Aleglitazar

Research use only, not for human use.

A potent and balanced dual PPARα/γ agonist (EC50= 50/21 nM).

A potent and balanced dual PPARα/γ agonist (EC50= 50/21 nM); shows high efficacy in animal models of type II diabetes.Diabetes Phase 2 Discontinued.

Aleglitazar exhibits species selectivity with respect to PPARα, with an EC50s of 50 nM, 2.26 μM and 2.34 μM for human PPARα, rat PPARα and mouse PPARα, respectively.Aleglitazar (0.01-40 μM; 12-48 hours) does not significantly increase lactate dehydrogenase (LDH) release at concentrations of 0.1 μM to 20?μM, but significant increases LDH release at concentrations of 30 μM and 40?μM.Aleglitazar (0.01-20?μM; 48?hours) decreases hyperglycaemic conditions (HG, glucose 25?mM)-induced apoptosis, caspase-3 activity and cytochrome-C release.Aleglitazar improves cell viability in cells exposed to hyperglycaemia. Cell Cytotoxicity 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, 48hours Result:Increased LDH release at concentrations of 30 μM and 40?μM.Apoptosis Analysis Cell Line:HCM, mCM-WT Concentration:0.01?μM, 0.05?μM, 0.1?μM, 0.5?μM, 1 μM, 5 μM, 10 μM, 20 μM Incubation Time:48?hours Result:Dose dependently decreased apoptosis, caspase-3 activity and cytochrome-C release induced by HG.

Aleglitazar (0.3-3.0 mg/kg; i.p.; daily; for 7 days) exerts beneficial effects on structural and functional outcomes of mild brain ischemia.Aleglitazar reduces key aspects of microglia activation including NO production, release of proinflammatory cytokines, migration, and phagocytosis.Aleglitazar attenuates inflammatory responses in post-ischemic brain. Animal Model:Male 129S6/SvEv mice (24-30 g), middle cerebral artery occlusion (MCAo) models Dosage:0.3 mg/kg, 3.0 mg/kg Administration:Intraperitoneal injection, daily, for 7 days Result:Reduced the size of the ischemic lesion as assessed using NeuN immunohistochemistry on day 7.

R1439 | RO0728804 | R-1439 | RO-0728804 | R 1439 | RO 0728804

Metabolic Enzyme/Protease

PPAR

PPAR

Metabolic Disease

Diabetes

475479-34-6

437.5081

C24H23NO5S

>98% (HPLC)

10 mM in DMSO

CC1=C(N=C(O1)C2=CC=CC=C2)CCOC3=C4C=CSC4=C(C=C3)C[C@@H](C(=O)O)OC

Benzo[b]thiophene-7-propanoic acid, α-methoxy-4-[2-(5-methyl-2-phenyl-4-oxazolyl)ethoxy]-, (αS)-

(-20℃)

With Ice Pack

≥ 2 years