RG-12525

RG-12525 is a a specific, competitive and orally effective antagonist of the peptidoleukotrienes, LTC4, LTD4 and LTE4, inhibiting LTC4-, LTD4- and LTE4-inducd guinea pig parenchymal strips contractions, with IC50s of 2.6 nM, 2.5 nM and 7 nM, respectively; RG-12525 is also a peroxisome proliferator-activated receptor gamma (PPAR-gamma) agonist with IC50 of appr 60 nM and a potent inhibitor of CYP3A4, with a Ki value of 0.5 μM.

Product Specifications

CAS Number

[120128-20-3]

Product Name Alternative

NID 525

UNSPSC

12352005

Target

Cytochrome P450; Leukotriene Receptor; PPAR

Type

Reference compound

Related Pathways

Cell Cycle/DNA Damage; GPCR/G Protein; Metabolic Enzyme/Protease; Vitamin D Related/Nuclear Receptor

Applications

Metabolism-sugar/lipid metabolism

Field of Research

Metabolic Disease

Assay Protocol

https://www.medchemexpress.com/RG-12525.html

Purity

98.31

Solubility

DMSO : 25 mg/mL (ultrasonic)

Smiles

C1(COC2=CC=C(OCC3=CC=CC=C3CC4=NN=NN4)C=C2)=NC5=CC=CC=C5C=C1

Molecular Formula

C25H21N5O2

Molecular Weight

423.47

References & Citations

[1]Van Inwegen RG, et al. Antagonism of peptidoleukotrienes and inhibition of systemic anaphylaxis by RG 12525 in guinea pigs. Life Sci. 1989;44 (12) :799-807.|[2]Fayer JL, et al. Lack of correlation between in vitro inhibition of CYP3A-mediated metabolism by a PPAR-gamma agonist and its effect on the clinical pharmacokinetics of midazolam, an in vivo probe of CYP3A activity. J Clin Pharmacol. 2001 Mar;41 (3) :305-16.|[3]Carnathan GW, et al. The effect of RG 12525 on leukotriene D4-mediated pulmonary responses in guinea pigs. Agents Actions. 1989 Jun;27 (3-4) :316-8.