Aleglitazar - CAS:475479-34-6

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Aleglitazar (Synonyms:阿格列扎; R1439; RO0728804)

目录号 : KM12067 CAS No. : 475479-34-6 纯度 : 98%

Data Sheet 产品使用指南

Aleglitazar (R1439;RO0728804) 是一种高效的 PPARα/γ 双重激动剂，对人 PPARα 和 PPARγ 作用的 IC₅₀ 分别为 38 nM 和 19 nM。Aleglitazar 可用于 II 型糖尿病的研究。

规格	价格	是否有货	数量
5mg		In-stock

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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.

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, 48 hours
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.

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.

分子式

C₂₄H₂₃NO₅S

分子量

437.51

CAS号

475479-34-6

中文名称

阿格列扎

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

溶解性数据

In Vitro:

DMSO : ≥ 50 mg/mL (114.28 mM)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	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

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°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 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。

临床试验

纯度： 98%

Data Sheet

产品使用指南

摩尔计算器
稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量

浓度

体积

分子量*

重置计算

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2

浓度

体积

浓度

体积

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Other Forms of Rapamycin:

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The molarity calculator equation

The dilution calculator equation