SR 1664

Names

[ Name ]:
SR 1664

[Synonym ]:
4'-[(2,3-Dimethyl-5-{[(1S)-1-(4-nitrophenyl)ethyl]carbamoyl}-1H-indol-1-yl)methyl]-2-biphenylcarboxylic acid
[1,1'-Biphenyl]-2-carboxylic acid, 4'-[[2,3-dimethyl-5-[[[(1S)-1-(4-nitrophenyl)ethyl]amino]carbonyl]-1H-indol-1-yl]methyl]-

Biological Activity

[Description]:

SR1664 is a PPARγ antagonist. SR1664 binds to PPARγ and potently inhibits Cdk5-mediated PPARγ phosphorylation (IC50=80 nM; Ki= 28.67 nM)[1][2].

[Related Catalog]:

Signaling Pathways >> Cell Cycle/DNA Damage >> PPAR

Research Areas >> Metabolic Disease

[Target]

PPAR-γ:80 nM (IC50)

[In Vitro]

SR1664 (1uM; HEK293T cells) pharmacological effect on PPARγ activity is altered by mutagenesis of F282 to alanine (F282A)[1].

[References]

[1]. Marciano DP, Kuruvilla DS, Boregowda SV, et al. Pharmacological repression of PPARγ promotes osteogenesis. Nat Commun. 2015;6:7443. Published 2015 Jun 12.

[2]. Choi JH, et al. Antidiabetic actions of a non-agonist PPARγ ligand blocking Cdk5-mediated phosphorylation. Nature. 2011;477(7365):477-481. Published 2011 Sep 4.

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Boiling Point ]:
828.8±65.0 °C at 760 mmHg

[ Molecular Formula ]:
C₃₃H₂₉N₃O₅

[ Molecular Weight ]:
547.601

[ Flash Point ]:
455.0±34.3 °C

[ Exact Mass ]:
547.210693

[ PSA ]:
120.64000

[ LogP ]:
6.75

[ Vapour Pressure ]:
0.0±3.2 mmHg at 25°C

[ Index of Refraction ]:
1.648

[ Storage condition ]:
2-8°C

MSDS

Click to get detail MSDS

Safety Information

[ Hazard Statements ]:
H413

[ RIDADR ]:
NONH for all modes of transport