Description

Product Description

PL-3994 (CAS 952295-80-6) is a synthetic analog of natriuretic peptides and functions as a selective agonist of natriuretic peptide receptor-A (NPR-A). Designed for enhanced stability, it is resistant to neutral endopeptidase degradation, which significantly prolongs its biological half-life compared to native peptides. This property makes PL-3994 a valuable research tool in respiratory, cardiovascular, and endocrine studies.

Background:
Natriuretic peptides (ANP, BNP, CNP) regulate cardiovascular, renal, and pulmonary physiology through interaction with NPR-A and NPR-B receptors. NPR-A activation leads to increased intracellular cyclic GMP (cGMP) levels, resulting in vasodilation, natriuresis, diuresis, and smooth muscle relaxation. However, native peptides are rapidly degraded by neutral endopeptidase (NEP), limiting their research applications. PL-3994 overcomes this challenge with structural modifications that confer NEP resistance.

Pharmacological Role:
As a bronchodilator, PL-3994 induces relaxation of pre-contracted airway smooth muscle. In preclinical guinea pig trachea models, it produces concentration-dependent smooth muscle relaxation with an IC?? of 42.7 nM. This potency, combined with NEP resistance, allows prolonged and reproducible effects in respiratory research models.

Research Importance:
PL-3994 is applied in multiple fields:

• Respiratory research: bronchodilation studies, asthma, COPD, airway reactivity.

• Cardiovascular research: regulation of vascular tone, cardiac hypertrophy, and hypertension models.

• Renal physiology: effects on natriuresis, diuresis, and fluid balance.

• Pharmacology: evaluation of NPR-A signaling and drug discovery targeting peptide receptor pathways.

Advantages over Native Peptides:

• Resistant to rapid degradation by NEP.

• Longer half-life and enhanced stability in vitro and in vivo.

• Potent agonist activity with reproducible dose-response profiles.

GMP-Grade Reliability:
Produced under GMP-certified conditions, PL-3994 ensures high purity, structural integrity, and batch consistency. This quality is critical for reproducibility in preclinical studies.

Disclaimer: For laboratory research use only. Not for human or veterinary use.

Product Specifications

Mechanism of Action & Research Applications

PL-3994 functions by binding selectively to NPR-A receptors. Upon activation, NPR-A stimulates guanylyl cyclase activity, increasing intracellular cyclic GMP (cGMP) levels. Elevated cGMP mediates smooth muscle relaxation, vasodilation, natriuresis, and inhibition of pathological remodeling.

Mechanism Highlights:

• NPR-A receptor agonism: direct activation of guanylyl cyclase.

• cGMP pathway activation: promotes relaxation of airway and vascular smooth muscle.

• NEP resistance: prevents rapid peptide degradation, ensuring sustained effects.

Research Applications:

• Respiratory pharmacology: bronchodilation in asthma, COPD, and airway reactivity models.

• Cardiovascular models: regulation of blood pressure, cardiac hypertrophy, and vascular compliance.

• Renal studies: exploration of natriuretic and diuretic responses to NPR-A agonism.

• Endocrine research: interplay of natriuretic peptides with RAAS (renin-angiotensin-aldosterone system).

• Pharmacological development: benchmark compound for peptide agonist drug discovery.

• Translational relevance: informs novel therapeutic approaches for cardiopulmonary disease.

Side Effects (For Reference in Research Models)

• Respiratory system: dose-dependent bronchodilation (intended effect).

• Cardiovascular effects: transient hypotension or tachycardia in some models.

• Renal responses: enhanced urine output and electrolyte shifts.

• Species variability: potency and pharmacokinetics differ across models.

• Stability factors: activity may decline with repeated freeze-thaw cycles.

• Hormonal modulation: may interact with RAAS in experimental setups.

Note: These observations are model-specific and provided strictly for laboratory reference. PL-3994 is not intended for human or veterinary use.

Disclaimer

For laboratory research use only. Not for human or veterinary use.

 Keywords

PL-3994 CAS 952295-80-6
NPR-A agonist peptide
Bronchodilator research peptide
Natriuretic peptide analog
Neutral endopeptidase-resistant peptide
PL-3994 GMP supplier
Respiratory pharmacology research peptide
Cardiovascular peptide agonist
cGMP pathway activator peptide