PF-184563 | V1a receptor antagonist | Probechem Biochemicals

Chemical Structure : PF-184563

PF-184563 (PF 184563)

Catalog No.: PC-21617Not For Human Use, Lab Use Only.

PF-184563 is a potent and selective vasopressin V1a antagonist with IC50 of 6.7 nM (hV1a).

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Biological Activity

PF-184563 is a potent and selective vasopressin V1a antagonist with IC50 of 6.7 nM (hV1a).
PF-184563 shows little binding to V1b or OT receptors (>10 μM).
PF-184563 dsiplays no significant inhibition of Cytochrome P450 (IC50 values >30 μM for CYP 1A2, 2C9, 2C19, 2D6 and 3A4) or blockade of the hERG channel.
PF-184563 shows weak binding hV2 receptor (IC50=8490 nM).

Physicochemical Properties

M.Wt	394.91
Formula	C21H23ClN6
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
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Solubility	10 mM in DMSO
Chemical Name/SMILES	8-chloro-5-methyl-1-(1-(pyridin-2-yl)piperidin-4-yl)-5,6-dihydro-4H-benzo[f][1,2,4]triazolo[4,3-a][1,4]diazepine

References

1. Johnson PS, et al. Bioorg Med Chem Lett. 2011 Oct 1;21(19):5684-7.

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PF-184563 (PF 184563)

Biological Activity

Physicochemical Properties

References

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