SR10171 is a PPARα agonist. SR10171 is an optimized analog of SR1664 which demonstrates high-affinity binding to PPARγ and unlike SR1664, exhibits partial inverse agonism of PPRE-mediated transcriptional activity and demonstrates modest PPARα agonist activity (EC50=1.5μM). The structure-activity relation-ship (SAR) of SR10171 is consistent with other examples from this chemical series. Importantly, SR10171 effectively blocks phosphorylation of S273 (pS273), which has been shown to correlate with PPARγ insulin sensitizing activity; however, in contrast to full agonist rosiglitazone, SR10171 inverse agonism actively suppresses PPARγ basal transcriptional activity.
MedKoo Cat#: 125877
Name: SR10171
CAS#: 1415321-54-8
Chemical Formula: C34H40N2O4
Exact Mass: 540.2988
Molecular Weight: 540.70
Elemental Analysis: C, 75.53; H, 7.46; N, 5.18; O, 11.84
The following data is based on the product molecular weight 540.70 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 |