VU0152100

VU0152100 is a positive allosteric modulator of M4 muscarinic acetylcholine receptors. It potentiates calcium mobilization induced by acetylcholine (ACh) in CHO-K1 cells expressing the rat M4 receptor with an EC50 value of 380 nM. VU0152100 is selective for M4 over M1, M2, M3 and M5 receptors, as well as a panel of 68 additional GPCRs, ion channels, transporters, and enzymes, but does bind to the benzodiazepine binding site of the GABAA receptor at 10 µM. It reduces cocaine-induced increases in locomotor activity and cocaine self-administration in mice when administered at a dose of 1 mg/kg.Formal Name: 3-amino-N-[(4-methoxyphenyl)methyl]-4,6-dimethyl-thieno[2,3-b]pyridine-2-carboxamide. CAS Number: 409351-28-6. Molecular Formula: C18H19N3O2S. Formula Weight: 341.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, DMSO:PBS (pH 7.2) (1:6): 0.14 mg/ml. lambdamax: 218, 283 nm. SMILES: O=C(C1=C(N)C2=C(C)C=C(C)N=C2S1)NCC3=CC=C(C=C3)OC. InChi Code: InChI=1S/C18H19N3O2S/c1-10-8-11(2)21-18-14(10)15(19)16(24-18)17(22)20-9-12-4-6-13(23-3)7-5-12/h4-8H,9,19H2,1-3H3,(H,20,22). InChi Key: MDNWGCQSCGNTKH-UHFFFAOYSA-N.