PDE10A-IN-2 hydrochloride is a potent, highly selective and orally active phosphodiesterase 10A (PDE10A) inhibitor with an IC 50 of 2.8 nM. PDE10A-IN-2 hydrochloride shows selectivity of >3500-fold against other PDE subtypes. PDE10A-IN-2 hydrochloride can be used for pulmonary arterial hypertension (PAH) research.
性状
Solid
IC50 & Target[1][2]
PDE10A 2.8 nM (IC50)
体内研究(In Vivo)
PDE10A-IN-2 hydrochloride (compound 14 3HCL; 2.5 mg/kg; oral administration; daily; for 3 weeks) treatment decreases the typical symptoms of PAH in rats.
In Sprague-Dawley rats, the pharmacokinetic study of PDE10A-IN-2 hydrochloride (compound 14 3HCL; 10 mg/kg) shows the oral bioavailability up to ~50%, and the T 1/2 is 5.2 hours (p.o.), and the C max is 272 ng/mL. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
参考文献
[1]. Yuncong Yang, et al. Discovery of highly selective and orally available benzimidazole-based phosphodiesterase 10 inhibitors with improved solubility and pharmacokinetic properties for treatment of pulmonary arterial hypertension. Acta Pharm Sin B. 2020 De
溶解度数据
In Vitro: DMSO : 100 mg/mL (159.48 mM; Need ultrasonic)配制储备液