| 生物活性 | Aleglitazar (R1439) is a potent dualPPARα/γagonist, withIC50s of 38 nM and 19 nM for human PPARa andPPARγ, respectively. Aleglitazar can be used for the research of type II diabetes[1]. |
| IC50& Target | PPARγ 19 nM (IC50) | PPARα 38 nM (IC50) |
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体外研究
(In Vitro) | 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[1].
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[2].
Aleglitazar (0.01-20 μM; 48 hours) decreases hyperglycaemic conditions (HG, glucose 25 mM)-induced apoptosis, caspase-3 activity and cytochrome-C release[2].
Aleglitazar improves cell viability in cells exposed to hyperglycaemia[2].
Cell Cytotoxicity Assay[2] | 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. |
Apoptosis Analysis[2] | 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. |
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体内研究
(In Vivo) | 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[3].
Aleglitazar reduces key aspects of microglia activation including NO production, release of proinflammatory cytokines, migration, and phagocytosis[3].
Aleglitazar attenuates inflammatory responses in post-ischemic brain[3].
| Animal Model: | Male 129S6/SvEv mice (24-30 g), middle cerebral artery occlusion (MCAo) models[3] | | 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. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : ≥ 50 mg/mL(114.28 mM) *"≥" means soluble, but saturation unknown. 配制储备液 | 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 |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (5.71 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (5.71 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (5.71 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (5.71 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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