THPP-1 是SGC推荐的一个化学探针， 是有效的、具有口服活性的磷酸二酯酶10A (PDE10A) 的抑制剂，其对人和大鼠的 Ki 值分别为 1 nM 和 1.3 nM。THPP-1 具有良好的药理学特性。
| Cas No. | 1257051-63-0 |
| Canonical SMILES | O=C(C1=C2C=CC=CN2C=N1)N3CCC4=NC(C5=CC=C(N=C5)Cl)=NC(OCCOC)=C4C3 |
| 分子式 | C23H21ClN6O3 |
| 分子量 | 464.9 |
| 溶解度 | DMSO: 31.25 mg/mL (67.22 mM) |
| 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 | THPP-1, a SGC chemical probe, is a potent and orally bioavailable phosphodiesterase 10A (PDE10A) inhibitor, with Ki values of 1 nM and 1.3 nM for human and rat PDE10A, respectively. THPP-1 has excellent pharmacokinetic properties in preclinical species[1]. [1]. Smith SM, et al. The novel phosphodiesterase 10A inhibitor THPP-1 has antipsychotic-like effects in rat and improves cognition in rat and rhesus monkey. Neuropharmacology. 2013 Jan;64:215-23.
[2]. Vardigan JD, et al. Behavioral and qEEG effects of the PDE10A inhibitor THPP-1 in a novel rhesus model of antipsychotic activity. Psychopharmacology (Berl). 2016 Jul;233(13):2441-50. |
