PioglitazonehydrochlorideisapotentandselectivePPARγagonistwithhighaffinitybindingtothePPARγligand-bindingdomainwithEC₅₀of0.93and0.99μMforhumanandmousePPARγ,respectively.

EC50:0.93μM(humanPPARγ),0.99μM(mousePPARγ)^[1]

AGEs-inducedbetacellnecrosisiscompletelyabrogatedbyaddingPioglitazonetotheAGEsculturemedium.FurThermorePioglitazonecompletelypreventedanyAGEs-inducedincrementincaspase-3activation,therebyrestoringcaspase-3activitytothesamelevelsasthecontrolcells.AsexpectedAGisabletocounteractAGEs-inducedimpairedviABIlity^[2].

Theserum-freefattyacidandtriglyceridelevelsaswellasADIpocytesizesinob/obandadipo^-/-ob/obmiceareunchangedafter10mg/kgPioglitazonebutaresignificantlyreducedtoasimilardegreeafter30mg/kgPioglitazone.Moreover,theexpressionsofTNFαandresistininadiposetissuesofob/obandadipo^-/-ob/obmiceareunchangedafter10mg/kgPioglitazonebutaredecreasedafter30mg/kgPioglitazone.Thus,Pioglitazone-inducedameliorationofinsulinresistanceanddiabetesmayoccuradiponectindependentlyintheliverandadiponectinindependentlyinskeletalmuscle^[3].Pioglitazone(10mg/kgperd)treatmentsignificantlyattenuatesthelossofbodyweight(BW)andcardiachypertrophy.Pioglitazonetreatmentsignificantlyreducestheelevatedserumglucoselevelsandmarkedlyimprovedtheassociateddyslipidemia.Furthermore,thereisaslightbutsignificantincreaseinserumcreatininelevelinDratsovertheirNcontrols(P<0.05). however,="" a="" marked="" renal="" dysfunction="" is="" observed="" in="" diabetic="" nephropathic="" (dn)="" group=""><0.05). moreover,="" dn="" rats="" exhibits="" the="" highest="" serum="" activity="" of="" ck-mb,="" relative="" to="" both="" n="" and="" d="" rats=""><0.05). pioglitazone="" is="" able="" to="" decrease="" the="" elevated="" serum="" levels="" of="" both="" creatinine="" and="" creatine="" kinase-mb="">^[4].

• [1].KuwabaraK,etal.Anovelselectiveperoxisomeproliferator-activatedreceptoralphaagonist,2-methyl-c-5-[4-[5-methyl-2-(4-methylphenyl)-4-oxazolyl]butyl]-1,3-dioxane-r-2-carboxylicacid(NS-220),potentlydecreasesplasmatriglycerideandglucoseleve

  [2].PudduA,etal.Pioglitazoneattenuatesthedetrimentaleffectsofadvancedglycationend-productsinthepancreaticbetacelllineHIT-T15.RegulPept.2012Aug20;177(1-3):79-84.

  [3].KubotaN,etal.Pioglitazoneamelioratesinsulinresistanceanddiabetesbybothadiponectin-dependentand-independentpathways.JBiolChem.2006Mar31;281(13):8748-55.

  [4].ElrashidyRA,etal.Pioglitazoneattenuatescardiacfibrosisandhypertrophyinaratmodelofdiabeticnephropathy.JCardiovascPharmacolTher.2012Sep;17(3):324-33.

Inordertoevaluatecellproliferation,HIT-T15cellsareseededon96-wellplates(3×10⁴cells/well)andculturedfor5daysasdescribed.ViablecellsaredeterminedusingtheCellTiter96AqueousOneSolutionCellProliferationAssay.Toevaluatecellapoptosisandcellnecrosis,HIT-T15cellsareplatedon6-welldishes(7×10⁵cells/well)for5daysinstandardconditions(CTR)orinthepresenceofAGEs(AGEs)withorwithoutPioglitazone(0.5or1μM)orAG(1mM).Theyarethenprocessedtomeasureboththeactivityofcaspase-3andtheactivityoflactatedehydrogenase(LDH)(astablecytosolicenzymethatisaMarkerofcellmembranedamageandcelldeathduetonecrosis)usingCytotox96NonRadioactiveCytotoxicityAssay^[2].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

Pioglitazone(AD4833)hydrochlorideispreparedin0.25%carboxymethylcellulose(Mice)^[3].
PioglitazonehydrochlorideissUSPendedin0.5%carboxymethylcellulose(Rat)^[4].

