Product Name Nesiritide Acetate (BNP-32)
Sequence
Cas No. 114471-18-0
Molecular Formula C143H244N50O42 S4
Molecular Weight 3464.04
Purity (HPLC) 97.0%min.
Appearance White powder
Single Impurity(HPLC) 1.0%max
Amino Acid Composition ±10% of theoretical
Peptide Content(N%) ≥78.0%
Water Content(Karl Fischer) ≤6.0%
Acetate Content(HPIC) ≤15.0%
MS(ESI) Consistent
Mass Balance 95.0~105.0%
Mechanism of action
Human BNP binds to the particulate guanylate cyclase receptor of vascular smooth muscle and endothelial cells, leading to increased intracellular concentrations of guanosine 3'5'-cyclic monophosphate (cGMP) and smooth muscle cell relaxation. Cyclic GMP serves as a second messenger to dilate veins and arteries. Nesiritide has been shown to relax isolated human arterial and venous tissue preparations that were precontracted with either endothelin-1 or the alpha-adrenergic agonist, phenylephrine. In human studies, nesiritide produced dose-dependent reductions in pulmonary capillary wedge pressure (PCWP) and systemic arterial pressure in patients with heart failure. In animals, nesiritide had no effects on cardiac contractility or on measures of cardiac electrophysiology such as atrial and ventricular effective refractory times or atrioventricular node conduction. Naturally occurring atrial natriuretic peptide (ANP), a related peptide, increases vascular permeability in animals and humans and may reduce intravascular volume. The effect of nesiritide on vascular permeability has not been studied.
Biological Activity
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.
| Nesiritide Acetate |
| Product Name |
Nesiritide Acetate |
Cas No. |
114471-18-0 |
| Molecular Formula |
C143H244N50O42S4 |
Molecular Weight |
3464.04 |
| GT # |
|
GT Name |
|
| Sequence |
BRAIN(B-TYPE) NATRIURETIC PEPTIDE-32 (HUMAN) |
| TEST |
SPECIFICATION |
| 1. |
Appearance |
White powder |
| 2. |
Purity (%)(HPLC) |
³>98.0% |
| 3. |
Solubility |
Soluble in water or 1% HAc at a concentration of 1mg/ml to give a clear,colorless solution |
| 4. |
QC Data |
MS and HPLC |
| 5. |
Storage |
2-8℃,keep dry and dark |
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