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

Tryptophan Hydroxylase

Tryptophan Hydroxylase

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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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-B1368
    Fenclonine
    		Inhibitor 99.92%
    Fenclonine is a selective and irreversible tryptophan hydroxylase inhibitor, which is a rate-limiting enzyme in the biosynthesis of serotonin. Fenclonine can be used in carcinoid syndrome research.
    Fenclonine
  • HY-101456
    PCPA methyl ester hydrochloride
    		Inhibitor 99.89%
    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.
    PCPA methyl ester hydrochloride
  • HY-W019599
    4-Chloro-L-phenylalanine
    		Inhibitor ≥98.0%
    4-Chloro-L-phenylalanine (L-PCPA) is a 5-HT biosynthesis inhibitor. 4-Chloro-L-phenylalanine is also a nonspecific antagonist of both isoforms of tryptophan hydroxylase (TPH1 and TPH2).
    4-Chloro-L-phenylalanine
  • HY-13055B
    Telotristat
    		Inhibitor 99.42%
    Telotristat (LP-778902) is a potent tryptophan hydroxylase inhibitor with an in vivo IC50 of 0.028 μM.
    Telotristat
  • HY-13055
    Telotristat etiprate
    		Inhibitor 99.89%
    Telotristat etiprate (LX1606 Hippurate) is a novel, orally-delivered inhibitor of tryptophan hydroxylase that reduces serotonin production.
    Telotristat etiprate
  • HY-15849
    LP-533401
    		Inhibitor 98.68%
    LP-533401 is a Tryptophan hydroxylase 1 inhibitor that regulates serotonin production in the gut.
    LP-533401
  • HY-13041
    LX-1031
    		Inhibitor 99.14%
    LX-1031 is a potent, orally available tryptophan 5-hydroxylase (TPH) inhibitor that reduces serotonin (5-HT) synthesis peripherally.
    LX-1031
  • HY-13055A
    Telotristat ethyl
    		Inhibitor 99.79%
    Telotristat ethyl (LX1032) is a novel, orally-delivered inhibitor of tryptophan hydroxylase that reduces serotonin production.
    Telotristat ethyl
  • HY-15849A
    LP-533401 hydrochloride
    		Inhibitor 98.02%
    LP-533401 hydrochloride is a tryptophan hydroxylase 1 inhibitor that regulates serotonin production in the gut.
    LP-533401 hydrochloride
  • HY-23460
    p-Ethynylphenylalanine
    		Inhibitor 99.93%
    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. p-Ethynylphenylalanine is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    p-Ethynylphenylalanine
  • HY-101124
    Rodatristat ethyl
    		Inhibitor ≥98.0%
    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).
    Rodatristat ethyl
  • HY-W092533
    6-Fluorotryptophan
    		Inhibitor 99.55%
    6-Fluorotryptophan, a competitive inhibitor of tryptophan hydroxylase, produced a transient disruption of sleep in rats chronically implanted with EEG recording electrodes.
    6-Fluorotryptophan
  • HY-N0137
    Tetrahydropapaverine hydrochloride
    		Inhibitor 99.08%
    Tetrahydropapaverine hydrochloride is a tetrahydroisoquinoline (TIQ) compound with inhibitory effects on tryptophan hydroxylase (TPH) (IC50 = 5.7 μM). Tetrahydropapaverine hydrochloride decreases intracellular serotonin content in murine mastocytoma P815 cells, with an IC50 value of 6.2 μM. Tetrahydropapaverine hydrochloride can be used for studies on potential neurotoxicity in monoaminergic neurons.
    Tetrahydropapaverine hydrochloride
  • HY-23460A
    p-Ethynylphenylalanine hydrochloride
    		Inhibitor 99.23%
    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. p-Ethynylphenylalanine (hydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    p-Ethynylphenylalanine hydrochloride
  • HY-120083
    Rodatristat
    		Inhibitor 98.41%
    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.
    Rodatristat
  • HY-W772850
    Fenclonine hydrochloride
    		Inhibitor 98.60%
    Fenclonine hydrochloride is a selective and irreversible tryptophan hydroxylase inhibitor, which is a rate-limiting enzyme in the biosynthesis of serotonin. Fenclonine hydrochloride can be used in carcinoid syndrome research.
    Fenclonine hydrochloride
  • HY-157014
    TPT-004
    		Inhibitor 99.90%
    TPT-004 is a selective and oraly active tryptophan hydroxylases (TPH) inhibitor with IC50s of 77 nM and 16 nM for TPH1 and TPH2, repsectively. TPT-004 exhibits exceptional selectivity for TPH1 compared with other members of the AAAH family. TPT-004 shows efficacy peripheral serotonin attenuation and colorectal tumor growth in mice[1][2].
    TPT-004
  • HY-156093
    TPH1-IN-1
    		Inhibitor
    TPH1-IN-1 (compound 40) is a xanthine derivative and an inhibitor of tryptophan hydroxylase TPH1 (IC50: 110.1 nM). TPH1-IN-1 has good in vitro activity and liver microsome stability, and effectively inhibits adipocyte differentiation of T3-L1 cells.
    TPH1-IN-1
  • HY-13055E
    Telotristat besilate
    		Inhibitor
    Telotristat besilate is a potent tryptophan hydroxylase inhibitor with an in vivo IC50 of 0.028 μM.
    Telotristat besilate
  • HY-19596
    Fenprinast
    Fenprinast is a cromotyn-like bronchodilator used for the research of allergy and exercise-induced asthma. Fenprinast has oral bioactivity.
    Fenprinast
Cat. No. Product Name / Synonyms Application Reactivity