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  3. Aleglitazar

Aleglitazar (Synonyms: R1439; RO0728804)

Cat. No.: HY-14728 Purity: 99.30%
Handling Instructions

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

Aleglitazar Chemical Structure

CAS No. : 475479-34-6

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5 mg USD 650 In-stock
Estimated Time of Arrival: December 31
10 mg USD 950 In-stock
Estimated Time of Arrival: December 31
50 mg USD 2500 Get quote
100 mg USD 3500 Get quote
200 mg   Get quote  
500 mg   Get quote  

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Description

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[1].

IC50 & Target[5]

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].

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].

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

SMILES

CC1=C(CCOC2=CC=C(C[[email protected]@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 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 50 mg/mL (114.28 mM)

H2O : < 0.1 mg/mL (insoluble)

*"≥" 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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.71 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 99.30%

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Keywords:

AleglitazarR1439 RO0728804R 1439R-1439RO0728804RO 0728804RO-0728804PPARPeroxisome proliferator-activated receptorsperoxisomeproliferator-activatedreceptorPPARαPPARγhyperglycemiacardiovascularriskdiabeticmicroglianeuroinflammationstrokeInhibitorinhibitorinhibit

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Aleglitazar
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