What is Crisaborole?
Crisaborole powder is the first topical prescription product approved by FDA for atopic dermatitis in recent ten years, and it is the first topical dermatological drug to enter the list of overseas new drugs urgently needed in clinic.
Crisaborole binds to the catalytic site of PDE-4 enzyme, blocking the down-regulation of cAMP, increasing intracellular cAMP level, activating PKA (protein kinase A) and blocking other downstream signals such as NF-κB and NF-AT, thus inhibiting the production of inflammatory cytokines, such as TNF-α, IFN-γ, IL-2, IL-5 and IL-10. The mechanism of action of topical glucocorticoid (TCS) is blocking NF-κB pathway, and that of topical calcineurin inhibitor (TCI) is blocking NF-AT pathway.
Boron atoms contained in Crisaborole structure can repair skin. Since 1990, boron has been proved to significantly improve wound healing. Further in vitro studies published in 2002 show that these beneficial effects of boron are due to the direct action of boron on specific enzymes in fibroblasts: elastase, trypsin-like enzyme, collagenase and alkaline phosphatase. Boron promotes the activities of these key enzymes in fibroblasts, synthesizes extracellular matrix and collagen, and plays a key role in wound healing.
| Product name | Crisaborole |
| CAS | 906673-24-3 |
| Molecular formula | C14H10BNO3 |
| Molecular weight | 251.05 |
| EINECS Number | 250-635-4 |
| Storage condition | room temp |
| Melting point | >130°C (softened) |
| Solubility | Soluble in DMSO (a little) and methanol (a little) |
| Appearance | White to beige powder |
| Boiling point | 425.9±55.0 °C(Predicted) |
| Density | 1.33±0.1 g/cm3(Predicted) |
What are the uses of Crisaborole?
Crisaborole powder has broad-spectrum bactericidal effect, which can effectively inhibit and kill a variety of bacteria, viruses, fungi and parasites, and can effectively prevent the spread of infectious diseases. Crisaborole can also be used to prevent and treat skin infections, disinfect and clean wounds, and has anti-inflammatory effects. It is worth noting that Crisaborole is a strong oxidant, and correct operation methods and safety precautions should be followed when using it to ensure safe use.
Product Specification
| Item | Specification | Results |
| Appearance | White or off-white solid powder | Complies |
| Iden tification | By IR | Complies |
| ByHPLC | Complies | |
| Solubili ty | Soluble | Complies |
| Loss on Drying | ≤1.00% | 0.55% |
| ResidualSolven ts | Methanol:≤3000ppm | ND |
| Ethanol:≤5000ppm | 4000ppm | |
| Related Substances | Any single impurity:≤0.30% | 0.10% |
| Total Impurities:≤1.00% | 0.28% | |
| Assay(HPLC basis on drying) | 98.0%~102.0% | 99.85% |
| Pseudom onas aeruginosa |
Negative | Negative |
| Staphylococcus aureus | Negative | Negative |
| Conclusion | Confom with enterprise specification. | |
What are the main applications of Crisaborole?
Fertilizer market: Crisaborole powder is a commonly used potassium chloride fertilizer, which is rich in potassium and is very important for plant growth. With the continuous development of agriculture and the increase of crop planting, Crisaborole has a high demand in the fertilizer market. The price of potassium chloride fertilizer is relatively stable, which also promotes the market stability of Crisaborole.
Oilfield exploitation market: during oilfield exploitation, Crisaborole is used to adjust wellhead pressure and stabilize borehole wall to prevent bottom hole collapse. This plays an important role in the process of oilfield exploitation, because wellhead pressure and wellbore stability are very important for safety and return on investment.
Medical industry: The demand for Crisaborole is relatively small, but it is still an important market.
HTML5 atlas of Crisaborole
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Biological activity of Crisaborole:
| Describe | Crisaborole (AN-2728) is an effective inhibitor of PDE4 and cytokine release, and the IC50 value of inhibiting PDE4 is 0.49 μM m. |
| Target spot | IC50: 0.49 μM (PDE4) |
| In vitro study | Crisaborole(AN-2728) inhibited 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 5.3μM, respectively. Crisaborole(AN-2728) showed the most effective activity on the catalytic domain of PDE4, but it also showed the inhibition on PDE1A3,PDE3Cat and PDE7A1. Crisaborole(AN-2728) inhibited PDE isoenzymes PDE1A3,PDE3Cat,PDE4Cat and PDE7A1, with IC50 values of 6.1,6.4,0.11 and 0.73μ m respectively [1]. Crystallography shows that the interaction between benzoxazolyboron ring and hydrophobic pocket in PDE4 catalytic domain increases their affinity for PDE4. These benzooxides strongly inhibit the secretion of cytokines related to Ps and AD. Crisaborole(AN-2728) is a boron-containing anti-inflammatory compound, which can inhibit the activity of PDE4, thus inhibiting the release of TNFalpha,IL-12,IL-23 and other cytokines. |
| In vivo study | Crisaborole(AN-2728) showed significant inhibition of ear edema caused by phorbol ester after administration of 1mg/ear 2× (78% and 68% respectively). The curative effect is equivalent to that of dexamethasone, indicating that Crisaborole(AN-2728) has good anti-inflammatory activity and skin permeability. It is reported that Crisaborole(AN-2728) has good tolerance and has a significant effect on therapeutic markers, and the results are equivalent to the positive control in clinical trials. |
| 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. [3]. 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. |
What are the advantages of Crisaborole?
Crisaborole is a commonly used chemical reagent, which has many advantages in chemical experiments and industrial production. Here are some product advantages of Crisaborole:
High purity: Crisaborole powder is made of high-purity raw materials, which ensures the high purity and stability of chemical reagents and can provide accurate experimental results.
Stable quality: Crisaborole has undergone strict quality control and standardized production process, and each batch of products has undergone strict inspection and testing to ensure the quality and stability of products.
A variety of specifications can be selected: Crisaborole provides a variety of specifications and packaging options, which can meet different experimental needs and personalized requirements of users.
Environmental protection and safety: Crisaborole meets environmental protection standards, and has undergone strict safety assessment and testing, so it is safe and reliable to use.
To sum up, Crisaborole has become one of the indispensable chemical reagents in chemical experiments and industrial production because of its high purity, stability and wide application.
What is the difference between Crisaborole and Tacrolimus?
The difference between Crisaborole and Tacrolimus is generally different in composition, efficacy and applicable symptoms.
1, the composition is different
The main component of Crisaborole is Crisaborole powder, which is a white powder. The main component of Tacrolimus is Tacrolimus powder, which is a powerful immunosuppressant.
2, the effect is different
Crisaborole generally has anti-inflammatory effect, which can be used to treat specific dermatitis, eczema, contact dermatitis and other diseases. Tacrolimus can generally be used to treat people with normal immune function but eczema, and can relieve skin itching, redness and other symptoms caused by specific dermatitis.
3, the applicable symptoms are different
Crisaborole can generally be used to treat mild to moderate specific dermatitis. Tacrolimus can generally be used to treat eczema on the face, scalp and other parts, and can relieve the symptoms of chronic specific dermatitis, such as itching, redness and swelling of the skin.
How and where to buy Crisaborole powder wholesale?
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We conduct independent laboratory tests on all products and then sell them to our respected customers.
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Note: This compound should be used for research purposes only. These claims have not been evaluated by the Food and Drug Administration. Please consult your doctor and learn about available studies before using them. This product is not intended to diagnose, treat, cure, or prevent any disease.
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