1. Temocaprilat

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

Cat. No.: HY-A0117
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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.

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Temocaprilat Chemical Structure

Temocaprilat Chemical Structure

CAS No. : 110221-53-9

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Description

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].

In Vitro

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.

In Vivo

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.

Animal Model: Six 10-week-old WKYs and SHRs and six 50-week-old (aging control) SHRs[3].
Dosage: 1 mg/kg/d.
Administration: Intravenous injection; 4 weeks.
Result: Reduced the expression levels of myocardial fibrosis, transforming growth factor-β1 (TGF-β1) mRNA and fibroblast growth factor-2 (FGF-2) mRNA in the left ventricle (LV).
Weakened the expression levels of 8-isoprostane, p22phox mRNA, p47phox mRNA and gp91phox mRNA in LV.
Molecular Weight

448.56

Formula

C21H24N2O5S2

CAS No.
SMILES

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

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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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