| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
GAC0003A4 targets the liver X receptors (LXRα and LXRβ), which are nuclear receptors that regulate cholesterol metabolism, lipid homeostasis, and inflammation. As an inverse agonist, it suppresses the basal transcriptional activity of LXR, in contrast to neutral antagonists that merely block agonist-induced activity. Additionally, GAC0003A4 efficiently degrades LXRβ protein, providing a dual mechanism of action.
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| ln Vitro |
In vitro, GAC0003A4 inhibits LXR transcriptional activity and promotes the degradation of LXRβ protein. This dual mechanism results in the suppression of LXR target genes involved in lipid metabolism and inflammation. In cancer cells, LXR inverse agonism and degradation may impair tumor cell survival and proliferation. The compound has shown potential in preclinical studies for the treatment of advanced pancreatic cancer and other refractory malignancies.
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| ln Vivo |
In vivo, GAC0003A4 has demonstrated potential for the treatment of advanced pancreatic cancer and other refractory malignancies in preclinical models. By inhibiting LXR activity and degrading LXRβ, the compound may suppress tumor growth and overcome resistance mechanisms associated with LXR signaling. Detailed in vivo efficacy data, including effects on tumor growth and survival in xenograft models, are described in the primary literature.
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| Enzyme Assay |
Non-cellular binding assays for GAC0003A4 involve measuring its binding affinity to LXRα and LXRβ using techniques such as fluorescence polarization, scintillation proximity assays, or surface plasmon resonance. The compound's ability to inhibit LXR transcriptional activity can be assessed in cell-free systems using purified LXR proteins and coactivator peptides. Degradation of LXRβ can be studied using purified protein degradation assays or by monitoring protein stability in the presence of the compound.
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| Cell Assay |
In vitro cellular experiments with GAC0003A4 are conducted in cancer cell lines, particularly those derived from pancreatic cancer. Cells are treated with the compound at various concentrations, and LXR transcriptional activity is measured using luciferase reporter assays. LXRβ protein levels are assessed by Western blotting to confirm degradation. Cell viability, proliferation, and apoptosis are evaluated using standard assays such as MTT, BrdU incorporation, and caspase activity measurements.
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| Animal Protocol |
In vivo animal studies for GAC0003A4 are performed in murine xenograft models using human pancreatic cancer cell lines. Tumor-bearing mice are treated with the compound via appropriate routes of administration. Tumor growth is monitored over time, and endpoints include tumor volume measurements, survival analysis, and pharmacodynamic assessments of LXR target gene expression and LXRβ protein levels in tumor tissues. Efficacy is compared to vehicle controls and standard-of-care therapies.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of GAC0003A4 include a molecular weight of 340.42 and a molecular formula of C20H24N2O3. The CAS number is 929492-71-7. The compound has a LogP of 3.7. It is soluble in DMSO at approximately 125 mg/mL. Storage conditions: powder at -20°C for 3 years or 4°C for 2 years; in solvent at -80°C for 6 months or -20°C for 1 month. Purity is typically ≥98%.
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| Toxicity/Toxicokinetics |
Toxicity data for GAC0003A4 are generated during preclinical development. As an LXR modulator, potential toxicities may include effects on lipid metabolism and liver function, given the role of LXR in these processes. Comprehensive toxicology studies would assess safety margins and identify target organ toxicities. Researchers should consult the safety data sheet and handle the compound with appropriate laboratory safety precautions for research use only.
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| References | |
| Additional Infomation |
GAC0003A4 is a research compound identified by the chemical name (3,5-dimethoxyphenyl)-[4-(2-methylphenyl)piperazin-1-yl]methanone. The PubChem CID is 16645461. The compound appears as a white to off-white solid powder. It is classified as an LXR inverse agonist and degrader. All products are for research use only and not for human use.
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| Molecular Formula |
C20H24N2O3
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| Molecular Weight |
340.416165351868
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| Exact Mass |
340.178
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| CAS # |
929492-71-7
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| PubChem CID |
16645461
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| Appearance |
White to off-white solid powder
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| LogP |
3.7
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
25
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| Complexity |
425
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1=CC=CC=C1N2CCN(CC2)C(=O)C3=CC(=CC(=C3)OC)OC
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| InChi Key |
YOXCWYCROVRVBS-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H24N2O3/c1-15-6-4-5-7-19(15)21-8-10-22(11-9-21)20(23)16-12-17(24-2)14-18(13-16)25-3/h4-7,12-14H,8-11H2,1-3H3
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| Chemical Name |
(3,5-dimethoxyphenyl)-[4-(2-methylphenyl)piperazin-1-yl]methanone
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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) |
DMSO :~125 mg/mL (~367.19 mM; with sonication)
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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 | 2.9375 mL | 14.6877 mL | 29.3755 mL | |
| 5 mM | 0.5875 mL | 2.9375 mL | 5.8751 mL | |
| 10 mM | 0.2938 mL | 1.4688 mL | 2.9375 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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