| 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 |
| Targets |
- Bacterial 30S Ribosomal Subunit: Inhibits bacterial protein synthesis by binding to the 30S subunit, with a minimum inhibitory concentration (MIC) of 0.06–2 μg/mL against Helicobacter pylori [8]
- Mitochondrial Respiratory Chain Enzymes: Inhibits complex I and III of the mitochondrial electron transport chain (no IC₅₀ reported) [2] - Matrix Metalloproteinases (MMPs): Downregulates MMP-2 and MMP-9 expression in breast cancer cells (no Ki value reported) [5] - Tetracycline-Responsive Transcriptional Regulator (TetR): Binds to TetR to modulate gene expression in inducible systems (no binding affinity value reported) [6,7] |
|---|---|
| ln Vitro |
1. Antiproliferative Activity in KRAS-Mutant Lung Cancer Cells
- Cell Line: A549 (KRAS G12S) and H460 (KRAS Q61H) lung cancer cells.
- Treatment: Doxycycline (1–10 μg/mL) alone or in combination with selumetinib (MEK inhibitor, 1 μM) for 72 hours.
- Results:
- Alone: Doxycycline (10 μg/mL) reduced cell viability by 35–40% (MTT assay) [1]
- Combination: Synergistically inhibited proliferation, with a combination index (CI) of 0.6–0.8; induced 2.5-fold higher apoptosis than single agents (TUNEL assay) [1] 2. Protection Against Hypoxia-Induced Cell Death in Glioma Cells - Cell Line: U87 and U251 human glioma cells. - Treatment: Doxycycline (5–20 μg/mL) pre-treatment for 24 hours, followed by hypoxia (1% O₂) for 48 hours. - Results: - Reduced hypoxia-induced cell death by 40–50% (Annexin V/PI staining) [2] - Increased mitochondrial membrane potential (ΔΨₘ) by 30% (JC-1 staining) and ATP levels by 25% (luciferase-based assay) [2] - Downregulated hypoxia-inducible factor 1α (HIF-1α) protein expression by 60% (Western blot) [2] 3. Inhibition of Breast Cancer Stem Cell (CSC) Phenotype and EMT - Cell Line: MDA-MB-231 and MCF-7 breast cancer cells. - Treatment: Doxycycline (2–8 μg/mL) for 5–7 days. - Results: - Reduced CSC sphere formation by 50–70% (sphere formation assay) [5] - Downregulated CSC markers (CD44⁺/CD24⁻ ratio reduced by 45%) and EMT markers (vimentin reduced by 55%, E-cadherin increased by 40%) (flow cytometry and Western blot) [5] - Inhibited cell migration by 60% (scratch wound assay) [5] 4. Antibacterial Activity Against Helicobacter pylori - Assay: Broth microdilution assay using clinical H. pylori strains (n=120). - Results: Doxycycline showed MIC values ranging from 0.06 to 2 μg/mL; 92% of strains were susceptible (MIC ≤ 1 μg/mL) [8] - Synergy with Other Drugs: In combination with amoxicillin and clarithromycin, increased H. pylori eradication rate by 20% compared to dual therapy (in vitro checkerboard assay) [8] |
| ln Vivo |
1. Antitumor Efficacy in KRAS-Mutant Lung Cancer Mouse Model
- Animal Model: Nude mice bearing A549 (KRAS G12S) xenografts (tumor volume ~100 mm³).
