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3-異丁基-1-甲基黃嘌呤 |
CAS No.: |
28822-58-4 |
分子式: |
C10H14N4O2 |
分子量: |
222.24 |
備注: |
中文名稱3-異丁基-1-甲基黃嘌呤中文同義詞3-異丁基-1-甲基-2,6(1H,3H)-嘌呤二酮;3-異丁基-1-甲基黃嘌呤(IBMX),99%;3-ISOBUTYL-1-METHYLXANTHINE3-異丁基-1-甲基黃嘌呤IBMX;3-異丁基-1-甲基黃嘌呤(IBMX、1-甲基-3-異丁基黃嘌呤、3,7-二氫-3-異丁基-1-甲基-1H-嘌呤-2,6-二酮);3-異丁基-1-甲基-1H-嘌呤-2,6(3H,9H)-二酮;3-異丁基-1-甲基-3,9-二氫-1H-嘌呤-2,6-二酮;IBMX、1-甲基-3-異丁基黃嘌呤;3-異丁基-1-甲基黃嘌呤(IBMX)英文名稱3-ISOBUTYL-1-METHYLXANTHINE英文同義詞1H-Purine-2,6-dione,3,7-dihydro-1-methyl-3-(2-methylpropyl)-;3,7-dihydro-1-methyl-3-(2-methylpropyl)-1h-purine-6-dione;3-Isobutyl-1-methyl-3,7-dihydro-1H-purine-2,6-dione;3-Isobutyl-1-methylanxthine;3-isobutyl-1-methyl-xanthin;IMX;Isobutylmethylxanthine;MethylisobutylxanthineCAS號28822-58-4分子式C10H14N4O2分子量222.24EINECS號249-259-3相關(guān)類別生化試劑;小分子抑制劑;嘌呤;有機(jī)砌塊;其他生化試劑;雜環(huán)砌塊;其他化學(xué)試劑;科研試劑;標(biāo)準(zhǔn)品;其它;原料;Inhibitors;AllInhibitors;Intermediates&FineChemicals;PharmaceuticalsMol文件28822-58-4.mol結(jié)構(gòu)式3-異丁基-1-甲基黃嘌呤性質(zhì)熔點(diǎn)200-201°C(lit.)沸點(diǎn)363.42°C(roughestimate)密度1.2042(roughestimate)折射率1.6500(estimate)儲存條件-20°C溶解度DMSO:1M,慢慢升溫酸度系數(shù)(pKa)8.61±0.70(Predicted)形態(tài)粉末顏色米白色BRN247859穩(wěn)定性可在-20°C下的DMSO或乙醇溶液保存長達(dá)3個月。InChIKeyAPIXJSLKIYYUKG-UHFFFAOYSA-NCAS數(shù)據(jù)庫28822-58-4(CASDataBaseReference)3-異丁基-1-甲基黃嘌呤用途與合成方法生物活性IBMX(Isobutylmethylxanthine,1-Methyl-3-Isobutylxanthine)是一種非特異性phosphodiesterase(PDE)抑制劑,對PDE3、PDE4、PDE5的IC50值分別為6.5±1.2,26.3±3.9和31.7±5.3μM。它能增強(qiáng)細(xì)胞內(nèi)cAMP水平,是adenosine(A1)receptor拮抗劑。靶點(diǎn)TargetValuePDE3()6.5μMPDE4()26.3μMPDE5()31.7μM體外研究At100μM,KMUP-1(axanthinederivative)andIBMXarethemosteffectiveatinducingtrachealrelaxation;themagnitudeoftherelaxationresponsesinducedbyKMUP-1andIBMXareChemicalbooknotsignificantlydifferent.IBMX(100μM)activatesrenaloutermedullaryK+(ROMK)channels(n=6,P<0.05)andpreventsfurtherchannelactivationbyANGII(n=6,P=NS)orcGMP.Ofnoteisthatpretreatmentofcorticalcollectingduct(CCDs)isolatedfromhigh-K+(HK)-fedratswithIBMX(100μM)for20minleadstoasignificantincreaseintubularcAMPcontentto1.43±0.35pg/mmtubulelength(n=14)comparewiththatmeasuredinvehicle-treatedcontrols(0.61±0.13pg/mmtubulelength,n=12,P<0.05).體內(nèi)研究IBMX,anon-selectivePDEinhibitorsignificantlydecreasestheliverglycogenstorage(mg/g,IBMX22±1.5P<0.001).Incomparisonwiththecontrolgroup,IBMXandmc5significantlyincreaseplasmaglucose(bloodglucose,mg/dl,control=141±3,IBMX=210±17P<0.001andmc5=191±13P<0.01)whileothertestcompounds(mc1,mc6,MCPIPandWin47203)donotproducesignificanteffect(control=141±3,mc1160±7,mc6175±9,MCPIP179±8andWin47203116±2P>0.05)alsomc2doesnotchangeplasmaglucose(control=141±3andmc2=145±5).IBMXhasthehighestefficacyonincreasingplasmaglucose.TreatmentswithIBMXandApocyninsignificantlydecreasecold-inducedelevationofrightventricular(RV)systolicpressure(23.5±1.8and24.2±0.6mmHg,respectively)althoughtheydonotdecreaseRVpressuretothewarmcontrollevels.IBMXorApocyninsignificantlyreducesmediallayerthickness(19.0±0.9,and16.9±0.8μm,respectively)andincreaseslumendiameter(62.7±4.2,and59.5±4.3μm,respectively)ofsmallPAsincold-exposedrats.用途環(huán)核苷酸磷酸二酯酶蛋白抑制劑。用途cAMP和cGMP磷酸二脂酶的非專一性抑制劑。IBMX抑制了磷酸二脂酶,cAMP的增加激活了PKA,其結(jié)果是減少增殖,增加分化和誘發(fā)凋亡.IBMX抑制由苯腎上腺素誘導(dǎo)的色胺(來自于神經(jīng)內(nèi)分泌上皮細(xì)胞的減少粘液IC50:1.3μM)的減少。也作為腺苷受體拮抗劑。 |
結(jié)構(gòu)式: |
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聯(lián)系人: |
金經(jīng)理 |
地 址: |
湖北省武漢市東湖新技術(shù)開發(fā)區(qū)光谷大道03號 |
郵 編: |
430000 |
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18995560451 |
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15102708508 |
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18995560451 |
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