Biological Activity
Selective Na+/Ca2+-exchange (NCX) inhibitor; displays some selectivity for NCX1. IC50 values are 2.9, 16 and 8.6 μM for inhibition of intracellular Na+-dependent 45Ca2+ uptake by cells expressing NCX1, NCX2 and NCX3 respectively. Has some affinity for mACh receptors (IC50 = 18 μM) but minimal activity against NCKX2 and various receptors and ion channels (IC50 > 30 μM). Preferentially blocks Ca2+ influx mode and is more selective for NCX isoforms than KB-R7943 (Cat. No. 1244). Anti-ischemic; potently protects against hypoxia-induced renal tubular cell damage (IC50 = 0.63 μM).
Compound Libraries
SN-6 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 402.16 |
| Formula | C20H22N2O5S |
| Storage | Desiccate at +4°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 415697-08-4 |
| PubChem ID | 10222761 |
| InChI Key | ZVYIJXLMBWCGHP-UHFFFAOYSA-N |
| Smiles | CCOC(=O)C1CSC(CC2=CC=C(OCC3=CC=C(C=C3)[N+]([O-])=O)C=C2)N1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 40.22 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 402.16. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.49 mL | 12.43 mL | 24.87 mL |
| 5 mM | 0.5 mL | 2.49 mL | 4.97 mL |
| 10 mM | 0.25 mL | 1.24 mL | 2.49 mL |
| 50 mM | 0.05 mL | 0.25 mL | 0.5 mL |
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References
References are publications that support the products' biological activity.
Iwamoto et al (2004) The exchanger inhibitory peptide region-dependent inhibition of Na+/Ca2+ exchange by SN-6 [2-[4-(4-nitrobenzyloxy)benzyl]thiazolidine-4-carboxylic acid ethyl ester], a novel benzyloxyphenyl derivative. Mol.Pharmacol. 66 45 PMID: 15213295
Iwamoto (2004) Forefront of Na+/Ca2+ exchanger studies: molecular pharmacology of N+/Ca2+ exchange inhibitors. J.Pharmacol.Sci. 96 27 PMID: 15359084
Keywords: SN-6, supplier, Selective, Na+/Ca2+, exchange, inhibitors, inhibits, reverse, mode, Sodium, Calcium, Exchanger, Ion, Transporters, Pumps, Ca2+, Signaling, Signalling, NCX1, Na+/Ca2+, Exchanger, Na+/Ca2+, Exchanger, Tocris Bioscience
TocrisBioscience是一家专卖生命科学研究chemicals,peptidesandantibodies的知名品牌，其产品也广为各大药厂、大学、研究机构，超过五万名科学研究者所采用。目前，產品內容已超過一千六百種以上，並每年持續不斷的增加新的產品。目前，产品内容已超过一千六百种以上，并每年持续不断的增加新的产品。 Tocrisbioscience是位于英国布里斯托尔（Bristol）的高品质试剂提供商，共有2000多种产品，主要集中在神经科学和信号传导领域，产品类型包括小分子、多肽、抗体、配体和化合物筛选文库等，主要产品包括GPCRligands，神经传递素，离子通道调控剂，信号通路抑制剂等，这些产品被广泛选择性地用于阻断或激活生物学通路。Tocris是世界上神经科学研究领域无可争议的领导者，其生产的影响神经系统的化学物质被多次引用，这些物质很多都来自JeffWatkins（Tocris的创立人）在Bristol大学原创性的研究工作。 TocrisBioscience的主要产品包括：SmallMoleculesPeptidesAptamersControlledSubstancesCompoundLibrariesDREADDLigandsFluorescentImagingLigandSetsOptopharmacologyReagentsToxins 按照研究领域细分：CancerCardiovascularSystemEndocrinologyImmunologyNeurosciencePain&InflammationRespiratorySystem
