酶抑制劑庫(kù) FDA藥物庫(kù) 天然產(chǎn)物庫(kù) 已知活性藥物庫(kù)-I 生物活性庫(kù)Ⅱ	點(diǎn)擊展開

細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例

細(xì)胞系	實(shí)驗(yàn)類型	給藥濃度	孵育時(shí)間	活性描述	文獻(xiàn)信息
Hep2	Antichlamydial assay	4 ug/ml	8 hrs	Anti-Chlamydial activity against Chlamydia trachomatis Serovar LGV-L2 infected in Hep2 cells assessed as reduction in size and number of chlamydial inclusion at 4 ug/ml treated at 8 hrs post-infection and 24 hrs later re-infecting fresh Hep2 cells monolay	32227948
HeLa 299	Antichlamydial assay		44 to 48 hrs	Antichlamydial activity against Chlamydia trachomatis serovar L2 infected in human HeLa 299 cells assessed as reduction in number of inclusion bodies measured after 44 to 48 hrs by DAPI staining-based HCS assay, IC50=0.727μM.	29232584
THP1	Function assay		30 mins	Drug uptake in human THP1 cells at pH 6 to 7 after 30 mins	19564365
THP1	Function assay		24 hrs	Drug uptake in human THP1 cells after 24 hrs in presence of verapamil	19564365
THP1	Function assay		24 hrs	Drug uptake in human THP1 cells after 24 hrs in presence of gemfibrozil	19564365
Vero E6	Antiviral assay		2 days	Antiviral efficacy against SARS-CoV-2 (strain BavPat1) in Vero E6 cells assessed by inhibition of viral RNA replication measured by RT-PCR after 2 days, EC50=2.12μM.	ChEMBL
Vero E6	Antiviral assay		2 days	Antiviral efficacy against SARS-CoV-2 (strain BavPat1) in Vero E6 cells assessed by inhibition of viral RNA replication measured by RT-PCR after 2 days, EC90=8.65μM.	ChEMBL
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生物活性

產(chǎn)品描述

Azithromycin是一種抑制蛋白合成的抗生素，用于細(xì)菌感染的治療。

靶點(diǎn)

protein synthesis ^[1]

體外研究(In Vitro)
體外研究活性	Azithromycin在囊性纖維癥細(xì)胞中減少大約40%的IL-8 mRNA和蛋白質(zhì)表達(dá)，達(dá)到非CF細(xì)胞中的水平。Azithromycin導(dǎo)致NF-kappaB和AP-1 DNA結(jié)合分別減少50%和70%，使其達(dá)到非CF細(xì)胞中的水平。^[1]在樹突細(xì)胞中(DCs)， Azithromycin顯著增強(qiáng)共刺激分子，CD80對(duì)DCs的作用強(qiáng)度，但不增強(qiáng)CD86和CD40對(duì)DCs的作用。Azithromycin顯著增加IL-10的產(chǎn)生，而Clarithromycin (CAM)顯著抑制DCs產(chǎn)生IL-6。衍生自脾臟的原始T細(xì)胞與預(yù)先用LPS和這些大環(huán)內(nèi)酯類抗生素處理過(guò)的DCs共培養(yǎng)時(shí)，Azithromycin增加IL-10，而CAM顯著減少IL-2產(chǎn)生。^[2] 在J774小鼠巨噬細(xì)胞中，Azithromycin選擇性抑制辣根過(guò)氧化物酶和熒光黃的液相內(nèi)吞。Azithromycin延遲受體結(jié)合轉(zhuǎn)鐵蛋白和過(guò)氧化物酶抗過(guò)氧化物酶免疫復(fù)合物進(jìn)入細(xì)胞表面內(nèi)吞孔和囊泡。Azithromycin下調(diào)細(xì)胞表面轉(zhuǎn)鐵蛋白受體，但不影響Fcγ受體，通過(guò)引起內(nèi)部化轉(zhuǎn)鐵蛋白受體進(jìn)入再循環(huán)路徑嚴(yán)重延遲，而不減慢隨后流出，導(dǎo)致表面池到細(xì)胞內(nèi)池的重新分配。^[3] Azithromycin插入到DOPC脂質(zhì)雙分子層，從而降低其內(nèi)聚力，并促進(jìn)DPPC整合到DOPC液體基質(zhì)。^[4]

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試驗(yàn)信息 (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT05972772	Not yet recruiting	Infectious Disease\|Therapeutics	Lao-Oxford-Mahosot Hospital Wellcome Trust Research Unit\|Mahidol Oxford Tropical Medicine Research Unit	March 20 2024	Phase 2\|Phase 3
NCT05796362	Not yet recruiting	Infectious Disease\|Drug Effect\|Clinical Infection	Brigham and Women''s Hospital\|Bill and Melinda Gates Foundation	April 2023	Phase 1

參考文獻(xiàn)
[1] Cigana C, et al. P Biochem Biophys Res Commun, 2006, 350(4), 977-982. [2] Sugiyama K, et al. Clin Exp Immunol, 2007, 147(3), 540-546. [3] Tyteca D, et al. Exp Cell Res, 2002, 281(1), 86-100. [4] Fa N, et al. Biochim Biophys Acta, 2007, 1768(7), 1830-1838. + 展開

參考文獻(xiàn)

[1] Cigana C, et al. P Biochem Biophys Res Commun, 2006, 350(4), 977-982.
[2] Sugiyama K, et al. Clin Exp Immunol, 2007, 147(3), 540-546.
[3] Tyteca D, et al. Exp Cell Res, 2002, 281(1), 86-100.

[4] Fa N, et al. Biochim Biophys Acta, 2007, 1768(7), 1830-1838.

+ 展開