tph a

TPh A (Triphenyl Compound A) is an inhibitor of the nuclear protein pirin (Ki: 0.6 uM), a protein that can be used as a bioprobe to regulate pirin-related functions.

TPH2 agonist-1 (compound 20e) is an orally active TPH2 agonist that can penetrate the blood-brain barrier and is derived from 1,3,4-oxadiazol-2(3H)-one. In models with SCN1A defects, TPH2 agonist-1 enhances TPH2 expression and increases levels of 5-HT and GABA, demonstrating anticonvulsant activity. It stabilizes neuronal network electrophysiological activity and suppresses abnormal spike and burst activities. TPH2 agonist-1 shows no significant hERG inhibition or cytotoxicity and is suitable for studies related to severe myoclonic epilepsy in infancy (Dravet syndrome).

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].

p-Ethynylphenylalanine (4-Ethynyl-L-phenylalanine), a selective, effective, and reversible tryptophan hydroxylase (TPH) inhibitor, exhibits competitive inhibition with a Ki of 32.6 μM.

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].

LP-533401 hydrochloride is a peripheral Tph inhibitor that cannot cross the blood-brain barrier that inhibits 5-hydroxytryptamine synthesis and can be used to study periodontal disease and hepatic steatosis.

AGN-2979 is a tryptophan hydroxylase (TPH) activation inhibitor that shows antidepressant properties in rodent models of depression.

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.