Crisaborole (AN2728)

Crisaborole (AN2728) is a small-molecule, boron-based, selective PDE4 inhibitor and has broad-spectrum anti-inflammatory activity.

Crisaborole (AN2728) Chemical Structure

Crisaborole (AN2728) Chemical Structure

CAS: 906673-24-3

Purity & Quality Control

Batch: S501401 DMSO] 50 mg/mL] false] ] ] false] ] ] false Purity: 98%
98

Choose Selective PDE Inhibitors

Biological Activity

Description Crisaborole (AN2728) is a small-molecule, boron-based, selective PDE4 inhibitor and has broad-spectrum anti-inflammatory activity.
Targets
PDE4 [1]
(Cell-free assay)
In Vivo
In vivo Crisaborole is well tolerated and not tumorigenic in mice[1].
Animal Research Animal Models Experimentally naïve male and female (325 each) Crl:CD1(ICR) mice
Dosages 0, 30, 100, or 300 mg/kg/day
Administration oral administration
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04800185 Active not recruiting Atopic Dermatitis|Atopic Dermatitis Eczema University of California Irvine|Pfizer March 23 2021 Early Phase 1
NCT03954158 Completed Atopic Dermatitis Pfizer June 15 2019 Phase 2
NCT03260595 Completed Healthy|Atopic Dermatitis Pfizer September 13 2017 Phase 1
NCT01652885 Completed Dermatitis Atopic Pfizer July 2012 Phase 1|Phase 2

Chemical lnformation & Solubility

Molecular Weight 251.05 Formula

C14H10BNO3

CAS No. 906673-24-3 SDF --
Smiles B1(C2=C(CO1)C=C(C=C2)OC3=CC=C(C=C3)C#N)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 50 mg/mL ( (199.16 mM); Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

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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 %

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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

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