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SQ28603(SQ28,603)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
SQ28603(SQ28,603)图片
CAS NO:100845-83-8
规格:98%
分子量:267.34
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议
20mg电议

产品介绍
SQ28603是一种有效的选择性中性内肽酶3.4.24.11(NEP)抑制剂。
CAS:100845-83-8
分子式:C13H17NO3S
分子量:267.34
纯度:98%
存储:Store at -20°C

Background:

SQ28603 is a potent and selective inhibitor of neutral endopeptidase 3.4.24.11 (NEP), an enzyme that degrades atrial natriuretic peptide (ANP).



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[1]. 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[2].


[1]. Seymour AA, et al. Antihypertensive and renal activity of SQ 28,603, an inhibitor of neutral endopeptidase. J Cardiovasc Pharmacol. 1991 Feb;17(2):296-304. [2]. Seymour AA, et al. Evaluation of SQ 28,603, an inhibitor of neutral endopeptidase, in conscious monkeys. Can J Physiol Pharmacol. 1991 Oct;69(10):1609-17.