PDE10A-IN-2 hydrochloride |
| رقم الكتالوجGC65258 |
هيدروكلوريد PDE10A-IN-2 هو مثبط فوسفوديستيراز 10A (PDE10A) قوي ، انتقائي للغاية ونشط عن طريق الفم مع IC50 من 2.8 نانومتر
Products are for research use only. Not for human use. We do not sell to patients.
Sample solution is provided at 25 µL, 10mM.
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PDE10A-IN-2 hydrochloride is a potent, highly selective and orally active phosphodiesterase 10A (PDE10A) inhibitor with an IC50 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[1].
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[1].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 T1/2 is 5.2 hours (p.o.), and the Cmax is 272 ng/mL[1].
[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 Dec;10(12):2339-2347.
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