(R)-VU6008667 是 VU6008667 的活性对映异构体，是一种口服活性的乙酰胆碱受体 5 亚型 (M5 NAM) 抑制剂，IC50 值分别为 1.2 μM (human) 和 1.6 μM (rat)。(R)-VU6008667 对 M5 的选择性高于 M1-4，CNS 渗透率高。
货号:ajcx14332
CAS:2097818-14-7
分子式:C24H17ClF2N2O2
分子量：438.85
溶解度:DMSO: 100 mg/mL (227.87 mM)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

(R)-VU 6008667, an active enantiomer of VU6008667, is a orally active acetylcholine receptor subtype 5 (M5 NAM) inhibitor with IC50 values of 1.2 μM (human) and 1.6 μM (rat), respectively. (R)-VU6008667 is selective for M5 over M1-4, high CNS penetration[1].

(R)-VU6008667 (intravenous injection, 1mg/kg; orally administration, 3 mg/kg) displays the desired diminished elimination half-life (t1/2= 2.3 hr) driven by a smaller volume (Vss=7.4 L/kg) and higher clearance (CLp= 82 mL/min/kg), with moderate oral bioavailability (17% F) in rat. (PK study)[1].

[1]. Jung ME, et al.Discovery of indirubin derivatives as new class of DRAK2 inhibitors from high throughput screening.Bioorg Med Chem Lett. 2016 Jun 1;26(11):2719-23