For research use only. Not for therapeutic Use.
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].
| Catalog Number | I038167 |
| CAS Number | 2101737-32-8 |
| Synonyms | 5-amino-N-[1-(2,3-difluorophenyl)azetidin-3-yl]-3,4-dimethylthieno[2,3-c]pyridazine-6-carboxamide |
| Molecular Formula | C18H17F2N5OS |
| Purity | ≥95% |
| InChI | InChI=1S/C18H17F2N5OS/c1-8-9(2)23-24-18-13(8)15(21)16(27-18)17(26)22-10-6-25(7-10)12-5-3-4-11(19)14(12)20/h3-5,10H,6-7,21H2,1-2H3,(H,22,26) |
| InChIKey | KWYCAGNWNMBWOL-UHFFFAOYSA-N |
| SMILES | CC1=C(N=NC2=C1C(=C(S2)C(=O)NC3CN(C3)C4=C(C(=CC=C4)F)F)N)C |
| Reference | [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. |
