| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
HSF1/AMPK activator 1 (compound 11) (0-20 μM; 48 h) effectively inhibited fibronectin expression in TGF-β1-treated human LX-2 cells with an IC50 of 0.7 μM. At a concentration of 10 μM for 48 h, the inhibition rate was 91.6 ± 3.8%, and no cytotoxicity was observed [1]. HSF1/AMPK activator 1 (0-80 μM; 48 h) did not show cytotoxicity to human LX-2 and HEK-293 cells even at concentrations as high as 80 μM [1]. HSF1/AMPK activator 1 (2.5-10 μM; 48 h) inhibited the proliferation of TGF-β1-treated human LX-2 cells in a dose-dependent manner [1]. HSF1/AMPK activator 1 (2.5–10 μM; 48 h) dose-dependently reduced the transcriptional and translational levels of fibronectin, type I collagen, and α-smooth muscle actin (α-SMA) (a marker of fibrosis) in TGF-β1-treated human LX-2 cells [1]. HSF1/AMPK activator 1 (2.5–10 μM; 48 h) dose-dependently inhibited TGF-β1-induced phosphorylation and nuclear translocation of Smad3 in human LX-2 cells, thereby inhibiting the TGF-β1/Smad signaling pathway [1]. HSF1/AMPK activator 1 (2.5–10 μM; 48 h) dose-dependently inhibited the proliferation, fibrosis, and TGF-β1/Smad signaling pathway in TGF-β1-treated mouse hepatic stellate cells [1]. HSF1/AMPK activator 1 (2.5–10 μM; 48 hours) can dose-dependently activate the HSF1/AMPK metabolic axis in TGF-β1-treated human LX-2 cells and mouse hepatic stellate cells, increase the phosphorylation levels of AMPK and HSF1, and promote the nuclear localization of activated HSF1 [1].
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|---|---|
| ln Vivo |
HSF1/AMPK activator 1 (compound 11) (10-30 mg/kg; intraperitoneal injection; every other day; 4 weeks) significantly improved liver injury, liver inflammation and liver fibrosis in CCl4-treated mice [1].
|
| Animal Protocol |
Animal/Disease Models:C57BL/6J (male, 8 weeks old, 18-20 g, CCl4-induced liver fibrosis) [1]
Doses: 10 mg/kg; 30 mg/kg Route of Administration: Intraperitoneal injection; every other day; for 4 weeks Experimental Results: Reduced liver weight. Decreased plasma AST and ALT levels. Decreased liver caspase-3 signal intensity. Decreased liver CD68 signal intensity (a marker of liver inflammation). Downregulated mRNA and protein levels of liver fibrosis markers fibronectin, type I collagen, and α-SMA. Decreased liver Smad3 phosphorylation. Masson staining and immunofluorescence detection of α-SMA and fibronectin showed that liver fibrosis accumulation was inhibited. |
| References |
| Molecular Formula |
C24H26O8
|
|---|---|
| Molecular Weight |
442.46
|
| CAS # |
2170935-59-6
|
| Appearance |
Typically exists as solids at room temperature
|
| SMILES |
O=C1OC(C)(C2=C[C@H]3[C@]4(C)C5=C([C@H](O[C@]6([C@@]5([C@@](C)(C[C@]4([C@]7(C2=C1)OC7)[H])C(O6)=O)O)[H])C)O3)C
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| 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 | 2.2601 mL | 11.3005 mL | 22.6009 mL | |
| 5 mM | 0.4520 mL | 2.2601 mL | 4.5202 mL | |
| 10 mM | 0.2260 mL | 1.1300 mL | 2.2601 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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