8-Bromo-cGMP-sodium-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemE8-Bromo-cGMPsodiumCat.No.:HY-101379ACASNo.:51116-01-9分⼦式:C₁₀H₁₀BrN₅NaO₇P分⼦量:446.08作⽤靶点:CalciumChannel作⽤通路:MembraneTransporter/IonChannel;NeuronalSignaling储存⽅式:-20°C,sealedstorage,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoisture)溶解性数据体外实验H2O:100mg/mL(224.18mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.2418mL11.2088mL22.4175mL5mM0.4484mL2.2418mL4.4835mL10mM0.2242mL1.1209mL2.2418mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month(sealedstorage,awayfrommoisture)。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。体内实验请根据您的实验动物和给药⽅式选择适当的溶解⽅案。以下溶解⽅案都请先按照InVitro⽅式配制澄的储备液，再依次添加助溶剂：(为保证实验结果的可靠性，澄的储备液可以根据储存条件，适当保存；体内实验的⼯作液，建议您现⽤现配，当天使⽤；以下溶剂前显⽰的百分⽐指该溶剂在您配制终溶液中的体积占⽐；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的⽅式助溶)1.请依序添加每种溶剂：PBSSolubility:100mg/mL(224.18mM);Clearsolution;Needultrasonic1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEBIOLOGICALACTIVITY⽣物活性8-Bromo-cGMPsodiumcGMP的膜渗透性类似物，⼀种PKG激活剂。8-Bromo-cGMPsodium可显抑制Ca2+宏观电流并损害⾼K+刺激的胰岛素释放。8-Bromo-cGMPsodium具有缓解疼痛和⾎管舒张作⽤。体外研究8-Bromo-cGMPsodium(1-100μM;8h)increasesresistanceofLLC-PK1cellstoCsAtoxicityconcentration-dependently[3].8-Bromo-cGMPsodium(1-100μM;16h)inducesthesynthesisofHO-1proteininaconcentration-dependentfashion[3].CellViabilityAssay[3]CellLine:LLC-PK1cells(ATCCCL101)Concentration:1-100μMIncubationTime:8hoursResult:IncreasedresistanceofLLC-PK1cellstoCyclosporinA(CsA)toxicityconcentration-dependentlyandaugmentedcellviabilitybyupto65%.WesternBlotAnalysis[3]CellLine:LLC-PK1cells(ATCCCL101)Concentration:1-100μMIncubationTime:16hoursResult:InducedthesynthesisofHO-1proteininaconcentration-dependentfashion.体内研究8-Bromo-cGMPsodium(0.3,1,3.0nmol;intrathecaladministration;10minbeforetest)dose-dependentlyandsignificantlyincreasesthetail-flicklatencyinVincristine-treatedmicetothelevelobservedinvehicle-treatednaivemice(maleICRmice,4weeksofageandweighing20g).Vincristine(0.05mg/kg1dayafterthepre-drugtail-flicklatency,andthen0.125mg/kgtwiceaweekfor6weeks)caninducepainfulneuropathyinmice[4].8-Bromo-cGMPsodium(10mg/kg;iv;singledose)resultsinvasodilatorresponsesineNOS-TgmiceandWTlittermatesinC57BL/6background(19-35g)[5].REFERENCES[1].SarkarO,etal.NitricoxideattenuatesoverexpressionofGiαproteinsinvascularsmoothmusclecellsfromSHR:RoleofROSandROS-mediatedsignaling.PLoSOne.2017Jul10;12(7):e0179301.[2].TegederI,etal.Dualeffectsofspinallydelivered8-bromo-cyclicguanosinemono-phosphate(8-bromo-cGMP)informalin-inducednociceptioninrats.NeurosciLett.2002Oct31;332(2):146-50.[3].TobiasPolte,etal.Atrialnatriureticpeptidereducescyclosporintoxicityinrenalcells:roleofcGMPandhemeoxygenase-1.FreeRadicBiolMed.2002Jan1;32(1):56-63.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE[4].JunzoKamei,etal.Possibleinvolvementofthespinalnitricoxide/cGMPpathwayinvincristine-inducedpainfulneuropathyinmice.Pain.2005Sep;117(1-2):112-20.[5].ElzaDvanDeel,etal.Vasomotorcontrolinmiceoverexpressinghumanendothelialnitricoxidesynthase.AmJPhysiolHeartCircPhysiol.2007Aug;293(2):H1144-53.McePdfHeightCaution:Producthasnot