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Crisaborole

Crisaborole Struktur
906673-24-3
CAS-Nr.
906673-24-3
Englisch Name:
Crisaborole
Synonyma:
4-[(1,3-Dihydro-1-hydroxy-2,1-benzoxaborol-5-yl)oxy]benzonitrile AN 2728;AN 2728;CS-1895;Cleboro;Creborol;Crisaborole;PF-06930164;AN2728/AN-2728;AN-2728, >=98%;Crisaborole EP
CBNumber:
CB42518350
Summenformel:
C14H10BNO3
Molgewicht:
251.05
MOL-Datei:
906673-24-3.mol

Crisaborole Eigenschaften

Schmelzpunkt:
>130°C (softened)
Siedepunkt:
425.9±55.0 °C(Predicted)
Dichte
1.33±0.1 g/cm3(Predicted)
storage temp. 
room temp
L?slichkeit
DMSO (Slightly), Methanol (Slightly)
pka
7.00±0.20(Predicted)
Aggregatzustand
powder
Farbe
white to beige
Stabilit?t:
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
Sicherheit
  • Risiko- und Sicherheitserkl?rung
  • Gefahreninformationscode (GHS)
Bildanzeige (GHS) GHS hazard pictograms
Alarmwort Achtung
Gefahrenhinweise
Code Gefahrenhinweise Gefahrenklasse Abteilung Alarmwort Symbol P-Code
H315 Verursacht Hautreizungen. Hautreizung Kategorie 2 Warnung GHS hazard pictogramssrc="/GHS07.jpg" width="20" height="20" /> P264, P280, P302+P352, P321,P332+P313, P362
H319 Verursacht schwere Augenreizung. Schwere Augenreizung Kategorie 2 Warnung GHS hazard pictogramssrc="/GHS07.jpg" width="20" height="20" /> P264, P280, P305+P351+P338,P337+P313P
H335 Kann die Atemwege reizen. Spezifische Zielorgan-Toxizit?t (einmalige Exposition) Kategorie 3 (Atemwegsreizung) Warnung GHS hazard pictogramssrc="/GHS07.jpg" width="20" height="20" />
Sicherheit
P261 Einatmen von Staub vermeiden.
P301+P310 BEI VERSCHLUCKEN: Sofort GIFTINFORMATIONSZENTRUM/Arzt/... (geeignete Stelle für medizinische Notfallversorgung vom Hersteller/Lieferanten anzugeben) anrufen.
P305+P351+P338 BEI KONTAKT MIT DEN AUGEN: Einige Minuten lang behutsam mit Wasser spülen. Eventuell vorhandene Kontaktlinsen nach M?glichkeit entfernen. Weiter spülen.
P311 GIFTINFORMATIONSZENTRUM/Arzt anrufen.

Crisaborole Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung

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.

Verwenden

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.

Definition

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. ?

Nebenwirkungen

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

Crisaborole Upstream-Materialien And Downstream Produkte

Upstream-Materialien

Downstream Produkte


Crisaborole Anbieter Lieferant Produzent Hersteller Vertrieb H?ndler.

Global( 414)Lieferanten
Firmenname Telefon E-Mail Land Produktkatalog Edge Rate
HAINAN POLY PHARMCEUTICAL CO. LTD
+86-0571-89385087 +8613616530509
ff@hnpoly.com China 118 58
Shenzhen Excellent Biomedical Technology Co.,Ltd.
+86-0755-26050679 +86-15915472436
sale@ex-biotech.cn China 1031 58
S&Y Biochem Co.,Ltd
+8617774091612
marketing@sybiochem.com China 126 58
Hebei Yanxi Chemical Co., Ltd.
+8617531190177
peter@yan-xi.com China 5858 58
Shanghai UCHEM Inc.
+862156762820 +86-13564624040
sales@myuchem.com China 7388 58
shandong perfect biotechnology co.ltd
+86-53169958659; +8618596095638
sales@sdperfect.com China 294 58
Hangzhou ICH Biofarm Co., Ltd
+86-0571-28186870; +undefined8613073685410
sales@ichemie.com China 998 58
Zibo Hangyu Biotechnology Development Co., Ltd
+86-0533-2185556 +8617865335152
Mandy@hangyubiotech.com China 10986 58
Hebei Xinsheng New Material Technology Co., LTD.
+86-16632316109
xinshengkeji@xsmaterial.com China 1085 58
Anhui Ruihan Technology Co., Ltd
+8617756083858
daisy@anhuiruihan.com China 973 58

  • 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
  • 906673-24-3
  • C14H10BNO3
  • API
  • 906673-24-3
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