Tryptophan Hydroxylase

Related Products

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 Inhibitors (15)

Tryptophan Hydroxylase Related Products (15):

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.

HY-15849A

LP-533401 hydrochloride	Inhibitor	98.02%
LP-533401 hydrochloride is a tryptophan hydroxylase 1 inhibitor that regulates serotonin production in the gut.

HY-13055

Telotristat etiprate	Inhibitor	99.90%
Telotristat etiprate (LX1606 Hippurate) is a novel, orally-delivered inhibitor of tryptophan hydroxylase that reduces serotonin production.

HY-13041

LX-1031	Inhibitor	98.32%
LX-1031 is a potent, orally available tryptophan 5-hydroxylase (TPH) inhibitor that reduces serotonin (5-HT) synthesis peripherally.

HY-13055A

Telotristat ethyl	Inhibitor	99.79%
Telotristat ethyl (LX1032) is a novel, orally-delivered inhibitor of tryptophan hydroxylase that reduces serotonin production.

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).

HY-157014

TPT-004	Inhibitor
TPT-004 is a TPH inhibitor. TPT-004 has superior pharmacokinetic and pharmacodynamic properties. TPT-004 also has good efficacy in preclinical models of peripheral serotonin attenuation and colorectal tumor growth.

HY-23460

p-Ethynylphenylalanine	Inhibitor	99.96%
p-Ethynylphenylalanine (4-Ethynyl-L-phenylalanine) is a potent, selective, reversible and competitive inhibitor of tryptophan hydroxylase (TPH), with a K_i 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.

HY-13055B

Telotristat	Inhibitor	99.76%
Telotristat (LP-778902) is a potent tryptophan hydroxylase inhibitor with an in vivo IC₅₀ of 0.028 μM.

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 K_i 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.

HY-15849

LP-533401	Inhibitor	98.68%
LP-533401 is a Tryptophan hydroxylase 1 inhibitor that regulates serotonin production in the gut.

HY-W092533

6-Fluorotryptophan	Inhibitor	99.37%
6-Fluorotryptophan, a competitive inhibitor of tryptophan hydroxylase, produced a transient disruption of sleep in rats chronically implanted with EEG recording electrodes.

HY-120083

Rodatristat	Inhibitor	99.11%
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	≥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).

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.

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