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189349-50-6

中文名稱 L-765314
英文名稱 L-765,314
CAS 189349-50-6
分子式 C27H34N6O5
分子量 522.6
MOL 文件 189349-50-6.mol
更新日期 2025/01/22 01:54:33
189349-50-6 結(jié)構(gòu)式 189349-50-6 結(jié)構(gòu)式

基本信息

中文別名
(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
英文別名
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)-
所屬類別
生物化工:生化試劑

物理化學(xué)性質(zhì)

密度1.269±0.06 g/cm3(Predicted)
儲存條件Keep in dark place,Sealed in dry,2-8°C
溶解度DMSO:75.0(Max Conc. mg/mL);143.51(Max Conc. mM)
Ethanol:100.0(Max Conc. mg/mL);191.35(Max Conc. mM)
酸度系數(shù)(pKa)14.99±0.20(Predicted)
形態(tài)Solid
顏色White to off-white
L-765314價格(試劑級)
報價日期產(chǎn)品編號產(chǎn)品名稱CAS號包裝價格
2024/11/08S0862L-765314
L-765314
189349-50-65mg1220.31元
2024/11/08S0862L-765314
L-765314
189349-50-625mg3660.93元

常見問題列表

生物活性
L-765314 是 α1b 腎上腺素能受體 (α1b adrenergic receptor) 的一個有效的、選擇性拮抗劑,其在大鼠和人體中的 Ki 值分別為 5.4 nM 和 2.0 nM。
靶點

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).

體外研究

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.

體內(nèi)研究

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).

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