Solithromycin

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.

Product information

CAS Number: 760981-83-7

Molecular Weight: 845.01

Formula: C43H65FN6O10

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-methyloxan-2-yl]oxy}-4-ethyl-7-fluoro-11-methoxy-3a,7,9,11,13,15-hexamethyl-tetradecahydro-1H-oxacyclotetradeca[4,3-d][1,3]oxazole-2,6,8,14-tetrone

Smiles: CN(C)[C@H]1C[C@@H](C)O[C@H](O[C@@H]2[C@H](C)C(=O)[C@](C)(F)C(=O)O[C@H](CC)[C@@]3(C)OC(=O)N(CCCCN4C=C(N=N4)C4=CC(N)=CC=C4)[C@@H]3[C@@H](C)C(=O)[C@H](C)C[C@]2(C)OC)[C@@H]1O

InChiKey: IXXFZUPTQVDPPK-AIHKGPLESA-N

InChi: InChI=1S/C43H65FN6O10/c1-12-32-43(8)35(50(40(55)60-43)19-14-13-18-49-23-30(46-47-49)28-16-15-17-29(45)21-28)26(4)33(51)24(2)22-41(6,56-11)37(27(5)36(53)42(7,44)39(54)58-32)59-38-34(52)31(48(9)10)20-25(3)57-38/h15-17,21,23-27,31-32,34-35,37-38,52H,12-14,18-20,22,45H2,1-11H3/t24-,25-,26+,27-,31+,32-,34-,35-,37-,38-,41+,42+,43-/m1/s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : ≥ 32 mg/mL (37.87 mM). H2O : < 0.1 mg/mL (insoluble).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

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.

Products are for research use only. Not for human use.