Darunavir Ethanolate

製品コードS1620 バッチS162005

化学情報

	Synonyms	TMC-114, UIC 94017	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₂₇H₃₇N₃O₇S.C₂H₅OH
	分子量	593.73	CAS No.	635728-49-3
Solubility (25°C)*	体外	DMSO	100 mg/mL (168.42 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	Darunavir Ethanolate (TMC-114, UIC 94017) is a nonpeptidic HIV protease inhibitor, used to treat HIV infection.
in vitro	Darunavir displays potent activity against HIV strains resistant to other available protease inhibitor. Darunavir inhibits P-glycoprotein-mediated efflux of calcein-acetoxymethyl ester in L-MDR1 cells with the inhibitory potency of 121 mM. ^[1] Darunavir is a protein inhibits that mimics the phenylalanine sequences at positions 167 and 168 of the gag-pol polypeptide and binds to the active sites of the HIV protease, thereby inhibiting its activity. Darunavir blocks the infectivity and replication of each of the HIV-1 variants at concentrations up to 5 μM. Darunavir shows strong ARV activity against a selected panel of 19 recombinant clinical isolates carrying multiple protease mutations conferring resistance to an average of five other protien inhibitors. Darunavir inhibits 75% of 1501 PI-resistant viruses tested with a half maximal effective concentration (EC50) of < 10 nM. ^[2]

製品説明

Darunavir Ethanolate (TMC-114, UIC 94017) is a nonpeptidic HIV protease inhibitor, used to treat HIV infection.

in vitro

Darunavir displays potent activity against HIV strains resistant to other available protease inhibitor. Darunavir inhibits P-glycoprotein-mediated efflux of calcein-acetoxymethyl ester in L-MDR1 cells with the inhibitory potency of 121 mM. ^[1] Darunavir is a protein inhibits that mimics the phenylalanine sequences at positions 167 and 168 of the gag-pol polypeptide and binds to the active sites of the HIV protease, thereby inhibiting its activity. Darunavir blocks the infectivity and replication of each of the HIV-1 variants at concentrations up to 5 μM. Darunavir shows strong ARV activity against a selected panel of 19 recombinant clinical isolates carrying multiple protease mutations conferring resistance to an average of five other protien inhibitors. Darunavir inhibits 75% of 1501 PI-resistant viruses tested with a half maximal effective concentration (EC50) of < 10 nM. ^[2]

プロトコル(参考用のみ)

参考

カスタマーフィードバック

: , , Drug Metab Dispos, 2016, 44(3):398-408.

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：

Reduction of CD8 T cell functionality but not inhibitory capacity by integrase inhibitors [ J Virol, 2022, JVI0173021]	PubMed: 35019724
Integrative multiomics and in silico analysis revealed the role of ARHGEF1 and its screened antagonist in mild and severe COVID-19 patients [ J Cell Biochem, 2022, 10.1002/jcb.30213]	PubMed: 35037717
Characterization of fluorescent probe substrates to develop an efficient high-throughput assay for neonatal hepatic CYP3A7 inhibition screening [ Sci Rep, 2021, 11(1):19443]	PubMed: 34593846
Discovery of M Protease inhibitors encoded by SARS-CoV-2 [ Antimicrob Agents Chemother, 2020, AAC.00872-20]	PubMed: 32669265
Effect of HIV infection and antiretroviral therapy on immune cellular functions. [ JCI Insight, 2019, 4(12)]	PubMed: 31217351
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
Solitary inhibition of the breast cancer resistance protein (BCRP) efflux transporter results in a clinically significant drug-drug interaction with rosuvastatin by causing up to a two-fold increase in statin exposure [Elsby R, et al. Drug Metab Dispos, 2015, 44(3):398-408]	PubMed: 26700956
Sequence-Specific Alterations of Epitope Production by HIV Protease Inhibitors. [Kourjian G, et al. J Immunol, 2014, 192(8):3496-506]	PubMed: 24616479

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。

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