Ramipril-d4
Ramipril-d4 is deuterated labeled Ramipril (HY-B0279). Ramipril (HOE-498) is an angiotensin-converting enzyme (ACE) inhibitor with IC50 of 5 nM.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 1132661-83-6
- 分子式: C23H28D4N2O5
- 分子量:420.54
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].
Ramipril (HOE-498) is an angiotensin-converting enzyme (ACE) inhibitor with IC50 of 5 nM[2]. Ramipril (HOE-498) enhances the activity of ACE-associated CK2 and the phosphorylation of ACE Ser1270 in cultured endothelial cells, but is unable to activate JNK or stimulate the nuclear accumulation of c-Jun in endothelial cells expressing a S1270A ACE mutant or in ACE-deficient cells. Prolonged Ramipril treatment increases ACE expression in primary cultures of human endothelial cells and in vivo (mouse lung), which can be prevented by pretreatment with the JNK inhibitor SP600125[3].
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.
1. This compound can be used as a tracer
2. This compound can be used as an internal standard for quantitative analysis by NMR, GC-MS, or LC-MS.
化学情報
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CAS 番号 1132661-83-6
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非標識Cas 87333-19-5
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分子量 420.54
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分子式 C23H28D4N2O5
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SMILES
CCOC([C@H](CCC1=CC=CC=C1)N[C@@]([2H])(C([2H])([2H])[2H])C(N2[C@]3([H])[C@](CCC3)([H])C[C@H]2C(O)=O)=O)=O
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別名
HOE-498-d4
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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
参考文献
[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53(2):211-216. [Content Brief]
[2]. Raasch, W., et al., Combined blockade of AT1-receptors and ACE synergistically potentiates antihypertensive effects in SHR. J Hypertens, 2004. 22(3): p. 611-8. [Content Brief]
[3]. Stevens, B.R., M.I. Phillips, and A. Fernandez, Ramipril inhibition of rabbit (Oryctolagus cuniculus) small intestinal brush border membrane angiotensin converting enzyme. Comp Biochem Physiol C, 1988. 91(2): p. 493-7. [Content Brief]
[4]. Kohlstedt, K., et al., Angiotensin-converting enzyme is involved in outside-in signaling in endothelial cells. Circ Res, 2004. 94(1): p. 60-7. [Content Brief]
[5]. Ceconi, C., et al., Differences in the effect of angiotensin-converting enzyme inhibitors on the rate of endothelial cell apoptosis: in vitro and in vivo studies. Cardiovasc Drugs Ther, 2007. 21(6): p. 423-9. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)