Lobeglitazone sulfate
Based on 1 Customer Validation
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.
For research use only. We do not sell to patients.
- Purity: 99.63%
- CAS No.: 763108-62-9
- Formula: C24H26N4O9S2
- Molecular Weight:578.61
-
Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Biological Activity
|
PPARγ 137.4 nM (EC50) |
PPARα 546.3 nM (EC50) |
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.
-
Cell Line:BMDM
-
Concentration:50-200 µM
-
Incubation Time:24 h
-
Result:Inhibited the expression of IL-1β, IL-6, iNOS, COX-2 and MCP-1.
-
Cell Line:primary human corneal fibroblast
-
Concentration:1-10 µM
-
Incubation Time:48 h
-
Result:Inhibited expression of α-SMA and fibronectin.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:ApoE−/− mouse aortic atherosclerosis models[4]
-
Dosage:1-10 mg/kg
-
Administration:po for 8 weeks
-
Result:Reduced aortic arch plaques.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
-
CAS No. 763108-62-9
-
Appearance Solid
-
Molecular Weight 578.61
-
Formula C24H26N4O9S2
-
Color White to off-white
-
SMILES
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
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : 25 mg/mL (43.21 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
-
Data Sheet (274 KB)
-
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
-
Handling Instructions (2659 KB)
References
[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]
Complete Stock Solution Preparation Table
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.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.7283 mL | 8.6414 mL | 17.2828 mL | 43.2070 mL |
| 5 mM | 0.3457 mL | 1.7283 mL | 3.4566 mL | 8.6414 mL | |
| 10 mM | 0.1728 mL | 0.8641 mL | 1.7283 mL | 4.3207 mL | |
| 15 mM | 0.1152 mL | 0.5761 mL | 1.1522 mL | 2.8805 mL | |
| 20 mM | 0.0864 mL | 0.4321 mL | 0.8641 mL | 2.1603 mL | |
| 25 mM | 0.0691 mL | 0.3457 mL | 0.6913 mL | 1.7283 mL | |
| 30 mM | 0.0576 mL | 0.2880 mL | 0.5761 mL | 1.4402 mL | |
| 40 mM | 0.0432 mL | 0.2160 mL | 0.4321 mL | 1.0802 mL |