Tolvaptan , ≥98% , 150683-30-0

Synonym(s):
N-[4-[(7-Chloro-2,3,4,5-tetrahydro-5-hydroxy-1H-1-benzazepin-1-yl)carbonyl]-3-methylphenyl]-2-methylbenzamide;OPC 41061

CAS NO.：150683-30-0

Empirical Formula: C26H25ClN2O3

Molecular Weight: 448.94

MDL number: MFCD09838782

EINECS: 691-537-5

PRODUCT Properties

• Melting point: 219-222°C
• Boiling point: 594.4±50.0 °C(Predicted)
• Density: 1.311±0.06 g/cm3(Predicted)
• storage temp.: 2-8°C
• solubility: DMSO: ≥15mg/mL
• form: powder
• pka: 13.00±0.70(Predicted)
• color: white to tan
• InChIKey: GYHCTFXIZSNGJT-UHFFFAOYSA-N
• SMILES: C(NC1=CC=C(C(N2C3=CC=C(Cl)C=C3C(O)CCC2)=O)C(C)=C1)(=O)C1=CC=CC=C1C

Description and Uses

The potent antidiuretic hormone AVP orchestrates the regulation of free water absorption, body fluid osmolality, cell contraction, blood volume, and blood pressure through stimulation of three G-proteincoupled receptor subtypes:V₁-vascular types a and b, V₂-renal, and V₃-pituitary. Increased AVP secretion is the trademark of several pathophysiological disorders, including heart failure, impaired renal function, liver cirrhosis, and SIADH. As a consequence, these patients experience excess water retention or inadequate free-water excretion, which results in the dilution of sodium concentrations, frequently manifesting as clinical hyponatremia (serum sodium concentration <135 mmol/L). This electrolyte imbalance increases mortality rates by 60-fold. Selective antagonism of the AVP V₂receptor promotes water excretion without perturbing electrolyte balance making it an appealing target for preventing disease progression. Following the introduction of the dual AVP V_1a/V₂ receptor antagonist conivaptan, tolvaptan has recently been launched as a nonpeptide, selective V₂ receptor antagonist with potent aquaretic attributes for the treatment of hypervolemic and euvolemic hyponatremia (serum sodium concentration of <125 mmol/L or less distinct hyponatremia that is symptomatic and has resisted correction with fluid restriction). As a more potent and selective V₂ receptor antagonist, tolvaptan is a follow-up to mozavaptan, which possesses weak V₁ receptor antagonism and was approved for the treatment of SIADH in Japan. .

Tolvaptan (OPC-41061) is a selective, competitive arginine vasopressin receptor 2 antagonist with an IC50 of 1.28μM for the inhibition of AVP-induced platelet aggregation. Tolvaptan (OPC-41061) is used to treat hyponatremia (low blood sodium levels) assoc

Safety

• Symbol(GHS): GHS08
• Signal word: Warning
• Hazard statements: H362-H361
• Precautionary statements: P201-P260-P263-P264-P270-P308+P313-P201-P202-P281-P308+P313-P405-P501
• WGK Germany: 3