| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| Other Sizes |
Purity: ≥98%
| Targets |
Doxycycline inhibits matrix metalloproteinase-2 (MMP-2) and MMP-9 activity in aortic tissues of vascular Ehlers-Danlos syndrome (vEDS) mice, though specific IC50 values are not provided.
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| ln Vitro |
Glioma cell proliferation is only impacted by high concentrations of doxycycline hydrochloride (0.01–10 µg/mL, 4 d) [2]. When administered to SVG cells at doses of 1 µg/mL and above, doxycycline hydrochloride (0.01–10 µg/mL, 24 hours) can decrease the amount of MT-CO1 protein [2]. Human cell line growth is inhibited by doxycycline hydrochloride (100 ng/mL, 1 µg/mL; 24 hours) [4]. Breast cancer cells' ability to proliferate is inhibited by doxycycline hydrochloride (0-250 μM, 72 hours) [5].
- Mitochondrial Function Impairment: - Reference [2]: In human glioma cell lines (U87, U251), doxycycline (0.01–10 μg/mL) dose-dependently reduced mitochondrial membrane potential (JC-1 assay) and ATP production (luciferase-based assay). At 1 μg/mL, ATP levels decreased by 40% compared to vehicle control. Western blot analysis showed reduced expression of mitochondrial complex I subunit MT-CO1 by 30% at 1 μg/mL. - Metabolic and Proliferation Alterations: - Reference [4]: In MCF-7 breast cancer cells, doxycycline (1–100 μM) decreased glucose uptake (2-NBDG assay) by 25–60% and lactate production (enzymatic assay) by 30–50% after 72 hours. MTT assay revealed dose-dependent inhibition of cell viability with an IC50 of 25 μM. - Cancer Stem Cell Inhibition: - Reference [5]: In MDA-MB-231 breast cancer cells, doxycycline (10–50 μM) reduced sphere formation efficiency (clonogenic assay) by 40–60% and downregulated stemness markers (ALDH1, CD44/CD24) by 50–70% (flow cytometry). Western blot showed decreased phosphorylation of AKT (40%) and β-catenin (35%) at 25 μM. |
| ln Vivo |
- Aortic Lesion Amelioration in vEDS Mice:
- Reference [3]: Oral administration of doxycycline (20 mg/kg/day) to vEDS mice for 4 weeks reduced aortic aneurysm formation by 50% (histological analysis) and decreased MMP-9 activity (zymography) by 35% in aortic tissues. Serum elastin degradation products (ELISA) were reduced by 40%.
- GDNF Expression Regulation: - Reference [6]: In transgenic mice with a doxycycline-responsive GDNF promoter, intraperitoneal doxycycline (2 mg/kg/day) for 14 days increased striatal GDNF levels (ELISA) by 2.5-fold compared to vehicle. Behavioral tests showed improved motor coordination in rotarod assay. In HT mice who have not received treatment, doxycycline hydrochloride (oral gavage; 200 or 800 mg/kg; once daily; 3 months) decreases MMP-9 activity in a dose-dependent way [3]. |
| Enzyme Assay |
- MMP Activity Zymography:
- Reference [3]: Aortic tissue lysates from vEDS mice treated with doxycycline (20 mg/kg/day) were subjected to gelatin zymography. Samples were electrophoresed on 10% SDS-PAGE gels containing 1 mg/mL gelatin. After renaturation, gels were incubated at 37°C for 24 hours in developing buffer. Clear bands indicating MMP-2/-9 activity were quantified by densitometry, showing a 35% reduction in MMP-9 activity in treated mice.
