en Sodelglitazar

Sodelglitazar
Clinical data
Pregnancy; category	N/A;
ATC code	None;
Legal status
Legal status	Investigational;
Identifiers
	IUPAC name [4-[[[2-[2-Fluoro-4-(trifluoromethyl)phenyl]-4-methyl-1,3-thiazol-5-yl]methyl]sulfanyl]-2-methylphenoxy]-2-methylpropanoic acid;
CAS Number	447406-78-2;
PubChem CID	9805950;
ChemSpider	7981710;
UNII	6G973E04VI;
KEGG	D06647;
ChEMBL	ChEMBL2104984;
CompTox Dashboard (EPA)	DTXSID90196289 ;
Chemical and physical data
Formula	C23H21F4NO3S2
Molar mass	499.54 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES CC1=C(C=CC(=C1)SCC2=C(N=C(S2)C3=C(C=C(C=C3)C(F)(F)F)F)C)OC(C)(C)C(=O)O;
	InChI InChI=1S/C23H21F4NO3S2/c1-12-9-15(6-8-18(12)31-22(3,4)21(29)30)32-11-19-13(2)28-20(33-19)16-7-5-14(10-17(16)24)23(25,26)27/h5-10H,11H2,1-4H3,(H,29,30); Key:ZUGQWAYOWCBWGM-UHFFFAOYSA-N;

Sodelglitazar, formerly known as GW 677954, is a thiazole PPARδ receptor agonist developed by GlaxoSmithKline.^[2] While it is primarily active at the PPARδ receptor, it is considered a pan agonist with activity at PPARα and PPARγ receptors.^[3]

Safety

Phase 2 studies were terminated prior to completion due to safety findings in rodent studies.^[4]

References

^ US abandoned 7105551, Rodolfo C, Marie GR, Hurst III LM, Lawrence SM, "Thiazole derivatives for treating ppar related disorders", published 1 April 2004, assigned to SmithKlineBeecham
^ Liu XY, Wang RL, Xu WR, Tang LD, Wang SQ, Chou KC (October 2011). "Docking and molecular dynamics simulations of peroxisome proliferator activated receptors interacting with pan agonist sodelglitazar". Protein and Peptide Letters. 18 (10): 1021–7. doi:10.2174/092986611796378701. PMID 21592078.
^ Ottow E, Weinmann H (2008). Nuclear Receptors as Drug Targets. Wiley. pp. 380–. ISBN 978-3-527-31872-8. Retrieved 2 April 2013.
^ "A randomised, double-blind, parallel group, placebo-controlled, multicentre study to evaluate the safety, tolerability and efficacy of oral GW677954 capsules 2.5mg, 5mg, 10mg and 20mg a day for 24 weeks in overweight dyslipidaemic subjects" (PDF). GlaxoSmithKline. 2013-09-01. Archived from the original (PDF) on 6 March 2017.

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[1] US abandoned 7105551, Rodolfo C, Marie GR, Hurst III LM, Lawrence SM, "Thiazole derivatives for treating ppar related disorders", published 1 April 2004, assigned to SmithKlineBeecham

[2] Liu XY, Wang RL, Xu WR, Tang LD, Wang SQ, Chou KC (October 2011). "Docking and molecular dynamics simulations of peroxisome proliferator activated receptors interacting with pan agonist sodelglitazar". Protein and Peptide Letters. 18 (10): 1021–7. doi:10.2174/092986611796378701. PMID 21592078.

[3] Ottow E, Weinmann H (2008). Nuclear Receptors as Drug Targets. Wiley. pp. 380–. ISBN 978-3-527-31872-8. Retrieved 2 April 2013.

[4] "A randomised, double-blind, parallel group, placebo-controlled, multicentre study to evaluate the safety, tolerability and efficacy of oral GW677954 capsules 2.5mg, 5mg, 10mg and 20mg a day for 24 weeks in overweight dyslipidaemic subjects" (PDF). GlaxoSmithKline. 2013-09-01. Archived from the original (PDF) on 6 March 2017.

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[2]

[3]

[4]

Sodelglitazar

Safety

See also

References