ROSiglitazone 是噻唑烷二酮类胰岛素增敏剂，也是选择性的，具有口服活性PPARγ激动剂。它也是TRPC5的激活剂和TRPM3的抑制剂。

Rosiglitazone is an insulin sensitizing agent and thiazolidinedione that is indicated for the treatment of type 2 diabetes. Rosiglitazone has been linked to rare instances of acute liver injury.

Rosiglitazone会降低骨形成率,同时增加骨髓中的脂肪含量.Rosiglitazone减少成骨细胞特异性基因Runx2/Cbfa1,DLX5,以及α1（I）胶原蛋白的表达,而脂肪细胞特异性脂肪酸结合蛋白AP2的表达是增加的.Rosiglitazone会造成明显的骨丢失,包括减少骨量,骨小梁宽度和骨小梁数量,并增加骨小梁间距.Rosiglitazone增加ob/ob小鼠中白色脂肪细胞中编码线粒体蛋白的基因转录,伴随线粒体数量和线粒体结构的改变.

在一些细胞系中,Rosiglitazone以与过氧化物酶体增殖物激活受体γ无关的方式降低胆固醇合成。Rosiglitazone明显增加AMP依赖的蛋白激酶的α亚基中苏氨酸172的磷酸化,提高AMP:ATP比值。 Rosiglitazone增加脂联素从网膜细胞的分泌高达2.3倍,而从皮下脂肪细胞的分泌不受影响。 在3T3-L1脂肪细胞中,Rosiglitazone改变线粒体的形态学特征和蛋白质图谱。Rosiglitazone激活两个含α1-和α2-AMPK的配合物,这导致在乙酰辅酶A羧化酶的磷酸化明显增加。 Rosiglitazone激活PPAR-gamma2,充当小鼠骨髓在体外的成骨细胞生成的主导抑制剂。

Rosiglitazone is dissolved in DMSO and stored, and then diluted with appropriate medium before use[2]. Human neuroblastoma SH-SY5Y cells are maintained in Dulbecco's modified Eagle's medium (DMEM) supplemented with 10% fetal bovine serum, 100 μg/mL Streptomycin and 100 U/mL Penicillin G. SH-SY5Y cells are transfected with the longest isoform of human tau (2N4R) tagged with GFP using lipofectamine. 24 hr after transfection, cells are treated with Rosiglitazone (10 μM, 50 μM) for 24 hr[2].

122320-73-4

C18H19N3O3S

357.43

罗格列酮;BRL49653

1eq. HCl:35.7 mg/mL (100 mM)
DMSO:35.7 mg/mL (100 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years