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JNJ-63533054

Chemical Structure : JNJ-63533054

CAS No.: 1802326-66-4

JNJ-63533054 (JNJ63533054;JNJ 63533054)

Catalog No.: PC-45741Not For Human Use, Lab Use Only.

JNJ-63533054 (JNJ63533054) is a potent, selective GPR139 agonist that specifically activates human GPR139 in the calcium mobilization with EC50 of 16 nM.

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Biological Activity

JNJ-63533054 (JNJ63533054) is a potent, selective GPR139 agonist that specifically activates human GPR139 in the calcium mobilization with EC50 of 16 nM.
JNJ-63533054 shows similar potency for rat and mouse GPR139 receptor (rat EC50 =63 nM, mouse EC50=28 nM).
JNJ-63533054 decreases spontaneous locomotor activity in rats; shows no cross-reactivity in a panel of 50 known GPCRs, ion channels, and transporters, and displays suitable pharmacokinetic properties for in vivo studies.
JNJ-63533054 is CNS-penetrable and orally bioavailable.

Physicochemical Properties

M.Wt 316.7821
Formula C17H17ClN2O2
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

Benzamide, 3-chloro-N-[2-oxo-2-[[(1S)-1-phenylethyl]amino]ethyl]-

References

1. Liu C, et al. Mol Pharmacol. 2015 Nov;88(5):911-25.

2. Dvorak CA, et al. ACS Med Chem Lett. 2015 Jul 20;6(9):1015-8.

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