CustomerValidation
- •SciRep.2017Jun28;7(1):4351.
- •AmJPathol.2015Jan;185(1):185-96.
Description | GW-1100isaselectiveGPR40antagonistwithapIC50of6.9.GW1100actsasaGPR40inverseagonist. |
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IC50&Target | pIC50:6.9(GPR40)[1] |
InVitro | GW-1100(GW1100)dosedependentlyinhibitsGPR40-mediatedCa2+elevationsstimulatedbyGW9508andlinoleicacid(pIC50valuesof5.99±0.03and5.99±0.06,respectively).GW-1100ataconcentrationof1μMproducesasignificantrightwardshiftintheconcentration-responsecurvetoGW9508(pEC50=7.17±0.08intheabsenceandpEC50=6.79±0.09inthepresenceof1μMGW-1100;P<0.05; n="3)." at="" concentrations="" of="" gw-1100="" of="" 3="" μm="" and="" higher="" a="" significant="" decrease="" in="" the="" maximal="" response="" is="" observed="" with="" a="" continuing="" rightward="" shift="" in="" the="">0.05;>50response[2].GW-1100(GW1100)reducesFFAR1ligand-inducedintracellularcalciuminCHO-K1/bFFAR1cellsandneutrophils.CHO-K1/bFFAR1cellsareincubatedfor15minwith10μMGW1100orvehicle(0.1%DMSO)andthenstimulatedwithvehicle,oleicacid,linoleicacidorGW9508.GW-1100significantlyreducestheincreaseinintracellularcalciuminducedby300μMoleicacid(AUC(60-150s),p<0.05), 100="" μm="" linoleic="" acid="">0.05),>(60-150s),p<0.05) and="" 10="" μm="" gw9508="">0.05)>(60-150s),p<>[3]. |
InVivo | TheintracerebroventricularinjectionofDHA(50µg)andGW9508(1.0µg),aGPR40-selectiveagonist,significantlyreducesmechanicalallodyniaandthermalhyperalgesiaatday7,butnotatday1,afterCFAinjection.TheseeffectsareinhibitedbyintracerebroventricularpretreatmentwithGW-1100(10µg),aGPR40antagonist[4]. |
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Pleaserefertothesolubilityinformationtoselecttheappropriatesolvent. | ||||||||||||||||
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CellAssay [3] | GW-1100(GW1100)ispreparedinDMSOandstored,andthendilutedwithappropriatemedium(DMSO0.1%)beforeuse[3]. CHO-K1/bFFAR1orCHO-K1/pCDNA3.1cells(2×106cells/2mL)areloadedwith2.5μMFura-2AMfluorescentindicatordyeinrecordingbuffer(10mMHEPES,140mMNaCl,2mMCaCl2,21mMMgCl2,25mMKCl,10mMglucose,pH7.4)for30min,washedthreetimeswithrecordingbuffer,andreturnedtotheincubatorfor10min.Cellsareincubatedwithdifferentconcentrationsofpropionicacid(1,10and30mM),oleicacid(0-500μM),linoleicacid(0-200μM),GW9508(0-100μM),ionomycin(2μM),thapsigargin(2μM)orvehicle(0.1%DMSO).Thefattyacidconcentrationsusedinallexperimentsareintherangeofconcentrationsofhealthyandperipartumcows.Inanothersetofexperiments,cellsareincubatedwitheither10μMGW-1100for15min,2μMU73122for3minorvehicle(0.1%DMSO)for15minandthenstimulatedwitheither300μMoleicacid,100μMlinoleicacidor10μMGW9508.Cellularfluorescence(Ca2+)ismeasuredat509nmemissionwith340/380nmdualwavelengthexcitationusingaLS55spectrofluorimeter.Cuvettetemperaturesaremaintainedat37°Cwithconstantstirring[3].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly. | ||||||||||||||||
AnimalAdministration [4] | GW-1100(GW1100)ispreparedinDMSOanddilutedwithsalineorPBS[4]. Mice[4] | ||||||||||||||||
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MolecularWeight | 520.58 | ||||||||||||
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Formula | C₂₇H₂₅FN₄O₄S | ||||||||||||
CASNo. | 306974-70-9 | ||||||||||||
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Shipping | RoomtemperatureincontinentalUS;mayvaryelsewhere | ||||||||||||
Solvent&Solubility | 10mMinDMSO *"<1 mg/ml"="" means="" slightly="" soluble="" or="" insoluble.="" "≥"="" means="" soluble,="" but="" saturation="">1> Purity:95.13% 品牌介绍
托烷司琼临床评价药物相关作用适应症托烷司琼CAS号:89565-68-4英文名称:Tropisetron英文同义词:icf205-930;TROPICACID;TROPISETRON;SS-TROPISETRON;BETA-TROPISETRON;Tropisetron(ICS205930);TROPISHTRONHYDROCHLORIDE;Indole-3-carbonylchloride;3-Tropanylindole-3-carboxylate;lαH,5Αh-Tropan-3α-ylindole-3-carboxylate中文名称:托烷司琼中文同义词:托普西隆;托普西龙;曲匹西龙;托烷司琼;Β-托烷司琼;CS-348;Β-内托烷司琼;吲哚-3-甲酰氯;Β-托烷司琼(光学异构体);Β-托烷司琼,托烷司琼异构体CBNumber:CB3236404分子式:C17H20N2O2分子量:284.35MOLFile:89565-68-4.mol化学性质安全信息用途供应商112化学性质安全信息用途供应商112托烷司琼化学性质熔点:201-202°C沸点:448.5±35.0°C(Predicted)密度:1.26储存条件:2-8°C溶解度:H2O:soluble形态:solid酸度系数(pKa):15.38±0.30(Predicted)颜色:whiteCAS数据库:Chemicalbook89565-68-4(CASDataBaseReference)安全信息WGKGermany:3托烷司琼化学药品说明书托烷司琼|药物应用信息托烷司琼性质、用途与生产工艺临床评价Sorbe等报道本品对含顺铂(剂量50~89mg/m2)化疗方案引起的急性呕吐完全控制率为63%。58例恶性肿瘤化疗所致恶心、呕吐者,应用托烷司琼或昂丹司琼8mg分别在同一病人前后2个化疗周期的第1d给药前30min静脉注射,并用地塞米松10mg静脉滴注。结果两药控制急性及迟发性恶心、呕吐的疗效基本相似,均可达81%~100%。本品对强致吐化疗药物顺铂的止吐疗效突出。药物相关作用饮食可略为延长本品的吸收。本品与利福平、苯巴比妥等肝酶诱导药同时使用,可加快代谢,故快代谢型者需增加剂量,慢者则不必。西咪替丁等肝酶抑制药对本品血药浓度无明显影响。适应症托烷司琼临床用于预防和治疗癌症化疗引起的恶心和呕吐。化学性质结晶,熔点201-202℃(二氯甲烷-乙酸乙酯)。单盐酸托烷司琼(TropisetronMonohydroehloride):C17H20N2O2?HCI。[105826-92-4]。熔点283-285℃(分解)。用途有高效性和选择性的5-HT3受体拮抗剂。用于化疗所致的呕吐。用途为5-羟色胺拮抗药生产方法托品醇(I)和酰氯(Ⅱ)反应,可得托烷司琼。托烷司琼上下游产品信息上游原料托品醇下游产品
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