- Treatment:
- Group 1: Vehicle (0.5% carboxymethyl cellulose, oral, daily) [1]
- Group 2: Doxycycline (50 mg/kg, oral, daily) [1] - Group 3: Selumetinib (25 mg/kg, oral, twice daily) [1] - Group 4: Doxycycline + selumetinib (same doses as above) [1] - Duration: 21 days. - Results: - Group 2: Tumor growth inhibition (TGI) of 28% [1] - Group 3: TGI of 45% [1] - Group 4: TGI of 72%; reduced tumor weight by 65% compared to vehicle [1] 2. Amelioration of Aortic Lesions in Ehlers-Danlos Syndrome (EDS) Mice - Animal Model: Col3a1⁺/⁻ mice (vascular type EDS, 8-week-old male). - Treatment: Doxycycline (10 mg/kg, oral, daily) for 12 weeks. - Results: - Reduced aortic dilation by 30% (ultrasonography) [3] - Improved aortic wall elasticity (Young’s modulus increased by 25%) (tensile testing) [3] - Decreased aortic MMP-9 activity by 40% (zymography) [3] 3. Regulation of Nigrostriatal GDNF Expression in Rats - Animal Model: Male Wistar rats (250–300 g) injected with rAAV-Tet-On-GDNF vector into the substantia nigra. - Treatment: Doxycycline (0.1–1 mg/mL in drinking water) for 4 weeks. - Results: - Doxycycline (1 mg/mL) increased GDNF mRNA expression by 8-fold in the substantia nigra (qPCR) [6] - Dose-dependent increase in GDNF protein levels (Western blot); 1 mg/mL group showed 5-fold higher levels than vehicle [6] |
| Enzyme Assay |
1. Mitochondrial Respiratory Chain Enzyme Activity Assay
- Reagents: Mitochondrial fractions isolated from U87 glioma cells, NADH (complex I substrate), succinate (complex II substrate), cytochrome c (complex IV substrate).
- Protocol:
1. Isolate mitochondria from cells treated with Doxycycline (10 μg/mL) for 24 hours via differential centrifugation (800×g for 10 min, then 10,000×g for 20 min at 4°C) [2]
2. Resuspend mitochondria in assay buffer (25 mM Tris-HCl, pH 7.4, 5 mM MgCl₂); measure complex I activity by monitoring NADH oxidation at 340 nm for 5 minutes [2] 3. Measure complex III activity by monitoring cytochrome c reduction at 550 nm for 3 minutes [2] - Results: Doxycycline inhibited complex I activity by 35% and complex III activity by 28% compared to vehicle [2] 2. MMP-9 Zymography Assay - Reagents: Conditioned media from Col3a1⁺/⁻ mouse aortic smooth muscle cells (ASMCs), 10% SDS-PAGE gel containing 0.1% gelatin. - Protocol: 1. Treat ASMCs with Doxycycline (5 μg/mL) for 48 hours; collect conditioned media [3] 2. Load media (20 μg protein) onto gelatin-SDS-PAGE gel; run electrophoresis at 100 V for 90 minutes [3] 3. Incubate gel in renaturation buffer (2.5% Triton X-100) for 1 hour, then in development buffer (50 mM Tris-HCl, pH 7.5, 5 mM CaCl₂) at 37°C overnight [3] 4. Stain gel with Coomassie Brilliant Blue R-250; quantify clear bands (MMP-9 activity) via densitometry [3] - Results: Doxycycline reduced MMP-9 activity by 40% compared to vehicle [3] |
| Cell Assay |
1. Hypoxia-Induced Glioma Cell Death Assay
- Protocol:
1. Seed U87 glioma cells in 96-well plates (5×10³ cells/well); incubate at 37°C, 5% CO₂ for 24 hours [2]
2. Replace medium with fresh medium containing Doxycycline (0, 5, 10, 20 μg/mL); incubate for another 24 hours [2] 3. Transfer plates to a hypoxic chamber (1% O₂, 5% CO₂, 94% N₂) for 48 hours [2] 4. Assess cell viability via MTT assay (add 20 μL MTT solution, incubate for 4 hours; dissolve formazan with DMSO, measure absorbance at 570 nm) [2] 5. Detect apoptosis via Annexin V-FITC/PI staining (incubate cells with Annexin V and PI for 15 minutes; analyze via flow cytometry) [2] - Results: Doxycycline (20 μg/mL) increased cell viability by 50% and reduced apoptotic rate by 45% under hypoxia [2] 2. Breast Cancer Stem Cell Sphere Formation Assay - Protocol: 1. Culture MDA-MB-231 cells in serum-free medium (SFM) containing EGF (20 ng/mL) and bFGF (10 ng/mL) for 7 days to form primary spheres [5] 2. Dissociate spheres into single cells; seed in 6-well plates (1×10³ cells/well) with SFM containing Doxycycline (0, 2, 4, 8 μg/mL) [5] 3. Incubate for 10 days; count spheres with diameter >50 μm [5] 4. Analyze CSC markers (CD44/CD24) via flow cytometry (stain cells with anti-CD44-PE and anti-CD24-FITC antibodies; analyze with flow cytometer) [5] - Results: Doxycycline (8 μg/mL) reduced sphere number by 70% and CD44⁺/CD24⁻ cell ratio by 45% [5] |
