| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
Alsuvirine sodium (10 μM; 1 h) significantly blocked the interaction between ADSL and INSIG1/2 in high glucose-induced Huh7 cells, inhibited the cleavage activation and nuclear translocation of SREBP-1, blocked SRE-driven luciferase transcriptional activity, and inhibited the activation of the SREBP adipogenesis pathway [2]. Alsuvirine sodium (10 μM; 12 h) significantly inhibited the translocation of SCAP from the endoplasmic reticulum to the Golgi apparatus in high glucose-induced Huh7 cells, downregulated the mRNA expression levels of downstream adipogenesis target genes FASN, ACACA, SCD, and GPAM of SREBP-1, reduced the number of intracellular lipid droplets, and inhibited high glucose-induced intracellular lipid accumulation [2]. Alsuvirine sodium (10 μM; 8 h) significantly inhibited the conversion of 14C-glucose to triglycerides and fatty acids in Huh7 cells and blocked the de novo lipid synthesis process in cells [2]. The active metabolite of salsuvirine sodium, VM-1500A (serum-corrected EC50 of approximately 13.8 nM), can effectively inhibit the replication of HIV-1 clinical isolates in in vitro cell models [3].
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|---|---|
| ln Vivo |
In a nude mouse model of hepatocellular carcinoma with subcutaneous transplantation of Huh7 cells, salsuvirine sodium (10 mg/kg; orally; once daily for 20 days) significantly inhibited the growth of hepatocellular carcinoma, reduced the expression of the proliferation marker Ki-67 in tumor tissue, increased the apoptosis level of tumor cells, and downregulated the protein expression of SREBP-1, FASN and ACLY[2]. Salsuvirine sodium (10 mg/kg; orally; once daily for 20 days) combined with lenvatinib (with the same dosing regimen as salsuvirine sodium) showed a synergistic inhibitory effect on tumor growth in a nude mouse model of hepatocellular carcinoma with subcutaneous transplantation of Huh7 cells, and its efficacy was better than that of monotherapy[2].
|
| Cell Assay |
Western Blot Analysis [2]
Cell Types: Huh7 human hepatocellular carcinoma cells Tested Concentrations: 10 μM (elsulfavirine), 20 μM (tezacaftor), 100 μM (pyrithioxin) (as control compounds) Incubation Duration: 1 hour of pretreatment before high glucose stimulation Experimental Results: Significantly inhibited high glucose-induced SREBP-1 cleavage and activation in Huh7 cells, but had no effect on PKCε-mediated phosphorylation of ADSL at the S407 site. In contrast, the control compounds tezacaftor and pyrithioxin did not significantly inhibit SREBP-1 cleavage. Real-time quantitative PCR[2] Cell Types: Huh7 human liver cancer cells Tested Concentrations: 10 μM Incubation Duration: Co-treated with high glucose for 12 hours Experimental Results: In Huh7 cells, the mRNA expression of downstream adipogenesis target genes (including FASN, ACACA, SCD and GPAM) induced by high glucose was significantly downregulated. |
| Animal Protocol |
Animal/Disease Models:Male athymic BALB/c nude mice (6 weeks old) were used to establish a subcutaneous xenograft hepatocellular carcinoma (HCC) model by subcutaneous inoculation of 1 × 10⁶ Huh7 cells in the right abdomen [2] 10 mg/kg
Doses: 10 mg/kg< Route of Administration:Starting from day 7 after tumor cell inoculation, the cells were administered by gavage once a day for 20 consecutive days; in combination with or without 10 mg/kg lenvatinib. Experimental Experimental Results:Single-drug treatment: Compared with the vector control group, it significantly inhibited the growth of xenograft hepatocellular carcinoma tumors in nude mice, reduced the expression of the proliferation marker Ki-67 in tumor tissue, increased the level of tumor cell apoptosis, and downregulated the protein expression of SREBP-1 and adipogenesis-related enzymes (including FASN and ACLY) in tumor tissue. Combination therapy: Compared with elsuvirine or lenvatinib monotherapy, it has a synergistic inhibitory effect on hepatocellular carcinoma tumor growth, with more significant reduction in tumor volume and weight, lower Ki-67 expression, higher tumor cell apoptosis, and more significant downregulation of SREBP-1, FASN and ACLY in tumor tissue. |
| References |
|
| Molecular Formula |
C24H17BRCL2FN3NAO5S
|
|---|---|
| Molecular Weight |
652.27
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| CAS # |
867365-40-0
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| Appearance |
Typically exists as solids at room temperature
|
| 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
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.5331 mL | 7.6655 mL | 15.3311 mL | |
| 5 mM | 0.3066 mL | 1.5331 mL | 3.0662 mL | |
| 10 mM | 0.1533 mL | 0.7666 mL | 1.5331 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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