依法韦仑 T2393

Product Introduction
Bioactivity


英文名: Efavirenz

描述: Efavirenz (DMP 266) 是一种人类免疫缺陷病毒 1 非核苷类似物逆转录酶抑制剂。它也是一种野生型HIV-1 RT 抑制剂，Ki 为 2.93 nM，有效抑制 HIV-1 复制，IC95为 1.5 nM。

细胞实验: The OCR(O2 consumption rate) is measured in SH-SY5Y and U-251 mg cells exposed to vehicle, 10 μM efavirenz or 25 μM efavirenz for 1 h. (Only for Reference)

激酶实验: Recombinant RT enzymes are expressed, purified, and assessed for inhibition by Efavirenz (L-743726). Ki and Kii values are determined for each enzyme tested. The wild-type RT exhibited exclusively noncompetitive inhibition kinetics (data not shown), and, therefore, the Ki and Kii values are identical. Pure noncompetitive inhibition is not assumed for the mutant enzymes, and, hence, the values of both Ki and Kii are obtained from the linear mixed-type inhibition equation. The two- to threefold differences between the Ki and Kii values probably reflect a small contribution of competitive inhibition with the mutant RTs[1].

体外活性: 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].

体内活性: Efavirenz导致动脉硬化，但在所测试的剂量和持续时间内，并未导致ApoE(-/-)小鼠[4]的斑块进展增加。

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: Methanol : 10 mM
H2O : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 60 mg/mL (190.07 mM)


关键字: HIV | inhibit | DMP-266 | Reverse Transcriptase | DMP266 | Autophagy | Human immunodeficiency virus | L743726 | L 743726 | Efavirenz | Inhibitor

相关产品: NBD-557 | Bellidifolin | Oleanolic Acid | Pomolic acid | Islatravir | UC-781 | Etravirine | lavendustin B | Dolutegravir | 16beta,17-Dihydroxy-ent-kaurane-19-oic acid

相关库: Drug Repurposing Compound Library | Anti-COVID-19 Compound Library | Approved Drug Library | Anti-Cancer Drug Library | Bioactive Compounds Library Max | Anti-Cancer Clinical Compound Library | Inhibitor Library | Anti-Cancer Approved Drug Library | EMA Approved Drug Library | Anti-Viral Compound Library

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