| Identification | Back Directory | [Name]
ALEGLITAZAR | [CAS]
475479-34-6 | [Synonyms]
R1439
R-1439
R 1439
RO0728804
RO-0728804
RO 0728804
ALEGLITAZAR
Unii-41T4oag59u
R1439;RO0728804;R-1439;RO-0728804;R 1439;RO 0728804
Benzo[b]thiophene-7-propanoicacid, a-Methoxy-4-[2-(5-Methyl-2-phenyl-4-oxazolyl)ethoxy]-,(aS)-
(S)-2-Methoxy-3-[4-[2-(5-methyl-2-phenyloxazol-4-yl)ethoxy]benzo[b]thiophen-7-yl]propionic acid
(S)-2-methoxy-3-(4-(2-(5-methyl-2-phenyloxazol-4-yl)ethoxy)benzo[b]thiophen-7-yl)propanoic acid
Benzo[b]thiophene-7-propanoic acid, α-methoxy-4-[2-(5-methyl-2-phenyl-4-oxazolyl)ethoxy]-, (αS)-
(2S)-2-Methoxy-3-{4-[2-(5-methyl-2-phenyl-1,3-oxazol-4-yl)ethoxy]-1-benzothiophen-7-yl}propanoic acid | [Molecular Formula]
C24H23NO5S | [MDL Number]
MFCD09954107 | [MOL File]
475479-34-6.mol | [Molecular Weight]
437.51 |
| Chemical Properties | Back Directory | [Melting point ]
146-147 °C | [Boiling point ]
665.2±65.0 °C(Predicted) | [density ]
1.290 | [storage temp. ]
Store at -20°C | [solubility ]
DMSO: ≥ 50 mg/mL (114.28 mM); Water: < 0.1 mg/mL (insoluble) | [form ]
Powder | [pka]
3.54±0.46(Predicted) | [color ]
White to yellow |
| Hazard Information | Back Directory | [Uses]
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]. | [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. |
| [target]
PPAR | [IC 50]
PPARγ: 19 nM (IC50); PPARα: 38 nM (IC50) | [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. DOI:10.1016/j.bmcl.2009.03.036
[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. DOI:10.1177/1479164116679081
[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. DOI:10.1007/s00109-019-01801-0 |
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| Company Name: |
LGM Pharma
|
| Tel: |
1-(800)-881-8210 |
| Website: |
www.lgmpharma.com |
| Company Name: |
BOC Sciences
|
| Tel: |
1-631-485-4226; 16314854226 |
| Website: |
https://www.bocsci.com |
| Company Name: |
SPIRO PHARMA
|
| Tel: |
|
| Website: |
www.spiropharma.com.cn |
|