| Description |
Rodatristat (KAR5417) is a potent tryptophan hydroxylase 1 (TPH1) inhibitor with an IC50 value of 33 nM, and shows robust reduction of intestinal serotonin (5-HT) levels in mice. Rodatristat also shows potent inhibition of TPH2 (IC50 of 7 nM)[1].
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| Related Catalog |
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| In Vivo |
Rodatristat (10 mg/kg and 50 mg/kg; oral administration; mice) treatment decreases intestinal 5-HT concentrations at 50 mg/kg, their efficacy drop off significantly at the lower 10 mg/kg dose[1]. Animal Model: Mice[1] Dosage: 10 mg/kg and 50 mg/kg Administration: Oral administration Result: Decreased intestinal 5-HT concentrations at 50 mg/kg, their efficacy dropped off significantly at the lower 10 mg/kg dose.
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| References |
[1]. Goldberg DR, et al. Optimization of spirocyclic proline tryptophan hydroxylase-1 inhibitors. Bioorg Med Chem Lett. 2017 Feb 1;27(3):413-419.
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