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SR-1664

  Cat. No.:  DC11750   Featured
Chemical Structure
1338259-05-4
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Field of application
SR-1664 is a novel potent, non-agonist PPARγ ligand that blocks the Cdk5-mediated phosphorylation in vitro (IC50=80 nM) and in vivo, without the classical agonism.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 1338259-05-4
Chemical Name: 4'-[[2,3-Dimethyl-5-[[[(1S)-1-(4-nitrophenyl)ethyl]amino]carbonyl]-1H-indol-1-yl]methyl]-[1,1'-biphenyl]-2-carboxylic acid
Synonyms: SR 1664;SR1664
SMILES: C(C1=CC=C(CN2C3=C(C=C(C(N[C@@H](C4=CC=C([N+]([O-])=O)C=C4)C)=O)C=C3)C(C)=C2C)C=C1)1=CC=CC=C1C(O)=O
Formula: C33H29N3O5
M.Wt: 547.6
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: SR-1644 is a novel potent, non-agonist PPARγ ligand that blocks the Cdk5-mediated phosphorylation in vitro (IC50=80 nM) and in vivo, without the classical agonism; exhibits potent anti-diabetic activity while not causing the fluid retention and weight gain that are serious side effects of many of the PPARγ drugs; effectively improves glucose homeostasis, and does not affect bone cell mineralization in culture.
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.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
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DC11750 SR-1664 SR-1664 is a novel potent, non-agonist PPARγ ligand that blocks the Cdk5-mediated phosphorylation in vitro (IC50=80 nM) and in vivo, without the classical agonism.
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