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GSK3787
GSK3787 is a selective and irreversible antagonist of PPARδ with pIC50 of 6.6, with no measurable affinity for hPPARα or hPPARγ.
CAS No. 188591-46-0
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純度：
99.46%
99.46
GSK3787関連製品
シグナル伝達経路
PPAR阻害剤の選択性比較
生物活性
| 製品説明 | GSK3787 is a selective and irreversible antagonist of PPARδ with pIC50 of 6.6, with no measurable affinity for hPPARα or hPPARγ. | ||
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| Targets |
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| In Vitro | ||||
| In vitro |
GSK3787 irreversibly antagonizes human and mouse PPARδ that covalently modifies Cys249 within the ligand binding pocket. GSK3787 (1 μM) effectively antagonizes the agonist GW0742 stimulated transcription of CPT1a and PDK4 in human skeletal muscle cells, and effectively antagonize the basal gene expression of CPT1a. GSK 3787 shows no effective antiproliferative activity against colorectal cancer cells. [1] GSK3787 (1 μM) completely antagonizes 50 nM GW0742-induced PPARβ/δ-dependent Angptl4 gene expression in wild-type fibroblasts and in keratinocytes. GSK3787 (1 μM) largely antagonizes 50 nM GW0742-induced Angptl4 and Adrp mRNAs expression in skin cancer cell A341. GSK3787 (1 μM) largely antagonizes GW0742-induced Angptl4 mRNAs expression in cancer cell lines MCF7 (breast), Huh7 (liver), and HepG2 (liver) cells but not in H1838 or A549 cells (lung). GSK3787 (1 μM) largely antagonizes GW0742-induced increase of Adrp mRNA in Huh7 and HepG2 cells but not in H1838 cells. GSK3787 does not antagonize basal expression of either of these two PPARβ/δtarget genes in these cells. Neither GW0742 nor GSK3787 has any effect on cell proliferation of these cells at concentrations ranging from 0.1 to 10 μM. GSK3787 is able to modulate the association of both PPARβ/δ and PPARγ coregulator peptides in response to ligand activation. Efficacy of GSK3787 to modulate PPARγ activity is markedly lower than the efficacy of GSK3787 to act as a PPARβ/δ antagonist. [2] |
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| Kinase Assay | Saturation binding assay | |||
| Using 96-well culture plates, 50 nM purified human PPARG LBD and the desired concentration of [3H]GW3738 are diluted to a total volume of 100 μL with buffer consisting of 50 mM KCl, 5 mM EDTA, 10 mM dithiothreitol (DTT), 50 mM HEPES, at pH 7. Saturation binding assays are conducted using concentrations of [3H]GW3738 ranging from 1 to 250 nM. Nonspecific binding at each concentration of [3H]GW3738 is estimated in parallel incubations containing 50 μM unlabeled GW 3738. Plates are incubated for 2 h at room temperature. Free ligand is separated from receptor-bound ligand by size exclusion chromatography using commercially available 96-well format spin columns. Samples (50 μL) from each well of a single test plate are loaded onto a buffer- and temperature-equilibrated 96-well gel filtration block. The block is placed on top of a clean microtiter plate and centrifuged at 1100 g for 4 min. Scintillation fluid (180 ul) is added to each well of the plate containing the eluent, and the plates are sealed and allowed to equilibrate for at least 4 h before counting in a counter. The amount of nonspecific binding at each concentration of [3H]GW3738 is subtracted from all wells and plots of [3H]GW3738 concentration versus counts per minute (cpm) bound are constructed. The Kd values for [3H]GW3738 are determined from a nonlinear least squares fit of the data to a simple binding model. | ||||
| In Vivo | ||
| In Vivo |
GSK3787 antagonizes ligand-induced PPARβ/δ-dependent gene expression in vivo. Oral administration of GSK3787 has no effect on the expression of Angptl4 and Adrp mRNA in mouse colon epithelium. Coadministration of GSK3787 (10 mg/kg) effectively prevents the GW0742-induced expression of both Angptl4 and Adrp mRNA in wild-type mouse colon epithelium, which is correlated with reduced promoter occupancy of PPARβ/δ on the Angptl4 and Adrp genes. Administration of GSK3787 had no effect on glucose tolerance. [2] |
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化学情報
| 分子量 | 392.78 | 化学式 | C15H12ClF3N2O3S |
| CAS No. | 188591-46-0 | SDF | Download GSK3787 SDFをダウンロードする |
| Smiles | C1=CC(=CC=C1C(=O)NCCS(=O)(=O)C2=NC=C(C=C2)C(F)(F)F)Cl | ||
| 保管 | |||
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In vitro |
DMSO : 79 mg/mL ( (201.13 mM)； 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。) Water : Insoluble Ethanol : Insoluble |
モル濃度計算器 |
|
in vivo Add solvents to the product individually and in order. |
投与溶液組成計算機 | ||||
実験計算
投与溶液組成計算機(クリア溶液)
ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）
mg/kg
g
μL
匹
ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
計算結果：
投与溶媒濃度： mg/ml;
DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )
投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH2O，を加え完全に溶解させます。
投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。
注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。
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