Lys-Des-Arg9-Bradykinin-TFA-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?Agonists?ScreeningLibrariesLys-[Des-Arg9]BradykininTFACat.No.:HY-103295A分?式:C??H??F?N??O??分?量:1146.22SequenceKRPPGFSPFShortening:作?靶點(diǎn):BradykininReceptor作?通路:GPCR/GProtein儲存?式:ProtectfromlightPowder-80°C2years-20°C1year*Insolvent:-80°C,6months;-20°C,1month(protectfromlight)溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:110mg/mL(95.97mM;Needultrasonic)H2O:50mg/mL(43.62mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM0.8724mL4.3622mL8.7243mL5mM0.1745mL0.8724mL1.7449mL10mM0.0872mL0.4362mL0.8724mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存?式和期限。體內(nèi)實(shí)驗(yàn)請根據(jù)您的實(shí)驗(yàn)動物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：為保證實(shí)驗(yàn)結(jié)果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)天使?；以下溶劑前顯?的百分?指該溶劑在您配制終溶液中的體積占?；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的?式助溶1.請依序添加每種溶劑：10%DMSO40%PEG3005%Tween-8045%salineSolubility:≥2.75mg/mL(2.40mM);Clearsolution此?案可獲得≥2.75mg/mL(2.40mM，飽和度未知)的澄溶液。以1mL?作液為例，取100μL27.5mg/mL的澄DMSO儲備液加到400μLPEG300中，混合均勻；向上述體系中加?50μLTween-80，混合均勻；然后繼續(xù)加?450μL?理鹽?定容?1mL。1/32.請依序添加每種溶劑：10%DMSO90%(20%SBE-β-CDinsaline)Solubility:≥2.75mg/mL(2.40mM);Clearsolution此?案可獲得≥2.75mg/mL(2.40mM，飽和度未知)的澄溶液。以1mL?作液為例，取100μL27.5mg/mL的澄DMSO儲備液加到900μL20%的SBE-β-CD?理鹽??溶3.液中，混合均勻。請依序添加每種溶劑：10%DMSO90%cornoilSolubility:≥2.75mg/mL(2.40mM);Clearsolution此?案可獲得≥2.75mg/mL(2.40mM，飽和度未知)的澄溶液，此?案不適?于實(shí)驗(yàn)周期在半個?以上的實(shí)驗(yàn)。以1mL?作液為例，取100μL27.5mg/mL的澄DMSO儲備液加到900μL??油中，混合均勻。BIOLOGICALACTIVITY?物活性Lys-[Des-Arg9]BradykininTFA?種天然存在的激肽，?種有效且?度選擇性的緩激肽B1受體激動劑，對?，??和兔?的B1受體的Ki值為0.12nM，1.7nM和0.23nM。Lys-[Des-Arg9]BradykininTFA對B2受體的抑制活性較低。體外研究Lys-[Des-Arg9]Bradykininisformedbytheproteolyticcleavageofbradykinin,exertsitseffectsthroughbradykininB1receptor(B1R)[1].Lys-[Des-Arg9]Bradykinin(Lda-BK;10μM)enhancesthesecretionofIL-12p70andinhibitsthesecretionofIL-12p40bymaturehMo-DCs.PretreatmentwithLys-[Des-Arg9]BradykinintreatmentreducesthemigrationofmaturehMo-DCstowardmediumalone,suggestingthatLys-[Des-Arg9]BradykininmayinhibitthechemokinesisofmaturehMo-DCs[1].體內(nèi)研究Lys-[Des-Arg9]Bradykinin(1μg;intra-artenalinjection;NewZealandWhiterabbits)treatmentreducesperipheralvascularresistanceinLPS-inducedrabbits,buttheeffectisbrief(T1/2is118-195s)[3].REFERENCES[1].RosalindGulliver,etal.Lys-des[Arg9]-bradykininaltersmigrationandproductionofinterleukin-12inmonocyte-deriveddendriticcells.AmJRespirCellMolBiol.2011Sep;45(3):542-9.[2].LMFredrikLeeb-Lundberg,etal.Internationalunionofpharmacology.XLV.Classificationofthekininreceptorfamily:frommolecularmechanismstopathophysiologicalconsequences.PharmacolRev.2005Mar;57(1):27-77.[3].GDrapeau,etal.HypotensiveeffectsofLys-des-Arg9-bradykininandmetabolicallyprotectedagonistsofB1receptorsforkinins.JPharmacolExpTher.1991Dec;259(3):997-1003.McePdfHeight2/3