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.

This pharmacology-related article is a stub. You can help Wikipedia by expanding it.

[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.

[1]

[2]

[3]

[4]

v t e PPARTooltip Peroxisome proliferator-activated receptor modulators
PPARαTooltip Peroxisome proliferator-activated receptor alpha	Agonists: 15-HETE 15-HpETE Aleglitazar Aluminium clofibrate Arachidonic acid Bezafibrate Chiglitazar Clofibrate CP-775146 Daidzein DHEA (prasterone) (in rodents) Elafibranor Etomoxir Fenofibrate Genistein Gemfibrozil GW-7647 Lanifibranor Leukotriene B₄ LG-101506 LG-100754 Lobeglitazone Muraglitazar Oleylethanolamide Palmitoylethanolamide Pemafibrate Perfluorononanoic acid Perfluorooctanoic acid Pioglitazone Saroglitazar Sodelglitazar Tesaglitazar Tetradecylthioacetic acid Troglitazone WY-14643 Antagonists: GW-6471 MK-886
PPARδTooltip Peroxisome proliferator-activated receptor delta	Agonists: 15-HETE 15-HpETE Arachidonic acid Bezafibrate Daidzein Elafibranor Fonadelpar Genistein GW-0742 GW-501516 L-165,041 Lanifibranor LG-101506 Seladelpar Sodelglitazar Tetradecylthioacetic acid Antagonists: FH-535 GSK-0660 GSK-3787
PPARγTooltip Peroxisome proliferator-activated receptor gamma	Agonists: 5-Oxo-ETE 5-Oxo-15-hydroxy-ETE 15-Deoxy-Δ^12,14-prostaglandin J₂ 15-HETE 15-HpETE Aleglitazar Arachidonic acid Balaglitazone Berberine Bezafibrate Cannabidiol Cevoglitazar Chiglitazar Ciglitazone Daidzein Darglitazone Edaglitazone Efatutazone Englitazone Etalocib Farglitazar Genistein GW-1929 Ibuprofen Imiglitazar Indeglitazar Lanifibranor LG-100268 LG-100754 LG-101506 Lobeglitazone Muraglitazar (muroglitazar) nTZDpa Naveglitazar Netoglitazone Oxeglitazar Peliglitazar Pemaglitazar Perfluorononanoic acid Pioglitazone Prostaglandin J₂ Ragaglitazar Reglitazar Rivoglitazone Rosiglitazone RS5444 Saroglitazar Sipoglitazar Sodelglitazar Telmisartan Tesaglitazar Troglitazone SPPARMsTooltip Selective PPARγ modulator: BADGE EPI-001 INT-131 MK-0533 S26948 Antagonists: FH-535 GW-9662 SR-202 T-0070907 Unknown: SR-1664
Non-selective	Agonists: Ciprofibrate Clinofibrate Clofibride Englitazone Etofibrate Farglitazar Netoglitazone Ronifibrate Rivoglitazone Simfibrate
See also Receptor/signaling modulators

Safety

See also

References