SA-898(SA-898) - 药物靶点：PREP_专利_临床

概要

基本信息

药物类型

小分子化药

别名

靶点

PREP

作用机制

PREP抑制剂(脯氨酰内肽酶抑制剂)

治疗领域

心血管疾病

在研适应症-

非在研适应症

高血压

原研机构

Santen Pharmaceutical Co., Ltd.

在研机构-

非在研机构

Santen Pharmaceutical Co., Ltd.

最高研发阶段无进展药物发现

首次获批日期-

最高研发阶段(中国)-

特殊审评-

结构

分子式C22H24N2O5S2

InChIKeySXLBNSMQRDQASV-XGHQBKJUSA-N

CAS号81018-05-5

关联

100 项与 SA-898 相关的临床结果

登录后查看更多信息

100 项与 SA-898 相关的转化医学

登录后查看更多信息

100 项与 SA-898 相关的专利（医药）

登录后查看更多信息

1

项与 SA-898 相关的文献（医药）

1996-01-01·Journal of Enzyme Inhibition

A Novel Synthetic Inhibitor of Endopeptidase

Article

作者: Shiro Mita ; Qiulin Li ; Susumu Ito ; Yuko Ukai

A novel synthetic inhibitor of endopeptidase-24.15 (EP-24.15, EC 3.4.24.15), N-[(2R,4R)-2-(2-hydroxyphenyl)-3-(3-mercaptopropionyl)-4-thiazolidine carbonyl] -L-phenylalanine (SA898) is described. This compound inhibited rat EP-24.15 competitively with an IC50 of 23 nM and Ki of 9.1 nM. These values were, respectively, 9.6 times and 6.3 times smaller than those for N-(1-carboxy-3-phenylpropyl)-alanyl-alanyl-phenylalanyl-p-aminobenzoate (cFP-AAF-pAB), which was one of the most potent inhibitors thus far reported. The inhibitory effect of SA898 on other endopeptidases, angiotensin converting enzyme (ACE, EC 3.4.15.1) and endopeptidase-24.11 (EP-24.11, EC 3.4.24.11) was also studied. SA898 inhibited ACE significantly, but the potency was about 20-fold lower than that for EP-24.15 in terms of the Ki value. The inhibitory effect of SA898 on EP-24.11 was almost negligible (Ki = 28 microM). In addition, the inhibitory activities of several SA898-related compounds were examined. Based on these data, the structure-activity relationships for EP-24.15 inhibitors are discussed.

100 项与 SA-898 相关的药物交易

登录后查看更多信息