1. Vitamin D Related/Nuclear Receptor Apoptosis
  2. Orphan Nuclear Receptor Ferroptosis
  3. (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.

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(Z)-GW 441756

(Z)-GW 441756 Chemical Structure

CAS No. : 504433-24-3

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Description

(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[1].

In Vitro

(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.

Cell Viability Assay[1]

Cell Line: HepG2
Concentration: 10, 30 μM+ 0.5 μM RSL3
Incubation Time: 24 h
Result: Significantly increased cell viability in both cell lines at 30 μM.
In Vivo

(Z)-GW 441756 (100 mg/kg; i.p.; two doses with a 24-hour interval) reduces serum triglyceride and total cholesterol levels in an acute dyslipidemia mouse model[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6 (male, 7-8 weeks old)[1]
Dosage: 100 mg/kg
Administration: i.p.; two doses with a 24-hour interval
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.
Molecular Weight

275.30

Formula

C17H13N3O

CAS No.
SMILES

O=C1/C(C2=NC=CC=C2N1)=C\C3=CN(C)C4=C3C=CC=C4

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Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
(Z)-GW 441756
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HY-18314B
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