Bioactivity | Enalkiren (A-64662) is a potent dipeptide renin inhibitor with an IC50 of 0.78 nM in a purified renal renin-angiotensinogen system (pH=6.0). Enalkiren suppresses renin activity, and also reduces systolic and diastolic blood pressure. Enalkiren can be used to research essential hypertension[1][2]. |
Target | IC50: 23 nM (hamster dipeptide renin), 14 nM (human dipeptide renin), 2.3 nM (cynomolgus monkey dipeptide renin) |
Invitro | Enalkiren inhibits the endogenous renin-angiotensinogen reaction with an IC50 value of 23 nM, 14 nM and 2.3 nM in hamster, human and cynomolgus monkey plasma, respectively, at pH 7.4[2]. |
In Vivo | Enalkiren (0.01-10 mg/kg; i.v.; single dosage) reduces mean arterial blood pressure in cynomolgus monkey[2]. Animal Model: |
Name | Enalkiren |
CAS | 113082-98-7 |
Formula | C35H56N6O6 |
Molar Mass | 656.86 |
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]. Boger RS, et al. Prolonged duration of blood pressure response to enalkiren, the novel dipeptide renin inhibitor, in essential hypertension. Hypertension. 1990 Jun;15(6 Pt 2):835-40. [2]. Kleinert, Hollis D., et al. Profile of the Renin Inhibitor, Enalkiren (ABBOTT‐64662). Cardiovascular Drug Reviews 8 (1990): 203-219. |