VU6000918 |
| Katalog-Nr.GC64970 |
VU6000918 ist ein muskarinischer Acetylcholin (M4) positiver allosterischer Modulator mit einem EC50 von 19 nM fÜr hM4.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2101737-32-8
Sample solution is provided at 25 µL, 10mM.
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VU6000918 is a muscarinic acetylcholine (M4) positive allosteric modulator, with an EC50 of 19 nM for hM4[1].
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].
[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.
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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