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| 5mg |
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| 25mg |
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| 50mg |
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| 100mg |
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Purity: ≥98%
Tesaglitazar (formerly AZ-242; Galida; AR-H-039242XX) is a dual peroxisome proliferator-activated receptor (PPARalpha/gamma) agonist with anti-diabetic effects. It was created with the intention of managing type 2 diabetes and has a strong affinity for PPARα and PPARγ. With EC50s of 13.4 μM and 3.6 μM for rat and human PPARα, respectively, and roughly 0.2 μM for both rat and human PPARγ, it is more potent on PPARγ than on PPARα. After the medication passed multiple phase III clinical trials, AstraZeneca declared in May 2006 that it was stopping development of the medication.
| Targets |
rat PPARα (EC50 = 13.4 μM); human PPARα (EC50 = 3.6 μM); PPARγ (EC50 = 0.2 μM)
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|---|---|
| ln Vitro |
Tesaglitazar stimulated DNA synthesis mainly in subcutaneous interstitial mesenchymal cells. The percentage of BrdU-labeled interstitial cells was increased at 1 and 10 micromol/kg after 2 weeks. The increase in DNA synthesis was still significant at the end of the 12-week treatment at 10 mumol/kg, the dose producing fibrosarcoma. However, at 1 micromol/kg, a dose below the no-observed-effect level for fibrosarcoma, the level of DNA synthesis was similar to control levels at 12 weeks.
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| References | |
| Additional Infomation |
Tesaglitazar is a dual peroxisome proliferator-activated receptor alpha/gamma agonist which improves apolipoprotein levels in non-diabetic subjects with insulin resistance. Tesaglitazar is a proposed treatment for type 2 diabetes and has completed several phase III clinical trials, however in May 2006 AstraZeneca announced that they had discontinued further development.
Tesaglitazar is a dual peroxisome proliferator-activated receptor (PPAR) agonist, with hypoglycemic activity. Tesaglitazar is more potent on the gamma subtype than on the alpha subtype of PPAR. This agent improves atherogenic dyslipidemia but may cause an increase in fibrosarcoma formation. Drug Indication Investigated for use/treatment in diabetes mellitus type 2. Pharmacodynamics Treatment with tesaglitazar lowered fasting plasma glucose, improved glucose tolerance, substantially reduced fasting and postload insulin levels, and markedly lowered fasting TG and improved lipid tolerance. |
| Molecular Formula |
C20H24O7S
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|---|---|
| Molecular Weight |
408.46536
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| Exact Mass |
408.124
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| Elemental Analysis |
C, 58.81; H, 5.92; O, 27.42; S, 7.85
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| CAS # |
251565-85-2
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| Related CAS # |
251565-85-2
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| PubChem CID |
208901
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| Appearance |
White to off-white solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
611.3±55.0 °C at 760 mmHg
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| Flash Point |
323.5±31.5 °C
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| Vapour Pressure |
0.0±1.8 mmHg at 25°C
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| Index of Refraction |
1.566
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| LogP |
2.64
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
11
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| Heavy Atom Count |
28
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| Complexity |
556
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| Defined Atom Stereocenter Count |
1
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| SMILES |
CCO[C@@H](CC1=CC=C(C=C1)OCCC2=CC=C(C=C2)OS(=O)(=O)C)C(=O)O
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| InChi Key |
CXGTZJYQWSUFET-IBGZPJMESA-N
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| InChi Code |
InChI=1S/C20H24O7S/c1-3-25-19(20(21)22)14-16-6-8-17(9-7-16)26-13-12-15-4-10-18(11-5-15)27-28(2,23)24/h4-11,19H,3,12-14H2,1-2H3,(H,21,22)/t19-/m0/s1
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| Chemical Name |
(2S)-2-ethoxy-3-[4-[2-(4-methylsulfonyloxyphenyl)ethoxy]phenyl]propanoic acid
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| Synonyms |
AZ-242; AR-H-039242XX; AZ242; AZ 242; ARH-039242XX; Galida; Tesaglitazar
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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: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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: ~200 mg/mL (~489.6 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 | 2.4482 mL | 12.2408 mL | 24.4816 mL | |
| 5 mM | 0.4896 mL | 2.4482 mL | 4.8963 mL | |
| 10 mM | 0.2448 mL | 1.2241 mL | 2.4482 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 |
| NCT00280865 | Completed | Drug: Tesaglitazar Drug: Pioglitazone |
Type 2 Diabetes | AstraZeneca | April 2002 | Phase 2 |
| NCT00229710 | Terminated | Drug: Tesaglitazar | Diabetes Mellitus, Type 2 | AstraZeneca | February 2005 | Phase 3 |
| NCT00229684 | Terminated | Drug: Tesaglitazar Drug: Pioglitazone |
Diabetes Mellitus, Type 2 | AstraZeneca | September 2004 | Phase 2 |
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