Molecular Formula | C16H9ClF3NO2 |
Molar Mass | 339.7 |
Density | 1.500±0.06 g/cm3(Predicted) |
Boling Point | 441.7±55.0 °C(Predicted) |
Solubility | Soluble in DMSO |
pKa | -3?+-.0.20(Predicted) |
Storage Condition | Sealed in dry,Room Temperature |
Use | VU0238441 is a potent agonist of human Muscarinic acetylcholine receptor M5 with EC50 of 2.1 μM. |
Target | M5 mAChR, M5 : 2.1μM(EC50), |
In vitro study | VU0238441 is an analogue of VU0119498. |
Reference Show more | [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. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.944 ml | 14.719 ml | 29.438 ml |
5 mM | 0.589 ml | 2.944 ml | 5.888 ml |
10 mM | 0.294 ml | 1.472 ml | 2.944 ml |
5 mM | 0.059 ml | 0.294 ml | 0.589 ml |
Biological activity | VU0238441 is a forward allosteric regulator (PAM) of pan-muscarinic acetylcholine receptor (mAChR). The EC50 values for M5, M3, M2, M1 and M4 are 2.1 μM, 2.2 μM, 2.8 μM, 3.2 μM and> 10 μM respectively. |
target | TargetValue mAChR M5 (Cell-free assay) 2.1 μM mAChR M3 (Cell-free assay) 2.2 μM mAChR M2 (Cell-free assay) 2.8 μM mAChR M1 (Cell-free assay) 3.2 μM mAChR M4 (Cell-free assay) >10 μM |
Target | Value |
mAChR M5 (Cell-free assay) | 2.1 μM |
mAChR M3 (Cell-free assay) | 2.2 μM |
mAChR M2 (Cell-free assay) | 2.8 μM |
mAChR M1 (Cell-free assay) | 3.2 μM |
mAChR M4 (Cell-free assay) | >10 μM |
in vitro study | VU0238441 is an analog of VU0119498. |