Isavuconazonium sulfate

SKU: orb1222974

Description

Isavuconazonium sulfate is hydrolyzed by plasma esterases to yield the active moiety isavuconazole. Isavuconazole binds to and inhibits the fungal cytochrome P450 family enzyme lanosterol 14-alpha-demethylase (CYP51), which catalyzes the demethylation of lanosterol to yield ergosterol, an important component of the fungal cell membrane. Isavuconazonium Sulfate is a prodrug of the triazole antifungal agent isavuconazole, with broad-spectrum antifungal activity. Inhibition of CYP51 leads to a decrease in fungal ergosterol production and disrupts the synthesis of the fungal cell membrane, which decreases membrane integrity, increases cell membrane permeability and promotes the loss of essential intracellular elements. This results in fungal cell lysis and death.

Key Properties

• CAS Number: 946075-13-4
• MW: 814.84
• Purity: >98% (HPLC)
• Formula: C₃₅H₃₆F₂N₈O₉S₂
• SMILES: n1(nc[n+](c1)C(C)OC(=O)N(c1c(cccn1)COC(=O)CNC)C)C[C@]([C@@H](C)c1scc(n1)c1ccc(cc1)C#N)(O)c1c(ccc(c1)F)F.S(=O)(=O)(O)[O-]
• Target: Antifection
• Solubility: In Vitro: DMSO : 100 mg/mL (122.72 mM)

Bioactivity

• In Vivo:
  Animal model: Neutropenic male ICR mouse model of intratracheal infection. Dosage: 215 mg/kg. Administration: Oral gavage (p.o.); Three times a day for 4 days. Result: Increased the survival rate of neutropenic mice infected with R. delemar. Reduced fungal load in the lungs and brains of mice.

Storage & Handling

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

Quick Database Links

Gene Symbol

Antifection