CM-675 是磷酸二酯酶 5 (PDE5)和I类组蛋白去乙酰化酶 (HDAC1) 的选择性抑制剂，其对 PDE5 和 HDAC1 的IC50 值分别为114 nM 和673 nM。CM-675 可用于阿尔兹海默症的研究。
货号:ajcx39558
CAS:1872466-47-1
分子式:C31H32N6O3
分子量：536.62
溶解度:DMSO : 25 mg/mL (46.59 mM; ultrasonic and warming and heat to 60°C)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

CM-675 is a dual phosphodiesterase 5 (PDE5) and class I histone deacetylases-selective inhibitor, with IC50 values of 114 nM and 673 nM for PDE5 and HDAC1, respectively. CM-675 has potential to treat Alzheimer's disease[1].

CM-675 (29a) shows a significant time-dependent effect on class I HDAC inhibition, particularly towards HDAC2. For HDAC1, its inhibitory potency also increased significantly (~1 log unit) with the pre-incubation time: 673 nM (30 min), 180 nM (4 hours) and 69 nM (6 hours) [1].

[1]. Rabal O, et al. Discovery of in Vivo Chemical Probes for Treating Alzheimer's Disease: Dual Phosphodiesterase 5 (PDE5) and Class I Histone Deacetylase Selective Inhibitors. ACS Chem Neurosci. 2019 Mar 20;10(3):1765-1782.

Protocol:

HDAC1 673nM(IC50,30min(time-dependent))

PDE5 114nMnM(IC50)