PQ-10 是一种有效的磷酸二酯酶 10A (PDE10A) 抑制剂，IC50 和 ED50 分别为 4.6 nM 和 13 mg/kg。
| Cas No. | 927691-21-2 |
| 别名 | 6,7-二甲氧基-4-[(3R)-3-(2-喹喔啉基氧基)-1-吡咯烷基]喹唑啉 |
| Canonical SMILES | COC1=CC2=C(C(N3CC[C@@H](OC4=NC(C=CC=C5)=C5N=C4)C3)=NC=N2)C=C1OC |
| 分子式 | C22H21N5O3 |
| 分子量 | 403.4 |
| 溶解度 | DMF: 25 mg/mL,DMF:PBS (pH 7.2) (1:20): 0.04 mg/mL,DMSO: 16 mg/mL |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | PQ-10 is a potent and selective inhibitor of phosphodiesterase type 10 (PDE10; Ki = 4 nM). It has >38-fold selectivity for PDE10 over a panel of 60 CNS-associated receptors, enzymes, and ion channels in vitro. Subcutaneous injection of PQ-10 (32 mg/kg) leads to increases in striatal cGMP and phosphorylation of cAMP response element binding protein (CREB) in murine striatum, known markers of in vivo PDE10 inhibition. PQ-10 at a dose of 0.3 mg/kg, p.o., reduces scopolamine- and MK-801-induced memory deficits in rats. PQ-10 also inhibits tumor cell growth with IC50 values of 0.29 and 0.22 mM for HCT116 and SW480 colon cancer cells, respectively. |
