| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
LIFR/GPBAR1 modulator 1 (Compound 2o) (0.1–50 μM) showed an 89.6% inhibition rate of LIFR (IC50 = 7.9 μM) at a concentration of 10 μM in HepG2 cells. In HEK293T cells, it showed a 79.4% activation rate of GPBAR1 (EC50 = 0.2 μM) at a concentration of 10 μM[1]. LIFR/GPBAR1 modulator 1 (1–10 μM, 24 h) modulates the expression of fibrosis-related genes in human hepatic stellate cells (HSC) LX2 in a concentration-dependent manner. At a concentration of 10 μM, it upregulated the mRNA expression of LIFR and GPBAR1 and significantly reduced the expression of profibrosis markers (COL1A1, ASMA, and TGFβ). Meanwhile, it reduces the expression of TIMP1 and increases the expression of MMP9, indicating that it promotes the degradation of extracellular matrix (ECM) [1].
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|---|---|
| ln Vivo |
LIFR/GPBAR1 modulator 1 (Compound 2o) (10 mg/kg, Gulf, once daily for 7 days) can effectively reverse carbon tetrachloride (CCl4)-induced acute liver fibrosis, specifically by reversing and reducing hepatocyte damage, factor-regulated response, extracellular matrix (ECM) deposition, and expression of pro-fibrotic genes in the retina [1].
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| Cell Assay |
Real Time qPCR[1]
Cell Types: Leukaemia inhibitory factor (LIF)-mediated human HSC LX2 Tested Concentrations: 1 μM, 5 μM, 10 μM Incubation Duration: 24 h Experimental Results: Upregulated the mRNA expression of LIFR and GPBAR1 and significantly reduced the expression of pro-fibrosis markers (COL1A1, ASMA, and TGFβ). Reduced TIMP1 expression and increased MMP9 expression. |
| Animal Protocol |
Animal/Disease Models: Liver fibrosis was induced by intraperitoneal (i.p.) administration of carbon tetrachloride (CCl4) at a dose of 500 μL/kg, dissolved in an equal volume of olive oil, and administered twice per week for 1 week to Male C57BL/6J mice[1].
Doses: 10 mg/kg Route of Administration: P.o., once daily for 7 days Experimental Results: Reduced weight loss. Significantly reduced plasma levels of AST, ALT, bilirubin, and LDH. Reduced CCl4-induced white blood cell (WBC) count elevation and modulated the percentages of neutrophils, lymphocytes, and monocytes. Improved hepatocellular necrosis and inflammatory infiltration and significantly reduced collagen deposition and fibrosis area. Significantly downregulated the mRNA expression of fibrosis marker genes (Colla1, aSma, Tgβ) in liver tissue. |
| References |
| Molecular Formula |
C32H31NO2
|
|---|---|
| Molecular Weight |
461.59
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| Appearance |
Typically exists as solids 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 | 2.1664 mL | 10.8321 mL | 21.6642 mL | |
| 5 mM | 0.4333 mL | 2.1664 mL | 4.3328 mL | |
| 10 mM | 0.2166 mL | 1.0832 mL | 2.1664 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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