 
        
        
        Avoralstat(BCX4161)是一种有效的口服活性血浆激肽酶抑制剂,用于研究遗传性血管性水肿。 Polygalaxanthone III抑制CYP450酶,并通过其IC50为50.56μM的CYP2E1催化的氯索磺酮6-羟基化来抑制。
 
                                 
                                
                            

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| Concentration | Treated Time | Description | References | |
| Calu-3 2B4 cells | 100 nM | 24 h | To test the inhibitory effect of Avoralstat on SARS-CoV-2, results showed that Avoralstat significantly reduced viral RNA signal. | J Clin Invest. 2021 May 17;131(10):e147973 | 
| 293TAT cells | 1.4 μM | 48 h | Evaluate the inhibitory effect of Avoralstat on SARS-CoV-2 infection, results showed IC50 of 1.4 μM | Microbiol Spectr. 2022 Oct 26;10(5):e0333122 | 
| Calu-3 cells | 2.6 μM | 96 h | Evaluate the inhibitory effect of Avoralstat on SARS-CoV-2 infection, results showed IC50 of 2.6 μM | Microbiol Spectr. 2022 Oct 26;10(5):e0333122 | 
| Administration | Dosage | Frequency | Description | References | ||
| BALB/c mice | Ad5-hACE2 transduced BALB/c mice | Intraperitoneal injection | 30 mg/kg | Administered 4 hours before and after infection, then twice daily for 3 days | To test the prophylactic effect of Avoralstat on SARS-CoV-2 infection, results showed that Avoralstat significantly reduced lung tissue titers and mitigated weight loss. | J Clin Invest. 2021 May 17;131(10):e147973 | 
| 计算器 | ||||
| 存储液制备 |  | 1mg | 5mg | 10mg | 
| 1 mM 5 mM 10 mM | 1.95mL 0.39mL 0.19mL | 9.74mL 1.95mL 0.97mL | 19.47mL 3.89mL 1.95mL | |
| CAS号 | 918407-35-9 | 
| 分子式 | C28H27N5O5 | 
| 分子量 | 513.54 | 
| SMILES Code | O=C(O)C1=NC(C(NCC2CC2)=O)=CC=C1C3=CC(OC)=C(C=C)C=C3C(NC4=CC=C(C(N)=N)C=C4)=O | 
| MDL No. | MFCD28502152 | 
| 别名 | BCX4161 | 
| 运输 | 蓝冰 | 
| 存储条件 | In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Keep in dark place, inert atmosphere, store in freezer, under -20°C | 
| 溶解方案 | DMSO: 50 mg/mL(97.36 mM),配合低频超声,并水浴加热至45℃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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