Moexipril-d3
Moexipril-d3 is deuterated labeled Moexipril (HY-117281). Moexipril is an orally active inhibitor of angiotensin-converting enzyme (ACE), and becomes effective by being hydrolyzed to moexiprila hydrochloride. Moexipril exhibits antihypertensive and neuroprotective effects-.
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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。
- 分子式: C27H31D3N2O7
- 分子量:501.59
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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
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].
Moexipril is devoid of anti-inflammatory properties and has no effect on platelet function[3].
Moexipril hydrolyzes to Moexiprilat, and Moexiprilat inhibits ACE in guinea pig serum as well as on purified ACE from rabbit lung with IC50s of 2.6 nM and 4.9 nM, respectively[3].
Moexipril (0.01 nM-0.1 mM) exhibits high potency against both ACE in rats plasma and purified ACE from rabbit lung, with IC50s of 1.75 nM and 2.1 nM, respectively[4].
Moexipril (0-100 μM, 24 h) significantly reduced the percentage of damaged neurons in a dose-dependent manner[5].
Moexipril (0-100 μM, 24 h) significantly attenuates Fe2+/3+-induced neurotoxicity[5].
Moexipril dose not cause significant changes in the percentage of apoptotic neurons[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Moexipril (3 mg/kg, 30 mg/kg and 10 mg/kg; p.o.; once daily; 5 days) exhibits a dose-dependent and antihypertensive effects in renal hypertensive rats, spontaneously hypertensive rats and perinephritic hypertensive dogs, respectively[4].
Moexipril (0.3 mg/kg, i.p.) significantly reduces the infarct area on the mouse brain surface in NMRI mice[5].
Moexipril (0.1 mg/kg, i.p.) significantly attenuates the cortical infarct volume in Long-Evans rats[5].
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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非標識Cas 103775-10-6
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分子量 501.59
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分子式 C27H31D3N2O7
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SMILES
O=C([C@H]1N(C([C@@H](N[C@H](C(OCC)=O)CCC2=CC=CC=C2)C([2H])([2H])[2H])=O)CC3=C(C=C(OC)C(OC)=C3)C1)O
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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]. Chrysant, S.G. and G.S. Chrysant, Pharmacological and clinical profile of moexipril: a concise review. J Clin Pharmacol, 2004. 44(8): p. 827-36. [Content Brief]
[3]. Friehe H, et al. Pharmacological and toxicological studies of the new angiotensin converting enzyme inhibitor moexipril hydrochloride. Arzneimittelforschung. 1997 Feb. 47(2):132-44. [Content Brief]
[4]. Edling O, et al. Moexipril, a new angiotensin-converting enzyme (ACE) inhibitor: pharmacological characterization and comparison with enalapril. J Pharmacol Exp Ther. 1995 Nov;275(2):854-63. [Content Brief]
[5]. Ravati A, et al. Enalapril and moexipril protect from free radical-induced neuronal damage in vitro and reduce ischemic brain injury in mice and rats. Eur J Pharmacol. 1999 May 28;373(1):21-33. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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