| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
FXR/HSD17B13 regulator-2 (compound 10) activated FXR 24 hours after transfection into HepG2 cells, with an EC50 of 79 nM [1]. FXR/HSD17B13 regulator-2 is highly selective for FXR and HSD17B13, and has no detectable activity against other HSD17B subtypes or 17 nuclear receptors at a concentration of 10 μM [1].
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|---|---|
| ln Vivo |
FXR/HSD17B13 modulator-2 (compound 10) (5–20 mg/kg; orally; once daily; for 4 weeks) alleviated MASH in a WD+CCl4-induced mouse model in a dose-dependent manner by modulating lipid metabolism, inflammation, and fibrosis [1]. FXR/HSD17B13 modulator-2 (20 mg/kg; orally; once daily; for 5 days) preferentially accumulated in the liver (hepatic plasma ratio 14.2) and activated the FXR signaling pathway in the liver and ileum after oral administration of 20 mg/kg daily for 5 consecutive days in healthy male C57BL/6 mice [1].
|
| Animal Protocol |
Animal/Disease Models:C57BL/6 (male, 8 weeks old, MASH induced by a high-sugar, high-fat diet for 12 weeks plus intraperitoneal injection of 0.2% carbon tetrachloride twice a week) [1]
Doses: 5 mg/kg; 10 mg/kg; 20 mg/kg Route of Administration: Oral; once daily; for 4 weeks (dose adjusted every 5 days from week 8 to week 12 according to body weight) Experimental Results: Dose-dependent reduction in non-alcoholic fatty liver disease activity score (NAS) and reduction in histopathological features of MASH, including steatosis, lobular inflammation and hepatocyte ballooning degeneration. At a dose of 20 mg/kg, its efficacy was comparable to that of obeticholic acid at a dose of 20 mg/kg. It dose-dependently reduced liver injury markers (ALT, AST, ALP, TBIL, TBA), serum lipid levels, liver lipid levels, liver hydroxyproline levels, and inflammatory cytokine levels (IL-6, IL-1β, TNFα). It downregulated the pro-fibrotic cytokine TGF-β. |
| References |
| Molecular Formula |
C27H24CL2N2O5S
|
|---|---|
| Molecular Weight |
559.46
|
| Appearance |
Typically exists as solids at room temperature
|
| SMILES |
ClC1=CC=CC(Cl)=C1C2=NOC(C(C)C)=C2COC3=CC=C(C4=CC=C(C(NS(=O)(C)=O)=O)C=C4)C=C3
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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 | 1.7874 mL | 8.9372 mL | 17.8744 mL | |
| 5 mM | 0.3575 mL | 1.7874 mL | 3.5749 mL | |
| 10 mM | 0.1787 mL | 0.8937 mL | 1.7874 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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