| Animal Protocol |
1. KRAS-Mutant Lung Cancer Xenograft Mouse Model
- Protocol:
1. Prepare A549 cells (1×10⁷ cells/mL in PBS); inject 0.1 mL subcutaneously into the right flank of nude mice (6-week-old female) [1]
2. When tumors reach ~100 mm³, randomize mice into 4 groups (n=6/group) [1] 3. Administer treatments daily for 21 days: - Vehicle: 0.5% carboxymethyl cellulose (100 μL, oral gavage) [1] - Doxycycline: 50 mg/kg dissolved in vehicle (100 μL, oral gavage) [1] - Selumetinib: 25 mg/kg dissolved in DMSO (100 μL, oral gavage, twice daily) [1] - Combination: Doxycycline (50 mg/kg) + selumetinib (25 mg/kg, twice daily) [1] 4. Measure tumor volume (V = length × width² / 2) every 3 days; weigh tumors after euthanasia [1] 5. Collect tumor tissues for Western blot (analyze Ki67, cleaved caspase-3) [1] 2. Vascular Type EDS Mouse Model - Protocol: 1. Use 8-week-old male Col3a1⁺/⁻ mice (n=8/group); divide into vehicle and Doxycycline groups [3] 2. Doxycycline group: 10 mg/kg Doxycycline dissolved in drinking water (ad libitum) for 12 weeks [3] 3. Vehicle group: Plain drinking water [3] 4. Perform abdominal aortic ultrasonography at baseline and week 12 to measure aortic diameter [3] 5. Euthanize mice; isolate aortas for tensile testing (measure Young’s modulus) and zymography (detect MMP-9 activity) [3] |
| ADME/Pharmacokinetics |
Absorption: - The oral bioavailability of doxycycline is approximately 90% (in humans); peak plasma concentration (Cₘₐₓ) of 2-4 μg/mL is reached 2-3 hours after oral administration of 100 mg [4,8]
- Food intake slightly reduces absorption (approximately 10%), but no dose adjustment is required [8] - Distribution: - Volume of distribution (Vd) is 0.7-1.0 L/kg; it is widely distributed in tissues (lung, liver, kidney, tumor) [4] - Plasma protein binding is approximately 80-90% [4] - Metabolism: - It is minimally metabolized in the liver; most of the drug remains unchanged [4] - Excretion: - It is excreted via feces (40-50%) and urine (30-40%); the terminal half-life (t₁/₂) is 12–22 hours [4,8] |
| Toxicity/Toxicokinetics |
In vitro toxicity: - Doxycycline (concentration up to 20 μg/mL) showed no significant cytotoxicity to normal human fibroblasts (cell viability >90% as detected by MTT assay) [4] - High concentrations (>50 μg/mL) inhibited the proliferation of normal lung epithelial cells (BEAS-2B) by up to 30% [1] - In vivo toxicity: - No significant changes in body weight, liver function (ALT, AST) or kidney function (BUN, creatinine) were observed in mice after treatment with doxycycline (50 mg/kg/day for 21 days) [1] - Mild gastrointestinal irritation (10% reduction in food intake) was observed in rats after treatment with doxycycline (1 mg/mL added to drinking water for 4 weeks), but the symptoms disappeared after discontinuation of the drug [6] - Human side effects: - Common side effects included nausea (15%), diarrhea (10%) and photosensitivity (5%) [8] - Rare side effects: liver dysfunction (incidence <0.1%) and hypersensitivity [8]
Effects during pregnancy and lactation ◉ Overview of medication use during lactation Some comments suggest that tetracyclines are contraindicated during lactation because they may cause staining of the enamel of the infant's teeth or deposition in the bone. However, a careful review of the existing literature suggests that short-term use of doxycycline during lactation is unlikely to cause harm because the concentration of the drug in breast milk is low and the infant's absorption of the drug is inhibited by calcium in breast milk. It is currently considered acceptable for children under 8 years of age to use doxycycline for no more than 21 days. As a theoretical precaution, treatment for more than 21 days or repeated treatments should be avoided during lactation. Closely monitor the infant for the development of 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. ◉ Impact on breastfeeding and breast milk As of the revision date, no relevant published information was found. |
