product name VU 0361737
Description: VU 0361737 is a selective positive allosteric modulator (PAM) for mGlu4 receptor with EC50 of 240 nM and 110 nM at human and rat receptors, respectively, it exibits weak activity at mGlu5 and mGlu8 receptors, is inactive at mGlu1, mGlu2, mGlu3, mGlu6 and mGlu7 receptors, and can penetrate into CNS.
References: J Med Chem. 2009 Jul 23;52(14):4115-8; J Med Chem. 2011 Feb 24;54(4):1106-10.
262.69
Formula
C13H11ClN2O2
CAS No.
1161205-04-4
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 53 mg/mL (201.8 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
Synonyms
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19423540
| In Vitro |
In vitro activity: VU0361737 is inactive at mGlu1, mGlu2, mGlu3, mGlu6 and mGlu7 receptors and displays weak activity at mGlu5 and mGlu8 receptors. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | VU0361737 shows high in vivo CL in rat, a short half-life (T1/2 20 min), and demonstrates significant brain exposure (brain-to-plasma ratio of 4.1). |
| Animal model | Sprague-Dawley rats |
| Formulation & Dosage | Dissolved in 10% Tween-80; 10 ml/kg; i.p. administration |
| References | J Med Chem. 2009 Jul 23;52(14):4115-8; J Med Chem. 2011 Feb 24;54(4):1106-10. |
