Bioactivity | Ramipril-d4 is deuterated labeled Ramipril (HY-B0279). Ramipril (HOE-498) is an angiotensin-converting enzyme (ACE) inhibitor with IC50 of 5 nM. |
Invitro | 氢、碳和其他元素的稳定重同位素已被纳入药物分子中,主要作为药物开发过程中定量的示踪剂。氘化引起了人们的关注,因为它可能影响药物的药代动力学和代谢谱[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> Ramipril-d4 相关抗体: |
In Vivo | Chronic in vivo administration of Ramipril (HOE-498) to rats at a dosage that has similar hypotensive effects in vitro HUVECs significantly reduces the rate of LPS-induced apoptosis compared to the other ACE inhibitors, which contrasts with the apoptosis effect in vitro[4]. Ramipril (HOE-498) inhibits systolic blood pressure (SBP) with IC50 of 1.97 mg/kg in spontaneously hypertensive rats (SHR). When in combination with AT1-receptor blockade by candesartan-cilexetil increases SBP reduction synergistically rather than additively[5]. MCE has not independently confirmed the accuracy of these methods. They are for reference only. |
CAS | 1132661-83-6 |
Formula | C23H28D4N2O5 |
Molar Mass | 420.54 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53(2):211-216. [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. [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. [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. [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. |