Bioactivity | 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]. | ||||||||||||
Invitro | SR1664 (1uM; HEK293T cells) pharmacological effect on PPARγ activity is altered by mutagenesis of F282 to alanine (F282A)[1]. | ||||||||||||
Name | SR1664 | ||||||||||||
CAS | 1338259-05-4 | ||||||||||||
Formula | C33H29N3O5 | ||||||||||||
Molar Mass | 547.60 | ||||||||||||
Appearance | Solid | ||||||||||||
Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
Storage |
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Reference | [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. |