2. Cell Cycle/DNA Damage Vitamin D Related/Nuclear Receptor Metabolic Enzyme/Protease MAPK/ERK Pathway Stem Cell/Wnt TGF-beta/Smad Immunology/Inflammation NF-κB
  3. PPAR ERK JNK TGF-beta/Smad NO Synthase COX NF-κB Interleukin Related
  4. Lobeglitazone

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.

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Lobeglitazone

Lobeglitazone Chemical Structure

CAS No. : 607723-33-1

Size Prix Stock Quantité
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 En stock
Solution
10 mM * 1 mL in DMSO En stock
Solid
5 mg En stock
10 mg En stock
25 mg En stock
50 mg En stock
100 mg En stock
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Other Forms of Lobeglitazone:

Lobeglitazone Related Antibodies

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PPARα PPARβ/δ PPARγ PPAR PPARδ

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ERK ERK1 ERK2 ERK5 ERK8

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JNK1 JNK2 JNK3 JNK

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nNOS iNOS eNOS

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COX COX-1 COX-2 COX-3

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NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

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IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22 IL-18

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Description

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[1][2][3][4][5][6].

IC50 & Target

PPARγ

137.4 nM (EC50)

PPARα

546.3 nM (EC50)

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.

Lobeglitazone Related Antibodies

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.
Masse moléculaire

480.54

Formule

C24H24N4O5S
CAS No.
Appearance

Solid

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
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvant et solubilité
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0810 mL 10.4050 mL 20.8099 mL
5 mM 0.4162 mL 2.0810 mL 4.1620 mL
View the 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Calculateur de molarité

  • Calculateur de dilution

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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

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.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • 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

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureté et documentation
Références

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. 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 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Lobeglitazone607723-33-1PPARERKJNKTGF-beta/SmadNO SynthaseCOXNF-κBInterleukin RelatedPeroxisome proliferator-activated receptorsExtracellular signal regulated kinasesc-Jun N-terminal kinaseTransforming growth factor betaNitric oxide synthasesNOSCyclooxygenaseNuclear factor-κBNuclear factor-kappaBILtype 2 diabetes mellitusT2DMSprague Dawley ratA549atherosclerosisInhibitorinhibitorinhibit

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