JNJ-63533054 是一种有效的，选择性的，具有口服活性的 GPR139 激动剂，对人 GPR139 的EC₅₀ 为 16 nM。JNJ-63533054 对 GPR139 的选择性高于其他 GPCR，离子通道和转运蛋白。JNJ-63533054 可以穿过血脑屏障 (BBB)。

JNJ-63533054 is a potent, selective and orally active GPR139 agonist with an EC 50 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).

Solid

EC50: 16 nM (Human GPR139), 63 nM (Rat GPR139) and 28 nM (Mouse GPR139)

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).
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). has not independently confirmed the accuracy of these methods. They are for reference only.

JNJ-63533054 (3-30 mg/kg; oral administration; once; SD rats) treatment induces a dose-dependent reduction in locomotor activity in the first hour.
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 C max is 317 ng/mL (~1 μM), the t 1/2 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. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[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.

In Vitro: DMSO : ≥ 50 mg/mL (157.84 mM)配制储备液