| Size | Price | Stock | Qty |
|---|---|---|---|
| 250mg |
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| 1g |
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| 2g |
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| 10g |
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| Other Sizes |
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Purity: ≥98%
Demeclocycline HCl (also known as demeclocycline hydrochloride; trade names: Detravis; Ledermycin), a protein translation inhibitor and potential calpain inhibitor, is a potent tetracycline antibiotic that inhibits the protein synthesis in bacteria, it is used for the treatment of bacterial infections. Demeclocycline is a semisynthetic tetracycline antibiotic which was derived from a strain of Streptomyces aureofaciens. Demeclocycline binds to bacterial 30S ribosomal subunit and prevents binding of aminoacyl-tRNA to the mRNA-ribosome complex, thereby inhibiting protein synthesis. Demeclocycline also inhibits the effect of vasopressin on the renal tubules, thereby causing diuresis.
| Targets |
Tetracycline
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|---|---|
| References |
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| Additional Infomation |
Demeclocycline Hydrochloride (internal use) can cause developmental toxicity according to state or federal government labeling requirements.
Demeclocycline hydrochloride is the hydrochloride salt of demeclocycline. A tetracycline antibiotic, 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 and an aquaretic. It contains a demeclocycline. 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); Demeclocycline Hydrochloride (annotation moved to). |
| Molecular Formula |
C21H21CLN2O8.HCL
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|---|---|---|
| Molecular Weight |
501.31
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| Exact Mass |
500.075
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| Elemental Analysis |
C, 50.31; H, 4.42; Cl, 14.14; N, 5.59; O, 25.53
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| CAS # |
64-73-3
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| Related CAS # |
Demeclocycline;127-33-3
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| PubChem CID |
54686764
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| Appearance |
Solid powder
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| Boiling Point |
795.9ºC at 760 mmHg
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| Melting Point |
>245°C (dec.)
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| Flash Point |
435.2ºC
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| LogP |
1.767
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| Hydrogen Bond Donor Count |
7
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
33
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| Complexity |
961
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| Defined Atom Stereocenter Count |
5
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| SMILES |
ClC1C([H])=C([H])C(=C2C(=C3C([C@@]4(C(=C(C(N([H])[H])=O)C([C@]([H])([C@]4([H])C([H])([H])[C@]3([H])[C@@]([H])(C2=1)O[H])N(C([H])([H])[H])C([H])([H])[H])=O)O[H])O[H])=O)O[H])O[H].Cl[H]
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| InChi Key |
GVSJQNRGSCOSNJ-KBHRXELFSA-N
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| InChi Code |
InChI=1S/C21H21ClN2O8.ClH/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;/h3-4,6-7,14-15,25-26,28-29,32H,5H2,1-2H3,(H2,23,31);1H/t6-,7-,14-,15-,21-;/m0./s1
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| Chemical Name |
(4S,4aS,5aS,6S,12aS)-7-chloro-4-(dimethylamino)-3,6,10,12,12a-pentahydroxy-1,11-dioxo-1,4,4a,5,5a,6,11,12a-octahydrotetracene-2-carboxamide hydrochloride
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| Synonyms |
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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. |
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| 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 : ~100 mg/mL ( ~199.47 mM )
Water : 33.33 ~40 mg/mL(~66.49 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.99 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 25.0 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: 2.5 mg/mL (4.99 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 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. View MoreSolubility in Formulation 3: font color= ‘FF0000’>10% DMSO+40% PEG300+5% Tween-80+45% Saline: ≥ 2.5 mg/mL (4.99 mM) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9948 mL | 9.9739 mL | 19.9477 mL | |
| 5 mM | 0.3990 mL | 1.9948 mL | 3.9895 mL | |
| 10 mM | 0.1995 mL | 0.9974 mL | 1.9948 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT02740933 | UNKNOWN | Drug: Demeclocycline | Brain Tumor | Massachusetts General Hospital | 2016-04 | Phase 1 |
| NCT02576652 | COMPLETED | Other:Tetracycline Other:Demeclocycline Procedure:Total Hip Replacement |
Osteoporosis | Amgen | 2015-12-22 | Phase 4 |
| NCT00873808 | WITHDRAWN | Drug:clodronate disodium Drug:demeclocycline hydrochloride Drug:ibandronate sodium |
Breast Cancer | SWOG Cancer Research Network |
2008-10 | |
| NCT01279187 | TERMINATED | Drug: Teriparatide | Implant | University of Michigan | 2011-02 | Phase 2 |
| NCT03960437 | COMPLETED | Drug: Etelcalcetide | Chronic Kidney Disease Mineral and Bone Disorder Hyperparathyroidism; Secondary, Renal Renal Osteodystrophy Vascular Calcification |
Thomas Nickolas, MD MS | 2018-09-06 | Phase 2 |
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