Conivaptan
Based on 14 publication(s) in Google Scholar
Conivaptan (YM 087 free base) is an orally active dual vasopressin V1a/V2 receptor antagonist with Ki values of 0.48 nM and 3.04 nM for vasopressin V1a receptor and V2 receptor, respectively. Conivaptan competitively and reversibly blocks vasopressin-mediated antidiuresis, vasoconstriction, and cellular hypertrophy, while inhibiting CYP3A4. Conivaptan inhibits vasopressin-induced intracellular calcium, cAMP, and mitogen-activated kinase activation in vascular smooth muscle cells and cardiomyocytes. Conivaptan induces water diuresis while improving hemodynamics in heart failure models, reducing left ventricular end-diastolic pressure, vascular resistance, and organ weight. Conivaptan is used for research on hyponatremia and congestive heart failure.
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- No. CAS: 210101-16-9
- Fòrmula: C32H26N4O2
- Peso molecular:498.57
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Publications Citing Use of MedChemExpress (MCE) Conivaptan
More- Cell. 2026 May 28;189(11):3444-3464.e28. [Abstract]
- Nat Commun. 2025 Nov 4;16(1):9734. [Abstract]
- J Transl Med. 2025 Jan 22;23(1):103. [Abstract]
- J Med Chem. 2024 Apr 11;67(7):5935-5944. [Abstract]
- J Med Chem. 2022 Jul 14;65(13):9295-9311. [Abstract]
- Biomed J. 2020 Aug;43(4):368-374. [Abstract]
- Eur J Pharmacol. 2020 Aug 5:880:173157. [Abstract]
- Front Pharmacol. 2019 Nov 15:10:1380. [Abstract]
- J Pharm Biomed Anal. 2021 Feb 20:195:113870. [Abstract]
- Neurogastroenterol Motil. 2019 Feb;31(2):e13493. [Abstract]
- Dig Dis Sci. 2022 Aug;67(8):3683-3692. [Abstract]
- Biomed Pharmacother. 2025 Aug:189:118246. [Abstract]
- SSRN. 2025 Jun 18.
- SSRN. 2023 May 30.
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Bio/Physico-chemical Assay
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Bio/Physico-chemical Assay
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In Vivo Efficacy Study
Ver todos los productos específicos de isoformas Vasopressin Receptor
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
V1a Receptor 0.48 nM (Ki) |
V2 Receptor 3.04 nM (Ki) |
CYP3A4 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| COS-1 | IC50 |
14.3 nM
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Inhibition of AVP-induced intracellular Ca2+ increase in COS1 cells expressing human V1a receptors.
Inhibition of AVP-induced intracellular Ca2+ increase in COS1 cells expressing human V1a receptors.
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10.1111%2Fj.1527-3466.2007.00019.x |
| COS-1 | IC50 |
2.0 nM
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Inhibition of AVP-induced cAMP increase in COS1 cells expressing human V2 receptors.
Inhibition of AVP-induced cAMP increase in COS1 cells expressing human V2 receptors.
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10.1111%2Fj.1527-3466.2007.00019.x |
In Vitro
Conivaptan binds to vasopressin V1a receptors (Ki = 0.48 nM) and vasopressin V2 receptors (Ki = 3.04 nM) in a competitive and reversible manner, and shows almost no activity against vasopressin V1b receptors[1].
Conivaptan inhibits vasopressin-triggered intracellular calcium elevation in vascular smooth muscle cells (IC50 = 1.16 nM) and simultaneously inhibits vasopressin-induced cAMP accumulation (IC50 = 17.3 nM)[1].
Conivaptan binds with high affinity to canine platelet V1a receptors (Ki = 0.6 nM) and canine kidney V2 receptors (Ki = 0.7 nM), binds to rhesus monkey liver V1a receptors (Ki = 26 nM) and rhesus monkey kidney V2 receptors (Ki = 10 nM), and inhibits AVP binding to human cloned V1a receptors (Ki = 6.3 nM) and V2 receptors (Ki = 1.1 nM) in COS1 cells.
Conivaptan inhibits AVP-induced increases in Ca2+ and cAMP in COS1 cells expressing human receptors, with IC50 values of 2.0-14.3 nM; it inhibits AVP-induced Ca2+, mitogen-activated kinase, and protein synthesis in rat cardiomyocytes expressing V1a receptors; and it inhibits AVP-induced proliferation and hypertrophy of vascular smooth muscle cells in growth-arrested rats[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Ensayo clínico
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 210101-16-9
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Peso molecular 498.57
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Fòrmula C32H26N4O2
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SMILES
O=C(C1=C(C2=CC=CC=C2)C=CC=C1)NC3=CC=C(C(N4C5=C(C6=C(CC4)N=C(C)N6)C=CC=C5)=O)C=C3
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Synonyms
YM 087 free base
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (14)
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Journal Impact Factor
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Most Recent
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Cell
2026 May 28;189(11):3444-3464.e28. PMID: 41923641 -
Nat Commun
2025 Nov 4;16(1):9734. PMID: 41188237
Conivaptan purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Nov 4;16(1):9734. [Abstract]
Effects of pocket residue mutations in V2R on the antagonistic activity of Conivaptan hydrochloride.
