生物缓冲液

CAS号：26305-03-3

品名：胃酶抑素APepstatinA

中文别名：抑肽素;胃蛋白酶抑制剂;

英文别名：pepsininhibitors735a;peptistatinA;PEPSTATINASYNTHETIC;Isovalerylpepstatin;procidins735a;PepstainA;PEPSTATIN;pepstatineA;ahpatininc;IVA-VAL-VAL-STA-ALA-STA;

分子式：C34H63N5O9

分子量：685.892

精确质量：685.463

Psa：223.26

RTECS号：SC6155000

BRN号：2201362

EINECS号：247-600-0

MDL号：MFCD00060740

PubChem号：24898620

外观与性状：固体

密度：1.117 g/cm3

沸点：997.6ºC at 760 mmHg

熔点：233°C (dec.)(lit.)

闪点：557.1ºC

折射率：1.504

稳定性：Stable. Incompatible with strong bases, strong acids.

储存条件：2-8ºC

蒸汽压：0mmHg at 25°C

安全说明：S22-S24/25

WGK Germany：2

简介：Pepstatinisapotentinhibitorofaspartylproteases.Itisahexa-peptidecontainingtheunusualaminoacidstatine(Sta,(3S,4S)-4-amino-3-hydroxy-6-methylheptanoicacid),havingthesequenceIsovaleryl-Val-Val-Sta-Ala-Sta(Iva-Val-Val-Sta-Ala-Sta).ItwasoriginallyisolatedfromculturesofvariousspeciesofActinomycesduetoitsabilitytoinhibitpepsinatpicomolarconcentrations.PepstatinAiswellknowntobeaninhibitorofasparticproteinasessuchaspepsin,cathepsinsDandE.Exceptforitsroleasaproteinaseinhibitor,however,thepharmacologicalactionofpepstatinAuponcellsremainunclear.PepstatinAsuppressesreceptoractivatorofNF-κBligand(RANKL)–inducedosteoclastdifferentiation.PepstatinAsuppressestheformationofmultinuclearosteoclastsdose-dependently.Thisinhibitionoftheformationonlyaffectedosteoclastcells,i.e.,notosteoblast-likecells.Furthermore,pepstatinAalsosuppressesdifferentiationfrompre-osteoclastcellstomononuclearosteoclastcellsdose-dependently.ThisinhibitionseemstobeindependentoftheactivitiesofproteinasessuchascathepsinD,becausetheformationofosteoclastswasnotsuppressedwiththeconcentrationthatinhibitedtheactivityofcathepsinD.CellsignalinganalysisindicatedthatthephosphorylationofERKwasinhibitedinpepstatinA-treatedcells,whilethephosphorylationofIκBandAktshowedalmostnochange.Furthermore,pepstatinAdecreasedtheexpressionofnuclearfactorofactivatedTcellsc1(NFATc1).TheseresultssuggestthatpepstatinAsuppressesthedifferentiationofosteoclaststhroughtheblockadeofERKsignalingandtheinhibitionofNFATc1expression.