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PDE10A-IN-2 hydrochloride
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
PDE10A-IN-2 hydrochloride图片
规格:98%
分子量:627.05
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议

产品介绍
PDE10A-IN-2 hydrochloride 是一种有效的,高选择性,具有口服活性的 磷酸二酯酶 10A (PDE10A) 的抑制剂,IC50 为 2.8 nM。PDE10A-IN-2 hydrochloride 对其他 PDE 亚型显示出大于 3500 倍的选择性,并可用于肺动脉高压 (PAH) 的研究。
货号:ajcx39228
CAS:N/A
分子式:C33H38Cl3N5O
分子量:627.05
溶解度:DMSO : 100 mg/mL (159.48 mM; Need ultrasonic)
纯度:98%
存储:Store at -20°C
库存:现货

Background:

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.

Protocol:

PDE10A

2.8nM(IC50)