Simeprevir NEW
| Price | $30 | $46 | $61 |
| Package | 2mg | 5mg | 10mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-11 |
Product Details
| Product Name: Simeprevir | CAS No.: 923604-59-5 |
| Purity: 99.77% | Supply Ability: 10g |
| Release date: 2024/11/11 |
Product Introduction
Bioactivity
| 名稱 | Simeprevir |
| 描述 | Simeprevir (TMC435) is a potent HCV NS3/4A protease inhibitor, and inhibits HCV replication with EC50 of 8 nM. |
| 細胞實驗 | Huh7-Luc cells are seeded at a density of 2,500 cells/well in a 384-well plate in Dulbecco's modified Eagle's medium plus 10% fetal calf serum and incubated with a range of concentrations of serially diluted simeprevir, in a final DMSO concentration of 0.5% in the absence of G418. After 72 h of incubation, Steady Lite reagent is added in a 1:1 ratio to the medium, and luciferase signal is measured using a ViewLux reader. |
| 激酶實驗 | In vitro inhibition of NS3/4A activity is determined using a fluorescence resonance energy transfer cleavage assay with the RetS1 peptide substrate, derived from the genotype 1a NS4A-4B junction, and bacterially expressed full-length NS3 protease domain, supplemented with an NS4A peptide. Briefly, NS3/4A is preincubated in the presence of TMC435350 for 10 min, and then the RetS1 substrate is added and fluorescence is continuously measured for 20 min (excitation, 355 nm; emission, 500 nm). Cleavage of the substrate is expressed as a percentage of the cleavage seen with the vehicle control. |
| 動物實驗 | Twenty-four male specific-pathogen-free Sprague-Dawley rats, weighing between 200 and 300 g at the time of dosing, are divided into eight groups of three rats each. Seven groups are dosed orally (p.o.) by gastric intubation of a vitamin E acetate-d-α-tocopheryl polyethylene glycol 1000 succinate-polyethylene glycol 400 solution of Simeprevir (TMC435350) at 2 mL/kg body weight to provide a dose of 40 mg/kg. One group is dosed intravenously (i.v.) by slow bolus injection in a tail vein of a 20% 2-hydroxypropyl-β-cyclodextrin formulation of TMC435350 (containing TMC435350, 100 mg/mL 2-hydroxypropyl-β-cyclodextrin, 0.1 N NaOH to pH 8.0±0.1, and mannitol-and pyrogen-free water) at 2 mL/kg body weight to provide a dose of 4 mg/kg. Water and food are available ad libitum during the study. |
| 體外活性 | In Huh7-Luc cells, antiviral activity of simeprevir (Simeprevir) is dose dependent, and the EC50 and EC90 values determined for Simeprevir are 8 nM and 24 nM, respectively. Inhibition of Simeprevir on NS3/4A protease is time dependent, and the overall Kis are estimated to be 0.5 nM for genotype 1a and 0.4 nM for genotype 1b, respectively. Simeprevir is a potent inhibitor of HCV NS3/4A protease (Ki=0.36 nM) and viral replication (replicon EC50=7.8 nM). |
| 體內(nèi)活性 | In rats, TMC435350 (40 mg/kg, p.o.) is extensively distributed to the liver and intestinal tract (tissue/plasma area under the concentration-time curve ratios of >35), and the absolute bioavailability is 44%. |
| 存儲條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 55 mg/mL (73.34 mM) H2O : Insoluble |
| 關(guān)鍵字 | HCV Protease | Virus replication | TMC 435 | Hepatitis C virus | TMC435350 | immune responses | SARS-CoV | inhibit | HCV | Remdesivir | Huh7-Luc | Inhibitor | TMC 435350 | RNA-dependent RNA polymerase | SARS coronavirus | Simeprevir | DNA/RNA Synthesis | RdRp | TMC-435 |
| 相關(guān)產(chǎn)品 | EIDD-1931 | Remdesivir | Ribavirin | Silymarin | Umifenovir hydrochloride | Hydroxychloroquine | Ritonavir | Chloroquine phosphate | Artemisinin |
| 相關(guān)庫 | FDA上市及藥典收錄分子庫 | 大環(huán)化合物庫 | 經(jīng)典已知活性庫 | 肝臟毒性化合物庫 | EMA 上市藥物庫 | 藥物功能重定位化合物庫 | 抗病毒庫 | 抑制劑庫 | FDA 上市藥物庫 | 已知活性化合物庫 |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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