tph 1

TPH1-IN-1 (compound 40) is a xanthine derivative and inhibitor of tryptophan hydroxylase TPH1, with an IC50 of 110.1 nM. It demonstrates robust in vitro activity and liver microsome stability, effectively impeding the adipocyte differentiation of T3-L1 cells [1].

Rodatristat ethyl (KAR5585) is a groundbreaking, orally active, and potent inhibitor of tryptophan hydroxylase 1 (TPH1) that significantly reduces 5-hydroxytryptamine (5-HT) levels and decreases pulmonary arterial hypertension (PAH) at low concentrations.

Rodatristat is an effective tryptophan hydroxylase 1 and TPH2 inhibitor (IC50s: 33 nM and 7 nM, respectively).

p-Ethynylphenylalanine hydrochloride (4-Ethynyl-L-phenylalanine HCL) is a novel, potent, and specific inhibitor of TPH[1]. Its potential to selectively and reversibly inhibit serotonin biosynthesis may contribute to characterizing the role of serotonin in behavioral and physiological activities[1].

ACT-678689 (Compound Example 1.53.4) is a tryptophan hydroxylase (TPH) inhibitor with an IC50 of 8 nM[1].

TPT-004, a TPH inhibitor, exhibits superior pharmacokinetic and pharmacodynamic properties, and demonstrates efficacy in preclinical models for attenuating peripheral serotonin [1] and impeding colorectal tumor growth.