SR 16832 Chemical Properties

Boiling point:

492.3±45.0 °C(Predicted)

Density 

1.469±0.06 g/cm3(Predicted)

storage temp. 

Store at -20°C

solubility 

DMSO: soluble

form 

A crystalline solid

pka

9.71±0.43(Predicted)

color 

White to off-white

InChI

InChI=1S/C17H12ClN3O4/c1-25-11-3-5-15-13(9-11)16(6-7-19-15)20-17(22)12-8-10(21(23)24)2-4-14(12)18/h2-9H,1H3,(H,19,20,22)

InChIKey

CVTZAGCRUDYUGB-UHFFFAOYSA-N

SMILES

C(NC1C2C(N=CC=1)=CC=C(OC)C=2)(=O)C1=CC([N+]([O-])=O)=CC=C1Cl

SR 16832 Usage And Synthesis

Description

SR 16832 is a dual-site covalent antagonist of peroxisome proliferator-activated receptor γ (PPARγ). It inhibits MRL20-induced allosteric activation of PPARγ in a reporter assay using HEK293T cells when used at a concentration of 5 μM. SR 16832 also reduces basal activity of PPARγ and inhibits binding of docosahexaenoic acid to PPARγ in a time-resolved FRET (TR-FRET) assay.

Uses

SR 16832 is a dual site PPARγ inhibitor. Acts at orthosteric and allosteric sites in the ligand binding domain. Inhibits binding of endogenous ligands and transcriptional activity of PPARγ, more effectively than the orthosteric covalent antagonists.

Biological Activity

SR16832 is a PPARγ antagonist. It acts as a dual-site covalent inhibitor of PPARγ inhibiting both orthosteric and allosteric cellular activation by the PPARγ agonists.

IC 50

PPARγ

storage

Store at +4°C

References

[1] RICHARD BRUST. Modification of the Orthosteric PPARγ Covalent Antagonist Scaffold Yields an Improved Dual-Site Allosteric Inhibitor[J]. ACS Chemical Biology, 2017, 12 4: 969-978. DOI:10.1021/acschembio.6b01015.
[2] SHANG J, KOJETIN D. Crystal Structure of Human PPARgamma Ligand Binding Domain in Complex with SR16832[C]. 2018: 0. DOI:10.2210/pdb6aug/pdb.

GRADES AVAILABLE

SR 16832 is supplied as a crystalline solid. A stock solution may be made by dissolving the SR 16832 in the solvent of choice, which should be purged with an inert gas. SR 16832 is soluble in the organic solvent DMSO.

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