Temocaprilat_product_DataBase

Bioactivity	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].
Invitro	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]。
In Vivo	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]。 Animal Model:
Name	Temocaprilat
CAS	110221-53-9
Formula	C21H24N2O5S2
Molar Mass	448.56
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[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. [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. [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. [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.

PeptideDB

Temocaprilat

CAS: 110221-53-9 F: C21H24N2O5S2 W: 448.56