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/ Azithromycin Dihydrate/阿奇霉素二水合物

Azithromycin Dihydrate/阿奇霉素二水合物 {[allProObj[0].p_purity_real_show]}

货号：A385826 同义名： 阿奇霉素二水合物 / CP-62993 dihydrate; Azithromycin hydrate

Azithromycin hydrate是一种抗生素，能够抑制寄生虫的生长，IC50 为 8.4 μM。

Azithromycin Dihydrate/阿奇霉素二水合物 化学结构 CAS号：117772-70-0
Azithromycin Dihydrate/阿奇霉素二水合物 化学结构
CAS号：117772-70-0
Azithromycin Dihydrate/阿奇霉素二水合物 3D分子结构
CAS号：117772-70-0
Azithromycin Dihydrate/阿奇霉素二水合物 化学结构 CAS号：117772-70-0
Azithromycin Dihydrate/阿奇霉素二水合物 3D分子结构 CAS号：117772-70-0
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Azithromycin Dihydrate/阿奇霉素二水合物 纯度/质量文件 产品仅供科研

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Azithromycin Dihydrate/阿奇霉素二水合物 生物活性

描述 Azithromycin (Dihydrate) is an azalide, a subclass of macrolide antibiotics. It prevents bacteria from growing by interfering with their protein synthesis. It binds to the 50S subunit of the bacterial ribosome and thus inhibits translation of mRNA. Azithromycin is used to treat or prevent certain bacterial infections, most often those causing middle ear infections, strep throat, pneumonia, typhoid, bronchitis, and sinusitis[3]. Azithromycin dose-dependently augmented viral-induced IFNβ (interferons, IFNs) expression in asthmatic, but not in healthy bronchial epithelial cells. Clinically relevant concentrations of azithromycin produce MDA5-dependent, anti-viral, IFN-inducing effects in bronchial epithelium distinctly from asthmatic donors[4]. Azithromycin treatment induced a perturbation in the gut microbiota 14 days after randomization but did not have long-lasting effects on the gut microbiota composition[5].

Azithromycin Dihydrate/阿奇霉素二水合物 细胞实验

Cell Line
Concentration Treated Time Description References
SW480 cells 5–225 µmol/L 24–72 hours Azithromycin inhibited the proliferation of SW480 cells in a dose- and time-dependent manner. The half-inhibitory concentration (IC50) upon 48-h treatment was 140.85 ± 32.81 µmol/L. Cancer Commun (Lond). 2018 Jul 3;38(1):43.
HCT-116 cells 5–225 µmol/L 24–72 hours Azithromycin inhibited the proliferation of HCT-116 cells in a dose- and time-dependent manner. The half-inhibitory concentration (IC50) upon 48-h treatment was 63.19 ± 24.60 µmol/L. Cancer Commun (Lond). 2018 Jul 3;38(1):43.
HeLa cells 4.5 μg/ml (EC50) Azithromycin dose-dependently increased LC3-II levels, indicating autophagosome accumulation. J Clin Invest. 2011 Sep;121(9):3554-63.
Human lung fibroblasts 10 μg/ml 24 hours Azithromycin inhibits TGFB1-induced NOX4 and myofibroblast differentiation. Autophagy. 2017 Aug 3;13(8):1420-1434.
Bone marrow-derived macrophages (BMDMs) 10 or 30 μM 6 hours To evaluate the effect of azithromycin on macrophage phenotype, results showed that azithromycin significantly decreased the production of pro-inflammatory cytokine IL-12 and increased the production of anti-inflammatory cytokine IL-10 J Neuroinflammation. 2015 Nov 24;12:218.
Rabbit ventricular myocytes 100μM Acute exposure Azithromycin significantly inhibited L-type Ca++ currents with an IC50 of ~67μM. Circ Arrhythm Electrophysiol. 2017 Apr;10(4):e003560.
CHO cells 100μM Acute exposure Azithromycin mildly inhibited IKs currents with an IC50 of ~184μM. Circ Arrhythm Electrophysiol. 2017 Apr;10(4):e003560.
HL-1 cardiomyocytes 100μM Acute exposure Azithromycin slowed beat rate, reduced phase 0 upstroke slope, and prolonged repolarization. Circ Arrhythm Electrophysiol. 2017 Apr;10(4):e003560.
Mouse ventricular myocytes 50-100μM Acute exposure Azithromycin significantly inhibited Na+ currents with an IC50 of ~116μM. Circ Arrhythm Electrophysiol. 2017 Apr;10(4):e003560.
HEK 293 cells 50-100μM Acute exposure Azithromycin significantly inhibited SCN5A currents with an IC50 of ~110μM. Circ Arrhythm Electrophysiol. 2017 Apr;10(4):e003560.
Acinetobacter baumannii (AB) 0.5 mg/L 24 hours Evaluated the bactericidal activity of azithromycin against Acinetobacter baumannii, showing significant bactericidal effects in RPMI + 5% LB media. EBioMedicine. 2015 Jun 10;2(7):690-8.
Klebsiella pneumoniae (KP) 1 mg/L 24 hours Evaluated the bactericidal activity of azithromycin against Klebsiella pneumoniae, showing significant bactericidal effects in RPMI + 5% LB media. EBioMedicine. 2015 Jun 10;2(7):690-8.
Pseudomonas aeruginosa (PA) 4 mg/L 24 hours Evaluated the bactericidal activity of azithromycin against Pseudomonas aeruginosa, showing significant bactericidal effects in RPMI + 5% LB media. EBioMedicine. 2015 Jun 10;2(7):690-8.
Beige or brown adipocytes 5 μM 24 hours Azithromycin inhibits thermogenic and mitochondrial gene programs in beige adipocytes Theranostics. 2022 Jan 1;12(3):1187-1203.

