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OPC-51803

Chemical Structure : OPC-51803

CAS No.: 192514-54-8

OPC-51803 (OPC 51803, OPC51803)

Catalog No.: PC-27932Not For Human Use, Lab Use Only.

OPC-51803 (OPC 51803, OPC51803) is a potent, selective, nonpeptide vasopressin V(2) receptor (V2R) agonist, displaced [3H]-AVP binding to human V2R with Ki of 91.9 nM, 9-fold selective over V1aR.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

OPC-51803 (OPC 51803, OPC51803) is a potent, selective, nonpeptide vasopressin V(2) receptor (V2R) agonist, displaced [3H]-AVP binding to human V2R with Ki of 91.9 nM, 9-fold selective over V1aR.
OPC-51803 concentration-dependently increased cyclic adenosine 3′, 5′-monophosphate (cyclic AMP) production in HeLa cells expressing human V2-receptors with an EC50 of 189 nM, does not increase the intracellular Ca2+ concentration ([Ca2+]i) in HeLa cells expressing human V1a-receptors.
OPC-51803 is the first nonpeptide agonist for human AVP V2-receptors without agonistic activities for V1a- and V1b-receptors.

Physicochemical Properties

M.Wt 454.01
Formula C26H32ClN3O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(R)-2-(1-(2-chloro-4-(pyrrolidin-1-yl)benzoyl)-2,3,4,5-tetrahydro-1H-benzo[b]azepin-5-yl)-N-isopropylacetamide

References

1. Nakamura S, et al. Br J Pharmacol. 2000 Apr;129(8):1700-6.

2. Nakamura S, et al. J Pharmacol Exp Ther. 2000 Dec;295(3):1005-11.

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