| Identification | Back Directory | [Name]
[1,4'-Bipiperidine]-1'-carboxylic acid, 3-[(2-methylbenzoyl)amino]-, ethyl ester, (3R)- | [CAS]
1240514-87-7 | [Synonyms]
VU0364572
[1,4'-Bipiperidine]-1'-carboxylic acid, 3-[(2-methylbenzoyl)amino]-, ethyl ester, (3R)- | [Molecular Formula]
C21H31N3O3 | [MOL File]
1240514-87-7.mol | [Molecular Weight]
373.49 |
| Hazard Information | Back Directory | [Uses]
VU0364572 is a selective allosteric agonist of the M1 muscarinic receptor with an EC50 of 0.11 μM. VU0364572 has neuroprotective potential for preventing memory impairments and reducing neuropathology in Alzheimer’s Disease. VU0364572 is orally active and is CNS penetrant[1][3]. | [in vivo]
VU0364572 (10 mg/kg/day; oral; 4 months) shows neuroprotective effects in 5XFAD transgenic Alzheimer’s mice. VU0364572 has a half life of 45 minutes[1]. | [References]
[1] Lebois EP, et al. Disease-Modifying Effects of M1 Muscarinic Acetylcholine Receptor Activation in an Alzheimer's Disease Mouse Model. ACS Chem Neurosci. 2017 Jun 21;8(6):1177-1187. DOI:10.1021/acschemneuro.6b00278
[2] Faruk MO, et al. Muscarinic signaling regulates voltage-gated potassium channel KCNQ2 phosphorylation in the nucleus accumbens via protein kinase C for aversive learning. J Neurochem. 2022 Feb;160(3):325-341. DOI:10.1111/jnc.15555
[3] Lebois EP, et al. Development of a highly selective, orally bioavailable and CNS penetrant M1 agonist derived from the MLPCN probe ML071. Bioorg Med Chem Lett. 2011 Nov 1;21(21):6451-5. DOI:10.1016/j.bmcl.2011.08.084 |
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| Company Name: |
Biorbyt Ltd.
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+44 (0)1223 859 353 |
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http://www.biorbyt.com |
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