Efavirenz

製品コードS4685 バッチS468502

印刷

化学情報

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

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	7.500mg/ml (23.76mM)	Taking the 1 mL working solution as an example, add 50 μL of 150 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	7.500mg/ml (23.76mM)	Taking the 1 mL working solution as an example, add 50 μL of 150 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

* <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. This compound 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 this chemical 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 this compound 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

参考

https://pubmed.ncbi.nlm.nih.gov/20039714/
https://pubmed.ncbi.nlm.nih.gov/25925594/
https://pubmed.ncbi.nlm.nih.gov/23792026/

https://pubmed.ncbi.nlm.nih.gov/26050957/

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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：

Broad synergistic antiviral efficacy between a novel elite controller-derived dipeptide and antiretrovirals against drug-resistant HIV-1 [ Front Cell Infect Microbiol, 2024, 14:1334126]	PubMed: 38915925
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

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。