Top Suppliers:I want be here




150683-30-0

150683-30-0 structure
150683-30-0 structure
  • Name: Tolvaptan
  • Chemical Name: N-[4-(7-chloro-5-hydroxy-2,3,4,5-tetrahydro-1-benzazepine-1-carbonyl)-3-methylphenyl]-2-methylbenzamide
  • CAS Number: 150683-30-0
  • Molecular Formula: C26H25ClN2O3
  • Molecular Weight: 448.941
  • Catalog: Biochemical Inhibitor G protein coupled receptor(GPCR & G Protein) Vasopressin Receptor Antagonist
  • Create Date: 2018-02-09 08:00:00
  • Modify Date: 2025-08-20 19:34:01
  • Tolvaptan is a selective, competitive arginine vasopressin receptor 2 antagonist with an IC50 of 1.28μM for the inhibition of AVP-induced platelet aggregation.IC50 value: 1.28 uM (inhibition of AVP-induced platelet aggregation)Target: vasopressin receptor 2Tolvaptan (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) associated with congestive heart failure, cirrhosis, and the syndrome of inappropriate antidiuretic hormone (SIADH). Tolvaptan (OPC-41061) is also in fast-track clinical trials for polycystic kidney disease. Treatment with t tolvaptan (OPC-41061) causes rapid and sustained body weight reductions concurrent with increases in urine output, improves and/or normalizes serum sodium in hyponatremic patients, reduces signs and symptoms of congestion and increases thirst. However, tolvaptan (OPC-41061) has not been shown to decrease heart failure re-hospitalization or mortality. As an adjunct to standard therapy, tolvaptan (OPC-41061) is unique in that it is virtually the only novel agent tested in patients hospitalized for acute heart failure syndrome (AHFS) to reach its primary end point for short-term efficacy without causing deleterious side effects.

Name N-[4-(7-chloro-5-hydroxy-2,3,4,5-tetrahydro-1-benzazepine-1-carbonyl)-3-methylphenyl]-2-methylbenzamide
Synonyms (±)-4'-[(7-chloro-2,3,4,5-tetrahydro-5-hydroxy-1H-1-benzazepin-1-yl)carbonyl]-o-tolu-m-toluidide
Tolvaptan
UNII-21G72T1950
olvaptan
N-{4-[(7-Chloro-5-hydroxy-2,3,4,5-tetrahydro-1H-1-benzazepin-1-yl)carbonyl]-3-methylphenyl}-2-methylbenzamide
Benzamide, N-[4-[(7-chloro-2,3,4,5-tetrahydro-5-hydroxy-1H-1-benzazepin-1-yl)carbonyl]-3-methylphenyl]-2-methyl-
Samsca
benzazepine derivative,32
N-[4-(9-chloro-6-hydroxy-2-azabicyclo[5.4.0]undeca-8,10,12-triene-2-carbonyl)-3-methyl-phenyl]-2-methyl-benzamide
Description Tolvaptan is a selective, competitive arginine vasopressin receptor 2 antagonist with an IC50 of 1.28μM for the inhibition of AVP-induced platelet aggregation.IC50 value: 1.28 uM (inhibition of AVP-induced platelet aggregation)Target: vasopressin receptor 2Tolvaptan (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) associated with congestive heart failure, cirrhosis, and the syndrome of inappropriate antidiuretic hormone (SIADH). Tolvaptan (OPC-41061) is also in fast-track clinical trials for polycystic kidney disease. Treatment with t tolvaptan (OPC-41061) causes rapid and sustained body weight reductions concurrent with increases in urine output, improves and/or normalizes serum sodium in hyponatremic patients, reduces signs and symptoms of congestion and increases thirst. However, tolvaptan (OPC-41061) has not been shown to decrease heart failure re-hospitalization or mortality. As an adjunct to standard therapy, tolvaptan (OPC-41061) is unique in that it is virtually the only novel agent tested in patients hospitalized for acute heart failure syndrome (AHFS) to reach its primary end point for short-term efficacy without causing deleterious side effects.
Related Catalog
References

[1]. Friedman B, Cirulli J.Hyponatremia in critical care patients: Frequency, outcome, characteristics, and treatment with the vasopressin V(2)-receptor antagonist tolvaptan.J Crit Care. 2012 Aug 8.

[2]. Inomata T.Tolvaptan (vasopressin receptor antagonist).Nihon Rinsho. 2011 Nov;69 Suppl 9:408-11.

[3]. Vaduganathan M, Gheorghiade M, Pang PS, Konstam MA, Zannad F, Swedberg K, Grinfeld L, Burnett JC Jr, Krasa HB, Zimmer C, Blair J, Ouyang J, Maggioni AP; EVEREST investigators.Efficacy of oral tolvaptan in acute heart failure patients with hypotension and renal impairment.J Cardiovasc Med (Hagerstown). 2012 Jul;13(7):415-22.

[4]. Y Yamamura et al. OPC-41061, a Highly Potent Human Vasopressin V2-Receptor Antagonist: Pharmacological Profile and Aquaretic Effect by Single and Multiple Oral Dosing in Rats. J. Pharmacol. Exp. Ther. 1998, 287(3), 860-867.

[5]. RW Schrier et al. Tolvaptan, a Selective Oral Vasopressin V2-Receptor Antagonist, for Hyponatremia. N Engl J Med 2006, 355, 2099-2112.

Density 1.3±0.1 g/cm3
Boiling Point 594.4±50.0 °C at 760 mmHg
Melting Point 219-222°C
Molecular Formula C26H25ClN2O3
Molecular Weight 448.941
Flash Point 313.3±30.1 °C
Exact Mass 448.155365
PSA 69.64000
LogP 4.09
Appearance white to tan
Vapour Pressure 0.0±1.8 mmHg at 25°C
Index of Refraction 1.664
Storage condition Refrigerator
Water Solubility DMSO: ≥15mg/mL
RIDADR NONH for all modes of transport
The content on this webpage is sourced from various professional data sources. If you have any questions or concerns regarding the content, please feel free to contact service1@chemsrc.com.