Referencia número: HY-112247

SR 16832

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Based on 1 Customer Validation

SR 16832 is a dual-site covalent, orthosteric and allosteric PPARγ antagonist. SR 16832 activates the TGF-β signaling pathway and upregulates the expression of Vimentin and Fibronectin (Fibronectin). SR 16832 is toxic to bronchial epithelium. SR 16832 can be used in research related to type 2 diabetes and pulmonary fibrosis.

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Pureza: 99.58%
No. CAS: 2088135-12-8
Fòrmula: C₁₇H₁₂ClN₃O₄
Peso molecular:357.75

Almacenamiento:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

SR 16832 Chemical Structure

No. CAS: 2088135-12-8

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Amount: USD 0.00

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Actividad biológica
- Descripciòn
- IC₅₀ & Target
- In Vitro
Chemical Information
Solvente y solubilidad
- In Vitro
Pureza y Documentación
Referencias
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

IC₅₀ & Target^[1]

PPARγ

Ver todos los productos específicos de isoformas PPAR :

Ver todos los productos específicos de isoformas TGF-beta/Smad :

Smad1
Smad3

In Vitro

SR 16832 (5 μM MRL20 post-treatment) completely inhibits allosteric cellular activation of Gal4-PPARγ LBD by MRL20 in HEK293T cells, while having minimal impact on basal Gal4-PPARγ LBD activity^[1].
SR 16832 lowers basal transactivation of full-length PPARγ and completely inhibits allosteric cellular activation of full-length PPARγ by MRL20 in HEK293T cells^[1].
SR 16832 weakens the allosteric potency of MRL20 to recruit TRAP220 coactivator peptide to purified PPARγ LBD, including in the presence of RXRα LBD^[1].
SR 16832 completely blocks allosteric binding of rosiglitazone to purified PPARγ LBD, preventing TRAP220 coactivator peptide recruitment^[1].
SR 16832 weakens the allosteric potency of MRL20 to modulate NCoR corepressor peptide binding to purified PPARγ LBD^[1].
SR 16832 completely inhibits allosteric cellular activation of Gal4-PPARγ LBD by Rosiglitazone (HY-17386) in HEK293T cells^[1].
SR 16832 (1, 2, ..., 200 μM) exhibits cytotoxicity in human bronchial epithelial BEAS-2B cells with an EC₂₀ of 5 μM^[2].
SR 16832 (5 μM; 4, 24, and 72 h) activates TGF-β signaling, increases inflammation, and upregulates vimentin and fibronectin expression in human bronchial epithelial BEAS-2B cells^[2].
SR 16832 (10 μM; 4, 24, and 72 h) activates TGF-β signaling, increases inflammation, and upregulates vimentin and fibronectin expression in primary normal human bronchial epithelial (NHBE) cells^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis^[2]

Cell Line:

human bronchial epithelial BEAS-2B cells
Concentration:

5 μM
Incubation Time:

4 h, 24 h, 72 h
Result:

Increased TGF-β expression 2-fold relative to control at 4 h (p < 0.01).
Increased TNF-α expression 1.5-fold relative to control at 24 h (p < 0.01).
Increased vimentin expression 3-fold relative to control at 24 h (p < 0.001).
Increased fibronectin expression 3.5-fold relative to control at 72 h (p < 0.001).

Western Blot Analysis^[2]

Cell Line:

primary normal human bronchial epithelial (NHBE) cells
Concentration:

10 μM
Incubation Time:

4 h, 24 h, 72 h
Result:

Increased TGF-β expression 4-fold relative to control at 4 h (p < 0.001).
Increased TNF-α expression 1.5-fold relative to control at 24 h (p < 0.01).
Increased vimentin expression 3.5-fold relative to control at 24 h (p < 0.01).
Increased fibronectin expression 4.5-fold relative to control at 72 h (p < 0.001).

Chemical Information

No. CAS 2088135-12-8
Appearance Solid
Peso molecular 357.75
Fòrmula C₁₇H₁₂ClN₃O₄
Color White to off-white
SMILES

O=C(NC1=CC=NC2=CC=C(OC)C=C12)C3=CC([N+]([O-])=O)=CC=C3Cl
Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvente y solubilidad

In Vitro:

DMSO : 250 mg/mL (698.81 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.7952 mL

13.9762 mL

27.9525 mL

5 mM

0.5590 mL

2.7952 mL

5.5905 mL

10 mM

0.2795 mL

1.3976 mL

2.7952 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Calculadora de molaridad

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (278 KB)
SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instrucciones de manejo (2659 KB)

Referencias

[1]. Brust R, et al. Modification of the Orthosteric PPARγ Covalent Antagonist Scaffold Yields an Improved Dual-Site Allosteric Inhibitor. ACS Chem Biol. 2017;12(4):969-978. [Content Brief]

[2]. Jeong J, et al. Advancing the Adverse Outcome Pathway for PPARγ Inactivation Leading to Pulmonary Fibrosis Using Bradford-Hill Consideration and the Comparative Toxicogenomics Database. Chem Res Toxicol. 2022 Feb 21;35(2):233-243. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.7952 mL	13.9762 mL	27.9525 mL	69.8812 mL
	5 mM	0.5590 mL	2.7952 mL	5.5905 mL	13.9762 mL
	10 mM	0.2795 mL	1.3976 mL	2.7952 mL	6.9881 mL
	15 mM	0.1863 mL	0.9317 mL	1.8635 mL	4.6587 mL
	20 mM	0.1398 mL	0.6988 mL	1.3976 mL	3.4941 mL
	25 mM	0.1118 mL	0.5590 mL	1.1181 mL	2.7952 mL
	30 mM	0.0932 mL	0.4659 mL	0.9317 mL	2.3294 mL
	40 mM	0.0699 mL	0.3494 mL	0.6988 mL	1.7470 mL
	50 mM	0.0559 mL	0.2795 mL	0.5590 mL	1.3976 mL
	60 mM	0.0466 mL	0.2329 mL	0.4659 mL	1.1647 mL
	80 mM	0.0349 mL	0.1747 mL	0.3494 mL	0.8735 mL
	100 mM	0.0280 mL	0.1398 mL	0.2795 mL	0.6988 mL

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SR 16832

Covalent Screening Library

Differentiation Inducing Compound Library

Anti-Obesity Compound Library

Angiogenesis-Related Compound Library

Transcription Factor-Targeted Library

Lipid Metabolism Compound Library

Anti-Liver Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Nuclear Receptor Compound Library

Osteogenesis Compound Library

Cancer Stem Cells Compound Library

Coagulation and Anti-coagulation Compound Library

Heterocyclic Compound Library

Metabolic Enzyme Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Covalent Screening Library Plus

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Cell Cycle/DNA Damage Compound Library

Immunology/Inflammation Compound Library

Metabolism/Protease Compound Library

Stem Cell Signaling Compound Library

TGF-beta/Smad Compound Library

Wnt/Hedgehog/Notch Compound Library

Anti-Aging Compound Library

Ver todos los productos específicos de isoformas PPAR

Ver todos los productos específicos de isoformas TGF-beta/Smad

Actividad biológica

Chemical Information

Solvente y solubilidad

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

SR 16832 Related Classifications

HY-112247 Related Classifications