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

Olgotrelvir sodium  (Synonyms: STI-1558 sodium)

Cat. No.: HY-156655A Purity: ≥95.0%
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Olgotrelvir sodium is an orally active dual inhibitor of coronavirus main protease (Mpro) and human cell cathepsin (Cathepsin L). Olgotrelvir sodium is readily converted to its active form, AC1115, in full blood and/or plasma. Olgotrelvir sodium can effectively inhibit both SARS-CoV-2 replication and entry into host cells.

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

Olgotrelvir sodium Chemical Structure

Olgotrelvir sodium Chemical Structure

CAS No. : 2763596-72-9

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Based on 1 publication(s) in Google Scholar

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Olgotrelvir sodium Related Antibodies

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Description

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

In Vitro

Olgotrelvir (0-100 μM; refreshed every other day for 3 to 5 days) sodium 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 sodium 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 1.90 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) sodium 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

516.54

Formula

C22H29N4NaO7S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(NCC1)[C@@H]1C[C@@H](C(O)S(=O)(O[Na])=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

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

H2O : 50 mg/mL (96.80 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9360 mL 9.6798 mL 19.3596 mL
5 mM 0.3872 mL 1.9360 mL 3.8719 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

=
Concentration (final)

C2

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Volume (final)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O 1 mM 1.9360 mL 9.6798 mL 19.3596 mL 48.3990 mL
5 mM 0.3872 mL 1.9360 mL 3.8719 mL 9.6798 mL
10 mM 0.1936 mL 0.9680 mL 1.9360 mL 4.8399 mL
15 mM 0.1291 mL 0.6453 mL 1.2906 mL 3.2266 mL
20 mM 0.0968 mL 0.4840 mL 0.9680 mL 2.4199 mL
25 mM 0.0774 mL 0.3872 mL 0.7744 mL 1.9360 mL
30 mM 0.0645 mL 0.3227 mL 0.6453 mL 1.6133 mL
40 mM 0.0484 mL 0.2420 mL 0.4840 mL 1.2100 mL
50 mM 0.0387 mL 0.1936 mL 0.3872 mL 0.9680 mL
60 mM 0.0323 mL 0.1613 mL 0.3227 mL 0.8066 mL
80 mM 0.0242 mL 0.1210 mL 0.2420 mL 0.6050 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Olgotrelvir sodium Related Classifications

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:

Olgotrelvir2763596-72-9STI-1558STI1558STI 1558CathepsinSARS-CoVSARS coronaviruscoronavirus main proteaseMproSARS-CoV-2Inhibitorinhibitorinhibit

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