Aleglitazar
-
Aleglitazar
structure -
-
CAS No:
475479-34-6
-
Formula:
C24H23NO5S
-
Chemical Name:
Aleglitazar
-
Synonyms:
Benzo[b]thiophene-7-propanoic acid,α-methoxy-4-[2-(5-methyl-2-phenyl-4-oxazolyl)ethoxy]-,(αS)-;(αS)-α-Methoxy-4-[2-(5-methyl-2-phenyl-4-oxazolyl)ethoxy]benzo[b]thiophene-7-propanoic acid;(S)-2-Methoxy-3-[4-[2-(5-methyl-2-phenyloxazol-4-yl)ethoxy]benzo[b]thiophen-7-yl]propionic acid;Aleglitazar;RO 0728804;R 1439
-
CAS No:
Description
Aleglitazar(R1439; RO-0728804) is a new dual PPAR-α/γ agonist with IC50 of 2.8 nM/4.6 nM.IC50 Value: 2.8 nM(PPAR-α); 4.6 nM(PPAR-γ)Target: PPARα/γAleglitazar (R1439) is a dual peroxisome proliferator-activated receptor (PPAR) agonist, with affinity to PPARα and PPARγ. Aleglitazar is being developed for the treatment of type II diabetes; It is currently in phase III clinical trials. In preliminary clinical studies, Aleglitazar has been demonstrated to improve hyperglycemia and dyslipidemi
Aleglitazar is an investigational drug from the company Hoffmann–La Roche and is currently in a phase III clinical trial called ALECARDIO. It is being investigated for use in patients with type II diabetes to reduce their risks of cardiovascular mortality and morbidity. Aleglitazar is an agonist at the peroxisome proliferator-activated receptor (PPAR) for both the PPARα and PPARγ receptor subtypes. In the phase II clinical trial called SYNCHRONY, with type II diabetic patients, aleglitazar was able to control both lipid and glucose levels in a synergistic manner while also having limited side effects and toxicity.|Aleglitazar is a dual peroxisome proliferator-activated receptor (PPAR) agonist, with hypoglycemic activity. Aleglitazar binds to both PPARalpha and PPARgamma and decreases plasma levels of glucose, LDL-C, triglycerides (TG) and increases HDL levels. This agent may be used for the treatment of diabetes and cardiovascular disease.
Drug Information
Investigated for use in patients with type II diabetes to reduce their risks of cardiovascular mortality and morbidity.
Aleglitazar was rationally designed to be an agonist at the peroxisome proliferator-activated receptor (PPAR) for both the PPARα and PPARγ receptor subtypes. Agonistic action at PPARα controls lipid levels, which improves dyslipidemia, and agonistic action at PPARγ controls glucose levels, which improves insulin sensitivity in diabetes.
aleglitazar
Computed Properties
Molecular Weight:437.5
XLogP3:5.1
Hydrogen Bond Donor Count:1
Hydrogen Bond Acceptor Count:7
Rotatable Bond Count:9
Exact Mass:437.12969401
Monoisotopic Mass:437.12969401
Topological Polar Surface Area:110
Heavy Atom Count:31
Complexity:586
Defined Atom Stereocenter Count:1
Covalently-Bonded Unit Count:1
Compound Is Canonicalized:Yes