| Company Name: |
ChemeGen
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| Tel: |
18818260767 |
| Email: |
2625930290@qq.com |
| Products Intro: |
Product Name:Mpro Inhibitor 11a
CAS:2103278-86-8
Purity:98% Package:10 mg;50 mg;100 mg;500 mg;1 g;5 g;10 g
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| Company Name: |
TargetMol Chemicals Inc.
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| Tel: |
4008200310 |
| Email: |
marketing@tsbiochem.com |
| Products Intro: |
Product Name:Bofutrelvir
CAS:2103278-86-8
Purity:99.92% Package:1mg/RMB 1410;5mg/RMB 4490;10mg/RMB 6330
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1H-Indole-2-carboxamide, N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-formyl-2-[(3S)-2-oxo-3-pyrrolidinyl]ethyl]amino]-2-oxoethyl]- manufacturers
- Bofutrelvir
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- $198.00 / 1mg
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2025-11-10
- CAS:2103278-86-8
- Min. Order:
- Purity: 99.92%
- Supply Ability: 10g
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| | 1H-Indole-2-carboxamide, N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-formyl-2-[(3S)-2-oxo-3-pyrrolidinyl]ethyl]amino]-2-oxoethyl]- Basic information |
| | 1H-Indole-2-carboxamide, N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-formyl-2-[(3S)-2-oxo-3-pyrrolidinyl]ethyl]amino]-2-oxoethyl]- Chemical Properties |
| storage temp. | Store at -20°C | | solubility | DMF: 30 mg/ml,DMSO: 30 mg/ml,Ethanol: 30 mg/ml | | form | A crystalline solid | | color | White to light yellow |
| | 1H-Indole-2-carboxamide, N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-formyl-2-[(3S)-2-oxo-3-pyrrolidinyl]ethyl]amino]-2-oxoethyl]- Usage And Synthesis |
| Uses | Bofutrelvir (FB2001) is a SARS-CoV-2 main protease Mpro inhibitor with an IC50 value of 53 nM and an EC50 value of 0.53 μM. Bofutrelvir exhibits potent antiviral efficacy against several current SARS-CoV-2 variants with EC50 values of 0.26-0.42 μM. Bofutrelvir has an additive antiviral effect when combined with Remdesivir.html" class="link-product" target="_blank">Remdesivir (HY-104077)[1][2]. | | Definition | ChEBI: N-[(2S)-3-cyclohexyl-1-oxo-1-({(2S)-1-oxo-3-[(3S)-2-oxopyrrolidin-3-yl]propan-2-yl}amino)propan-2-yl]-1H-indole-2-carboxamide is a secondary carboxamide resulting from the formal condensation of the carboxy group of 1H-indole-2-carboxylic acid with the primary amino group of 3-cyclohexyl-N-{(2S)-1-oxo-3-[(3S)-2-oxopyrrolidin-3-yl]propan-2-yl}-L-alaninamide. It is an inhibitor of SARS coronavirus main proteinase and inhibits SARS-CoV-2 replication in cell culture (EC50 = 0.53 muM). It has a role as an EC 3.4.22.69 (SARS coronavirus main proteinase) inhibitor and an anticoronaviral agent. It is an indolecarboxamide, a member of pyrrolidin-2-ones, an aldehyde, a secondary carboxamide and an oligopeptide. | | Biological Activity | Inhibitor 11a is a COVID-19 corona virus SARS-CoV-2 inhibitor th at covalently targets the main protease (Mpro; a.k.a. 3C-like protease or 3CLpro) substrate site Cys145 (IC50 = 53 nM; 10 min pre-incubation with 30 nM SARS-CoV-2 Mpro prior to the addition of 20 μM substrate). Inhibitor 11a effectively inhibits SARS-CoV-2 replication in Vero E6 cultures (IC50 = 0.53 μM 24 h post infection with MOI = 0.05; cytotoxicity CC50 >100 μM) with good pharmacokinetic properties in mice in vivo (5 mg/kg via i.p. or i.v.). | | in vivo | Bofutrelvir (100 and 200 mg/kg; i.p. once daily on day 0 and twice daily on day 1, 2 and 3 for 4 consecutive days) effectively against SARS-CoV-2 delta variant infection in vivo[2]. | Animal Model: | K18-hACE2 mice with SARS-CoV-2 delta variant infection[2] | | Dosage: | 100 and 200 mg/kg | | Administration: |
Intraperitoneal injection; 100 and 200 mg/kg once daily on day 0 and twice daily on day 1, 2 and 3 for 4 consecutive days | | Result: | Showed a dose-dependent efficacy to virus titers of lung. Effectively reduces the lung viral loads. Dose-dependently showed antiviral activity against the SARS-CoV-2 Delta variant and significantly reduced viral load in mouse lung and brain.
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| | References | [1] Ullrich S, Nitsche C. The SARS-CoV-2 main protease as drug target. Bioorg Med Chem Lett. 2020 Sep 1;30(17):127377. DOI:10.1016/j.bmcl.2020.127377
[2] Shang W, et al. In vitro and in vivo evaluation of the main protease inhibitor FB2001 against SARS-CoV-2. Antiviral Res. 2022 Dec;208:105450. DOI:10.1016/j.antiviral.2022.105450 |
| | 1H-Indole-2-carboxamide, N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-formyl-2-[(3S)-2-oxo-3-pyrrolidinyl]ethyl]amino]-2-oxoethyl]- Preparation Products And Raw materials |
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