Nesiritide acetate is an agonist of natriuretic peptide receptors (NPRs), with Kd values of 7.3 and 13 pM for NPR-A and NPR-C, respectively. Nesiritide plays a role after binding to the natriuretic peptide type A and B receptors. In addition to increasing the production of cGMP, Nesiritide can also reduce the renin-angiotensin system (RAS) and sympathetic nerve activity. Nesiritide acetate has a clear expansion effect on small arteries and venules throughout the body; it can significantly reduce pulmonary capillary wedges Entrapment and right atrial pressure reduce the preload of the heart in heart failure. Nesiritide can also significantly reduce the total peripheral vascular resistance, thereby reducing the cardiac afterload in heart failure. Nesiritide acetate has the effect of increasing the cardiac index, and its mechanism is related to reducing the cardiac afterload; it has a specific dilatation effect on the coronary arteries; it also reduces the role of myocardial oxygen consumption.
| Molecular Weight | 3506.07 |
| Formula | C145H246N50O43S4 |
| CAS Number | 114471-18-0 |
| Solubility (25°C) | Water ≥ 40 mg/mL |
| Storage | -20°C, protect from light, sealed |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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