Solithromycin |
| Catalog No.GC12833 |
솔리트로마이신(CEM-101)은 경구 생체이용 가능한 효과적인 항균제이며 세포 생존, 단백질 합성 및 성장률 억제에 대한 IC50은 폐렴 연쇄상구균, 포도상구균에 대해 7.5ng/mL, 40ng/mL 및 125ng/mL입니다. 각각 aureus 및 Haemophilus influenzae입니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 760981-83-7
Sample solution is provided at 25 µL, 10mM.
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Solithromycin (CEM-101) is a new, potent and broad-spectrum fluoroketolide antibiotic [1][2].
Antibiotic is an antimicrobial used in the treatment and prevention of bacterial infection.
Solithromycin (CEM-101) is a broad-spectrum fluoroketolide antibiotic. CEM-101 exhibited high potency against diverse groups of Gram-positive and Gram-negative bacteria, including mycoplasma and ureaplasma, as well as bacteria associated with respiratory tract infections and skin infections, with MIC50 values of 0.015 μg/mL and 4 μg/mL, respectively [1]. Solithromycin (CEM-101) bound to the large 50S subunit of the ribosome and inhibited protein biosynthesis. In Streptococcus pneumoniae, Staphylococcus aureus, and Haemophilus influenzae, solithromycin inhibited cell viability, protein synthesis, and growth rate with IC50 values of 7.5, 40, and 125 ng/ml. Solithromycin also inhibition the formation of the 50S subunit [3]. In monocytic U937 cells, solithromycin inhibited TNFα/CXCL8 production and MMP9 activity. In PBMC isolated from chronic obstructive pulmonary disease (COPD) patients, solithromycin (10 μM) inhibited TNFα release and MMP9 activity. In monocytic U937 cells, solithromycin (10 μM) significantly inhibited NF-κB activity activated by oxidative stress [4].
In C57BL/6J mice, solithromycin also inhibited cigarette smoke-induced neutrophilia and pro-MMP9 production [4]. CEM-101 was also an effective antimicrobial for the prevention and treatment of intrauterine infection [2].
References:
[1]. Putnam SD, Castanheira M, Moet GJ, et al. CEM-101, a novel fluoroketolide: antimicrobial activity against a diverse collection of Gram-positive and Gram-negative bacteria. Diagn Microbiol Infect Dis, 2010, 66(4): 393-401.
[2]. Keelan JA, Kemp MW, Payne MS, et al. Maternal administration of solithromycin, a new, potent, broad-spectrum fluoroketolide antibiotic, achieves fetal and intra-amniotic antimicrobial protection in a pregnant sheep model. Antimicrob Agents Chemother, 2014, 58(1): 447-454.
[3]. Rodgers W, Frazier AD, Champney WS. Solithromycin inhibition of protein synthesis and ribosome biogenesis in Staphylococcus aureus, Streptococcus pneumoniae, and Haemophilus influenzae. Antimicrob Agents Chemother, 2013, 57(4): 1632-1637.
[4]. Kobayashi Y, Wada H, Rossios C, et al. A novel macrolide solithromycin exerts superior anti-inflammatory effect via NF-κB inhibition. J Pharmacol Exp Ther, 2013, 345(1): 76-84.
| Cas No. | 760981-83-7 | SDF | |
| Chemical Name | (3aS,4R,7S,9S,10R,11S,13R,15R,15aR)-1-(4-(4-(3-aminophenyl)-1H-1,2,3-triazol-1-yl)butyl)-10-(((2R,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]oxacyclotet | ||
| Canonical SMILES | CC[C@](O1)([H])[C@@]2([C@@](N(C(O2)=O)CCCCN3C=C(N=N3)C4=CC(N)=CC=C4)([H])[C@@](C([C@](C[C@@]([C@@](O[C@]5([H])[C@@](O)([H])[C@](N(C)C)([H])C[C@@](O5)([H])C)([H])[C@](C([C@@](C1=O)(F)C)=O)([H])C)(OC)C)([H])C)=O)([H])C)C | ||
| Formula | C43H65FN6O10 | M.Wt | 845.01 |
| Solubility | ≥ 34.35mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 36 reference(s) in Google Scholar.)
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