(Z)-GW 441756
(Z)-GW 441756 is a hepatocyte nuclear factor 4α (HNF4α) activator, with an EC50 of 9.2 μM and a Ka of 4.6 μM in human systems. (Z)-GW 441756 directly interacts with the ligand-binding domain of HNF4α via persistent hydrogen bonds and hydrophobic interactions within the binding pocket. (Z)-GW 441756 reduces the accumulation of triglycerides and total cholesterol. (Z)-GW 441756 inhibits ferroptosis through a non-antioxidant mechanism. (Z)-GW 441756 decreases plasma triglyceride and total cholesterol levels in animal models of hyperlipidemia. (Z)-GW 441756 can be used in studies related to hyperlipidemia.
For research use only. We do not sell to patients.
- CAS No.: 504433-24-3
- Formula: C17H13N3O
- Molecular Weight:275.30
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Sf21 | IC50 |
0.003 μM
Compound: GW441756
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Inhibition of human N- terminal GST-tagged TrkA cytoplasmic domain (436 to 790 residues) expressed in baculovirus infected sf21 cells using biotinylated peptide substrate incubated for 15 mins followed by addition of ATP measured after 30 mins by TR-FRET
Inhibition of human N- terminal GST-tagged TrkA cytoplasmic domain (436 to 790 residues) expressed in baculovirus infected sf21 cells using biotinylated peptide substrate incubated for 15 mins followed by addition of ATP measured after 30 mins by TR-FRET
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[PMID: 27856237] |
| Sf9 | IC50 |
2 nM
Compound: 2
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Inhibition of human TrkA expressed in Sf9 cells by amplified luminescent proximity assay
Inhibition of human TrkA expressed in Sf9 cells by amplified luminescent proximity assay
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[PMID: 18646745] |
(Z)-GW 441756 ((Z)-19) (0.1-100 μM; 24 h) acts as an HNF4α agonist in HEK293T cells overexpressing HNF4α, with an EC50 of 17 μM for activating the luciferase reporter gene[1].
(Z)-GW 441756 (20-50 μM; 48 h) reduces the accumulation of total cholesterol and triglycerides in OA/PA-induced HepG2 cells, with the 20 μM concentration decreasing TC by 20.34% and TG by 38.23%[1].
(Z)-GW 441756 (10-30 μM; 24 h) protects HepG2 and HT22 cells from RSL3 (HY-100218A)-induced ferroptosis in a concentration-dependent manner via a non-antioxidant mechanism, and treatment with 30 μM significantly increases the cell viability of both cell lines[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HepG2
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Concentration:10, 30 μM+ 0.5 μM RSL3
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Incubation Time:24 h
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Result:Significantly increased cell viability in both cell lines at 30 μM.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 (male, 7-8 weeks old)[1]
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Dosage:100 mg/kg
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Administration:i.p.; two doses with a 24-hour interval
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Result:Produced a larger reduction in serum triglyceride levels than reference compound NCT at 200 mg/kg.
Achieved a comparable reduction in serum total cholesterol levels to reference compound NCT at 200 mg/kg.
Resulted in low serum alanine aminotransferase and aspartate aminotransferase levels.
Chemical Information
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CAS No. 504433-24-3
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Molecular Weight 275.30
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Formula C17H13N3O
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SMILES
O=C1/C(C2=NC=CC=C2N1)=C\C3=CN(C)C4=C3C=CC=C4
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
(Z)-GW 441756 Related Classifications
HY-18314B Related Classifications
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