Crisaborole (Synonyms: AN-2728; PF-06930164)

Name: Crisaborole
Brand: MedChemExpress
SKU: HY-10978
Rating: 5.0 (3 reviews)

Cat. No.: HY-10978 Purity: 99.92%: FAQs
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Crisaborole (AN-2728) is a potent inhibitor of PDE4 and cytokine release; inhibit PDE4 with an IC₅₀ of 0.49 μM.

For research use only. We do not sell to patients.

Crisaborole Chemical Structure

CAS No. : 906673-24-3

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 61	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 61	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 35	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 55	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 65	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 101	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 3 publication(s) in Google Scholar

Other Forms of Crisaborole:

Crisaborole-d₄ Get quote
Crisaborole (Standard) Get quote

3 Publications Citing Use of MCE Crisaborole

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View All Isoforms

PDE1 PDE2 PDE3 PDE4 PDE5 PDE6 PDE7 PDE9 PDE10 PDE11 PDE12 PDE8 Autotaxin

Biological Activity
Purity & Documentation
References
Customer Review

Description

Crisaborole (AN-2728) is a potent inhibitor of PDE4 and cytokine release; inhibit PDE4 with an IC₅₀ of 0.49 μM.

IC₅₀ & Target

PDE4

Cellular Effect

Cell Line	Type	Value	Description	References
PBMC	IC₅₀	0.54 μM Compound: 5b, AN2728	Antiinflammatory activity in human PBMC assessed as inhibition of LPS-induced TNFalpha release in after 24 hrs by FACS Array analysis Antiinflammatory activity in human PBMC assessed as inhibition of LPS-induced TNFalpha release in after 24 hrs by FACS Array analysis	[PMID: 19303290]
PBMC	IC₅₀	0.61 μM Compound: 5b, AN2728	Antiinflammatory activity in human PBMC assessed as inhibition of phytohemagglutininin-induced IL2 release after 24 hrs by FACS Array analysis Antiinflammatory activity in human PBMC assessed as inhibition of phytohemagglutininin-induced IL2 release after 24 hrs by FACS Array analysis	[PMID: 19303290]
PBMC	IC₅₀	0.83 μM Compound: 5b, AN2728	Antiinflammatory activity in human PBMC assessed as inhibition of phytohemagglutininin-induced IFN-gamma release after 24 hrs by FACSArray analysis Antiinflammatory activity in human PBMC assessed as inhibition of phytohemagglutininin-induced IFN-gamma release after 24 hrs by FACSArray analysis	[PMID: 19303290]
PBMC	IC₅₀	2.4 μM Compound: 5b, AN2728	Antiinflammatory activity in human PBMC assessed as inhibition of phytohemagglutininin-induced IL5 release after 48 hrs by FACS Array analysis Antiinflammatory activity in human PBMC assessed as inhibition of phytohemagglutininin-induced IL5 release after 48 hrs by FACS Array analysis	[PMID: 19303290]
PBMC	IC₅₀	5.3 μM Compound: 5b, AN2728	Antiinflammatory activity in human PBMC assessed as inhibition of phytohemagglutininin-induced IL10 release after 48 hrs by FACS Array analysis Antiinflammatory activity in human PBMC assessed as inhibition of phytohemagglutininin-induced IL10 release after 48 hrs by FACS Array analysis	[PMID: 19303290]
Sf9	IC₅₀	0.11 μM Compound: 5b, AN2728	Inhibition of human recombinant PDE4 catalytic domain expressed in baculovirus-infected insect Sf9 cells by modified two-step method Inhibition of human recombinant PDE4 catalytic domain expressed in baculovirus-infected insect Sf9 cells by modified two-step method	[PMID: 19303290]
Sf9	IC₅₀	0.73 μM Compound: 5b, AN2728	Inhibition of human recombinant PDE7A1 expressed in baculovirus-infected insect Sf9 cells by modified two-step method Inhibition of human recombinant PDE7A1 expressed in baculovirus-infected insect Sf9 cells by modified two-step method	[PMID: 19303290]
Sf9	IC₅₀	6.1 μM Compound: 5b, AN2728	Inhibition of human recombinant PDE1A3 expressed in baculovirus-infected insect Sf9 cells by modified two-step method Inhibition of human recombinant PDE1A3 expressed in baculovirus-infected insect Sf9 cells by modified two-step method	[PMID: 19303290]
Sf9	IC₅₀	6.4 μM Compound: 5b, AN2728	Inhibition of human recombinant PDE3 catalytic domain expressed in baculovirus-infected insect Sf9 cells by modified two-step method Inhibition of human recombinant PDE3 catalytic domain expressed in baculovirus-infected insect Sf9 cells by modified two-step method	[PMID: 19303290]
U-937	IC₅₀	0.49 μM Compound: 5b, AN2728	Inhibition of PDE4 in human U937 cells assessed as accumulation of [3H]adenosine by scintillation counting Inhibition of PDE4 in human U937 cells assessed as accumulation of [3H]adenosine by scintillation counting	[PMID: 19303290]

