Solithromycin
Based on 3 publication(s) in Google Scholar
Solithromycin (CEM-101) is an orally bioavailable, effective antimicrobial agent, with IC50s for inhibition of cell viability, protein synthesis, and growth rate are 7.5 ng/mL, 40 ng/mL, and 125 ng/mL for Streptococcus pneumonia, Staphylococcus aureus, and Haemophilus influenzae, respectively. Solithromycin binds to the large 50S subunit of the ribosome and inhibits protein biosynthesis.
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- Purity: 99.85%
- CAS No.: 760981-83-7
- 화학식: C43H65FN6O10
- 분자량:845.01
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Publications Citing Use of MedChemExpress (MCE) Solithromycin
MoreAll Antibiotic Isoforms
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Biological Activity
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Macrolide |
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Cell Line
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Type | Value | Description | References |
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| THP-1 | EC50 |
0.0068 mg/L
Compound: CEM-101
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Antibacterial activity against methicillin-sensitive Staphylococcus aureus ATCC 25923 infected in human THP1 cells assessed as decrease of CFU after 24 hrs
Antibacterial activity against methicillin-sensitive Staphylococcus aureus ATCC 25923 infected in human THP1 cells assessed as decrease of CFU after 24 hrs
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[PMID: 19564365] |
| THP-1 | EC50 |
0.052 mg/L
Compound: CEM-101
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Antibacterial activity against methicillin-sensitive Listeria monocytogenes EGD infected in human THP1 cells assessed as decrease of CFU after 24 hrs
Antibacterial activity against methicillin-sensitive Listeria monocytogenes EGD infected in human THP1 cells assessed as decrease of CFU after 24 hrs
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[PMID: 19564365] |
The IC50s values for Solithromycin on TNFα and CXCL8 release are 41.6 μM and 78.2 μM, respectively. Solithromycin markedly reduces MMP9 activity, with an IC50 of 14.9 μM[2].
Solithromycin (0-333 μM; 72 hours; U937 and PBMC cells) suppresses lipopolysaccharide-induced TNFα release and phorbol 12-myristate 13-acetate (PMA)-induced matrix metalloproteinase 9 (MMP9) activity, and does not affect cell viability in monocytic U937 and PBMC cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J mice (male, 4 weeks)[2]
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Dosage:100 mg/kg
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Administration:Oral administration; every day; for 8 days
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Result:Inhibited cigarette smoke-induced neutrophilia and pro-MMP9 production.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 760981-83-7
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Appearance Solid
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분자량 845.01
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화학식 C43H65FN6O10
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Color White to off-white
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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
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Synonyms
CEM-101; OP-1068
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (3)
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Journal Impact Factor
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Most Recent
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ACS Infect Dis
2021 Nov 12;7(11):3009-3024. PMID: 34699190 -
Antimicrob Agents Chemother
cis- and trans-Acting Factors Influence Expression of the norM-Encoded Efflux Pump of Neisseria gonorrhoeae and Levels of Gonococcal Susceptibility to Substrate Antimicrobials. [Abstract]2018 Jul 27;62(8). pii: e00821-18. PMID: 29891604 -
용액&용해도
DMSO : 100 mg/mL (118.34 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (2.96 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
순도&문서
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Data Sheet (280 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Rodgers W, et al. Solithromycin inhibition of protein synthesis and ribosome biogenesis in Staphylococcus aureus,Streptococcus pneumoniae, and Haemophilus influenzae. Antimicrob Agents Chemother. 2013 Apr;57(4):1632-1637. [Content Brief]
[2]. Kobayashi Y, et al. A novel macrolide solithromycin exerts superior anti-inflammatory effect via NF-κB inhibition. J Pharmacol Exp Ther. 2013 Apr;345(1):76-84. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.1834 mL | 5.9171 mL | 11.8342 mL | 29.5854 mL |
| 5 mM | 0.2367 mL | 1.1834 mL | 2.3668 mL | 5.9171 mL | |
| 10 mM | 0.1183 mL | 0.5917 mL | 1.1834 mL | 2.9585 mL | |
| 15 mM | 0.0789 mL | 0.3945 mL | 0.7889 mL | 1.9724 mL | |
| 20 mM | 0.0592 mL | 0.2959 mL | 0.5917 mL | 1.4793 mL | |
| 25 mM | 0.0473 mL | 0.2367 mL | 0.4734 mL | 1.1834 mL | |
| 30 mM | 0.0394 mL | 0.1972 mL | 0.3945 mL | 0.9862 mL | |
| 40 mM | 0.0296 mL | 0.1479 mL | 0.2959 mL | 0.7396 mL | |
| 50 mM | 0.0237 mL | 0.1183 mL | 0.2367 mL | 0.5917 mL | |
| 60 mM | 0.0197 mL | 0.0986 mL | 0.1972 mL | 0.4931 mL | |
| 80 mM | 0.0148 mL | 0.0740 mL | 0.1479 mL | 0.3698 mL | |
| 100 mM | 0.0118 mL | 0.0592 mL | 0.1183 mL | 0.2959 mL |
Solithromycin Related Classifications
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