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                同义名:
                    
                        
                            达卡他韦
                            
                             / BMS-790052; EBP 883
                            
                        
                    
                
                
                
                    
                     
                    
                     
                
            
Daclatasvir (BMS-790052) 是一种强效和口服活性的 HCV NS5A 蛋白抑制剂,对多种 HCV 复制子基因型的 EC50 值范围为 9 至 146 pM。Daclatasvir 也是有机阴离子转运多肽 1B (OATP1B) 和 1B3 (OATP1B3) 的抑制剂,IC50 值分别为 1.5 μM 和 3.27 μM。
 
                                 
                                
                            

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| 靶点 | 
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| 描述 | Daclatasvir is a first-in-class, highly-selective oral HCV NS5A inhibitor. | 
| Concentration | Treated Time | Description | References | |
| Huh7 cells | 1 nM | 10 days | To evaluate the effect of Daclatasvir on HCV replication and assembly/secretion. Results showed that Daclatasvir treatment led to a decline in intracellular HCV RNA, similar to the polymerase inhibitor NM107, but extracellular HCV titers declined more rapidly, indicating its inhibitory effect on viral assembly/secretion. | Proc Natl Acad Sci U S A. 2013 Mar 5;110(10):3991-6. | 
| primary RDEB dermal fibroblasts | 1 μM | 48 h | To evaluate the effect of Daclatasvir on TGF-β signaling pathway, results showed that Daclatasvir inhibited the expression of TGF-β pathway targets collagen I, phosphorylated AKT, and phosphorylated SMAD3. | EMBO Mol Med. 2024 Apr;16(4):870-884. | 
| Administration | Dosage | Frequency | Description | References | ||
| Humanized-liver mice | HBV/HCV co-infection model | Oral | 30 mg/kg | Once a day for 4 weeks | To evaluate the effect of DAA treatment on HBV replication in HBV/HCV-co-infected mice. Results showed that HCV was eliminated after DAA treatment, and HBV replication was upregulated. | Sci Rep. 2020 Jan 22;10(1):941 | 
| Alb-uPA/Scid mice | HCV genotype 1b or 3 infection model | Oral | 10 mg/kg | Once daily for 4 weeks | Evaluate the inhibitory effect and drug resistance of Daclatasvir monotherapy on HCV | Nat Microbiol. 2020 Dec;5(12):1532-1541. | 
| Human hepatocyte chimeric TK-NOG mice | HCV infection model | Oral | 30 mg/kg | Once daily for 4 weeks | To assess the origin of HCV NS5A L31V-Y93H double substitutions after treatment failure with daclatasvir and asunaprevir combination therapy | Sci Rep. 2017 Jan 30;7:41660 | 
| Mice | RDEB mouse model | Oral (via drinking water) | 30 mg/kg | From conception to weaning (28 days) | To evaluate the effect of Daclatasvir on fibrosis and quality of life in RDEB mice, results showed that Daclatasvir significantly improved survival, increased weight and activity, and reduced pruritus-induced hair loss. Additionally, the expression of fibrosis markers phospho-SMAD3 and collagen I was reduced in the skin. | EMBO Mol Med. 2024 Apr;16(4):870-884. | 
| NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 | 
| NCT02095860 | Hepatitis C | Phase 1 | Completed | - | United States, Texas ... 展开 >> Healthcare Discoveries, Llc D/B/A Icon Development Solutions San Antonio, Texas, United States, 78209 收起 << | 
| NCT02531269 | - | Completed | - | Switzerland ... 展开 >> Local Institution Basel, Switzerland 收起 << | |
| NCT03186313 | Hepatitis C | Phase 3 | Completed | - | Egypt ... 展开 >> Egyptian Liver Hospital Shirbīn, Dakahlia, Egypt, 35681 收起 << | 
| 计算器 | ||||
| 存储液制备 |  | 1mg | 5mg | 10mg | 
| 1 mM 5 mM 10 mM | 1.35mL 0.27mL 0.14mL | 6.77mL 1.35mL 0.68mL | 13.53mL 2.71mL 1.35mL | |
| CAS号 | 1009119-64-5 | 
| 分子式 | C40H50N8O6 | 
| 分子量 | 738.88 | 
| SMILES Code | O=C([C@@H](NC(OC)=O)C(C)C)N1CCC[C@H]1C2=NC=C(N2)C3=CC=C(C=C3)C4=CC=C(C5=CN=C([C@@H]6CCCN6C([C@@H](NC(OC)=O)C(C)C)=O)N5)C=C4 | 
| MDL No. | MFCD17129086 | 
| 别名 | 达卡他韦 ;BMS-790052; EBP 883 | 
| 运输 | 蓝冰 | 
| InChI Key | OVPGYLMBPQNZNE-GJVQWJCYSA-N | 
| Pubchem ID | 66575053 | 
| 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: 40 mg/mL(54.14 mM),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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