AN-2728PDE4 inhibitor,anti-inflammatory compound CAS# 906673-24-3 |
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Quality Control & MSDS
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| Cas No. | 906673-24-3 | SDF | Download SDF |
| PubChem ID | 44591583 | Appearance | Powder |
| Formula | C14H10BNO3 | M.Wt | 251.05 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Synonyms | Crisaborole | ||
| Solubility | DMSO : ≥ 100 mg/mL (398.33 mM) *"≥" means soluble, but saturation unknown. | ||
| Chemical Name | 4-[(1-hydroxy-3H-2,1-benzoxaborol-5-yl)oxy]benzonitrile | ||
| SMILES | B1(C2=C(CO1)C=C(C=C2)OC3=CC=C(C=C3)C#N)O | ||
| Standard InChIKey | USZAGAREISWJDP-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C14H10BNO3/c16-8-10-1-3-12(4-2-10)19-13-5-6-14-11(7-13)9-18-15(14)17/h1-7,17H,9H2 | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | AN-2728 is a potent inhibitor of PDE4 and cytokine release; inhibit PDE4 with an IC50 of 0.49 μM.In Vitro: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. AN-2728 shows the most potent activity against PDE4 catalytic domain, but it also shows inhibition against PDE1A3, PDE3Cat, and PDE7A1. 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]. 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].In Vivo: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 AN-2728 has good anti-inflammatory activity as well as skin penetration[1]. AN-2728 is reported to be well tolerated and to demonstrate significant effects on markers of efficacy, with results that were comparable to positive controls in clinical trials[3]. References: | |||||
AN-2728 Dilution Calculator
AN-2728 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 3.9833 mL | 19.9164 mL | 39.8327 mL | 79.6654 mL | 99.5818 mL |
| 5 mM | 0.7967 mL | 3.9833 mL | 7.9665 mL | 15.9331 mL | 19.9164 mL |
| 10 mM | 0.3983 mL | 1.9916 mL | 3.9833 mL | 7.9665 mL | 9.9582 mL |
| 50 mM | 0.0797 mL | 0.3983 mL | 0.7967 mL | 1.5933 mL | 1.9916 mL |
| 100 mM | 0.0398 mL | 0.1992 mL | 0.3983 mL | 0.7967 mL | 0.9958 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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AN-2728 is an inhibitor of PDE4 with IC50 value of 0.49 μM [1]. PDE4 is a phosphodiesterase and plays an important role in the chronic inflammation associated with psoriasis and atopic dermatitis [2].
AN-2728 is a boron-containing, anti-inflammatory, topically administered compound that inhibits PDE4 activity and suppresses the release of TNF-α, IL-23, IL-12 and other cytokines [2]. In cell based assays, AN-2728 inhibited cytokine release of TNF-α, IL-2, IFN-γ, IL-5 and IL-10 with IC50 values of 0.54, 0.61, 0.83, 2.4 and 5.3 μM, respectively [1].
AN-2728 was well tolerated and had good therapeutic potential. AN-2728 is now in clinical development for the treatment of psoriasis and atopic dermatitis [2].
References:
[1]. Akama T, Baker SJ, Zhang YK, 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, 19(8): 2129-2132.
[2]. Nazarian R, Weinberg JM. AN-2728, a PDE4 inhibitor for the potential topical treatment of psoriasis and atopic dermatitis. Curr Opin Investig Drugs, 2009, 10(11): 1236-1242.
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AN-2728, a PDE4 inhibitor for the potential topical treatment of psoriasis and atopic dermatitis.[Pubmed:19876791]
Curr Opin Investig Drugs. 2009 Nov;10(11):1236-42.
Cytokines are signaling molecules that are believed to be key factors in perpetuating the inflammatory process in psoriasis and atopic dermatitis. AN-2728, being developed by Anacor Pharmaceuticals Inc, 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. At the time of publication, three phase Ib clinical trials, a IIa trial and a IIb trial of AN-2728 in patients with psoriasis had been completed; the compound was also undergoing phase II development for atopic dermatitis, but no data were available for this indication. AN-2728 was reported to be well tolerated and to demonstrate significant effects on markers of efficacy, with results that were comparable to positive controls. AN-2728 appears to have good therapeutic potential, although further and larger trials are required to assess the long-term safety and characterize the broad utility of this drug.
