SR 16832
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.
For research use only. We do not sell to patients.
- Purity: 99.58%
- CAS No.: 2088135-12-8
- Formula: C17H12ClN3O4
- Molecular Weight:357.75
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Biological Activity
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PPARγ |
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.
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Cell Line:human bronchial epithelial BEAS-2B cells
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Concentration:5 μM
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Incubation Time:4 h, 24 h, 72 h
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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).
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Cell Line:primary normal human bronchial epithelial (NHBE) cells
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Concentration:10 μM
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Incubation Time:4 h, 24 h, 72 h
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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
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CAS No. 2088135-12-8
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Appearance Solid
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Molecular Weight 357.75
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Formula C17H12ClN3O4
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Color White to off-white
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SMILES
O=C(NC1=CC=NC2=CC=C(OC)C=C12)C3=CC([N+]([O-])=O)=CC=C3Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (278 KB)
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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)
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Handling Instructions (2659 KB)
References
[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]
Complete Stock Solution Preparation Table
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.
| 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 |
SR 16832 Related Classifications
HY-112247 Related Classifications
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