Cat. No.: HY-14928

Lobeglitazone

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Based on 1 Customer Validation

Lobeglitazone is a new type of thiazolidinedione. Lobeglitazone is the orally active agonist for PPAR with EC₅₀ of 137.4 nM and 546.3 nM for PPARγ and PPARα. Lobeglitazone is the inhibitor for ERK/JNK/Smad/NF-κB signaling pathway. Lobeglitazone exhibits anti-inflammatory, anti-diabetic, anti-fibrotic and anti-atherosclerotic properties.

For research use only. We do not sell to patients.

Purity: 96.18%
CAS No.: 607723-33-1
Formula: C₂₄H₂₄N₄O₅S
Molecular Weight:480.54

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Lobeglitazone Chemical Structure

CAS No.: 607723-33-1

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

PPARγ

137.4 nM (EC₅₀)

PPARα

546.3 nM (EC₅₀)

All PPAR Isoforms :

All ERK Isoforms :

All JNK Isoforms :

All TGF-beta/Smad Isoforms :

Smad1
Smad3

All NO Synthase Isoforms :

All COX Isoforms :

All NF-κB Isoforms :

All Interleukin Related Isoforms :

In Vitro

Lobeglitazone increases glucose uptake in 3T3-L1 adipocytes and L6 muscle cells^[1].
Lobeglitazone (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 (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 (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.

Real Time qPCR^[2]

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.

Western Blot Analysis^[2]

Cell Line:

primary human corneal fibroblast
Concentration:

1-10 µM
Incubation Time:

48 h
Result:

Inhibited expression of α-SMA and fibronectin.

In Vivo

Lobeglitazone (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.

Animal Model:

ApoE−/− mouse aortic atherosclerosis models^[4]
Dosage:

1-10 mg/kg
Administration:

po for 8 weeks
Result:

Reduced aortic arch plaques.

Chemical Information

CAS No. 607723-33-1
Appearance Solid
Molecular Weight 480.54
Formula C₂₄H₂₄N₄O₅S
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
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (208.10 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.0810 mL

10.4050 mL

20.8099 mL

5 mM

0.4162 mL

2.0810 mL

4.1620 mL

10 mM

0.2081 mL

1.0405 mL

2.0810 mL

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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (5.20 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.20 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 KB)
SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. 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	2.0810 mL	10.4050 mL	20.8099 mL	52.0248 mL
	5 mM	0.4162 mL	2.0810 mL	4.1620 mL	10.4050 mL
	10 mM	0.2081 mL	1.0405 mL	2.0810 mL	5.2025 mL
	15 mM	0.1387 mL	0.6937 mL	1.3873 mL	3.4683 mL
	20 mM	0.1040 mL	0.5202 mL	1.0405 mL	2.6012 mL
	25 mM	0.0832 mL	0.4162 mL	0.8324 mL	2.0810 mL
	30 mM	0.0694 mL	0.3468 mL	0.6937 mL	1.7342 mL
	40 mM	0.0520 mL	0.2601 mL	0.5202 mL	1.3006 mL
	50 mM	0.0416 mL	0.2081 mL	0.4162 mL	1.0405 mL
	60 mM	0.0347 mL	0.1734 mL	0.3468 mL	0.8671 mL
	80 mM	0.0260 mL	0.1301 mL	0.2601 mL	0.6503 mL
	100 mM	0.0208 mL	0.1040 mL	0.2081 mL	0.5202 mL

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Lobeglitazone

Bioactive Compound Library Max

Bioactive Compound Library

Cell Cycle/DNA Damage Compound Library

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

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All PPAR Isoforms

All ERK Isoforms

All JNK Isoforms

All TGF-beta/Smad Isoforms

All NO Synthase Isoforms

All COX Isoforms

All NF-κB Isoforms

All Interleukin Related Isoforms

Biological Activity

Chemical Information

Solvent & Solubility