| Size | Price | Stock | Qty |
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| 25mg |
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| 100mg |
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| 250mg |
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| 1g |
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Purity: ≥98%
Crisaborole (formerly known as AN-2728; PF-06930164; AN2728; PF06930164; trade name: Eucrisa) is a potent and selective PDE4 (phosphodiesterase 4) inhibitor with a broad-spectrum of anti-inflammatory activity. It is a new and effective nonsteroidal topical drug for atopic dermatitis. It was approved by FDA in 2016 to treat mild to moderate eczema (atopic dermatitis) in patients two years of age and older. Crisaborole is a small-molecule based on the boron element and can be topically administered. It acts by inhibiting PDE4, thereby suppressing the release of cytokines such as TNFα, IL-12, IL-23 etc. This compound is also undergoing various phase studies for indications including atopic dermatitis and psoriasis.
| ln Vitro |
Crisaborole (AN-2728) has IC50 values of 0.49, 0.54, 0.61, 0.83, 2.4, and 5.3 μM and inhibits PDE4, TNF-α, IL-2, IFN-γ, IL-5, and IL-10. The most effective compound against the PDE4 catalytic domain is crisaborole (AN-2728), however it also exhibits inhibition against PDE1A3, PDE3Cat, and PDE7A1. With IC50 values of 6.1, 6.4, 0.11, and 0.73 μM, crisaborole (AN-2728) inhibits PDE isozymes PDE1A3, PDE3Cat, PDE4Cat, and PDE7A1[1]. Crystallography shows that benzoxaboroles' affinity for PDE4 is increased when they engage with the hydrophobic pocket in the PDE4 catalytic domain. These benzoxaboroles significantly reduce the release of cytokines linked to AD and Ps[2]. Crisaborole (AN-2728) is an anti-inflammatory substance with boron that is used topically. It works by inhibiting PDE4 activity, which in turn prevents the release of TNFalpha, IL-12, IL-23, and other cytokines[3].
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| ln Vivo |
After dosing at 1 mg/ear×2, crisaborole (AN-2728) exhibits a considerable inhibition against the ear edema caused by phorbol ester (78% and 68%, respectively). It is possible that Crisaborole (AN-2728) has good skin penetration and anti-inflammatory activity because the efficacy is similar to that of dexamethasone[1]. According to reports, crisaborole (AN-2728) is well tolerated and exhibits notable impacts on efficacy markers, yielding outcomes similar to those of positive controls in clinical trials[3].
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| 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.
[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. |
| Molecular Formula |
C14H10BNO3
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|---|---|
| Molecular Weight |
251.05
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| CAS # |
906673-24-3
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| Related CAS # |
Crisaborole-d4;2268785-42-6
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| SMILES |
N#CC1=CC=C(OC2=CC=C3C(B(O)OC3)=C2)C=C1
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| Chemical Name |
4-((1-hydroxy-1,3-dihydrobenzo[c][1,2]oxaborol-6-yl)oxy)benzonitrile
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| Synonyms |
AN-2728; PF06930164; AN 2728; PF-06930164; AN2728; PF 06930164; trade name: Eucrisa
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (9.96 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (9.96 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (9.96 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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