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Demeclocycline (Detravis; Ledermycin), a semisynthetic tetracycline antibiotic derived from a strain of Streptomyces aureofaciens, is a protein translation inhibitor and calpain inhibitor of the tetracycline antibiotic class. It inhibits the protein synthesis in bacteria and is used for the treatment of bacterial infections.
| ln Vitro |
In mpkCCD cells, treatment with demetocycline (0-100 μM) for 24 hours decreases the amount of AQP2 [3]. Monocyte and macrophage activity is enhanced by demeclocycline (10 μM; 24 h) therapy [4]. Treatment with demeclocycline (1-10 μM; 72 h) directly impacts the development of cells that initiate brain tumors [4].
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| ln Vivo |
Demeclocycline (ip; 40 mg/kg; once daily; 48 hours) treatment resulted in a considerable reduction in hyponatremia and a significant correction of hypoosmolality without nephrotoxicity [3].
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| Cell Assay |
Western Blot Analysis [3]
Cell Types: MpkCCD Cell Tested Concentrations: 0-100 μM Incubation Duration: 24 hrs (hours) Experimental Results: AQP2 abundance diminished in mpkCCD cells, with a significant effect at 50 μM. Cell viability assay [4] Cell Types: Mouse bone marrow-derived macrophages and monocytes Tested Concentrations: 10 μM Incubation Duration: 24 hrs (hours) Experimental Results: Enhanced TNF-α production and modulated monocyte function. Cell viability assay[4] Cell Types: Brain Tumor Starting Cell Tested Concentrations: 1, 5 and 10 μM Incubation Duration: 72 hrs (hours) Experimental Results: Inhibition of cell growth in two ways: mediated by monocytes, and directly by affecting proliferation and Spheroid-forming ability of brain tumor-initiating cells. |
| Animal Protocol |
Animal/Disease Models: Male Wistar rat hyponatremia [3]
Doses: 40 mg/kg Route of Administration: intraperitoneal (ip) injection; 40 mg/kg; one time/day; 48 hrs (hrs (hours)) Experimental Results: increased urine output, diminished urine osmotic pressure, water The fractional excretion increased Dramatically. Animal/Disease Models: Male Wistar rat hyponatremia [3] Doses: 40 mg/kg Route of Administration: intraperitoneal (ip) injection; 40 mg/kg; one time/day; 48 hrs (hrs (hours)) Experimental Results: Specifically demonstrated the intrarenal medulla on AQP2 and AC5/6 and no secondary toxic effects. |
| Toxicity/Toxicokinetics |
Effects During Pregnancy and Lactation
◉ Summary of Use during Lactation A number of reviews have stated that tetracyclines are contraindicated during breastfeeding because of possible staining of infants' dental enamel or bone deposition. However, a close examination of available literature indicates that there is not likely to be harm in short-term use of demeclocycline during lactation because milk levels are low and absorption by the infant is inhibited by the calcium in breastmilk. Short-term use of demeclocycline is acceptable in nursing mothers. As a theoretical precaution, avoid prolonged or repeat courses during nursing. Monitor the infant for rash and for possible effects on the gastrointestinal flora, such as diarrhea or candidiasis (thrush, diaper rash). ◉ Effects in Breastfed Infants Relevant published information was not found as of the revision date. ◉ Effects on Lactation and Breastmilk Relevant published information was not found as of the revision date. |
| References |
[1]. I Chopra, et al. Tetracyclines, molecular and clinical aspects. J Antimicrob Chemother. 1992 Mar;29(3):245-77.
[2]. D Schnappinger, et al. Tetracyclines: antibiotic action, uptake, and resistance mechanisms. Arch Microbiol. 1996 Jun;165(6):359-69. [3]. Marleen L A Kortenoeven, et al. Demeclocycline attenuates hyponatremia by reducing aquaporin-2 expression in the renal inner medulla. Am J Physiol Renal Physiol. 2013 Dec 15;305(12):F1705-18. [4]. Susobhan Sarkar, et al. Demeclocycline Reduces the Growth of Human Brain Tumor-Initiating Cells: Direct Activity and Through Monocytes. Front Immunol. 2020 Feb 21;11:272. |
| Additional Infomation |
Demeclocycline is tetracycline which lacks the methyl substituent at position 7 and in which the hydrogen para- to the phenolic hydroxy group is substituted by chlorine. Like tetracycline, it is an antibiotic, but being excreted more slowly, effective blood levels are maintained for longer. It is used (mainly as the hydrochloride) for the treatment of Lyme disease, acne and bronchitis, as well as for hyponatraemia (low blood sodium concentration) due to the syndrome of inappropriate antidiuretic hormone (SIADH) where fluid restriction alone has been ineffective. It has a role as an antibacterial drug, a geroprotector and an aquaretic.
Demeclocycline is a Tetracycline-class Antimicrobial. A TETRACYCLINE analog having a 7-chloro and a 6-methyl. Because it is excreted more slowly than TETRACYCLINE, it maintains effective blood levels for longer periods of time. See also: Demeclocycline (annotation moved to). |
| Molecular Formula |
C21H21N2O8CL
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|---|---|
| Molecular Weight |
464.85304
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| Exact Mass |
464.098
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| CAS # |
127-33-3
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| Related CAS # |
Demeclocycline hydrochloride;64-73-3
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| PubChem CID |
54680690
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| Appearance |
Green to dark green solid powder
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| Density |
1.8±0.1 g/cm3
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| Boiling Point |
684.5±55.0 °C at 760 mmHg
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| Flash Point |
367.8±31.5 °C
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| Vapour Pressure |
0.0±2.2 mmHg at 25°C
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| Index of Refraction |
1.761
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| LogP |
0.57
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| Hydrogen Bond Donor Count |
6
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
32
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| Complexity |
961
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| Defined Atom Stereocenter Count |
5
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| SMILES |
NC(C1C(=O)[C@@H](N(C)C)[C@@H]2C[C@@H]3[C@H](O)C4=C(C=CC(O)=C4C(O)=C3C(=O)[C@]2(O)C=1O)Cl)=O
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| InChi Key |
GUXHBMASAHGULD-SEYHBJAFSA-N
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| InChi Code |
InChI=1S/C21H21ClN2O8/c1-24(2)14-7-5-6-10(16(27)12-9(25)4-3-8(22)11(12)15(6)26)18(29)21(7,32)19(30)13(17(14)28)20(23)31/h3-4,6-7,14-15,25-27,30,32H,5H2,1-2H3,(H2,23,31)/t6-,7-,14-,15-,21-/m0/s1
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| Chemical Name |
(4S,4aS,5aS,6S,12aR)-7-chloro-4-(dimethylamino)-1,6,10,11,12a-pentahydroxy-3,12-dioxo-4a,5,5a,6-tetrahydro-4H-tetracene-2-carboxamide
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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 |
| 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) |
DMSO : ~25 mg/mL (~53.78 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.25 mg/mL (2.69 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 1.25 mg/mL (2.69 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1512 mL | 10.7562 mL | 21.5123 mL | |
| 5 mM | 0.4302 mL | 2.1512 mL | 4.3025 mL | |
| 10 mM | 0.2151 mL | 1.0756 mL | 2.1512 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.
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