Rodatristat (KAR5417) 是一种有效的 tryptophan hydroxylase 1 (TPH1) 和 TPH2 抑制剂，其 IC50 值分别为 33 nM 和 7 nM，并显著降低小鼠肠道中的血清素 (5-HT) 水平。
货号:ajcx36464
CAS:1673568-73-4
分子式:C27H27ClF3N5O3
分子量：561.98
溶解度:N/A
纯度：98%
存储：Store at -20°C
库存：现货

Background:

Rodatristat (KAR5417) is a potent tryptophan hydroxylase 1 (TPH1) and TPH2 inhibitor with IC50s value of 33 nM and 7 nM, respectively, and shows robust reduction of intestinal serotonin (5-HT) levels in mice[1].

Rodatristat (10-50 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].

[1]. Goldberg DR, et al. Optimization of spirocyclic proline tryptophan hydroxylase-1 inhibitors. Bioorg Med Chem Lett. 2017 Feb 1;27(3):413-419.