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Solithromycin

SKU: orb1224053

Description

A novel fluoroketolide with lower MICs than those of telithromycin and macrolides; binds to the large 50S subunit of the ribosome and inhibits protein biosynthesis; exhibits MICs of 7.5, 40, and 125 ng/ml for Streptococcus pneumoniae,Staphylococcus aureus, and Haemophilus influenzae, respectively. Bacterial Infection Approved(In Vitro):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.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.(In Vivo):Solithromycin (100 mg/kg; oral administration; every day; for 8 days; C57BL/6J mice) treatment inhibits inflammatory cells accumulation and pro-MMP9 production in cigarette smoke-exposed mice.

Images & Validation

Key Properties

CAS Number760981-83-7
MW845.0088
Purity>98% (HPLC)
FormulaC43H65FN6O10
SMILESCC[C@@H]1[C@@]2([C@@H]([C@@H](C(=O)[C@@H](C[C@@]([C@@H]([C@H](C(=O)[C@@](C(=O)O1)(C)F)C)O[C@H]3[C@@H]([C@H](C[C@H](O3)C)N(C)C)O)(C)OC)C)C)N(C(=O)O2)CCCCN4C=C(N=N4)C5=CC(=CC=C5)N)C
TargetAntibacterial
SolubilityDMSO: ≥ 32 mg/mL

Storage & Handling

StorageStorage temperature: -20°C. Stability: ≥ 2 years
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

CEM-101 | OP-1068

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Solithromycin (orb1224053)

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