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商品描述
LyophilizedPowderLyophilizedPowder
Thisproductisfreezedried.Allwatermoleculeshavebeenremoved.
BioassayTestedBioassayTested
Everylotistried&testedinarelevantBIOLOGicalassay.
OurBioassay
SourceSynthetic
MW:343.45
Purity:>98%
Effectiveconcentration1-100nM.
Chemicalname3-(azepan-1-yl)-9-(dimethylamino)pyrido[1,2]thieno[3,4-d]pyrimidin-4-one.
MolecularformulaC17H21N5OS.
CASNo.:869802-58-4.
PubChemCID11559235
ActivityA-841720isapotentandselectivenoncompetitivemGluR1antagoNIST,actingonmGluR1andmGluR5withIC50 valuesof10nMand342nM,respectively1. Invivo itshowsanalgesicproperties,significantlyattenuatingspontaneouspost-operativepainbehaviorinrats(ED50 =10μmol/kg)2.
- Zheng,G.Z. etal.(2005) J.Med.Chem. 48, 7374.
- Zhu,C.Z. etal.(2008) Eur.J.Pharmacol. 580, 314.
ShippingandstorageShippedatroomtemperature.Productassuppliedcanbestoredintactatroomtemperatureforseveralweeks.Forlongerperiods,itshouldbestoredat-20°C.Protectfromlightandmoisture.
SolubilitySolubleinDMSO.Centrifugeallproductpreparationsbeforeuse(10000xg5min).
Storageofsolutions-20°C.
AlomoneLabsA-841720inhibitsmGluR1-mediatedCa2+ mobilizationinU2OScells.Dose-responseof A-841720 (#A-440)normalizedinhibitionofhumanmGluR1-mediated,L-glutamateevokedCa2+ mobilization.Cellswereloadedwithcalcium-sensitivedye,incubatedwitharangeofA-841720concentrations,andstimulatedwith5µML-glutamate(EC80).ChangesinintracellularCa2+ followingstimulationweredetectedaschangesinmaximumrelativefluorescence(RLU)usingFLIPRTETRA™.IC50 wasdeterminedat3.86nM.
References-Scientificbackground
- 1.Zheng,G.Z. etal.(2005) J.Med.Chem. 48, 7374.
- 2.Zhu,C.Z. etal.(2008) Eur.J.Pharmacol. 580, 314.
A-841720isapotent,non-competitiveantagonistofmGluR11,2withanIC50 of10nM1.AthigherconcentrationsitalsoinhibitsmGluR5receptorsdisplayinganIC50valueof342nM1.
Glutamateisthemostabundantexcitatoryneurotransmitterinthecentralnervoussystem.Itmodulatestheactivityofmanytypesofsynapsesbyactivatinginpartmetabotropicglutamatereceptors(mGluRs).mGluRsconsistofthreegroups:I,II,andIIIwithatotalofeightsubtypes,mGluR1tomGluR8.mGluR1playsanimportantroleinthecentralsensitizationofpainandinavarietyoffunctionswithpotentialimplicationsinneurologicalandpsychiatricdisorders1,2.
TargetmGluR1,mGluR5
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Lastupdate:25/09/2019
A-841720(#A-440) isahighlypure,synthetic,andbiologicallyactivecompound.
Forresearchpurposesonly,notforhumanuse
Discovery Antibodies的Cyclin dependant kinase 2 (CDK2) is a serine/threonine protein kinase which controls both G1/S and G2/M transitions. CDKs along with cyclins and CDK inhibitors regulate cell cycle progression. Specific cyclins activate different CDKs; in early G1, CDK2 pairs with cyclin E to promote entry into the S phase before switching to partner with cyclin A to drive the cell through S phase. Once activated CDKs phosphorylate downstream proteins to initiate signalling cascades. CDK2 phosphorylates and inactivates the RB1 (pRb) tumour suppressor family of proteins.CDK的活动受到严格控制。CDK2活性可以被包括P21在内的一系列抑制剂抑制。细胞周期失调和增殖控制的丧失与细胞转化和癌症密切相关。CDK2在DNA损伤反应（DDR）中的细胞周期停滞中也似乎起着积极作用，它的抑制作用会阻碍DDR，并使细胞对电离辐射敏感，从而诱导细胞死亡。该抗体与AlexaFluor®488偶联。AlexaFluor®488是一种流行的鲜绿色荧光染料，具有高pH稳定性。
