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Elsulfavirine

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Chemical Structure| 868046-19-9 同义名 : R-1206
CAS号 : 868046-19-9
货号 : A1251631
分子式 : C24H17BrCl2FN3O5S
纯度 : 97%
分子量 : 629.282
MDL号 : MFCD32215300
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
动物实验配方：
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].
实验方案
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
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.