| Size | Price | |
|---|---|---|
| 100mg | ||
| 250mg | ||
| 500mg | ||
| Other Sizes |
| Targets |
FXR 2.1 μM (IC50)
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|---|---|
| ln Vitro |
In HEK293T cells, FXR antagonist 1 (0-100 µM; 24 h) exhibits FXR antagonistic activities[1].
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| ln Vivo |
In GAN-diet-induced NASH mice, FXR antagonist 1 (10 mg/kg; po; once daily for 12 weeks) decreases obesity, enhances glucose sensitivity, and slows the advancement of NASH[1]. In GAN-diet-induced mice, FXR antagonist 1 (10 mg/kg; po; once daily for 12 weeks) suppresses intestinal FXR signaling but indirectly increases hepatic FXR signaling[1]. In rats put on an HFMCD diet, FXR antagonist 1 (3, 10, 30 mg/kg; po; once daily for 4 weeks) reduces NASH pathologies in a dose-dependent manner[1].
|
| Cell Assay |
Cell Viability Assay[1]
Cell Types: HEK293T cells (co-transfected with pCMV-Script-hFXR and pGL4.11-hSHP -Luciferase) Tested Concentrations: 0-100 µM Incubation Duration: 24 h Experimental Results: demonstrated FXR antagonistic activities with an IC50 value of 2.1 μM. |
| Animal Protocol |
Animal/Disease Models: Adult male C57BL/6 mice (GAN (Gubra-amylin NASH)-diet induced NASH model)[1].
Doses: 10 mg/kg Route of Administration: Oral administration; single daily for 12 weeks. Experimental Results: Reversed metabolic dysfunction in GAN-induced NASH mice. decreased GAN-diet-induced hepatic steatosis, injury, inflammation, and fibrosis. Inhibited the hepatic mRNA expression involved in lipid metabolism, inflammatory inflammation signaling, and fibrogenesis in GAN-diet-induced mice. Dramatically antagonized intestinal FXR signaling and bile acid reabsorption. Animal/Disease Models: Adult male C57BL/6 mice (HFMCD-diet induced NASH model)[1]. Doses: 3, 10, 30 mg/kg Route of Administration: Oral administration; single daily for 4 weeks. Experimental Results: Dramatically diminished serum ALT and AST levels at 30 mg/kg, and markedly lowered the hepatic TG concentration in both 10 and 30 mg/kg. Lowered hepatic hydroxyproline level. |
| References |
[1]. Zhang C, et al. Discovery of Betulinic Acid Derivatives as Potent Intestinal Farnesoid X Receptor Antagonists to Ameliorate Nonalcoholic Steatohepatitis. J Med Chem. 2022 Sep 15.
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| Molecular Formula |
C36H59NO5
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|---|---|
| Molecular Weight |
585.86
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| CAS # |
2295804-68-9
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| SMILES |
C(=O)(CNC([C@@]12CC[C@]3(C)[C@@]([H])([C@]1([C@H](C(C)C)CC2)[H])CC[C@@]1([C@@]2([C@@]([H])(CC[C@]13C)C(C)([C@H](OC(=O)CCC)CC2)C)C)[H])=O)O
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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.) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7069 mL | 8.5345 mL | 17.0689 mL | |
| 5 mM | 0.3414 mL | 1.7069 mL | 3.4138 mL | |
| 10 mM | 0.1707 mL | 0.8534 mL | 1.7069 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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