Lobeglitazone (sulfate)

Lobeglitazone sulfate is a new type of thiazolidinedione. Lobeglitazone sulfate is the orally active agonist for PPAR with EC₅₀ of 137.4 nM and 546.3 nM for PPARγ and PPARα. Lobeglitazone sulfate is the inhibitor for ERK/JNK/Smad/NF-κB signaling pathway. Lobeglitazone sulfate exhibits anti-inflammatory, anti-diabetic, anti-fibrotic and anti-atherosclerotic properties^{[1][2][3][4][5][6]}. In Vitro:Lobeglitazone sulfate increases glucose uptake in 3T3-L1 adipocytes and L6 muscle cells^[1].
Lobeglitazone sulfate (50-200 μM, 24 h) inhibits NO generation and the expressions of pro-inflammtory cytokines like IL-1β, IL-6, iNOS, COX-2 and MCP-1 in LPS (HY-D1056)-stimulated BMDMs^[2].
Lobeglitazone sulfate (10 μM, 48 h) inhibits TGF-β1-induced expression of α-SMA and fibronectin, inhibits Smad signaling pathway in primary human corneal fibroblast, and exhibits anti-fibrotic property^[3].
Lobeglitazone sulfate (1-15 μM, 24 h) inhibits PDGF-induced proliferation and migration of vascular smooth muscle cells (VSMCs), inhibits TNF-α-induced NF-κB p65 translocation^[4].
In Vivo:Lobeglitazone sulfate (1-10 mg/kg, po for 8 weeks) exhibits anti-atherosclerotic property in ApoE / mouse models^[4].