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Darglitazone (CP-86325) is a thiazolidinedione-based PPAR-γ agonist useful for controlling blood glucose and lipid metabolism, and may be used for type II diabetes.
| ln Vitro |
Cell lines that mirrored brown (HIB-1B) and white (T3-L1 and 3T3-F442A) adipose tissue and skeletal muscle (L6) were exposed to 30 μM daglitazone for four hours in order to separate the cells. In about 8 hours, increased protein 2 (UCP2) mRNA achieves a plateau of 5–10 times the basal value. Dapglitazone may use PPAR-γ to increase UCP2 gene expression[2].
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| ln Vivo |
Daglitazone therapy normalizes increased levels of triglycerides, corticosterone, and very-low-density lipoprotein while restoring euglycemia. In ob/ob mice, dapglitazone dramatically decreased the extent of the infarct following a 24-hour recovery period. In diabetic mice, daglitazone treatment dramatically enhances the recovery from hypoxic-ischemic (H/I) injury and reinstates the absent acute brain inflammatory response [1].
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| Animal Protocol |
Animal/Disease Models: Male diabetic ob/ob mice [1]
Doses: 1 mg/kg Route of Administration: Oral; daily; 7 days Experimental Results: Blood glucose in diabetic ob/ob mice normalized, circulating triglycerides (TG ) and very low-density lipoprotein (VLDL) were diminished, but had no effect in non-diabetic mice. |
| References |
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| Additional Infomation |
Darglitazone is an agent belonging to the glitazone class of antidiabetic agents with antihyperglycemic and anti-inflammatory activities. Darglitazone may be able to abrogate acute cerebral inflammatory responses via its suppression of proinflammatory gene expression.
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| Molecular Formula |
C23H20N2O4S
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|---|---|
| Molecular Weight |
420.4809
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| Exact Mass |
420.114
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| CAS # |
141200-24-0
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| Related CAS # |
Darglitazone Sodium;149904-87-0
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| PubChem CID |
60870
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| Appearance |
White to light yellow solid powder
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| LogP |
4.635
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
30
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| Complexity |
643
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
QQKNSPHAFATFNQ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C23H20N2O4S/c1-14-18(24-22(29-14)17-5-3-2-4-6-17)11-12-19(26)16-9-7-15(8-10-16)13-20-21(27)25-23(28)30-20/h2-10,20H,11-13H2,1H3,(H,25,27,28)
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| Chemical Name |
5-[[4-[3-(5-methyl-2-phenyl-1,3-oxazol-4-yl)propanoyl]phenyl]methyl]-1,3-thiazolidine-2,4-dione
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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 Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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 : ~50 mg/mL (~118.91 mM)
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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 | 2.3782 mL | 11.8912 mL | 23.7823 mL | |
| 5 mM | 0.4756 mL | 2.3782 mL | 4.7565 mL | |
| 10 mM | 0.2378 mL | 1.1891 mL | 2.3782 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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