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Tolvaptan

Catalog No. T2326 CAS 150683-30-0

Synonyms: OPC-41061

Tolvaptan (OPC-41061) is an orally bioavailable, selective, arginine vasopressin receptor 2 (V2, AVPR2) antagonist that can be used to treat hyponatremia.

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Tolvaptan, CAS 150683-30-0

Pack Size	Availability	Price/USD
1 mg	In stock	$ 32.00
2 mg	In stock	$ 45.00
5 mg	In stock	$ 74.00
10 mg	In stock	$ 117.00
25 mg	In stock	$ 217.00
50 mg	In stock	$ 383.00
100 mg	In stock	$ 509.00
500 mg	In stock	$ 1,150.00
1 mL * 10 mM (in DMSO)	In stock	$ 129.00

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Purity: 99.78%

Purity: 99.75%

Purity: 97%

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Storage & Solubility Information

Description	Tolvaptan (OPC-41061) is an orally bioavailable, selective, arginine vasopressin receptor 2 (V2, AVPR2) antagonist that can be used to treat hyponatremia.
Targets&IC50	V2 receptor:3 nM
In vitro	Tolvaptan reduces the pre-cardiac load in dogs with heart failure without adversely affecting renal function, systemic hemodynamics, or circulating neurohormones. In animal models of human polycystic kidney disease, Tolvaptan leads to a reduction in kidney weight and a decrease in cyst fibrosis and volume. Furthermore, Tolvaptan improves hyponatremia and prevents mortality in rat models of acute and chronic hyponatremia. In rats with heart failure, Tolvaptan significantly increases electrolyte-free water clearance (E-CH(2)O) and enhances the excretion of urinary arginine vasopressin.
In vivo	Tolvaptan demonstrates a concentration-dependent inhibition of arginine vasopressin (AVP)-induced cAMP production in cells affected by Autosomal Dominant Polycystic Kidney Disease (ADPKD), with an IC50 of 0.1 nM. It also suppresses AVP-induced ERK signaling and cell proliferation. Furthermore, Tolvaptan inhibits the secretion of chloride (-) induced by AVP and reduces the extracellular growth of cysts in ADPKD cells cultured in a three-dimensional collagen matrix. It inhibits the binding of [(3)H] AVP to human V(2) receptors with 29 times greater selectivity compared to the V(1a) receptor while showing no inhibitory effect on the V(1b) receptor. In HeLa cells induced by AVP, Tolvaptan inhibits not only the binding of [(3)H] AVP but also the expression of cyclic AMP.
Kinase Assay	Cell-free autophosphorylation assay using time-resolved fluorometry: Neratinib is prepared as 10 mg/mL stocks in DMSO and diluted in 25 mM HEPES (pH 7.5; 0.002 ng/mL-20 μg/mL). Purified recombinant COOH-terminal fragments of HER2 (amino acids 676-1255) or epidermal growth factor receptor (EGFR) (amino acids 645-1186) [diluted in 100 mM HEPES (pH 7.5) and 50% glycerol] is incubated with increasing concentrations of Neratinib in 4 mM HEPES (pH 7.5), 0.4 mM MnCl2, 20 μM sodium vanadate, and 0.2 mM DTT for 15 minutes at room temperature in 96-well ELISA plates. The kinase reaction is initiated by the addition of 40 μM ATP and 20 mM MgCl2 and allowed to proceed for 1 hour at room temperature. Plates are washed, and phosphorylation is detected using Europium-labeled anti-phospho-tyrosine antibodies (15 ng/well). After washing and enhancement steps, signal is detected using a Victor2 fluorescence reader (excitation wavelength 340 nm, emission wavelength 615 nm). The concentration of Neratinib that inhibits receptor phosphorylation by 50% (IC50) is calculated from inhibition curves.

Synonyms	OPC-41061
Molecular Weight	448.94
Formula	C26H25ClN2O3
CAS No.	150683-30-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: 4.5 mg/mL (10 mM)

DMSO: 44.9 mg/mL (100 mM)

References and Literature

1. Miyazaki T, et al. Cardiovasc Drug Rev, 2007, 25(1), 1-13. 2. Reif GA, et al. Am J Physiol Renal Physiol, 2011, 301(5), F12005-12013. 3. Veeraveedu PT, et al. Biochem Pharmacol, 2008, 75(6), 1322-1330.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Clinical Compound Library Anti-Cancer Approved Drug Library Anti-Cancer Drug Library EMA Approved Drug Library Pediatric Drug Library ReFRAME Related Library Inhibitor Library Anti-Cancer Compound Library Approved Drug Library NO PAINS Compound Library

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Tolvaptan 150683-30-0 Autophagy GPCR/G Protein Vasopressin Receptor antidiuretic hormone Inhibitor cell cycle OPC 41061 inhibit hyponatremia SIADH OPC41061 apoposis OPC-41061 inhibitor

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