クリサボロール
クリサボロール 物理性質
- 融点 :
- >130°C (softened)
- 沸点 :
- 425.9±55.0 °C(Predicted)
- 比重(密度) :
- 1.33±0.1 g/cm3(Predicted)
- 貯蔵温度 :
- room temp
- 溶解性:
- DMSO（微量）、メタノール（微量）
- 酸解離定数(Pka):
- 7.00±0.20(Predicted)
- 外見 :
- 粉
- 色:
- 白からベージュ
- 安定性：:
- Hygroscopic
- 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
- InChIKey:
- USZAGAREISWJDP-UHFFFAOYSA-N
- SMILES:
- C(#N)C1=CC=C(OC2=CC=C3B(O)OCC3=C2)C=C1
安全性情報
- リスクと安全性に関する声明
- 危険有害性情報のコード(GHS)
| メーカー |
製品番号 |
製品説明 |
CAS番号 |
包装 |
価格 |
更新時間 |
購入 |
|
Sigma-Aldrich Japan
|
PZ0037 |
クリサボロール ≥98% (HPLC)
Crisaborole ≥98% (HPLC) |
906673-24-3 |
5mg |
￥20500 |
2024-03-01 |
購入 |
|
Sigma-Aldrich Japan
|
PZ0037 |
クリサボロール ≥98% (HPLC)
Crisaborole ≥98% (HPLC) |
906673-24-3 |
25mg |
￥80100 |
2024-03-01 |
購入 |
クリサボロール 化学特性,用途語,生産方法
効能
乾癬治療薬, ホスホジエステラーゼ阻害薬
説明
Crisaborole is a phosphodiesterase- 4 (PDE4) inhibitor that was approved by FDA on December 14, 2016 as Eucrisa, a topical treatment of for mild to moderate atopic dermatitis (AD) in patients aged two years and older. The drug, which was developed by Anacor Pharmaceuticals and later acquired and marketed by Pfizer, is delivered as a 2% ointment, which is applied topically. Its structure contains a boron atom, which facilitates skin penetration and binding to the bimetal center of the phosphodiesterase 4 enzyme. The unique employment of boron within the chemical structure of the drug is designed to enable selective engagement of PDE4 (an enzyme involved in the conversion of cAMP into AMP, which signals for downstream inflammatory events), effective penetration of the drug through human skin, and rapid clearance to limit systemic circulation.
使用
A series of phenoxy benzoxaboroles were synthesized and screened for their inhibitory activity against PDE4 and cytokine release. 5-(4-Cyanophenoxy)-2,3-dihydro-1-hydroxy-2,1-benzoxaborole (AN2728) showed potent activity both in vitro and in vivo. AN2728 is being studied as an anti-inflammatory agent.
定義
ChEBI: Crisaborole is a member of the class of benzoxaboroles that is 5-hydroxy-1,3-dihydro-2,1-benzoxaborole in which the phenolic hydrogen has been replaced by a 4-cyanophenyl group. A phosphodiesterase 4 inhibitor that is used for treatment of mild to moderate atopic dermatitis in children and adults. It has a role as a phosphodiesterase IV inhibitor, an antipsoriatic and a non-steroidal anti-inflammatory drug. It is a benzoxaborole, an aromatic ether and a nitrile.
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副作用
EUCRISA may cause side effects.
Allergic reactions. EUCRISA may cause allergic reactions at or near the application site. These can be serious and may include hives, itching, swelling, and redness.
www.eucrisa.com
クリサボロール 上流と下流の製品情報
原材料
準備製品
クリサボロール 生産企業
Global( 394)Suppliers
- 906673-24-3
- AN-2728, >=98%
- AN2728, Crisaborole
- Crisaborole (AN2728)
- AN 2728
- AN2728/AN-2728
- 4-((1-Hydroxy-1,3-dihydrobenzo-[c][1,2]oxaborol-5-yl)oxy)benzonitrile
- 4-[(1,3-Dihydro-1-hydroxy-2,1-benzoxaborol-5-yl)oxy]benzonitrile
- AN-2728;AN2728;AN 2728
- 5-(4-cyanophenoxy)-2,3-dihydro-1-hydroxy-2,1-benzoxaborole
- Crisaborole
- Crisaborole （Eucrisa）
- 4-[(1-Hydroxy-1,3-dihydro-2,1-benzoxaborol-5-yl)oxy]benzonitrile
- 4-((1-hydroxy-1,3-dihydrobenzo
- 4-[(1-HYDROXY-3H-2,1-BENZOXABOROL-5-YL)OXY]BENZONITRILE
- CS-1895
- AN2728; AN 2728; AN2728; AN 2728
- PF-06930164
- Benzonitrile, 4-[(1,3-dihydro-1-hydroxy-2,1-benzoxaborol-5-yl)oxy]-
- 4-((1-hydroxy-1,3-dihydrobenzo[c][1,2]oxaborol-6-yl)oxy)benzonitrile
- NSAIDs for the topical treatment Crisaborole
- Crisaborole Impurity 18
- Crisaborole EP
- 4-((1-hydroxy-1,3-dihydrobenzo[c][1,2]oxaborolan-5-yl)oxy)benzonitrile
- Cleboro
- 4-[(1,3-Dihydro-1-hydroxy-2,1-benzoxaborol-5-yl)oxy]benzonitrile AN 2728
- G relenza boron
- 4-[(1,3- dihydro -1- hydroxy -2,1- benzoxeborane -5- yl) oxy] benzonitrile *
- Crisaborole In-House
- Creborol
- クリサボロール
- 4-[(1-ヒドロキシ-1,3-ジヒドロ-2,1-ベンゾオキサボロール-5-イル)オキシ]ベンゾニトリル
- オイクリサ
- 5-(4-シアノフェノキシ)-1-ヒドロキシ-1,3-ジヒドロ-2,1-ベンゾオキサボロール
- 5-(4-シアノフェノキシ)-1,3-ジヒドロ-2,1-ベンゾオキサボロール-1-オール