| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
ACLY-IN-3 (compound B1) (50 μM; 4 h) effectively reduced lipid accumulation in oleic acid-induced shNC HepG2 cells via an ACLY-dependent mechanism, and no cytotoxicity was observed at concentrations up to 50 μM [1]. ACLY-IN-3 (50 μM; 24 h) inhibited the expression of adipogenesis genes FASN, ACC1, and SREBP-1c in oleic acid-induced shNC HepG2 cells via an ACLY-dependent mechanism [1].
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|---|---|
| ln Vivo |
ACLY-IN-3 (compound B1) (10-30 mg/kg; intraperitoneal injection; daily; 8 weeks) significantly reduced body weight, hepatic steatosis, systemic insulin resistance, oxidative stress, inflammation and fibrosis in a high-fat diet-induced mouse MASH model [1].
|
| Cell Assay |
Real-time quantitative PCR[1]
Cell Types: Oleic acid (OA) induced shNC and shACLY HepG2 cells Tested Concentrations: 50 μM Incubation Duration: 24 hours (containing 1 mM OA) Experimental Results: In OA-induced shNC HepG2 cells, the mRNA expression of fatty acid synthase (FASN), acetyl-CoA carboxylase 1 (ACC1), and sterol regulatory element binding protein 1c (SREBP-1c) was significantly downregulated. In shACLY HepG2 cells, this effect disappeared. |
| Animal Protocol |
Animal/Disease Models:C57BL/6J (male, 8 weeks old, 18-20 g, high-fat diet-induced MASH) [1]
Doses: 10 mg/kg; 30 mg/kg Route of Administration: Intraperitoneal injection; once daily; for 8 weeks Experimental Results: Average body weight decreased from 49.5 g (high-fat diet group) to 41.7 g (10 mg/kg) and 35.7 g (30 mg/kg). Significantly reduced elevated serum triglyceride, total cholesterol, alanine aminotransferase, aspartate aminotransferase and low-density lipoprotein cholesterol levels, while restoring reduced serum high-density lipoprotein cholesterol to near control levels. Compared with the high-fat diet group, liver weight, liver triglycerides and liver total cholesterol were significantly reduced. Liver lipid accumulation (Oil Red O staining) was almost completely reversed. The hepatic mRNA expression of adipogenesis markers (FASN, LXR, SREBP-1c, HMGCR, ACC1) and fatty acid uptake marker CD36 was significantly downregulated, while the expression of fatty acid oxidation markers (PPARα, CPT1, PPARγ) and lipid metabolism regulator AMPKα1 was upregulated; the protein expression of FASN, ACC1, and PPARα also changed accordingly. Compared with the high-fat diet group, glucose tolerance (decreased area under the curve of oral glucose tolerance test) and insulin sensitivity (decreased area under the curve of insulin tolerance test) were both improved. Hepatic malondialdehyde levels (a marker of oxidative stress) were significantly reduced, and the mRNA expression of inflammatory markers (CD68, TNF-α, NLRP3, ASC) and the pro-fibrotic marker α-SMA was downregulated, and collagen deposition in liver tissue (Sirius red staining) was reduced. Hepatocyte morphology returned to normal (HE staining), and no obvious pathological changes were observed in the heart, spleen, lungs, and kidneys. |
| References |
| Molecular Formula |
C16H12O5
|
|---|---|
| Molecular Weight |
284.26
|
| Appearance |
Typically exists as solids at room temperature
|
| SMILES |
O=C1C2=CC(O)=C(C=C2C/C1=C\C3=CC=C(C(O)=C3)O)O
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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 | 3.5179 mL | 17.5895 mL | 35.1791 mL | |
| 5 mM | 0.7036 mL | 3.5179 mL | 7.0358 mL | |
| 10 mM | 0.3518 mL | 1.7590 mL | 3.5179 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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