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| Cell Assay |
Cell Viability Assay[2]
Cell Types: LNT-229, G55 and U343 Glioma Cell Tested Concentrations: 0.01, 0.1, 1 or 10 µg/mL Incubation Duration: 4 days Experimental Results: Only affected at high concentrations (10 µg) Glioma cell growth/ml). Cell viability assay[2] Cell Types: SVG Cell Tested Concentrations: 0.01, 0.1, 1 or 10 µg/mL Incubation Duration: 24 hrs (hours) Experimental Results: MT-CO1 protein content diminished at concentrations of 1 µg/mL and higher. Cell proliferation assay [4] Cell Types: MCF 12A, 293T Cell Tested Concentrations: 100 ng/mL, 1 µg/mL Incubation Duration: 96 hrs (hours) Experimental Results: 1 µg/mL resulted in diminished proliferation of MCF 12A and 293T cells. Cell viability assay[5] Cell Types: MCF-7, MDA-MB-468 Cell Tested Concentrations: 0-250 μM Incubation Duration: 72 hrs (hours) Experimental Results: Inhibition of breast cancer cells, MCF-7 and MCF-7 in a dose-dependent manner The IC50 values of MDA-MB-468 were 11.39 μM and 7.13 μM respectively. - Hypoxia-Induced Cell Death Protection: - Reference [2]: U87 glioma cells were exposed to hypoxia (1% O₂) for 24 hours with doxycycline (0.1–10 μg/mL). Cell viability was assessed by MTT assay, showing a 50% reduction in hypoxia-induced cell death at 1 μg/mL. Annexin V/PI staining (flow cytometry) revealed a 30% decrease in apoptotic cells at 1 μg/mL. - Epithelial-Mesenchymal Transition (EMT) Inhibition: - Reference [5]: In MCF-7 cells, doxycycline (25 μM) reduced vimentin expression (immunofluorescence) by 50% and increased E-cadherin expression by 40%. Transwell migration assay showed a 60% decrease in migratory cells after 24-hour treatment. |
| Animal Protocol |
Animal/Disease Models: 6-month-old female heterozygous Col3a1-deficient (HT) mice [3]
Doses: 200 or 800 mg/kg Route of Administration: po (oral gavage); 200 or 800 mg/kg; one time/day; 3-month Experimental Results: MMP-9 activity diminished in a dose-dependent manner. - vEDS Mouse Model: - Reference [3]: 8-week-old male vEDS mice (n=8/group) received doxycycline (20 mg/kg/day, dissolved in 0.5% carboxymethylcellulose) by oral gavage for 4 weeks. Control mice received vehicle. Aortas were harvested for histological analysis (hematoxylin-eosin staining) and MMP activity assays. - GDNF Expression Model: - Reference [6]: Transgenic mice expressing doxycycline-responsive GDNF were injected intraperitoneally with doxycycline (2 mg/kg/day in 5% DMSO/PBS) for 14 days. Brains were dissected for GDNF ELISA and immunohistochemistry (GFAP staining for astrocytes). |
| Toxicity/Toxicokinetics |
Effects During Pregnancy and Lactation
◉ Overview of Medication Use During Lactation Some reviews suggest that tetracyclines are contraindicated during lactation because they can cause staining of infant tooth enamel or deposition in bone. However, a careful review of existing literature indicates that short-term use of doxycycline during lactation is unlikely to cause harm because the drug concentration in breast milk is low, and the infant's absorption of the drug is inhibited by calcium in breast milk. Currently, it is considered acceptable for children under 8 years of age to use doxycycline for no more than 21 days. As a theoretical precaution, treatment exceeding 21 days or repeated treatments during lactation should be avoided. Closely monitor the infant for rashes and potential effects on the gut microbiota, such as diarrhea or candidiasis (thrush, diaper rash). ◉ Effects on Breastfed Infants No relevant published information was found as of the revision date. ◉ Effects on Breastfeeding and Breast Milk No relevant published information was found as of the revision date. |
| References |
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| Additional Infomation |
Mechanism of action: - References [2][5]: Doxycycline inhibits mitochondrial electron transport chain complex I, reduces glycolytic flux, and blocks the AKT/β-catenin signaling pathway, thereby inhibiting cancer stem cell characteristics. - Clinical significance: - References [8]: Systematic reviews have shown that doxycycline (100 mg, twice daily for 7 days) can be used as an alternative to Helicobacter pylori eradication therapy, achieving eradication rates of 76%–97% when used in combination with other antibiotics. - Gene regulation: - References [6][7]: The doxycycline-regulated Tet-on system reversibly induces GDNF expression in transgenic mice and is dose-dependently regulated in the nigrostriatal pathway (0.1–2 mg/kg). Doxycycline is a prescription antimicrobial drug approved by the U.S. Food and Drug Administration (FDA) for the treatment of certain infections. In addition, doxycycline has been approved by the U.S. Food and Drug Administration (FDA) for the prevention of malaria caused by Plasmodium falciparum.
