For research use only. Not for therapeutic Use.
VU0364572 TFA is an orally active and selective allosteric agonist of the M1 muscarinic receptor with an EC50 of 0.11 μM. VU0364572 TFA has neuroprotective potential for preventing memory impairments and reducing neuropathology in Alzheimer’s Disease. VU0364572 TFA is CNS penetrant[1][3].
VU0364572 (30 μM; 25 min) TFA promotes KCNQ2, NR1 and MARCKS phosphorylation in striatal/NAc slices[2].
VU0364572 (10 mg/kg/day; oral; 4 months) TFA shows neuroprotective effects in 5XFAD transgenic Alzheimer’s mice. VU0364572 has a half life of 45 minutes[1].
| Catalog Number | I011317 |
| CAS Number | 1240514-89-9 |
| Synonyms | ethyl 4-[(3R)-3-[(2-methylbenzoyl)amino]piperidin-1-yl]piperidine-1-carboxylate;2,2,2-trifluoroacetic acid |
| Molecular Formula | C23H32F3N3O5 |
| Purity | ≥95% |
| InChI | InChI=1S/C21H31N3O3.C2HF3O2/c1-3-27-21(26)23-13-10-18(11-14-23)24-12-6-8-17(15-24)22-20(25)19-9-5-4-7-16(19)2;3-2(4,5)1(6)7/h4-5,7,9,17-18H,3,6,8,10-15H2,1-2H3,(H,22,25);(H,6,7)/t17-;/m1./s1 |
| InChIKey | QEFQJTFXOBPBLZ-UNTBIKODSA-N |
| SMILES | CCOC(=O)N1CCC(CC1)N2CCCC(C2)NC(=O)C3=CC=CC=C3C.C(=O)(C(F)(F)F)O |
| Reference | [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. [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. [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. |
