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GW4064 | non-steroidal FXR agonist

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Price:
$69.00
Catalog #:
C4940-5
Quantity:


Product Description

GW4064 is a potent, orally-available, non-steroidal, isoxazole-based agonist of FXR with an EC50 of 15 nM. In a Fisher rat model, GW4064 was found to lower serum triglyceride levels in a dose-dependent manner and an ED50 of 20 mg/kg. (1)

In C57BL/6 mice, GW4064 has been shown to stimulate plasma corticosterone levels, thus suggesting a role in the modulation of adrenal cholesterol metabolism and glucocorticoid synthesis. (2)

Followup SAR studies have led to equipotent FXR analogs of GW4064 with improved developability parameters, including reduced toxicity and cholestasis. (3)


Technical information:

Chemical Formula:   C28H22Cl3NO4
CAS #:   278779-30-9
Molecular Weight:   542.84
Purity:   > 98%
Appearance:   white
Chemical Name:   (E)-3-(2-chloro-4-((3-(2,6-dichlorophenyl)-5-isopropylisoxazol-4-yl)methoxy)styryl)benzoic acid
Solubility:   Up to 100 mM in DMSO
Synonyms:   GW4064, GW-4064, GW 4064

Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.


Reference:

1. Maloney et al., Identification of a Chemical Tool for the Orphan Nuclear Receptor FXR. J. Med. Chem. 2000, 43(16), 2971-2974. Pubmed ID: 10956205
2. Hoekstra et al., FXR agonist GW4064 increases plasma glucocorticoid levels in C57BL/6 mice. Mol. Cell. Endocrinol. 2012, 362, 69-75. Pubmed ID: 22643070
3. Akwabi-Ameyaw et al., Conformationally constrained farnesoid X receptor (FXR) agonists: Naphthoic acid-based analogs of GW 4064. Bioorg. Med. Chem. Lett. 2008, 18, 4339-4343. Pubmed ID: 18621523

Other Information:

Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.

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