| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
ACLY-IN-4 (compound C1) (50 μM; co-incubated with 1 mM OA for 4 h) inhibited oleic acid-induced lipid accumulation in shNC HepG2 cells, but this inhibitory effect was weakened in shACLY HepG2 cells, indicating that its mechanism of action is dependent on ACLY[1]. ACLY-IN-4 (50 μM; co-incubated with 1 mM OA for 24 h) downregulated the expression of adipogenic genes (FASN, ACC1, SREBP-1c) in oleic acid-induced shNC HepG2 cells through an ACLY-dependent mechanism[1].
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|---|---|
| ln Vivo |
ACLY-IN-4 (compound C1) (10-30 mg/kg; intraperitoneal injection; daily; 8 weeks) significantly reduced hepatic steatosis, systemic insulin resistance, oxidative stress, inflammation and fibrosis in a mouse MASH model induced by HFD [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 FASN, ACC1, and SREBP-1c was significantly downregulated. In OA-induced shACLY HepG2 cells, the downregulation effect of OA on the mRNA expression of FASN, ACC1, and SREBP-1c 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 to 46.0 g (10 mg/kg) and 32.9 g (49.5 g in the high-fat diet control group), respectively. Serum triglycerides (TG), total cholesterol (T-CHO), alanine aminotransferase (ALT), aspartate aminotransferase (AST), low-density lipoprotein cholesterol (LDL-C), liver weight, liver triglycerides, and liver total cholesterol were significantly reduced in the 10 mg/kg dose group. Serum high-density lipoprotein cholesterol (HDL-C) levels returned to normal at the 10 mg/kg dose. At a dose of 10 mg/kg, hepatic lipid accumulation was significantly reduced (confirmed by Oil Red O staining). At a dose of 10 mg/kg, the mRNA expression of hepatic adipogenesis markers (FASN, LXR, SREBP-1c, HMGCR, ACC1, CD36) and pro-inflammatory/fibrotic markers (CD68, TNF-α, NLRP3, ASC, α-SMA) was inhibited. At a dose of 10 mg/kg, the mRNA expression of fatty acid oxidation markers (PPARα, CPT1, PPARγ, AMPKα1) returned to normal. At a dose of 10 mg/kg, hepatic malondialdehyde (MDA) levels decreased. At a dose of 10 mg/kg, hepatic FASN, ACC1, NLRP3, ASC, and α-SMA protein levels decreased, while PPARα protein levels increased. Compared with the 10 mg/kg dose group, the 30 mg/kg dose group showed more significant effects in reducing body weight, serum and hepatic lipid parameters, liver weight, and hepatic lipid accumulation. The 30 mg/kg dose group also produced significant effects on the gene and protein expression of markers of adipogenesis, fatty acid oxidation, inflammation, and fibrosis, similar to those in the 10 mg/kg dose group. Hepatocyte morphology in the 30 mg/kg dose group was almost restored to that of the standard diet control group (confirmed by H&E staining). |
| References |
| Molecular Formula |
C15H10O6
|
|---|---|
| Molecular Weight |
286.24
|
| Appearance |
Typically exists as solids at room temperature
|
| SMILES |
O=C(C1=CC2=CC(O)=C(C=C2O1)O)C3=CC(O)=C(C=C3)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 | 3.4936 mL | 17.4679 mL | 34.9357 mL | |
| 5 mM | 0.6987 mL | 3.4936 mL | 6.9871 mL | |
| 10 mM | 0.3494 mL | 1.7468 mL | 3.4936 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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