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Medchemexpress/(-)-Blebbistatin(Synonyms: (S)-(-)-Blebbistatin)/HY-13441/5mg
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Medchemexpress/(-)-Blebbistatin(Synonyms: (S)-(-)-Blebbistatin)/HY-13441/5mg
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4000-520-616
(-)-BlebbistatinisanSenantiomerofblebbistatin.BlebbistatinisapotentandselectivemyosinIIinhibitorwithIC50valuesrangingfrom0.5to5μM.
Description

(-)-BlebbistatinisanSenantiomerofblebbistatin.BlebbistatinisapotentandselectivemyosinIIinhibitorwithIC50valuesrangingfrom0.5to5μM.

IC50&Target

IC50:0.5to5μM(myosinII)[1]

InVitro

BlebbistatinpotentlyinhibitsseveralstriatedmusclemyosinsaswellasvertebratenonmusclemyosinIIAandIIBwithIC50valuesrangingfrom0.5to5μM.Smoothmusclemyosinisonlypoorlyinhibited(IC50=80μM)[1].Blebbistatindoesnotcompetewithnucleotidebindingtotheskeletalmusclemyosinsubfragment-1.TheinhibitorpreferentiallybindstotheATPaseintermediatewithADPandphosphateboundattheactivesite,anditslowsdownphosphaterelease.Itblocksthemyosinheadsinaproductscomplexwithlowactinaffinity[2].Inculture-activatedhepaticstellatecells,blebbistatinisfoundtochangebothcellmorphologyandfunction.Stellatecellsbecomesmaller,acquireadendriticmorphologyandhavelessmyosinIIA-containingstressfibresandvinculin-containingfocaladhesions.Blebbistatinimpairssiliconewrinkleformation,reducescollagengelcontractionandblocksendothelin-1-inducedintracellularCa2+release.Itpromoteswound-inducedcellmigration[3].

InVivo

Blebbistatindose-dependentlyandcompletelyrelaxbothKCl-andcarbachol-inducedratdetrusorandendothelin-1-inducedhumanbladdercontraction.Pre-incubationwith10μMblebbistatinattenuatescarbacholresponsivenessby65%whileblockingelectricalfieldstimulation-inducedbladdercontractionreaching50%inhibitionat32Hz[4].

References
  • [1].LimouzeJ,etal.Specificityofblebbistatin,aninhibitorofmyosinII.JMuscleResCellMotil.2004;25(4-5):337-41.

    [2].KovácsM,etal.MechanismofblebbistatininhibitionofmyosinII.JBiolChem.2004Aug20;279(34):35557-63.

    [3].LiuZ,etal.Blebbistatininhibitscontractionandacceleratesmigrationinmousehepaticstellatecells.BrJPharmacol.2010Jan1;159(2):304-15.

    [4].ZhangX,etal.InvitroandinvivorelaxationofurinarybladdersmoothmusclebytheselectivemyosinIIinhibitor,blebbistatin.BJUInt.2011Jan;107(2):310-7.

PreparingStockSolutions
ConcentrationVolumeMass1mg5mg10mg
1mM3.4208mL17.1040mL34.2079mL
5mM0.6842mL3.4208mL6.8416mL
10mM0.3421mL1.7104mL3.4208mL
Pleaserefertothesolubilityinformationtoselecttheappropriatesolvent.
CellAssay
[3]

FreshlyisolatedHSCsarereplatedon96-wellplate.Atday3,mediumisreplacedbyserum-freemediumandcellsarestarvedovernight,treatedwithorwithoutblebbistatin(25μM)for2hfollowedbystimulationwithplatelet-derivedgrowthfactor-BB(20ng/mL).Afteranovernightincubation,theWST-1cellproliferationassayareperformed[3].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

References
  • [1].LimouzeJ,etal.Specificityofblebbistatin,aninhibitorofmyosinII.JMuscleResCellMotil.2004;25(4-5):337-41.

    [2].KovácsM,etal.MechanismofblebbistatininhibitionofmyosinII.JBiolChem.2004Aug20;279(34):35557-63.

    [3].LiuZ,etal.Blebbistatininhibitscontractionandacceleratesmigrationinmousehepaticstellatecells.BrJPharmacol.2010Jan1;159(2):304-15.

    [4].ZhangX,etal.InvitroandinvivorelaxationofurinarybladdersmoothmusclebytheselectivemyosinIIinhibitor,blebbistatin.BJUInt.2011Jan;107(2):310-7.

MolecularWeight

292.33

Formula

C₁₈H₁₆N₂O₂

CASNo.

856925-71-8

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

RoomtemperatureincontinentalUS;mayvaryelsewhere

Solvent&Solubility

DMSO:5.2mg/mL(Needultrasonicandwarming)

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

Purity:99.47%