Anidulafungin

SKU: orb1225987

Description

Anidulafungin (LY303366), an echinocandin derivative, inhibits glucan synthase activity, used as an antifungal drug.(In Vitro):Anidulafungin (LY-303366) has MICs of ≤0.32 μg/mL for all Candida albicans (n=99), Candida glabrata (n=18), and Candida tropicalis (n=10) isolates tested. Anidulafungin is also active against Aspergillus species (minimum effective concentration at which 90% of the isolates are inhibited, 0.02 μg/mL) (n=20), is less active against Candida parapsilosis (MIC at which 90% of the isolates are inhibited [MIC90], 5.12 μg/mL) (n=10), and is inactive against C. neoformans (MIC90 >10.24 μg/mL) (n=15) and B. dermatitidis (MIC90, 16 μg/mL) (n=29).The MICs of Fluconazole for three strains of C. tropicalis, seven strains of C. glabrata, and two strains of Candida krusei are ≥16 μg/mL. The MICs of Anidulafungin for 11 of these 12 strains range from 0.08 to 0.32 mg/mL. The twelfth strain is a C. krusei strain (Fluconazole MIC, 32 μg/mL) for which the Anidulafungin MIC is 1.28 mg/mL. The MIC at which 90% of the isolates are inhibited (MIC90) for these 12 strains is 0.32 μg/mL. The Anidulafungin MIC90 for the remaining 18 C. glabrata isolates and C. tropicalis isolates for which the Fluconazole MICs are ≥ 8 μg/mL is also 0.32 mg/mL. Anidulafungin appeares equally active against Candida species for which the fluconazole MICs are ≥16 mg/mL and against those for which the fluconazole MICs are ≥ 8 μg/mL. Anidulafungin has significantly less activity against C. neoformans and B. dermatitidis than against C. albicans, C. glabrata, and C. tropicalis. Ketoconazole and amphotericin B are the most active antifungal agents tested for both C. neoformans and B. dermatitidis. Anidulafungin demonstrated potent in vitro activity against Aspergillus species with a MEC90 of 0.02 μg/mL. MICs of Anidulafungin for the control strain yeast isolates are 0.02 μg/mL for C. albicans ATCC 90028, 0.16 mg/mL for C. glabrata ATCC 90030, and >10.24 μg/mL for C. neoformans ATCC 90112. Strains selected with CD101 that have a 2-fold or greater CD101 MIC increase also have at least a 2-fold MIC increase for Anidulafungin (ANF) and/or Caspofungin (CSF).

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 166663-25-8
• MW: 1140.24
• Purity: >98% (HPLC)
• Formula: C₅₈H₇₃N₇O₁₇
• SMILES: CCCCCOC1=CC=C(C2=CC=C(C3=CC=C(C(N[C@@H]4C[C@@H](O)[C@@H](O)NC([C@@H]5[C@@H](O)[C@@H](C)CN5C([C@H]([C@@H](O)C)NC([C@H]([C@@H](O)[C@@H](O)C6=CC=C(O)C=C6)NC([C@@H]7C[C@@H](O)CN7C([C@H]([C@@H](O)C)NC4=O)=O)=O)=O)=O)=O)=O)C=C3)C=C2)C=C1
• Target: glucan synthase
• Solubility: DMSO:100 mg/mL warmed (87.7 mM); Ethanol:<1 mg/mL warmed (<1 mM); Water:<1 mg/mL (<1 mM)

Bioactivity

• In Vitro:
  Anidulafungin (LY-303366) has MICs of ≤0.32 μg/mL for all Candida albicans (n=99), Candida glabrata (n=18), and Candida tropicalis (n=10) isolates tested. Anidulafungin is also active against Aspergillus species (minimum effective concentration at which 90% of the isolates are inhibited, 0.02 μg/mL) (n=20), is less active against Candida parapsilosis (MIC at which 90% of the isolates are inhibited [MIC90], 5.12 μg/mL) (n=10), and is inactive against C. neoformans (MIC90 >10.24 μg/mL) (n=15) and B. dermatitidis (MIC90, 16 μg/mL) (n=29). The MICs of Fluconazole for three strains of C. tropicalis, seven strains of C. glabrata, and two strains of Candida krusei are ≥16 μg/mL. The MICs of Anidulafungin for 11 of these 12 strains range from 0.08 to 0.32 mg/mL. The twelfth strain is a C. krusei strain (Fluconazole MIC, 32 μg/mL) for which the Anidulafungin MIC is 1.28 mg/mL. The MIC at which 90% of the isolates are inhibited (MIC90) for these 12 strains is 0.32 μg/mL. The Anidulafungin MIC90 for the remaining 18 C. glabrata isolates and C. tropicalis isolates for which the Fluconazole MICs are ≥ 8 μg/mL is also 0.32 mg/mL. Anidulafungin appeares equally active against Candida species for which the fluconazole MICs are ≥16 mg/mL and against those for which the fluconazole MICs are ≥ 8 μg/mL. Anidulafungin has significantly less activity against C. neoformans and B. dermatitidis than against C. albicans, C. glabrata, and C. tropicalis. Ketoconazole and amphotericin B are the most active antifungal agents tested for both C. neoformans and B. dermatitidis. Anidulafungin demonstrated potent in vitro activity against Aspergillus species with a MEC90 of 0.02 μg/mL. MICs of Anidulafungin for the control strain yeast isolates are 0.02 μg/mL for C. albicans ATCC 90028, 0.16 mg/mL for C. glabrata ATCC 90030, and >10.24 μg/mL for C. neoformans ATCC 90112. Strains selected with CD101 that have a 2-fold or greater CD101 MIC increase also have at least a 2-fold MIC increase for Anidulafungin (ANF) and/or Caspofungin (CSF).

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

LY303366

Quick Database Links

Gene Symbol

glucan synthase