GW6471 | CAS#880635-03-0 | PPAR Antagonist

MedKoo Cat#: 406131 | Name: GW6471

Description:

WARNING: This product is for research use only, not for human or veterinary use.

GW6471 is a PPAR α antagonist (IC50 = 0.24 μ M). GW6471 enhances the binding affinity of the PPAR α ligand-binding domain to the co-repressor proteins SMRT and NCoR.

Chemical Structure

GW6471

CAS#880635-03-0

Theoretical Analysis

MedKoo Cat#: 406131

Name: GW6471

CAS#: 880635-03-0

Chemical Formula: C35H36F3N3O4-

Exact Mass: 619.2658

Molecular Weight: 619.69

Elemental Analysis: C, 67.84; H, 5.86; F, 9.20; N, 6.78; O, 10.33

Price and Availability

Size	Price	Availability
25mg	USD 350.00	2 Weeks
50mg	USD 600.00	2 Weeks
100mg	USD 950.00	2 Weeks
200mg	USD 1,450.00	2 Weeks
500mg	USD 2,850.00	2 Weeks

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Related CAS #

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Synonym

GW6471; GW-6471; GW 6471

IUPAC/Chemical Name

(S,Z)-N-(3-(4-(2-(5-methyl-2-phenyloxazol-4-yl)ethoxy)phenyl)-2-((4-oxo-4-(4-(trifluoromethyl)phenyl)but-2-en-2-yl)amino)propyl)propionamide

InChi Key

TYEFSRMOUXWTDN-DYQICHDWSA-N

InChi Code

InChI=1S/C35H36F3N3O4/c1-4-33(43)39-22-29(40-23(2)20-32(42)26-12-14-28(15-13-26)35(36,37)38)21-25-10-16-30(17-11-25)44-19-18-31-24(3)45-34(41-31)27-8-6-5-7-9-27/h5-17,20,29,40H,4,18-19,21-22H2,1-3H3,(H,39,43)/b23-20-/t29-/m0/s1

SMILES Code

CCC(NC[C@@H](N/C(C)=C\C(C1=CC=C(C(F)(F)F)C=C1)=O)CC2=CC=C(OCCC3=C(C)OC(C4=CC=CC=C4)=N3)C=C2)=O

Appearance

Solid powder

Purity

>98%

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO, not in water

Shelf Life

>5 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Product Data

Product Data

Instruction

View handling instruction

Biological target:

GW6471 is a potent PPARα antagonist.

In vitro activity:

The obtained mammospheres were then treated with the specific PPARα antagonist GW6471, after which, glucose, lipid metabolism, and invasiveness were analyzed. Notably, GW6471 reduced cancer stem cell viability, proliferation, and spheroid formation, leading to apoptosis and metabolic impairment. Reference: Biomedicines. 2021 Jan 28;9(2):127. https://pubmed.ncbi.nlm.nih.gov/33525605/

In vivo activity:

In summary, the capability of GW6471 to increase thorn protein deposition in the liver was also translated to an in vivo system, as it was apparent from collagen and cytokeratin accumulation in GW6471-treated mouse livers. Reference: Cells. 2022 May 10;11(10):1597. https://pubmed.ncbi.nlm.nih.gov/35626634/

	Solvent	mg/mL	mM
Solubility
	DMF	20.0	32.27
	DMF:PBS (pH 7.2) (1:2)	0.3	0.53
	DMSO	70.6	113.96
	Ethanol	12.1	19.47

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 619.69 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

1. Castelli V, Catanesi M, Alfonsetti M, Laezza C, Lombardi F, Cinque B, Cifone MG, Ippoliti R, Benedetti E, Cimini A, d'Angelo M. PPARα-Selective Antagonist GW6471 Inhibits Cell Growth in Breast Cancer Stem Cells Inducing Energy Imbalance and Metabolic Stress. Biomedicines. 2021 Jan 28;9(2):127. doi: 10.3390/biomedicines9020127. PMID: 33525605; PMCID: PMC7912302. 2. Pridgeon CS, Bolhuis DP, Milosavljević F, Manojlović M, Végvári Á, Gaetani M, Jukić MM, Ingelman-Sundberg M. Hepatocyte Thorns, A Novel Drug-Induced Stress Response in Human and Mouse Liver Spheroids. Cells. 2022 May 10;11(10):1597. doi: 10.3390/cells11101597. PMID: 35626634; PMCID: PMC9139950.

In vitro protocol:

In vivo protocol:

1. Pridgeon CS, Bolhuis DP, Milosavljević F, Manojlović M, Végvári Á, Gaetani M, Jukić MM, Ingelman-Sundberg M. Hepatocyte Thorns, A Novel Drug-Induced Stress Response in Human and Mouse Liver Spheroids. Cells. 2022 May 10;11(10):1597. doi: 10.3390/cells11101597. PMID: 35626634; PMCID: PMC9139950.

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