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Tolvaptan

Catalog No. T2326 CAS 150683-30-0

Synonyms: OPC-41061

Tolvaptan 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: 99.75%

Purity: 97%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Tolvaptan is an orally bioavailable, selective, arginine vasopressin receptor 2 (V2, AVPR2) antagonist that can be used to treat hyponatremia.
Targets&IC50	vasopressin receptor 2:3 nM
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	448.941
Formula	C26H25ClN2O3
CAS No.	150683-30-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 2 years

Solubility Information

Ethanol: 4.5 mg/mL (10 mM)

DMSO: 44.9 mg/mL (100 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

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：

Endocrinology-Hormone Compound Library Orally Active Compound Library FDA-Approved & Pharmacopeia Drug Library Anti-Cancer Drug Library Drug-induced Liver Injury (DILI) Compound Library ReFRAME Related Library Anti-Cancer Clinical Compound Library NO PAINS Compound Library Inhibitor Library Autophagy Compound Library

Related Products

Related compounds with same targets

OPC-51803 Argipressin Atosiban d[Cha4]-AVP acetate(500170-27-4 free base) Conopressin S acetate(111317-90-9 free base) Terlipressin Acetate Felypressin Balovaptan

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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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 inhibit OPC-41061 hyponatremia SIADH OPC 41061 apoposis OPC41061 inhibitor

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