1. Anti-infection
  2. SARS-CoV
  3. VPC285785

VPC285785 是一种具有口服活性的 SARS-CoV-2 主蛋白酶抑制剂,IC50 为 0.8 μM,Kd 为 2.7 μM。VPC285785 可在功能上抑制病毒复制所需的病毒多蛋白前体的病毒主蛋白酶加工过程。VPC285785 可降低 MHV 感染小鼠的肝脏、脑和脾脏组织中的病毒载量。VPC285785 可用于冠状病毒感染的研究。

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VPC285785

VPC285785 Chemical Structure

CAS No. : 2759276-10-1

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

VPC285785 is an orally active SARS-CoV-2 main protease inhibitor with an IC50 of 0.8 μM and a Kd of 2.7 μM. VPC285785 functionally inhibits the viral main protease-mediated processing of viral polyprotein precursors required for viral replication. VPC285785 reduces viral loads in the liver, brain and spleen tissues of MHV-infected mice. VPC285785 is applicable to the research of coronavirus infections[1].

体外研究
(In Vitro)

VPC285785 (10 μM) 对人组织蛋白酶 L (CatL) 表现出弱抑制作用,在 10 μM浓度下仅观察到 15%的抑制率[1]

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

药代动力学
(Parmacokinetics)
Species Dose Route Cmax AUClast AUC0-inf T1/2 Vz Tmax Bioavailability
Mice[1] 10 mg/kg i.v. 18700 ng/mL 16.833 μg·h/mL 17 μg·h/mL 36.5 min 0.5 L/kg / /
Mice[1] 10 mg/kg p.o. 953 ng/mL 2.433 μg·h/mL 149 μg·h/mL 2.48 min / 30 min 15 %
体内研究
(In Vivo)

VPC285785 (150 mg/kg;口服;每日 1 次;连续 3 天) 可显著降低 MHV-A59 感染小鼠肝脏、脑和脾脏中的病毒载量,同时维持其肝肾功能[1]

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

Animal Model: Balb/CJ (female, 8-10 weeks old, 18.5-26.5 g, intranasal infection with MHV-A59)[1]
Dosage: 150 mg/kg
Administration: p.o.; once daily; 3 days (day 1, 2, 3 post-infection)
Result: Reduced liver enzyme levels: alanine transaminase (ALT) 65.5 U/L, aspartate aminotransferase (AST) 126.0 U/L, and total protein (TP) 54.16 g/L.
Showed less pronounced decrease in blood urea nitrogen (BUN) levels.
Lowered white blood cell (WBC) counts.
Achieved statistically significant reduction in viral load in the liver, brain, and spleen; no significant differences in viral load observed in the lung, heart, or kidney.
分子量

469.48

Formula

C24H25F2N5O3

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
  • 摩尔计算器

  • 稀释计算器

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
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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:
VPC285785
目录号:
HY-181983
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