Dolutegravir (GSK1349572)

Integrase Inhibitors

Moligand™

10mM in DMSO

CAS编号: 1051375-16-6(DMSO)
分子式: C₂₀H₁₉F₂N₃O₅
分子量: 419.38

有货

库存信息

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货号 (SKU)	包装规格	是否现货	价格	数量
D408160-1ml	1ml	现货

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Compound libraries (12332)

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基本描述

别名	多替拉韦(GSK1349572)
英文别名	S/GSK1349572 \| 2H-Pyrido[1',2':4,5]pyrazino[2,1-b][1,3]oxazine-9-carboxamide, N-[(2,4-difluorophenyl)methyl]-3,4,6,8,12,12a-hexahydro-7-hydroxy-4-methyl-6,8-dioxo-, (4R,12aS)-
规格或纯度	Moligand™, 10mM in DMSO
英文名称	Dolutegravir (GSK1349572)
生化机理	Dolutegravir（GSK1349572，S/GSK1349572）是一种双金属结合型 HIV 整合酶抑制剂，在无细胞试验中的 IC50 值为 2.7 nM，对拉替拉韦耐药的特征突变体 Y143R、Q148K、N155H 和 G140S/Q148H 有适度活性。
储存温度	-80℃储存
运输条件	超低温冰袋运输
产品介绍	S/GSK1349572 inhibits recombinant HIV-1 integrase-catalyzed strand transfer in vitro. S/GSK1349572 potently inhibits HIV replication in cells infected with a self-inactivating PHIV lentiviral vector, such as peripheral blood mononuclear cells (PBMCs), MT-4 cells and CIP4. S/GSK1349572 exhibits potent activity against five different nonnucleoside reverse transcription inhibitor--resistant or nucleoside reverse transcription inhibitor--resistant viruses in vitro. S/GSK1349572 shows equivalent activity against two protease inhibitor-resistant viruses similarly to that against wild-type virus.Dolutegravir (GSK1349572)是一种HIV整合酶抑制剂，IC50为2.7 nM，适度有效作用于抗Raltegravir的显著突变体Y143R， Q148K， N155H，和G140S/Q148H。 Information Dolutegravir (GSK1349572) Dolutegravir (GSK1349572, S/GSK1349572) is a two-metal-binding HIV integrase inhibitor with IC50 of 2.7 nM in a cell-free assay, modest activity against raltegravir-resistant signature mutants Y143R, Q148K, N155H, and G140S/Q14 In vitro S/GSK1349572 shows the potent inhibitory effect on nine clinical isolates from integrase inhibitor-naive HIV-2-infected patients with EC50 ranging from 0.2 nM -1.4 nM. In vitro, S/GSK1349572 inhibits recombinant HIV-1 integrase-catalyzed strand transfer with IC50 of 2.7 nM. Furthermore, S/GSK1349572 potently inhibits HIV replication in cells such as peripheral blood mononuclear cells (PBMCs), MT-4 cells and CIP4 cells infected with a self-inactivating PHIV lentiviral vector with EC50 of 0,51 nM, 0.71 nM and 2.2 nM, respectively. In vitro, S/GSK1349572 exhibits potent activity against five different nonnucleoside reverse transcription inhibitor--resistant or nucleoside reverse transcription inhibitor--resistant viruses with EC50 ranging from 1.3 nM -2.1 nM. Similarly to that against wild-type virus, S/GSK1349572 shows equivalent activity against two protease inhibitor-resistant viruses with EC50 of 0.36 nM and 0.37 nM, respectively. In vivo Cell Data cell lines：T4302 CD133+ cells Concentrations：0 to 10 μM Incubation Time：4 days or 5 days Powder Purity:≥99%

产品属性

ALogP	0.3
hba_count	4
HBD Count	2
Rotatable Bond	3

关联靶点（人）

TMEM97 Tchem Sigma 细胞内受体 2(Sigma intracellular receptor 2) (1 活性数据)

点击查看靶蛋白信息： TMEM97

活性类型	活性值-log(M)	作用机制	期刊	参考文献(PubMed IDs)

名称和识别符

分子类型	小分子
Canonical SMILES	CC1CCOC2CN3C=C(C(=O)NCC4=C(F)C=C(F)C=C4)C(=O)C(=C3C(=O)N12)O
分子量	419.38
Reaxy-Rn	22829518
Reaxys-RN link address	https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=22829518&ln=