Mice^[3]
10mg/kgPioglitazoneHClorvehicle(0.25%carboxymethylcellulose)isadnimisteredtoob/obandadipo^-/-ob/obmicebyoralgavageoncedailyfor14consecutivedays.30mg/kgPioglitazoneorvehicleisalsoadnimisteredtoob/obandadipo^-/-ob/obmicebyoralgavageoncedailyfor14consecutivedays.
Rat^[4]
MaleWistaralbinorats(weighing250±20g)areued.Ratsthatachievedserumglucoselevel≥250mg/dLandserumcreatininelevel≥1.5mg/dLaredividedinto2groups(n=10pereachgroup):diabeticnephropathic(DN)groupinwhichratsreceivedanequalamountofvehicle(0.5%carboxymethylcellulose)andPioglitazone-treated(DN+Pio)groupinwhichratstreatedwithPioglitazone.Pioglitazone(10mg/kgBW)isgivenorallybygastricgavage,oncedaily,for4weeks.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

• [1].KuwabaraK,etal.Anovelselectiveperoxisomeproliferator-activatedreceptoralphaagonist,2-methyl-c-5-[4-[5-methyl-2-(4-methylphenyl)-4-oxazolyl]butyl]-1,3-dioxane-r-2-carboxylicacid(NS-220),potentlydecreasesplasmatriglycerideandglucoseleve

  [2].PudduA,etal.Pioglitazoneattenuatesthedetrimentaleffectsofadvancedglycationend-productsinthepancreaticbetacelllineHIT-T15.RegulPept.2012Aug20;177(1-3):79-84.

  [3].KubotaN,etal.Pioglitazoneamelioratesinsulinresistanceanddiabetesbybothadiponectin-dependentand-independentpathways.JBiolChem.2006Mar31;281(13):8748-55.

  [4].ElrashidyRA,etal.Pioglitazoneattenuatescardiacfibrosisandhypertrophyinaratmodelofdiabeticnephropathy.JCardiovascPharmacolTher.2012Sep;17(3):324-33.

392.9

C₁₉H₂₁ClN₂O₃S

112529-15-4

RoomtemperatureincontinentalUS;mayvaryelsewhere

10mMinDMSO

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

Purity:99.53%

SelectBatch:HY-14601-10107

DataSheet(133KB)SDS(388KB)

COA(93KB)HNMR(359KB)LCMS(296KB)

HandlingInstructions(1252KB)

• [1].KuwabaraK,etal.Anovelselectiveperoxisomeproliferator-activatedreceptoralphaagonist,2-methyl-c-5-[4-[5-methyl-2-(4-methylphenyl)-4-oxazolyl]butyl]-1,3-dioxane-r-2-carboxylicacid(NS-220),potentlydecreasesplasmatriglycerideandglucoseleve

  [2].PudduA,etal.Pioglitazoneattenuatesthedetrimentaleffectsofadvancedglycationend-productsinthepancreaticbetacelllineHIT-T15.RegulPept.2012Aug20;177(1-3):79-84.

  [3].KubotaN,etal.Pioglitazoneamelioratesinsulinresistanceanddiabetesbybothadiponectin-dependentand-independentpathways.JBiolChem.2006Mar31;281(13):8748-55.

  [4].ElrashidyRA,etal.Pioglitazoneattenuatescardiacfibrosisandhypertrophyinaratmodelofdiabeticnephropathy.JCardiovascPharmacolTher.2012Sep;17(3):324-33.

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

公司介绍

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-

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