1. Signaling Pathways
  2. Metabolic Enzyme/Protease
  3. Tryptophan Hydroxylase

Tryptophan Hydroxylase

Tryptophan hydroxylase (TPH) is the rate-limiting enzyme in the biosynthesis of the biogenic monoamine serotonin (5-hydroxytryptamine, 5-HT). TPH belongs to the family of the aromatic amino acid hydroxylases, including phenylalanine hydroxylase (PAH) and tyrosine hydroxylase (TH), which all have a strict requirement for dioxygen, non-heme iron (II) and tetrahydrobiopterin (BH4).Tryptophan hydroxylase is activated by phosphorylating conditions (ATP-Mg2+) in a calcium-dependent, cyclic AMP-independent manner. Two existing TPH isoforms (TPH-1 and TPH-2) are responsible for the generation of two distinct serotonergic systems in vertebrates.

TPH1, predominantly expressed in the gastrointestinal tract and pineal gland, mediates 5-HT biosynthesis in non-neuronal tissues, while TPH2, mainly found in the raphe nuclei of the brain stem, is accountable for the production of 5-HT in the brain. TPH-1, the principal enzyme for peripheral serotonin biosynthesis, provides a novel target to design anabolic agents for osteoporosis. TPH2 is a phenotypic marker for serotonin neurons and is known to be extremely labile to oxidation. As a major modulator of 5-HT neurotransmission and the stress response, TPH2 is of both pathophysiological and pharmacological significance, and is emerging as a new therapeutic target for the treatment of stress disorders.

Tryptophan Hydroxylase Related Products (13):

Cat. No. Product Name Effect Purity
  • HY-B1368
    Fenclonine Inhibitor
    Fenclonine is a potent and irreversible inhibitor of tryptophan (Trp) hydroxylase, the rate-limiting enzyme in serotonin biosynthesis.
  • HY-13055B
    Telotristat Inhibitor 98.91%
    Telotristat (LP-778902) is a potent tryptophan hydroxylase inhibitor with an in vivo IC50 of 0.028 μM.
  • HY-13055A
    Telotristat ethyl Inhibitor 99.68%
    Telotristat ethyl (LX1032) is a novel, orally-delivered inhibitor of tryptophan hydroxylase that reduces serotonin production.
  • HY-15849A
    LP-533401 hydrochloride Inhibitor 98.62%
    LP-533401 hydrochloride is a tryptophan hydroxylase 1 inhibitor that regulates serotonin production in the gut.
  • HY-13055
    Telotristat etiprate Inhibitor
    Telotristat etiprate (LX1606 Hippurate) is a novel, orally-delivered inhibitor of tryptophan hydroxylase that reduces serotonin production.
  • HY-120083
    Rodatristat Inhibitor
    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.
  • HY-101124
    Rodatristat ethyl Inhibitor
    Rodatristat ethyl (KAR5585) is a first-in-class oral tryptophan hydroxylase 1 (TPH1) Inhibitor with nanomolar in vitro potency. Rodatristat ethyl reduces the level of 5-HT and significantly reduces pulmonary arterial hypertension (PAH).
  • HY-101456
    PCPA methyl ester hydrochloride Inhibitor 99.67%
    PCPA methyl ester hydrochloride (4-Chloro-DL-phenylalanine methyl ester hydrochloride), a reversible tryptophan hydroxylase inhibitor, is a serotonin (5-HT) synthesis inhibitor. PCPA methyl ester hydrochloride crosses the blood brain barrier and reduces 5-HT central availability.
  • HY-23460
    p-Ethynylphenylalanine Inhibitor 98.25%
    p-Ethynylphenylalanine (4-Ethynyl-L-phenylalanine) is a potent, selective, reversible and competitive inhibitor of tryptophan hydroxylase (TPH), with a Ki of 32.6 μM.
  • HY-13041
    LX-1031 Inhibitor 99.58%
    LX-1031 is a potent, orally available tryptophan 5-hydroxylase (TPH) inhibitor that reduces serotonin (5-HT) synthesis peripherally.
  • HY-15849
    LP-533401 Inhibitor ≥98.0%
    LP-533401 is a Tryptophan hydroxylase 1 inhibitor that regulates serotonin production in the gut.
  • HY-23460A
    p-Ethynylphenylalanine hydrochloride Inhibitor 99.42%
    p-Ethynylphenylalanine hydrochloride (4-Ethynyl-L-phenylalanine hydrochloride) is a potent, selective, reversible and competitive inhibitor of tryptophan hydroxylase (TPH), with a Ki of 32.6 μM.
  • HY-19572
    ACT-678689 Inhibitor
    ACT-678689 (Compound Example 1.53.4) is a tryptophan hydroxylase (TPH) inhibitor with an IC50 of 8 nM.
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