Catalog No.: PC-49746Not For Human Use, Lab Use Only.
HTL14242 (HTL0014242) a potent, selective mGlu5 negative allosteric modulator (NAM) with pKi of 9.3 and pIC50 of 9.2, shows high selectivity within the metabotropic family of GPCRs.
HTL14242 (HTL0014242) a potent, selective mGlu5 negative allosteric modulator (NAM) with pKi of 9.3 and pIC50 of 9.2, shows high selectivity within the metabotropic family of GPCRs.
HTL14242 displays 10-100 fold lower affinities and potencies than mavoglurant (pKi 8.0, pIC50 8.0) and dipraglurant (pKi 6.9, pIC50 6.9).
HTL0014242 (oral dose of 3 mg/kg) demonstrated 80% mGlu5 target receptor occupancy and in rats.
