120128-20-3
基本信息
RG 12525
2-[4-[2-(1H-Tetrazol-5-ylmethyl)benzyloxy]phenoxymethyl]quinoline
Quinoline, 2-[[4-[[2-(2H-tetrazol-5-ylmethyl)phenyl]methoxy]phenoxy]methyl]-
物理化学性质
| 沸点 | 667.0±65.0 °C(Predicted) |
| 密度 | 1.308±0.06 g/cm3(Predicted) |
| 储存条件 | -20°C储存 |
| 溶解度 | 溶于二甲基亚砜 |
| 酸度系数(pKa) | 4.72±0.10(Predicted) |
| 形态 | Solid |
| 颜色 | White to yellow |
常见问题列表
|
LTD 4 2.5 nM (IC 50 , Guinea pig) |
LTC 4 2.6 nM (IC 50 , Guinea pig) |
LTE 4 7 nM (IC 50 , Guinea pig) |
PPARγ 60 nM (IC 50 ) |
CYP3A4 0.5 μM (Ki) |
RG 12525 competitively inhibits 3 H-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.
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.