2. Anti-infection Metabolic Enzyme/Protease
  3. Virus Protease SARS-CoV Cathepsin
  4. Olgotrelvir

Olgotrelvir (STI-1558) is an orally active dual inhibitor of coronavirus main protease (Mpro) and human cell cathepsin (Cathepsin L). Olgotrelvir is readily converted to its active form, AC1115, in full blood and/or plasma. Olgotrelvir can effectively inhibit both SARS-CoV-2 replication and entry into host cells.

The free form of the compound is prone to instability, it is advisable to consider the stable salt form (Olgotrelvir sodium) that retains the same biological activity.

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Olgotrelvir

Olgotrelvir Estructura química

No. CAS : 2763596-71-8

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Olgotrelvir Related Antibodies

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Descripciòn

Olgotrelvir (STI-1558) is an orally active dual inhibitor of coronavirus main protease (Mpro) and human cell cathepsin (Cathepsin L). Olgotrelvir is readily converted to its active form, AC1115, in full blood and/or plasma. Olgotrelvir can effectively inhibit both SARS-CoV-2 replication and entry into host cells[1][2].

In Vitro

Olgotrelvir (0-100 μM; refresh every other day for 3 to 5 days) displays antiviral activity against all tested SARS-CoV-2 VOCs, including WA-1, Alpha, Beta, Delta, Lambda, and Gamma variants with average EC50 values of 0.28 to 4.26 μM in vero E6 cells[2].

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

Olgotrelvir Related Antibodies
Parmacokinetics
Species Dose Route AUC T1/2 Plasma Concentration Tmax Bioavailability
Cynomolgus Monkey 84 mg/kg p.o. 90900 ng·h/mL 4.84 h 18800 ng/mL 2.7 h 48.3 %
Dog 12.5 mg/kg p.o. 15200 ng·h/mL 4.01 h 3600 ng/mL 2.0 h 83.1 %
Dog 25 mg/kg p.o. 30500 ng·h/mL 3.76 h 7080 ng/mL 1.5 h 83.5 %
Dog 50 mg/kg p.o. 61800 ng·h/mL 3.51 h 13200 ng/mL 2.0 h 84.7 %
Mice 300 mg/kg p.o. 8030 ng·h/mL 1.58 h 7290 ng/mL 0.25 h 5.06 %
Mice 500 mg/kg p.o. 12400 ng·h/mL 1.9 h 10600 ng/mL 0.25 h 4.69 %
Rat 100 mg/kg p.o. 2000 ng·h/mL 1.48 h 1200 ng/mL 0.17 h 2.94 %
Rat 200 mg/kg p.o. 3580 ng·h/mL 1.84 h 2650 ng/mL 0.083 h 2.62 %
Rat 500 mg/kg p.o. 8050 ng·h/mL 2.03 h 6460 ng/mL 0.083 h 2.36 %
In Vivo

Olgotrelvir (400-1000 mg/kg; p.o.; twice a day immediately after viral inoculation) has antiviral activity and reduces lung pathology in K18-hACE2 transgenic mice[2].

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

Animal Model: K18-hACE2 transgenic mice (express human ACE2 in the lung epithelia, including airway epithelia, under the control of the human keratin 18 promoter)[2]
Dosage: 400, 500, 1000 mg/kg
Administration: Oral gavage (p.o.); twice a day immediately after SARS-CoV-2 WA-1 strain inoculation
Result: Prevented weight loss.
On day 5 post infection, virus was below the detectable level in the lungs.
Pathological changes caused by SARS-CoV-2 infection were relieved.
At a dose of 1000 mg/kg at the 12th hour post-infection resulted in significant reduction of viral RNA shedding and prevention of the body weight loss.
Blocked pro-inflammatory cytokine (IL-6, TNF-α, GM-CSF) release at 400 mg/kg dosage.
Ensayo clínico
Peso molecular

494.56

Fòrmula

C22H30N4O7S
No. CAS
SMILES

O=C(NCC1)[C@@H]1C[C@@H](C(O)S(=O)(O)=O)NC([C@H](CC(C)C)NC(C2=CC3=CC=CC=C3N2)=O)=O
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento

Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
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Olgotrelvir Related Classifications

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The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
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.

Keywords:

Olgotrelvir2763596-71-8STI-1558STI1558STI 1558Virus ProteaseSARS-CoVCathepsinSARS coronaviruscoronavirus main proteaseMproSARS-CoV-2Inhibitorinhibitorinhibit

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Nombre del producto:
Olgotrelvir
Cat. No.:
HY-156655
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