Lixivaptan
Based on 4 publication(s) in Google Scholar
Lixivaptan (VPA-985, WAY-VPA 985) is an orally active and selective vasopressin receptor V2 antagonist, with IC50 values of 1.2 and 2.3 nM for human and rat V2, respectively.
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- Pureza: 99.67%
- No. CAS: 168079-32-1
- Fòrmula: C27H21ClFN3O2
- Peso molecular:473.93
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Almacenamiento:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Publications Citing Use of MedChemExpress (MCE) Lixivaptan
MoreVer todos los productos específicos de isoformas Vasopressin Receptor
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Actividad biológica
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V2 Receptor |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
124 nM
Compound: 2, lixivaptan, CL-347985
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Displacement of [3H]manning ligand from human vasopressin V1a receptor expressed in CHO cells
Displacement of [3H]manning ligand from human vasopressin V1a receptor expressed in CHO cells
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[PMID: 17855087] |
| CHO | IC50 |
519 nM
Compound: 2, lixivaptan, CL-347985
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Displacement of [3H]oxytocin from human oxytocin receptor expressed in CHO cells
Displacement of [3H]oxytocin from human oxytocin receptor expressed in CHO cells
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[PMID: 17855087] |
| Fibroblast | IC50 |
1.2 nM
Compound: VPA-985
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In vitro inhibition of [3H]AVP binding to human V2 receptor from murine fibroblast cell line (LV2)
In vitro inhibition of [3H]AVP binding to human V2 receptor from murine fibroblast cell line (LV2)
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[PMID: 10406632] |
| Fibroblast | IC50 |
1.2 nM
Compound: 1 (WAY-VPA-985)
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Displacement of [3H]AVP from human vasopressin V2-receptor expressed in murine fibroblast cell (LV2) membranes
Displacement of [3H]AVP from human vasopressin V2-receptor expressed in murine fibroblast cell (LV2) membranes
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[PMID: 10782686] |
| Fibroblast | IC50 |
1.2 nM
Compound: 9
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Displacement of [3H]AVP from human V2 receptor expressed in murine fibroblast cell line (LV2) membranes
Displacement of [3H]AVP from human V2 receptor expressed in murine fibroblast cell line (LV2) membranes
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[PMID: 9651149] |
| HEK293 | IC50 |
150 nM
Compound: lixivaptan, VPA-985
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Displacement of [3H]Arg-vasopressin from human recombinant vasopressin V1a receptor expressed in HEK293 cells
Displacement of [3H]Arg-vasopressin from human recombinant vasopressin V1a receptor expressed in HEK293 cells
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[PMID: 17942308] |
| HEK293 | IC50 |
5 nM
Compound: lixivaptan, VPA-985
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Displacement of [3H]Arg-vasopressin from human recombinant vasopressin V2 receptor expressed in HEK293 cells
Displacement of [3H]Arg-vasopressin from human recombinant vasopressin V2 receptor expressed in HEK293 cells
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[PMID: 17942308] |
| HEK293 | IC50 |
91 nM
Compound: lixivaptan, VPA-985
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Antagonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced cAMP levels
Antagonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced cAMP levels
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[PMID: 17942308] |
| HEK293 | IC50 |
>5000 nM
Compound: lixivaptan, VPA-985
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Antagonist activity at human vasopressin V1a receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced intracellular calcium level
Antagonist activity at human vasopressin V1a receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced intracellular calcium level
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[PMID: 17942308] |
Lixivaptan displays competitive antagonist activity at V2 receptors[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 168079-32-1
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Appearance Solid
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Peso molecular 473.93
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Fòrmula C27H21ClFN3O2
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Color White to off-white
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SMILES
O=C(C1=C(Cl)C=C(NC(C2=CC(F)=CC=C2C)=O)C=C1)N(C3)C4=CC=CC=C4CN5C3=CC=C5
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Synonyms
VPA-985; WAY-VPA 985
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications (4)
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Journal Impact Factor
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Most Recent
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Eur J Pharmacol
Revisit ligand-receptor interaction at the human vasopressin V2 receptor: A kinetic perspective. [Abstract]2020 Aug 5;880:173157. PMID: 32360346 -
Transl Oncol
2025 Sep 29:62:102549. PMID: 41027284 -
Continence (Amst)
Endogenous vasopressin and vasopressin receptor 2 in bladder as anti-diuretic / anti-spasmodic targets for the treatment of multifactorial nocturia. [Abstract]2025 Dec:16:102292. PMID: 41503219 -
Solvente y solubilidad
DMSO : ≥ 150 mg/mL (316.50 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" 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 (protect from 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 (protect from 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: ≥ 2.08 mg/mL (4.39 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
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 (protect from 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.
Pureza y Documentación
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Ficha de datos (279 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Albright JD, et al. 5-Fluoro-2-methyl-N-[4-(5H-pyrrolo[2,1-c]-[1, 4]benzodiazepin-10(11H)-ylcarbonyl)-3-chlorophenyl]benzamide (VPA-985): an orally active arginine vasopressin antagonist with selectivity for V2 receptors. J Med Chem. 1998 Jul 2;41(14):2442-4. [Content Brief]
[2]. Ghali JK, et al. Lixivaptan, a non-peptide vasopressin V2 receptor antagonist for the potential oral treatment of hyponatremia. IDrugs. 2010 Nov;13(11):782-92. [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 (protect from 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 | 2.1100 mL | 10.5501 mL | 21.1002 mL | 52.7504 mL |
| 5 mM | 0.4220 mL | 2.1100 mL | 4.2200 mL | 10.5501 mL | |
| 10 mM | 0.2110 mL | 1.0550 mL | 2.1100 mL | 5.2750 mL | |
| 15 mM | 0.1407 mL | 0.7033 mL | 1.4067 mL | 3.5167 mL | |
| 20 mM | 0.1055 mL | 0.5275 mL | 1.0550 mL | 2.6375 mL | |
| 25 mM | 0.0844 mL | 0.4220 mL | 0.8440 mL | 2.1100 mL | |
| 30 mM | 0.0703 mL | 0.3517 mL | 0.7033 mL | 1.7583 mL | |
| 40 mM | 0.0528 mL | 0.2638 mL | 0.5275 mL | 1.3188 mL | |
| 50 mM | 0.0422 mL | 0.2110 mL | 0.4220 mL | 1.0550 mL | |
| 60 mM | 0.0352 mL | 0.1758 mL | 0.3517 mL | 0.8792 mL | |
| 80 mM | 0.0264 mL | 0.1319 mL | 0.2638 mL | 0.6594 mL | |
| 100 mM | 0.0211 mL | 0.1055 mL | 0.2110 mL | 0.5275 mL |
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