Description

Velmupressin is a synthetic peptidic agonist of the vasopressin V2 receptor (V2R), designed with a unique cyclic peptide backbone c(Bua-Cpa-Thi-Val-Asn-Cys)-Pro-d-Arg-NEt2. This structural modification allows Velmupressin to exhibit high receptor affinity, remarkable selectivity, and short-acting pharmacological characteristics, making it a valuable research tool in endocrinology, nephrology, and receptor pharmacology studies.

With EC50 values of 0.07 nM for human V2R and 0.02 nM for rat V2R, Velmupressin demonstrates a strong potency profile, facilitating detailed investigations into vasopressin receptor-mediated signaling, water reabsorption mechanisms, and potential applications in water balance disorders. Unlike native vasopressin, Velmupressin’s pharmacokinetic profile has been engineered for controlled receptor activation, allowing researchers to analyze transient V2R stimulation without prolonged systemic effects.

As a GMP-manufactured peptide, Velmupressin ensures high purity, reproducibility, and reliability in preclinical and translational studies. It is often applied in experimental models to explore renal physiology, aquaporin regulation, and novel therapeutic pathways for conditions such as nephrogenic diabetes insipidus, SIADH (syndrome of inappropriate antidiuretic hormone secretion), and electrolyte imbalance research.

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

Product Specifications

Mechanism of Action & Research Applications

Velmupressin exerts its biological activity by selectively binding to and activating the vasopressin V2 receptor (V2R), a G-protein coupled receptor (GPCR) expressed primarily in the renal collecting ducts. Upon activation, the receptor stimulates adenylate cyclase activity via Gs protein coupling, leading to an increase in intracellular cAMP levels. This cascade promotes aquaporin-2 (AQP2) translocation to the apical membrane, enhancing water reabsorption in kidney tubules.

Research applications of Velmupressin include:

• Renal physiology studies – Investigation of AQP2 regulation, water balance, and electrolyte homeostasis.

• Endocrinology research – Analysis of vasopressin-mediated signaling pathways in disease models.

• Short-acting V2R agonist studies – Comparison with long-acting analogues to assess temporal effects of receptor activation.

• SIADH & water imbalance models – Understanding the role of V2R signaling in pathological water retention.

• Pharmacology screening – Benchmark compound for developing novel V2R modulators.

Velmupressin’s short half-life allows precise control in experimental setups, minimizing long-term compensatory effects. This makes it highly suitable for preclinical studies requiring transient stimulation of vasopressin pathways.

Side Effects (For Reference in Research Models)

While Velmupressin is strictly intended for laboratory use, data from related V2R agonists provide insight into potential experimental side effects:

• Electrolyte imbalance: Alterations in sodium and potassium levels due to increased water reabsorption.

• Hyponatremia: Excess water retention leading to dilutional sodium reduction.

• Renal stress: Overactivation of aquaporin pathways may influence renal tubular load.

• Vascular effects: Although highly selective for V2R, off-target vasopressin receptor interactions may affect vascular tone.

• Transient fluid shifts: Related to its short-acting but potent aquaretic modulation.

Disclaimer

 is supplied exclusively for laboratory research purposes. It is not intended for human use, veterinary use, or as a drug, food additive, or household chemical. Proper laboratory handling and storage conditions are required.

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