GSK3787
GSK3787 is a novel and irreversible antagonist of the peroxisome proliferator-activated receptor-β/δ (PPAR-β/δ) that covalently binds to a cysteine residue in the ligand-binding domain of PPAR- β/δ. Although it responses to ligand activation to modulate the association of both PPAR-β/δ and PPAR-γ coregulator peptides, GSK3787 exhibits considerably higher antagonism of PPAR-β/δ than that of PPAR-γ. Results of recent studies have shown that oral administration of GSK3787 results in the antagonism of GW0742-induced overexpression of Angptl4 and Adrp mRNA in wild-type mouse colon, which is correlated with reduced promoter occupancy of PPAR-β/δ on the Angptl4 and Adrp genes.
Reference
Palkar PS, Borland MG, Naruhn S, Ferry CH, Lee C, Sk UH, Sharma AK, Amin S, Murray IA, Anderson CR, Perdew GH, Gonzalez FJ, Müller R, Peters JM. Cellular and pharmacological selectivity of the peroxisome proliferator-activated receptor-beta/delta antagonist GSK3787. Mol Pharmacol. 2010;78(3):419-430
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 392.78 |
| Cas No. | 188591-46-0 |
| Formula | C15H12ClF3N2O3S |
| Synonyms | GSK-3787,GSK 3787 |
| Solubility | insoluble in H2O; ≥15.8 mg/mL in DMSO; ≥2.89 mg/mL in EtOH with gentle warming and ultrasonic |
| Chemical Name | 4-chloro-N-[2-[5-(trifluoromethyl)pyridin-2-yl]sulfonylethyl]benzamide |
| SDF | Download SDF |
| Canonical SMILES | C1=CC(=CC=C1C(=O)NCCS(=O)(=O)C2=NC=C(C=C2)C(F)(F)F)Cl |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Cell experiment [1]: | |
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Cell lines |
Fibroblasts, keratinocytes, skin cancer cell A341, cancer cell lines MCF7 (breast), Huh7 (liver), and HepG2 (liver) cells, Huh7, HepG2 cells |
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Preparation method |
The solubility of this compound in DMSO is > 15.8 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reacting condition |
0.1-1.0 μM, 24 h |
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Applications |
GSK3787 (1 μM) completely antagonized 50 nM GW0742-induced PPARβ/δ-dependent Angptl4 gene expression in wild-type fibroblasts and in keratinocytes. GSK3787 (1 μM) largely antagonized 50 nM GW0742-induced Angptl4 and Adrp mRNAs expression in skin cancer cell A341. GSK3787 (1 μM) largely antagonized GW0742-induced Angptl4 mRNAs expression in cancer cell lines MCF7 (breast), Huh7 (liver), and HepG2 (liver) cells. GSK3787 (1 μM) largely antagonizesd GW0742-induced increase of Adrp mRNA in Huh7 and HepG2 cells. |
| Animal experiment [1]: | |
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Animal models |
male wild-type and Pparβ/δ-null mice |
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Dosage form |
10 mg/kg, oral gavage 3 h before euthanasia |
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Application |
Administration of GSK3787 (10 mg/kg) effectively prevented the GW0742-induced expression of both Angptl4 and Adrp mRNA in wild-type mouse colon epithelium, which was correlated with reduced promoter occupancy of PPARβ/δ on the Angptl4 and Adrp genes. Administration of GSK3787 showed no effect on glucose tolerance. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1]. Palkar P S, Borland M G, Naruhn S, et al. Cellular and pharmacological selectivity of the peroxisome proliferator-activated receptor-β/δ antagonist GSK3787[J]. Molecular pharmacology, 2010, 78(3): 419-430. | |
| Description | GSK3787 is an irreversible antagonist of PPARβ/δ with pIC50 value of 6.6. | |||||
| Targets | PPARβ | PPARδ | ||||
| IC50 | 6.6 (pIC50) | 6.6 (pIC50) | ||||
Quality Control & MSDS
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Chemical structure
