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OPC-51803

Catalog No. T28257 CAS 192514-54-8

Synonyms: SOU-003, SOU 003, SOU003, OPC51803, OPC 51803

OPC-51803 is an orally available nonapeptidylpressor (AVP) V(2) receptor selective agonist for the treatment of urinary incontinence and nocturia.

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OPC-51803, CAS 192514-54-8

Pack Size	Availability	Price/USD
1 mg	In stock	$ 350.00
5 mg	In stock	$ 828.00
10 mg	In stock	$ 1,130.00
25 mg	In stock	$ 1,590.00
50 mg	In stock	$ 1,980.00
100 mg	In stock	$ 2,500.00
500 mg	In stock	$ 4,900.00

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Purity: 100%

ee: 98.84%

Purity: 100%

ee: 99.06%

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Description	OPC-51803 is an orally available nonapeptidylpressor (AVP) V(2) receptor selective agonist for the treatment of urinary incontinence and nocturia.
Targets&IC50	V2 receptor:91.9+10.8 nM(Ki), cAMP:189+/-14 nM(EC50), V2 receptor:189+14 Nm(EC50), V1a receptor:819+39 nM(Ki)
In vitro	OPC-51803 and dDAVP displaced [(3)H]-AVP binding to human V(2)- and V(1a)-receptors with K(i) values of 91.9+/-10.8 nM (n = 6) and 3.12+/-0.38 nM (n = 6) for V(2)-receptors, and 819+/-39 nM (n = 6) and 41.5+/-9.9 nM (n = 6) for V(1a)-receptors, indicating that OPC-51803 was about nine times more selective for V(2)-receptors, similar to the selectivity of dDAVP.[5] OPC-51803 concentration-dependently increased cyclic adenosine 3', 5'-monophosphate (cyclic AMP) production in HeLa cells expressing human V(2)-receptors with an EC(50) value of 189+/-14 nM (n = 6).[5]
In vivo	OPC-51803 shows antidiuretic action in dogs. OPC-51803 (0.03 to 0.3 mg/kg; oral) decreased urine volume and increased urinary osmolality in a dose-dependent manner in water-loaded dogs.[4] OPC-51803 infusions (0.3 and 3 microg x kg(-1) x min(-1); Intravenous ) did not affect renal or systemic hemodynamics in anesthetized dogs.[4]

Synonyms	SOU-003, SOU 003, SOU003, OPC51803, OPC 51803
Molecular Weight	454
Formula	C26H32ClN3O2
CAS No.	192514-54-8

Storage

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

Solubility Information

DMSO: 45 mg/mL (99.12 mM)

References and Literature

1. Nakamura S, et al. Antidiuretic effects of a nonpeptide vasopressin V(2)-receptor agonist, OPC-51803, administered orally to rats. J Pharmacol Exp Ther. 2000 Dec;295(3):1005-11. 2. Nakamura S, et al. Effects of OPC-51803, a novel, nonpeptide vasopressin V2-receptor agonist, on micturition frequency in Brattleboro and aged rats. J Pharmacol Sci. 2003 Dec;93(4):484-8. 3. Mishra S, et al. Enantioselective Alkyne Conjugate Addition Enabled by Readily Tuned Atropisomeric P,N-Ligands. J Am Chem Soc. 2017 Feb 21. 4. Nakamura S, et al. Antidiuretic effects of a novel nonpeptide vasopressin V(2)-receptor agonist, OPC-51803, administered orally to dogs. J Pharmacol Sci. 2004 Apr;94(4):426-33. 5. Nakamura S, et al. Characterization of a novel nonpeptide vasopressin V(2)-agonist, OPC-51803, in cells transfected human vasopressin receptor subtypes. Br J Pharmacol. 2000;129(8):1700-1706.

Related compound libraries

This product is contained In the following compound libraries：

Membrane Protein-targeted Compound Library GPCR Compound Library Bioactive Compound Library Bioactive Compounds Library Max

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Keywords

OPC-51803 192514-54-8 GPCR/G Protein Vasopressin Receptor SOU-003 SOU 003 SOU003 OPC51803 OPC 51803 inhibitor inhibit

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