Olgotrelvir sodium
Based on 1 Customer Validation
Olgotrelvir (STI-1558) 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.
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- Purity: 95.0%
- CAS No.: 2763596-72-9
- 화학식: C22H29N4NaO7S
- 분자량:516.54
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보관:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Biological Activity
Olgotrelvir (0-100 μM; refresh 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.
| Species | Dose | Route | AUC | Bioavailability | T1/2 | Tmax | Plasma Concentration |
|---|---|---|---|---|---|---|---|
| Cynomolgus Monkey | 84 mg/kg | p.o. | 90900 ng·h/mL | 48.3 % | 4.84 h | 2.7 h | 18800 ng/mL |
| Dog | 12.5 mg/kg | p.o. | 15200 ng·h/mL | 83.1 % | 4.01 h | 2.0 h | 3600 ng/mL |
| Dog | 25 mg/kg | p.o. | 30500 ng·h/mL | 83.5 % | 3.76 h | 1.5 h | 7080 ng/mL |
| Dog | 50 mg/kg | p.o. | 61800 ng·h/mL | 84.7 % | 3.51 h | 2.0 h | 13200 ng/mL |
| Mice | 300 mg/kg | p.o. | 8030 ng·h/mL | 5.06 % | 1.58 h | 0.25 h | 7290 ng/mL |
| Mice | 500 mg/kg | p.o. | 12400 ng·h/mL | 4.69 % | 1.90 h | 0.25 h | 10600 ng/mL |
| Rat | 100 mg/kg | p.o. | 2000 ng·h/mL | 2.94 % | 1.48 h | 0.17 h | 1200 ng/mL |
| Rat | 200 mg/kg | p.o. | 3580 ng·h/mL | 2.62 % | 1.84 h | 0.083 h | 2650 ng/mL |
| Rat | 500 mg/kg | p.o. | 8050 ng·h/mL | 2.36 % | 2.03 h | 0.083 h | 6460 ng/mL |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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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]
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Dosage:400, 500, 1000 mg/kg
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Administration:Oral gavage (p.o.); twice a day immediately after SARS-CoV-2 WA-1 strain inoculation
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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.
Chemical Information
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CAS No. 2763596-72-9
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Appearance Solid
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분자량 516.54
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화학식 C22H29N4NaO7S
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Color White to off-white
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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
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Synonyms
STI-1558 sodium
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선적
Room temperature in continental US; may vary elsewhere.
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보관
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
용액&용해도
H2O : 50 mg/mL (96.80 mM; Need ultrasonic)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
순도&문서
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Data Sheet (276 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
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.
Olgotrelvir sodium Related Classifications
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