Mozavaptan |
Catalog No.GC14880
One-Click Copy Product Info
|
novel competitive vasopressin receptor antagonist
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 137975-06-5
Sample solution is provided at 25 µL, 10mM.
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Mozavaptan (OPC31260) is a orally effective, nonpeptide vasopressin V2 receptor antagonist with an IC50 of 14 nM.
Mozavaptan causes a competitive displacement of [3H]-arginine vasopressin (AVP) binding to both V1 and V2 receptors with IC50 values of 1.2 μM and 14 nM, respectively. The Kd of [3H]-AVP is reduced significantly in both rat liver and kidney in the presence of mozavaptan (Kd=1.1 nM in liver, Kd=1.38 nM in kidney)[1].
Mozavaptan at doses of 10 to 100 μg/kg, i.v., inhibits the antidiuretic action of exogenously administered arginine vasopressin in water-loaded, alcohol-anaesthetized rats in a dose-dependent manner. Mozavaptan does not exert an antidiuretic activity suggesting that it is not a partial V2 receptor agonist. Mozavaptan dose-dependently increases urine flow and decreases urine osmolality after oral administration at doses of 1 to 30 mg/kg in normal conscious rats[1].
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.
Kinase experiment: | To determine binding kinetic constants, liver or kidney plasma membranes are incubated with increasing concentrations of [3H]-AVP with or without excess (1 μM) unlabelled AVP to obtain a saturation curve. To investigate whether mozavaptan interacts competitively or noncompetitively, the saturation binding of [3H]-AVP is examined in the absence and presence of mozavaptan at concentrations of 0.3 μM and 1 μM in liver membranes and 3 nM, and 10 nM in kidney membranes. Data on the saturation curve are plotted according to the method of Scatchard and fitted by a regression analysis[1]. |
Animal experiment: | Rats: Mozavaptan is dissolved in DMSO at a concentration of 10 mM and diluted with assay buffer. Female Brattleboro rats homozygous for hypothalamic diabetes insipidus and weighing between 180 and 280g are used. Mozavaptan (30 mg/kg) and vehicle (5% gum arabic) are administered orally in a volume of 2 mL/kg and d(CH2)5Tyr(Et)VAVP (10pgkg-1) is administered in a volume of 1 mL/kg. Spontaneously voided urine is collected for 6h with metabolic cages. Both before and during the study, the rats received water and food ad libitum[1]. |
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. | |
| Cas No. | 137975-06-5 | SDF | |
| Chemical Name | N-[4-[5-(dimethylamino)-2,3,4,5-tetrahydro-1-benzazepine-1-carbonyl]phenyl]-2-methylbenzamide | ||
| Canonical SMILES | CC1=CC=CC=C1C(=O)NC2=CC=C(C=C2)C(=O)N3CCCC(C4=CC=CC=C43)N(C)C | ||
| Formula | C27H29N3O2 | M.Wt | 427.54 |
| Solubility | DMSO : 6.2 mg/mL (14.50 mM; Need warming) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.339 mL | 11.6948 mL | 23.3896 mL |
| 5 mM | 467.8 μL | 2.339 mL | 4.6779 mL |
| 10 mM | 233.9 μL | 1.1695 mL | 2.339 mL |
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μL
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 6 reference(s) in Google Scholar.)