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Tocris/Tolvaptan/5181/10/10 mg

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货号: 5181/10

品牌: Tocris

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Description: Potent and selective vasopressin V₂ receptor antagonist; renoprotective and orally active

Alternative Names: OPC-41061

Chemical Name: N-[4-[(7-Chloro-2,3,4,5-tetrahydro-5-hydroxy-1H-1-benzazepin-1-yl)carbonyl]-3-methylphenyl]-2-methylbenzamide

Purity: ≥98% (HPLC)

Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity

Potent and selective competitive vasopressin V₂ receptor antagonist (K_i values are 0.06 and 12.3 nM for V₂ and V_1a receptors respectively). Decreases urine osmolality and increases serum sodium concentrations. Delays the onset of end-stage renal disease in a mouse model of polycystic kidney disease. Exhibits myocardial and renal protective effects in hypertensive heart failure rats. Orally active.

Compound Libraries

Tolvaptan is also offered as part of the Tocriscreen Plus and Tocriscreen Library of FDA-Approved Compounds. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt	448.94
Formula	C₂₆H₂₅ClN₂O₃
Storage	Store at +4°C
Purity	≥98% (HPLC)
CAS Number	150683-30-0
PubChem ID	216237
InChI Key	GYHCTFXIZSNGJT-UHFFFAOYSA-N
Smiles	OC1C2=C(C=CC(Cl)=C2)N(C(C3=C(C)C=C(NC(C4=CC=CC=C4C)=O)C=C3)=O)CCC1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	44.89	100
	ethanol	4.49	10

Preparing Stock Solutions

The following data is based on the product molecular weight 448.94. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	2.23 mL	11.14 mL	22.27 mL
5 mM	0.45 mL	2.23 mL	4.45 mL
10 mM	0.22 mL	1.11 mL	2.23 mL
50 mM	0.04 mL	0.22 mL	0.45 mL

Product Datasheets

Certificate of Analysis / Product Datasheet

Safety Datasheet

References

References are publications that support the products' biological activity.

Kondo et al (1999) 7-Chloro-5-hydroxy-1-[2-methyl-4-(2-methylbenzoyl-amino)benzoyl ]-2,3,4,5-tetrahydro-1H-1-benzazepine (OPC-41061): a potent, orally active nonpeptide arginine vasopressin V₂ receptor antagonist. Bioorg.Med.Chem. 7 1743 PMID: 10482466

Ghali et al (2009) Tolvaptan. Nat.Rev.Drug Discov. 8 611 PMID: 19644472

Aihara et al (2014) Tolvaptan delays the onset of end-stage renal disease in a polycystic kidney disease model by suppressing increases in kidney volume and renal injury. J.Pharmacol.Exp.Ther. 349 258 PMID: 24570071

Morooka et al (2012) Chronic administration of oral vasopressin type 2 receptor antagonist tolvaptan exerts both myocardial and renal protective effects in rats with hypertensive heart failure. Circ.Heart.Fail. 5 484 PMID: 22628529

Keywords: Tolvaptan, supplier, Tolvaptan, potent, selective, competitive, vasopressin, receptors, antagonists, V2, renal, cardial, protective, renoprotective, hyponatremia, OPC-41061, Vasopressin, Receptors, Vasopressin, Receptors, Tocris Bioscience

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