Aleglitazar (Synonyms: R1439; RO0728804)

Cat. No.: HY-14728 Purity: 99.74%: FAQs
Data Sheet SDS COA Handling Instructions

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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.

For research use only. We do not sell to patients.

Aleglitazar Chemical Structure

CAS No. : 475479-34-6

Size	Price	Stock
1 mg	USD 350	Ask For Quote & Lead Time

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PPARα PPARβ/δ PPARγ PPAR PPARδ

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

PPARγ

19 nM (IC₅₀)

PPARα

38 nM (IC₅₀)

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.

Clinical Trial

Molecular Weight

437.51

Formula

C₂₄H₂₃NO₅S

CAS No.

475479-34-6

Appearance

Solid

Color

White to yellow

SMILES

CC1=C(CCOC2=CC=C(C[C@@H](C(O)=O)OC)C3=C2C=CS3)N=C(C4=CC=CC=C4)O1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : ≥ 50 mg/mL (114.28 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

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

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.71 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (5.71 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.74%

Select Batch:

Data Sheet (282 KB) SDS (0 KB)

COA (256 KB) LCMS (93 KB)

Handling Instructions (2659 KB)

References

[1]. Bénardeau A, Benz J, Binggeli A, et al. Aleglitazar, a new, potent, and balanced dual PPARalpha/gamma agonist for the treatment of type II diabetes. Bioorg Med Chem Lett. 2009 May 1;19(9):2468-73. [Content Brief]

[2]. Yan Chen, et al. Aleglitazar, a dual peroxisome proliferator-activated receptor-α and -γ agonist, protects cardiomyocytes against the adverse effects of hyperglycaemia. Diab Vasc Dis Res. 2017 Mar; 14(2): 152–162. [Content Brief]

[3]. Valérie Boujon, et al. Dual PPARα/γ agonist aleglitazar confers stroke protection in a model of mild focal brain ischemia in mice. J Mol Med (Berl). 2019; 97(8): 1127-1138. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.2857 mL	11.4283 mL	22.8566 mL	57.1415 mL
	5 mM	0.4571 mL	2.2857 mL	4.5713 mL	11.4283 mL
	10 mM	0.2286 mL	1.1428 mL	2.2857 mL	5.7142 mL
	15 mM	0.1524 mL	0.7619 mL	1.5238 mL	3.8094 mL
	20 mM	0.1143 mL	0.5714 mL	1.1428 mL	2.8571 mL
	25 mM	0.0914 mL	0.4571 mL	0.9143 mL	2.2857 mL
	30 mM	0.0762 mL	0.3809 mL	0.7619 mL	1.9047 mL
	40 mM	0.0571 mL	0.2857 mL	0.5714 mL	1.4285 mL
	50 mM	0.0457 mL	0.2286 mL	0.4571 mL	1.1428 mL
	60 mM	0.0381 mL	0.1905 mL	0.3809 mL	0.9524 mL
	80 mM	0.0286 mL	0.1429 mL	0.2857 mL	0.7143 mL
	100 mM	0.0229 mL	0.1143 mL	0.2286 mL	0.5714 mL

Aleglitazar Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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