| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Targets |
Fedovapagon selectively targets the vasopressin V2 receptor (V2R), a G protein-coupled receptor primarily expressed in the kidney collecting ducts. Activation of V2R by fedovapagon stimulates an increase in water permeability through the insertion of aquaporin-2 channels into the apical membrane of collecting duct cells, leading to antidiuresis and reduced urine output. The compound has an EC50 of 24 nM for V2R activation.
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| ln Vitro |
Fedovapagon is a potent V2 receptor agonist with an EC50 of 24 nM. Its selectivity for V2R over other vasopressin receptor subtypes contributes to its favorable efficacy and safety profile. In vitro studies have characterized the compound's agonist activity using cell-based assays measuring V2R-mediated cAMP accumulation. Fedovapagon also inhibits the growth of intersegmental vessels in zebrafish, demonstrating its biological activity in a whole-organism model.
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| ln Vivo |
Rats' urine production is inhibited by fedovapagon (1 mg/kg, orally) at an 81% inhibition rate[1].
Fedovapagon has demonstrated positive antidiuretic effects in vivo and has been evaluated in clinical trials for the treatment of nocturia. The compound's V2R agonism leads to increased water reabsorption in the kidney, reducing urine volume and frequency of urination. A large Phase 3 trial has recently been completed in male patients with nocturia. Fedovapagon is also being studied for overactive bladder and painful bladder syndromes. |
| Enzyme Assay |
Non-cellular receptor binding assays for fedovapagon involve competitive radioligand binding displacement studies using membrane preparations from cells expressing the human vasopressin V2 receptor. The membranes are incubated with a radiolabeled V2R ligand (e.g., [³H]AVP or [¹²⁵I]d(CH₂)₅[Tyr(Me)²]AVP) and varying concentrations of fedovapagon. Following incubation and filtration, the radioactivity is measured to determine the IC50, which is then converted to a Ki value using the Cheng-Prusoff equation.
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| Cell Assay |
In vitro cellular assays for fedovapagon involve treating cells expressing the human vasopressin V2 receptor with the compound and measuring receptor-mediated signaling. Cells are treated with varying concentrations of fedovapagon, and the activation of V2R is measured by quantifying cAMP accumulation using a cAMP ELISA or HTRF-based assay (as V2R is coupled to Gs proteins). The EC50 for receptor activation is determined from dose-response curves. The compound's effects on cell proliferation or other downstream pathways may also be assessed.
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| Animal Protocol |
Animal/Disease Models: Brattleboro rat[1]
Doses: 1 mg/kg, 3 mg/kg Route of Administration: Oral Experimental Results:diminished urine output, almost complete suppression of urine output within 2 hrs (hrs (hours)). Allow urine to return to normal levels 5 hrs (hrs (hours)) after dosing. In vivo animal experiments with fedovapagon have been conducted in zebrafish and rodent models. In zebrafish, the compound inhibits the growth of intersegmental vessels, demonstrating its biological activity in a whole-organism model. In rodent models of nocturia and overactive bladder, fedovapagon is administered via oral or intravenous routes, and its effects on urine output, bladder function, and voiding frequency are measured. Pharmacokinetic and toxicological studies have also been performed to support clinical development. |
| ADME/Pharmacokinetics |
Fedovapagon has a molecular weight of 462.58-462.59 and a molecular formula of C27H34N4O3. It is a solid at room temperature and is typically stored at 2-8°C. The compound is soluble in DMSO and other organic solvents. Purity is typically ≥98%. It is stable under recommended storage conditions and is protected from light and moisture.
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| Toxicity/Toxicokinetics |
Fedovapagon is an investigational compound that has been evaluated in clinical trials for the treatment of nocturia. In preclinical and clinical studies, it has been generally well-tolerated. As a V2 receptor agonist, it may cause side effects related to fluid retention, including hyponatremia, edema, and weight gain. The compound should be used with caution in patients with heart failure or renal impairment. Standard laboratory safety precautions should be followed when handling the compound.
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| References | |
| Additional Infomation |
Fedovapagon has been used in trials investigating the treatment of nocturia.
Fedovapagon (VA106483; CAS 347887-36-9) is a potent, selective, and non-peptidic vasopressin V2 receptor agonist with an EC50 of 24 nM. It has been developed for the treatment of nocturia, overactive bladder, and painful bladder syndromes. The compound has recently completed a large Phase 3 clinical trial in male patients with nocturia. Fedovapagon is available from various commercial suppliers for research applications. |
| Molecular Formula |
C27H34N4O3
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|---|---|
| Molecular Weight |
462.594
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| Exact Mass |
462.263
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| CAS # |
347887-36-9
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| PubChem CID |
10298385
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| Appearance |
Off-white to light yellow solid powder
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| LogP |
3.947
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
34
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| Complexity |
741
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| Defined Atom Stereocenter Count |
1
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| SMILES |
CC1=C(C=CC(=C1)C(=O)N2CCCCC3=CC=CC=C32)CNC(=O)N4CCC[C@H]4C(=O)N(C)C
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| InChi Key |
RUOLFWZIFNQQGH-DEOSSOPVSA-N
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| InChi Code |
InChI=1S/C27H34N4O3/c1-19-17-21(25(32)30-15-7-6-10-20-9-4-5-11-23(20)30)13-14-22(19)18-28-27(34)31-16-8-12-24(31)26(33)29(2)3/h4-5,9,11,13-14,17,24H,6-8,10,12,15-16,18H2,1-3H3,(H,28,34)/t24-/m0/s1
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| Chemical Name |
(2S)-2-N,2-N-dimethyl-1-N-[[2-methyl-4-(2,3,4,5-tetrahydro-1-benzazepine-1-carbonyl)phenyl]methyl]pyrrolidine-1,2-dicarboxamide
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| Synonyms |
VA 106483; VA-106483; VA106483
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ≥ 125 mg/mL (~270.22 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.50 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.50 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (4.50 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1617 mL | 10.8087 mL | 21.6174 mL | |
| 5 mM | 0.4323 mL | 2.1617 mL | 4.3235 mL | |
| 10 mM | 0.2162 mL | 1.0809 mL | 2.1617 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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