| Size | Price | Stock | Qty |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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Solithromycin (CEM-101; OP1068; CEM101; OP-1068) is a novel and potent ketolide antibiotic with improved antimicrobial effectiveness. It has a broad spectrum of activity against Gram-positive respiratory tract pathogens, including macrolide-resistant strains. Solithromycin is being studied in clinical trials for the treatment of community-acquired pneumonia (CAP) and other infections.
| Targets |
Macrolide
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|---|---|
| ln Vitro |
The half-life of solithromycin on the release of TNFα and CXCL8 is 41.6 μM and 78.2 μM, respectively. MMP9 activity is significantly reduced by solithromycin, with an IC50 of 14.9 μM[2].
In monocytic U937 and PBMC cells, levofloxacin (0-333 μM; 72 hours) inhibits the release of TNFα induced by lipopolysaccharide and the activity of matrix metalloproteinase 9 (MMP9) induced by phorbol 12-myristate 13-acetate (PMA). It has no effect on cell viability[2].
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| ln Vivo |
After exposing C57BL/6J mice to cigarette smoke for eight days, oral administration of levofloxacin (100 mg/kg) inhibits the accumulation of inflammatory cells and the production of pro-MMP9[2].
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| Animal Protocol |
Animal Model: C57BL/6J mice (male, 4 weeks)[2]
Dosage: 100 mg/kg Administration: Oral administration; every day; for 8 days Result: prevented the production of pro-MMP9 and neutrophilia brought on by cigarette smoke. |
| References |
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| Molecular Formula |
C43H65FN6O10
|
|---|---|
| Molecular Weight |
845.01
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| Exact Mass |
844.47462
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| Elemental Analysis |
C, 61.12; H, 7.75; F, 2.25; N, 9.95; O, 18.93
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| CAS # |
760981-83-7
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| Appearance |
Solid powder
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| SMILES |
C[C@]([C@H](OC([C@@](F)(C([C@H](C)[C@H]1O[C@@](O[C@H](C)C[C@@H]2N(C)C)([H])[C@@H]2O)=O)C)=O)CC)(O3)[C@]([C@H](C([C@@H](C[C@@]1(C)OC)C)=O)C)([H])N(CCCCN4C=C(C5=CC(N)=CC=C5)N=N4)C3=O
|
| InChi Key |
IXXFZUPTQVDPPK-QIFQIIIXSA-N
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| InChi Code |
InChI=1S/C43H65FN6O10/c1-12-32-43(8)35(50(40(55)60-43)19-14-13-18-49-23-30(46-47-49)28-16-15-17-29(45)21-28)26(4)33(51)24(2)22-41(6,56-11)37(27(5)36(53)42(7,44)39(54)58-32)59-38-34(52)31(48(9)10)20-25(3)57-38/h15-17,21,23-27,31-32,34-35,37-38,52H,12-14,18-20,22,45H2,1-11H3/t24-,25-,26-,27+,31+,32-,34-,35-,37-,38+,41-,42-,43-/m1/s1
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| Chemical Name |
3aS,4R,7R,9R,10R,11R,13R,15S,15aR)-1-(4-(4-(3-aminophenyl)-1H-1,2,3-triazol-1-yl)butyl)-10-(((2S,3R,4S,6R)-4-(dimethylamino)-3-hydroxy-6-methyltetrahydro-2H-pyran-2-yl)oxy)-4-ethyl-7-fluoro-11-methoxy-3a,7,9,11,13,15-hexamethyloctahydro-1H-[1]oxacyclotetradecino[4,3-d]oxazole-2,6,8,14(7H,9H)-tetraone
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| Synonyms |
CEM 101; OP1068; OP1068; OP 1068; Solithromycin;CEM101; CEM101
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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 : 32~100 mg/mL ( 37.87~118.34 mM )
Ethanol : ~25 mg/mL
H2O : ~1 mg/mL (~1.18 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (2.96 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 (2.96 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 900 μL of corn oil and mix evenly. View More
Solubility in Formulation 3: 10% DMSO+40% PEG300+5% Tween-80+45% Saline: ≥ 2.5 mg/mL (2.96 mM) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.1834 mL | 5.9171 mL | 11.8342 mL | |
| 5 mM | 0.2367 mL | 1.1834 mL | 2.3668 mL | |
| 10 mM | 0.1183 mL | 0.5917 mL | 1.1834 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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