120128-20-3
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- CAS号:
- 120128-20-3
- 英文名:
- RG 12525
- 英文别名:
- NID 525;RG 12525;RG 12525,RG12525;2-[4-[2-(1H-Tetrazol-5-ylmethyl)benzyloxy]phenoxymethyl]quinoline;Quinoline, 2-[[4-[[2-(2H-tetrazol-5-ylmethyl)phenyl]methoxy]phenoxy]methyl]-
- 中文名:
- 120128-20-3
- 中文别名:
- 化合物 T16739
- CBNumber:
- CB31392943
- 分子式:
- C25H21N5O2
- 分子量:
- 423.47
- MOL File:
- 120128-20-3.mol
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120128-20-3化学性质
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沸点:
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667.0±65.0 °C(Predicted)
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密度:
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1.308±0.06 g/cm3(Predicted)
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储存条件:
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Store at -20°C
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溶解度:
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Soluble in DMSO
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形态:
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Solid
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酸度系数(pKa):
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4.72±0.10(Predicted)
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颜色:
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White to yellow
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120128-20-3性质、用途与生产工艺
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。
LTD
4
2.5 nM (IC
50
, Guinea pig)
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LTC
4
2.6 nM (IC
50
, Guinea pig)
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LTE
4
7 nM (IC
50
, Guinea pig)
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PPARγ
60 nM (IC
50
)
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CYP3A4
0.5 μM (Ki)
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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.
120128-20-3
上下游产品信息
上游原料
下游产品
更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
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2024/04/30 | HY-101676 | RG-12525 | | 1 mg | 1590元 |
2024/04/30 | HY-101676 | 120128-20-3 RG-12525 | 120128-20-3 | 5mg | 3500元 |
120128-20-3, 120128-20-3 相关搜索:
- 化合物 T16739
- 120128-20-3
- RG 12525,RG12525
- Quinoline, 2-[[4-[[2-(2H-tetrazol-5-ylmethyl)phenyl]methoxy]phenoxy]methyl]-
- NID 525
- 2-[4-[2-(1H-Tetrazol-5-ylmethyl)benzyloxy]phenoxymethyl]quinoline
- RG 12525