Dolutegravir Sodium

製品コードS4642 バッチS464204

化学情報

	Synonyms	GSK-1349572A	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₂₀H₁₉F₂N₃O₅.Na
	分子量	441.36	CAS No.	1051375-19-9
Solubility (25°C)*	体外	DMSO	5 mg/mL (11.32 mM)
		Water	Insoluble
		Ethanol	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Dolutegravir Sodium (GSK-1349572A) is a HIV integrase inhibitor with IC50 of 2.7 nM.
in vitro	Dolutegravir(S/GSK1349572) inhibits HIV-1 integrase-catalyzed strand transfer with a 50% inhibitory concentration (IC50) of 2.7 nM. S/GSK1349572 inhibits both the HIV integration reaction strand transfer step in vitro and HIV replication in cells with similar potencies. The inhibitor has no effect on total viral DNA synthesis in infected cells but blocks the integration of viral DNA into host DNA with the same potency as its antiviral effect^[1].
in vivo	The bioavailability of dolutegravir was high when administered as a solution, but was limited by dissolution rate or solubility when administered as a suspension. Dolutegravir is the major circulating component in mice, rats, and monkeys, with direct ether glucuronidation shown to be the primary biotransformation pathway. Dolutegravir is primarily eliminated via the feces either unabsorbed or by hydrolysis of the glucuronide or glucose conjugate^[2].

プロトコル(参考用のみ)

細胞アッセイ	細胞株	MT-4 cells
	濃度	0.16, 0.8, 4, 20 nM
	反応時間	6 h or 18 h
	実験の流れ	In vitro growth inhibition (cytotoxicity) studies are conducted with S/GSK1349572 in proliferating human leukemic and lymphomic cell lines (IM-9, U-937, MT-4, and Molt-4) as well as in stimulated and unstimulated human PBMCs. ATP levels are quantified by using the CellTiter-Glo luciferase reagent to measure the ability of a compound to inhibit cell growth as an indicator of the compound's potential for cytotoxicity.
動物実験	動物モデル	male Crl:CD (SD) rats, cynomolgus monkeys,
	投薬量	5 mg/kg for i.v.; 5, 50, 100, and 250 mg/kg(rats, oral); 3, 10, and 50 mg/kg(monkeys, oral)
	投与方法	i.v./oral administration

参考

カスタマーフィードバック

: Data from [Data independently produced by , , Retrovirology, 2015, 12:10]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Spectrum of Activity of Raltegravir and Dolutegravir Against Novel Treatment-Associated Mutations In HIV-2 Integrase: A Phenotypic Analysis Using An Expanded Panel of Site-Directed Mutants [ J Infect Dis, 2022, jiac037]	PubMed: 35134180
Inhibition of Adipose Tissue Beiging by HIV Integrase Inhibitors, Dolutegravir and Bictegravir, Is Associated with Adipocyte Hypertrophy, Hypoxia, Elevated Fibrosis, and Insulin Resistance in Simian Adipose Tissue and Human Adipocytes [ Cells, 2022, 11(11)1841]	PubMed: 35681536
Reduction of CD8 T cell functionality but not inhibitory capacity by integrase inhibitors [ J Virol, 2022, JVI0173021]	PubMed: 35019724
Effects of Injection Volume and Route of Administration on Dolutegravir In Situ Forming Implant Pharmacokinetics [ Pharmaceutics, 2022, 14(3)615]	PubMed: 35335991
Impact of combinations of clinically observed HIV integrase mutations on phenotypic resistance to integrase strand transfer inhibitors (INSTIs): a molecular study [ J Antimicrob Chemother, 2022, dkab498]	PubMed: 35061879
Activation of PERK-ATF4-CHOP pathway as a novel therapeutic approach for efficient elimination of HTLV-1-infected cells. [ Blood Adv, 2020, 12;4(9):1845-1858]	PubMed: 32369565
HIV-1 Subtype C with PYxE Insertion Has Enhanced Binding of Gag-p6 to Host Cell Protein ALIX and Increased Replication Fitness. [ J Virol, 2019, 93(9)]	PubMed: 30760577
Interactions of Prototype Foamy Virus Capsids with Host Cell Polo-Like Kinases Are Important for Efficient Viral DNA Integration [ PLoS Pathog, 2016, 12(8):e1005860]	PubMed: 27579920

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。