GW9662

目录号: GC13969纯度: >98.00%同义词: 2-氯-5-硝基-N-苯基苯酰胺

GW9662是一种特异性的过氧化物酶体增殖物激活受体-γ(PPAR-γ)抑制剂,其IC50为3.3 nM。

Cas No.: 22978-25-2

规格	价格	库存	数量
5mg	¥357.00	现货	1
10mg	¥410.00	现货	1
25mg	¥714.00	现货	1
50mg	¥840.00	现货	1
10mM (in 1mL DMSO)	¥368.00	现货	1

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618, 1017–1023 (2023)
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610, 366–372 (2022)
Cell
187(9):2288-2304 (2024)
Cell
183(7):1867-1883 (2020)
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388(6745) (2025)
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387(6739) (2025)
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387(6734) (2025)
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产品描述 Description

GW9662 is a specific inhibitor of peroxisome proliferator activated receptor-gamma (PPAR-gamma) with an IC50 of 3.3 nM, GW9662 acts 10 to 600 times more selectively on PPARγ in cells than on PPARα and PPARδ[1-3].

Treatment with GW9662 significantly attenuated LPS-induced expression of Il1b, interleukin 6 (Il6) and inducible nitric oxide synthase (iNos) as well as NO2-formation in J774A.1 cells^[4]. DMBA-induced mammary alveolar lesions (MAL) were significantly inhibited by PPARγ antagonist GW9662[5]. GW9662(2.5/5 µM) prevented disruption of the Colon carcinoma cells cycle induced by resveratrol and consequently abrogated resveratrol-induced apoptosis[6].

GW9662(p.o;3 mg/kg/day ;2 weeks) worsened the brain injury in alcohol-fed reperfusion mice[7]. Pretreatment with LPS significantly attenuated all markers of renal injury and dysfunction caused by I/R. Most notably, GW9662(1 mg/kg GW9662; IP;24 and 12 hours prior to ischemia) abolished the protective effects of LPS[8].

References:
[1]. Leesnitzer LM, Parks DJ, et,al. Functional consequences of cysteine modification in the ligand binding sites of peroxisome proliferator activated receptors by GW9662. Biochemistry. 2002 May 28;41(21):6640-50. doi: 10.1021/bi0159581. PMID: 12022867.
[2]. Lea MA, Sura M, et,al. Inhibition of cell proliferation by potential peroxisome proliferator-activated receptor (PPAR) gamma agonists and antagonists. Anticancer Res. 2004 Sep-Oct;24(5A):2765-71. PMID: 15517883.
[3]. Nielsen R, GrØntved L, et,al. Peroxisome proliferator-activated receptor subtype- and cell-type-specific activation of genomic target genes upon adenoviral transgene delivery. Mol Cell Biol. 2006 Aug;26(15):5698-714. doi: 10.1128/MCB.02266-05. PMID: 16847324; PMCID: PMC1592764.
[4]. Baumann A, Burger K,et,al. GW9662, a peroxisome proliferator-activated receptor gamma antagonist, attenuates the development of non-alcoholic fatty liver disease. Metabolism. 2022 Aug;133:155233. doi: 10.1016/j.metabol.2022.155233. Epub 2022 May 30. PMID: 35654114.
[5]. Mehta RG, Peng X, et,al. PPARγ antagonist GW9662 induces functional estrogen receptor in mouse mammary organ culture: potential translational significance. Mol Cell Biochem. 2013 Jan;372(1-2):249-56. doi: 10.1007/s11010-012-1466-9. Epub 2012 Sep 24. PMID: 23001870.
[6]. Aires V, Brassart B, et,al. A role for peroxisome proliferator-activated receptor gamma in resveratrol-induced colon cancer cell apoptosis. Mol Nutr Food Res. 2014 Sep;58(9):1785-94. doi: 10.1002/mnfr.201300962. Epub 2014 Jun 30. PMID: 24975132.
[7]. Sun H, Xiong W, et,al. Low-dose alcohol consumption protects against transient focal cerebral ischemia in mice: possible role of PPARγ. PLoS One. 2012;7(7):e41716. doi: 10.1371/journal.pone.0041716. Epub 2012 Jul 27. PMID: 22848576; PMCID: PMC3407212.
[8]. Collino M, Patel NS, et,al. The selective PPARgamma antagonist GW9662 reverses the protection of LPS in a model of renal ischemia-reperfusion. Kidney Int. 2005 Aug;68(2):529-36. doi: 10.1111/j.1523-1755.2005.00430.x. PMID: 16014029.

