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.

For research use only. We do not sell to patients.

Olgotrelvir Chemical Structure

Olgotrelvir Chemical Structure

CAS No. : 2763596-71-8

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Other Forms of Olgotrelvir:

Olgotrelvir Related Antibodies

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Description

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 Indicator value
Cynomolgus Monkey 84 mg/kg p.o. AUC0-inf 90900 ng·h/mL
Dog 12.5 mg/kg p.o. AUC0-inf 15200 ng·h/mL
Dog 25 mg/kg p.o. AUC0-inf 30500 ng·h/mL
Dog 50 mg/kg p.o. AUC0-inf 61800 ng·h/mL
Mice 300 mg/kg p.o. AUC0-inf 8030 ng·h/mL
Mice 500 mg/kg p.o. AUC0-inf 12400 ng·h/mL
Rat 100 mg/kg p.o. AUC0-inf 2000 ng·h/mL
Rat 200 mg/kg p.o. AUC0-inf 3580 ng·h/mL
Rat 500 mg/kg p.o. AUC0-inf 8050 ng·h/mL
Cynomolgus Monkey 84 mg/kg p.o. T1/2 4.84 hr
Dog 12.5 mg/kg p.o. T1/2 4.01 hr
Dog 25 mg/kg p.o. T1/2 3.76 hr
Dog 50 mg/kg p.o. T1/2 3.51 hr
Mice 300 mg/kg p.o. T1/2 1.58 hr
Mice 500 mg/kg p.o. T1/2 1.9 hr
Rat 100 mg/kg p.o. T1/2 1.48 hr
Rat 200 mg/kg p.o. T1/2 1.84 hr
Rat 500 mg/kg p.o. T1/2 2.03 hr
Cynomolgus Monkey 84 mg/kg p.o. Cmax 18800 ng/mL
Dog 12.5 mg/kg p.o. Cmax 3600 ng/mL
Dog 25 mg/kg p.o. Cmax 7080 ng/mL
Dog 50 mg/kg p.o. Cmax 13200 ng/mL
Mice 300 mg/kg p.o. Cmax 7290 ng/mL
Mice 500 mg/kg p.o. Cmax 10600 ng/mL
Rat 100 mg/kg p.o. Cmax 1200 ng/mL
Rat 200 mg/kg p.o. Cmax 2650 ng/mL
Rat 500 mg/kg p.o. Cmax 6460 ng/mL
Cynomolgus Monkey 84 mg/kg p.o. Tmax 2.7 hr
Dog 12.5 mg/kg p.o. Tmax 2.0 hr
Dog 25 mg/kg p.o. Tmax 1.5 hr
Dog 50 mg/kg p.o. Tmax 2.0 hr
Mice 300 mg/kg p.o. Tmax 0.25 hr
Mice 500 mg/kg p.o. Tmax 0.25 hr
Rat 100 mg/kg p.o. Tmax 0.17 hr
Rat 200 mg/kg p.o. Tmax 0.083 hr
Rat 500 mg/kg p.o. Tmax 0.083 hr
Cynomolgus Monkey 84 mg/kg p.o. F 48.3 %
Dog 12.5 mg/kg p.o. F 83.1 %
Dog 25 mg/kg p.o. F 83.5 %
Dog 50 mg/kg p.o. F 84.7 %
Mice 300 mg/kg p.o. F 5.06 %
Mice 500 mg/kg p.o. F 4.69 %
Rat 100 mg/kg p.o. F 2.94 %
Rat 200 mg/kg p.o. F 2.62 %
Rat 500 mg/kg p.o. F 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.
Molecular Weight

494.56

Formula

C22H30N4O7S
CAS No.
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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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 *
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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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