2. Cell Cycle/DNA Damage Vitamin D Related/Nuclear Receptor Metabolic Enzyme/Protease
  3. PPAR
  4. Naveglitazar

Naveglitazar  (Synonyms: LY519818)

Cat. No.: HY-U00036A Purity: 99.47%
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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.

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Naveglitazar Chemical Structure

Naveglitazar Chemical Structure

CAS No. : 476436-68-7

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Based on 1 publication(s) in Google Scholar

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Description

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 [3H]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.

Naveglitazar Related Antibodies
In Vivo

[14C]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
Molecular Weight

422.47

Formula

C25H26O6
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C(O)[C@@H](OC)CC1=CC=C(OCCCOC2=CC=C(OC3=CC=CC=C3)C=C2)C=C1
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
Purity & Documentation
References
Animal Administration
[1]

The single-dose plasma pharmacokinetics of Naveglitazar, LY591026, and radioactivity are studied in male ICR mice, and male Fischer 344 rats after oral administration of [14C]Naveglitazar. A separate study is conducted in rats to evaluate the pharmacokinetics of Naveglitazar and LY591026 after the administration of a single 10 mg/kg dose of each compound. Mice and rats are administered a 10 mg/kg oral dose of [14C]Naveglitazar with a specific activity of 50 μCi/kg[1].
Mice[1]
Mice are divided into three groups. Group 1 animals (n=3 per time point) are housed in shoebox cages and are used to determine the pharmacokinetics of Naveglitazar, LY591026, and radioactivity. Blood samples are collected for plasma from mice via cardiac puncture at 0.5, 1, 2, 4, 8, 12, 24, 48, 72, 96, and 120 h postdose. Group 2 mice are housed in metabolism cages (n=3 per cage) for the collection of excreta to determine the mass balance and metabolism of Naveglitazar. Urine, feces, and cage wash are collected in 24 h intervals for up to 120 h. The third group of animals (n=3 per time point) are housed in shoebox cages and used to evaluate the metabolites present in plasma.
Rat[1]
Rats are divided into three groups. Group 1 animals (n=3 per time point) are housed in shoebox cages and are used to determine the pharmacokinetics of Naveglitazar, LY591026, and radioactivity. Blood samples are collected for plasma from rats via cardiac puncture at 0.5, 1, 2, 4, 8, 12, 24, 48, and 72 h postdose. Group 2 rats (n=4) are individually housed in metabolism cages for the collection of excreta to determine the mass balance and metabolism of Naveglitazar. Urine, feces, and cage wash are collected in 24 h intervals for up to 120 h. Group 3 animals, which are bile-cannulated rats (n=4), are individually housed in metabolism cages for the collection of excreta to determine the mass balance and metabolism of Naveglitazar. Urine, feces, and cage wash are collected in 24 h intervals for up to 72 h, whereas bile is collected in 8-h intervals. In a separate study, rats are given Naveglitazar or LY591026. In this study, blood samples for plasma are collected at 0.5, 1, 2, 4, 8, 12, and 24 h to determine pharmacokinetics of each analyte.

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

Keywords:

Naveglitazar476436-68-7LY519818LY 519818LY-519818PPARPeroxisome proliferator-activated receptorsInhibitorinhibitorinhibit

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