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Chemical Structure : HTL14242
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.
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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.
| M.Wt | 310.72 | |
| Formula | C16H8ClFN4 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Bennett KA, et al. Adv Pharmacol. 2020;88:35-58.
2. Bennett KA, et al. J Pharmacol Exp Ther. 2021 Apr;377(1):157-168.
3. Christopher JA, et al. J Med Chem 58:6653–6664.
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