Azithromycin Dihydrate/阿奇霉素二水合物 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Mice Pneumonia model Subcutaneous injection 50 or 100 mg/kg Once every 24 hours Evaluated the therapeutic effects of azithromycin monotherapy against MDR Gram-negative bacterial infections, showing significant reduction in lung bacterial counts. EBioMedicine. 2015 Jun 10;2(7):690-8.
Mice High-fat diet-induced obesity model Drinking water 50 mg/kg/day 12 weeks Azithromycin exposure leads to increased adiposity and metabolic dysfunctions in mice under high fat diet Theranostics. 2022 Jan 1;12(3):1187-1203.
BALB/c nude mice HCT-116 xenograft model Oral administration 50 mg/kg/day 3 consecutive days per week for 32 days Combined treatment with azithromycin and TRAIL significantly inhibited the growth of HCT-116 xenografts. The anti-tumor rate of the combined group was 45.88%. Ki-67 expression was significantly lower in the combination group than either azithromycin or TRAIL alone. Cancer Commun (Lond). 2018 Jul 3;38(1):43.
Mice Bleomycin-induced lung fibrosis model Intraperitoneal injection 150 mg/kg Once daily for 14 days Azithromycin attenuates bleomycin-induced lung fibrosis development by reducing NOX4 protein levels and enhancing proteasome activation. Autophagy. 2017 Aug 3;13(8):1420-1434.
Mice Conventional wild-type mice Drinking water 0.1 g/L 2 weeks Azithromycin induced a trend towards K. pneumoniae outgrowth Microbiome. 2022 Mar 10;10(1):43
Mice M. abscessus infection model Gavage 100 mg/kg 5 days per week for 30 days Azithromycin treatment led to persistent lung infection associated with extensive granulomatous inflammation and failure of macrophage degradation of intracellular mycobacteria. J Clin Invest. 2011 Sep;121(9):3554-63.
C57BL/6J mice Moderate-severe thoracic contusion SCI model Oral gavage 160 mg/kg/day Once daily for 3 days prior and 7 days post To evaluate the effect of azithromycin on macrophage phenotype and functional recovery after SCI, results showed that azithromycin significantly increased anti-inflammatory macrophage gene expression, decreased pro-inflammatory macrophage gene expression, and improved tissue sparing and locomotor function recovery J Neuroinflammation. 2015 Nov 24;12:218.
Mice Conscious mice Intraperitoneal injection 50mg/kg and 100mg/kg Single injection Azithromycin caused significant sinus slowing and increased PR, QRS, QT, and QTc intervals. Circ Arrhythm Electrophysiol. 2017 Apr;10(4):e003560.

