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Rosiglitazone

CAS No. : 122320-73-4

MCE 站：Rosiglitazone

产品活性：Rosiglitazone (BRL 49653)，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，对 PPARγ1、PPARγ2 和 PPARγ 的 EC₅₀ 值分别为 30 nM、100 nM 和 60 nM。Rosiglitazone 与 PPARγ 结合，K_d 约为 40 nM。Rosiglitazone 也是 TRPC5 的激活剂 (EC₅₀=?30 μM) 和 TRPM3 的抑制剂。

研究领域：Cell Cycle/DNA Damage  |  Neuronal Signaling  |  Membrane Transporter/Ion Channel  |  Autophagy  |  Apoptosis

作用靶点：PPAR  |  TRP Channel  |  Autophagy  |  Ferroptosis

In Vitro: Rosiglitazone is a potent and selective activator of PPARγ, with EC₅₀s of 30 nM and 100 nM for PPARγ1 and PPARγ2, respectively, and a K_d of appr 40 nM for PPARγ. Rosiglitazone (BRL49653, 0.1, 1,10 μM) promotes differentiation of C3H10T1/2 stem cells to adipocytes. Rosiglitazone (Compound 6) activates PPARγ, with an EC₅₀ of 60 nM. Rosiglitazone (1 μM) activates PPARγ, which binds to NF-α1 promoter to activate gene transcription in neurons. Rosiglitazone (1 μM) also protects Neuro2A cells and hippocampal neurons against oxidative stress, and up-regulates BCL-2 expression in an NF-α1-dependent manner. Rosiglitazone completely inhibits TRPM3 with IC₅₀ values of 9.5 and 4.6 μM against nifedipine- and PregS-evoked activity, but such effects are not via PPARγ. Rosiglitazone inhibits TRPM2 at higher concentration, with an IC₅₀ of appr 22.5 μM. Rosiglitazone is a strong stimulator of TRPC5 channels, with an EC₅₀ of ~30 μM.

In Vivo: Rosiglitazone (5 mg/kg, p.o.) decreases the serum glucose in diabetic rats. Rosiglitazone also decreases IL-6, TNF-α, and VCAM-1 levels in diabetic group. Rosiglitazone in combination with losartan increases glucose compared to diabetic and Los-treated groups. Rosiglitazone significantly ameliorates endothelial dysfunction indicated by a significantly lower contractile response to PE and Ang II and enhancement of ACh-provoked relaxation in aortas isolated from diabetic rats.

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