120128-20-3

中文名称 120128-20-3

英文名称 RG 12525

CAS 120128-20-3

分子式 C25H21N5O2

分子量 423.47

MOL 文件 120128-20-3.mol

120128-20-3 结构式

基本信息物理化学性质常见问题列表

基本信息

中文别名

化合物 T16739

英文别名

NID 525
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

生物活性

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， Ki 值为 0.5 µM。

靶点

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)

体外研究

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.

体内研究

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.