Nosiheptide

SKU: orb1217877

Description

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.

Key Properties

• CAS Number: 56377-79-8
• MW: 1222.36
• Purity: >98% (HPLC)
• Formula: C₅₁H₄₃N₁₃O₁₂S₆
• SMILES: 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
• Target: Antibiotic
• Solubility: DMSO:125 mg/mL (102.26 mM; Need ultrasonic)

Bioactivity

• In Vivo:
  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.
• In Vitro:
  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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Multhiomycin | RP 9671

Quick Database Links

Gene Symbol

Antibiotic