Elsulfavirine
CAS No. : 868046-19-9
(Synonyms: R-1206)
Price and Availability of
CAS No. : 868046-19-9
| Size | Price | Stock |
|---|---|---|
| 5mg | $195 | In-stock |
| 10mg | $310 | In-stock |
| 25mg | $620 | In-stock |
| 50mg | $930 | In-stock |
| 100mg | $1395 | In-stock |
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| Cat. No. : | HY-109056 |
| M.Wt: | 629.28 |
| Formula: | C24H17BrCl2FN3O5S |
| Purity: | >98 % |
| Solubility: | DMSO : 62.5 mg/mL (ultrasonic) |
Introduction of
868046-19-9
:
Elsulfavirine (treated at 10 μM for 12 h) significantly inhibits high glucose-induced translocation of SCAP from the endoplasmic reticulum to the Golgi apparatus in Huh7 cells, downregulates the mRNA expression levels of SREBP-1 downstream lipogenic target genes FASN, ACACA, SCD, and GPAM, reduces the number of intracellular lipid droplets, and inhibits high glucose-induced intracellular lipid accumulation[2].
Elsulfavirine (10 μM; 8 h treatment) significantly inhibits the conversion of 14C-glucose to triglycerides and fatty acids in Huh7 cells, and blocks the de novo lipid synthesis process in cells[2].
VM-1500A, the active metabolite of Elsulfavirine (with a serum-corrected EC50 of approximately 13.8 nM), potently inhibits the replication of HIV-1 clinical isolates in in vitro cell models[3]. In Vivo:Elsulfavirine (10 mg/kg; oral administration; once daily; 20 days) significantly inhibits hepatocellular carcinoma tumor growth, reduces the expression of proliferation marker Ki-67 in tumor tissues, increases the apoptosis level of tumor cells, and downregulates the protein expression of SREBP-1, FASN and ACLY in a subcutaneous xenograft hepatocellular carcinoma model of Huh7 cells in nude mice[2].
Combination treatment with Elsulfavirine (10 mg/kg; oral administration; once daily for 20 consecutive days) and Lenvatinib (HY-10981) (administered via the same regimen as Elsulfavirine) exerts a synergistic inhibitory effect on hepatocellular carcinoma tumor growth in a nude mouse subcutaneous xenograft model of Huh7 cells, and achieves a better efficacy than monotherapy[2].
Elsulfavirine (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 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 and Lenvatinib (HY-10981) produces a synergistic anti-tumor effect. Elsulfavirine is converted into the active metabolite VM1500A in vivo, blocks the DNA polymerase activity of reverse transcriptase, and inhibits HIV-1 replication. Elsulfavirine exhibits a Ki of 1960 nM-52400 nM against human carbonic anhydrase isoforms including I, VII, VI, VA, VB, IX, XIII, XIV. Elsulfavirine is used in studies related to HIV-1 infection and liver cancer[1][2][3][4].
In Vitro:Elsulfavirine (10 μM; 1 h pre-treatment) significantly blocks high glucose-induced interaction between ADSL and INSIG1/2 in Huh7 cells, inhibits the cleavage activation and nuclear translocation of SREBP-1, blocks SRE-driven luciferase transcriptional activity, and suppresses the activation of the SREBP lipogenic pathway[2].Elsulfavirine (treated at 10 μM for 12 h) significantly inhibits high glucose-induced translocation of SCAP from the endoplasmic reticulum to the Golgi apparatus in Huh7 cells, downregulates the mRNA expression levels of SREBP-1 downstream lipogenic target genes FASN, ACACA, SCD, and GPAM, reduces the number of intracellular lipid droplets, and inhibits high glucose-induced intracellular lipid accumulation[2].
Elsulfavirine (10 μM; 8 h treatment) significantly inhibits the conversion of 14C-glucose to triglycerides and fatty acids in Huh7 cells, and blocks the de novo lipid synthesis process in cells[2].
VM-1500A, the active metabolite of Elsulfavirine (with a serum-corrected EC50 of approximately 13.8 nM), potently inhibits the replication of HIV-1 clinical isolates in in vitro cell models[3]. In Vivo:Elsulfavirine (10 mg/kg; oral administration; once daily; 20 days) significantly inhibits hepatocellular carcinoma tumor growth, reduces the expression of proliferation marker Ki-67 in tumor tissues, increases the apoptosis level of tumor cells, and downregulates the protein expression of SREBP-1, FASN and ACLY in a subcutaneous xenograft hepatocellular carcinoma model of Huh7 cells in nude mice[2].
Combination treatment with Elsulfavirine (10 mg/kg; oral administration; once daily for 20 consecutive days) and Lenvatinib (HY-10981) (administered via the same regimen as Elsulfavirine) exerts a synergistic inhibitory effect on hepatocellular carcinoma tumor growth in a nude mouse subcutaneous xenograft model of Huh7 cells, and achieves a better efficacy than monotherapy[2].
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