Nosiheptide

Research use only, not for human use.

Nosiheptide is a thiopeptide antibiotic produced by Streptomyces actuosus.

Nosiheptide is a thiopeptide antibiotic produced by Streptomyces actuosus. Nosiheptide has been widely used as a feed additive for animal growth. Nosiheptide inhibits bacterial protein synthesis and bears a unique indole side ring system and regiospecific hydroxyl groups on the characteristic macrocyclic core.

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.

Nosiheptide (20 mg/kg; intraperitoneal injection; injected at 1 and 8 h post-infection; female CD1 mice) provids significant protection against mortality. Ten out of 10 of the Nosiheptide-treated mice remains alive on day 3, while 6/10 of the controls died on day 1. Animal Model:Eight week old female CD1 mice injected with HA-Staphylococcus aureus strain Sanger 252 Dosage:20 mg/kg Administration:Intraperitoneal injection; injected at 1 and 8 h post-infection Result:Provided significant protection against mortality.

Multhiomycin | RP 9671

Microbiology/Virology

Antibiotic

Antibiotic|Bacterial

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56377-79-8

1222.36

C51H43N13O12S6

>98% (HPLC)

DMSO:125 mg/mL (102.26 mM; Need ultrasonic)

OC1=C(C2=NC(C(NC(C(N)=O)=C)=O)=CS2)N=C(C3=CSC(C4NC(C5=CSC(C(CC(C(OCC6=C7C(C)=C(NC7=CC=C6)C(SC4)=O)=O)O)NC(C8=CSC(/C(NC(C(C(O)C)NC(C9=CSC%10=N9)=O)=O)=C\C)=N8)=O)=N5)=O)=N3)C%10=C1

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(-20℃)

With Ice Pack

≥ 2 years