Efavirenz

製品コードS4685 バッチS468501

印刷

化学情報

Chemical Structure Synonyms DMP-266 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C14H9ClF3NO2
分子量 315.67 CAS No. 154598-52-4
Solubility (25°C)* 体外 DMSO 63 mg/mL (199.57 mM)
Ethanol 63 mg/mL (199.57 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 Efavirenz is a synthetic non-nucleoside reverse transcriptase (RT) inhibitor with antiviral activity.
in vitro Efavirenz has direct inhibitory effect on the mitochondrial respiratory function of cultured glioblastoma and differentiated neuroblastoma cell lines[2]. ER stress markers, including CHOP and GRP78 expression (both protein and mRNA), phosphorylation of eIF2a, and presence of the spliced form of XBP1 are upregulated. Efavirenz also enhances cytosolic Ca2+ content and induced morphological changes in the ER suggestive of ER stress. This response is greatly attenuated in cells with altered mitochondrial function (Rho). The effects of Efavirenz on the ER, and particularly in regard to the mitochondrial involvement, differs from those elicited by a standard pharmacological ER stressor[3].
in vivo Efavirenz leads to arterial stiffening but, for the dose and duration tested, did not lead to elevated plaque progression in ApoE(-/-) mice[4].

プロトコル(参考用のみ)

細胞アッセイ 細胞株 human glioma U-251MG, neuroblastoma SH-SY5Y (ATCC CRL-2266) cells
濃度 10 μM, 25μM
反応時間 1 h
実験の流れ

The OCR(O2 consumption rate) is measured in SH-SY5Y and U-251MG cells exposed to vehicle, 10 μM efavirenz or 25 μM efavirenz for 1 h.
動物実験 動物モデル Sprague-Dawley rats
投薬量 10, 40, and 160 mg/kg(oral); 2, 5, 10, 15 mg/kg(i.v.)
投与方法 i.v. or p.o. administration

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：

Chemical inhibition of DPP9 sensitizes the CARD8 inflammasome in HIV-1-infected cells [ Nat Chem Biol, 2023, 19(4):431-439] PubMed: 36357533
Biological and Structural Analyses of New Potent Allosteric Inhibitors of HIV-1 Integrase [ Antimicrob Agents Chemother, 2023, 67(7):e0046223] PubMed: 37310224
Revealing viral and cellular dynamics of HIV-1 at the single-cell level during early treatment periods [ Cell Rep Methods, 2023, 3(6):100485] PubMed: 37426753
ATAD3A oligomerization promotes neuropathology and cognitive deficits in Alzheimer's disease models [ Nat Commun, 2022, 13(1):1121] PubMed: 35236834
Memory CD4+ T cells that co-express PD1 and CTLA4 have reduced response to activating stimuli facilitating HIV latency [ Cell Rep Med, 2022, 3(10):100766] PubMed: 36198308
Unexpected similarity between HIV-1 reverse transcriptase and tumor necrosis factor binding sites revealed by computer vision [ J Cheminform, 2021, 13(1):90] PubMed: 34814950
Reverse transcriptase inhibition potentiates target therapy in BRAF-mutant melanomas: effects on cell proliferation, apoptosis, DNA-damage, ROS induction and mitochondrial membrane depolarization [ Cell Commun Signal, 2020, 18(1):150] PubMed: 32933538
Altered Gut Microbiome under Antiretroviral Therapy: Impact of Efavirenz and Zidovudine [ ACS Infect Dis, 2020, 10.1021/acsinfecdis.0c00536] PubMed: 33346662
Conformational Changes in HIV-1 Reverse Transcriptase that Facilitate Its Maturation. [ Structure, 2019, 27(10):1581-1593] PubMed: 31471129
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

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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