产品
编 号：F364676
分子式：C24H23NO5S
分子量：437.51
分子式：C24H23NO5S
分子量：437.51
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CAS No: 475479-34-6
产品详情
生物活性：
Aleglitazar (R1439) is a potent dual PPARα/γ agonist, with IC50s of 38 nM and 19 nM for human PPARa and PPARγ, respectively. Aleglitazar can be used for the research of type II diabetes.
体内研究：
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.
体外研究：
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.
Aleglitazar (R1439) is a potent dual PPARα/γ agonist, with IC50s of 38 nM and 19 nM for human PPARa and PPARγ, respectively. Aleglitazar can be used for the research of type II diabetes.
体内研究：
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.
体外研究：
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.
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