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。
货号:ajcx16660
CAS:1257051-63-0
分子式:C23H21ClN6O3
分子量:464.9
溶解度:DMSO: 31.25 mg/mL (67.22 mM)
纯度:98%
存储:Store at -20°C
库存:
现货
Background:
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.