Nesiritide acetate | CAS No. 1684439-46-0

Description

Product Description

Nesiritide acetate (CAS No. 1684439-46-0) is the acetate salt of recombinant human B-type natriuretic peptide (BNP-32). BNP is a cardiac hormone secreted primarily by the ventricles of the heart in response to excessive stretching of heart muscle cells (cardiomyocytes). It plays a crucial role in the regulation of blood pressure, vascular tone, fluid balance, and cardiac function. Nesiritide acetate is a synthetic form developed to mimic these physiological effects, with optimized stability for laboratory applications.

Structural and Biochemical Profile

• Peptide length: 32 amino acids (BNP-32)

• Molecular form: Recombinant human peptide, acetate salt

• Receptor targets:

  • NPR-A (Natriuretic Peptide Receptor-A): Kd = 7.3 pM

  • NPR-C (Natriuretic Peptide Receptor-C): Kd = 13 pM

• Downstream effect: Activates guanylyl cyclase → ↑ cGMP → vascular smooth muscle relaxation and natriuresis.

Cardiovascular Significance

BNP, along with atrial natriuretic peptide (ANP) and C-type natriuretic peptide (CNP), belongs to the natriuretic peptide family, essential for cardiovascular homeostasis. Nesiritide acetate’s recombinant form provides researchers a reliable agent for:

• Studying heart failure pathophysiology

• Investigating vascular remodeling after arterial injury

• Understanding renal sodium handling and diuresis mechanisms

• Modeling blood pressure regulation through vasodilatory effects

Key Research Applications

1. Heart Failure Models

   • Nesiritide mimics endogenous BNP secretion in failing hearts.

   • Reduces cardiac preload and afterload via vasodilation.

   • Promotes diuresis, relieving fluid overload.

2. Vascular Biology

   • Investigates smooth muscle cell relaxation mechanisms.

   • Used in studies of vascular remodeling and repair.

3. Renal Physiology

   • Enhances sodium excretion (natriuresis).

   • Improves glomerular filtration rate (GFR).

4. Electrophysiology Research

   • Modulates L-type calcium channel V1/2 activation/inactivation, influencing cardiac action potential dynamics.

Product Specifications

Mechanism of Action

Nesiritide acetate functions as a natriuretic peptide receptor (NPR) agonist, primarily binding NPR-A and NPR-C, leading to downstream cGMP signaling.

Receptor Binding and Signal Transduction

• NPR-A activation → stimulates guanylyl cyclase activity → ↑ intracellular cGMP → smooth muscle relaxation.

• NPR-C binding → regulates peptide clearance and additional signaling roles.

Cardiovascular Effects

• Vasodilation: Reduces systemic vascular resistance (afterload).

• Diuresis & Natriuresis: Promotes excretion of sodium and water via kidneys.

• Cardiac unloading: Decreases venous return (preload), lowering cardiac stress.

• Anti-hypertrophic action: Prevents maladaptive remodeling of cardiac tissue.

Modulation of Calcium Channel Activity

Nesiritide regulates V1/2 activation and inactivation of the L-type calcium channel, a key determinant of myocardial contractility and electrophysiological stability.

Research Implications

• Heart Failure Research: Clarifies BNP role in acute decompensated heart failure.

• Vascular Injury & Remodeling: Studies BNP impact on endothelial and smooth muscle regeneration.

• Kidney Function: Helps dissect natriuretic peptide role in renal clearance and GFR.

  

Side Effects

Though Nesiritide acetate is restricted to research use, experimental data suggest potential side effects:

Cardiovascular System

• Hypotension due to vasodilation.

• Reflex tachycardia in some experimental settings.

Renal System

• Excessive natriuresis leading to electrolyte imbalance.

• Transient changes in kidney function under high exposure.

CNS Effects

• Headache and dizziness related to reduced blood pressure.

Gastrointestinal System

• Nausea or mild GI discomfort in animal studies.

Laboratory Safety

• Handle as a research peptide with protective equipment.

• Avoid repeated freeze-thaw cycles to preserve integrity.

Disclaimer

Nesiritide acetate is provided for laboratory research only. It is not intended for human or veterinary use, clinical application, or diagnostic procedures.

Keywords

Nesiritide acetate, CAS 1684439-46-0, BNP-32 peptide, natriuretic peptide receptor agonist, cardiovascular peptide, heart failure research, vasodilatory peptide, renal sodium regulation, vascular remodeling, cGMP signaling.

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