| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
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| ln Vitro |
Mozavaptan (OPC-31260) is around 100 times more specific for the V2 receptor and competitively inhibits AVP binding to the plasma membrane of rat kidney (V2 receptor) and liver (V1 receptor). Rat liver has a [3H]-AVP Kd value of 1.1 nM, while rat kidney has a concentration of 1.38 nM. Mozavaptan considerably decreased the Kd of [3H]-AVP in the rat liver and kidney (Kd for V1 receptor was 2.47 nM and 5.51 nM at dosages of 0.3 μM and 1 μM, respectively; Kd at 2.4 nM and 1 μM). At 0.3 μM and 1 μM dosages, the concentration of V2 receptor is 4.03 nM [1].
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| ln Vivo |
The oral medication mozavaptan (OPC-31260; 1–30 mg/kg) dose-dependently enhances urine flow and lowers urine osmolality in hydrated conscious rats [1]. In rats that have been sedated with alcohol and loaded with water, mozavaptan (OPC-31260; 10-100 μg/kg; intravenous; male Sprague-Dawley rats) therapy suppresses exogenous arginine vasopressin (AVP) in a dose-dependent way. impact of antidiuretics[1].
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| Animal Protocol |
Animal/Disease Models: Hydrated conscious rat (300-350 g) [1]
Doses: 1 mg/kg, 3 mg/kg, 10 mg/kg, 30 mg/kg Route of Administration: Oral Experimental Results: Dose-dependent increase in urinary flow and diminished urine osmolarity. |
| References |
[1]. Yamamura Y, et al. Characterization of a novel aquaretic agent, OPC-31260, as an orally effective, nonpeptide vasopressin V2 receptor antagonist. Br J Pharmacol. 1992 Apr;105(4):787-91.
[2]. Yamaguchi K, et al. Clinical implication of the antidiuretic hormone (ADH) receptor antagonist mozavaptan hydrochloride in patients with ectopic ADH syndrome. Jpn J Clin Oncol. 2011 Jan;41(1):148-52. |
| Molecular Formula |
C27H30CLN3O2
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|---|---|
| Molecular Weight |
464.006
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| CAS # |
138470-70-9
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| Related CAS # |
Mozavaptan;137975-06-5
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| SMILES |
CC1=CC=CC=C1C(=O)NC2=CC=C(C=C2)C(=O)N3CCCC(C4=CC=CC=C43)N(C)C.Cl
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| Synonyms |
OPC31260l; OPC31260; OPC 31260
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| 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 : ~20.83 mg/mL (~44.89 mM)
H2O : ~10 mg/mL (~21.55 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.48 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 (4.48 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 (4.48 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 | 2.1551 mL | 10.7756 mL | 21.5513 mL | |
| 5 mM | 0.4310 mL | 2.1551 mL | 4.3103 mL | |
| 10 mM | 0.2155 mL | 1.0776 mL | 2.1551 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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