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516567 PPARβ/δ Antagonist, GSK3787 - CAS 188591-46-0 - Calbiochem

The PPARβ/δAntagonist II, PT-S58, also referenced under CAS 188591-46-0, controls the biological activity of PPARβ/δ. This small molecule/inhibitor is primarily used for Biochemicals applications.

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: 4-Chloro-N-(2-((5-trifluoromethyl)-2-pyridyl) sulfonyl)ethyl)benzamide, PPARβ Antagonist I, PPARδ Antagonist I

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516567
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Overview

Replacement Information

Key Specifications Table

CAS #Empirical Formula
188591-46-0C₁₅H₁₂ClF₃N₂O₃S

Products

Catalog NumberPackaging Qty/Pack
516567-10MG Glass bottle 10 mg
Description
OverviewA cell-permeable pyridylsulfone that acts as a selective, high affinity PPARβ (PPARδ) ligand (IC50 in PPAR ligand displacement assays = 200 nM against human PPARβ and >10 µM against PPARα or PPARγ) and effectively antagonizes agonist-induced, but not basal, PPARβ transcription activity both in cultures in vitro (IC50 = 126 nM in CV-1 cells) and in mice in vivo (82% and 71% inhibition of 10 mg/kg GW0742-induced Adrp and Angptl4 mRNA upregulation, respectively, in colon epithelium; 10 mg/kg GSK3787; p.o.) by covalently modifying PPARβ at Cys249. GSK3787 is also shown to exhibit weak agonistic activity toward PPARγ (1.2-fold increase above basal level by 1 µM GSK3787), and effectively block the more potent agonist GW1929 (Cat. Nos. 370695) from further stimulation (1.5 and 3.5-fold above basal by 0.3 µM GW1929 in the presence or absence of 1 µM GSK3787, respectively).
Catalogue Number516567
Brand Family Calbiochem®
Synonyms4-Chloro-N-(2-((5-trifluoromethyl)-2-pyridyl) sulfonyl)ethyl)benzamide, PPARβ Antagonist I, PPARδ Antagonist I
References
ReferencesPalkar, P.S., et al. 2010. Mol. Pharmacol. 78, 419.
Shearer, B,G., et al. 2010. J. Med. Chem. 53, 1857.
Product Information
CAS number188591-46-0
FormWhite solid
Hill FormulaC₁₅H₁₂ClF₃N₂O₃S
Chemical formulaC₁₅H₁₂ClF₃N₂O₃S
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Purity≥99% by HPLC
Physicochemical Information
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
Toxicity Standard Handling
Storage +2°C to +8°C
Protect from Light Protect from light
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications
Global Trade Item Number
Catalog Number GTIN
516567-10MG 04055977198201

Documentation

PPARβ/δ Antagonist, GSK3787 - CAS 188591-46-0 - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

PPARβ/δ Antagonist, GSK3787 - CAS 188591-46-0 - Calbiochem Certificates of Analysis

TitleLot Number
516567

References

Reference overview
Palkar, P.S., et al. 2010. Mol. Pharmacol. 78, 419.
Shearer, B,G., et al. 2010. J. Med. Chem. 53, 1857.
Data Sheet

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision02-October-2012 JSW
Synonyms4-Chloro-N-(2-((5-trifluoromethyl)-2-pyridyl) sulfonyl)ethyl)benzamide, PPARβ Antagonist I, PPARδ Antagonist I
DescriptionA cell-permeable and orally available pyridylsulfone compound that acts as a selective, high affinity PPARβ (PPARδ) ligand (IC50 in PPAR ligand displacement assays = 200 nM against human PPARβ and >10 µM against PPARα or PPARγ) and effectively antagonizes agonist-induced, but not basal, PPARβ transcription activity both in cultures in vitro (IC50 = 126 nM against 2 nM GW501516-induced reporter transcription in CV-1 cells) and in mice in vivo (82% and 71% inhibition of 10 mg/kg GW0742-induced Adrp and Angptl4 mRNA upregulation, respectively, in colon epithelium by 10 mg/kg GSK3787; p.o.) by covalently modifying PPARβ at Cys249. GSK3787 is also shown to exhibit weak agonistic activity toward PPARγ (1.2-fold increase above basal level by 1 µM GSK3787), and effectively block the more potent agonist GW1929 (Cat. Nos. 370695) from further stimulation (1.5 and 3.5-fold above basal by 0.3 µM GW1929 in the presence or absence of 1 µM GSK3787, respectively).
FormWhite solid
Intert gas (Yes/No) Packaged under inert gas
CAS number188591-46-0
Chemical formulaC₁₅H₁₂ClF₃N₂O₃S
Structure formulaStructure formula
Purity≥99% by HPLC
SolubilityDMSO (50 mg/ml; clear, colorless solution)
Storage Protect from light
+2°C to +8°C
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Toxicity Standard Handling
ReferencesPalkar, P.S., et al. 2010. Mol. Pharmacol. 78, 419.
Shearer, B,G., et al. 2010. J. Med. Chem. 53, 1857.