Product Details
Product Name:
Leritrelvir |
CAS No.:
2923310-64-7 |
Purity:
97.42% |
Supply Ability:
10g |
Release date:
2024/11/15 |
Product Introduction
Bioactivity
名稱(chēng) | Leritrelvir |
描述 | Leritrelvir (RAY1216) is an orally active and highly potent protease inhibitor with antiviral activity that blocks cleavage of viral precursor proteins and inhibits viral replication in SARS-CoV-2. |
體外活性 | Leritrelvir has a residence time of 104 minutes on the target.
Leritrelvir forms covalent binding to the Cys145 catalytic site via the α-ketoamide warhead.
0-1000 nM Leritrelvir, treated for 72 hours, demonstrated antiviral effects against SARS-CoV-2 wild type and its variants. [1] |
體內(nèi)活性 | Leritrelvir was effective in prolonging the survival time of SARS-CoV-2 infected mice for 5 consecutive days under oral administration conditions in the dose range of 150-600 mg/kg/day. The pharmacokinetic parameters of the drug have been studied in a variety of animals demonstrating the exposure and metabolic properties of the drug.
In mice, the area under the drug curve (AUC(0-last)) at an intravenous (IV) dose of 3.0 mg/kg was 7789 nM/h, but peak concentration (C_max) and time to peak (T_max) were not provided. In comparison, an oral (PO) dose of 10 mg/kg produced a C_max of 1287 nM, a T_max of 2.0 hours, an AUC(0-last) of 5698 nM/h, an elimination half-life (T_1/2) of 2.6 hours, and an oral bioavailability (F%) of 22.
In rats, the intravenous (IV) dose of 2.0 mg/kg yielded an AUC(0-last) of 4505 nM/h, whereas the oral (PO) dose of 10 mg/kg produced a C_max of 916 nM, a T_max of 0.9 h, an AUC(0-last) of 7429 nM/h, a T_1/2 of 4.3 h, and an F% of 33.
In cynomolgus monkeys, the intravenous (IV) dose of 1.0 mg/kg had an AUC(0-last) of 1157 nM/h, whereas the oral (PO) dose of 5.0 mg/kg yielded a C_max of 102 nM, a T_max of 1.5 h, an AUC(0-last) of 458 nM/h, a T_1/2 of 14.9 h, and a F% of 8. [1] |
存儲(chǔ)條件 | keep away from moisture,keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
相關(guān)產(chǎn)品 | Nirmatrelvir | EIDD-1931 | Remdesivir | Andrographolide | Silymarin | Umifenovir hydrochloride | Hydroxychloroquine | Ritonavir | Chloroquine phosphate | Dexamethasone | Favipiravir | Imatinib |
Company Profile Introduction
TargetMol Chemicals Inc. is headquartered in Boston, MA, and specializes in products and services that serve the research needs of chemical and biological scientists worldwide. With a client base in 40+ countries, TargetMol has evolved into one of the biggest global research suppliers for compound libraries and small molecule compounds.
170+ Compound Libraries, 10000+ Noval Small Molecucles,16000+ Nature Compounds
TargetMol diligently updates and offers over 170 types of compound libraries and a wide range of high-quality research chemicals, including inhibitors, activators, natural products, peptides, antibodies , and novel life-science kits for laboratory and scientific use. In addition, our lab allows us to conduct CADD (computer-aided drug design) and chemical synthesis to meet the customization needs of our clients.
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Recommended supplier
Product name |
Price |
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Suppliers |
Update time |
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$/ |
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Anhui Ruihan Technology Co., Ltd
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2023-08-21 |