关于Tocris高品质生命科学试剂的领先供应商超过三十年来，TocrisBioscience一直与科学家携手合作，致力于为生命科学研究提供最尖端和最具创新性的研究工具。我们了解，对于研究人员，试剂的可靠性是至关重要的，从这一点出发，我们为客户提供最高品质的产品，让您在发表研究成果时倍感自信。要了解关于Tocris的更多信息，请点击下方的图块。Tocris是Bio-Techne的分支机构，专精于生命科学领域，旗下包含多个著名品牌，如 R&DSystems、NovusBIOLOGicals、ProteinSimple 和 AdvancedCellDiagnostics。Bio-Techne汇聚众多品牌的力量，为研究人员提供全方位的产品，包括研究试剂、定量分析和蛋白质分析平台。要了解关于Bio-Techne及其旗下品牌的更多信息，请访问 bio-techne.com。Tocris职业发展环境保护活动和会议授权我们的理念我们的历史Tocris新闻
TocrisBioscience主要产品分类 1、小分子在生物科学中，小分子作为研究材料具有许多优点，它们可设计成是选择性的、有效的、水溶性的或细胞可渗透的。应用作为激动剂和GPCR的拮抗剂，以及酶抑制剂，核受体配体和离子通道调节剂。许多常用药物是小分子，不像肽和蛋白质，它们可被设计为代谢稳定和口服活性。2、肽肽是由酰胺键连接的α-氨基酸形成的链。肽通常由20种天然存在氨基酸与非天然氨基酸组成。3、对照底物对照底物包含药物或化合物，来自于英国药物生产商的前沿技术。4、毒素毒素是由活细胞或组织产生的有毒物质。5、复合笼利用光解技术，使邻近的受体配体释放，防止扩撒效应。6、光控开关配体光控开关配体是光敏感的化合物，不同波长的光应于神经元的离子通道和受体的调节，能控制神经信号的强度。7、荧光探针结合到受体或蛋白质的荧光探针使研究人员能够检测的复杂生物分子的组件，如活细胞，具有高灵敏度和选择性。Tocris也提供荧光染料、标签等。8、筛选文库9、其他试剂
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转运体是介导分子或离子转运跨过生物膜的物质。通常是蛋白质或酶。说得简单一点就是“运输工具”
受体是能与细胞外专一信号分子（配体）结合引起细胞反应的蛋白质。受体与配体结合即发生分子构象变化，从而引起细胞反应，如介导细胞间信号转导、细胞间黏合、细胞胞吞等细胞过程。它起的是“传达员” 的作用
硝酸根从根向地上部茎的长距离运输过程中首先要进行木质部的装载。台湾科学家发现NRT1.5是一个低亲和且依赖于pH的双向转运蛋白，位于质膜并在靠近木质部的中柱鞘细胞中表达，对于硝酸根在木质部的装载具有重要作用。
所以NRT1.5是双向性的转运蛋白
QianWang,JessamyTiffen,CharlesG.Bailey,MelanieL.Lehman,WilliamRitchie,LadanFazli,CynthiaMetierre,Yue(Julie)Feng,EstelleLi,MartinGleave,GrantBuchanan,ColleenC.Nelson,JohnE.J.Rasko,JeffHolst
Correspondenceto:JeffHolst,PhD,OriginsofCancerLaboratory,LockedBag6,Newtown,NSW2042Australia.(e-mail:j.holst@centenary.org.au).
BackgroundL-typeaminoacidtransporters(LATs)uptakeneutralaminoacidsincludingL-leucineintocells,stimulatingmammaliantargetofrapamycincomplex1signalingandproteinsynthesis.LAT1andLAT3areoverexpressedatdifferentstagesofprostatecancer,andtheyareresponsIBLeforincreasingnutrientsandstimulatingcellgrowth.
MethodsWeexaminedLAT3proteinexpressioninhumanprostatecancertissuemicroarrays.LATfunctionwasinhibitedusingaleucineanalog(BCH)inandrogen-dependentand-independentenvironments,withgeneexpressionanalyzedbymicroarray.APC-3xenograftmousemodelwasusedtostudytheeffectsofinhibitingLAT1andLAT3expression.ResultswereanalyzedwiththeMann-WhitneyUorFisherexacttests.Allstatisticaltestsweretwo-sided.
