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度鲁特韦钠盐

HIV-1整合酶抑制剂
规格或纯度: 99%
有货

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库存信息

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货号 (SKU) 包装规格 是否现货 价格 数量
D275163-5mg 5mg 现货 Stock Image
D275163-25mg 25mg 现货 Stock Image
D275163-50mg 50mg 现货 Stock Image
D275163-100mg 100mg 现货 Stock Image

基本描述

规格或纯度 99%
英文名称 Dolutegravir Sodium
别名 (4R,12aS)-9-[(2,4-二氟苯基)甲基氨基甲酰基]-4-甲基-6,8-二氧代-3,4,12,12a-四氢-2H-吡啶基[5,6]吡嗪并[2,6-b][1,3]恶嗪-7-油酸钠盐
英文别名 (4R,12aS)-9-[(2,4-Difluorophenyl)methylcarbamoyl]-4-methyl-6,8-dioxo-3,4,12,12a-tetrahydro-2H-pyrido[5,6]pyrazino[2,6-b][1,3]oxazin-7-olatesodiumsalt
生化机理 Dolutegravir Sodium是一种HIV-1整合酶抑制剂,IC 50为2.7nM。对感染细胞中的总病毒DNA合成没有影响,但会阻止病毒DNA整合到宿主DNA中。
储存温度 -20°C储存
运输条件 超低温冰袋运输
产品介绍


Integrase inhibitors are a new class of antiretroviral drugs blocking the action of HIV integrase, which catalyses several key steps in the life cycle of the virus and is essential for insertion of the viral genome into the host cell DNA. GSK1349572 is a next-generation HIV integrase (IN) inhibitor.

In vitro: GSK1349572 is a two-metal-binding HIV integrase strand transfer inhibitor whose mechanism of action was established through resistance passage experiments, integrase enzyme assays, mechanistic cellular assays and activity against viral strains resistant to other classes of anti-HIV agents. In a variety of cellular antiviral assays, GSK1349572 inhibited HIV replication with subnanomolar or low-nanomolar potency and with a selectivity index of 9,400. The protein-adjusted half-maximal effective concentration extrapolated to 100% human serum was 38 nM .

In vivo: No animial in vivo data are available for GSK1349572 so far.

Clinical trial: GSK1349572 was effective when given once daily without a pharmacokinetic booster and was well tolerated at all assessed doses. These findings support the assessment of once daily 50 mg GSK1349572 in phase 3 trials.

名称和标识符

IUPAC Name sodium;(3S,7R)-13-[(2,4-difluorophenyl)methylcarbamoyl]-7-methyl-9,12-dioxo-4-oxa-1,8-diazatricyclo[8.4.0.03,8]tetradeca-10,13-dien-11-olate
INCHI InChI=1S/C20H19F2N3O5.Na/c1-10-4-5-30-15-9-24-8-13(17(26)18(27)16(24)20(29)25(10)15)19(28)23-7-11-2-3-12(21)6-14(11)22;/h2-3,6,8,10,15,27H,4-5,7,9H2,1H3,(H,23,28);/q;+1/p-1/t10-,15+;/m1./s1
InChi Key UGWJRRXTMKRYNK-VSLILLSYSA-M
Canonical SMILES CC1CCOC2N1C(=O)C3=C(C(=O)C(=CN3C2)C(=O)NCC4=C(C=C(C=C4)F)F)[O-].[Na+]
分子式

C20H18F2N3NaO5

PubChem CID 46216142
分子量 441.36

化学和物理性质

溶解性 0.2mg/ml in DMSO.
敏感性 对湿度敏感

安全信息

象形图
ghs09

Environmental Hazard

信号词 Warning
危险声明 H400: Very toxic to aquatic life
H410: Very toxic to aquatic life with long lasting effects
预防措施声明 P273,P501,P391

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