1. Anti-infection
  2. SARS-CoV Virus Protease
  3. ALG-097558

ALG-097558 是一种具有口服活性的 3CL 蛋白酶抑制剂。ALG-097558 对多种 SARS-CoV-2 变体以及其他人类冠状病毒 (如 SARS-CoV-1、α-HCoV 229E 和 β-HCoV OC43) 表现出泛冠状病毒活性。ALG-097558 表现出强大的抑制活性,对 SARS-CoV-2 3CL 蛋白酶的 IC50 为 2 nM,对 229E 3CL 蛋白酶 的 IC50 为 6 nM。ALG-097558 在 SARS-CoV-2 仓鼠感染模型中显示出抗病毒活性。ALG-097558 可用于病毒感染的研究。

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ALG-097558 Chemical Structure

ALG-097558 Chemical Structure

CAS No. : 2892287-29-3

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

ALG-097558 is an orally active 3CLpro inhibitor. ALG-097558 demonstrates pan-coronavirus activity against various SARS-CoV-2 variants as well as other human coronaviruses (HCoVs) such as SARS-CoV-1, α-HCoV 229E, and β-HCoV OC43. ALG-097558 demonstrates potent inhibition with IC50s of 2 nM (SARS-CoV-2 3CLpro) and 6 nM (229E 3CLpro). ALG-097558 demonstrates antiviral activity in the SARS-CoV-2 hamster infection model. ALG-097558 can be used for the study of viral infections[1].

体外研究
(In Vitro)

ALG-097558 (Compound 7) 表现出强大的抑制活性,对 SARS-CoV-2 3CL 蛋白酶的 IC50 为 2 nM,对 229E 3CL 蛋白酶 的 IC50 为 6 nM[1]
ALG-097558 通过强烈抑制人类 β-CoV OC43 (EC50 = 8 nM) 、SARS-CoV-1 (EC50 = 22 nM) 和 B.1.1.7 AS49D (EC50 = 11 nM),显示出强大的泛冠状病毒抗病毒活性[1]
ALG-097558可抑制 β 型中东呼吸综合征冠状病毒 β MERS-CoV (IC50 = 59 nM)、OC43hCoV OC43 (IC50 = 0.6 nM)、α CoV 229E (IC50 = 2.8 nM) 和 γ Beluga whale CoV (IC50 = 1 nM) 的 3CL 蛋白酶活性[1]
ALG-097558 (0-1 μM, 4 days) 在气液界面培养的原代人支气管上皮细胞 (HAEC) 中抑制 SARS-CoV-2 B.1.1.7 的复制[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Real Time qPCR[1]

Cell Line: Primary human bronchial airway epithelial cells
Concentration: 0-1 μM
Incubation Time: 4 days
Result: Inhibited SARS-CoV-2 replication with mean EC90, EC99, and EC99.9 values of 24, 36, and 43 nM respectively.
体内研究
(In Vivo)

ALG-097558 (Compound 7) (2.5-150 mg/kg,口服,每日两次,连续 3 天) 与 Ritonavir (HY-90001) 共同给药时,在 SARS-CoV-2 仓鼠感染模型中显示出抗病毒活性[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: SARS-CoV-2 infected hamsters[1]
Dosage: 25, 50, 100, 150 mg/kg with Ritonavir (50 mg/kg) prophylactically (just before infection) or 2.5, 25, and 75 mg/kg with Ritonavir at 8 and 24 h postinfection (pi)
Administration: p.o. twice a day for 3 days
Result: Reduced lung infectious viral titer by more than four log10 TCID50/mg lung tissue when using a prophylactic dosing regimen.
Reduced the infectious virus loads in the lungs below or near the lower limit of quantification (10 TCID50mg lung tissue) in most animals when administered therapeutically starting from 8 h pi.
Reduced the infectious virus at doses of 25 and 75 mg/kg BID when administered therapeutically starting from 24 h pi.
分子量

540.00

Formula

C25H32ClF2N5O4

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
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  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
ALG-097558
目录号:
HY-175029
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