2. Anti-infection Others Metabolic Enzyme/Protease
  3. HIV Drug Intermediate Reverse Transcriptase Carbonic Anhydrase
  4. 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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Elsulfavirine sodium

Elsulfavirine sodium Chemical Structure

CAS No. : 867365-40-0

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Elsulfavirine sodium Related Antibodies

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CA CA I CA Ⅱ CA IX CA XII CA VII CA VI CA VA CA VB CA XIII CA XIV

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Description

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].

IC50 & Target[1][2][3][4]

HIV-1

 

hCA I

52400 nM (Ki)

hCA II

12500 nM (Ki)

CA VA

4290 nM (Ki)

CA VB

14200 nM (Ki)

CA VI

5670 nM (Ki)

hCA IX

2390 nM (Ki)

hCA IX

6650 nM (Ki)

hCA XII

9801 nM (Ki)

CA XIII

4820 nM (Ki)

CA XIV

1960 nM (Ki)

In Vitro

Elsulfavirine sodium (10 μM; 1 h) 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 sodium (10 μM; 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 sodium (10 μM; 8 h) 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 sodium (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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Elsulfavirine sodium Related Antibodies

Western Blot Analysis[2]

Cell Line: Huh7 human hepatocellular carcinoma cells
Concentration: 10 μM (elsulfavirine), 20 μM (tezacaftor), 100 μM (pyrithioxin) as control compounds
Incubation Time: 1 h pre-treatment before high-glucose stimulation
Result: Markedly suppressed the cleavage and activation of SREBP-1 induced by high glucose in Huh7 cells, while it did not affect the phosphorylation of ADSL at S407 mediated by PKCε.
In contrast, the control compounds tezacaftor and pyrithioxin showed no significant inhibitory effect on SREBP-1 cleavage.

Real Time qPCR[2]

Cell Line: Huh7 human hepatocellular carcinoma cells
Concentration: 10 μM
Incubation Time: 12 h co-treatment with high glucose
Result: Significantly downregulated the high glucose-induced mRNA expression of SREBP-1 downstream lipogenic target genes, including FASN, ACACA, SCD and GPAM, in Huh7 cells.
In Vivo

Elsulfavirine (10 mg/kg; oral administration; once daily; 20 days) sodium 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) sodium and Lenvatinib (HY-10981) (administered via the same regimen as Elsulfavirine sodium) 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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male athymic BALB/c nude mice (6-week-old) with subcutaneous xenograft hepatocellular carcinoma (HCC) model established by subcutaneous inoculation of 1 × 106 Huh7 cells in the right flank[2]10 mg/kg
Dosage: 10 mg/kg
Administration: Administered via gavage once daily for 20 consecutive days, starting on day 7 after tumor cell inoculation; with 10 mg/kg lenvatinib or not.
Result: As for monotherapy:
Significantly inhibited the growth of HCC xenografts in nude mice, reduced the expression of proliferation marker Ki-67 in tumor tissues, increased the level of tumor cell apoptosis, and downregulated the protein expression of SREBP-1 and lipogenesis-related enzymes including FASN and ACLY in tumor tissues, compared with the vehicle control group.
As for combination:
Exerted a synergistic inhibitory effect on HCC tumor growth, with a more significant reduction in tumor volume and weight, lower Ki-67 expression, higher tumor cell apoptosis, and more pronounced downregulation of SREBP-1, FASN and ACLY in tumor tissues, compared with the Elsulfavirine or lenvatinib monotherapy groups.
Molecular Weight

652.27

Formula

C24H17BrCl2FN3NaO5S
CAS No.
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]
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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Elsulfavirine sodium Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Elsulfavirine867365-40-0R-1206R1206R 1206HIVDrug IntermediateReverse TranscriptaseCarbonic AnhydraseHuman immunodeficiency virusDrug IintermediateCarbonate dehydratasehuman carbonic anhydrase VAhuman carbonic anhydrase Ihuman carbonic anhydrase VBhuman carbonic anhydrase VIHIV-1 infectionshuman carbonic anhydrase XIIIhuman carbonic anhydrase XIVhuman carbonic anhydrase VIIhuman carbonic anhydrase IXhuman carbonic anhydrase IIInhibitorinhibitorinhibit

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