GW9662

製品コードS2915 バッチS291502

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C13H9ClN2O3
分子量 276.68 CAS No. 22978-25-2
Solubility (25°C)* 体外 DMSO 55 mg/mL (198.78 mM)
Water Insoluble
Ethanol Insoluble
体内 （毎回新しく調製した物を用意してください）
Clear solution
5%DMSO Corn oil
9.0mg/ml Taking the 1 mL working solution as an example, add 50 μL of 180 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 GW9662 is a selective PPAR antagonist for PPARγ with IC50 of 3.3 nM in a cell-free assay, with at least 10- to 600-fold functional selectivity in cells with PPARγ versus PPARα and PPARδ.
in vitro GW9662 binds to Cys(285) on PPARgamma which is conserved among all three PPARs. GW9662 acts as an antagonist of PPARgamma which is confirmed in an assay of adipocyte differentiation inhibition. [1] GW9662 prevents activation of PPARγ and inhibits growth of human mammary tumour cell lines (MCF7, MDA-MB-468, MDA-MB-231) with IC50 of 20 μM-30 μM, suggesting either the existence of PPARγ agonistic properties of GW9662 or growth-inhibitory mechanisms independent of PPARγ. Co-treatment with both Rosiglitazone (50 μM) and GW9662 (10 μM) results in statistically lower viable cell numbers after 7 days in MDA-MB-231 cells. [2] PPARγ1 ligands could suppress RANKL-induced osteoclast formation in primary murine myeloid (BMs) and RAW264.7 cells. Importantly, suppression by these ligands is reversed in a concentration-dependent fashion with GW 9662 (2 μM). GW 9662 (2 μM) blocks IL-4 suppression of osteoclast formation in BMs. GW 9662 (1 μM) blocks RANKL activation of NF-κB in RAW264.7 cells. [3] GW9662 (10 μM) inhibits hormone- and agonist-induced adipogenesis of primary preadipocytes from patients with thyroid eye disease. [4]
in vivo Pretreatment with LPS (1 mg/kg i.p.) significantly attenuates all markers of renal injury and dysfunction caused by ischemia/reperfusion (I/R) injury in rats. Most notably, GW9662 (1 mg/kg i.p.) abolishes the protective effects of LPS. [5]

プロトコル(参考用のみ)

キナーゼアッセイ Binding assay
The human PPARα, PPARγ, and PPARδ ligand binding domains (LBDs) are expressed in E. coli as polyhistidine-tagged fusion proteins. Receptors are immobilized on SPA beads by addition of the desired receptor (15 nM) to a slurry of streptavidin-modifed SPA beads (0.5 mg/mL) in assay buffer. The mixture is allowed to equilibrate for at least 1 hour at room temperature, and the beads are pelleted by centrifugation at 1×103 g. The supernate is discarded, and the beads are resuspended in the original volume of fresh assay buffer with gentle mixing. The centrifugation/resuspension procedure is repeated, and the resulting slurry of receptor-coated beads is used immediately or stored at 4 ℃ for up to 1 week before use. [3H]GW2443 are used as radioligands for determination of competition binding to PPARα, PPARγ, and PPARδ, respectively. Unless otherwise indicated, the buffer used for all assays is 50 mM HEPES (pH 7), 50 mM NaCl, 5 mM CHAPS, 0.1 mg/mL BSA, and 10 mM DTT. For some experiments, the HEPES (pH 7) is replaced with 50 mM Tris (pH 8).
細胞アッセイ 細胞株 MDA-MB-231 cells
濃度 10 μM
反応時間 10 days
実験の流れ MDA-MB-231 cells are seeded at a density of 1 × 105 cells per 25 cm3 tissue culture flask. After 24 h (day 0), the growth medium is replaced with fresh medium containing rosiglitazone (50 μM), GW9662 (10 μM) or both together. Control flasks receives 0.1% DMSO. Cells are harvested on days 0, 3, 5, 7, 10 for each treatment condition by trypsinisation, stained using trypan blue, and the total and viable number of cells per flask calculates using a haemocytometer.
動物実験 動物モデル male Wistar rats
投薬量 1 mg/kg
投与方法 intraperitoneal injection

カスタマーフィードバック

Data from [Data independently produced by , , Theranostics, 2018, 8(15):4262-4278]

Data from [Data independently produced by , , Sci Rep, 2016, 6:36382.]

Data from [Data independently produced by , , Toxicol Appl Pharmacol, 2016, 316:17-26.]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

FFAR2 expressing myeloid-derived suppressor cells drive cancer immunoevasion [ J Hematol Oncol, 2024, 17(1):9] PubMed: 38402237
Celastrol Stabilizes Glycolipid Metabolism in Hepatic Steatosis by Binding and Regulating the Peroxisome Proliferator-Activated Receptor γ Signaling Pathway [ Metabolites, 2024, 14(1)64] PubMed: 38276299
MiR-552-3p Regulates Multiple Fibrotic and Inflammatory genes Concurrently in Hepatic Stellate Cells Improving NASH-associated Phenotypes [ Int J Biol Sci, 2023, 19(11):3456-3471] PubMed: 37496991
MiR-552-3p Regulates Multiple Fibrotic and Inflammatory genes Concurrently in Hepatic Stellate Cells Improving NASH-associated Phenotypes [ Int J Biol Sci, 2023, 19(11):3456-3471] PubMed: 37496991
KLF2/PPARγ axis contributes to trauma-induced heterotopic ossification by regulating mitochondrial dysfunction [ Cell Prolif, 2023, e13521.] PubMed: 37340819
3β-Hydroxy-12-oleanen-27-oic Acid Exerts an Antiproliferative Effect on Human Colon Carcinoma HCT116 Cells via Targeting FDFT1 [ Int J Mol Sci, 2023, 10.3390/ijms241915020] PubMed: 37834468
Multiple gene-drug prediction tool reveals Rosiglitazone based treatment pathway for non-segmental vitiligo [ Inflammation, 2023, 10.1007/s10753-023-01937-9] PubMed: 38159176
The TFPI2-PPARγ axis induces M2 polarization and inhibits fibroblast activation to promote recovery from post-myocardial infarction in diabetic mice [ J Inflamm (Lond), 2023, 10.1186/s12950-023-00357-8] PubMed: 37915070
IL-23 signaling prevents ferroptosis-driven renal immunopathology during candidiasis [ Nat Commun, 2022, 13(1):5545] PubMed: 36138043
TIP60 buffers acute stress response and depressive behaviour by controlling PPARγ-mediated transcription [ Brain Behav Immun, 2022, S0889-1591(22)00025-3] PubMed: 35114329

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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