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| 10mg |
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Purity: ≥98%
Lobeglitazone Sulfate (CKD-501) is a thiazolidinedione class of antidiabetic agent acting as a potent agonist for both PPARα and PPARγ, working as an insulin sensitizer by binding to the PPAR receptors in fat cells and making the cells more responsive to insulin.
| Targets |
strong>Lobeglitazone is a peroxisome proliferator-activated receptor gamma (PPAR-γ) agonist [1] [4]
PPARγ (EC50 = 137.4 nM); PPARα (EC50 = 546.3 nM) |
|---|---|
| ln Vitro |
In lipopolysaccharide (LPS)-stimulated bone-marrow derived macrophages (BMDMs), Lobeglitazone (1-10 μM) reduces the production of pro-inflammatory cytokines, including TNF-α, IL-6, and IL-1β, in a dose-dependent manner. It also inhibits the expression of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2), thereby decreasing nitric oxide (NO) production. Mechanistically, it suppresses LPS-induced activation of the NF-κB and MAPK (p38, JNK) signaling pathways [2]
In human corneal fibroblasts, Lobeglitazone (1-10 μM) inhibits TGF-β1-induced fibrosis by reducing the expression of α-smooth muscle actin (α-SMA), collagen type I, and fibronectin. It blocks TGF-β-mediated Smad2/3 phosphorylation and nuclear translocation, while increasing the expression of Smad7 (an inhibitory Smad) [3] |
| ln Vivo |
rats with balloon-induced carotid artery injury, oral administration of Lobeglitazone (0.3, 1, or 3 mg/kg/day) for 2 weeks reduces neointimal formation in a dose-dependent manner (by 24-56% compared to controls). It decreases the number of proliferating cell nuclear antigen (PCNA)-positive cells in the neointima and inhibits the expression of monocyte chemoattractant protein-1 (MCP-1) and vascular cell adhesion molecule-1 (VCAM-1) [4]
In an atherosclerotic mouse model (apoE-/- mice fed a high-fat diet), Lobeglitazone (1 or 3 mg/kg/day, oral for 12 weeks) reduces atherosclerotic plaque area in the aorta (by 30-45%) and decreases plaque lipid content. It also lowers serum triglyceride and LDL-cholesterol levels, while increasing HDL-cholesterol [4] In a 52-week open-label study with type 2 diabetes patients, Lobeglitazone (0.5 mg/day, oral) significantly reduces HbA1c levels (by 0.7-0.8%) and fasting plasma glucose (by 1.5-2.0 mmol/L) compared to baseline. It also improves insulin sensitivity, as indicated by reduced HOMA-IR [5] |
| Cell Assay |
For BMDM experiments, macrophages are isolated from mouse bone marrow, differentiated, and treated with Lobeglitazone (1-10 μM) for 1 hour prior to LPS stimulation (100 ng/mL). After 24 hours, culture supernatants are collected to measure cytokines (TNF-α, IL-6) via ELISA, and NO production is assessed using a Griess reagent. Western blotting is performed to analyze NF-κB and MAPK pathway proteins [2]
In corneal fibroblast studies, cells are treated with Lobeglitazone (1-10 μM) 1 hour before TGF-β1 stimulation (5 ng/mL). After 48-72 hours, α-SMA, collagen I, and fibronectin expression is measured by western blot and immunofluorescence. Smad2/3 phosphorylation and nuclear translocation are analyzed via western blot (nuclear/cytoplasmic fractions) and immunocytochemistry [3] |
| Animal Protocol |
For balloon injury in rats, male Sprague-Dawley rats undergo carotid artery balloon dilation. Starting 3 days before injury, rats receive Lobeglitazone (0.3, 1, or 3 mg/kg/day) or vehicle via oral gavage, continued for 2 weeks post-injury. Rats are euthanized, and carotid arteries are harvested for histomorphometric analysis (neointimal area, media area) and immunohistochemistry (PCNA, MCP-1) [4]
In apoE-/- mice, 8-week-old mice are fed a high-fat diet and randomized to Lobeglitazone (1 or 3 mg/kg/day) or vehicle via oral gavage for 12 weeks. Aortic tissues are collected to quantify atherosclerotic plaques, and serum lipids are measured using biochemical assays [4] |
| ADME/Pharmacokinetics |
In humans, after oral administration of lobeglitazone (0.5 mg), peak plasma concentration (Cmax) is reached in 1.5–2 hours, and the elimination half-life is approximately 24 hours. The drug has a high protein binding rate (>99%) and is mainly metabolized by hepatic CYP3A4. Approximately 30% and 60% of the administered dose are excreted in urine and feces, respectively. [1]
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| Toxicity/Toxicokinetics |
In a 52-week clinical study, lobeglitazone (0.5 mg/day) was well tolerated. The most common adverse events were mild edema (5-7%) and weight gain (2-3%). No significant changes in liver function (ALT, AST) or kidney function (creatinine) were observed[5]. Animal studies have shown that no significant toxicity, including hepatotoxicity or nephrotoxicity, was observed at doses up to 3 mg/kg/day[4].
