Cas(1051375-16-6), Dolutegravir (GSK1349572)-阿拉丁试剂, GSK1349572;度鲁特韦,Dolutegravir (GSK1349572),

货号 (SKU)	包装规格	是否现货
D127636-5mg	5mg	现货
D127636-10mg	10mg	现货
D127636-50mg	50mg	现货

货号 (SKU)

包装规格

是否现货

价格

数量

D127636-5mg

5mg

现货

D127636-10mg

10mg

现货

D127636-50mg

50mg

现货

基本描述

别名	GSK1349572;度鲁特韦
英文别名	Dolutegravir;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	≥99%
英文名称	Dolutegravir (GSK1349572)
生化机理	Dolutegravir (DTG, GSK1349572) is an integrase inhibitor being developed for the treatment of human immunodeficiency virus (HIV)-1 infection by GlaxoSmithKline (GSK) on behalf of Shionogi-ViiV Healthcare LLC. Dolutegravir (DTG, GSK1349572) is metabolized primarily by uridine diphosphate glucuronyltransferase (μgT)1A1, with a minor role of cytochrome P450 (CYP)3A, and with renal elimination of unchanged drμg being extremely low (< 1% of the dose). Fifty-three percent of the total oral dose is excreted unchanged in the feces but it is unknown if all or part of this is due to unabsorbed drμg or some percentage of biliary excretion of the glucuronide conjμgate which can be further degraded to form the parent compound in the gut lumen. The current Food and Drμg Administration (FDA) draft guidance for renal impairment studies states that a pharmacokinetic (PK) study in patients with renal impairment should be conducted even for those drμgs primarily metabolized or secrete.Potent\xa0HIV integrase inhibitor (IC 50 = 2.7 nM for HIV-1 integrase-catalyzed strand transfer in vitro) . Inhibits HIV-1 viral replication (EC 50 = 0.51 nM) in peripheral blood mononuclear cells (PBMCs).
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.

名称和标识符

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
PubChem CID	54726191
分子量	419.38

数据库链接

PubChem CID	54726191
Wikipedia	Dolutegravir
CAS Registry No.	1051375-16-6
ChEMBL Ligand	CHEMBL1229211
DrugBank Ligand	DB08930
RCSB PDB Ligand	DLU
DrugCentral Ligand	4805

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).

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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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