| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
Compound 3a, or FXR agonist 3, exhibits anti-fibrotic effect at 5 μM for 24 hours, as evidenced by a dose-dependent decrease in the levels of numerous fibrosis biomarkers in LX-2 cells [1]. On LX2 cells, FXR agonist 3 has a cytotoxic concentration (CC50) of 70.36 μM [1]. Species T1/2(h) CLInt(mic)(μg/min/mg) CLInt(liver)(μg/min/mg) Remaining Ratio(%)(T=60 min) Human 53.3 26.0 23.4 44.1 Rat 7.4 187.8 338.0 0.4 Mouse 7.4 187.9 744.1 39.0 Metabolic stability of FXR agonist 3 in human, rat, and mouse liver microsomes [1]
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|---|---|
| ln Vivo |
Compound 3a, or FXR agonist 3 (200 mg/kg; oral; daily for 4 weeks) reduced the degree of fibrosis in a high-fat, choline-deficient, l-amino acid-deficient NASH animal model by a significant margin [1]. FXR agonist 3 (oral; 200 mg/kg; taken once day for four weeks) also demonstrates anti-fibrotic and hepatoprotective properties in a rat model of fibrosis [1].
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| Cell Assay |
Western Blot Analysis[1]
Cell Types: LX-2 cells Tested Concentrations: 0, 2.5, 5, 7.5, and 10 μM Incubation Duration: 24 hrs (hours); with or without 2 ng/mL TGF-β1 for another 24 hr Experimental Results: diminished COL1A1, TGF-β1, α-SMA, and TIMP1 protein expressions in a dose-dependent manner. |
| Animal Protocol |
Animal/Disease Models: C57BL/6 N mice fed CDAHFD diet for 16 weeks[1]
Doses: 200 mg/kg Route of Administration: po (oral gavage); daily for 4 weeks after CDAHFD-induced Experimental Results: diminished expression of IL-1β and IL-6 in livers , indicating the liver-protective effect of 3a in CDAHFD mice may partially through inhibiting inflammasome activation. Lowered the serum levels of biochemical markers of ALT, AST, ALP, LDH, LDL and TBiL Dramatically, while raised HDL and GLU levels. Animal/Disease Models: C57BL/6 N mice inuced with BDL[1] Doses: 200 mg/kg Route of Administration: po (oral gavage); daily for 4 weeks after induced Experimental Results: Protected liver from accumulated bile acid-induced injury. Increased the expression of FXR and diminished the expression of NTCP in BDL rats. |
| References |
[1]. Zhang N, et al. Discovery and development of palmatine analogues as anti-NASH agents by activating farnesoid X receptor (FXR). Eur J Med Chem. 2023 Jan 5;245(Pt 1):114886.
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| Molecular Formula |
C28H28BRNO4
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|---|---|
| Molecular Weight |
522.43
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| Appearance |
Typically exists as solid at room temperature
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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 | 1.9141 mL | 9.5707 mL | 19.1413 mL | |
| 5 mM | 0.3828 mL | 1.9141 mL | 3.8283 mL | |
| 10 mM | 0.1914 mL | 0.9571 mL | 1.9141 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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