Naveglitazar racemate free base

Naveglitazar racemate (LY519818 racemate) is the racemate of Naveglitazar.

For research use only. Not for human or veterinary use.

Target PPAR

Research area Metabolic Disease

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Data Sheet SDS COA

Naveglitazar racemate structure

CAS No.: 916085-47-7

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
25 mg	USD 1,480.00	BP-02215-25mg	In stock	Get quote
50 mg	USD 2,360.00	BP-02215-50mg	In stock	Get quote
100 mg	USD 3,780.00	BP-02215-100mg	In stock	Get quote
250 mg	Inquire	BP-02215-250mg	In stock	Inquire

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Description

Naveglitazar racemate (LY519818 racemate) is the racemate of Naveglitazar. Naveglitazar is a nonthiozolidinedione peroxisome proliferator-activated receptor (PPAR) α-γ dual, γ-dominant agonist that has shown glucose-lowering potential in animal models[1].

Biological activity

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. 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.

Identifiers

SMILES: O=C(O)C(OC)CC1=CC=C(OCCCOC2=CC=C(OC3=CC=CC=C3)C=C2)C=C1
InChIKey: OKJHGOPITGTTIM-UHFFFAOYSA-N

Specifications

MW (average): 422.4703
Formula: C₂₅H₂₆O₆
CAS No.: 916085-47-7
Physical state: Solid
Color: off-white to yellow
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder 4℃ 2 years; In solvent -20℃ 1 month;

Solubility

soluble in DMSO

Documents

References

[1]. Yi P, et al. The disposition and metabolism of naveglitazar, a peroxisome proliferator-activated receptor alpha-gamma dual, gamma-dominant agonist in mice, rats, and monkeys. Drug Metab Dispos. 2007 Jan;35(1):51-61.

Same target

Search PPAR

Same research area

Search Metabolic Disease