Tolvaptan
- CAS No.
- 150683-30-0
- Chemical Name:
- Tolvaptan
- Synonyms
- SaMsca;Tolvptan;olvaptan;Toptan *;OPC-41061;OPC 41061;Tolvaptan;TOIVAPTAN;Tolvaptan-d7;Tolvaptan powder
- CBNumber:
- CB41454279
- Molecular Formula:
- C26H25ClN2O3
- Molecular Weight:
- 448.94
- MOL File:
- 150683-30-0.mol
- MSDS File:
- SDS
- Modify Date:
- 2024/4/10 13:06:19
| 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 |
SAFETY
Risk and Safety Statements
| 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 |
Tolvaptan price More Price(2)
Tolvaptan Chemical Properties,Uses,Production
Description
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 V1a/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. .
Chemical Properties
White Solid
Uses
Labelled Tolvaptan s, and the syndrome of inappropriate antidiuretic hormone (SIADH).
Clinical Use
Tolvaptan, also known as OPC-41061, is a selective, competitive arginine vasopressin receptor 2 antagonist used to treat hyponatremia (low blood sodium levels) associated with congestive heart failure, cirrhosis, and the syndrome of inappropriate antidiuretic hormone (SIADH). Otsuka Pharmaceutical licensed tolvaptan under the trade name Samsca after the FDA approved the drug in May 2009. Tolvaptan has also shown efficacy against polycystic kidney disease. In a 2004 trial, tolvaptan administered with traditional diuretics was noted to increase excretion of excess fluids and improve blood sodium levels in patients with heart failure without producing side effects such as hypotension (low blood pressure) or hypokalemia (decreased blood levels of potassium). The drug also exhibited no adverse effect on kidney function.
Side effects
The most common adverse events were thirst, dry mouth, asthenia, constipation, pollakiuria or polyuria, and hyperglycemia. The recommended starting dose is 15 mg daily with a daily 15-mg adjustment to a maximum of 60 mg daily to raise serum sodium concentration. Initiation should be in a hospital setting where serum sodium and volume status may be monitored since too rapid correction of hyponatremia (>12 mEq/L/24 h) can cause osmotic demyelination resulting in dysarthria, mutism, dysphagia, lethargy, spastic quadriparesis, seizures, coma, and death. In addition to avoiding concomitant use of strong CYP3A4 inhibitors, tolvaptan is contraindicated in settings of urgent need to raise serum sodium acutely, in patients with an inability to sense or appropriately respond to thirst, in hypovolemic hyponatremia conditions, and in anuric patients.
Tolvaptan Preparation Products And Raw materials
| Supplier | Tel | Country | ProdList | Advantage | Inquiry |
|---|---|---|---|---|---|
| Lewens Labs | +917043057100 | Gujarat, India | 30 | 58 | Inquiry |
| Lupin Ltd | +91-8019896181 +91-8019896181 | Maharashtra, India | 93 | 58 | Inquiry |
| Rivashaa Agrotech Biopharma Pvt. Ltd. | +91-26463395 +91-7926462688 | Gujarat, India | 1615 | 58 | Inquiry |
| Zydus Lifesciences Ltd. | +91-0265-2315243 +91-6358895661 | Gujarat, India | 89 | 58 | Inquiry |
| ASolution Pharmaceuticals Pvt Ltd | +91-9028098511 +91-9028098510 | Maharashtra, India | 15 | 58 | Inquiry |
| RPG Life Sciences Ltd | +91-2266606375 +91-2266606375 | Maharashtra, India | 15 | 58 | Inquiry |
| Aadivighnesh Chem Private Ltd. | 91-22-28020015 | Maharashtra, India | 119 | 58 | Inquiry |
| Manus Aktteva | +91 (79) 6512-3395 | New Delhi, India | 581 | 34 | Inquiry |
| ALKEM LABORATORIES LTD | +91 22 3982 99 99 | New Delhi, India | 27 | 58 | Inquiry |
| HETERO DRUGS LTD | +91 40 23704923 / 24 / 25 | New Delhi, India | 98 | 58 | Inquiry |
| Supplier | Advantage |
|---|---|
| Lewens Labs | 58 |
| Lupin Ltd | 58 |
| Rivashaa Agrotech Biopharma Pvt. Ltd. | 58 |
| Zydus Lifesciences Ltd. | 58 |
| ASolution Pharmaceuticals Pvt Ltd | 58 |
| RPG Life Sciences Ltd | 58 |
| Aadivighnesh Chem Private Ltd. | 58 |
| Manus Aktteva | 34 |
| ALKEM LABORATORIES LTD | 58 |
| HETERO DRUGS LTD | 58 |
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