Crisaborole

한글명:Crisaborole

카스 번호906673-24-3

상품명:Crisaborole

CBNumberCB42518350

분자식C14H10BNO3

포뮬러 무게251.05

MOL 파일906673-24-3.mol

화학적 성질

녹는점	>130°C (softened)
끓는 점	425.9±55.0 °C(Predicted)
밀도	1.33±0.1 g/cm3(Predicted)
저장 조건	room temp
용해도	DMSO(약간 용해됨), 메탄올(약간 용해됨)
산도 계수 (pKa)	7.00±0.20(Predicted)
물리적 상태	가루
색상	흰색에서 베이지색
안정성	흡습성
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

그림문자(GHS)

Crisaborole 화학적 특성, 용도, 생산

개요
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.
용도
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.
정의
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of the class of benzoxaboroles that is 5-hydroxy-1,3-dihydro-2,1-benzoxaborole in which the phenolic hydrogen has been replaced by a 4-cyanophenyl group.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. ?
부작용
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

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