rosiglitazone

Rosiglitazone (BRL49653) 是一种 PPARγ 激动剂、TRPC5 激活剂和 TRPM3 抑制剂，具有口服活性。Rosiglitazone 也是一种降糖剂，是噻唑烷二酮类胰岛素增敏剂。

Rosiglitazone maleate (BRL 49653) 是一种选择性PPARγ激活剂，具有抗糖尿病特性和潜在抗肿瘤活性。它也是TRP 通道调节剂，可抑制 TRPM2、TRPM3 的活性，激活 TRPC5。

Rosiglitazone hydrochloride (BRL-49653 HCl) 是一种降血糖药物，通过与脂肪细胞中的 PPAR 受体结合来刺激胰岛素分泌。它对 PPARγ1、PPARγ2 和 PPARγ 的EC50值分别为 30 nM、100 nM 和 60 nM。它也是TRPC5的激活剂和TRPM3的抑制剂。

N-desmethyl Rosiglitazone is a major metabolite of rosiglitazone , a potent and selective PPARγ ligand present in formulations that have been used to treat type 2 diabetes. Rosiglitazone is metabolized by the cytochrome P450 (CYP) isoform CYP2C8 to form N-desmethyl rosiglitazone.

Rosiglitazone (BRL 49653) potassium is a potent and selective PPARγ agonist (EC 50: 60 nM, Kd: 40 nM), administered orally. It also serves as an activator of TRPC5 (EC 50: 30 μM) and an inhibitor of TRPM3. This compound, widely used in research, has shown promise in investigating obesity, diabetes, senescence, and ovarian cancer [1] [2] [4] [7].

Rosiglitazone sodium 作为一种高效的选择性PPARγ激活剂，对PPARγ1、PPARγ2及PPARγ具有不同程度的选择性，其EC50值分别为30 nM、100 nM和60 nM，Kd值约为40 nM。此外，Rosiglitazone sodium 还能调节TRP channels，具体表现为抑制TRPM2和TRPM3的活性，同时激活TRPC5的活性。

ISOGINKGETIN (4',4'''-Dimethylamentoflavone) 是一种MMP9抑制剂，也是一种Pre-mRNA Splicing 抑制剂。

DS-6930 是一种有效的和选择性的 PPARγ激动剂（EC50= 41 nM）。DS-6930 可有效降低血浆葡萄糖 (PG)水平，此外，与 Rosiglitazone 相比，具有更少的 PPARγ 相关不良反应。DS-6930 在糖尿病中具有研究价值。

The peroxisome proliferator-activated receptors (PPARs) are lipid-activated transcription factors often used as drug targets for the treatment of metabolic disorders. CAY10573 is a PPAR agonist that displays potent binding at PPARα, γ, and δ with IC50 values of 113, 50, and 223 nM, respectively. It potently transactivates PPARα, γ, and δ with EC50 values of 8, 70, and 500 nM, respectively. CAY10573 demonstrates stronger binding and functional activity for PPARγ than the antidiabetic compound rosiglitazone (IC50 = 92 nM; EC50 = 220 nM).

Cajanin has potential hypolipidemic effects,possibly via up-regulating the ABCA1 protein expression,subsequently resulting in increased macrophage cholesterol efflux and RCT, it can significantly improve basal glucose uptake in HepG2 cells, its improving effect is concentration dependent, it exhibits effects stronger than that of rosiglitazone, which has been used as an antidiabetic drug.

2-Hydroxy-1-Methoxyaporphine can inhibit CYP2D6 activity, it also increase the glucose consumption significantly as rosiglitazone.

Resveratrol-3-O-sulfate is a metabolite of resveratrol . In U-937 cells stimulated with LPS, resveratrol-3-O-sulfate (1 μM) decreases the expression of IL-1α, IL-1β, and IL-6 by 61.2, 76.6, and 42.2%, respectively, and decreases the release of TNF-α and IL-6 to similar levels as resveratrol. It has antioxidant activity in a Trolox assay, dose-dependently decreases growth of Caco-2 colorectal adenocarcinoma cells when used at concentrations ranging from 10 to 100 μM, and induces apoptosis at concentrations of 25 and 50 μM. Resveratrol-3-O-sulfate also displaces rosiglitazone from the outer mitochondrial protein mitoNEET (IC50 = 3.36 μM for the human protein), indicating that it binds to the thiazolidine-2,4-dione (TZD) binding pocket.

Azelaoyl PAF是一种强效的PPARγ激动剂，能够竞争性地结合噻唑烷二酮类药物，与罗格列酮（rosiglitazone）的效力相当。​在动脉粥样硬化研究中，Azelaoyl PAF通过上调CD36的表达，促进巨噬细胞对氧化低密度脂蛋白（oxLDL）的摄取。在Friedreich's ataxia（FRDA）患者的成纤维细胞中，Azelaoyl PAF显著提高了铁蛋白的mRNA和蛋白质水平。