VU0152100|cas 409351-28-6|DC Chemicals

VU0152100|cas 409351-28-6|DC Chemicals

VU0152100 is a potent and selective allosteric potentiator of M4 mAChR with an EC50 of 380 ± 93 nM.

IC50 Value: 380 ± 93 nM (EC50)

Target: M4 mAChR

in vitro:  VU0152100 was selective for M4 relative to M1, M2, M3, and M5.

Product Name: VU0152100|Cat No: DC9497|Cas: 409351-28-6|Molecule Formular: C18H19N3O2S|Molecule Weight: 341.4274|Other names: VU0152100

VU0152100 is a potent and selective allosteric potentiator of M4 mAChR with an EC50 of 380 ± 93 nM.
in vitro:  VU0152100 was selective for M4 relative to M1, M2, M3, and M5.  VU0152100 dose-dependently potentiated the response to an EC20 concentration of ACh with EC50 values of 1.9 ± 0.2 ?M, and increased the maximal response to ACh to approximately 130%. VU0152100 (10 ?M) also enhanced the potency of ACh to induce GIRK-mediated thallium flux, as manifest by a robust (≈30-fold) leftward shift in the ACh CRC from 77 ± 1.2 nM (veh) to 2.35 ± 0.5 nM (VU0152100).
in vivo: Systemic administration of VU0152099 and VU0152100 provides robust brain levels of these compounds, the effects of VU0152099 and VU0152100 were evaluated in reversing amphetamine-induced hyperlocomotion in rats using a dose of 56.6 mg/kg i.p. for each compound with a 30-min pretreatment interval.

For research only, not for human use!