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Submit ReviewGSK 3787 is a potent and selective peroxisome proliferator-activated receptor δ (PPARδ) antagonist (pIC50 = 6.6). Displays no measurable affinity for PPARα or PPARγ in vitro (pIC50< 5).
GSK 3787 is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
分子量 | 392.78 |
公式 | C15H12ClF3N2O3S |
储存 | Store at +4°C |
纯度 | ≥99% (HPLC) |
CAS Number | 188591-46-0 |
PubChem ID | 2800647 |
InChI Key | JFUIMTGOQCQTPF-UHFFFAOYSA-N |
Smiles | O=C(C2=CC=C(Cl)C=C2)NCCS(C1=CC=C(C(F)(F)F)C=N1)(=O)=O |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 39.28 | 100 |
以下数据基于产品分子量 392.78。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 2.55 mL | 12.73 mL | 25.46 mL |
5 mM | 0.51 mL | 2.55 mL | 5.09 mL |
10 mM | 0.25 mL | 1.27 mL | 2.55 mL |
50 mM | 0.05 mL | 0.25 mL | 0.51 mL |
参考文献是支持产品生物活性的出版物。
Shearer et al (2010) Identification and characterization of 4-chloro-N(2-{[5-trifluoromethyl)-2-pyridyl]sulfonyl}ethyl)benzamide (GSK3787), a selective and irreversible peroxisome proliferator-activated receptor delta (PPARdelta) antagonist. J.Med.Chem. 53 1857 PMID: 20128594
Palkar et al (2010) Cellular and pharmacological selectivity of the peroxisone proliferator-activated receptor-β/δ antagonist GSK3787. Mol.Pharmacol. 78 419 PMID: 20516370
If you know of a relevant reference for GSK 3787, please let us know.
关键词: GSK 3787, GSK 3787 supplier, GSK3787, peroxisome, proliferator-activated, receptor, PPARd, PPARdelta, PPARδ, antagonists, Receptors, 3961, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 GSK 3787 的部分引用包括:
Samokhvalov et al (2015) PPARδ signaling mediates the cytotoxicity of DHA in H9c2 cells. Cell Cycle 232 44105 PMID: 25300478
Massimo et al (2022) Peroxisome Proliferator-Activated Receptor Activation in Precision-Cut Bovine Liver Slices Reveals Novel Putative PPAR Targets in Periparturient Dairy Cows. Front Vet Sci 9 931264 PMID: 35903133
Ning et al (2023) Nuclear receptor modulators inhibit osteosarcoma cell proliferation and tumour growth by regulating the mTOR signaling pathway. Cell Death Dis 14 51 PMID: 36681687
Sebastiano et al (2020) The interplay between non-esterified fatty acids and bovine peroxisome proliferator-activated receptors: results of an in vitro hybrid approach. J Anim Sci Biotechnol 11 91 PMID: 32793344
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