| Size | Price | Stock | Qty |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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| Other Sizes |
| Targets |
Fatostatin targets sterol regulatory element-binding proteins (SREBPs), specifically by binding to SCAP (SREBP cleavage-activating protein). This binding inhibits the ER-to-Golgi translocation of SREBPs, preventing their activation. It inhibits both SREBP-1 and SREBP-2 with an IC50 of 5.6 µM. By blocking SREBP activation, it reduces the expression of genes involved in lipid and cholesterol synthesis.
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| ln Vitro |
In vitro, Fatostatin inhibits 3T3-L1 cell insulin-induced adipogenesis and DU145 cell serum-independent growth. It decreases the transcription of lipogenic genes in cells. It is a specific inhibitor of SREBP activation, blocking SREBP-mediated gene expression. Its activity is measured by its ability to inhibit SREBP-dependent transcription and subsequent lipid synthesis in cultured cells.
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| ln Vivo |
In vivo, Fatostatin possesses antitumor properties and lowers hyperglycemia in ob/ob mice. It inhibits high glucose-induced upregulation of TGF-β. By inhibiting SREBP activation, it reduces the expression of lipogenic genes, leading to decreased lipid synthesis and improved metabolic parameters. Its in vivo effects make it a valuable tool for studying the role of SREBP in cancer and metabolic diseases.
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| Enzyme Assay |
In vitro assays for Fatostatin involve measuring its effects on SREBP activation and downstream gene expression. Cells are treated with the compound, and the translocation of SREBP from the ER to the Golgi is measured using microscopy or biochemical fractionation. SREBP-mediated gene expression is assessed by qRT-PCR for lipogenic genes like FASN and HMGCR. The IC50 of 5.6 µM is determined in these assays.
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| Cell Assay |
For in vitro cell-based assays, cells (e.g., 3T3-L1, DU145) are cultured and treated with Fatostatin hydrochloride. Its effects on adipogenesis are assessed by Oil Red O staining in 3T3-L1 cells. Its effects on cell growth are measured by MTT assays in DU145 cells. SREBP target gene expression is measured by qRT-PCR. Its inhibition of SREBP-mediated gene expression is the primary readout.
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| Animal Protocol |
In vivo animal studies with Fatostatin are conducted in mouse models of metabolic disease and cancer. ob/ob mice are treated with the compound to assess its effects on hyperglycemia. Tumor xenograft models are used to study its antitumor properties. Blood glucose, lipid profiles, and tumor growth are measured. The compound's effects on SREBP target gene expression in tissues are also analyzed.
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| ADME/Pharmacokinetics |
Fatostatin hydrochloride is a small molecule inhibitor of SREBP activation. Its exact CAS number is not provided in the search results, but it is known as Fatostatin A or 125B11. It is a solid and is typically stored as a powder. It is soluble in DMSO. The compound is intended for research purposes only.
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| Toxicity/Toxicokinetics |
Fatostatin hydrochloride is a research compound and is not approved for human therapeutic use. In preclinical studies, it has shown a manageable safety profile. In ob/ob mice, treatment led to a weight reduction of about 12% compared to untreated controls, indicating potential metabolic effects. Standard laboratory safety precautions should be followed when handling the compound.
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| Additional Infomation |
Fatostatin hydrochloride is a potent inhibitor of SREBP activation. It binds to SCAP, inhibiting SREBP translocation and subsequent expression of lipogenic genes. It possesses antitumor properties and lowers hyperglycemia. It is not an FDA-approved drug and is intended for research use only.
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| Appearance |
Typically exists as solid 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.) |
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.
Products are for research use only; We do not sell to patients
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