| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
F44-S101 is a potent and selective intestinal-restricted FXR antagonist with an IC50 value of 0.48 μM[1].
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|---|---|
| ln Vivo |
F44-S101 (10-100 mg/kg; gavage; single dose) dose-dependently reduced serum total cholesterol (TC), triglycerides (TG), and low-density lipoprotein cholesterol (LDL-C) levels in Triton-induced hyperlipidemic male C57BL/6 mice and reversed elevated liver enzymes. A dose of 100 mg/kg reduced serum TC by 18.9% and TG by 32.2% [1]. F44-S101 (10-100 mg/kg; gavage; 4 weeks) dose-dependently reduced serum TC, liver TC, serum LDL-C, inguinal adipose tissue, and serum ceramide levels in high-fat diet (HFD)-induced hyperlipidemic male C57BL/6 mice. A dose of 100 mg/kg reduced serum TC by 25.6% and liver TC by 17.3% [1].
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| Animal Protocol |
Animal/Disease Models:C57BL/6 (male, 8 weeks old; Triton WR-1339-induced acute hyperlipidemia) [1]
Doses: 10 mg/kg; 30 mg/kg; 100 mg/kg Route of Administration: Gavage Experimental Results: Compared with the solvent control group, the 100 mg/kg dose group showed a significant decrease of 18.9% in serum total cholesterol (TC) and 32.2% in serum triglycerides (TG). Compared with the solvent control group, serum low-density lipoprotein cholesterol (LDL-C) levels in all dose groups were significantly reduced by more than 38%. The Triton-induced increase in plasma alanine aminotransferase (ALT) and aspartate aminotransferase (AST) levels was reversed. Animal/Disease Models:C57BL/6 (male, adult; high-fat diet-induced hyperlipidemia) [1] Doses: 10 mg/kg; 30 mg/kg; 100 mg/kg Route of Administration: Gavage; 4 weeks Experimental Results: Compared with the solvent control group, the serum total cholesterol (TC) in the 100 mg/kg dose group was significantly reduced by 25.6%, and the liver TC was significantly reduced by 17.3%. Compared with the solvent control group, the plasma low-density lipoprotein cholesterol (LDL-C) concentration in the 100 mg/kg dose group was significantly reduced by 30.8%, and the LDL-C level was close to that of the control group. The mass of inguinal adipose tissue and its ratio to body weight decreased in a dose-dependent manner; compared with the solvent control group, the inguinal adipose weight was significantly reduced in the 100 mg/kg dose group. Compared with the solvent control group, the serum ceramide level decreased significantly in a dose-dependent manner. It had no significant effect on ALT, AST, brown adipose tissue weight, or epididymal fat weight. |
| References |
| Molecular Formula |
C27H25CLN2O6S2
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|---|---|
| Molecular Weight |
573.08
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| CAS # |
3124701-00-1
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| Appearance |
Typically exists as solids at room temperature
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| SMILES |
CCN(S(=O)(C1=CC2=C(SC(C(O)=O)=C2)C=C1)=O)C3=CC=C(C=C3CN(C(C4CC4)=O)CC5=CC=CO5)Cl
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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)
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| 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 | 1.7450 mL | 8.7248 mL | 17.4496 mL | |
| 5 mM | 0.3490 mL | 1.7450 mL | 3.4899 mL | |
| 10 mM | 0.1745 mL | 0.8725 mL | 1.7450 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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