(R)-VU 6008667

Names

[ CAS No. ]:
2097818-14-7

[ Name ]:
(R)-VU 6008667

Biological Activity

[Description]:

(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].

[Related Catalog]:

Signaling Pathways >> Neuronal Signaling >> mAChR

Signaling Pathways >> GPCR/G Protein >> mAChR

[In Vivo]

(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].

[References]

[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

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₄H₁₇ClF₂N₂O₂

[ Molecular Weight ]:
438.85

(R)-VU 6008667

Names

Biological Activity

Chemical & Physical Properties

Related Compounds