| Bioactivity | VU0238441 is a pan muscarinic acetylcholine receptor (mAChR) positive allosteric modulator (PAM) with EC50s of 3.2 μM, 2.8 μM, 2.2 μM, 2.1 μM, >10 μM for M1, M2, M3, M5 and M4, respectively[1][2]. | |||||||||
| Target | EC50: 3.2 μM (M1), 2.8 μM (M2), 2.2 μM (M3), 2.1 μM (M5) and >10 μM (M4) | |||||||||
| Invitro | VU0238441 is an analogue of VU0119498[2]. | |||||||||
| Name | VU0238441 | |||||||||
| CAS | 85511-68-8 | |||||||||
| Formula | C16H9ClF3NO2 | |||||||||
| Molar Mass | 339.70 | |||||||||
| Appearance | Solid | |||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | |||||||||
| Storage |
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| Reference | [1]. Thomas M Bridges, et al. Chemical lead optimization of a pan G(q) mAChR M(1), M(3), M(5) positive allosteric modulator (PAM) lead. Part I: Development of the first highly selective M(5) PAM. Bioorg Med Chem Lett. 2010 Jan 15;20(2):558-62. [2]. Thomas M Bridges, et al. Discovery of the first highly M5-preferring muscarinic acetylcholine receptor ligand, an M5 positive allosteric modulator derived from a series of 5-trifluoromethoxy N-benzyl isatins. J Med Chem. 2009 Jun 11;52(11):3445-8. |