SR 16832

Product Name: SR 16832
CAS No.: 2088135-12-8
Chemical Name: SR 16832
Synonyms: SR 16832;2-Chloro-N-(6-methoxy-4-quinolinyl)-5-nitrobenzamide;2-Chloro-N-(6-methoxyquinolin-4-yl)-5-nitrobenzamide;Benzamide, 2-chloro-N-(6-methoxy-4-quinolinyl)-5-nitro-;inhibit,Inhibitor,SR 16832,Peroxisome proliferator-activated receptors,PPAR
CBNumber: CB64902739
Molecular Formula: C17H12ClN3O4
Formula Weight: 357.75
MOL File: 2088135-12-8.mol

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SR 16832 Property

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

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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Cayman Chemical

Product number: 27632
Product name: SR 16832
Packaging: 5mg
Price: $95
Updated: 2024/03/01

Cayman Chemical

Product number: 27632
Product name: SR 16832
Packaging: 25mg
Price: $384
Updated: 2024/03/01

Cayman Chemical

Product number: 27632
Product name: SR 16832
Packaging: 1mg
Price: $36
Updated: 2024/03/01

Cayman Chemical

Product number: 27632
Product name: SR 16832
Packaging: 10mg
Price: $172
Updated: 2024/03/01

Tocris

Product number: 6383
Product name: SR16832
Purity: ≥98%(HPLC)
Packaging: 5
Price: $107
Updated: 2021/12/16

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SR 16832 Chemical Properties,Usage,Production

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.

SR 16832 Preparation Products And Raw materials

Raw materials

Preparation Products

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SR 16832 Suppliers

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2088135-12-8, SR 16832Related Search:

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2-Chloro-N-(6-methoxy-4-quinolinyl)-5-nitrobenzamide

SR 16832

Benzamide, 2-chloro-N-(6-methoxy-4-quinolinyl)-5-nitro-

2-Chloro-N-(6-methoxyquinolin-4-yl)-5-nitrobenzamide

inhibit,Inhibitor,SR 16832,Peroxisome proliferator-activated receptors,PPAR

2088135-12-8