中文名称嘌呤胺中文同义词9-环己基-N-[4-(4-吗啉基)苯基]-2-(1-萘氧基)-9H-嘌呤-6-胺(PURMORPHAMINE);9-环己基-N-[4-(4-吗啉基)苯基]-2-(1-萘氧基)-9H-嘌呤-6-胺;嘌呤胺;9-环己基-N-(4-吗啉苯基)-2-(萘-1-氧基)-9H-嘌呤-6-胺;化合物PURMORPHAMINE;嘌吗啡胺;PURMORPHAMINE,平滑受体激动剂;PURMORPHAMINE化学试剂英文名称Purmorphamine英文同义词2-(1-NAPHTHOXY)-6-(4-MORPHOLINOANILINO)-9-CYCLOHEXYLPURINE;PURMORPHAMINE;9-Cyclohexyl-N-[(4-morpholinyl)phenyl]-2-(1-naphthalenyloxy)-9H-purin-6-amine;9-Cyclohexyl-N-[4-(Morpholin-4-yl)phenyl]-2-(naphthalen-1-yloxy)-9H-purin-6-aMine;9-Cyclohexyl-N-[4-(4-Morpholinyl)phenyl]-2-(1-naphthalenyloxy)-;9-Cyclohexyl-N-[4-(4-morpholinyl)phenyl]-2-(1-naphthalenyloxy)-9H-purin-6-amine;9H-Purin-6-amine,9-cyclohexyl-N-[4-(4-morpholinyl)phenyl]-2-(1-naphthalenyloxy)-;9-Cyclohexyl-N-[4-(4-morpholinyl)phenyl]-2-(1-naphthalenyloxy)-9H-purin-6-aminePurmorphamineCAS号483367-10-8分子式C31H32N6O2分子量520.62EINECS号200-256-5相关类别原料药标样;干细胞与Wnt信号;小分子抑制剂,天然产物;小分子抑制剂;试剂;Inhibitors;Bases&RelatedReagents;Heterocycles;Intermediates&FineChemicals;Nucleotides;Pharmaceuticals;Lipidsignaling;HeterocyclicCompoundsMol文件483367-10-8.mol结构式嘌呤胺性质熔点210-212°C沸点790.3±70.0°C(Predicted)密度1.35±0.1g/cm3(PrChemicalbookedicted)储存条件-20°C溶解度DMSO:可溶5mg/mL,澄清(加热)酸度系数(pKa)5.44±0.40(Predicted)形态粉末颜色白色至米色稳定性可在-20°C的DMSO中的溶液下储存长达3个月。InChIKeyFYBHCRQFSFYWPY-UHFFFAOYSA-N嘌呤胺用途与合成方法生物活性Purmorphamine与Smo拮抗剂竞争性结合到Smoothened,并激活Smoothened,IC50约为1.5μM,也诱导成骨细胞分化,EC50为1μM。体外研究Purmorphamine与Cyclopamine(一种Smo拮抗剂)竞争,直接结合和激活Smoothened,而激活Hedgehog通路,IC50为1.5μM。Purmorphamine作用于全能C3H10T1/2细胞,是有效的骨生成诱导剂。Purmorphamine作用于C3H10T1/2细胞的EC50(根据ALP表达)为1μM。Purmorphamine(1μM)和BMP-4(100ng/mL)联用,作用于3T3-L1细胞,使ALP活性增强90多倍。与BMP-4相比,Purmorphamine作用于多能间充质祖细胞,诱导骨生成,通过激活Hedgehog信号。体内研究Purmorphamine作用于基于大鼠结构的人间充质干细胞,上调ALP表达。生物活性Purmorphamine(ShhSignalingAntagonistVI)直接结合并激活Smoothened,阻断BODIPY-cyclopamine与Smo结合,在HEK293T细胞中IC50约为1.5μM,也诱导成骨细胞分化,EC50为1μM。Purmorphamine可减少基础和诱导的自噬。靶点TargetValueSmoothened(HEK293Tcells)~1.5μM体外研究Purmorphamine与Cyclopamine(一种Smo拮抗剂)竞争,直接结合和激活Smoothened,而激活Hedgehog通路,IC50为1.5μM。Purmorphamine作用于全能C3H10T1/2细胞,是有效的骨生成诱导剂。Purmorphamine作用于C3H10T1/2细胞的EC50(根据ALP表达)为1μM。Purmorphamine(1μM)和BMP-4(100ng/mL)联用,作用于3T3-L1细胞,使ALP活性增强90多倍。与BMP-4相比,Purmorphamine作用于多能间充质祖细胞,诱导骨生成,通过激活Hedgehog信号。体内研究Purmorphamine作用于基于大鼠结构的人间充质干细胞,上调ALP表达。 |