Conivaptan hydrochloride
Based on 14 publication(s) in Google Scholar
Conivaptan (hydrochloride) is a non-peptide antagonist of vasopressin receptor, with Ki values of 0.48 and 3.04 nM for rat liver V1A receptor and rat kidney V2 receptor respectively.
For research use only. We do not sell to patients.
- Purity: 99.95%
- CAS No.: 168626-94-6
- Formula: C32H27ClN4O2
- Molecular Weight:535.04
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Storage:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Conivaptan hydrochloride
More- Cell. 2026 May 28;189(11):3444-3464.e28. [Abstract]
- Nat Commun. 2025 Nov 4;16(1):9734. [Abstract]
- Biomed Pharmacother. 2025 Jun 20:189:118246. [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]
- Front Pharmacol. 2019 Nov 15;10:1380. [Abstract]
- Eur J Pharmacol. 2020 Aug 5;880:173157. [Abstract]
- Biomed J. 2020 Aug;43(4):368-374. [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]
- SSRN. 2025 Jun 18.
- SSRN. 2023 May 30.
All Vasopressin Receptor Isoforms
More
Biological Activity
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V2 Receptor |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 168626-94-6
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Appearance Solid
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Molecular Weight 535.04
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Formula C32H27ClN4O2
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Color White to off-white
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SMILES
O=C(C1=CC=CC=C1C2=CC=CC=C2)NC3=CC=C(C(N4CCC(N=C(C)N5)=C5C6=CC=CC=C64)=O)C=C3.Cl
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Synonyms
YM 087
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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 -
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 Jun 20:189:118246. PMID: 40543162 -
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 -
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 -
Eur J Pharmacol
Revisit ligand-receptor interaction at the human vasopressin V2 receptor: A kinetic perspective. [Abstract]2020 Aug 5;880:173157. PMID: 32360346 -
Biomed J
2020 Aug;43(4):368-374. PMID: 32563698 -
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 -
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Solvent & Solubility
DMSO : ≥ 100 mg/mL (186.90 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.67 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.67 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
At 4 weeks after the operation, 39 myocardial infarction rats survived. Thirty are randomly selected without bias and divided into five groups such that the distribution of infarct size and body weight among groups are similar, and given vehicle, conivaptan (0.03, 0.1 and 0.3 mg/kg) or SR121463A (0.3 mg/kg) by intravenous administration. Sham rats are also divided into four groups and given vehicle or conivaptan (0.03, 0.1 and 0.3 mg/kg) by intravenous administration. Rats are then placed individually in metabolic cages and urine is collected for 3 h. Urine osmolality is measured by the freezing point depression method using an osmometer.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (283 KB)
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SDS (418 KB)
- English - EN (418 KB)
- Français - FR (418 KB)
- Deutsch - DE (418 KB)
- Norwegian - NO (418 KB)
- Español - ES (418 KB)
- Swedish - SV (418 KB)
- Italian - IT (418 KB)
- Portuguese - PT (418 KB)
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Handling Instructions (2659 KB)
References
[1]. Wada K, et al. Intravenous administration of conivaptan hydrochloride improves cardiac hemodynamics in rats with myocardial infarction-induced congestive heart failure. Eur J Pharmacol. 2005 Jan 10;507(1-3):145-51. Epub 2005 Jan 1. [Content Brief]
[2]. Fernandez-Varo G, et al. Effect of the V1a/V2-AVP receptor antagonist, Conivaptan, on renal water metabolism and systemic hemodynamics in rats with cirrhosis and ascites. J Hepatol. 2003 Jun;38(6):755-61. [Content Brief]
[3]. Yatsu T, et al. Cardiovascular and renal effects of conivaptan hydrochloride (YM087), a vasopressin V1A and V2 receptor antagonist, in dogs with pacing-induced congestive heart failure. Eur J Pharmacol. 1999 Jul 9;376(3):239-46. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.8690 mL | 9.3452 mL | 18.6904 mL | 46.7259 mL |
| 5 mM | 0.3738 mL | 1.8690 mL | 3.7381 mL | 9.3452 mL | |
| 10 mM | 0.1869 mL | 0.9345 mL | 1.8690 mL | 4.6726 mL | |
| 15 mM | 0.1246 mL | 0.6230 mL | 1.2460 mL | 3.1151 mL | |
| 20 mM | 0.0935 mL | 0.4673 mL | 0.9345 mL | 2.3363 mL | |
| 25 mM | 0.0748 mL | 0.3738 mL | 0.7476 mL | 1.8690 mL | |
| 30 mM | 0.0623 mL | 0.3115 mL | 0.6230 mL | 1.5575 mL | |
| 40 mM | 0.0467 mL | 0.2336 mL | 0.4673 mL | 1.1681 mL | |
| 50 mM | 0.0374 mL | 0.1869 mL | 0.3738 mL | 0.9345 mL | |
| 60 mM | 0.0312 mL | 0.1558 mL | 0.3115 mL | 0.7788 mL | |
| 80 mM | 0.0234 mL | 0.1168 mL | 0.2336 mL | 0.5841 mL | |
| 100 mM | 0.0187 mL | 0.0935 mL | 0.1869 mL | 0.4673 mL |
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