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 and 1000 nM; 72 h) relieves high glucose (22.2 mM) mediated inhibition of human aortic endothelial cells (HAECs) proliferation with dose-dependent manner. Temocaprilat inhibits oxidative stress induced by high glucose in HAECs^[1].
Temocaprilat (1 µM; 10 min) increases protein kinase C (PKC) activity in HAECs^[1].
Temocaprilat (0.1 µM) inhibits IL-1β induced IL-6 expression by reducing the stability of IL-6 mRNA^[4].

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

Temocaprilat (1 mg/kg/d; i.v.; 4 weeks) significantly reduces systolic blood pressure with time-dependent manner in spontaneously hypertensive (SHR) rats. Temocaprilat improves myocardial fibrosis and oxidative stress in Wistar-Kyoto (WKY) rats and SHR rats^[3].

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

448.56

C₂₁H₂₄N₂O₅S₂

110221-53-9

OC(CN1C[C@@H](C2=CC=CS2)SC[C@@H](C1=O)N[C@H](C(O)=O)CCC3=CC=CC=C3)=O

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.