产品资料

MedKoo Biosciences/Roflumilast/300320/250mg

Roflumilastisadrugwhichactsasaselective,long-actinginhibitoroftheenzymePDE-4.Ithasanti-inflammatoryeffectsandisunderdevelopmentasanorallyadmiNISTereddrugforthetreatmentofinflammatoryconditionsofthelungssuchasasthma,andchronicobstructivepulmonarydisease(COPD).InJune2010,DaxaswasapprovedintheEUforsevereCOPDassociatedwithchronicbronchitis.[9]InMarch2011,DalirespgainedFDAapprovalintheUSforreducingCOPDexacerbations.

MedKooCat#:300320
Name:Roflumilast
CAS#:162401-32-3
ChemicalFormula:C17H14Cl2F2N2O3
ExactMass:402.03495
MolecularWeight:403.21
ElementalAnalysis:C,50.64;H,3.50;Cl,17.58;F,9.42;N,6.95;O,11.90

Synonym:BY217;BY-217;BY217;B9302-107;B9302-107;B-9302-107;BYK20869;BYK-20869;BYK20869;Daxas;Daliresp

IUPAC/ChemicalName:3-(cyclopropylmethoxy)-N-(3,5-dichloropyridin-4-yl)-4-(difluoromethoxy)benzamide

InChiKey:MNDBXUUTURYVHR-UHFFFAOYSA-N

InChiCode:InChI=1S/C17H14Cl2F2N2O3/c18-11-6-22-7-12(19)15(11)23-16(24)10-3-4-13(26-17(20)21)14(5-10)25-8-9-1-2-9/h4-7,9,17H,1-2,8H2,(H,22,23,24)

SMILESCode:O=C(NC1=C(Cl)C=NC=C1Cl)C2=CC=C(OC(F)F)C(OCC3CC3)=C2

TechnicalData

Appearance:

solidpowder

Purity:

>98%(orrefertotheCertificateofAnalysis)

ShippingCondition:

Shippedunderambienttemperatureasnon-hazardouschemical.ThisproductisstableenoughforafewweeksduringordinaryshippingandtimespentinCustoms.

StorageCondition:

Dry,darkandat0-4Cforshortterm(daystoweeks)or-20Cforlongterm(monthstoyears).

Solubility:

SolubleinDMSO.

ShelfLife:

>2yearsifstoredproperly

DrugFormulation:

ThisdrugmaybeformulatedinDMSO

StockSolutionStorage:

0-4Cforshortterm(daystoweeks),or-20Cforlongterm(months).

HarmonizedSystemCode:

293490

References

1:ObaY,LoneNA.Efficacyandsafetyofroflumilastinpatientswithchronicobstructivepulmonarydisease:asystematicreviewandmeta-analysis.TherAdvRespirDis.2013Feb;7(1):13-24.doi:10.1177/1753465812466167.Epub2012Nov29.Review.PubMedPMID:23197074.

2:TaegtmeyerAB,LeuppiJD,Kullak-UblickGA.Roflumilast--aphosphodiesterase-4inhibitorlicensedforadd-ontherapyinsevereCOPD.SwissMedWkly.2012Jul25;142:w13628.doi:10.4414/smw.2012.13628.Review.PubMedPMID:22833385.

3:ReidDJ,PhamNT.Roflumilast:anoveltreatmentforchronicobstructivepulmonarydisease.AnnPharmacother.2012Apr;46(4):521-9.doi:10.1345/aph.1Q646.Epub2012Mar20.Review.PubMedPMID:22433610.

4:PinnerNA,HamiltonLA,HughesA.Roflumilast:aphosphodiesterase-4inhibitorforthetreatmentofseverechronicobstructivepulmonarydisease.ClinTher.2012Jan;34(1):56-66.doi:10.1016/j.clinthera.2011.12.008.Review.PubMedPMID:22284994.

5:LahuG,NassrN,HÃ¼nnemeyerA.Pharmacokineticevaluationofroflumilast.ExpertOpinDrugMetabToxicol.2011Dec;7(12):1577-91.doi:10.1517/17425255.2011.632409.Epub2011Nov8.Review.PubMedPMID:22059647.

6:IzquierdoAlonsoJL.[Phosphodiesterase-4inhibitors:roflumilast].RevClinEsp.2011Mar;211Suppl2:22-30.doi:10.1016/S0014-2565(11)70008-X.Review.Spanish.PubMedPMID:21596170.

7:AntoniuSA.NewtherapeuticoptionsinthemanagementofCOPD-focusonroflumilast.IntJChronObstructPulmonDis.2011;6:147-55.doi:10.2147/COPD.S7336.Epub2011Feb17.Review.PubMedPMID:21468165;PubMedCentralPMCID:PMC3064419.

8:RoflumilastforsevereCOPD?DrugTherBull.2011Apr;49(4):45-8;quiziii-iv.doi:10.1136/dtb.2011.02.0025.Review.PubMedPMID:21467576.

9:IzquierdoAlonsoJL.[Clinicalprofileofroflumilast].ArchBronconeumol.2010Dec;46Suppl10:25-32.doi:10.1016/S0300-2896(10)70053-3.Review.Spanish.PubMedPMID:21316553.

10:CortijoGimenoJ,MorcilloSÃ¡nchezE.[Pharmacologicalprofileofroflumilast].ArchBronconeumol.2010Dec;46Suppl10:19-24.doi:10.1016/S0300-2896(10)70052-1.Review.Spanish.PubMedPMID:21316552.

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MedKoo Biosciences/Roflumilast/300320/250mg

TechnicalData

References