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

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.

For research use only. We do not sell to patients.

Elsulfavirine

Elsulfavirine Chemical Structure

CAS No. : 868046-19-9

Size Price Stock Quantity
Free Sample (0.1 - 0.2 mg)   Apply Now  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 In-stock
Solution
10 mM * 1 mL in DMSO In-stock
Solid
5 mg In-stock
10 mg In-stock
25 mg In-stock
50 mg In-stock
100 mg In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 2 publication(s) in Google Scholar

Other Forms of Elsulfavirine:

Elsulfavirine Related Antibodies

Top Publications Citing Use of Products

View All HIV Isoform Specific Products:

View All Isoforms
HIV HIV-1 HIV-2

View All Carbonic Anhydrase Isoform Specific Products:

View All Isoforms
CA CA I CA Ⅱ CA IX CA XII CA VII CA VI CA VA CA VB CA XIII CA XIV

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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].

IC50 & Target

HIV-1

<br/> ()

hCA I

52400 nM (Ki)

CA VII

2390 nM (Ki)

CA VI

5670 nM (Ki)

CA VA

4290 nM (Ki)

CA VB

14200 nM (Ki)

hCA IX

6650 nM (Ki)

CA XIII

4820 nM (Ki)

CA XIV

1960 nM (Ki)

In Vitro

Elsulfavirine (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 (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 (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 (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 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) 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].

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]
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.
Clinical Trial
Molecular Weight

629.28

Formula

C24H17BrCl2FN3O5S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(NC1=CC=C(S(=O)(NC(CC)=O)=O)C=C1Cl)CC2=CC=C(Br)C(OC3=CC(C#N)=CC(Cl)=C3)=C2F
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 62.5 mg/mL (99.32 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.5891 mL 7.9456 mL 15.8912 mL
5 mM 0.3178 mL 1.5891 mL 3.1782 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 2.08 mg/mL (3.31 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.08 mg/mL (3.31 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.90%

SDS (396 KB)

COA (246 KB) LCMS (95 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.5891 mL 7.9456 mL 15.8912 mL 39.7279 mL
5 mM 0.3178 mL 1.5891 mL 3.1782 mL 7.9456 mL
10 mM 0.1589 mL 0.7946 mL 1.5891 mL 3.9728 mL
15 mM 0.1059 mL 0.5297 mL 1.0594 mL 2.6485 mL
20 mM 0.0795 mL 0.3973 mL 0.7946 mL 1.9864 mL
25 mM 0.0636 mL 0.3178 mL 0.6356 mL 1.5891 mL
30 mM 0.0530 mL 0.2649 mL 0.5297 mL 1.3243 mL
40 mM 0.0397 mL 0.1986 mL 0.3973 mL 0.9932 mL
50 mM 0.0318 mL 0.1589 mL 0.3178 mL 0.7946 mL
60 mM 0.0265 mL 0.1324 mL 0.2649 mL 0.6621 mL
80 mM 0.0199 mL 0.0993 mL 0.1986 mL 0.4966 mL
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

Elsulfavirine Related Classifications

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:

Elsulfavirine868046-19-9R-1206R1206R 1206Drug IntermediateHIVReverse TranscriptaseCarbonic AnhydraseDrug IintermediateHuman immunodeficiency virusCarbonate 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

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Requested Quantity *

Applicant Name *

 

Salutation

Email Address *

 

Phone Number *

Department

 

Organization Name *

City

State

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
Elsulfavirine
Cat. No.:
HY-109056
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

English - EN (396 KB) Français - FR (396 KB) Deutsch - DE (396 KB) Norwegian - NO (396 KB) Español - ES (396 KB) Swedish - SV (396 KB) Italian - IT (396 KB) Korean - KR (396 KB) Portuguese - PT (396 KB)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.