雷特格韦钾盐|T2239

Raltegravir potassium
871038-72-1

￥148 5mg 起订

￥223 10mg 起订

￥391 25mg 起订

上海更新日期：2024-09-14

TargetMol中国（陶术生物）

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产品详情:

中文名称：: 雷特格韦钾盐

英文名称：: Raltegravir potassium

CAS号：: 871038-72-1

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：: 99.45%

产品类别：: 抑制剂

货号：: T2239

Product Introduction

Bioactivity

Name	Raltegravir potassium
Description	Raltegravir potassium (MK 0518 potassium salt) salt(MK0518 potassium salt) is a potent integrase (IN) inhibitor, used to treat HIV infection.
Cell Research	Human MT-4 cells are infected for 2 hours with the SIVmac251, HIV-1 (IIIB) and HIV-2 (CDC 77618) stocks at a multiplicity of infection of, approximately, 0.1. Cells are then washed three times in phosphate buffered saline, and suspended at 5 × 105/mL in fresh culture medium (to primary cells 50 units/mL of IL-2 are added) in 96-well plates, in the presence or absence of a range of triplicate raltegravir concentrations (0.0001 μM-1 μM). Untreated infected and mock-infected controls are prepared too, in order to allow comparison of the data derived from the different treatments. Viral cytopathogeniciy in MT-4 cells is quantitated by the methyl tetrazolium (MTT) method (MT-4/MTT assay) when extensive cell death in control virus-infected cell cultures is detectable microscopically as lack of capacity to re-cluster. The capability of MT-4 cells to form clusters after infection. Briefly, clusters are disrupted by pipetting; and, after 2 hours of incubation at 37°C, the formation of new clusters is assessed by light microscopy (100× magnification). Cell culture supernatants are collected for HIV-1 p24 and HIV-2/SIVmac251 p27 core antigen measurement by ELISA. In CEMx174-infected cell cultures, which show a propensity to form syncytia induced by the virus envelope glycoproteins, syncytia are counted, in blinded fashion, by light microscopy for each well at 5 days following infection.
In vitro	PFV IN带有S217H突变的对Raltegravir的敏感性降低了10倍，其IC50为900 nM。PFV IN的活性仅为WT活性的10%，并且被Raltegravir以200 nM的IC50抑制，这表明与WT IN相比，对IN链转移抑制剂（INSTI）的敏感性大约降低了两倍。S217Q PFV IN对Raltegravir的敏感性与WT酶相同[1]。Raltegravir通过糖苷化作用而非通过肝脏代谢。Raltegravir对HIV-1具有强大的体外活性，其95%抑制浓度为31±20 nM，在人类T淋巴细胞培养中。Raltegravir还对HIV-2有效，当在CEMx174细胞中测试时，IC95为6 nM。Raltegravir的代谢主要通过糖苷化作用。强烈诱导糖苷化酶UGT1A1的药物会显著降低Raltegravir浓度，因此不应使用。Raltegravir对肝脏细胞色素P450活性具有弱抑制作用。Raltegravir不诱导CYP3A4 RNA表达或CYP3A4依赖的睾酮6-β-羟化酶活性[2]。在镁和钙存在下，Raltegravir的细胞渗透性降低[3]。Raltegravir及相关HIV-1整合酶(IN)链转移抑制剂（INSTIs）有效阻断病毒复制[4]。在急性感染的人类淋巴细胞CD4+ T细胞系MT-4和CEMx174中，Raltegravir有效抑制SIVmac251的复制，其EC90在低nM范围内[5]。
In vivo	Raltegravir 通过其单药治疗在进行中的 SIVmac251 感染的非人灵长类动物中引发病毒免疫学改善。有一种非人灵长类动物在接受 Raltegravir 单药治疗后，其病毒载量检测不到[5]。
Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
Solubility Information	DMSO : 87 mg/mL (180.3 mM)
Keywords	Raltegravir \| inhibit \| HIV \| Inhibitor \| MK 0518 \| Human immunodeficiency virus \| MK-0518 \| MK0518 \| HIV Integrase \| Raltegravir potassium \| MK 0518 potassium
Inhibitors Related	Emtricitabine \| Lamivudine \| Stavudine
Related Compound Libraries	Inhibitor Library \| Bioactive Compound Library \| Highly Selective Inhibitor Library \| FDA-Approved Drug Library \| Anti-Viral Compound Library \| Drug Repurposing Compound Library

雷特格韦钾盐|||Raltegravir potassium salt|||MK 0518 potassium salt|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