WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H522711
CAS#: 622402-22-6 (free acid)
Description: GW590735 is a potent and selective agonist of PPARα with an EC50 value of 4 nM for the expression a GAL4-responsive reporter gene and at least 500-fold selectivity versus PPARγ and PPARδ. GW590735 significantly increased HDL cholesterol, decreased LDL and VLDL cholesterol, and significantly reduced triglycerides. Maximal increases in HDL cholesterol were 37%, 53%, and 84% with fenofibrate, torcetrapib, and GW590735, respectively.
Hodoodo Cat#: H522711
Name: GW590735
CAS#: 622402-22-6 (free acid)
Chemical Formula: C23H21F3N2O4S
Exact Mass: 478.12
Molecular Weight: 478.486
Elemental Analysis: C, 57.73; H, 4.42; F, 11.91; N, 5.85; O, 13.37; S, 6.70
Related CAS #: 343322-50-9 (sodium) 622402-22-6 (free acid)
Synonym: GW590735; GW-590735; GW 590735.
IUPAC/Chemical Name: 2-methyl-2-(4-((4-methyl-2-(4-(trifluoromethyl)phenyl)thiazole-5-carboxamido)methyl)phenoxy)propanoic acid
InChi Key: ILUPZUOBHCUBKB-UHFFFAOYSA-N
InChi Code: InChI=1S/C23H21F3N2O4S/c1-13-18(33-20(28-13)15-6-8-16(9-7-15)23(24,25)26)19(29)27-12-14-4-10-17(11-5-14)32-22(2,3)21(30)31/h4-11H,12H2,1-3H3,(H,27,29)(H,30,31)
SMILES Code: CC(OC1=CC=C(CNC(C2=C(C)N=C(C3=CC=C(C(F)(F)F)C=C3)S2)=O)C=C1)(C)C(O)=O
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
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: >2 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:
| Biological target: | |
| In vitro activity: | |
| In vivo activity: |
The following data is based on the product molecular weight 478.49 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: | |
| In vitro protocol: | |
| In vivo protocol: |
1: Hansen MK, McVey MJ, White RF, Legos JJ, Brusq JM, Grillot DA, Issandou M,
Barone FC. Selective CETP inhibition and PPARalpha agonism increase HDL
cholesterol and reduce LDL cholesterol in human ApoB100/human CETP transgenic
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10.1177/1074248410362891. Epub 2010 Mar 23. PubMed PMID: 20332533.
2: Velkov T, Rimmer KA, Headey SJ. Ligand-enhanced expression and in-cell assay
of human peroxisome proliferator-activated receptor alpha ligand binding domain.
Protein Expr Purif. 2010 Apr;70(2):260-9. doi: 10.1016/j.pep.2009.09.012. Epub
2009 Sep 24. PubMed PMID: 19782138.
3: Christodoulides C, Dyson P, Sprecher D, Tsintzas K, Karpe F. Circulating
fibroblast growth factor 21 is induced by peroxisome proliferator-activated
receptor agonists but not ketosis in man. J Clin Endocrinol Metab. 2009
Sep;94(9):3594-601. doi: 10.1210/jc.2009-0111. Epub 2009 Jun 16. PubMed PMID:
19531592.
4: Billin AN. PPAR-beta/delta agonists for Type 2 diabetes and dyslipidemia: an
adopted orphan still looking for a home. Expert Opin Investig Drugs. 2008
Oct;17(10):1465-71. doi: 10.1517/13543784.17.10.1465 . Review. PubMed PMID:
18808307.
5: Risérus U, Sprecher D, Johnson T, Olson E, Hirschberg S, Liu A, Fang Z, Hegde
P, Richards D, Sarov-Blat L, Strum JC, Basu S, Cheeseman J, Fielding BA,
Humphreys SM, Danoff T, Moore NR, Murgatroyd P, O'Rahilly S, Sutton P, Willson T,
Hassall D, Frayn KN, Karpe F. Activation of peroxisome proliferator-activated
receptor (PPAR)delta promotes reversal of multiple metabolic abnormalities,
reduces oxidative stress, and increases fatty acid oxidation in moderately obese
men. Diabetes. 2008 Feb;57(2):332-9. Epub 2007 Nov 16. PubMed PMID: 18024853.
6: Sierra ML, Beneton V, Boullay AB, Boyer T, Brewster AG, Donche F, Forest MC,
Fouchet MH, Gellibert FJ, Grillot DA, Lambert MH, Laroze A, Le Grumelec C, Linget
JM, Montana VG, Nguyen VL, Nicodème E, Patel V, Penfornis A, Pineau O, Pohin D,
Potvain F, Poulain G, Ruault CB, Saunders M, Toum J, Xu HE, Xu RX, Pianetti PM.
Substituted 2-[(4-aminomethyl)phenoxy]-2-methylpropionic acid PPARalpha agonists.
1. Discovery of a novel series of potent HDLc raising agents. J Med Chem. 2007
Feb 22;50(4):685-95. Epub 2007 Jan 23. PubMed PMID: 17243659.
