Tolvaptan (Synonyms: OPC 41061) |
| Katalog-Nr.GC15575 |
Tolvaptan ist ein selektiver, kompetitiver und oral wirksamer Vasopressinrezeptor 2 (V2R)-Antagonist mit einer IC50 von 1,28 μM zur Hemmung der Arginin-Vasopressin (AVP)-induzierten Thrombozytenaggregation.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 150683-30-0
Sample solution is provided at 25 µL, 10mM.
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Tolvaptan is a selective and oral active antagonist of arginine vasopressin (AVP) V2-receptor with Ki value of 0.43nM [1].
Tolvaptan is a nonpeptide AVP V2-receptor antagonist. It prevents AVP from binding to V2-receptor. In the in vitro binding assay using HeLa cells expressing human AVP receptor subtypes, tolvaptan shows inhibitory activity against V2 and V1a receptors with Ki values of 0.43nM and 12.3nM, respectively. The V1b receptor and 30 other receptors or ion channels are not sensitive to tolvaptan, indicating that tolvaptan is selective to V2-receptor. Tolvaptan also inhibits the production of cAMP induced by AVP with IC50 value of 8nM [1].
In animal models, the tolvaptan induced aquaresis results in increased urine volume and serum sodium. In rat models of acute and chronic hyponatremia, administration of tolvaptan increases plasma sodium levels and decreases the mortality [1].
References:
[1] Miyazaki T, Fujiki H, Yamamura Y, et al. Tolvaptan, an Orally Active Vasopressin V2-Receptor Antagonist-Pharmacology and Clinical Trials. Cardiovascular drug reviews, 2007, 25(1): 1-13.
| Cas No. | 150683-30-0 | SDF | |
| Überlieferungen | OPC 41061 | ||
| Chemical Name | N-[4-(7-chloro-5-hydroxy-2,3,4,5-tetrahydro-1-benzazepine-1-carbonyl)-3-methylphenyl]-2-methylbenzamide | ||
| Canonical SMILES | CC1=CC=CC=C1C(=O)NC2=CC(=C(C=C2)C(=O)N3CCCC(C4=C3C=CC(=C4)Cl)O)C | ||
| Formula | C26H25ClN2O3 | M.Wt | 448.94 |
| Löslichkeit | ≥ 17.8mg/mL in DMSO | 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 | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.2275 mL | 11.1373 mL | 22.2747 mL |
| 5 mM | 0.4455 mL | 2.2275 mL | 4.4549 mL |
| 10 mM | 0.2227 mL | 1.1137 mL | 2.2275 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
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Calculation results:
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 ddH2O, 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%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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