[CAS NO. 476436-68-7] Naveglitazar
PRODUCTS SPECIFICATIONS [476436-68-7]
DESCRIPTION [476436-68-7]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 422.47 |
| Molecular Formula | C25H26O6 |
| SMILES | O=C(O)[C@@H](OC)CC1=CC=C(OCCCOC2=CC=C(OC3=CC=CC=C3)C=C2)C=C1 |
Summary
Naveglitazar (LY519818) is a nonthiozolidinedione peroxisome proliferator-activated receptor ( PPAR ) α-γ dual, γ-dominant agonist that has shown glucose-lowering potential in animal models [1] .
In Vitro
Naveglitazar, a non-thiazolidinediones (TZD), functions as a potent and efficacious insulin sensitizer in rodents, possessing a novel profile that may result in an improved therapeutic agent for the treatment of type 2 diabetes and associated dyslipidemia. The extent of in vitro binding of [ 3 H]Naveglitazar to plasma proteins is evaluated by ultracentrifugation in mouse, rat, and monkey plasma. The mean percentages±S.E.M. of protein binding of radioactivity in plasma over the concentration range of 0.1 to 1000 ng/ml after in vitro incubation at 37°C for 60 min are 99.5%±0.1% (mice), 99.6%±0.1% (rat), and 99.6%±0.3% (monkey). These results show that Naveglitazar is highly bound to plasma proteins among the species examined, and binding is independent of concentration [1] .
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
[ 14 C]Naveglitazar is quickly absorbed and moderately metabolized before elimination. After oral administration, 47, 31, and 62% of the radioactivity, as assessed by AUC values, are circulating as metabolites in mice, rats, and monkeys, respectively. Half-lives for Naveglitazar and radioactivity are similar within each species; however, monkeys have substantially longer half-lives in comparison to mice and rats. Naveglitazar and radioactivity are slowly cleared from the system circulation in all species evaluated [1] .
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT00065312 | Eli Lilly and Company |
Diabetes Mellitus, Non-Insulin-Dependent
|
Phase 2 |
Appearance
Solid
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 |