GW9662是一种特异性的过氧化物酶体增殖物激活受体-γ(PPAR-γ)抑制剂,其IC50为3.3 nM。在细胞中,GW9662相较于PPARα和PPARδ选择性地作用于PPARγ,选择性作用范围为10至600倍[1-3]。

使用GW9662可显著减轻LPS诱导的J774A.1细胞中Il1b、白细胞介素6(Il6)和诱导型一氧化氮合酶(iNos)的表达以及NO2-生成[4]。使用GW9662可显著抑制DMBA诱导的乳腺腺泡病变(MAL)[5]。GW9662(2.5/5µM)防止了白藜芦醇引起的结肠癌细胞周期紊乱,抵消引起的细胞凋亡[6]。

GW9662(p.o;3 mg/kg/day ;2 weeks)加剧了饮酒再灌注小鼠的脑损伤[7]。LPS预处理可显著减弱I/R引起的肾损伤和功能障碍的所有标志物。GW9662(1 mg/kg GW9662; IP;24 and 12 hours prior to ischemia)使LPS的保护效果消失[8]。

实验参考方法 Experimental Reference Method

Kinase experiment ^[1]:
Preparation method	Human PPARα, PPARγ, and PPARδ ligand binding domains (LBDs) are expressed in E. coli as polyhistidine labeled fusion proteins. In the experimental buffer, the desired receptor (15 nM) was added to the streptavitin modified SPA bead (0.5 mg/mL) pulp to fix the receptor to the SPA bead. The mixture was equilibrated at room temperature for at least 1 hour, then the beads were precipitated at 1x10³g rotation speed, the supernatant was removed, the beads were gently mixed, the beads were suspended in fresh experimental buffer, the centrifugation/re-suspension procedure was repeated, the resulting acceptor coated bead slurry was used immediately, or stored at 4℃ for up to 1 week before use. Competitive binding to PPARα,PPARγ, and PPARδ was determined using [³H]GW9662 as a radioligand. Unless otherwise indicated, all experimental buffers were 50 mM HEPES (pH 7), 50 mM NaCl, 5 mM CHAPS, 0.1 mg/mL BSA, and 10 mM DTT.In some experiments, 50 mM Tris (pH 8) was used instead of HEPES(pH 7).
Applications	GW9662 is a potent and selective PPARγ antagonist with an IC₅₀ of 3.3 nM.
Cell experiment ^[2]:
Cell lines	J774A.1 cells
Preparation method	Cells were challenged with 50 ng/ml lipopolysaccharide with(or no) 10 μM GW9662 or vehicle for 18 h.Cell culture supernatant was collected, cells were lysed for RNA separation, or cells were lysed with nitric oxide synthase (NOS) buffer added with protease inhibitors, and NOS activity was measured.
Reaction Conditions	10 μM GW9662;18 h
Applications	Treatment with GW9662 significantly attenuated LPS-induced expression of Il1b, interleukin 6 (Il6) and inducible nitric oxide synthase (iNos) as well as NO₂- formation.
Animal experiment^[3]:
Animal models	Male Wistar rats
Preparation method	Rats were pretreated with LPS (1 mg/kg, IP, 24 hours prior to ischemia) in the absence (control) or presence of the selective PPARγ antagonist GW9662(1 mg/kg, IP, 24 and 12 hours prior to ischemia). Twenty-four hours after injection of LPS, rats were subjected to 60 minutes of bilateral renal ischemia, followed by 6 hours of reperfusion.
Dosage form	1 mg/kg GW9662; IP;24 and 12 hours prior to ischemia
Applications	Administration of the selective PPARγ antagonist GW9662 24 and 12 hours before ischemia/reperfusion (I/R) eliminated the renal protection observed in LPS preconditioning.
References: [1]. Leesnitzer LM, Parks DJ,et,al. Functional consequences of cysteine modification in the ligand binding sites of peroxisome proliferator activated receptors by GW9662. Biochemistry. 2002 May 28;41(21):6640-50. doi: 10.1021/bi0159581. PMID: 12022867. [2].Baumann A, Burger K, et,al. GW9662, a peroxisome proliferator-activated receptor gamma antagonist, attenuates the development of non-alcoholic fatty liver disease. Metabolism. 2022 Aug;133:155233. doi: 10.1016/j.metabol.2022.155233. Epub 2022 May 30. PMID: 35654114. [3]. Collino M, Patel NS, et,al.The selective PPARgamma antagonist GW9662 reverses the protection of LPS in a model of renal ischemia-reperfusion. Kidney Int. 2005 Aug;68(2):529-36. doi: 10.1111/j.1523-1755.2005.00430.x. PMID: 16014029.

产品文档 Product Documents

批次：Purity:>98.00%

化学性质Chemical Properties

CAS 号

22978-25-2

同义词

2-氯-5-硝基-N-苯基苯酰胺

化学名

2-chloro-5-nitro-N-phenylbenzamide

SMILES

C1=CC=C(C=C1)NC(=O)C2=C(C=CC(=C2)[N+](=O)[O-])Cl

分子式

C₁₃H₉ClN₂O₃

分子量

276.68 g/mol

溶解性

≥ 13.75 mg/mL in DMSO, ≥ 9.08 mg/mL in EtOH with ultrasonic

保存条件

Store at -20°C

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储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
为了提高溶解度，请将管子加热至 37°C，然后在超声波浴中震荡一段时间。

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评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备 RT，或根据请求配备蓝冰。

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