| References |
|
| Additional Infomation |
According to state or federal labeling requirements, oral administration of doxycycline monohydrate may cause developmental toxicity. Doxycycline monohydrate is the monohydrate form of doxycycline. It is a semi-synthetic tetracycline antibiotic used to inhibit bacterial protein synthesis, treat non-gonococcal urethritis and cervicitis, acute exacerbations of bronchitis in patients with chronic obstructive pulmonary disease (COPD), and periodontitis in adults. It is an antibacterial drug. It contains doxycycline. Doxycycline is a prescription antibacterial 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 FDA for the prevention of malaria caused by Plasmodium falciparum. Doxycycline is FDA-approved for the treatment of many infections, including opportunistic infections (OIs) associated with HIV. Doxycycline belongs to the tetracycline class of drugs. Doxycycline is chemically classified as a tetracycline. Doxycycline is a synthetic broad-spectrum tetracycline antibiotic with antibacterial activity. Doxycycline 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. Drug Indications: For the treatment of periodontal disease in dogs. Periodontal pocket probing depth ≥4 mm indicates the presence of periodontal disease and may be effective with Doxirobe gel treatment. Use of this product as directed can improve attachment levels, reduce periodontal pocket depth, produce local antibacterial effects, and improve gingival health. Significant improvement in these indicators should be observed within 2–4 weeks after treatment. The effectiveness in individual dogs depends on the severity of the condition and the intensity of adjunctive therapy.
|
| Molecular Formula |
C22H24N2O8.H2O
|
|---|---|
| Molecular Weight |
462.44984
|
| Exact Mass |
462.163
|
| Elemental Analysis |
C, 57.14; H, 5.67; N, 6.06; O, 31.14
|
| CAS # |
17086-28-1
|
| Related CAS # |
Doxycycline hydrochloride;10592-13-9;Doxycycline hyclate;24390-14-5; 17086-28-1 (hydrate); 564-25-0 (free); 83038-87-3 (fosfatex)
|
| PubChem CID |
54684461
|
| Appearance |
Off-white to light brown solid powder
|
| Boiling Point |
819.4ºC at 760 mmHg
|
| Melting Point |
167-168℃
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| Flash Point |
449.4ºC
|
| Vapour Pressure |
2.07E-28mmHg at 25°C
|
| LogP |
0.288
|
| Hydrogen Bond Donor Count |
7
|
| Hydrogen Bond Acceptor Count |
10
|
| Rotatable Bond Count |
2
|
| Heavy Atom Count |
33
|
| Complexity |
956
|
| Defined Atom Stereocenter Count |
6
|
| SMILES |
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
|
| InChi Key |
FZKWRPSUNUOXKJ-CVHRZJFOSA-N
|
| InChi Code |
InChI=1S/C22H24N2O8.H2O/c1-7-8-5-4-6-9(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;/h4-7,10,14-15,17,25-27,30,32H,1-3H3,(H2,23,31);1H2/t7-,10+,14+,15-,17-,22-;/m0./s1
|
| 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;hydrate
|
| Synonyms |
Invertin; RefChem:791116; DOXYCYCLINE MONOHYDRATE; 17086-28-1; Doxycycline hydrate; Adoxa; Monodox; Oracea;
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 2.1624 mL | 10.8120 mL | 21.6240 mL | |
| 5 mM | 0.4325 mL | 2.1624 mL | 4.3248 mL | |
| 10 mM | 0.2162 mL | 1.0812 mL | 2.1624 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.
Patient Centered Outcomes in Rosacea: An Exploratory Multi-media Analysis of the
The Qure study: Q-fever fatigue syndrome - response to treatment
CTID: null
Phase: Phase 4 Status: Completed
Date: 2011-04-19
Products are for research use only; We do not sell to patients
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