2845128-05-2
Chemical Structure
Vixticibart
Synonym(s): REGN-5381
- CAS No.: 2845128-05-2
- Formula:N/A
- Molecular Weight:(146.16 kDa)
SMILES: [Vixticibart]
Biological Activity: Vixticibart (REGN-5381) is a fully human IgG4 monoclonal antibody and NPR1 agonist that targets NPR1. Vixticibart stabilizes the receptor in an activated conformation by binding to the N-terminal domain of NPR1, and enhances the activity of endogenous ligands ANP and BNP without blocking ligand binding when these ligands are present. Vixticibart exerts vasodilatory and hypotensive effects by inducing cGMP production, preferentially dilating venous vessels to reduce systolic and venous pressure, but does not induce diuresis and may trigger a compensatory increase in heart rate. Vixticibart produces a synergistic hypotensive effect when combined with angiotensin-converting enzyme inhibitors or angiotensin receptor blockers, and is currently mainly used in research related to heart failure and hypertension[1][2][3].
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Vixticibart | 97.83% | Vixticibart (REGN-5381) is a fully human IgG4 monoclonal antibody and NPR1 agonist that targets NPR1. Vixticibart stabilizes the receptor in an activated conformation by binding to the N-terminal domain of NPR1, and enhances the activity of endogenous ligands ANP and BNP without blocking ligand binding when these ligands are present. Vixticibart exerts vasodilatory and hypotensive effects by inducing cGMP production, preferentially dilating venous vessels to reduce systolic and venous pressure, but does not induce diuresis and may trigger a compensatory increase in heart rate. Vixticibart produces a synergistic hypotensive effect when combined with angiotensin-converting enzyme inhibitors or angiotensin receptor blockers, and is currently mainly used in research related to heart failure and hypertension. | ||||||||||||||||||||
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- [1]. Dunn ME, et al. Agonist antibody to guanylate cyclase receptor NPR1 regulates vascular tone. Nature. 2024;633(8030):654-661. [Content Brief]
- [2]. Dunn M, et al. A novel agonist antibody to membrane-bound guanylate cyclase receptor, natriuretic peptide receptor 1, induces sustained vasodilation[J]. 2023.
- [3]. Kithcart A P, et al. Effects of REGN5381, a natriuretic peptide receptor 1 agonist antibody, in hypertensive mouse models and mildly hypertensive but otherwise healthy adults in a phase 1 first-in-human study[J]. Journal of the American College of Cardiology, 2024, 83(13_Supplement): 1706-1706.
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