N-(4-{[(5R)-7-chloro-5-hydroxy-2,3,4,5-tetrahydro-1H-1-benzazepin-1-yl]carbonyl}-3-methylphenyl)-2-methylbenzamide
N-[4-(9-chloro-6-hydroxy-2-azabicyclo[5.4.0]undeca-8,10,12-triene-2-carbonyl)-3-methyl-phenyl]-2-methyl-benzamide
CAS: 150683-30-0
Molecular Formula: C26H25ClN2O3
N-(4-{[(5R)-7-chloro-5-hydroxy-2,3,4,5-tetrahydro-1H-1-benzazepin-1-yl]carbonyl}-3-methylphenyl)-2-methylbenzamide - Names and Identifiers
| Name | N-[4-(9-chloro-6-hydroxy-2-azabicyclo[5.4.0]undeca-8,10,12-triene-2-carbonyl)-3-methyl-phenyl]-2-methyl-benzamide |
| Synonyms | SaMsca OPC 41061 Tolvaptan OPC-41061 Tolvaptan Tablets N-[4-[(5R)-7-Chloro-5-hydroxy-2,3,4,5-tetrahydro-1-benzazepine-1-carbonyl]-3-methylphenyl]-2-methylbenzamide N-{4-[(7-chloro-5-hydroxy-2,3,4,5-tetrahydro-1H-1-benzazepin-1-yl)carbonyl]-3-methylphenyl}-2-methylbenzamide N-[4-(9-chloro-6-hydroxy-2-azabicyclo[5.4.0]undeca-8,10,12-triene-2-carbonyl)-3-methyl-phenyl]-2-methyl-benzamide N-(4-{[(5R)-7-chloro-5-hydroxy-2,3,4,5-tetrahydro-1H-1-benzazepin-1-yl]carbonyl}-3-Methylphenyl)-2-MethylbenzaMide N-(4-{[(5R)-7-chloro-5-hydroxy-2,3,4,5-tetrahydro-1H-1-benzazepin-1-yl]carbonyl}-3-methylphenyl)-2-methylbenzamide |
| CAS | 150683-30-0 |
| EINECS | 691-537-5 |
| InChI | InChI=1/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)/t24-/m1/s1 |
| InChIKey | GYHCTFXIZSNGJT-UHFFFAOYSA-N |
N-(4-{[(5R)-7-chloro-5-hydroxy-2,3,4,5-tetrahydro-1H-1-benzazepin-1-yl]carbonyl}-3-methylphenyl)-2-methylbenzamide - Physico-chemical Properties
| Molecular Formula | C26H25ClN2O3 |
| Molar Mass | 448.94 |
| Density | 1.311±0.06 g/cm3(Predicted) |
| Melting Point | 219-222°C |
| Boling Point | 594.4±50.0 °C(Predicted) |
| Flash Point | 313.3°C |
| Solubility | DMSO: ≥15mg/mL |
| Vapor Presure | 5.64E-15mmHg at 25°C |
| Appearance | powder |
| Color | white to tan |
| pKa | 13.00±0.70(Predicted) |
| Storage Condition | 2-8°C |
| Refractive Index | 1.663 |
| In vitro study | Tolvaptan inhibited [(3)H] AVP binding to human V(2) receptors 29-fold higher than V(1a) and did not exhibit inhibition of V(1B) receptors. Tolvaptan inhibits not only the binding of [(3)H] AVP but also the expression of cyclic AMP in HeLa cells induced by AVP. Tolvaptan showed significant nocturia in healthy and diseased animals. In autosomal dominant polycystic kidney disease (ADPKD) cells, Tolvaptan concentration-dependently inhibited arginine vasopressin-induced cAMP production with an IC50 of 0.1 nM. Tolvaptan inhibits AVP-induced ERK signaling and cell proliferation. Tolvaptan inhibits the secretion of chloride (-) by AVP and reduces the growth of cysts in vitro by ADPKD cells cultured in a three-dimensional collagen matrix. |
| In vivo study | In rat models-acute and chronic hyponatremia, Tolvaptan ameliorates hyponatremia, leading to prevention of death, and may improve organ water retention. Tolvaptan reduced cardiac preload without adversely affecting renal function, Systemic Hemodynamics, or circulating neurohormones in heart failure (HF) dogs. In an animal model of human polycystic kidney disease (PKD), Tolvaptan results in reduced kidney weight and cystic fibrosis and volume. In rat models-acute and chronic hyponatremia, Tolvaptan significantly increased the gap in the absence of electrolyte water (E-CH(2)O) or positive in aquaresis and increased urinary arginine vasopressin (AVP). Excretion in heart failure rats. |
N-(4-{[(5R)-7-chloro-5-hydroxy-2,3,4,5-tetrahydro-1H-1-benzazepin-1-yl]carbonyl}-3-methylphenyl)-2-methylbenzamide - Risk and Safety
| WGK Germany | 3 |
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CAS: 150683-30-0
Tel: +86-571-88162785
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QQ: 472954302
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CAS: 150683-30-0
Tel: +86-571-88162785
Email: Lucy@verypharm.com
Mobile: +86-13606544505
QQ: 472954302
Product List: View Catalog
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