Crisaborole
Based on 4 publication(s) in Google Scholar
Crisaborole (AN-2728) is a potent inhibitor of PDE4 and cytokine release; inhibit PDE4 with an IC50 of 0.49 μM.
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- Purity: 99.94%
- CAS No.: 906673-24-3
- 화학식: C14H10BNO3
- 분자량:251.05
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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용액&용해도
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Publications Citing Use of MedChemExpress (MCE) Crisaborole
More
Biological Activity
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PDE4 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| PBMC | EC50 |
0.53 μM
Compound: Crisaborole
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Inhibition of LPS-induced TNF-alpha production in human PBMC cells pretreated for 1 hr followed by LPS addition and measured after 24 hrs by ELISA
Inhibition of LPS-induced TNF-alpha production in human PBMC cells pretreated for 1 hr followed by LPS addition and measured after 24 hrs by ELISA
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[PMID: 38489246] |
| PBMC | IC50 |
0.54 μM
Compound: 5b, AN2728
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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
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[PMID: 19303290] |
| PBMC | IC50 |
0.61 μM
Compound: 5b, AN2728
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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
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[PMID: 19303290] |
| PBMC | IC50 |
0.83 μM
Compound: 5b, AN2728
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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
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[PMID: 19303290] |
| PBMC | IC50 |
2.4 μM
Compound: 5b, AN2728
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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
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[PMID: 19303290] |
| PBMC | IC50 |
5.3 μM
Compound: 5b, AN2728
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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
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[PMID: 19303290] |
| Sf9 | IC50 |
0.11 μM
Compound: 5b, AN2728
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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
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[PMID: 19303290] |
| Sf9 | IC50 |
0.73 μM
Compound: 5b, AN2728
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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
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[PMID: 19303290] |
| Sf9 | IC50 |
6.1 μM
Compound: 5b, AN2728
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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
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[PMID: 19303290] |
| Sf9 | IC50 |
6.4 μM
Compound: 5b, AN2728
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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
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[PMID: 19303290] |
| U-937 | IC50 |
0.49 μM
Compound: 5b, AN2728
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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
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[PMID: 19303290] |
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 906673-24-3
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Appearance Solid
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분자량 251.05
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화학식 C14H10BNO3
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Color White to off-white
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SMILES
N#CC1=CC=C(OC2=CC=C(B(O)OC3)C3=C2)C=C1
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Synonyms
AN-2728; PF-06930164
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (4)
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Journal Impact Factor
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Most Recent
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Int J Pharm
A new ex vivo skin model for mechanistic understanding of putative anti-inflammatory topical therapeutics. [Abstract]2022 Apr 5:617:121610. PMID: 35202723 -
Front Pharmacol
2022 Jun 22:13:920643. PMID: 35814244 -
Eur J Pharmacol
Anti-inflammatory effects of a novel phosphodiesterase-4 inhibitor, AA6216, in mouse dermatitis models. [Abstract]2021 Sep 5:906:174258. PMID: 34139195 -
Expert Rev Anti Infect Ther
Synergistic antifungal effects and potential mode of action of crisaborole combined with azoles against drug-resistant Candida albicans. [Abstract]2026 Jun 23. PMID: 42334844
용액&용해도
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.
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
순도&문서
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Data Sheet (274 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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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
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.
| 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 |
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