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Albaconazole

Catalog No. T7725   CAS 187949-02-6
Synonyms: W 0027, UR-9825, UR9825, W-0027

Albaconazole (W-0027) is a small molecule fungal cytochrome P450 family member 51 (fungal CYP51A1) inhibitor. It is used in the treatment of fungal infections, skin and musculoskeletal disorders, and can be used in the study of vulvovaginal candidiasis, Chagas disease and genitourinary disorders.

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Albaconazole Chemical Structure
Albaconazole, CAS 187949-02-6
Pack Size Availability Price/USD Quantity
1 mg In stock $ 350.00
5 mg In stock $ 828.00
10 mg In stock $ 1,130.00
25 mg In stock $ 1,590.00
50 mg In stock $ 1,980.00
100 mg In stock $ 2,500.00
500 mg In stock $ 4,900.00
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ee: 100%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Albaconazole (W-0027) is a small molecule fungal cytochrome P450 family member 51 (fungal CYP51A1) inhibitor. It is used in the treatment of fungal infections, skin and musculoskeletal disorders, and can be used in the study of vulvovaginal candidiasis, Chagas disease and genitourinary disorders.
In vivo Forty participants were enrolled in this Phase I, open-label, two-sequence crossover study. Twenty participants were exposed to a single 400-mg tablet dose of albaconazole before being crossed over to a single dose of four 100-mg albaconazole capsules. The second group of 20 participants received the study products in reverse order. Blood samples were taken over 15 days post-dose to assess the plasma concentrations and pharmacokinetic parameters of albaconazole and its primary metabolite, 6-hydroxyalbaconazole. Safety was assessed throughout the study. The area under the curve (AUC) and maximum measured plasma concentration (C(max)) of the albaconazole tablet were approximately 10% and 22% lower, respectively, than for the albaconazole capsules. Statistical significance was reached for the C(max) but not for the AUC measurements (AUC(0-t) and AUC(0-inf)). Because the 90% confidence intervals based on the differences between the tablet and capsule were outside the 80%-125% range for both the C(max) and AUC, we concluded that the formulations were not bioequivalent with respect to the rate or extent of absorption. The AUC and C(max) of albaconazole after a single 400-mg oral dose administered as a tablet formulation were lower than those of a capsule formulation. Albaconazole tablets and capsules cannot, therefore, be considered bioequivalent.[1]
Synonyms W 0027, UR-9825, UR9825, W-0027
Molecular Weight 431.82
Formula C20H16ClF2N5O2
CAS No. 187949-02-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: Soluble

TargetMolReferences and Literature

1. van Rossem K, et al. A Phase 1, randomized, open-label crossover study to evaluate the safety and pharmacokinetics of 400 mg albaconazole administered to healthy participants as a tablet formulation versus a capsule formulation. Clin Pharmacol. 2013;5:23-31. 2. Dietz AJ, et al. A randomized, double-blind, multiple-dose, placebo-controlled, dose escalation study with a 3-cohort parallel group design to investigate the tolerability and pharmacokinetics of albaconazole in healthy subjects. Clin Pharmacol Drug Dev. 2014;3(1):25-33. 3. Miller JL, et al. In vitro and in vivo efficacies of the new triazole albaconazole against Cryptococcus neoformans. Antimicrob Agents Chemother. 2004;48(2):384-387. 4. Morera-López Y, et al. Cryptococcus gattii: in vitro susceptibility to the new antifungal albaconazole versus fluconazole and voriconazole. Med Mycol. 2005;43(6):505-510.

Related compound libraries

This product is contained In the following compound libraries:
Drug Repurposing Compound Library Inhibitor Library Bioactive Compound Library Clinical Compound Library Bioactive Compounds Library Max

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Keywords

Albaconazole 187949-02-6 Metabolism Microbiology/Virology P450 Antifungal W 0027 W0027 UR-9825 UR9825 W-0027 UR 9825 inhibitor inhibit

 

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