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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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Aleglitazar (RG-1439; RO-0728804; RG1439; RO0728804) is a novel and potent agonist of peroxisome proliferator-activated receptor (PPARα and PPARγ) with potential antidiabetic effects. In type 2 diabetics, aleglitazar, a PPAR modulator with strong affinity for PPARα and PPARγ, can help with insulin sensitivity, glucose regulation, and lipid levels. Phase III clinical trials are investigating it as a potential treatment for type II diabetes. Aleglitazar may have a therapeutic role in modifying cardiovascular risk factors and improving glycemic control in patients with type 2 diabetes, in addition to its positive effects on lipid and glucose parameters.
Targets |
PPARγ (IC50 = 19 nM); PPARα (IC50 = 38 nM)
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ln Vitro |
Aleglitazar demonstrates species selectivity towards PPARα, as evidenced by its EC50 values of 50 nM, 2.26 µM, and 2.34 µM for PPARα in humans, rat PPARα, and mouse PPARα, respectively[1].
Aleglitazar (0.01-40 µM; 12-48 hours) significantly increases lactate dehydrogenase (LDH) release at concentrations of 30 µM and 40 µM, but not at concentrations of 0.1 µM to 20 µM[2]. Aleglitazar (0.01–20 µM; 48 hr) reduces caspase-3 activity, cytochrome-C release, and apoptosis induced by hyperglycemia (HG, glucose 25 mM)[2]. Aleglitazar increases the viability of cells exposed to high blood sugar levels[2]. |
ln Vivo |
Aleglitazar (0.3–3.0 mg/kg; intraperitoneal; daily; for 7 days) improves the anatomical and functional results of mild brain ischemia[3].
Aleglitazar inhibits the production of NO, the release of proinflammatory cytokines, migration, and phagocytosis, among other important aspects of microglia activation[3]. Aleglitazar reduces post-ischemic brain inflammatory responses[3]. |
Cell Assay |
Cell Line: human cardiomyocytes (HCM), wild-type mice cardiomyocytes (mCM-WT)
Concentration: 0.01 µM, 0.05 µM, 0.1 µM, 0.5 µM, 1 µM, 5 µM, 10 µM, 20 µM, 30 µM, 40 µM Incubation Time: 12 hours, 24 hours, 48 hours Result: Increased LDH release at concentrations of 30 µM and 40 µM. |
Animal Protocol |
Male 129S6/SvEv mice (24-30 g), middle cerebral artery occlusion (MCAo) models[3]
0.3 mg/kg, 3.0 mg/kg Intraperitoneal injection, daily, for 7 days |
References |
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Molecular Formula |
C24H23NO5S
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Molecular Weight |
437.51
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Exact Mass |
437.1297
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Elemental Analysis |
C, 65.89; H, 5.30; N, 3.20; O, 18.28; S, 7.33
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CAS # |
475479-34-6
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Related CAS # |
475479-34-6
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Appearance |
Solid powder
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SMILES |
CC1=C(N=C(O1)C2=CC=CC=C2)CCOC3=C4C=CSC4=C(C=C3)C[C@@H](C(=O)O)OC
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InChi Key |
DAYKLWSKQJBGCS-NRFANRHFSA-N
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InChi Code |
InChI=1S/C24H23NO5S/c1-15-19(25-23(30-15)16-6-4-3-5-7-16)10-12-29-20-9-8-17(14-21(28-2)24(26)27)22-18(20)11-13-31-22/h3-9,11,13,21H,10,12,14H2,1-2H3,(H,26,27)/t21-/m0/s1
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Chemical Name |
(2S)-2-methoxy-3-[4-[2-(5-methyl-2-phenyl-1,3-oxazol-4-yl)ethoxy]-1-benzothiophen-7-yl]propanoic acid
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Synonyms |
RG-1439; RO-0728804; RG1439; R 1439; R1439; RO0728804; RO 0728804; RG 1439; R-1439; Aleglitazar
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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: ≥ 50 mg/mL (~114.3 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.71 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 (5.71 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.2857 mL | 11.4283 mL | 22.8566 mL | |
5 mM | 0.4571 mL | 2.2857 mL | 4.5713 mL | |
10 mM | 0.2286 mL | 1.1428 mL | 2.2857 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 |
NCT01197911 | Completed | Drug: aleglitazar | Healthy Volunteer | Hoffmann-La Roche | September 2010 | Phase 1 |
NCT01701739 | Completed | Drug: aleglitazar Drug: digoxin |
Healthy Volunteer | Hoffmann-La Roche | October 2012 | Phase 1 |
NCT01679639 | Completed | Drug: aleglitazar Drug: rifampicin |
Healthy Volunteer | Hoffmann-La Roche | August 2012 | Phase 1 |
Aleglitazar reduces stroke damage and expression of inflammatory molecules after mild transient brain ischemia. J Mol Med (Berl) . 2019 Aug;97(8):1127-1138. td> |
Metabolic effects of aleglitazar. J Mol Med (Berl) . 2019 Aug;97(8):1127-1138. td> |
Effects of Aleglitazar on cytotoxicity in human cardiomyocytes (HCM) and wild-type mice cardiomyocytes (mCM-WT). Diab Vasc Dis Res . 2017 Mar;14(2):152-162. td> |
Effects of Aleglitazar on apoptosis, caspase-3 activity and cytochrome-C induced by HG in human cardiomyocytes (HCM), wild-type mouse cardiomyocytes (mCM-WT) and cardiac-specific inducible PPARγ KO mice cardiomyocytes (mCM-PPARγ KO). Diab Vasc Dis Res . 2017 Mar;14(2):152-162. td> |