PDF(Pubmed)
Abstract：
GW501516, also known by the name of cardarine, is a synthetic peroxisome-proliferator-activated receptor delta (PPR-δ) agonist agent developed for applications in the treatment of metabolic disorders and cardiovascular diseases. A broad polymorph screening in various solvents and mixtures was completed in order to explore its capabilities to grow polymorphs. The crystal structures of four polymorphs were elucidated using single-crystal X-ray diffraction, while one structure was solved via a powder X-ray diffraction method. The solid state features (nature of intermolecular interactions) were investigated by computational methods. The polymorphs were further investigated by thermal DSC analysis and X-ray diffraction on powders. From a pharmaceutical perspective, the stability and solubility of the polymorphs were analyzed as well.
摘要：
GW501516，也被称为cardarine，是一种合成的过氧化物酶体增殖物激活的受体δ（PPR-δ）激动剂，用于治疗代谢紊乱和心血管疾病。完成了在各种溶剂和混合物中的广泛多晶型物筛选,以探索其生长多晶型物的能力。使用单晶X射线衍射阐明了四种多晶型物的晶体结构，而一种结构是通过粉末X射线衍射方法解决的。通过计算方法研究了固态特征（分子间相互作用的性质）。通过对粉末的热DSC分析和X射线衍射进一步研究了多晶型物。从制药的角度来看，分析了多晶型物的稳定性和溶解性。
