TP-024 (FTBMT) 是选择性的GPR52激动剂,EC50为 75 nM。TP-024 有抗精神病和促进认知活性。
生物活性 | TP-024 (FTBMT) is a selectiveGPR52agonist with anEC50of 75 nM[1]. TP-024 has antipsychotic and procognitive properties[2]. |
IC50& Target | |
体外研究 (In Vitro) | TP-024 (FTBMT) (0.1-10 μM) increases intracellular cAMP levels in CHO cells expressing human, mouse, or rat GPR52, with pEC50s of 7.03, 6.85, and 6.87, respectively[2].
Cell Viability Assay[1] Cell Line: | CHO cells (expressing GPR52 receptors) cAMP assay | Concentration: | 0.1-10 μM | Incubation Time: | 30 minutes | Result: | FTBMT activated cAMP signaling in vitro[1]. |
|
体内研究 (In Vivo) | TP-024 (FTBMT) (30 mg/kg, 90 minutes) exhibits antipsychotic-like activity without causing catalepsy in mice[2]. TP-024 (3 or 10 mg/kg, 48 hours) improves recognition and spatial working memory in rats[2]. TP-024 (3, 10, 30 mg/kg, 2 hours) stimulates neuronal activity in brain regions related to cognition[2].
Animal Model: | Male Long-Evans rats (9 weeks old)[2] | Dosage: | 10 mg/kg | Administration: | Oral, 1 hour before memory test | Result: | A 1-hour pretreatment with FTBMT (10 mg/kg, p.o.) significantly decreases the number of memory errors induced by MK-801[2]. |
Animal Model: | Male ICR mice (7 to 8 weeks old)[2] | Dosage: | 3–30 mg/kg | Administration: | Oral, 60 minutes before s.c. administration of MK-801 | Result: | FTBMT increases phospho-DARPP32 levels in the NAc slices[2]. |
|
分子量 | |
性状 | |
Formula | |
CAS 号 | |
运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | 4°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light) |
溶解性数据 | In Vitro: DMSO : 50 mg/mL(127.44 mM;Need ultrasonic) 配制储备液 1 mM | 2.5487 mL | 12.7437 mL | 25.4874 mL | 5 mM | 0.5097 mL | 2.5487 mL | 5.0975 mL | 10 mM | 0.2549 mL | 1.2744 mL | 2.5487 mL |
*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 (protect from light)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。 In Vivo: 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: ≥ 2.08 mg/mL (5.30 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (5.30 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 20.8 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。 2. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 2.08 mg/mL (5.30 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (5.30 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 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。 *以上所有助溶剂都可在本网站选购。
|