Size | Price | Stock | Qty |
---|---|---|---|
5mg |
|
||
10mg |
|
||
25mg |
|
||
50mg |
|
||
100mg |
|
||
250mg |
|
||
500mg |
|
||
Other Sizes |
|
Purity: ≥98%
Tolvaptan (formerly OPC41061; OPC-41061; trade names Samsca; Jinarc; Resodim) is a selective, competitive, orally bioavailable and nonpeptide antagonist of arginine vasopressin V2 receptor with anti-hypernatremic activity. It inhibits the arginine vasopressin V2 receptor with an IC50 of 3 nM. The use of tolvaptan to treat hyponatremia has been approved. Vasopressin receptor 2 antagonists such as tolvaptan are used to treat hyponatremia, or low blood sodium levels, which is linked to cirrhosis, congestive heart failure, and the syndrome of inappropriate antidiuretic hormone (SIADH).
Targets |
vasopressin receptor 2 ( IC50 = 3 nM )
|
|
---|---|---|
ln Vitro |
|
|
ln Vivo |
|
|
Cell Assay |
Cell Line: HepG2 cells
Concentration: 0-100 μM Incubation Time: 24, 48, 96 and 168 hours Result: Time- and dose-dependently inhibited HepG2 cells with IC50s of >100, 52.2, 33.0 and 27.1 μM at 24, 48, 96 and 168 hours, respectively. |
|
Animal Protocol |
Male albino rats with cyclophosphamide intraperitoneal injection
10 mg/kg Oral gavage; 10 mg/kg once per day; for 22 days |
|
References |
Molecular Formula |
C26H25CLN2O3
|
---|---|
Molecular Weight |
448.94
|
Exact Mass |
448.16
|
Elemental Analysis |
C, 69.56; H, 5.61; Cl, 7.90; N, 6.24; O, 10.69
|
CAS # |
150683-30-0
|
Related CAS # |
Tolvaptan-d7; 1246818-18-7
|
Appearance |
Solid powder
|
SMILES |
N-[4-(7-chloro-5-hydroxy-2,3,4,5-tetrahydro-1-benzazepine-1-carbonyl)-3-methylphenyl]-2-methylbenzamide
|
InChi Key |
GYHCTFXIZSNGJT-UHFFFAOYSA-N
|
InChi Code |
InChI=1S/C26H25ClN2O3/c1-16-6-3-4-7-20(16)25(31)28-19-10-11-21(17(2)14-19)26(32)29-13-5-8-24(30)22-15-18(27)9-12-23(22)29/h3-4,6-7,9-12,14-15,24,30H,5,8,13H2,1-2H3,(H,28,31)
|
Chemical Name |
N-[4-(7-chloro-5-hydroxy-2,3,4,5-tetrahydro-1-benzazepine-1-carbonyl)-3-methylphenyl]-2-methylbenzamide
|
Synonyms |
OPC41061; Tolvaptan; OPC 41061; OPC-41061; trade names Samsca; Jinarc; Resodim
|
HS Tariff Code |
2934.99.9001
|
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)
|
Solubility (In Vitro) |
|
---|
Preparing Stock Solutions | 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 |
*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.
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT06171100 | Recruiting | Drug: Tolvaptan | Hyponatremia SIADH |
King's College Hospital NHS Trust | December 15, 2023 | N/A |
NCT05569655 | Recruiting | Drug: Tolvaptan Drug: Furosemide |
Pulmonary Arterial Hypertension Randomized Controlled Trial |
Chinese Pulmonary Vascular Disease Research Group |
April 6, 2021 | Not Applicable |
NCT04782258 | Recruiting | Drug: Tolvaptan Suspension Drug: Tolvaptan Tablets |
ARPKD | Otsuka Pharmaceutical Development & Commercialization, Inc. |
July 15, 2022 | Phase 3 |
NCT03406286 | Recruiting | Drug: Tolvaptan | Safety | Korea Otsuka Pharmaceutical Co., Ltd. |
July 19, 2016 | N/A |
NCT04790175 | Recruiting | Drug: Tolvaptan (SAMSCA) |
Antidiuretic Hormone, Inappropriate Secretion |
Otsuka Pharmaceutical Co., Ltd. | March 29, 2021 | N/A |
Effect of tolvaptan on intracellular cAMP levels in ADPKD cells stimulated with AVP. Am J Physiol Renal Physiol . 2011 Nov;301(5):F1005-13. td> |
Effect of tolvaptan on AVP-induced proliferation of human ADPKD and normal human kidney (NHK) cells. Am J Physiol Renal Physiol . 2011 Nov;301(5):F1005-13. td> |
Diuretic effects of the administration of tolvaptan alone and furosemide alone during 6 h post dosing in normal conscious beagle dogs. Cardiovasc Drug Rev . 2007 Spring;25(1):1-13. td> |
Effect of AVP and tolvaptan on ERK activation in human ADPKD cells. Am J Physiol Renal Physiol . 2011 Nov;301(5):F1005-13. td> |