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度鲁特韦 (GSK1349572)

强效\ xa0HIV整合酶抑制剂
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货号 (SKU) 包装规格 是否现货 价格 数量
D127636-5mg
 5mg 现货 Stock Image
D127636-10mg
 10mg 现货 Stock Image
D127636-50mg
 50mg 期货 Stock Image
大包装询价 收藏夹 比较  SDS中文版  DATASHEET
查看相关系列
Anti-infection (2825) HIV (248) HIV Integrase (29) Metabolic Enzyme/Protease (4888)
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基本描述

别名 度鲁特韦
英文别名 GSK1349572 | DOLUTEGRAVIR [VANDF] | GSK 1349572 | HSDB 8152 | Tivicay (TN) | 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) | SCHEMBL82071 | Z
规格或纯度 Moligand™, ≥99%
英文名称 Dolutegravir (GSK1349572)
生化机理 Dolutegravir（DTG，GSK1349572）是一种整合酶抑制剂，由葛兰素史克公司（GSK）代表 Shionogi-ViiV Healthcare LLC 开发，用于治疗人类免疫缺陷病毒（HIV）-1 感染。多罗替拉韦（DTG，GSK1349572）主要通过二磷酸尿苷葡萄糖醛酸转移酶（μgT）1A1进行代谢，细胞色素P450（CYP）3A的作用较小，未改变的drμg经肾排出量极低（<剂量的1%）。口服总剂量的 53% 未发生变化地从粪便中排出，但目前尚不清楚其中全部或部分是由于未吸收的 drμg 还是由于一定比例的葡萄糖醛酸轭合物的胆汁排泄，葡萄糖醛酸轭合物可在肠腔中进一步降解形成母体化合物。目前的食品与药物管理局（FDA）肾功能损害研究指南草案规定，即使是那些主要代谢或分泌的药物，也应在肾功能损害的患者中进行药代动力学（PK）研究。抑制外周血单核细胞（PBMCs）中 HIV-1 病毒的复制（EC 50 = 0.51 nM）。
储存温度 -20°C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。

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) is a two-metal-binding HIV integrase inhibitor with IC50 of 2.7 nM, modest activity against raltegravir-resistant signature mutants Y143R, Q148K, N155H, and G140S/Q148H.

关联靶点（人）

TMEM97 Tchem Sigma 细胞内受体 2(Sigma intracellular receptor 2) (1 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
CYP2C8 Tchem Cytochrome P450 2C8 (1492 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CYP2D6 Tclin Cytochrome P450 2D6 (33882 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
NR1I2 Tchem Pregnane X receptor (6667 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CYP1A2 Tchem Cytochrome P450 1A2 (26471 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
UGT1A4 Tbio UDP-glucuronosyltransferase 1A4 (288 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CYP2C9 Tchem Cytochrome P450 2C9 (32119 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CYP2C19 Tchem Cytochrome P450 2C19 (29246 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CYP3A4 Tclin Cytochrome P450 3A4 (53859 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CYP2A6 Tchem Cytochrome P450 2A6 (2861 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CYP2B6 Tchem Cytochrome P450 2B6 (1338 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
UGT2B7 Tchem UDP-glucuronosyltransferase 2B7 (787 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ABCG2 Tchem ATP-binding cassette sub-family G member 2 (4927 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
SLC22A1 Tchem Solute carrier family 22 member 1 (646 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ABCC2 Tchem Canalicular multispecific organic anion transporter 1 (1191 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
UGT2B4 Tbio UDP-glucuronosyltransferase 2B4 (139 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
UGT2B15 Tbio UDP-glucuronosyltransferase 2B15 (172 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
UGT1A1 Tchem UDP-glucuronosyltransferase 1-1 (448 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
SLCO1B1 Tchem Solute carrier organic anion transporter family member 1B1 (2672 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
SLCO1B3 Tchem Solute carrier organic anion transporter family member 1B3 (2517 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
SLC22A2 Tchem Solute carrier family 22 member 2 (261 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
UGT1A6 Tbio UDP-glucuronosyltransferase 1-6 (221 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
UGT1A9 Tbio UDP-glucuronosyltransferase 1-9 (343 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
UGT1A3 Tbio UDP-glucuronosyltransferase 1-3 (217 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID

