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Rosiglitazone maleate

CAS No. : 155141-29-0

MCE 站：Rosiglitazone maleate

产品活性：Rosiglitazone maleate (BRL 49653C) 是一种有效的，选择性的 PPARγ 激活剂，对 PPARγ1，PPARγ2 和 PPARγ 的 EC₅₀ 值分别为 30 nM，100 nM 和 60 nM，对 PPARγ 的 K_d 值约为 40 nM；Rosiglitazone maleate 同时为 TRP channels 的调节剂，可抑制 TRPM2, TRPM3 的活性，激活 TRPC5。

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 maleate 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.

相关产品：Drug Repurposing Compound Library Plus  |  FDA-Approved Drug Library Plus  |  Bioactive Compound Library Plus  |  Apoptosis Compound Library  |  Cell Cycle/DNA Damage Compound Library  |  Immunology/Inflammation Compound Library  |  Membrane Transporter/Ion Channel Compound Library  |  Neuronal Signaling Compound Library  |  FDA-Approved Drug Library  |  Anti-Cancer Compound Library  |  Autophagy Compound Library  |  Anti-Aging Compound Library  |  Drug Repurposing Compound Library  |  Diabetes Related Compound Library  |  Oxygen Sensing Compound Library  |  Ferroptosis Compound Library  |  Anti-COVID-19 Compound Library  |  NMPA-Approved Drug Library  |  FDA Approved & Pharmacopeial Drug Library  |  Drug-Induced Liver Injury (DILI) Compound Library  |  Erastin  |  Ferrostatin-1  |  Cisplatin  |  Cycloheximide  |  RSL3  |  Acetylcysteine  |  Deferoxamine mesylate  |  SP600125  |  Necrostatin-1  |  Retinoic acid  |  Rosiglitazone  |  SB 202190  |  GW9662  |  Capsaicin  |  Curcumin  |  Hemin  |  (-)-Epigallocatechin Gallate  |  TBHQ  |  Simvastatin  |  Diphenyleneiodonium chloride  |  Bardoxolone methyl  |  U-73122  |  Pifithrin-α hydrobromide  |  Lovastatin  |  Trolox  |  EIPA  |  Eprenetapopt  |  L-Glutathione reduced  |  Amiloride hydrochloride  |  GW6471

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