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Elsulfavirine {[allProObj[0].p_purity_real_show]}

货号:A1251631 同义名: R-1206 Ambeed 开学季,买赠积分,赢豪礼

Elsulfavirine 是一种 HIV-1 逆转录酶抑制剂,也是一种新型抗 HIV 活性分子。Elsulfavirine 主要用于 HIV 感染的治疗研究。

Elsulfavirine 化学结构 CAS号:868046-19-9
Elsulfavirine 化学结构
CAS号:868046-19-9
Elsulfavirine 3D分子结构
CAS号:868046-19-9
Elsulfavirine 化学结构 CAS号:868046-19-9
Elsulfavirine 3D分子结构 CAS号:868046-19-9
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Elsulfavirine 纯度/质量文件 产品仅供科研

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Elsulfavirine 生物活性

描述 HIV-1 reverse transcriptase (RT) is a multifunctional enzyme that is targeted by nucleoside analogs (NRTIs) and non-nucleoside RT inhibitors (NNRTIs). NNRTIs are allosteric inhibitors of RT, and constitute an integral part of several highly active antiretroviral therapy regimens. Under selective pressure, HIV-1 acquires resistance against NNRTIs primarily by selecting mutations around the NNRTI pocket[2]. NNRTIs interact with HIV-1 RT by binding to a single site on the p66 subunit of the p66/p51 heterodimeric enzyme, termed the NNRTI-binding pocket (NNRTI-BP). This binding interaction results in both short-range and long-range distortions of RT structure[3]. NNRTIs are extensively metabolized in the liver through cytochrome P450, leading to pharmacokinetic interactions with compounds utilizing the same metabolic pathway, particularly PIs, whose plasma levels are altered in the presence of NNRTIs. NNRTIs are drugs with a low genetic barrier, i.e. a single mutation in RT genoma induces a high-level of phenotypic resistance, preventing the use of NNRTIs as monotherapy[4].Combinations of two NNRTIs have shown additive or synergistic inhibitory effects on the HIV-1 reverse transcriptase activity and the viral replication of HIV-1 in vitro, although antagonistic effects have also been described. When nevirapine and efavirenz were administered in combination, the exposure to efavirenz was decreased due to induction of metabolism by nevirapine. When compared with single NNRTI regimens, dual NNRTI regimens showed similar but not superior results with regard to virological and immunological success in treatment-naive and pretreated HIV-1-infected patients[5].Elsulfavirine (Elpida®) is a new-generation non-nucleoside reverse transcriptase inhibitor (NNRTI) being developed by Viriom for the treatment and prevention of human immunodeficiency virus (HIV) infections. It is the prodrug of the active compound VM-1500A, a small molecule selective NNRTI, which prevents HIV replication[6].

Elsulfavirine 参考文献

[1]Al-Salama ZT. Elsulfavirine: First Global Approval. Drugs. 2017 Oct;77(16):1811-1816. doi: 10.1007/s40265-017-0820-3. PMID: 28940154.

[2] R S K Vijayan,et al. Molecular dynamics study of HIV-1 RT-DNA-nevirapine complexes explains NNRTI inhibition and resistance by connection mutations. Proteins. 2014 May;82(5):815-29.

[3] Nicolas Sluis-Cremer,et al. Conformational changes in HIV-1 reverse transcriptase induced by nonnucleoside reverse transcriptase inhibitor binding. Curr HIV Res. 2004 Oct;2(4):323-32.

[4] V Joly, P Yeni. Non-nucleoside reverse transcriptase inhibitors. Ann Med Interne (Paris). 2000 Jun;151(4):260-7.

[5]Bregt S Kappelhoff,et al. Should non-nucleoside reverse transcriptase inhibitors be combined? Drugs R D. 2005;6(2):61-9.

[6]Zaina T Al-Salama. Elsulfavirine: First Global Approval. Drugs. 2017 Oct;77(16):1811-1816.

Elsulfavirine 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.59mL

0.32mL

0.16mL

7.95mL

1.59mL

0.79mL

15.89mL

3.18mL

1.59mL

Elsulfavirine 技术信息

CAS号868046-19-9
分子式C24H17BrCl2FN3O5S
分子量 629.282
别名 R-1206
运输蓝冰
存储条件

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 60 mg/mL(95.35 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

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