ResultsLAT3proteinwasexpressedatallstagesofprostatecancer,withastatisticallysignificantdecreaseinexpressionafter4–7monthsofneoadjuvanthormonetherapy(4–7monthmean=1.571;95%confidenceinterval=1.155to1.987vs0month=2.098;95%confidenceinterval=1.962to2.235;P=.0187).InhibitionofLATfunctionledtoactivatingtranscriptionfactor4–mediatedupregulationofaminoacidtransportersincludingASCT1,ASCT2,and4F2hc,allofwhichwerealsoregulatedviatheandrogenreceptor.LATinhibitionsuppressedM-phasecellcyclegenesregulatedbyE2Ffamilytranscriptionfactorsincludingcriticalcastration-resistantprostatecancerregulatorygenesUBE2C,CDC20,andCDK1.InsilicoanalysisofBCH-downregulatedgenesshowedthat90.9%arestatisticallysignificantlyupregulatedinmetastaticcastration-resistantprostatecancer.Finally,LAT1orLAT3knockdowninxenograftsinhibitedtumorgrowth,cellcycleprogression,andspontaneousmetastasisinvivo.
ConclusionInhibitionofLATtransportersmayprovideanoveltherapeutictargetinmetastaticcastration-resistantprostatecancer,viasuppressionofmammaliantargetofrapamycincomplex1activityandM-phasecellcyclegenes.
L-typeaminoacidtransporters(LATs)supplycellswithlargeneutralaminoacids,whicharenotonlyrequiredforproteinsynthesisbutalsocontributetovarioussignalingpathways.Intracellularleucinelevelsaresensedbytheleucyl-transferRNAsynthetase,previouslyknowntocatalyzetheadenosinetriphosphate–dependentligationofL-leucinetotransferRNAduringproteinsynthesis(1,2).Leucyl-transferRNAsynthetaseactivatestheRagguanosinetriphosphatasecomplexandbindstoRaptortoactivatemammaliantargetofrapamycincomplex1(mTORC1)signalingonthesurfaceoflysosomes(1–3).Inthiswayleucineisnotonlyanessentialaminoacidbutactsasarate-limitingsignalingmoleculeinthemTORC1pathway.
Incellsdeprivedofaminoacids,thereisanaccumulationofunchargedtransferRNA,whichbindstoandactivatesthegeneralcontrolnonrepressed2(GCN2)kinase.Inturn,GCN2phosphorylatesthetranslationinitiationfactor2α(eIF2α)onserine51,triggeringtranslationalupregulationofactivatingtranscriptionfactor(ATF)4(4).ATF4itselfupregulatestheexpressionofaminoacidtransportersasameansofrestoringintracellularaminoacidlevels(5).Therefore,understandinghowaminoacidtransportersregulateintracellularleucinelevels,andgeneratingnovelinhibitorsofthesetransporters,mayleadtopotentsuppressorsofmTORC1signaling.
ThetwodistinctfamiliesofLATsare1)solutecarrier7(SLC7)members(LAT1/SLC7A5andLAT2/SLC7A8),whichmediateNa+-independentneutralaminoacidexchangeasheterodimerswiththe4F2cell-surfaceantigenheavychain(4F2hc/SLC3A2/CD98)glycoprotein(6,7);and2)SLC43proteins(LAT3/SLC43A1andLAT4/SLC43A2)thatmediateNa+-independentuniportofneutralaminoacids(8,9).AlthoughtheexpressionofeachLATmembervariesdramaticallyindifferenttissues,thesetransportersarecommonlyupregulatedincancer.IncreasedLAT1expressionhasbeendetectedinlungcancer,coloncancer,breastcancer,headandneckcancer,genitalcancers,andsofttissuesarcomas(10–12).WeandothershaveshownthatLAT1andLAT3areoverexpressedinprostatecancer(11–14),withLAT1expressionincreasedinmetastasiscomparedwithprimarycancer(10,12).
WehypothesizedthatinhibitionofLAT1andLAT3mayofferaneffectivetherapeuticapproachforprostatecancer.
感觉这样的提问是没有意义的
还是自己找下资料吧
微生物吸收营养和排出废弃物都需要通过细胞膜。而细胞膜是磷脂双分子层结构，无论是亲水物质还是疏水物质都无法通过细胞膜。
细胞膜上镶嵌有蛋白质，叫转运蛋白。蛋白质既有疏水基团，又有亲水基团，正是靠蛋白质的这种特殊结构，能够与两类物质结合，并通过蛋白质结构的细微变化，把这两类物质运送到细胞膜的另一侧。
所以，微生物吸收营养物质必须用镶嵌在细胞膜上的转运蛋白来实现。
