| Bioactivity | JNJ-63533054 is a potent, selective and orally active GPR139 agonist with an EC50 of 16 nM for human GPR139 (hGPR139). JNJ-63533054 shows selective for GPR139 over other GPCRs, ion channels, and transporters. JNJ-63533054 can cross the blood-brain barrier (BBB)[1][2]. | ||||||||||||
| Target | EC50: 16 nM (Human GPR139), 63 nM (Rat GPR139) and 28 nM (Mouse GPR139) | ||||||||||||
| Invitro | JNJ-63533054 specifically activates human GPR139 in the calcium mobilization (EC50 of 16 nM) and GTPγS binding (EC50 of 17 nM) assays. JNJ-63533054 also activates the rat and mouse GPR139 receptor with similar potency (rat EC50 of 63 nM, mouse EC50 of 28 nM)[1]. In a saturation study for human GPR139, a single population of high-affinity binding sites for [3H] JNJ-63533054 is observed (Kd of 10 nM). The Bmax value is 26 pmol/mg of protein. Saturation studies for the rat GPR139 and mouse GPR139 yielded Kd values within the same range (32 nM and 23 nM, respectively; Bmax = 8.5 pmol/mg of protein and 6.2 pmol/mg of protein, respectively)[1]. | ||||||||||||
| In Vivo | JNJ-63533054 (3-30 mg/kg; oral administration; once; SD rats) treatment induces a dose-dependent reduction in locomotor activity in the first hour[1].The pharmacokinetics of JNJ-63533054 (Compound 7c; 1 mg/kg iv; 5 mg/kg po) in rat is examined. The IV clearance is 53 mL/min/kg, the Cmax is 317 ng/mL (~1 μM), the t1/2 is 2.5 hours, and JNJ-63533054 is able to cross the blood-brain barrier (BBB) with a brain to plasma ratio (b/p) of 1.2[2]. Animal Model: | ||||||||||||
| Name | JNJ-63533054 | ||||||||||||
| CAS | 1802326-66-4 | ||||||||||||
| Formula | C17H17ClN2O2 | ||||||||||||
| Molar Mass | 316.78 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Liu C, et al. GPR139, an Orphan Receptor Highly Enriched in the Habenula and Septum, Is Activated by the Essential Amino Acids L-Tryptophan and L-Phenylalanine. Mol Pharmacol. 2015 Nov;88(5):911-25. [2]. Dvorak CA, et al. Identification and SAR of Glycine Benzamides as Potent Agonists for the GPR139 Receptor. ACS Med Chem Lett. 2015 Jul 20;6(9):1015-8. |
JNJ-63533054
CAS: 1802326-66-4 F: C17H17ClN2O2 W: 316.78
JNJ-63533054 is a potent, selective and orally active GPR139 agonist with an EC50 of 16 nM for human GPR139 (hGPR139). J
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