Solithromycin

Research use only, not for human use.

A novel fluoroketolide with lower MICs than those of telithromycin and macrolides.

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.

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.

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. Animal Model:C57BL/6J mice (male, 4 weeks)Dosage:100 mg/kg Administration:Oral administration; every day; for 8 days Result:Inhibited cigarette smoke-induced neutrophilia and pro-MMP9 production.

CEM-101 | OP-1068

GPCR/G Protein

Antibacterial

Antibiotic

Infection

Bacterial Infection

760981-83-7

845.0088

C43H65FN6O10

>98% (HPLC)

DMSO: ≥ 32 mg/mL

CC[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

2H-Oxacyclotetradecino[4,3-d]oxazole-2,6,8,14(1H,7H,9H)-tetrone, 1-[4-[4-(3-aminophenyl)-1H-1,2,3-triazol-1-yl]butyl]-4-ethyl-7-fluorooctahydro-11-methoxy-3a,7,9,11,13,15-hexamethyl-10-[[3,4,6-trideoxy-3-(dimethylamino)-β-D-xylo-hexopyranosyl]oxy]-, (3aS,

(-20℃)

With Ice Pack

≥ 2 years