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J Transl Med
Single-cell profiling of SLC family transporters: uncovering the role of SLC7A1 in osteosarcoma. [Abstract]2025 Jan 22;23(1):103. PMID: 39844299 -
J Med Chem
Long-Residence Time Peptide Antagonist for the Vasopressin V2 Receptor to Treat Autosomal Dominant Polycystic Kidney Disease. [Abstract]2024 Apr 11;67(7):5935-5944. PMID: 38509003 -
J Med Chem
Benzodiazepine Derivatives as Potent Vasopressin V2 Receptor Antagonists for the Treatment of Autosomal Dominant Kidney Disease. [Abstract]2022 Jul 14;65(13):9295-9311. PMID: 35579344 -
Biomed J
2020 Aug;43(4):368-374. PMID: 32563698 -
Eur J Pharmacol
Revisit ligand-receptor interaction at the human vasopressin V2 receptor: A kinetic perspective. [Abstract]2020 Aug 5:880:173157. PMID: 32360346
Conivaptan purchased from MedChemExpress. Usage Cited in: Eur J Pharmacol. 2020 Aug 5:880:173157. [Abstract]
All compounds produced concentration-dependent inhibition of specific Conivaptan hydrochloride-red binding.
Conivaptan purchased from MedChemExpress. Usage Cited in: Eur J Pharmacol. 2020 Aug 5:880:173157. [Abstract]
Saturation experiments for Conivaptan hydrochloride-red (0.1-100 nM, final concentration) binding to the SNAP-tagged HEK293hV2R cells at 25 ℃ and 37 ℃; total binding, non-specific binding and specific binding are shown. Nonspecific binding was determined in the presence of 100 μM Conivaptan hydrochloride and represented less than 10% of the total Conivaptan hydrochloride-red binding. Data are from three independent experiments each performed in duplicate.
Conivaptan purchased from MedChemExpress. Usage Cited in: Eur J Pharmacol. 2020 Aug 5:880:173157. [Abstract]
Equilibrium and kinetic binding profiles of conivaptan-red at the vasopressin V2 receptor.
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Front Pharmacol
Intradermal Injection of Oxytocin Aggravates Chloroquine-Induced Itch Responses via Activating the Vasopressin-1a Receptor/Nitric Oxide Pathway in Mice. [Abstract]2019 Nov 15:10:1380. PMID: 31824317
Conivaptan purchased from MedChemExpress. Usage Cited in: Front Pharmacol. 2019 Nov 15:10:1380. [Abstract]
The OT-mediated enhancement of CQ-induced scratching behavior was significantly suppressed in mice pretreated with the V1AR antagonist Conivaptan hydrochloride (1 µg/site).
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J Pharm Biomed Anal
Screening method of mildronate and over 300 doping agents by reversed-phase liquid chromatography-high resolution mass spectrometry. [Abstract]2021 Feb 20:195:113870. PMID: 33453569 -
Neurogastroenterol Motil
Vasopressin augments TNBS-induced colitis through enteric neuronal V1a receptor-mediated COX-2-dependent prostaglandin release from mast cells in mice. [Abstract]2019 Feb;31(2):e13493. PMID: 30334342 -
Dig Dis Sci
A New Role for Conivaptan in Ulcerative Colitis in Mice: Inhibiting Differentiation of CD4+T Cells into Th1 Cells. [Abstract]2022 Aug;67(8):3683-3692. PMID: 34751838 -
Biomed Pharmacother
Identification of nsp16 inhibitors of SARS -CoV-2, SARS -CoV-1 and MERS-CoV from FDA-approved drugs using in silico and in vitro methods. [Abstract]2025 Aug:189:118246. PMID: 40543162 -
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Protocolo
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Calcium Spark Assay
Calcium sparks are localized, transient increases in intracellular calcium concentration ([Ca2+]i) that occur in cardiac myocytes and represent elementary events underlying excitation-contraction coupling. These events are generated by the coordinated opening of clusters of ryanodine receptors (RyRs) on the sarcoplasmic reticulum membrane, leading to a brief release of Ca2+ into the cytosol. The detection and analysis of calcium sparks provide insights into the mechanisms of calcium handling and signaling in cardiac cells. Imaging techniques using fluorescent calcium indicators such as Fluo-3 are employed to visualize these subcellular calcium transients with high spatial and temporal resolution. The protocol is based on established methodologies described in primary literature for both experimental measurement and automated analysis of calcium sparks.
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Research Protocol for Cardiovascular Diseases
Cardiovascular disease can be modeled as maladaptive cardiac remodeling, where ischemic injury or pressure overload activates inflammatory signaling, fibroblast activation, extracellular-matrix deposition, cardiomyocyte hypertrophy, vascular remodeling, and progressive ventricular dysfunction. The TGF-β/SMAD axis is a central profibrotic pathway after myocardial injury and pressure overload, while innate immune and cytokine pathways regulate leukocyte recruitment, scar formation, and adverse remodeling. Key unresolved questions include which inflammatory signals are reparative versus harmful, when fibrosis is protective versus maladaptive, and whether pathway inhibition improves function without weakening necessary infarct healing or compensatory remodeling.
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Ca2+ Staining Technique
Ca2+ staining is an experimental technique that utilizes specific fluorescent probes (such as Fluo-4 AM, Fura-2, etc.) to qualitatively or quantitatively detect dynamic changes in intracellular Ca2+ concentrations; this is achieved by monitoring the changes in fluorescent signals generated when these probes bind to free intracellular calcium ions. The underlying principle relies primarily on the presence of chelating groups within the probe's molecular structure that possess high affinity for calcium ions.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Conivaptan Related Classifications
HY-18347 Related Classifications
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