Doxycycline calcium
Doxycycline calcium Basic information
- Product Name:
- Doxycycline calcium
- Synonyms:
-
- DOXYCYCLINECALCIUM
- 2-Naphthacenecarboxamide, 4-(dimethylamino)-1,4,4a,5,5a,6,11,12a-octahydro-3,5,10,12,12a-pentahydroxy-6-methyl-1,11-dioxo-, calcium salt (1:2), [4S-(4alpha,4aalpha,5alpha,5aalpha,6alpha,12aalpha)]-
- Doxycycline calcium USP/EP/BP
- CAS:
- 94088-85-4
- MF:
- C22H26CaN2O8
- MW:
- 486.53
- EINECS:
- 302-088-9
- Mol File:
- 94088-85-4.mol
Doxycycline calcium Usage And Synthesis
Uses
Doxycycline calcium, an antibiotic, is an orally active and broad-spectrum metalloproteinase (MMP) inhibitor[1]. Doxycycline calcium shows antibacterial activity and anti-cancer cell proliferation activity. Doxycycline calcium can be used to construct gene expression regulation models[1][2][3][4][5].
Veterinary Drugs and Treatments
Although there are no veterinary-approved doxycycline products available, its favorable pharmacokinetic parameters (longer halflife, higher CNS penetration) when compared to either tetracycline HCl or oxytetracycline HCl make it a reasonable choice to use in small animals when a tetracycline is indicated, particularly when a tetracycline is indicated in an azotemic patient.
in vivo
Doxycycline calcium and Tetracycline (HY-A0107), act systemically after absorption from the upper gastrointestinal tract. The main advantage of Doxycycline calcium over Tetracycline is its longer activity, and it can be taken twice or once a day. The peak concentration of both agents is similar, but in the case of Doxycycline the time to peak concentration is shorter, and half life is significantly longer[6].
Doxycycline (Dox) calcium is often used as an inducer in molecular biology studies to induce gene expression. In cells or model animals that have constructed tetracycline induced expression systems (Tet-On/Tet-Off systems), the expression of target genes can be precisely controlled by adding or removing Dox[7][8][9][10].
Dose reference for Dox induction[7][8]:
(1) Model animal: male Sprague-Dawley rats
Tet regulatory system: 20-3000 ppm of Dox is supplied in diet.
(2) Model animal: Cags mice
Tet regulatory system: 625 ppm of Dox is supplied in diet.
Doxycycline and Tetracycline both act systemically after being absorbed by the upper gastrointestinal tract. In comparison, the main advantage of Doxycycline is that it has a longer activity and can be taken twice or once a day. Although the peak concentrations of the two are similar, Doxycycline takes a shorter time to reach peak concentration and has a significantly longer half-life.
Administration: (for GDNF as targeted gene) 3g/kg (Doxycycline; dietary with regular food) ? po ? once daily for 6 days
(2) 3 g/kg dietary DOX produced DOX serum levels equivalent to 1mg/ml DOX in drinking water.
| Animal Model: | 6-month-old female Heterozygous Col3a1-deficient (HT) mice[3] |
| Dosage: | 200 or 800 mg/kg |
| Administration: | Oral gavage; 200 or 800 mg/kg; once daily; 3 months |
| Result: | Reduced MMP-9 activity in a dose-dependent manner. |
IC 50
Tetracycline
References
[1] Eusebio Manchado, et al. A combinatorial strategy for treating KRAS-mutant lung cancer. Nature. 2016 Jun 30;534(7609):647-51. DOI:10.1038/nature18600
[2] Anna-Luisa Luger, et al. Doxycycline Impairs Mitochondrial Function and Protects Human Glioma Cells from Hypoxia-Induced Cell Death: Implications of Using Tet-Inducible Systems. Int J Mol Sci. 2018 May 17;19(5):1504. DOI:10.3390/ijms19051504
[3] Wilfried Briest, et al. Doxycycline ameliorates the susceptibility to aortic lesions in a mouse model for the vascular type of Ehlers-Danlos syndrome. J Pharmacol Exp Ther. 2011 Jun;337(3):621-7. DOI:10.1124/jpet.110.177782
[4] Ethan Ahler, et al. Doxycycline alters metabolism and proliferation of human cell lines. PLoS One. 2013 May 31;8(5):e64561. DOI:10.1371/journal.pone.0064561
[5] Le Zhang, et al. Doxycycline inhibits the cancer stem cell phenotype and epithelial-to-mesenchymal transition in breast cancer. Cell Cycle. 2017 Apr 18;16(8):737-745. DOI:10.1080/15384101.2016.1241929
[6] Manfredsson FP, et al. Tight Long-term dynamic doxycycline responsive nigrostriatal GDNF using a single rAAV vector. Mol Ther. 2009 Nov;17(11):1857-67. DOI:10.1038/mt.2009.196
[7] Kistner A, et al. Doxycycline-mediated quantitative and tissue-specific control of gene expression in transgenic mice. Proc Natl Acad Sci U S A. 1996 Oct 1;93(20):10933-8. DOI:10.1073/pnas.93.20.10933
[8] Niv Y. Doxycycline in Eradication Therapy of Helicobacter pylori--a Systematic Review and Meta-Analysis. Digestion. 2016;93(2):167-73. DOI:10.1159/000443683
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