867365-40-0
Chemical Structure
Elsulfavirine sodium
Synonym(s): R-1206 sodium
- CAS No.: 867365-40-0
- Formula:C24H17BrCl2FN3NaO5S
- Molecular Weight:652.27
InChIKey: QFVVGQLPAJYBII-UHFFFAOYSA-N
SMILES: N#CC1=CC(Cl)=CC(OC2=C(F)C(CC(NC3=CC=C(S(=O)(NC(CC)=O)=O)C=C3Cl)=O)=CC=C2Br)=C1.[Na]
Biological Activity: Elsulfavirine sodium (R-1206) is an orally active human carbonic anhydrase (carbonic anhydrase, CA) inhibitor and an allosteric inhibitor of HIV-1 non-nucleoside reverse transcriptase (NNRT). Elsulfavirine sodium also targets and blocks the interaction between adenylosuccinate lyase (ADSL) and insulin-induced gene proteins INSIG1/2, blocks SREBP-1-mediated de novo lipid synthesis, and inhibits the proliferation of liver cancer cells. The combination of Elsulfavirine sodium and Lenvatinib (HY-10981) produces a synergistic anti-tumor effect. Elsulfavirine sodium is converted into the active metabolite VM1500A in vivo, blocks the DNA polymerase activity of reverse transcriptase, and inhibits HIV-1 replication. Elsulfavirine sodium exhibits a Ki of 1960 nM-52400 nM against human carbonic anhydrase isoforms including I, VII, VI, VA, VB, IX, XIII, XIV. Elsulfavirine sodium is used in studies related to HIV-1 infection and liver cancer[1][2][3][4].
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Elsulfavirine sodium | Elsulfavirine sodium (R-1206) is an orally active human carbonic anhydrase (carbonic anhydrase, CA) inhibitor and an allosteric inhibitor of HIV-1 non-nucleoside reverse transcriptase (NNRT). Elsulfavirine sodium also targets and blocks the interaction between adenylosuccinate lyase (ADSL) and insulin-induced gene proteins INSIG1/2, blocks SREBP-1-mediated de novo lipid synthesis, and inhibits the proliferation of liver cancer cells. The combination of Elsulfavirine sodium and Lenvatinib (HY-10981) produces a synergistic anti-tumor effect. Elsulfavirine sodium is converted into the active metabolite VM1500A in vivo, blocks the DNA polymerase activity of reverse transcriptase, and inhibits HIV-1 replication. Elsulfavirine sodium exhibits a Ki of 1960 nM-52400 nM against human carbonic anhydrase isoforms including I, VII, VI, VA, VB, IX, XIII, XIV. Elsulfavirine sodium is used in studies related to HIV-1 infection and liver cancer. | |||||||||||||||||||||
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- [1]. Supuran CT, et al. Biochemical profiling of anti-HIV prodrug Elsulfavirine (Elpida®) and its active form VM1500A against a panel of twelve human carbonic anhydrase isoforms. J Enzyme Inhib Med Chem. 2021;36(1):1056-1060. [Content Brief]
- [2]. Duan Y, et al. INSIG1/2 succination mediated by the moonlighting function of ADSL promotes lipogenesis and liver tumorigenesis[J]. Nature Communications, 2026.
- [3]. Wang Y, et al. Current and emerging non-nucleoside reverse transcriptase inhibitors (NNRTIs) for HIV-1 treatment[J]. Expert opinion on drug metabolism & toxicology, 2019, 15(10): 813-829.
- [4]. Luan B, et al. Targeting proteases for treating COVID-19[J]. Journal of proteome research, 2020, 19(11): 4316-4326.
Keywords
