Tenofovir Disoproxil Fumarate

製品コードS1400 バッチS140001

化学情報

	Synonyms	GS 1278, Tenofovir DF	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₁₉H₃₀N₅O₁₀P.C₄H₄O₄
	分子量	635.51	CAS No.	202138-50-9
Solubility (25°C)*	体外	DMSO	128 mg/mL (201.41 mM)
		Ethanol	44 mg/mL (69.23 mM)
		Water	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	Tenofovir Disoproxil Fumarate belongs to a class of antiretroviral drugs, it inhibits the activity of HIV reverse transcriptase by competing with the natural substrate deoxyadenosine 5’-triphosphate and, after incorporation into DNA, by DNA chain termination.
in vitro	Tenofovir is eliminated from systemic circulation renally through a combination of glomerular filtration and active tubular secretion. Tenofovir is not a substrate for human organic cation transporter type 1 (hOCT1) or hOCT2. Tenofovir accumulates to fivefold lower levels in MRP4-overexpressing cells, and its accumulation could be increased by an MRP inhibitor. ^[1] Tenofovir produces no significant changes in mitochondrial DNA (mtDNA) levels in human hepatoblastoma (HepG2) cells, skeletal muscle cells (SkMCs), or renal proximal tubule epithelial cells. Tenofovir elevates lactate production by less than 20% in HepG2 cells or SkMCs. ^[2] Tenofovir is efficiently phosphorylated to tenofovir diphosphate (TFV-DP) in both HepG2 cells and primary human hepatocytes. Tenofovir has a 50% effective concentration of 1.1 mM against HBV in cell-based assays, and potency is improved > 50-fold by the addition of bis-isoproxil progroups. Tenofovir has previously demonstrated full activity against lamivudine-resistant HBV in vitro and clinically. ^[3] Tenofovir inhibits the proliferation of liver-derived HepG2 cells and normal skeletal muscle cells with CC(50) values of 398 μM and 870 μM, respectively. Tenofovir shows substantially weaker effects on proliferation and viability of renal proximal tubule epithelial cells than cidofovir, a related nucleotide analog with the potential to induce renal tubular dysfunction. ^[4]

製品説明

Tenofovir Disoproxil Fumarate belongs to a class of antiretroviral drugs, it inhibits the activity of HIV reverse transcriptase by competing with the natural substrate deoxyadenosine 5’-triphosphate and, after incorporation into DNA, by DNA chain termination.

in vitro

Tenofovir is eliminated from systemic circulation renally through a combination of glomerular filtration and active tubular secretion. Tenofovir is not a substrate for human organic cation transporter type 1 (hOCT1) or hOCT2. Tenofovir accumulates to fivefold lower levels in MRP4-overexpressing cells, and its accumulation could be increased by an MRP inhibitor. ^[1] Tenofovir produces no significant changes in mitochondrial DNA (mtDNA) levels in human hepatoblastoma (HepG2) cells, skeletal muscle cells (SkMCs), or renal proximal tubule epithelial cells. Tenofovir elevates lactate production by less than 20% in HepG2 cells or SkMCs. ^[2] Tenofovir is efficiently phosphorylated to tenofovir diphosphate (TFV-DP) in both HepG2 cells and primary human hepatocytes. Tenofovir has a 50% effective concentration of 1.1 mM against HBV in cell-based assays, and potency is improved > 50-fold by the addition of bis-isoproxil progroups. Tenofovir has previously demonstrated full activity against lamivudine-resistant HBV in vitro and clinically. ^[3] Tenofovir inhibits the proliferation of liver-derived HepG2 cells and normal skeletal muscle cells with CC(50) values of 398 μM and 870 μM, respectively. Tenofovir shows substantially weaker effects on proliferation and viability of renal proximal tubule epithelial cells than cidofovir, a related nucleotide analog with the potential to induce renal tubular dysfunction. ^[4]

プロトコル(参考用のみ)

細胞アッセイ	細胞株	VK2 cells
	濃度	450 μM or 1,350 μM
	反応時間	15 min to 12 h
	実験の流れ	VK2 cells were exposed to TDF (90 μM or 450 μM) and TFV (450 μM or 1,350 μM) in serum-free RPMI 1640 at 37°C for 15 min to 12 h. At different times postexposure, cells were washed with ice-cold PBS and metabolites were extracted overnight in 70% (vol/vol) methanol, followed by centrifugation at 18,000 × g for 10 min at 4°C.
動物実験	動物モデル	BALB/c mice
	投薬量	50, 500, or 1000 mg/kg
	投与方法	oral administration

参考

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カスタマーフィードバック

: Data from [Data independently produced by , , Sci Transl Med, 2014, 6(262): 262ra157 ]

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：

IKAROS expression drives the aberrant metabolic phenotype of macrophages in chronic HIV infection [ Clin Immunol, 2024, 260:109915]	PubMed: 38286172
Acute antagonism in three-drug combinations for vaginal HIV prevention in humanized mice [ Sci Rep, 2023, 13(1):4594]	PubMed: 36944714
Establishment and characterization of a new cell culture system for hepatitis B virus replication and infection [ Virol Sin, 2022, S1995-820X(22)00081-5]	PubMed: 35568375
Reduction of CD8 T cell functionality but not inhibitory capacity by integrase inhibitors [ J Virol, 2022, JVI0173021]	PubMed: 35019724
Female Genital Fibroblasts Diminish the In Vitro Efficacy of PrEP against HIV [ Viruses, 2022, 14(8)1723]	PubMed: 36016345
Impaired differentiation of small airway basal stem/progenitor cells in people living with HIV [ Sci Rep, 2022, 12(1):2966]	PubMed: 35194053
Preclinical characterization of AB-506, an inhibitor of HBV replication targeting the viral core protein [ Antiviral Res, 2021, 197:105211]	PubMed: 34826506
People with HIV-1 demonstrate type 1 interferon refractoriness associated with upregulated USP18 [ J Virol, 2021, JVI.01777-20]	PubMed: 33658340
Altered Gut Microbiome under Antiretroviral Therapy: Impact of Efavirenz and Zidovudine [ ACS Infect Dis, 2020, 10.1021/acsinfecdis.0c00536]	PubMed: 33346662
Reciprocal Modulation of Antiretroviral Drug and Steroid Receptor Function In Vitro. [ Antimicrob Agents Chemother, 2019, 64(1)]	PubMed: 31658973

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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