VU 6008667
VU 6008667 Basic information
- Product Name:
- VU 6008667
- Synonyms:
-
- VU 6008667
- 5H-Imidazo[2,1-a]isoindol-5-one, 9b-(4-chloro-3-methylphenyl)-1-(3,4-difluorobenzoyl)-1,2,3,9b-tetrahydro-, (9bS)-
- CAS:
- 2092923-21-0
- MF:
- C24H17ClF2N2O2
- MW:
- 438.85
- Mol File:
- 2092923-21-0.mol
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VU 6008667 Chemical Properties
- Boiling point:
- 616.1±55.0 °C(Predicted)
- Density
- 1.48±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO: 100 mg/mL (227.87 mM)
- pka
- -2.76±0.40(Predicted)
- form
- Solid
- color
- Light yellow to yellow
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VU 6008667 Usage And Synthesis
Uses
VU 6008667 is a selective negative allosteric modulator of M5 NAM with IC50s of 1.2 μM and 1.6 μM for human M5 and rat M5, respectively. High CNS penetration[1].
in vivo
VU 6008667 (1 mg/kg)/PO (3 mg/kg, solution dose) displays a 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)[1].
Animal Model: | RAT (PK study)[1] |
Dosage: | 1 mg/kg; 3 mg/kg |
Administration: | oral adminstration |
Result: | Had a desired short half-life in rat (t1/2= 2.3 hr), with moderate oral bioavailability (17% F). |
IC 50
mAChR5
References
[1] McGowan KM et al, Continued optimization of the M5 NAM ML375: Discovery of VU6008667, an M5 NAM with high CNS penetration and a desired short half-life in rat for addiction studies. Bioorg Med Chem Lett. 2017 Mar 15;27(6):1356-1359. DOI:10.1016/j.bmcl.2017.02.020
VU 6008667Supplier
Shanghai EFE Biological Technology Co., Ltd.
- Tel
- 021-65675885 18964387627
- info@efebio.com
Fan De(Beijing) Biotechnology Co., Ltd.
- Tel
- 15911056312
- liming@bio-fount.com
TargetMol Chemicals Inc.
- Tel
- +1-781-999-5354 +1-00000000000
- marketing@targetmol.com
BOC Sciences
- Tel
- info@bocsci.com
ChemeGen(Shanghai) Biotechnology Co.,Ltd.
- Tel
- 18818260767
- sales@chemegen.com
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