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RG-12525 (NID 525) (Synonyms: NID 525)

Katalog-Nr.GC33780

RG-12525 (NID 525) ist ein spezifischer, kompetitiver und oral wirksamer Antagonist der Peptidoleukotriene LTC4, LTD4 und LTE4, der LTC4-, LTD4- und LTE4-induzierte Parenchymstreifenkontraktionen von Meerschweinchen mit IC50-Werten von 2,6 nM, 2,5 nM hemmt bzw. 7 nM; RG-12525 (NID 525) ist auch ein Peroxisom-Proliferator-aktivierter Rezeptor-Gamma (PPAR-Gamma)-Agonist mit einem IC50 von ca. 60 nM und ein starker Inhibitor von CYP3A4 mit einem Ki-Wert von 0,5 μM.

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RG-12525 (NID 525) Chemische Struktur

Cas No.: 120128-20-3

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10mM (in 1mL DMSO)
347,00 $
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5mg
315,00 $
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10mg
522,00 $
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25mg
990,00 $
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50mg
1.530,00 $
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100mg
2.250,00 $
Auf Lager

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Sample solution is provided at 25 µL, 10mM.

Description Chemical Properties Product Documents Related Products

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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