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当前位置： 首页 > 产品中心 > Small_molecule > Medchemexpress/Pasireotide二氟乙酸（同义词：SOM230二氟乙酸；帕西罗梯TFA盐）/HY-79135/5mg
商品详细Medchemexpress/Pasireotide二氟乙酸（同义词：SOM230二氟乙酸；帕西罗梯TFA盐）/HY-79135/5mg
Medchemexpress/Pasireotide二氟乙酸（同义词：SOM230二氟乙酸；帕西罗梯TFA盐）/HY-79135/5mg
Medchemexpress/Pasireotide二氟乙酸（同义词：SOM230二氟乙酸；帕西罗梯TFA盐）/HY-79135/5mg
商品编号： HY-79135-10mM*1mLinDMSO
品牌： MedChemExp
市场价： ¥30860.00
美元价： 18516.00
产地： 美国(厂家直采)
公司：
产品分类： 小分子
公司分类： Small_molecule
联系Q Q： 3392242852
电话号码： 4000-520-616
电子邮箱： info@ebiomall.com
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商品介绍
Pasireotide(ditrifluoroacetate)isastablecyclohexapeptidesomatostatinmimicthatexhibitsuniquehigh-affinitybindingtohumansomatostatinreceptors(subtypessst1/2/3/4/5,pKi=8.2/9.0/9.1/<7.0/9.9, respectively).
Description

Pasireotide(ditrifluoroacetate)isastablecyclohexapeptidesomatostatinmimicthatexhibitsuniquehigh-affinitybindingtohumansomatostatinreceptors(subtypessst1/2/3/4/5,pKi=8.2/9.0/9.1/<7.0 .9,="" respectively).="">

IC50&Target

pKi:8.2(sst1),9.0(sst2),9.1(sst3),<7.0 (sst4),="" 9.9="">

InVitro

Pasireotideeffectivelyinhibitsthegrowthhormonereleasinghormone(GHRH)inducedgrowthhormone(GH)releaseinprimaryculturesofratpituitarycellswithanIC50 of0.4±0.1nM[1].

InVivo

PasireotidepotentlysuppressessGHsecretioninrats.TheED50 valuesdeterminedat1and6hafterinjectionof pasireotideindicatesitsverylongdurationofactioninvivo.Intherat, pasireotide stronglydecreasesIGF-1plasmalevels,withtheefficacybeingmarkedlyenhancedcomparedwiththeeffectselicitedby SMS201-995 after7daysoftreatment.FurThermore,inrats,dogs,andrhesusmonkeys,pasireotidepotentlyanddose-dependentlydecreasesIGF-1levelsforprolongedperiodsoftimewithoutdesensitization[1].Pasireotide(160mg/kg/month,s.c.)decreasesseruminsulinlevelsandincreasesserumglucoselevels,reducesPNETtumorsize,anddemonstratesareductionintumoractivityonPET/CTscaninPdx1-Cre;Men1floxed/floxedconditionalknockoutmice[2].Pasireotide(50μg/kg)inhibitsarthriticjointswellinginadose-dependentmanner,stronglyinhibitsjointswellingduringtheacutephaseofAIA.Pasireotide-andoctreotide-treatedmiceshowsignificantlyincreasedmechanicalthresholdsontheinflamedside.Pasireotidepotentlydecreasessecondaryhyperalgesiatomechanicalandthermalstimuli.Mechanicalthresholdsinthepasireotide-treatedmicearesignificantlyhigherthanthoseinthesaline-treatedoroctreotide-treatedanimals[3].

ClinicalTrial
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References

  • [1].LewisI,etal.Anovelsomatostatinmimicwithbroadsomatotropinreleaseinhibitoryfactorreceptorbindingandsuperiortherapeuticpotential.JMedChem.2003Jun5;46(12):2334-44.

    [2].QuinnTJ,etal.Pasireotide(SOM230)iseffectiveforthetreatmentofpancreaticneuroendocrinetumors(PNETs)inamultipleendocrineneoplasiatype1(MEN1)conditionalknockoutmousemodel.Surgery.2012Dec;152(6):1068-77.

    [3].ImhofAK,etal.Differentialantiinflammatoryandantinociceptiveeffectsofthesomatostatinanalogsoctreotideandpasireotideinamousemodelofimmune-mediatedarthritis.ArthritisRheum.2011Aug;63(8):2352-62.

PreparingStockSolutions
ConcentrationVolumeMass1mg5mg10mg
1mM0.7842mL3.9208mL7.8416mL
5mM0.1568mL0.7842mL1.5683mL
10mM0.0784mL0.3921mL0.7842mL
Pleaserefertothesolubilityinformationtoselecttheappropriatesolvent.
AnimalAdmiNISTration
[1]

Pasireotideisformulatedinsaline.

Miceareanesthetizedusinghalothaneandthenshavedontheirflankforsubcutaneousinjectionofeitherphosphatebufferedsaline(PBS)bufferorPasireotideataconcentrationof160mg/Kg/month(64mg/mL)everymonthfor4months.Themiceunderwenta24-hfastpriortocollectingwholebloodviaaretro-orbitalbleedingtechniqueweeklyatpre-andpost-treatments.SerumglucoseismeasuredbyenzymaticcolorimetricassayusingaGM7Analyzer.Seruminsulinismeasuredbyenzyme-linkedimmunosorbentassay(ELISA)withtheUltrasensitiveMouseInsulinELISAkitaccordingtothemanufacturer’sinstructions.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

References

  • [1].LewisI,etal.Anovelsomatostatinmimicwithbroadsomatotropinreleaseinhibitoryfactorreceptorbindingandsuperiortherapeuticpotential.JMedChem.2003Jun5;46(12):2334-44.

    [2].QuinnTJ,etal.Pasireotide(SOM230)iseffectiveforthetreatmentofpancreaticneuroendocrinetumors(PNETs)inamultipleendocrineneoplasiatype1(MEN1)conditionalknockoutmousemodel.Surgery.2012Dec;152(6):1068-77.

    [3].ImhofAK,etal.Differentialantiinflammatoryandantinociceptiveeffectsofthesomatostatinanalogsoctreotideandpasireotideinamousemodelofimmune-mediatedarthritis.ArthritisRheum.2011Aug;63(8):2352-62.

MolecularWeight

1275.25

Formula

C₆₂H₆₈F₆N₁₀O₁₃

Storage
Powder-20°C3years
 4°C2years
Insolvent-80°C6months
 -20°C1month
Shipping

RoomtemperatureincontinentalUS;mayvaryelsewhere

Solvent&Solubility

10mMinDMSO

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

Purity:99.51%