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

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.

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VPC285785

VPC285785 Chemical Structure

CAS No. : 2759276-10-1

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Description

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].

In Vitro

VPC285785 (10 μM) exerts weak inhibitory effects on human cathepsin L (CatL), with only 15% inhibition observed at the concentration of 10 μM[1].

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

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 %
In Vivo

VPC285785 (150 mg/kg; p.o.; once daily; for 3 consecutive days) significantly reduces viral loads in the liver, brain and spleen of MHV-A59-infected mice while preserving their liver and kidney functions[1].

MedChemExpress (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.
Molecular Weight

469.48

Formula

C24H25F2N5O3

CAS No.
SMILES

FC1=CC(F)=C(C=C(C(N2C[C@H](C3(C)C)[C@H]3[C@H]2C(N[C@H](C#N)C[C@@H]4CCNC4=O)=O)=O)N5)C5=C1

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Room temperature in continental US; may vary elsewhere.

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

Purity & Documentation
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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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Product Name:
VPC285785
Cat. No.:
HY-181983
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