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100845-83-8

中文名稱 100845-83-8
英文名稱 SQ 28603
CAS 100845-83-8
分子式 C13H17NO3S
分子量 267.34
MOL 文件 100845-83-8.mol
100845-83-8 結(jié)構(gòu)式 100845-83-8 結(jié)構(gòu)式

基本信息

中文別名
化合物 T12994
英文別名
SQ 28603
Squibb 28603
3-[(2-benzyl-3-sulfanylpropanoyl)amino]propanoic acid
N-[2-(Mercaptomethyl)-1-oxo-3-phenylpropyl]-β-alanine
β-Alanine, N-[2-(mercaptomethyl)-1-oxo-3-phenylpropyl]-
3-[[2-(Mercaptomethyl)-1-oxo-3-phenylpropyl]amino]propanoic acid

物理化學(xué)性質(zhì)

沸點(diǎn)533.3±50.0 °C(Predicted)
密度1.216±0.06 g/cm3(Predicted)
儲(chǔ)存條件-20°C儲(chǔ)存
溶解度溶于二甲基亞砜
酸度系數(shù)(pKa)4.32±0.10(Predicted)

常見問題列表

生物活性
SQ28603 是一種有效的選擇性中性內(nèi)肽酶 3.4.24.11 (NEP) 抑制劑。
靶點(diǎn)

NEP

體內(nèi)研究

In conscious deoxycorticosterone acetate (DOCA)/salt hypertensive rats, 300 μmol/kg, i.v., of SQ28603 significantly lowers mean arterial pressure (MAP) from 177±12 to 154±8 mm Hg and increases urinary cyclic guanosine monophosphate (GMP) excretion from 204±70 to 1,068±326 pmol/kg/min within 2 h. SQ28603 also significantly reduces NEP activity by 95% in the kidneys (1.28±0.08 vs. 18.35±0.61 μmol/min after SQ28603 and vehicle respectively) and by 77% in the lungs (0.29±0.03 vs. 0.92±0.14 μmol/kg after SQ28603 and vehicle, respectively). In conclusion, inhibition of NEP activity by SQ28603 significantly decreases MAP and increases plasma ANP concentrations and urinary excretion of cyclic GMP in conscious DOCA/salt hypertensive rats. The potent neutral endopeptidase inhibitor SQ28603 significantly increases excretion of sodium from 4.9±2.3 to 14.3±2.1 muequiv./min and cyclic 3',5'-guanosine monophosphate from 118±13 to 179±18 pmol/min after intravenous administration of 300 μmol/kg (approximately 80 mg/kg) in conscious female cynomolgus monkeys.

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