For research use only. Not for therapeutic Use.
VU0483605 is a potent and brain-penetrated mGlu1 receptor positive allosteric modulator (PAM). VU0483605 shows excellent mGlu1 PAM activity at both human and rat, with EC50 values of 390 and 356 nM, respectively[1].
VU0483605 proves superior with excellent mGlu1 PAM activity at both human (EC50 = 390 nM) and rat (EC50 = 356 nM, pEC50 = 6.45 ± 0.11, 113 ± 5% Glu Max) and no activity as an mGlu4 PAM (EC50 >10 μM)[1].
| Catalog Number | I010057 |
| CAS Number | 1623101-11-0 |
| Synonyms | 3-chloro-N-[3-chloro-4-(4-chloro-1,3-dioxoisoindol-2-yl)phenyl]pyridine-2-carboxamide |
| Molecular Formula | C20H10Cl3N3O3 |
| Purity | ≥95% |
| InChI | InChI=1S/C20H10Cl3N3O3/c21-12-4-1-3-11-16(12)20(29)26(19(11)28)15-7-6-10(9-14(15)23)25-18(27)17-13(22)5-2-8-24-17/h1-9H,(H,25,27) |
| InChIKey | HJQXPBKPTGWZCF-UHFFFAOYSA-N |
| SMILES | C1=CC2=C(C(=C1)Cl)C(=O)N(C2=O)C3=C(C=C(C=C3)NC(=O)C4=C(C=CC=N4)Cl)Cl |
| Reference | [1]. Cho HP, Garcia-Barrantes PM, Brogan JT, et al. Chemical modulation of mutant mGlu1 receptors derived from deleterious GRM1 mutations found in schizophrenics. ACS Chem Biol. 2014;9(10):2334-2346. |
