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Medchemexpress/Octreotide acetate(Synonyms: SMS 201995)/HY-17365/10mg
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Medchemexpress/Octreotide acetate(Synonyms: SMS 201995)/HY-17365/10mg
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Octreotide(acetate)isalong-actingoctapeptideandsomatostatinanalogwithpharmacologicactionsmimickingthoseofthenaturalhormonesomatostatin.
Description

Octreotide(acetate)isalong-actingoctapeptideandsomatostatinanalogwithpharmacologicactionsmimickingthoseofthenaturalhormonesomatostatin.

InVivo

Octreotide-treatedgroupsshowasignificantreductioninthetumorvolumewhencomparedwithsalinegroup.Octreotide-PPSG(1.4mg/kg,i.p.)showsgreaterantitumoreffectthanOctreotide-soln(100μg/kg,i.p.).Octreotide-treatmentsresultsinsignificantinhibitoryeffectontheexpressionlevelsofSSTR2andSSTR5inprimaryHCC-bearingratscomparedwiththesalinegroup.Octreotide-PPSGappearstoinhibittheexpressionofSSTR2andSSTR5toagreaterextentthanthatofOctreotide-solntreatedgroup[1].Atestdoseofoctreotideacetatesignificantlydecreasestheserumgastrinleveltoapproximatelyonethirdofthebaselinein2hrandtheeffectlastedapproximatelyfor6hr.Onday21,treatmentwithsustained-releaseformulationofoctreotideacetatea(5mgintramuscular,q4wk)isinitiated[2].

References
  • [1].WangM,etal.Pharmacokineticandpharmacodynamicstudyofaphospholipid-basedphaseseparationgelforonceamonthadmiNISTrationofoctreotide.JControlRelease.2016May28;230:45-56.

    [2].KimS,etal.TreatmentofGastrin-SecretingTumorWithSustained-ReleaseOctreotideAcetateinaDog.JAmAnimHospAssoc.2015Nov-Dec;51(6):407-12.

PreparingStockSolutions
ConcentrationVolumeMass1mg5mg10mg
1mM0.9265mL4.6327mL9.2654mL
5mM0.1853mL0.9265mL1.8531mL
10mM0.0927mL0.4633mL0.9265mL
Pleaserefertothesolubilityinformationtoselecttheappropriatesolvent.
AnimalAdministration
[1]

Octreotide(acetate)isformulatedinsaline.

Mice[1]
ThirtymicewithHCCxenograftsarerandomLydividedintothreegroups:(A)Octreotide-solngroup,(B)Octreotide-PPSGgroup,and(C)controlgroup.Octreotide-solngroupreceivesi.p.injectionof100μg/kgoctreotide-solnonceadayandtotallyforconsecutive14days.Octreotide-PPSGgroupreceivesasinglesubcutaneousinjectionof1.4mg/kgOctreotide-PPSG,andtheinjectionvolumeisabout0.2mL.Controlgroupreceivesi.p.injectionofsalineonceadayforconsecutive14days.TreatmentstartsonthenextdayafterinjectionofH22hepatomacellsUSPensionandmaintainsfor14days.Tumorgrowthismonitoredbyperiodiccalipermeasurementsonday7andday14postseeding.Tumorvolumes(V)arecalculatedbasedonthelengthandwidthoftumorbyEq.
Rat[1]
TwelvemaleSDratsaredividedintotwogroups,andhousedinstandardcagesat25°C,withfreeaccesstofoodandwaterforaweekpriortotheexperiment.RatsaresubcutaneouslyinjectedwithOctreotidereotidesolution(Octreotide-soln)orOctreotide-PPSGatanequivalentsingledoseof20 mg/kg.ThedoseisdeterminedbasedontheclinicaldoseofOctreotide-solninhuman.Ratsarefastedfor12 hbeforedosingandfoodisreturnedapproximately2 hpostdosing.BloodsamplesarecollectedatpredeterminedtimepointsusingheparinizedEppendorftubes.Immediatelyaftercollection,thebloodsamplesareplacedoniceuntilcentrifugedat3000 g for10 minwithin1 h.Theplasmaiscollectedandstoredat−20°Cuntilanalysis.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

References
  • [1].WangM,etal.Pharmacokineticandpharmacodynamicstudyofaphospholipid-basedphaseseparationgelforonceamonthadministrationofoctreotide.JControlRelease.2016May28;230:45-56.

    [2].KimS,etal.TreatmentofGastrin-SecretingTumorWithSustained-ReleaseOctreotideAcetateinaDog.JAmAnimHospAssoc.2015Nov-Dec;51(6):407-12.

MolecularWeight

1079.29

Formula

C₅₁H₇₀N₁₀O₁₂S₂

CASNo.

79517-01-4

Storage
Powder-80°C2years
 -20°C1year
Insolvent-80°C6months
 -20°C1month
Shipping

RoomtemperatureincontinentalUS;mayvaryelsewhere

Solvent&Solubility

DMSO:≥29mg/mL

*"<1 mg/ml"="" means="" slightly="" soluble="" or="" insoluble.="" "≥"="" means="" soluble,="" but="" saturation="">

Purity:99.78%