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SR1664
CAS No. 1338259-05-4
SR1664( SR 1664 )
Catalog No. M27718 CAS No. 1338259-05-4
SR1664 is a potent and selective PPARγ inhibitor with potential antidiabetic activity. SR1664 binds to PPARγ and potently inhibits Cdk5-mediated PPARγ phosphorylation (IC50 = 80 nM; Ki = 28.67 nM) without exhibiting PPARγ agonist activity.
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| Size | Price / USD | Stock | Quantity |
| 1 mL x 10 mM in DMSO | 119 | In Stock |
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| 2MG | 65 | In Stock |
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| 5MG | 107 | In Stock |
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| 10MG | 140 | In Stock |
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| 25MG | 283 | In Stock |
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| 50MG | 403 | In Stock |
|
| 100MG | 578 | In Stock |
|
| 200MG | 816 | In Stock |
|
| 500MG | Get Quote | In Stock |
|
| 1G | Get Quote | In Stock |
|
Biological Information
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Product NameSR1664
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NoteResearch use only, not for human use.
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Brief DescriptionSR1664 is a potent and selective PPARγ inhibitor with potential antidiabetic activity. SR1664 binds to PPARγ and potently inhibits Cdk5-mediated PPARγ phosphorylation (IC50 = 80 nM; Ki = 28.67 nM) without exhibiting PPARγ agonist activity.
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DescriptionSR1664 is a potent and selective PPARγ inhibitor with potential antidiabetic activity. SR1664 binds to PPARγ and potently inhibits Cdk5-mediated PPARγ phosphorylation (IC50 = 80 nM; Ki = 28.67 nM) without exhibiting PPARγ agonist activity.(In Vitro):Mutagenesis of F282 to alanine (F282A) altered the pharmacology of SR1664 on PPARγ activity, acting as an agonist of the mutant receptor in a transcriptional activity assay, and differentially displacing nuclear receptor co-repressor 1. Together these results suggest that SR1664 actively antagonizes PPARγ through a stereo-specific AF2-mediated, F282-dependent clash, and that stereospecificity confers antagonism within the biaryl indole scaffold.
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In Vitro——
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In Vivo——
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SynonymsSR 1664
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PathwayMetabolic Enzyme/Protease
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TargetPPAR
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RecptorReverse Transcriptase
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Research Area——
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Indication——
Chemical Information
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CAS Number1338259-05-4
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Formula Weight547.611
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Molecular FormulaC33H29N3O5
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Purity>98% (HPLC)
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SolubilityIn Vitro:?DMSO : 100 mg/mL (182.62 mM)
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SMILES[H][C@@](C)(\N=C(/O)c1ccc2n(Cc3ccc(cc3)-c3ccccc3C(O)=O)c(C)c(C)c2c1)c1ccc(cc1)N(=O)=O
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Chemical Name——
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1.Oshima T, et al. Selective extraction of histidine derivatives by metal affinity with a copper(II)-chelating ligand complex in an aqueous two-phase system. J Chromatogr B Analyt Technol Biomed Life Sci. 2015;990:73-79.
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