Vixticibart
Based on 1 Customer Validation
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.
For research use only. We do not sell to patients.
- Purity: 97.83%
- CAS No.: 2845128-05-2
- Molecular Weight:146.16 kDa
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Human IgG4 kappa
Human
NPR1
Vixticibart specifically binds to human and monkey natriuretic peptide receptor 1 extracellular domain proteins, with no cross-reactivity to mouse natriuretic peptide receptor 1, natriuretic peptide receptor 2, or natriuretic peptide receptor 3, and does not interfere with atrial natriuretic peptide binding to human natriuretic peptide receptor 1[1].
Vixticibart (10-12 to 10-6 M; under conditions supporting binding) dose-dependently binds to human and monkey natriuretic peptide receptor 1-expressing HEK293 cells, with enhanced binding in the presence of atrial natriuretic peptide or brain natriuretic peptide, and EC50 values ranging from 2.27 to 5.69 nM[1].
Vixticibart (10-15 to 10-5 M) dose-dependently agonizes human and monkey natriuretic peptide receptor 1 in a calcium flux bioassay, with EC50 values ranging from 42.5 to 82.2 nM, and achieves maximum activation comparable to natriuretic peptide ligands at high concentrations[1].
Vixticibart (10-14 to 10-5 M) dose-dependently activates human natriuretic peptide receptor 1 to induce cGMP accumulation in HEK293 cells, acts as a partial agonist relative to natriuretic peptide ligands, and shows enhanced activation in the presence of low concentrations of atrial natriuretic peptide or brain natriuretic peptide[1].
Vixticibart (molar excess; overnight at 4°C) binds to the N-terminal domain of human NPR1 dimers, stabilizing an active conformation in the presence of atrial natriuretic peptide and an active-like conformation in the absence of atrial natriuretic peptide, which drives downstream signaling[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Vixticibart (25 mg/kg; i.v.; single bolus dose) reduces systolic blood pressure, central venous pressure, and pulmonary arterial pressure, while increasing urinary cGMP levels, in normotensive beagle canines[1].
Vixticibart (REGN-5381) (25 mg/kg; i.v.; single dose) induces a sustained reduction in systolic blood pressure and increased urinary cGMP in normotensive telemetered beagle dogs following a single 25 mg/kg intravenous dose[2].
Vixticibart (REGN-5381) (25 mg/kg; i.v.; single dose) reduces central venous pressure and triggers compensatory tachycardia in anesthetized beagle dogs following a single 25 mg/kg intravenous dose[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NPR1hu/hu (C57BL/6NTac [75%]/129S6SvEvTac [25%] background)[1]
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Dosage:1 mg/kg; 5 mg/kg; 25 mg/kg; 50 mg/kg
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Administration:s.c.; single dose
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Result:Induced a 10-15 mm Hg reduction in systolic blood pressure.
Showed dose-dependent duration of effect: effect lost after 10 days at 1 mg/kg, persisted for ~3 weeks at 5 and 25 mg/kg, and remained through 28-day study at 50 mg/kg.
Demonstrated no difference in blood pressure reduction magnitude between 5 and 25 mg/kg groups, indicating 5 mg/kg is a saturating dose.
Increased urinary cGMP significantly with no measurable effect on urine output.
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Animal Model:NPR1hu/hu mice (C57BL/6NTac [75%]/129S6SvEvTac [25%] background)[2]
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Dosage:1 mg/kg; 5 mg/kg; 25 mg/kg; 50 mg/kg
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Administration:s.c.; single dose
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Result:Induced a 10-15 mmHg reduction in systemic systolic blood pressure.
Showed dose-dependent duration of effect: lost BP-lowering effect after 10 days at 1 mg/kg; maintained moderate effects for approximately 3 weeks at 5 and 25 mg/kg; showed persistent BP-lowering effect through 28-day observation period at 50 mg/kg.
Increased urinary cyclic guanosine monophosphate (cGMP) significantly, with no change in urine output detected.
Unconjugated
The product can be reconstituted/diluted with sterile PBS or saline.
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IgG4-kappa
ELISA, FACS, Functional assay
Chemical Information
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CAS No. 2845128-05-2
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Appearance Liquid
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Molecular Weight 146.16 kDa
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Color Colorless to light yellow
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SMILES
[Vixticibart]
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Synonyms
REGN-5381
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Shipping
Shipping with dry ice.
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Formulation
Please refer to the lot-specific COA for specific buffer information.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
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Data Sheet (263 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Inhibitory Antibodies User Guide (603 KB)
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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