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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 |
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| 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
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Alliin
Alliin is a garlic organosulfur compound that possesses various pharmacological properties.alliin protected against LPS-induced ALI by activating PPARγ which subsequently inhibited LPS-induced NF-κB activation and inflammatory response.?
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GW 6471
GW6471 is an antagonist of PPARα with IC50 of 0.24 μ M. GW6471 enhances the binding affinity of the PPAR α ligand-binding domain to the co-repressor proteins SMRT and NCoR.A specific PPARα antagonist.
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GW7647
GW7647 is a potent agonist of PPARα (EC50s: 6 nM, 1.1 μM, and 6.2 μM for human PPARα, PPARγ, and PPARδ, respectively).GW7647 (50 nM) stimulates the PI3K phosphorylation followed by the Akt (Ser473) phosphorylation, which causes NOS1 phosphorylation increased the amounts of NO released in the stripped antral mucosa.
