GW9662
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
GW9662是一种有效的PPARγ拮抗剂,其IC50值为3.3 μM[1]。
PPARγ属于核受体超家族。抑制PPARγ可用于多种癌症的治疗,包括乳腺癌。在无细胞和基于细胞的试验中,GW9662作为一种有效的、不可逆的和选择性的PPARγ拮抗剂,修饰PPARγ配体结合位点的半胱氨酸残基。在三种乳腺癌细胞系中,包括MCF7、MDA-MB-231和MDA-MB-468,GW9662抑制细胞活性,其IC50值范围为20 ~ 30 μM。此外,据报道,GW9662废除脂多糖对肾缺血/再灌注(I/R)模型的保护作用。在此模型中,脂多糖可显著缓解由I/R引起的肾/肾小球功能障碍、肾小管功能障碍和再灌注损伤,但给予GW9662会将此效果逆转[2,3]。
参考文献:
[1] Fong WH, Tsai HD, Chen YC, Wu JS, Lin TN. Anti-apoptotic actions of PPAR-gamma against ischemic stroke. Mol Neurobiol. 2010 Jun;41(2-3):180-6.
[2] Seargent JM, Yates EA, Gill JH. GW9662, a potent antagonist of PPARgamma, inhibits growth of breast tumour cells and promotes the anticancer effects of the PPARgamma agonist rosiglitazone, independently of PPARgamma activation. Br J Pharmacol. 2004 Dec;143(8):933-7.
[3] Collino M, Patel NS, Lawrence KM, Collin M, Latchman DS, Yaqoob MM, Thiemermann C. 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.
- 1. Ai Wei, Qi Gao, et al. "Inhibition of DNA methylation derepresses PPARγ and attenuates pulmonary fibrosis." Br J Pharmacol. 2021 Aug 11. PMID:34378791
- 2. WeijieSuna, XiaoyuDuana, et al. "Adipogenic activity of 2-ethylhexyl diphenyl phosphate via peroxisome proliferator-activated receptor γ pathway." Science of The Total Environment. Available online 18 November 2019, 134810.
- 3. LianyingZhangab, WeijieSuna, et al. "Promoting differentiation and lipid metabolism are the primary effects for DINP exposure on 3T3-L1 preadipocytes." Environmental Pollution. Available online 13 September 2019, 113154.
- 4. Guo X, Yan F, et al. "SIRT3 inhibits Ang II-induced transdifferentiation of cardiac fibroblasts through β-catenin/PPAR-γ signaling." Life Sci. 2017 Oct 1;186:111-117. PMID:28760678
Storage | Store at -20°C |
M.Wt | 276.68 |
Cas No. | 22978-25-2 |
Formula | C13H9ClN2O3 |
Solubility | insoluble in H2O; ≥13.75 mg/mL in DMSO; ≥9.08 mg/mL in EtOH with ultrasonic |
Chemical Name | 2-chloro-5-nitro-N-phenylbenzamide |
SDF | Download SDF |
Canonical SMILES | C1=CC=C(C=C1)NC(=O)C2=C(C=CC(=C2)[N+](=O)[O-])Cl |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
细胞实验 [1]: | |
细胞系 |
人乳腺癌细胞系MCF7、MDA-MB-468和MDA-MB-231 |
制备方法 |
在DMSO中的溶解度大于13.75 mg/mL。若配制更高浓度的溶液,一般步骤如下:请将试管置于37 °C加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20 °C可放置数月。 |
反应条件 |
0.1 ~ 50 μM;72小时 |
实验结果 |
在上述3种人乳腺癌细胞系中,GW9662使细胞活力下降至类似的程度。在MDA-MB-231细胞中,GW9662与Rosiglitazone联合用药对细胞存活产生协同作用,而不会削弱Rosiglitazone的作用。MDA-MB-231细胞的细胞生长动力学分析结果进一步证实,GW9662不能抑制Rosiglitazone诱导的生长抑制,却增强了Rosiglitazone的作用。 |
动物实验 [2]: | |
动物模型 |
肾缺血再灌注大鼠模型 (I/R) |
给药剂量 |
1 mg/kg;腹腔注射;实施缺血前的12小时和24小时 |
实验结果 |
在肾缺血再灌注大鼠模型中,GW9662消除脂多糖 (LPS) 预处理诱导的肌酐清除。在经过LPS预处理的缺血再灌注大鼠中,给予GW9662增加钠排泄分数和减少尿量,从而减弱LPS对管状功能障碍的保护作用。此外,GW9662逆转LPS预处理对血清天冬氨酸氨基转移酶和γ-谷氨酰转移酶的清除作用。 |
注意事项 |
请于室内测试所有化合物的溶解度。虽然化合物的实际溶解度可能与其理论值略有不同,但仍处于实验系统误差的允许范围内。 |
References: [1]. Seargent JM, Yates EA, Gill JH. GW9662, a potent antagonist of PPARgamma, inhibits growth of breast tumour cells and promotes the anticancer effects of the PPARgamma agonist rosiglitazone, independently of PPARgamma activation. Br J Pharmacol. 2004 Dec;143(8):933-7. [2]. Collino M, Patel NS, Lawrence KM, Collin M, Latchman DS, Yaqoob MM, Thiemermann C. 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. |
描述 | GW9662是一种选择性的、不可逆的和有效的PPARγ拮抗剂,对人PPARγ的IC50值为3.3 ?M。 | |||||
靶点 | PPARγ | |||||
IC50 | 3.3 ?M (human) |
质量控制和MSDS
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