| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| Other Sizes |
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| ln Vitro |
Ciglitazone (0–20 μM; 24 hours) uses the PPAR non-smoking pathway to sense cells. Ciglitazone increases intracellular Ca2+ and produces reactive oxygen species [4].
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|---|---|
| ln Vivo |
In C57BL/6J-ob/ob, ciglitazone (100 mg/kg/day; 2 days) resulted in the recovery of hypertension. In ob/ob treated with 100 mg/kg/day Ciglitazone for 41–44 days, regranulation of pancreatic beta cells and enhanced islet insulin content were noted [3].
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| References |
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| Additional Infomation |
Ciglitazone is an aromatic ether that consists of 1,3-thiazolidine-2,4-dione with position 5 substituted by a 4-[(1-methylcyclohexyl)methoxy]benzyl group. A selective PPARgamma agonist. It has a role as an insulin-sensitizing drug and an antineoplastic agent. It is a thiazolidinone and an aromatic ether.
Developed by Takeda Pharmaceuticals in the early 1980s, it is considered the prototypical compound for the thiazolidinedione class. Ciglitazone was never used as a medication, but it sparked interest in the effects of thiazolidinediones. Several analogues were later developed, some of which—such as pioglitazone and troglitazone—made it to the market. Ciglitazone significantly decreases VEGF production by human granulosa cells in an in vitro study, and may potentially be used in ovarian hyperstimulation syndrome. Ciglitazone is a potent and selective PPARγ ligand with an EC50 of 3.0 µM. It is also an anti-hyperglycemic agent in the ob/ob murine model in vivo. Ciglitazone increases adipogenesis, decreases differentiation and angiogenesis in human umbilical vein endothelial cell (HUVEC), and osteoblastogenesis in human mesenchymal stem cells. Ciglitazone is an agent belonging to the glitazone (thiazolidinedione) class of antidiabetic agents with antihyperglycemic activity. Ciglitazone also exerts anti-inflammatory activity through the modulation of nuclear factor-kappaB-mediated pathways. In addition, this agent inhibits angiogenesis by reducing vascular endothelial growth factor (VEGF) production and inhibits growth of melanoma cells by inhibiting the expression of (C-X-C motif) ligand 1 (CXCL1). This agent is the prototypical compound for the thiazolidinedione class, and has never been marketed. |
| Molecular Formula |
C18H23NO3S
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|---|---|
| Molecular Weight |
333.44
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| Exact Mass |
333.139
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| CAS # |
74772-77-3
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| PubChem CID |
2750
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| Appearance |
White to off-white solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
504.5±23.0 °C at 760 mmHg
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| Melting Point |
130-131ºC
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| Flash Point |
258.9±22.6 °C
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| Vapour Pressure |
0.0±1.3 mmHg at 25°C
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| Index of Refraction |
1.568
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| LogP |
4.69
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
23
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| Complexity |
440
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
YZFWTZACSRHJQD-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H23NO3S/c1-18(9-3-2-4-10-18)12-22-14-7-5-13(6-8-14)11-15-16(20)19-17(21)23-15/h5-8,15H,2-4,9-12H2,1H3,(H,19,20,21)
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| Chemical Name |
5-[[4-[(1-methylcyclohexyl)methoxy]phenyl]methyl]-1,3-thiazolidine-2,4-dione
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| Synonyms |
ADD3878 U63287 ADD-3878 ADD 3878U-63287
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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 (~299.90 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 | 2.9990 mL | 14.9952 mL | 29.9904 mL | |
| 5 mM | 0.5998 mL | 2.9990 mL | 5.9981 mL | |
| 10 mM | 0.2999 mL | 1.4995 mL | 2.9990 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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