Temocaprilat
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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- CAS No.: 110221-53-9
- Formule: C21H24N2O5S2
- Masse moléculaire:448.56
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Six 10-week-old WKYs and SHRs and six 50-week-old (aging control) SHRs[3].
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Dosage:1 mg/kg/d.
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Administration:Intravenous injection; 4 weeks.
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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.
Chemical Information
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CAS No. 110221-53-9
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Masse moléculaire 448.56
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Formule C21H24N2O5S2
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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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Synonyms
Temocapril diacid; Temocaprilate; RS 5139
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
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Fiche technique (275 KB)
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SDS (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
[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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Temocaprilat Related Classifications
HY-A0117 Related Classifications
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