Isavuconazole

Synonyms: BAL-4815, RO-0094815

Isavuconazole (BAL-4815, RO-0094815) is a new extended-spectrum triazole with activity against yeasts, molds, and dimorphic fungi that inhibits cytochrome P450 (CYP)-dependent 14α-lanosterol demethylation, which is essential for fungal cell membrane ergosterol synthesis.

Isavuconazole Chemical Structure

Isavuconazole Chemical Structure

CAS: 241479-67-4

Selleck's Isavuconazole has been cited by 1 publication

Purity & Quality Control

Batch: S372201 DMSO] 87 mg/mL] false] Ethanol] 87 mg/mL] false] Water] Insoluble] false Purity: 99.99%
99.99

Isavuconazole Related Products

Choose Selective Fungal Inhibitors

Biological Activity

Description Isavuconazole (BAL-4815, RO-0094815) is a new extended-spectrum triazole with activity against yeasts, molds, and dimorphic fungi that inhibits cytochrome P450 (CYP)-dependent 14α-lanosterol demethylation, which is essential for fungal cell membrane ergosterol synthesis.
In vitro
In vitro Isavuconazole inhibits cytochrome P450 (CYP)–dependent 14α-lanosterol demethylation, which is essential for fungal cell membrane ergosterol synthesis. This blockade produces methylated sterols in the fungal membrane, altering its function and allowing the accumulation of ergosterol toxic precursors in the cytoplasm, which leads to cell death[1].
In Vivo
In vivo Isavuconazonium sulfate, the prodrug of isavuconazole, is available in both intravenous and oral formulations. After intravenous infusion, the prodrug is broken down quickly to the active component, isavuconazole, and an inactive cleavage product. Following oral administration, plasma concentrations of the active compound reach maximum concentrations (Cmax) by 2–3 hours; the prodrug and cleavage product are not measurable in plasma after oral administration. In healthy adult volunteers, isavuconazole exhibits linear and dose-proportional pharmacokinetics. The oral bioavailability of isavuconazole is 98%. Absorption of isavuconazole is not affected by food intake. In addition to excellent bioavailability, isavuconazole serum concentrations show low intersubject variability. In healthy volunteers, the Cmax at steady state was 2.5 ± 1.0 µg/mL. Isavuconazole has a large volume of distribution, is >99% protein bound, and has a long terminal half-life of 100-130 hours. Metabolism of isavuconazole takes place in the liver via the CYP enzyme family, specifically CYP3A4 and CYP3A5 isoenzymes[1].
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05630976 Recruiting
Invasive Fungal Disease
Pfizer
February 7 2023 Phase 4
NCT04486885 Unknown status
Cerebral Aspergillosis|Invasive Aspergillosis
Imagine Institute
August 1 2021 --
NCT04777058 Completed
Invasive Fungal Infections|Pharmacokinetics|Intensive Care Unit
Radboud University Medical Center
March 1 2021 --
NCT04550936 Unknown status
Invasive Aspergillosis|Mucormycosis
Pfizer
March 10 2021 --

Chemical Information & Solubility

Molecular Weight 437.47 Formula

C22H17F2N5OS
 

CAS No. 241479-67-4 SDF Download Isavuconazole SDF
Smiles CC(C1=NC(=CS1)C2=CC=C(C=C2)C#N)C(CN3C=NC=N3)(C4=C(C=CC(=C4)F)F)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 87 mg/mL ( (198.87 mM); Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 87 mg/mL

Water : Insoluble


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy Isavuconazole | Isavuconazole supplier | purchase Isavuconazole | Isavuconazole cost | Isavuconazole manufacturer | order Isavuconazole | Isavuconazole distributor