Temocaprilat  (Synonyms: Temocapril diacid; Temocaprilate; RS 5139)

Temocaprilat (Temocapril diacid) is an inhibitor of angiotensin-converting enzyme (ACE). Temocaprilat alleviates the inhibitory effect of high glucose on the proliferation of aortic endothelial cells. Temocaprilat has potential applications in hypertension and vascular inflammation^[1][2][3][4].

Temocaprilat (1、10、100 和 1000 nM；72 h) 以剂量依赖性方式缓解了高糖 (22.2 mM) 介导的人主动脉内皮细胞 (HAECs) 增殖抑制。Temocaprilat 在 HAECs 中抑制高糖诱导的氧化应激^[1]。
Temocaprilat (1 µM；10 min) 在 HAECs 中增加了蛋白激酶 C (PKC) 活性^[1]。
Temocaprilat (0.1 µM) 通过降低 IL-6 mRNA 的稳定性抑制 IL-1β 诱导的 IL-6 表达^[4]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Temocaprilat (1 mg/kg/d；静脉注射；4 周) 在自发性高血压大鼠 (SHRs) 中，以时间依赖性方式显著降低了收缩压。Temocaprilat 改善了 Wistar-Kyoto (WKY) 小鼠和 SHR 小鼠的心肌纤维化及氧化应激^[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

448.56

C₂₁H₂₄N₂O₅S₂

110221-53-9

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Yasunari K, et al. Converting enzyme inhibitor temocaprilat prevents high glucose-mediated suppression of human aortic endothelial cell proliferation. J Cardiovasc Pharmacol. 2003 Dec;42 Suppl 1:S55-60.  [Content Brief]

  [2]. Püchler K, et al. Single dose and steady state pharmacokinetics of temocapril and temocaprilat in young and elderly hypertensive patients. Br J Clin Pharmacol. 1998 Oct;46(4):363-7.  [Content Brief]

  [3]. Ito N, et al. Renin-angiotensin inhibition reverses advanced cardiac remodeling in aging spontaneously hypertensive rats. Am J Hypertens. 2007 Jul;20(7):792-9.  [Content Brief]

  [4]. Yang Z H, et al. P-540: Olmesartan and temocaprilat suppress IL-1 [beta]-induced IL-6 expression via a decrease in mRNA stability in vascular smooth muscle cells[J]. American Journal of Hypertension, 2002, 15(S3): 228A.