RG-12525 是一种特异性的，竞争性的，可口服的 LTC4，LTD4 和 LTE4 拮抗剂，能够抑制 LTC4，LTD4 和 LTE4 诱导的豚鼠薄壁带收缩，IC₅₀ 值分别为 2.6 nM，2.5 nM 和 7 nM；RG-12525 也是 PPAR-γ 的激动剂，IC₅₀ 值约为 60 nM，CYP3A4 的抑制剂， K_i 值为 0.5 µM。

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 IC 50 s 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 IC 50 of appr 60 nM and a potent inhibitor of CYP3A4, with a K i value of 0.5 μM.

Solid

PPARγ 60 nM (IC50) CYP3A4 0.5 μM (Ki)pa

RG 12525 competitively inhibits H-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 (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. has not independently confirmed the accuracy of these methods. They are for reference only.

RG 12525 orally inhibits LTD4 induced wheal formation (ED 50 = 5 mg/kg with a t 1/2 = 10 hrs at 9 mg/kg), LTD4 induces bronchoconstriction (ED 50 = 0.6 mg/kg), and anaphylactic death (ED 50 = 2.2 mg/kg with a t 1/2 = 7 hrs at 10 mg/kg) and antigen induces bronchoconstriction (ED 50 = 0.6 mg/kg). RG 12525 inhibits antigen-induced mortality in the systemic anaphylaxis model with an ED 50 (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 ED 50 = 0.6 (0.4-1.0) mg/kg. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[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

In Vitro: DMSO : 25 mg/mL (59.04 mM; Need ultrasonic)配制储备液