In Vitro

Crisaborole (AN-2728) inhibits PDE4, TNF-α, IL-2, IFN-γ, IL-5 and IL-10 with IC₅₀ values of 0.49, 0.54, 0.61, 0.83, 2.4 and 5.3 μM. Crisaborole (AN-2728) shows the most potent activity against PDE4 catalytic domain, but it also shows inhibition against PDE1A3, PDE3Cat, and PDE7A1. Crisaborole (AN-2728) inhibits PDE isozymes PDE1A3, PDE3Cat , PDE4Cat and PDE7A1 with IC₅₀ values of 6.1, 6.4, 0.11 and 0.73 μM^[1]. Crystallography reveals that interaction of benzoxaboroles with the hydrophobic pocket in the PDE4 catalytic domain increase their affinity for PDE4. These benzoxaboroles strongly suppresses the secretion of cytokines associated with Ps and AD^[2]. Crisaborole (AN-2728) is a topically administered, boron-containing, anti-inflammatory compound that inhibits PDE4 activity and thereby suppresses the release of TNFalpha, IL-12, IL-23 and other cytokines^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Crisaborole (AN-2728) shows significant inhibition against the ear edema caused by phorbol ester after dosing at 1 mg/ear×2 (78% and 68%, respectively). The efficacy is comparable to that of dexamethasone, suggesting that Crisaborole (AN-2728) has good anti-inflammatory activity as well as skin penetration^[1]. Crisaborole (AN-2728) is reported to be well tolerated and to demonstrate significant effects on markers of efficacy, with results that are comparable to positive controls in clinical trials^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

Molecular Weight

251.05

Formula

C₁₄H₁₀BNO₃

CAS No.

906673-24-3

Appearance

Solid

Color

White to khaki

SMILES

N#CC1=CC=C(OC2=CC=C(B(O)OC3)C3=C2)C=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Store at room temperature, keep dry and cool

In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : ≥ 100 mg/mL (398.33 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	3.9833 mL	19.9164 mL	39.8327 mL
5 mM	0.7967 mL	3.9833 mL	7.9665 mL
10 mM	0.3983 mL	1.9916 mL	3.9833 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (9.96 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (9.96 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (9.96 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.92%

Select Batch:

Data Sheet (274 KB) SDS (393 KB)

COA (247 KB) RP-HPLC (95 KB)

Handling Instructions (2659 KB)

References

[1]. Akama T, et al. Discovery and structure-activity study of a novel benzoxaborole anti-inflammatory agent (AN2728) for the potential topical treatment of psoriasis and atopic dermatitis. Bioorg Med Chem Lett. 2009 Apr 15;19(8):2129-32. [Content Brief]

[2]. Nazarian R, et al. AN-2728, a PDE4 inhibitor for the potential topical treatment of psoriasis and atopic dermatitis. Curr Opin Investig Drugs. 2009 Nov;10(11):1236-42. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	3.9833 mL	19.9164 mL	39.8327 mL	99.5818 mL
	5 mM	0.7967 mL	3.9833 mL	7.9665 mL	19.9164 mL
	10 mM	0.3983 mL	1.9916 mL	3.9833 mL	9.9582 mL
	15 mM	0.2656 mL	1.3278 mL	2.6555 mL	6.6388 mL
	20 mM	0.1992 mL	0.9958 mL	1.9916 mL	4.9791 mL
	25 mM	0.1593 mL	0.7967 mL	1.5933 mL	3.9833 mL
	30 mM	0.1328 mL	0.6639 mL	1.3278 mL	3.3194 mL
	40 mM	0.0996 mL	0.4979 mL	0.9958 mL	2.4895 mL
	50 mM	0.0797 mL	0.3983 mL	0.7967 mL	1.9916 mL
	60 mM	0.0664 mL	0.3319 mL	0.6639 mL	1.6597 mL
	80 mM	0.0498 mL	0.2490 mL	0.4979 mL	1.2448 mL
	100 mM	0.0398 mL	0.1992 mL	0.3983 mL	0.9958 mL

Crisaborole Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Crisaborole906673-24-3AN-2728 PF-06930164AN2728AN 2728PF06930164PF 06930164PF-06930164Phosphodiesterase (PDE)Inhibitorinhibitorinhibit

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Crisaborole (Synonyms: AN-2728; PF-06930164)

Customer Review

Other Forms of Crisaborole:

Crisaborole Related Antibodies

3 Publications Citing Use of MCE Crisaborole

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Phosphodiesterase (PDE) Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Crisaborole Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Crisaborole Related Classifications

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