84680-54-6
Enalaprilat Dihydrate
CAS: 84680-54-6
Molecular Formula: C18H26N2O6
84680-54-6 - Names and Identifiers
84680-54-6 - Physico-chemical Properties
| Molecular Formula | C18H26N2O6 |
| Molar Mass | 366.41 |
| Melting Point | 151-159°C |
| Specific Rotation(α) | [α]D25 -53.0～-56.0゜ (c=1, CH3OH) (Calculated on dehydrous basis) |
| Solubility | Soluble in water (5 mg/ml at 25 °C), ethanol (1 mg/ml at 25 °C), DMSO (70 mg/ml |
| Appearance | neat |
| Color | White to Off-White |
| Storage Condition | 2-8°C |
| Use | An active metabolite of the ACE inhibitor, Enalapril. |
| In vitro study | Enalaprilat is a divalent acid metabolite of Enalapril and has no biological activity orally and must be treated intravenously. HEK 293 cells expressing B1R-YFP did not respond to Enalaprilat-activated phospholipase A2, but responded strongly to Lys-des-Arg9-BK. Radiolabeled Enalaprilat does not bind to cells expressing recombinant human B1R, but binds with high specificity to human umbilical vein endothelial cells recombinant ACE (0.25-10 nM) or normal expression of ACE (KD = 0.23 nM). Enalaprilat acts on HEK 293a cells expressing B1Rs and does not stimulate the calcium signaling pathway. In vitro studies have shown that Enalaprilat effectively inhibits brain ACE, whereas enalapril has a weak inhibitory effect. |
| In vivo study | Enalaprila acts on spontaneously hypertensive rats and produces significant ACE inhibitory effects on tissues (serum, kidney, brain, and aorta). In vivo, the absorption of the active metabolite Enalaprilat in serum results in enalapril inhibiting aortic ACE activity. Enalaprilat activates the B1 receptor and stimulates NO production in the kidney, promoting vasodilation. |
84680-54-6 - Risk and Safety
| WGK Germany | 3 |
| RTECS | TW3590600 |
| HS Code | 2933995300 |
84680-54-6 - Introduction
Enalaprilat Dihydrate is a new angiotensin converting enzyme (ACE) inhibitor with IC50 of 1.2 nM.
Last Update：2022-10-16 17:41:50
84680-54-6 - Reference Information
| biological activity | Enalaprilat (MK-422) is a novel vascular Nervousness peptide converting enzyme (ACE) inhibitor, the IC50 was 1.2 nM. Active metabolite of enalapril. Enalapril EP impurity C (dihydrate). |
| Target | TargetValue ACE 1.94 nM |
| Target | Value |
| ACE | 1.94 nM |
| in vitro study | Enalaprilat is a divalent acid metabolite of Enalapril, which is biologically inactive orally and must be treated intravenously. HEK 293 cells expressing B1R-YFP did not respond to Enalaprilat-activated phospholipase A2, but responded strongly to Lys-des-Arg9-BK. Radiolabeled Enalaprilat does not bind to cells expressing recombinant human B1R, but binds with high specificity to human umbilical vein endothelial cells recombinant ACE (0.25-10 nM) or normal expression of ACE (KD = 0.23 nM). Enalaprilat acts on HEK 293a cells expressing B1Rs and does not stimulate the calcium signaling pathway. In vitro studies have shown that Enalaprilat effectively inhibits brain ACE, whereas enalapril has a weak inhibitory effect. |
| in vivo study | Enalaprila acts on tissues (serum, kidney, brain, and aorta) in spontaneously hypertensive rats A significant ACE inhibitory effect was produced. In vivo, the absorption of the active metabolite Enalaprilat in serum results in enalapril inhibiting aortic ACE activity. Enalaprilat activates the B1 receptor and stimulates NO production in the kidney, promoting vasodilation. |
| EPA chemical substance information | information is provided by: ofmpeb.epa.gov (external link) |
Last Update：2024-04-09 21:01:54
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Product Name: Enalaprilat Dihydrate Visit Supplier Webpage Request for quotationCAS: 84680-54-6
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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