Name | Nosiheptide |
Synonyms | 101159 CS-2680 priMofax Nosiheptide Multhiomycin Nosiheptide VETRANAL Nosiheptide (Multhiomycin) |
CAS | 56377-79-8 |
EINECS | 260-138-4 |
InChI | InChI=1/C51H43N13O12S6/c1-5-23-46-60-28(14-79-46)41(70)56-25-10-33(67)50(74)76-11-21-7-6-8-24-34(21)18(2)35(54-24)51(75)82-17-31(57-42(71)29-15-80-47(25)61-29)48-58-26(12-78-48)37-22(45-59-30(13-77-45)43(72)64-36(20(4)65)44(73)55-23)9-32(66)38(63-37)49-62-27(16-81-49)40(69)53-19(3)39(52)68/h5-9,12-16,20,25,31,33,36,54,65-67H,3,10-11,17H2,1-2,4H3,(H2,52,68)(H,53,69)(H,55,73)(H,56,70)(H,57,71)(H,64,72)/b23-5- |
Molecular Formula | C51H43N13O12S6 |
Molar Mass | 1222.34 |
Density | 1.534±0.06 g/cm3(Predicted) |
Melting Point | 310-320° (dec) |
Specific Rotation(α) | D20 +38° (c = 1 in pyridine) |
Solubility | DMSO (Slightly), Methanol (Slightly) |
Appearance | Solid |
Color | Light Yellow to Light Brown |
pKa | 1.42±0.60(Predicted) |
Storage Condition | Sealed in dry,Store in freezer, under -20°C |
Refractive Index | 1.698 |
In vitro study | Nosiheptide exhibits extremely potent activity against all contemporary Staphylococcus aureus strains tested including multiple drug-resistant clinical isolates, with MIC values ≤ 0.25 mg/L. Nosiheptide is also highly active against Enterococcus spp and the contemporary hypervirulent BI strain of Clostridium difficile but is inactive against most Gram-negative strains tested. Time-kill analysis reveals Nosiheptide to be rapidly bactericidal against Staphylococcus aureus in a concentration- and time-dependent manner, with a nearly 2-log kill noted at 6 hours at 10X MIC. Furthermore, Nosiheptide is found to be non-cytotoxic against mammalian cells at >> 100X MIC, and its anti- Staphylococcus aureus activity is not inhibited by 20% human serum. Notably, Nosiheptide exhibits a significantly prolonged post-antibiotic effect against both healthcare- and community-associated Staphylococcus aureus compared to vancomycin. |