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2101737-32-8

2101737-32-8 structure
2101737-32-8 structure
  • Name: VU6000918
  • Chemical Name: VU6000918
  • CAS Number: 2101737-32-8
  • Molecular Formula: C18H17F2N5OS
  • Molecular Weight: 389.42
  • Catalog: Signaling Pathways GPCR/G Protein mAChR
  • Create Date: 2021-09-13 23:04:33
  • Modify Date: 2024-01-11 11:49:02
  • VU6000918 is a muscarinic acetylcholine (M4) positive allosteric modulator, with an EC50 of 19 nM for hM4[1].

Name VU6000918
Description VU6000918 is a muscarinic acetylcholine (M4) positive allosteric modulator, with an EC50 of 19 nM for hM4[1].
Related Catalog
Target

EC50: 19 nM (hM4)[1].

In Vitro VU6000918 demonstrates statistically significant AHL reversal (18%) from a low oral dose of 0.03 mg/kg and reaches maximal reversal (74%) from a 3 mg/kg dose, with a resulting in vivo plasma EC50 of 74 nM (0.66 nM unbound) based on terminal concentrations measured in the study animals (1.5 hr post-administration of 17j)[1].
References

[1]. James C Tarr, et al. Challenges in the development of an M 4 PAM preclinical candidate: The discovery, SAR, and in vivo characterization of a series of 3-aminoazetidine-derived amides. Bioorg Med Chem Lett. 2017 Jul 1;27(13):2990-2995.

Molecular Formula C18H17F2N5OS
Molecular Weight 389.42