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| 25mg |
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| 50mg |
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| 100mg |
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Purity: ≥98%
Balaglitazone (also known as NNC-610645; NNC-612344; NN-2344; DRF-2593) is a selective partial agonist of PPARγ (peroxisome proliferator-activated receptor) with an EC50 of 1.351 μM for human PPARγ. PPARγ is a promising target for the treatment of Type II Diabetes because it is involved in the regulation of insulin, triglycerides, and lipid metabolism. In a number of animal models, balaglitazone has demonstrated strong blood glucose-lowering properties.
| Targets |
PPARγ (EC50 = 351 nM)
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|---|---|
| ln Vitro |
Balaglitazone is a selective partial PPARγ agonist with an EC50 of 1.351 μM[1]. The cytotoxicity of balaglitazone (5-100 μM) on K562 and K562/DOX cells is equivalent. In K562 and K562/DOX cells, balaglitazone reduces the cytotoxicity of doxorubicin with IC50 values of 0.117 μM and 0.53 μM, respectively. In K562/DOX cells, balaglitazone reverses multidrug resistance (MDR). While balaglitazone (25 µM) does not increase MFI in K562 cells, it does increase Rh123 accumulation in K562/DOX cells. Balaglitazone inhibits PTEN expression in K562/DOX cells, which results in a downregulation of P-gp expression in K562/DOX cells. PTEN inhibition reverses these effects[2].
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| ln Vivo |
Balaglitazone (3 mg/kg, p.o.) exhibits more potent antihyperglycemic action than rosiglitazone, the full PPARγ agonist, in fully diabetic and insulin-resistant db/db mice[1]. In obese male rats fed a diet, balaglitazone (10 mg/kg, p.o.) reduces insulin levels, suppresses total glucose, and increases body weight; these effects are comparable to those of pioglitazone (30 mg/kg)[3].
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| Cell Assay |
Cell viability analyses employ the MTT assay. In short, a density of 2 × 104 cells/well is seeded with K562 and K562/DOX cells in a 96-well plate using RPMI-1640 medium supplemented with 10% FBS. RPMI-1640 medium (without FBS) is used to dilute different concentrations of doxorubicin (DOX) with or without balaglitazone, which are then added to each well after a 24-hour incubation period. There is a blank control and three duplicates of each group's experiment carried out. The medium is taken out after 48 hours of treatment, and 200 μL of RPMI-1640 medium that has been supplemented with 10% FBS and 10% MTT (5 mg/mL) is added. Substituting 100 μL of RPMI-1640 medium with an equivalent volume of dimethyl sulfoxide (DMSO) dissolves the reduced intracellular formazan product following an additional 4-hour incubation period. Using a microplate reader, absorbance values are determined at 570 nm. It is calculated what each experiment's half maximal inhibitory concentration (IC50) is. By dividing the treatment's IC50 value in resistant cells by the treatment's IC50 value in corresponding parental cells, the resistance fold (RF) is computed[2].
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| Animal Protocol |
In adult male diabetic db/db mice, the antihyperglycemic effects of rosiglitazone and balaglitazone are evaluated. Animals are divided into 11 groups (n = 6) based on their fasting blood glucose at the age of 14 weeks. Over the course of nine days, mice are given increasing doses of either rosiglitazone (0.2; 0.6; 2.0; 6.0 mg/kg/day) or balaglitazone (0.1; 0.3; 1.0; 3.0; 10.0 mg/kg/day) or a vehicle (0.2% carboxymethyl cellulose (CMC) + 0.4% Tween-80 in saline). Following a 7-day course of treatment, insulin and glucose levels are measured in morning plasma samples collected between 8:00 and 10:00 AM. The animals are given an oral glucose tolerance test (OGTT; 3.0 g/kg) following a course of treatment lasting nine days. For every dose, the resulting area under the curve is computed[1].
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| References |
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| Molecular Formula |
C20H17N3O4S
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|---|---|
| Molecular Weight |
395.43168
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| Exact Mass |
395.09
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| Elemental Analysis |
C, 60.75; H, 4.33; N, 10.63; O, 16.18; S, 8.11
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| CAS # |
199113-98-9
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| Related CAS # |
199113-98-9
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| Appearance |
A crystalline solid
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| SMILES |
CN1C(=NC2=CC=CC=C2C1=O)COC3=CC=C(C=C3)CC4C(=O)NC(=O)S4
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| InChi Key |
IETKPTYAGKZLKY-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H17N3O4S/c1-23-17(21-15-5-3-2-4-14(15)19(23)25)11-27-13-8-6-12(7-9-13)10-16-18(24)22-20(26)28-16/h2-9,16H,10-11H2,1H3,(H,22,24,26)
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| Chemical Name |
5-[[4-[(3-methyl-4-oxoquinazolin-2-yl)methoxy]phenyl]methyl]-1,3-thiazolidine-2,4-dione
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| Synonyms |
DRF 2593; NNC-61-0645; DRF2593; NNC 61-0645; DRF-2593; NNC-610645; NNC-61-2344; NNC-612344; NNC61-2344; NN-2344; NN2344; NN 2344; NNC-610645; NNC610645; NNC 610645; NNC-612344; NNC 612344; NNC612344
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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) |
DMSO: ~100 mg/mL (~252.9 mM）
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.32 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.32 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.32 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5289 mL | 12.6445 mL | 25.2889 mL | |
| 5 mM | 0.5058 mL | 2.5289 mL | 5.0578 mL | |
| 10 mM | 0.2529 mL | 1.2644 mL | 2.5289 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT00515632 | Completed | Drug: Balaglitazone | Diabetes Mellitus, Type 2 | Rheoscience A/S | July 2007 | Phase 3 |
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