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 番号: 110221-53-9
- 分子式: C21H24N2O5S2
- 分子量:448.56
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
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.
化学情報
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CAS 番号 110221-53-9
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分子量 448.56
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分子式 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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別名
Temocapril diacid; Temocaprilate; RS 5139
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
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データシート (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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取扱説明書 (2659 KB)
参考文献
[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
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Temocaprilat 関連分類
HY-A0117 関連分類
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