Ramiprilat
CAS No. : 87269-97-4
(Synonyms: HOE 498 diacid; Ramipril diacid)
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| Cat. No. : | HY-A0115 |
| M.Wt: | 388.46 |
| Formula: | C21H28N2O5 |
| Purity: | >98 % |
| Solubility: | DMSO : 125 mg/mL (ultrasonic) |
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].
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].
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