产品属性:
产品名称 | (R)-VU 6008667 |
规格 | 1mg、5mg、10mg、25mg、50mg、100mg、200mg、500mg |
货号 | EY-01Y17564 |
Cas No.: 2097818-14-7
别名: N/A
化学名: N/A
分子式: C24H17ClF2N2O2
分子量: 438.85
溶解度: DMSO: 100 mg/mL (227.87 mM)
储存条件: Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述:
(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
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