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|---|---|---|---|---|---|---|---|
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                                     {[ getRatePriceInt(item.pr_rmb, 1,1) ]} {[ getRatePriceInt(item.pr_rmb_sale, 1,1) ]} {[ suihuo_tips(item.pr_tag_price, item.pr_am) ]} | 
                                
                                     {[ getRatePriceInt(item.pr_rmb, 1,1) ]} {[ getRatePriceInt(item.pr_rmb,item.pr_rate,1) ]} {[ suihuo_tips(item.pr_tag_price, item.pr_am) ]} | 
                                {[ getRatePriceInt(item.pr_rmb, 1,1) ]}{[ suihuo_tips(item.pr_tag_price, item.pr_am) ]} | {[ getRatePrice(item.pr_rmb_sale, 1,1,item.mem_isinteger) ]} {[ getRatePrice(item.pr_rmb,item.pr_rate,item.mem_rate,item.mem_isinteger) ]} {[ getRatePrice(item.pr_rmb,1,item.mem_rate,item.mem_isinteger) ]} | 现货 | 1周 咨询 | - + | 
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| 产品名称 | Transferase ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Tipifarnib | 
                                                
                                                    +++
                                                    
                                                    
                                                     FTase, IC50: 0.6 nM  | 
                                            
                                        
                                        99%+ | |||||||||||||||||
| Tolcapone | 
                                                
                                                    +
                                                    
                                                    
                                                     COMT, Ki: 30 nM  | 
                                            
                                        
                                        99%+ | |||||||||||||||||
| Lonafarnib | 
                                                
                                                    +++
                                                    
                                                    
                                                     H-ras, IC50: 1.9 nM K-ras-4B, IC50: 2.8 nM  | 
                                            
                                        
                                        99%+ | |||||||||||||||||
| (E)-Daporinad | 
                                                
                                                    ++++
                                                    
                                                    
                                                     NMPRTase, Ki: 0.4 nM  | 
                                            
                                        
                                        99%+ | |||||||||||||||||
| FTI-277 HCl | 
                                                
                                                    ++++
                                                    
                                                    
                                                     FTase, IC50: 500 pM  | 
                                            
                                        
                                        98% | |||||||||||||||||
| A 922500 | 
                                                
                                                    ++
                                                    
                                                    
                                                     mouse DGAT-1, IC50: 24 nM human DGAT-1, IC50: 7 nM  | 
                                            
                                        
                                        98% | |||||||||||||||||
| Lomeguatrib | 
                                                
                                                    ++
                                                    
                                                    
                                                     O6-alkylguanine-DNA-alkyltransferas, IC50: 5 nM  | 
                                            
                                        
                                        99%+ | |||||||||||||||||
| PF-04620110 | 
                                                
                                                    +
                                                    
                                                    
                                                     DGAT1, IC50: 19 nM  | 
                                            
                                        
                                        99% | |||||||||||||||||
| LB42708 | 
                                                
                                                    +++
                                                    
                                                    
                                                     FTase (N-ras), IC50: 1.2 nM FTase (K-Ras), IC50: 0.8 nM  | 
                                            
                                        
                                        98% | |||||||||||||||||
| GGTI298 Trifluoroacetate | ✔ | 98%+ | |||||||||||||||||
| 1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 | |||||||||||||||||||
| 描述 | Ibiglustat is a potent and selective glucosylceramide synthase inhibitor and ceramide glucosyltransferase inhibitor. | 
| Concentration | Treated Time | Description | References | |
| colonoids | 5 μmol/L | 24 hours | Inhibition of glucosylceramide synthase (GCS) activity, reducing glucosylceramide levels, leading to colonoid bursting in the presence of BFT | FASEB J. 2020 Dec;34(12):15922-15945 | 
| HCT116 cells | 0.5 μM | 72 hours | Evaluate the inhibitory effect of Ibiglustat on NTMT1, showing significant reductions in me3-RCC1 and me3-SET levels at 1 μM | J Med Chem. 2022 Sep 22;65(18):12334-12345 | 
| HEK293 cells | 1 μM | 3 days | Evaluate the inhibitory effect of venglustat on me3-RCC1 and me3-SET in HEK293 cells, showing significant inhibition at 1 μM | J Med Chem. 2023 Jan 26;66(2):1601-1615 | 
| Administration | Dosage | Frequency | Description | References | ||
| Mice | GBA-related synucleinopathy model | Oral | 0.03% wt/wt | 8 months | To evaluate the effects of sustained GCS inhibition on disease pathologies, results showed venglustat significantly reduced glycosphingolipid accumulation and improved cognitive deficits. | Sci Rep. 2021 Oct 22;11(1):20945 | 
| Mice | Neurological Gaucher disease model | Oral | 15 mg | Once daily for 1 year | To evaluate the safety and tolerability of venglustat and measure changes in the concentration of glucosylceramide and glucosylsphingosine in CSF. Results showed detectable venglustat in CSF and sustained reductions in glucosylceramide and glucosylsphingosine concentrations in 10 patients. | Brain. 2023 Feb 13;146(2):461-474 | 
| C57BL/6 mice | Normal mice and CBE-induced Gaucher disease type 3 mouse model | Intraperitoneal injection | 10 mg/kg | Once daily for 14 days | Evaluate the effect of compound 17 in reducing brain glucosylceramide and glucosylsphingosine, results showed that at 10 mg/kg dose, compound 17 had comparable effects to venglustat, reducing brain GlcCer and glucosylsphingosine by 19% and 39%, respectively | ACS Chem Neurosci. 2020 Oct 21;11(20):3464-3473 | 
| Mice | GBA11/L444P knock-in mice | Oral | 60 mg/kg body weight/day | Starting 1 week after injections until the day of death | To assess the effect of venglustat on α-synuclein inclusion formation, showing no significant reduction in hippocampal or SNc α-synuclein inclusions. | J Neurosci. 2023 Jan 18;43(3):501-521 | 
| 计算器 | ||||
| 存储液制备 | ![]()  | 
                        1mg | 5mg | 10mg | 
| 
                             1 mM 5 mM 10 mM  | 
                        
                             2.57mL 0.51mL 0.26mL  | 
                        
                             12.84mL 2.57mL 1.28mL  | 
                        
                             25.67mL 5.13mL 2.57mL  | 
                    |
| CAS号 | 1401090-53-6 | 
| 分子式 | C20H24FN3O2S | 
| 分子量 | 389.49 | 
| SMILES Code | O=C(O[C@@H]1CN2CCC1CC2)NC(C)(C3=CSC(C4=CC=C(F)C=C4)=N3)C | 
| MDL No. | MFCD28502073 | 
| 别名 | Venglustat; SAR402671; GZ/SAR402671; Genz-682452; GZ402671 | 
| 运输 | 蓝冰 | 
| InChI Key | YFHRCLAKZBDRHN-MRXNPFEDSA-N | 
| Pubchem ID | 60199242 | 
| 存储条件 | 
                                
                                    
                                             In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Sealed in dry, 2-8°C  | 
                        
| 溶解方案 | 
                                
                                    
                                     DMSO: 50 mg/mL(128.37 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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