Synonym
GW 1929; GW-1929; GW1929.
IUPAC/Chemical Name
(S)-2-((2-benzoylphenyl)amino)-3-(4-(2-(methyl(pyridin-2-yl)amino)ethoxy)phenyl)propanoic acid
InChi Key
QTQMRBZOBKYXCG-MHZLTWQESA-N
InChi Code
InChI=1S/C30H29N3O4/c1-33(28-13-7-8-18-31-28)19-20-37-24-16-14-22(15-17-24)21-27(30(35)36)32-26-12-6-5-11-25(26)29(34)23-9-3-2-4-10-23/h2-18,27,32H,19-21H2,1H3,(H,35,36)/t27-/m0/s1
SMILES Code
O=C(C1=CC=CC=C1)C(C=CC=C2)=C2N[C@H](C(O)=O)CC3=CC=C(OCCN(C4=CC=CC=N4)C)C=C3
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
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
Biological target:
GW1929 is a potent PPAR-γ agonist, with a pKi of 8.84 for human PPAR-γ, and pEC50s of 8.56 and 8.27 for human PPAR-γ and murine PPAR-γ, respectively.
In vitro activity:
Pre-treating neuron cultures with GW1929 inhibited caspase-3 activity, compared with TBBPA treatment, by 57.7 and 94.5 % after 6 and 24 h of exposure, respectively (Fig. 5a). The cytotoxic effect of 10 μM TBBPA, measured based on LDH release, in the presence of GW1929 was also inhibited after 6 and 24 h of exposure to 51.3 and 90.8 %, respectively, compared with the TBBPA-stimulated LDH release (Fig. 5b).
Reference: Neurotox Res. 2014 Apr;25(3):311-22. https://pubmed.ncbi.nlm.nih.gov/24132472/
In vivo activity:
Treatment with GW1929 attenuated VCD-induced increase in ROS levels and decrease in CAT, SOD and GST in comparison with the model group. These observations revealed that GW1929 was able to relieve the oxidative stress in perimenopause rat.
Reference: Am J Transl Res. 2020 May 15;12(5):1884-1893. https://pubmed.ncbi.nlm.nih.gov/32509184/
|
Solvent |
mg/mL |
mM |
| Solubility |
| DMF |
30.0 |
60.54 |
| DMSO |
32.5 |
65.58 |
| DMSO:PBS (pH 7.2) (1:1) |
0.5 |
1.01 |
| Ethanol |
20.0 |
40.36 |
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
495.58
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. Wojtowicz AK, Szychowski KA, Kajta M. PPAR-γ agonist GW1929 but not antagonist GW9662 reduces TBBPA-induced neurotoxicity in primary neocortical cells. Neurotox Res. 2014 Apr;25(3):311-22. doi: 10.1007/s12640-013-9434-z. Epub 2013 Oct 17. PMID: 24132472; PMCID: PMC3936120.
2. Wang X, Xu K, Xiong Y, Li Q, Zhao X. Effects of GW1929 on uterus, ovary and bone metabolism function in perimenopause rats. Am J Transl Res. 2020 May 15;12(5):1884-1893. PMID: 32509184; PMCID: PMC7270032.
In vitro protocol:
1. Wojtowicz AK, Szychowski KA, Kajta M. PPAR-γ agonist GW1929 but not antagonist GW9662 reduces TBBPA-induced neurotoxicity in primary neocortical cells. Neurotox Res. 2014 Apr;25(3):311-22. doi: 10.1007/s12640-013-9434-z. Epub 2013 Oct 17. PMID: 24132472; PMCID: PMC3936120.
In vivo protocol:
1. Wang X, Xu K, Xiong Y, Li Q, Zhao X. Effects of GW1929 on uterus, ovary and bone metabolism function in perimenopause rats. Am J Transl Res. 2020 May 15;12(5):1884-1893. PMID: 32509184; PMCID: PMC7270032.
1: Hahn SS, Tang Q, Zheng F, Zhao S, Wu J. GW1929 inhibits α7 nAChR expression
through PPARγ-independent activation of p38 MAPK and inactivation of PI3-K/mTOR:
The role of Egr-1. Cell Signal. 2014 Apr;26(4):730-9. doi:
10.1016/j.cellsig.2013.12.019. Epub 2014 Jan 8. PubMed PMID: 24412748.
2: Wojtowicz AK, Szychowski KA, Kajta M. PPAR-γ agonist GW1929 but not antagonist
GW9662 reduces TBBPA-induced neurotoxicity in primary neocortical cells. Neurotox
Res. 2014 Apr;25(3):311-22. doi: 10.1007/s12640-013-9434-z. Epub 2013 Oct 17.
PubMed PMID: 24132472; PubMed Central PMCID: PMC3936120.
3: Kaundal RK, Sharma SS. Ameliorative effects of GW1929, a nonthiazolidinedione
PPARγ agonist, on inflammation and apoptosis in focal cerebral
ischemic-reperfusion injury. Curr Neurovasc Res. 2011 Aug 1;8(3):236-45. PubMed
PMID: 21722092.
4: Kaundal RK, Sharma SS. GW1929: a nonthiazolidinedione PPARγ agonist,
ameliorates neurological damage in global cerebral ischemic-reperfusion injury
through reduction in inflammation and DNA fragmentation. Behav Brain Res. 2011
Jan 20;216(2):606-12. doi: 10.1016/j.bbr.2010.09.001. Epub 2010 Sep 15. PubMed
PMID: 20833208.
5: Moore-Carrasco R, Figueras M, Ametller E, López-Soriano FJ, Argilés JM,
Busquets S. Effects of the PPARgamma agonist GW1929 on muscle wasting in
tumour-bearing mice. Oncol Rep. 2008 Jan;19(1):253-6. PubMed PMID: 18097603.
6: Huang WC, Chio CC, Chi KH, Wu HM, Lin WW. Superoxide anion-dependent
Raf/MEK/ERK activation by peroxisome proliferator activated receptor gamma
agonists 15-deoxy-delta(12,14)-prostaglandin J(2), ciglitazone, and GW1929. Exp
Cell Res. 2002 Jul 15;277(2):192-200. PubMed PMID: 12083801.
