RG-12525 is a PPAR-gamma agonist (IC50: appr 60 nM) and a potent inhibitor of CYP3A4 (Ki: 0.5 μM). RG-12525 is a specific and competitive antagonist of the peptidoleukotrienes, LTC4, LTD4, and LTE4, inhibiting LTC4-, LTD4- and LTE4-induced guinea pig parenchymal strips contractions (IC50s: 2.6 nM, 2.5 nM, and 7 nM, respectively).

RG 12525 competitively suppresses 3H-LTD4 binding to lung membranes (Ki = 3.0 /- 0.3 nM) and competitively antagonizes the spasmogenic activity of LTC4, LTD4 and LTE4 on lung strips (KB values = 3 nM) with greater than 8000 fold selectivity. RG 12525 (25 μM) induces a substantial amount of inhibition at the 5 and 10 μM midazolam concentrations. RG 12525 (2.5 μM or 25 μM) suppresses the microsomal activity of CYP2C9 and -3A4, but does not significantly inhibit CYP1A2,-2A6, -2C19, or -2D6 [1][2].

RG 12525 inhibits antigen-induced mortality in the systemic anaphylaxis model (ED50 (95% confidence interval) = 2.2 (0.8-6.4) mg/kg). RG 12525 inhibits LTD4 induced wheal formation (ED50 = 5 mg/kg and a t1/2 = 10 hrs at 9 mg/kg), LTD4 induces bronchoconstriction (ED50 = 0.6 mg/kg), and anaphylactic death (ED50 = 2.2 mg/kg and a t1/2 = 7 hrs at 10 mg/kg) and antigen induces bronchoconstriction (ED50 = 0.6 mg/kg). RG 12525 also protects against LTD4-induced bronchoconstriction in a model measuring changes in pulmonary function (ED50 = 0.6 (0.4-1.0) mg/kg)[1][3].

120128-20-3

C25H21N5O2

423.47

NID 525;RG-12525

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years