GW4064
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.
GW4064是一种FXR激动剂，在分离的受体活性实验和转染人FXR的细胞实验中的EC50值分别为15 nM和 90 nM [1]。
GW4064作为一种高效选择性非甾类FXR激动剂，对不同动物物种的胆固醇和TG可产生有益影响，能有效降低KK-Ay 和 ob/ob小鼠血清中的TG水平。对KK-Ay小鼠给药1周，结果表明GW4064能显著降低VLDL分泌水平。在SHP+/+小鼠中也可降低血清中的TGs水平[2]。
由于一些条件限制，比如有限的溶解度、潜在的有毒二苯乙烯药效团和紫外光不稳定性，GW4064并不是较好的候选药物，目前通常用作研究FXR生理功能的一种工具化合物[3]。
参考文献：
[1] Chiang PC, Thompson DC, Ghosh S, Heitmeier MR. A formulation-enabled preclinical efficacy assessment of a farnesoid X receptor agonist, GW4064, in hamsters and cynomolgus monkeys. J Pharm Sci. 2011 Nov;100(11):4722-33.
[2] Watanabe M, Houten SM, Wang L, Moschetta A, Mangelsdorf DJ, Heyman RA, Moore DD, Auwerx J. Bile acids lower triglyceride levels via a pathway involving FXR, SHP, and SREBP-1c. J Clin Invest. 2004 May;113(10):1408-18.
[3] Li W, Fu J, Cheng F, Zheng M, Zhang J, Liu G, Tang Y. Unbinding pathways of GW4064 from human farnesoid X receptor as revealed by molecular dynamics simulations. J Chem Inf Model. 2012 Nov 26;52(11):3043-52.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 542.85 |
| Cas No. | 278779-30-9 |
| Formula | C28H22Cl3NO4 |
| Solubility | insoluble in H2O; insoluble in EtOH; ≥24.7 mg/mL in DMSO |
| Chemical Name | 3-[(E)-2-[2-chloro-4-[[3-(2,6-dichlorophenyl)-5-propan-2-yl-1,2-oxazol-4-yl]methoxy]phenyl]ethenyl]benzoic acid |
| SDF | Download SDF |
| Canonical SMILES | CC(C)C1=C(C(=NO1)C2=C(C=CC=C2Cl)Cl)COC3=CC(=C(C=C3)C=CC4=CC(=CC=C4)C(=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。 |
| Description | GW4064是一种选择性的非甾类法尼醇X受体（FXR）激动剂，EC50值为15 nM。 | |||||
| 靶点 | FXR | |||||
| IC50 | 15 nM (EC50) | |||||
质量控制和MSDS
- 批次:
化学结构
相关生物数据
