(R)-VU 6008667 |
| カタログ番号GC38110 |
(R)-VU 6008667 は、VU 6008667 より活性の低い (R)-エナンチオマーであり、M5 NAM 活性を欠いています (IC50 > 10 μM)。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2097818-14-7
Sample solution is provided at 25 µL, 10mM.
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(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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