L-765314
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- CAS号:
- 189349-50-6
- 英文名:
- L-765,314
- 英文别名:
- Adrenergic Receptor,L-765314,Inhibitor,Beta Receptor,L765314,inhibit,L 765314;Benzyl (S)-4-(4-amino-6,7-dimethoxyquinazolin-2-yl)-2-(tert-butylcarbamoyl)piperazine-1-carboxylate;1-Piperazinecarboxylic acid, 4-(4-amino-6,7-dimethoxy-2-quinazolinyl)-2-[[(1,1-dimethylethyl)amino]carbonyl]-, phenylmethyl ester, (S)-;1-Piperazinecarboxylic acid, 4-(4-amino-6,7-dimethoxy-2-quinazolinyl)-2-[[(1,1-dimethylethyl)amino]carbonyl]-, phenylmethyl ester, (2S)-
- 中文名:
- L-765314
- 中文别名:
- 化合物L-765314;(S)-4-(4-氨基-6,7-二甲氧基喹唑啉-2-基)-2-(叔丁基氨基甲酰基)哌嗪-1-甲酸苄酯;(2S)-4-(4-氨基-6,7-二甲氧基-2-喹唑啉基)-2-[[(1,1-二甲基乙基)氨基]羰基]-1-哌嗪甲酸苯甲酯
- CBNumber:
- CB22642473
- 分子式:
- C27H34N6O5
- 分子量:
- 522.6
- MOL File:
- 189349-50-6.mol
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L-765314化学性质
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密度:
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1.269±0.06 g/cm3(Predicted)
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储存条件:
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2-8°C(protect from light)
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溶解度:
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DMSO:75.0(Max Conc. mg/mL);143.51(Max Conc. mM)
Ethanol:100.0(Max Conc. mg/mL);191.35(Max Conc. mM)-
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酸度系数(pKa):
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14.99±0.20(Predicted)
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形态:
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Solid
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颜色:
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White to off-white
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L-765314性质、用途与生产工艺
L-765314 是 α1b 肾上腺素能受体 (α1b adrenergic receptor) 的一个有效的、选择性拮抗剂，其在大鼠和人体中的 Ki 值分别为 5.4 nM 和 2.0 nM。
Ki: 5.4±0.6 nM (rat α1b receptor ), 2.0±0.66 nM (human α1b receptor), 50±8 nM (rat α1d receptor), 34±6 nM (human α1d receptor), 500±20 nM (rat α1b receptor ), 420±62 nM (human α1b receptor).
L-765314 exhibits two displacement sites. The high-affinity site accounts for approximately 25% of binding (IC
50
) 1.90 nM and represents binding to the R1b sites. The low-affinity site accounts for the residual 75% of binding (IC
50
) 790 nM and represents binding to the R1a sites.
The results of plasma assayed by liquid chromatograph/mass spectrometer (LCMS) show that the mean C
max
of L-765314 (A322312) is 1.05 μM and the t
1/2
is 0.5 h. L-765314 shows weak potency for inhibiting the pressor response to either phenylephrine or A-61603 (AD
25
>3 mg/kg for each). On the basis of the inhibition of pressor responses to the R1a subtype selective agonist A-61603, L-765314 appears to be selective versus the R1a receptor up to a dose of 0.3 mg/kg. The results of hypotensive potency in rats show that both L-765314 and terazosin tend to decrease heart rate (about 25 bpm at 1 mg/kg iv).
L-765314
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 |
|---|
| 2024/11/08 | S0862 | L-765314
L-765314 | 189349-50-6 | 5mg | 1220.31元 |
| 2024/11/08 | S0862 | L-765314
L-765314 | 189349-50-6 | 25mg | 3660.93元 |
189349-50-6, L-765314 相关搜索:
- 抑制剂
- 化合物L-765314
- (S)-4-(4-氨基-6,7-二甲氧基喹唑啉-2-基)-2-(叔丁基氨基甲酰基)哌嗪-1-甲酸苄酯
- (2S)-4-(4-氨基-6,7-二甲氧基-2-喹唑啉基)-2-[[(1,1-二甲基乙基)氨基]羰基]-1-哌嗪甲酸苯甲酯
- 189349-50-6
- Adrenergic Receptor,L-765314,Inhibitor,Beta Receptor,L765314,inhibit,L 765314
- Benzyl (S)-4-(4-amino-6,7-dimethoxyquinazolin-2-yl)-2-(tert-butylcarbamoyl)piperazine-1-carboxylate
- 1-Piperazinecarboxylic acid, 4-(4-amino-6,7-dimethoxy-2-quinazolinyl)-2-[[(1,1-dimethylethyl)amino]carbonyl]-, phenylmethyl ester, (2S)-
- 1-Piperazinecarboxylic acid, 4-(4-amino-6,7-dimethoxy-2-quinazolinyl)-2-[[(1,1-dimethylethyl)amino]carbonyl]-, phenylmethyl ester, (S)-