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| References |
[1]. Lobeglitazone: A Novel Thiazolidinedione for the Management of Type 2 Diabetes Mellitus. Diabetes Metab J. 2021 May;45(3):326-336.
[2]. Lobeglitazone Exerts Anti-Inflammatory Effect in Lipopolysaccharide-Induced Bone-Marrow Derived Macrophages. Biomedicines. 2021 Oct 10;9(10):1432. [3]. Lobeglitazone attenuates fibrosis in corneal fibroblasts by interrupting TGF-beta-mediated Smad signaling. Graefes Arch Clin Exp Ophthalmol. 2022 Jan;260(1):149-162. [4]. 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. [5]. Safety and efficacy of lobeglitazone monotherapy in patients with type 2 diabetes mellitus over 52 weeks: An open-label extension study. Diabetes Res Clin Pract. 2015 Dec;110(3):e27-30. |
| Additional Infomation |
Lobeglitazone is a thiazolidinedione (TZD) drug used to treat type 2 diabetes and has been approved for marketing in South Korea. Its mechanism of action involves PPAR-γ activation, thereby enhancing insulin sensitivity in adipose tissue, muscle and liver. In addition to glycemic control, it also has anti-inflammatory, anti-atherosclerotic and anti-fibrotic effects, suggesting that it may have potential benefits in complications such as cardiovascular disease and tissue fibrosis [1][2][3][4][5].
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| Molecular Formula |
C24H24N4O5S.H2O4S
|
|---|---|
| Molecular Weight |
578.615
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| Exact Mass |
578.114
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| Elemental Analysis |
C, 49.82; H, 4.53; N, 9.68; O, 24.89; S, 11.08
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| CAS # |
763108-62-9
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| Related CAS # |
Lobeglitazone;607723-33-1
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| PubChem CID |
15951505
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| Appearance |
White to off-white solid powder
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| LogP |
4.435
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| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
13
|
| Rotatable Bond Count |
10
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| Heavy Atom Count |
39
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| Complexity |
751
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| Defined Atom Stereocenter Count |
0
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| SMILES |
S(O)(O)(=O)=O.COC1=CC=C(OC2=NC=NC(CNCCOC3=CC=C(CC4SC(=O)NC4=O)C=C3)=C2)C=C1
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| InChi Key |
IFBYQAMJTBOBHB-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C24H24N4O5S.H2O4S/c1-28(21-14-22(26-15-25-21)33-19-9-7-17(31-2)8-10-19)11-12-32-18-5-3-16(4-6-18)13-20-23(29)27-24(30)34-201-5(2,3)4/h3-10,14-15,20H,11-13H2,1-2H3,(H,27,29,30)(H2,1,2,3,4)
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| Chemical Name |
5-(4-(2-((6-(4-methoxyphenoxy)pyrimidin-4-yl)(methyl)amino)ethoxy)benzyl)thiazolidine-2,4-dione sulfate
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| Synonyms |
CKD-501; Lobeglitazone sulfate; 763108-62-9; 95C712E83P; UNII-95C712E83P; CKD 501; CKD501 Duvie
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7282 mL | 8.6412 mL | 17.2825 mL | |
| 5 mM | 0.3457 mL | 1.7282 mL | 3.4565 mL | |
| 10 mM | 0.1728 mL | 0.8641 mL | 1.7282 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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