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                同义名:
                    
                        
                            
                                Shh Signaling Antagonist VI
                            
                        
                    
                
                
                
                    
                     
                    
                     
                
            
Purmorphamine是一种Smo (smoothened/Smo receptor) 激动剂,EC50 为 1 μM。
 
                                 
                                
                            

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| 描述 | Purmorphamine acts as a smoothened/Smo receptor agonist with an EC50 of 1 μM[1]. | 
| 体外研究 | Purmorphamine (10, 20 μM) in conjunction with sirolimus significantly reduces cell numbers according to the MTT assay. Purmorphamine induces up-regulation of alkaline phosphatase activity and expression of RUNX-2 on day 14. Up-regulation of osteocalcin is detected at the 3 and 5 μM doses of purmorphamine on day 14 post-induction. However, matrix mineralization remains unchanged in the presence or absence of purmorphamine[1]. Purmorphamine induces phosphorylation of STAT3 in the mouse ES cell line ES14 and the mesenchymal stem cell line C3H10T1/2[2]. Purmorphamine enhances the expression of osteoblast phenotype markers - ALP activity and bone-like nodule formation - in human bone marrow mesenchymal cells[3]. Purmorphamine (GMP), at a concentration of 1.5 μM for a duration of 1 week, can generate embryoid bodies (EBs) from human iPS cells (hiPS2) and hESCs (HSF1)[1]. Purmorphamine (GMP) at a concentration of 1.5 μM converts hPSCs to NKX2-1 positive MGE cells[2]. During days 28-35, Purmorphamine (GMP) at a concentration of 2 μM promotes ventralization of brain spheroids during the differentiation process from hiPSCs[3]. Purmorphamine (GMP), at a concentration of 1 μM, in combination with retinoic acid (RA, 2 μM) facilitates hiPSC differentiation into functional neural tissue, as indicated by the expression of the neuronal marker β-tubulin III (βT-III)[4]. Between days 5 and 7, Purmorphamine (GMP) induces differentiation of hESCs into dopaminergic (DA) neurons[5]. | 
| 细胞系 | 浓度 | 检测类型 | 检测时间 | 活性说明 | 数据源 | 
| HEK293T cells | 5 μM | Function assay | 4 h | Inhibition of BODIPY-cyclopamine binding to Smo C-terminal cytoplasmic domain expressed in HEK293T cells at 5 uM after 4 hrs by fluorescence microscopy | 16408088 | 
| mouse C3H10T1/2 cells | Function assay | Induction of osteogenesis in mouse C3H10T1/2 cells assessed as induction of osteoblast specific marker alkaline phosphatase by immunofluorescence method, EC50=1 μM | 16408003 | ||
| mouse Shh Light2 cells | Function assay | 30 h | Activation of Shh in mouse Shh Light2 cells after 30 hrs by luciferase reporter gene assay, EC50=1 μM | 16408088 | 
| Dose | Rat: 0.5 mg/kg - 5 mg/kg[3] (i.p.) | 
| Administration | i.p. | 
| 计算器 | ||||
| 存储液制备 |  | 1mg | 5mg | 10mg | 
| 1 mM 5 mM 10 mM | 1.92mL 0.38mL 0.19mL | 9.60mL 1.92mL 0.96mL | 19.21mL 3.84mL 1.92mL | |
| CAS号 | 483367-10-8 | 
| 分子式 | C31H32N6O2 | 
| 分子量 | 520.62 | 
| SMILES Code | N1(C2CCCCC2)C=NC3=C(NC4=CC=C(N5CCOCC5)C=C4)N=C(OC6=C7C=CC=CC7=CC=C6)N=C13 | 
| MDL No. | MFCD09037557 | 
| 别名 | Shh Signaling Antagonist VI | 
| 运输 | 蓝冰 | 
| InChI Key | FYBHCRQFSFYWPY-UHFFFAOYSA-N | 
| Pubchem ID | 5284329 | 
| 存储条件 | In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Keep in dark place, sealed in dry, store in freezer, under -20°C | 
| 溶解方案 | DMSO: 35 mg/mL(67.23 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶 
 
 
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