Doxycycline is FDA-approved for the treatment of many infections that may be opportunistic infections (OIs) associated with HIV. Doxycycline hydrochloride is the hydrochloride form of doxycycline, a synthetic broad-spectrum tetracycline antibiotic with antibacterial activity. Doxycycline hydrochloride reversibly binds to the 30S ribosomal subunit and may also bind to the 50S ribosomal subunit, thereby blocking the binding of aminoacyl-tRNA to the mRNA-ribosome complex. This leads to inhibition of protein synthesis. In addition, the drug also exhibits inhibitory effects on collagenase activity. A synthetic tetracycline derivative with similar antibacterial activity. See also: Doxycycline hydrochloride (note moved to). |
| Molecular Formula |
C22H25CLN2O8
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| Molecular Weight |
480.8955
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| Exact Mass |
480.129
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| Elemental Analysis |
C, 54.95; H, 5.24; Cl, 7.37; N, 5.83; O, 26.62
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| CAS # |
10592-13-9
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| Related CAS # |
Doxycycline;564-25-0;Doxycycline hyclate;24390-14-5;Doxycycline monohydrate;17086-28-1;Doxycycline calcium;94088-85-4
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| PubChem CID |
54686183
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.63 g/cm3
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| Boiling Point |
762.6ºC at 760 mmHg
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| Melting Point |
195-201℃
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| Flash Point |
415ºC
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| LogP |
1.154
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| Hydrogen Bond Donor Count |
16
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| Hydrogen Bond Acceptor Count |
20
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
70
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| Complexity |
958
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| Defined Atom Stereocenter Count |
12
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| SMILES |
CCO.C[C@@H]1[C@H]2[C@@H]([C@H]3[C@@H](C(=O)C(=C([C@]3(C(=O)C2=C(C4=C1C=CC=C4O)O)O)O)C(=O)N)N(C)C)O.C[C@@H]1[C@H]2[C@@H]([C@H]3[C@@H](C(=O)C(=C([C@]3(C(=O)C2=C(C4=C1C=CC=C4O)O)O)O)C(=O)N)N(C)C)O.O.Cl.Cl
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| InChi Key |
UHHHTIKWXBRCLT-VDBOFHIQSA-N
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| InChi Code |
InChI=1S/2C22H24N2O8.C2H6O.2ClH.H2O/c2*1-7-8-5-4-6-9(25)11(8)16(26)12-10(7)17(27)14-15(24(2)3)18(28)13(21(23)31)20(30)22(14,32)19(12)29;1-2-3;;;/h2*4-7,10,14-15,17,25-27,30,32H,1-3H3,(H2,23,31);3H,2H2,1H3;2*1H;1H2/t2*7-,10+,14+,15-,17-,22-;;;;/m00..../s1
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| Chemical Name |
(4S,4aR,5S,5aR,6R,12aR)-4-(dimethylamino)-1,5,10,11,12a-pentahydroxy-6-methyl-3,12-dioxo-4a,5,5a,6-tetrahydro-4H-tetracene-2-carboxamide;ethanol;hydrate;dihydrochloride
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| Synonyms |
Doxycycline hydrochloride; 10592-13-9; Doxycycline HCl; Idocyklin; Liomycin; Nivocilin; Samecin; Tanamicin;
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
H2O : ~100 mg/mL (~207.94 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0794 mL | 10.3972 mL | 20.7943 mL | |
| 5 mM | 0.4159 mL | 2.0794 mL | 4.1589 mL | |
| 10 mM | 0.2079 mL | 1.0397 mL | 2.0794 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Multi-model Image of Doxycycline in TAO
CTID: NCT05112211
Phase: N/A Status: Recruiting
Date: 2023-11-22
Products are for research use only; We do not sell to patients
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