西咪匹韦|T4686

Simeprevir
923604-59-5

￥415 2mg 起订

￥835 5mg 起订

￥1255 10mg 起订

上海更新日期：2024-09-14

TargetMol中国（陶术生物）

VIP12年

联系人：邵小姐

电话：021-021-33632979拨打

手机：15002134094 拨打

邮箱：marketing@targetmol.com

产品详情:

中文名称：: 西咪匹韦

英文名称：: Simeprevir

CAS号：: 923604-59-5

品牌：: TargetMol

产地：: 美国

保存条件：: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

纯度规格：: 99.77%

产品类别：: 抑制剂

货号：: T4686

Product Introduction

Bioactivity

名称	Simeprevir
描述	Simeprevir (TMC435) is a potent HCV NS3/4A protease inhibitor, and inhibits HCV replication with EC50 of 8 nM.
细胞实验	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.
激酶实验	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.
动物实验	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.
体外活性	在Huh7-Luc细胞中，Simeprevir的抗病毒活性与剂量呈依赖关系，其EC50和EC90值分别为8 nM和24 nM。Simeprevir对NS3/4A蛋白酶的抑制作用随时间依赖性增强，针对基因型1a和1b的总Kis估计值分别为0.5 nM和0.4 nM。Simeprevir是一种强效的HCV NS3/4A蛋白酶抑制剂（Ki=0.36 nM）以及病毒复制的抑制剂（复制子EC50=7.8 nM）。
体内活性	在大鼠中，TMC435350（40 mg/kg，p.o.）广泛分布于肝脏和肠道（组织/血浆浓度-时间曲线下面积比值>35），且绝对生物利用度为44%。
存储条件	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
关键字	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
相关产品	Umifenovir hydrochloride \| Chloroquine phosphate \| Dexamethasone \| Hydroxychloroquine \| Artemisinin \| EIDD-1931 \| Methyl 2-amino-5-bromobenzoate \| Silymarin \| Nirmatrelvir \| Ritonavir \| Ribavirin \| Remdesivir
相关库	抑制剂库 \| 经典已知活性库 \| 已知活性化合物库 \| 肝脏毒性化合物库 \| EMA 上市药物库 \| 蛋白酶抑制剂库 \| 抗病毒库 \| FDA 上市药物库 \| 大环化合物库 \| 药物功能重定位化合物库

西咪匹韦|||TMC-435350|||TMC435|||Olysio|TargetMol

上海陶术生物科技有限公司为美国Target Molecule Corp. ( Target Mol ) 在上海建立的全资子公司。我们与美国波士顿、德国慕尼黑的同事一起，为北美、欧洲和亚洲从事药物研发和生物学研究的科学家提供优质的产品和专业的服务。公司下设筛选事业部，化学事业部，生物事业部和新材料部。从虚拟筛选到实体化合物分子供应；从商业化产品销售到个性化定制合成；从对明确靶点的分子筛选到对明确分子的多靶点筛选，从高通量筛选到化学结构优化，我们都可以满足您的科研用品及技术服务的需求。经过在中国市场五年的精心耕耘，我们已成为筛选化合物领域优秀的供应商，为超过五百家学校和各类企业提供了品质卓越的小分子化合物和药物筛

成立日期	(12年)
注册资本	566.2651万人民币
员工人数	100-500人
年营业额	￥ 1亿以上
经营模式	贸易,试剂,定制,服务
主营行业	化学试剂,生物活性小分子