Azithromycin Dihydrate/阿奇霉素二水合物 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00694694 Malaria Phase 3 Completed - Tanzania ... 展开 >> Teule Hospital Muheza, Tanga Region, Tanzania 收起 <<
NCT01235546 Endometritis ... 展开 >>Wound Infection Abscess Surgical Site Infection 收起 << Not Applicable Completed - United States, Alabama ... 展开 >> University of Alabama at Birmingham Birmingham, Alabama, United States, 35233 United States, Louisiana Ochsner Clinic Foundation New Orleans, Louisiana, United States, 70121 United States, Mississippi University of Mississippi Medical Center Jackson, Mississippi, United States, 39216 United States, New York Columbia University New York, New York, United States, 10032 United States, North Carolina Mission Hospital Asheville, North Carolina, United States, 28801 University of North Carolina Chapel Hill, North Carolina, United States, 27599-7516 United States, Texas University of Texas Medical Branch Galveston, Texas, United States, 77555-0587 University of Texas Health Science Center at Houston Houston, Texas, United States, 77225 United States, Utah University of Utah Salt Lake City, Utah, United States, 84132 收起 <<
NCT02527005 Malaria Pregn... 展开 >>ant HIV 收起 << Phase 1 Completed - Nigeria ... 展开 >> University College Hospital, Ibadan, Oyo, Nigeria, 200001 收起 <<

Azithromycin Dihydrate/阿奇霉素二水合物 参考文献

[1]Menzel M, Akbarshahi H, et al. Azithromycin augments rhinovirus-induced IFNβ via cytosolic MDA5 in experimental models of asthma exacerbation. Oncotarget. 2017 May 9;8(19):31601-31611.

[2]Vandooren J, Knoops S, et al. Differential inhibition of activity, activation and gene expression of MMP-9 in THP-1 cells by azithromycin and minocycline versus bortezomib: A comparative study. PLoS One. 2017 Apr 3;12(4):e0174853.

[3]Bakheit AH, Al-Hadiya BM, Abd-Elgalil AA. Azithromycin. Profiles Drug Subst Excip Relat Methodol. 2014;39:1‐40

[4]Menzel M, Akbarshahi H, Tufvesson E, Persson C, Bjermer L, Uller L. Azithromycin augments rhinovirus-induced IFNβ via cytosolic MDA5 in experimental models of asthma exacerbation. Oncotarget. 2017;8(19):31601‐31611

[5]Wei S, Mortensen MS, Stokholm J, et al. Short- and long-term impacts of azithromycin treatment on the gut microbiota in children: A double-blind, randomized, placebo-controlled trial. EBioMedicine. 2018;38:265‐272

Azithromycin Dihydrate/阿奇霉素二水合物 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.27mL

0.25mL

0.13mL

6.37mL

1.27mL

0.64mL

12.74mL

2.55mL

1.27mL

Azithromycin Dihydrate/阿奇霉素二水合物 技术信息

CAS号117772-70-0
分子式C38H76N2O14
分子量 785.02
SMILES Code O=C1[C@H](C)[C@@H](O[C@H]2C[C@@](C)(OC)[C@@H](O)[C@H](C)O2)[C@H](C)[C@@H](O[C@H]3[C@H](O)[C@@H](N(C)C)C[C@@H](C)O3)[C@](C)(O)C[C@@H](C)CN(C)[C@H](C)[C@@H](O)[C@](C)(O)[C@@H](CC)O1.[H]O[H].[H]O[H]
MDL No. MFCD01862248
别名 阿奇霉素二水合物 ;CP-62993 dihydrate; Azithromycin hydrate
运输蓝冰
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place,Inert atmosphere,2-8°C
溶解方案

DMSO: 105 mg/mL(133.76 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

Tags: Azithromycin hydrate | CP-62993 dihydrate;Azithromycin Dihydrate | 阿奇霉素二水合物 | Drug Standard | Macrolide | Antiparasitic | AmBeed-信号通路专用抑制剂 | Azithromycin Dihydrate/阿奇霉素二水合物 纯度/质量文件 | Azithromycin Dihydrate/阿奇霉素二水合物 生物活性 | Azithromycin Dihydrate/阿奇霉素二水合物 临床数据 | Azithromycin Dihydrate/阿奇霉素二水合物 参考文献 | Azithromycin Dihydrate/阿奇霉素二水合物 实验方案 | Azithromycin Dihydrate/阿奇霉素二水合物 技术信息

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