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]}.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Lobeglitazone sulfate (1-10 mg/kg, po for 8 weeks) exhibits anti-atherosclerotic property in ApoE−/− mouse models^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

578.61

C₂₄H₂₆N₄O₉S₂

763108-62-9

Solid

White to off-white

O=C(SC1CC2=CC=C(C=C2)OCCN(C)C3=NC=NC(OC4=CC=C(C=C4)OC)=C3)NC1=O.O=S(O)(O)=O

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

• [1]. Bae J, et al. Lobeglitazone: A Novel Thiazolidinedione for the Management of Type 2 Diabetes Mellitus. Diabetes Metab J. 2021 May;45(3):326-336.

  [2]. Jeong D, et al., Lobeglitazone Exerts Anti-Inflammatory Effect in Lipopolysaccharide-Induced Bone-Marrow Derived Macrophages. Biomedicines. 2021 Oct 10;9(10):1432.  [Content Brief]

  [3]. Nuwormegbe S, et al. Lobeglitazone attenuates fibrosis in corneal fibroblasts by interrupting TGF-beta-mediated Smad signaling. Graefes Arch Clin Exp Ophthalmol. 2022 Jan;260(1):149-162.  [Content Brief]

  [4]. Lim S, et al., Effect of a new PPAR-gamma agonist, lobeglitazone, on neointimal formation after balloon injury in rats and the development of atherosclerosis. Atherosclerosis. 2015 Nov;243(1):107-19.  [Content Brief]