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Technical Data
| Formula | C26H25ClN2O3 |
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| Molecular Weight | 448.94 | CAS No. | 150683-30-0 | |
| Solubility (25°C)* | In vitro | DMSO | 90 mg/mL (200.47 mM) | |
| Water | Insoluble | |||
| Ethanol | Insoluble | |||
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
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Biological Activity
| Description | Tolvaptan (OPC-41061) is an orally effective nonpeptide arginine vasopressin V2 receptor antagonist with IC50 of 3 nM, used to treat hyponatremia. | ||
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| In vitro | Tolvaptan blocks the binding of [(3)H]AVP to human V(2) receptors with 29-fold greater selectivity than that for V(1a) receptors, and showed no inhibition of V(1b) receptors. Tolvaptan inhibits not only the binding of [(3)H]AVP but also the AVP-induced production of cyclic AMP in human V(2)-receptor-expressing HeLa cells. Tolvaptan shows marked aquaresis in healthy and diseased animals. [1] Tolvaptan causes a concentration-dependent inhibition of arginine vasopressin-induced cAMP production with an apparent IC(50) of 0.1 nM in autosomal dominant polycystic kidney disease (ADPKD) cells. Tolvaptan inhibits AVP-induced ERK signaling and cell proliferation. Tolvaptan inhibits AVP-induced Cl(-) secretion and decreases in vitro cyst growth of ADPKD cells cultured within a three-dimensional collagen matrix. [2] | ||
| In vivo | Tolvaptan improves hyponatremia, resulting in the prevention of death, and improves organ water retention in rat models with acute and chronic hyponatremia. Tolvaptan reduces cardiac preload without unfavorable effects on renal functions, systemic hemodynamics, or circulating neurohormones in dogs with heart failure (HF). Tolvaptan shows a decrease in kidney weight as well as in cyst and fibrosis volume in animal models of human polycystic kidney disease (PKD). [1] Tolvaptan markedly elevates electrolyte-free water clearance (E-CH(2)O) or aquaresis to a positive value and increases urinary Arginine vasopressin (AVP) excretion in rats with heart failure. [3] |
Protocol (from reference)
References
Customer Product Validation
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Data from [Data independently produced by Am J Physiol Renal Physiol, 2014, 306(3), F359-66]
Selleck's Tolvaptan has been cited by 4 publications
| Acidosis-induced activation of distal nephron principal cells triggers Gdf15 secretion and adaptive proliferation of intercalated cells [ Acta Physiol (Oxf), 2021, 10.1111/apha.13661] | PubMed: 33840159 |
| In vitro 3D phenotypic drug screen identifies celastrol as an effective in vivo inhibitor of polycystic kidney disease [ J Mol Cell Biol, 2020, 12(8):644-653] | PubMed: 31065693 |
| Cyclophosphamide-induced vasopressin-independent activation of aquaporin-2 in the rat kidney [Kim S, et al. Am J Physiol Renal Physiol, 2015, 309(5):F474-83] | PubMed: 26109089 |
| Tolvaptan as a tool in renal physiology [Miranda CA, et al. Am J Physiol Renal Physiol, 2014, 306(3):F359-66] | PubMed: 24305472 |
RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.
SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.