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RG-12525

CAS No. : 120128-20-3

MCE 国际站：RG-12525

产品活性：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。

研究领域：GPCR/G Protein  |  Vitamin D Related/Nuclear Receptor  |  Cell Cycle/DNA Damage  |  Metabolic Enzyme/Protease

作用靶点：Leukotriene Receptor  |  PPAR  |  Cytochrome P450

In Vitro: RG 12525 competitively inhibits ³H-LTD4 binding to lung membranes (K_i = 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.

In Vivo: RG 12525 orally inhibits LTD4 induced wheal formation (ED₅₀ = 5 mg/kg with a t_1/2 = 10 hrs at 9 mg/kg), LTD4 induces bronchoconstriction (ED₅₀ = 0.6 mg/kg), and anaphylactic death (ED₅₀ = 2.2 mg/kg with a t_1/2 = 7 hrs at 10 mg/kg) and antigen induces bronchoconstriction (ED₅₀ = 0.6 mg/kg). 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.

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