关联靶点（其它种属）

pol Human immunodeficiency virus type 1 reverse transcriptase (18245 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Vesicular acetylcholine transporter (105 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Sigmar1 Sigma opioid receptor (160 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Abcb1b P-glycoprotein 1 (174 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Hdac6 Histone deacetylase 6 (222 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
pol Human immunodeficiency virus type 1 integrase (9041 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
pol Human immunodeficiency virus type 2 integrase (9 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Human immunodeficiency virus 1 (70413 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Human immunodeficiency virus (3636 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
SIGMAR1 Sigma-1 receptor (3326 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
rep Replicase polyprotein 1ab (378 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
gag-pol Gag-Pol polyprotein (8 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Liver microsome (341 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Tmem97 Sigma intracellular receptor 2 (922 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
SARS-CoV-2 (38078 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Vero C1008 (1716 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID

作用机制

作用机制 Action Type target ID Target Name Target Type Target Organism Binding Site Name 参考文献

名称和识别符

分子类型 小分子
IUPAC Name (3S,7R)-N-[(2,4-difluorophenyl)methyl]-11-hydroxy-7-methyl-9,12-dioxo-4-oxa-1,8-diazatricyclo[8.4.0.03,8]tetradeca-10,13-diene-13-carboxamide
INCHI InChI=1S/C20H19F2N3O5/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)/t10-,15+/m1/s1
InChi Key RHWKPHLQXYSBKR-BMIGLBTASA-N
Canonical SMILES CC1CCOC2N1C(=O)C3=C(C(=O)C(=CN3C2)C(=O)NCC4=C(C=C(C=C4)F)F)O
Isomeric SMILES C[C@@H]1CCO[C@@H]2N1C(=O)C3=C(C(=O)C(=CN3C2)C(=O)NCC4=C(C=C(C=C4)F)F)O
PubChem CID 54726191
分子量 419.38

化学和物理性质

溶解性 Soluble in DMSO (84 mg/ml at 25 °C), water (<1 mg/ml at 25 °C), and ethanol (<1 mg/ml at 25 °C).
分子量 419.400 g/mol
XLogP3 2.400
氢键供体数Hydrogen Bond Donor Count 2
氢键受体数Hydrogen Bond Acceptor Count 8
可旋转键计数Rotatable Bond Count 3
精确质量Exact Mass 419.129 Da
单同位素质量Monoisotopic Mass 419.129 Da
拓扑极表面积Topological Polar Surface Area 99.200 Ų
重原子数Heavy Atom Count 30
形式电荷Formal Charge 0
复杂度Complexity 829.000
同位素原子数Isotope Atom Count 0
定义的原子立体中心计数Defined Atom Stereocenter Count 2
未定义的原子立体中心计数Undefined Atom Stereocenter Count 0
定义的键立体中心计数Defined Bond Stereocenter Count 0
未定义的键立体中心计数Undefined Bond Stereocenter Count 0
所有立体化学键的总数The total count of all stereochemical bonds 0
共价键合单元计数Covalently-Bonded Unit Count 1

安全和危险性（GHS）

 SDS英文版

质量标准

Nitrogen by Elemental Analysis 9.7-10.2（%）
Purity(HPLC) 99-100（%）
Oxygen by Elemental Analysi 18.7-19.3（%）
Carbon by Elemental Analysis 56.5-57.5（%）
Appearance（D127636) White to off-white solid
NMR spectrum Conforms to Structure

 质量标准

质检证书（CoA,COO,BSE/TSE 和分析图谱)

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批号(Lot Number) 证书类型 日期 货号
B1526013 分析证书 24-06-12 D127636

可替换产品

  1. Dolutegravir (GSK1349572)
    Dolutegravir (GSK1349572)

    ¥995.90

参考文献

1. Ozono S et al..  (2020)  Super-rapid quantitation of the production of HIV-1 harboring a luminescent peptide tag..  J Biol Chem,  295  (37): (13023-13030).  [PMID:32719008]

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