Bioactivity | VU0409106 is a potent and selective mGlu5 negative allosteric modulator (NAM) with an IC50 of 24 nM. VU0409106 shows anxiolytic effects in rat models in a concentration-dependent manner. VU0409106 also penetrates the blood-brain barrier (BBB)[1][2]. |
In Vivo | VU0409106 (10 mg/kg; i.p.; once) penetrates the blood-brain barrier (BBB) and demonstrates good brain to plasma ratio that near unity[1]. Animal Model: |
Name | VU0409106 |
CAS | 1276617-62-9 |
Formula | C15H11FN4O2S |
Molar Mass | 330.34 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. Felts AS, et al. Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety. Bioorg Med Chem Lett. 2013 Nov 1;23(21):5779-85. [2]. Morrison RD, et al. The role of aldehyde oxidase and xanthine oxidase in the biotransformation of a novel negative allosteric modulator of metabotropic glutamate receptor subtype 5. Drug Metab Dispos. 2012 Sep;40(9):1834-45. |