SR 16832

Name: SR 16832
Brand: MedChemExpress
SKU: HY-112247
Rating: 4.5 (1 reviews)

Cat. No.: HY-112247 Purity: 99.58%: Data Sheet
COA

SDS
Handling Instructions
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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.

SR 16832 Chemical Structure

CAS No. : 2088135-12-8

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
500 mg	Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

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PPARα PPARβ/δ PPARγ PPAR PPARδ

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

PPARγ

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).

Molecular Weight

357.75

Formula

C₁₇H₁₂ClN₃O₄

CAS No.

2088135-12-8

Appearance

Solid

Color

White to off-white

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the 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.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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In Vivo Dissolution Calculator

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Working solution concentration: mg/mL

Purity & Documentation

Purity: 99.58%

Select Batch:

Data Sheet (278 KB) SDS (254 KB)

COA (252 KB) HNMR (263 KB) LCMS (341 KB)

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

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

Metabolic Disease Inflammation/Immunology

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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SR 16832

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Complete Stock Solution Preparation Table

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