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MedChemExpressModel Ramiprilat -87269-97-4

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Ramiprilat (HOE 498 diacid), an active metabolite of Ramipril, is a potent and orally active angiotensin converting enzyme (ACE) inhibitor with a Ki value of 7 pM. Ramiprilat has acute antlhypertensive effect. Ramiprilat can be used for high blood pressure and heart failure research[1][2][3][4][5].
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Ramiprilat

MCE China:Ramiprilat

Brand:MedChemExpress (MCE)

Cat. No.HY-A0115

CAS:87269-97-4

Synonyms:HOE 498 diacid; Ramipril diacid

Purity:97.09%

Storage:Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month

Shipping:Room temperature in continental US; may vary elsewhere.

Description:Ramiprilat (HOE 498 diacid), an active metabolite of Ramipril, is a potent and orally active angiotensin converting enzyme (ACE) inhibitor with a Ki value of 7 pM. Ramiprilat has acute antlhypertensive effect. Ramiprilat can be used for high blood pressure and heart failure research.

In Vitro:Ramiprilat (0.1, 1 μM, 0-30 min) induces cyclic GMP increase in endothelial cells[2]. Ramiprilat (0.3 μM, 15 min) elicits a significant nitric oxide release and an increase in prostaglandin I2 (PGI2) release in endothelial cells[2].

In Vivo:Ramiprilat (2 mg/kg, i.v., a single dose for 60 min) decreases the blood pressure of spontaneously hypertensive rats[5]. Pharmacokinetic-pharmacodynamic parameters (mean±SD) for Ramiprilat after different IV and PO ramipril doses[4] Parameters IV (0.05 mg/kg) PO (0.40 mg/kg) PO (0.80 mg/kg) k10 (1/h) 5.09 5.49 4.10 t1/2 k10 (h) 0.16 (0.09-0.31) 0.13 (0.10-0.16) 0.17 (0.10-0.27) Vc (L/kg) 0.15 Vc/F (L/kg) 2.35 1.97 Cl (L/kg/h) 0.77 Cl/F (L/kg/h) 12.82 7.79 F (%) 6.52 9.08 Kd (nmol/L) 1.35 1.47 1.19 fcirc (%) 5.01 5.80 6.08 Bmax (nmol/L) 109.46 79.31 91.72 Pmax (nmol/L) 5.27 4.60 5.08 IC50 (nmol/L) 1.05 1.07 0.88

IC50 & Target:Ki: 7 pM (ACE)[1] In Vitro Ramiprilat (0.1, 1 μM, 0-30 min) induces cyclic GMP increase in endothelial cells[2]. Ramiprilat (0.3 μM, 15 min) elicits a significant nitric oxide release and an increase in prostaglandin I2 (PGI2) release in endothelial cells[2]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> Ramiprilat Related Antibodies

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References:

[1]. Ramiprilat (HOE 498 diacid), an active metabolite of Ramipril, is a potent and orally active angiotensin converting enzyme (ACE) inhibitor with a Ki value of 7 pM. Ramiprilat can be used for high blood pressure and heart failure research[1].  [Content Brief]

[2]. Wiemer G, et al. Ramiprilat enhances endothelial autacoid formation by inhibiting breakdown of endothelium-derived bradykinin. Hypertension. 1991 Oct;18(4):558-63.  [Content Brief]

[3]. Wall TM, et al. Ramiprilat attenuates hypoxia/reoxygenation injury to cardiac myocytes via a bradykinin-dependent mechanism. Eur J Pharmacol. 1996 Jun 13;306(1-3):165-74.  [Content Brief]

[4]. Serrano-Rodríguez JM, et al. Pharmacokinetics and pharmacodynamics of ramipril and ramiprilat after intravenous and oral doses of ramipril in healthy horses. Vet J. 2016 Feb;208:38-43.  [Content Brief]

[5]. Cachofeiro V, et al. Kinins, nitric oxide, and the hypotensive effect of captopril and ramiprilat in hypertension. Hypertension. 1992 Feb;19(2):138-45.  [Content Brief]

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