RG-12525 (NID 525) (Synonyms: NID 525) |
| Catalog No.GC33780 |
RG-12525 (NID 525) est un antagoniste spécifique, compétitif et efficace par voie orale des peptidoleucotriènes, LTC4, LTD4 et LTE4, inhibant les contractions des bandes parenchymateuses de cobaye induites par LTC4, LTD4 et LTE4, avec des IC50 de 2,6 nM, 2,5 nM et 7 nM, respectivement; RG-12525 (NID 525) est également un agoniste du récepteur gamma activé par les proliférateurs de peroxysomes (PPAR-gamma) avec une IC50 d'environ 60 nM et un puissant inhibiteur du CYP3A4, avec une valeur Ki de 0,5 μM.
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Cas No.: 120128-20-3
Sample solution is provided at 25 µL, 10mM.
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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.
RG 12525 competitively inhibits 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[1]. RG 12525 (2.5 µM or 25 µM) inhibits the microsomal activity of CYP2C9 and -3A4, but does not significantly inhibit CYP1A2,-2A6, -2C19, or -2D6. RG 12525 (25 µM) also causes a substantial amount of inhibition at the 5 and 10 µM midazolam concentrations[2].
RG 12525 orally inhibits LTD4 induced wheal formation (ED50 = 5 mg/kg with 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 with a t1/2 = 7 hrs at 10 mg/kg) and antigen induces bronchoconstriction (ED50 = 0.6 mg/kg)[1]. RG 12525 inhibits antigen-induced mortality in the systemic anaphylaxis model with an ED50 (95% confidence interval) = 2.2 (0.8-6.4) mg/kg. RG 12525 also protects against LTD4-induced bronchoconstriction in a model measuring changes in pulmonary function with an ED50 = 0.6 (0.4-1.0) mg/kg[3].
[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.
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