Art. -Nr.: HY-109056A

Elsulfavirine sodium

(Synonyms: R-1206 sodium)

2 Cited Publications

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Based on 2 publication(s) in Google Scholar

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 K_i 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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CAS. Nr.: 867365-40-0
Formel: C₂₄H₁₇BrCl₂FN₃NaO₅S
Molecular Weight:652.27

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

Elsulfavirine sodium Chemical Structure

CAS. Nr.: 867365-40-0

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (2)
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Bioz

Biologische Aktivität

Beschreibung

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)

Alle HIV Isoform-spezifische Produkte anzeigen :

Alle Carbonic Anhydrase Isoform-spezifische Produkte anzeigen :

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.

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.

Chemical Information

CAS. Nr. 867365-40-0
Molecular Weight 652.27
Formel C₂₄H₁₇BrCl₂FN₃NaO₅S
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]
Synonyms

R-1206 sodium
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Publications (2)

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Journal Impact Factor

Nat Commun

INSIG1/2 succination mediated by the moonlighting function of ADSL promotes lipogenesis and liver tumorigenesis. [Abstract]

2026 Mar 15;17(1):4002. PMID: 41833955
Anal Chem

Exposome-Scale Investigation of Cl-/Br-Containing Chemicals Using High-Resolution Mass Spectrometry, Multistage Machine Learning, and Cloud Computing. [Abstract]

2025 Jun 3;97(21):11099-11109. PMID: 40401576

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[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.

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1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Elsulfavirine sodium

2 Cited Publications

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Elsulfavirine sodium

Publications Citing Use of MedChemExpress (MCE) Elsulfavirine sodium

Alle HIV Isoform-spezifische Produkte anzeigen

Alle Carbonic Anhydrase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (2)

Reinheit & Dokumentation

Verweise

Calculators

Help & FAQs

Elsulfavirine sodium Related Classifications

HY-109056A Related Classifications