JNJ-63533054 is a potent, selective and orally activeGPR139agonist with anEC₅₀of 16 nM forhumanGPR139(hGPR139). JNJ-63533054 shows selective forGPR139over other GPCRs, ion channels, and transporters. JNJ-63533054 can cross the blood-brain barrier (BBB)^[1][2].

EC50: 16 nM (Human GPR139), 63 nM (Rat GPR139) and 28 nM (Mouse GPR139)^[1]

JNJ-63533054 specifically activates human GPR139 in the calcium mobilization (EC₅₀of 16 nM) and GTPγS binding (EC₅₀of 17 nM) assays. JNJ-63533054 also activates the rat and mouse GPR139 receptor with similar potency (rat EC₅₀of 63 nM, mouse EC₅₀of 28 nM)^[1].
In a saturation study for human GPR139, a single population of high-affinity binding sites for [3H] JNJ-63533054 is observed (K_dof 10 nM). The B_maxvalue is 26 pmol/mg of protein. Saturation studies for the rat GPR139 and mouse GPR139 yielded K_dvalues within the same range (32 nM and 23 nM, respectively; B_max= 8.5 pmol/mg of protein and 6.2 pmol/mg of protein, respectively)^[1].

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 C_maxis 317 ng/mL (~1 μM), the t_1/2is 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].

316.78

Solid

C₁₇H₁₇ClN₂O₂

1802326-66-4

Room temperature in continental US; may vary elsewhere.

DMSO : ≥ 50 mg/mL(157.84 mM)

*"≥" means soluble, but saturation unknown.

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

• 1.

  请依序添加每种溶剂： 10% DMSO    40%PEG300   5%Tween-80   45% saline

  Solubility: ≥ 2.5 mg/mL (7.89 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (7.89 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

  将 0.9 g 氯化钠，完全溶解于 100 mL ddH2O 中，得到澄清透明的生理盐水溶液
• 2.

  请依序添加每种溶剂： 10% DMSO    90%corn oil

  Solubility: ≥ 2.5 mg/mL (7.89 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (7.89 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。