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FASN/SCD-IN-1

FASN/SCD-IN-1 is a silymarin derivative and an orally effective fatty acid synthase (FASN)/stearoyl-CoA desaturase (SCD) inhibitor.
FASN/SCD-IN-1
FASN/SCD-IN-1 Chemical Structure CAS No.: 3063509-61-2
Product category: FASN
This product is for research use only, not for human use. We do not sell to patients.
Size Price
500mg
1g
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Product Description
FASN/SCD-IN-1 is a Silybin derivative and an orally active inhibitor of fatty acid synthase (FASN)/stearoyl-CoA desaturase (SCD). In vitro, FASN/SCD-IN-1 exhibits activities that inhibit lipid deposition, reduce FASN and SCD transcription levels, and possess antioxidant, anti-inflammatory, and anti-fibrotic properties. In a rat model of acute liver injury, FASN/SCD-IN-1 demonstrates significant hepatoprotective effects. In a mouse model of myeloproliferative steatohepatitis (MASH), FASN/SCD-IN-1 improves the pathological features of MASH liver, including steatosis, inflammation, and fibrosis. FASN/SCD-IN-1 can be used to study MASH.
Biological Activity I Assay Protocols (From Reference)
ln Vitro
FASN/SCD-IN-1 (Compound A2) (100-200 μM, 20-30 min) showed scavenging activity against DPPH and O2•–, with scavenging rates of 92.9% and 82.9%, respectively, and IC50 values of 33.4 and 28.1 μM, respectively. In the lipid peroxidation inhibition capacity (LPIC) assay, LPIC showed an inhibition rate of 67.0% and an IC50 of 41.7 μM[1]. FASN/SCD-IN-1 (10-40 μM, 24 hours) can reduce triglyceride (TG) levels and inhibit lipid accumulation in LO2 cells and mouse primary hepatocytes stimulated by Palmitic acid/Oleic acid (PO). It can also reduce the transcription levels of fatty acid synthase (FASN) and stearoyl-CoA desaturase (SCD) in PO-stimulated LO2 cells and reduce the expression of ACACA (encoding acetyl-CoA carboxylase) and FASN in PO-stimulated mouse primary hepatocytes [1]. FASN/SCD-IN-1 (1-10 μM, 24 hours) can reduce the levels of excess ROS and IL-6 and TNF-α mRNA in LO2 cells and mouse primary hepatocytes stimulated by Carbon tetrachloride (CCl4) [1]. FASN/SCD-IN-1 (10-40 μM, 48 hours) can inhibit the levels of collagen I and fibronectin (FN) in TGF-β stimulated LX2 cells [1].
ln Vivo
FASN/SCD-IN-1 (Compound A2) (100 mg/kg, gavage, once daily for 7 days) can protect against acute liver injury in a CCl4-induced acute liver injury model by restoring liver function, reducing electrolyte damage and repairing oxidative stress, thereby alleviating liver function damage [1]. FASN/SCD-IN-1 (150 mg/kg, injury, once daily for 4 weeks) can reduce steatosis and enhance oxidative, neural responses and liver fibrosis in HFD + CCl4-induced MASH mice, thus significantly improving the progression of MASH mice [1].
Cell Assay
Western Blot AnalysisTGF-β-stimulated LX2 cells
Cell Types: TGF-β-stimulated LX2 cells
Tested Concentrations: 10 μM, 20 μM, 40 μM
Incubation Duration: 48 h
Experimental Results: Suppressed collagen I and FN levels.
Animal Protocol
Animal/Disease Models: CCl4 (1 mg/kg, i.p.)-induced acute liver injury SD rat (male, 6 weeks) model[1]
Doses: 100 mg/kg
Route of Administration: i.g. once a day, 7 days
Experimental Results: Alleviated typical features of fatty liver disease, such as partial yellowing, darkening of the liver margins, white fat granules, and a rough surface. Reduced the hepatopancreatic somatic index (HSI) and liver-to-body weight ratio. Reduced serum AST, ALT, and LDH levels. Reduced liver vacuoles, acute fat deposition, elevation of the MDA level and and restored SOD activity.
Animal/Disease Models: HFD + CCl4 (0.2 mg/kg, i.p., once a week)-induced MASH C57BL/6 mice (male, 6 weeks) model[1]
Doses: 150 mg/kg
Route of Administration: p.o., once a day, 4 weeks
Experimental Results: Protected body weight and counteracts CCl4 toxicity. Reduced hepatopancreatic somatic index (HSI) and alleviates liver swelling. Alleviated liver damage and reverses CCl4-induced liver enlargement, pale color, and mottled texture. Reduced serum AST and ALT levels. Improved liver structural distortion and reverses CCl4-induced hepatocellular ballooning, inflammation, and steatosis. Ameliorated the dyslipidemia, reduced the elevated serum TG, cholesterol (CHO), and low-density lipoprotein cholesterol (LDL-c) levels and increased the lowered high-density lipoprotein cholesterol (HDL-c) levels. Reduced the hepatic TG and CHO levels. Restored the decreased liver GSH level and decrease the elevated MDA level, restore the decreased levels of both SOD and GSH-Px. Reduced IL-6 and TNF-α levels, reduced collagen deposition, levels of α-SMA and collagen I in the liver tissue.
References

[1]. https://pubmed.ncbi.nlm.nih.gov/40493802/

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C25H22O9S
Molecular Weight
498.50
CAS #
3063509-61-2
Appearance
Typically exists as solids at room temperature
HS Tariff Code
2934.99.9001
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 Data
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
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
(e.g. IP/IV/IM/SC)
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution 50 μL Tween 80 850 μL Saline)
*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 : PEG300Tween 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).
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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)]
*Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO 100 μLPEG300 200 μL castor oil 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10: 10 : 80 (i.e. 100 μL Ethanol 100 μL Cremophor 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH 400 μLPEG300 50 μL Tween 80 450 μL 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).
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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders


Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.0060 mL 10.0301 mL 20.0602 mL
5 mM 0.4012 mL 2.0060 mL 4.0120 mL
10 mM 0.2006 mL 1.0030 mL 2.0060 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.

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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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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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