Antibacterial Solithromycin binds to the large 50S subunit of the ribosome and inhibits protein biosynthesis. The mean 50% inhibitory concentrations (IC50s) for Solithromycin inhibition of cell viability, protein synthesis, and growth rate were 7.5, 40, and 125 ng/ml for Streptococcus pneumoniae,Staphylococcus aureus, and Haemophilus influenzae, respectively.
|Cell lines||S. aureus cells|
|Preparation method||For S. pneumoniae, 12 9-ml cultures of cells comprised of one control set and one set with solithromycin at 7.5 ng/ml were grown to a Klett reading of 15.|
|Animal models||donor mic|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||32 mg/mL in DMSO|
Solithromycin inhibition of protein synthesis and ribosome biogenesis in Staphylococcus aureus, Streptococcus pneumoniae, and Haemophilus influenzae.
Rodgers W, et al. Antimicrob Agents Chemother. 2013 Apr;57(4):1632-7. PMID: 23318809.
In vitro and in vivo activity of solithromycin (CEM-101) against Plasmodium species.
Wittlin S, et al. Antimicrob Agents Chemother. 2012 Feb;56(2):703-7. PMID: 22083475.
CA3 has potent inhibitory effects on YAP1/Tead transcriptional activity and primarily targets YAP1 high and therapy-resistant esophageal adenocarcinoma cells endowed with CSC properties.
YM 511 is a potent aromatase (CYP19) inhibitor.
|YM 298198 hydrochloride
YM 298198 hydrochloride is a highly potent, selective non-competitive mGlu 1 antagonist.
YM 022 is a highly potent, selective non-peptide CCK 2 antagonist.
YK 3-237 is a sIRT1 activator.
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