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

Tryptophan Hydroxylase (色氨酸羟化酶)

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 相关产品 (13):

目录号 产品名 作用方式 纯度
  • HY-B1368
    Fenclonine Inhibitor
    Fenclonine 是有效的色氨酸羟化酶 (Trp) 的不可逆抑制剂,色氨酸羟化酶是 5-羟色胺生物合成的限速酶。
  • HY-13055A
    Telotristat ethyl Inhibitor 99.68%
    Telotristat ethyl (LX1032) 是一种可口服的色氨酸羟化酶抑制剂,能够减少血清素的产生。
  • HY-15849A
    LP-533401 hydrochloride Inhibitor 98.62%
    LP-533401 hydrochloride 是色氨酸羟化酶 1 (tryptophan hydroxylase 1) 抑制剂,可以调节肠道中血清素的产生。
  • HY-13055B
    Telotristat Inhibitor 98.91%
    Telotristat (LP-778902) 是一种有效的色氨酸羟化酶 (tryptophan hydroxylase) 抑制剂,在体内的 IC50 值为0.028 μM。
  • HY-13055
    Telotristat etiprate Inhibitor
    Telotristat etiprate (LX1606 Hippurate) 是色氨酸羟化酶抑制剂,能够减少血清素的产生。
  • HY-23460
    p-Ethynylphenylalanine Inhibitor 99.96%
    p-Ethynylphenylalanine (4-Ethynyl-L-phenylalanine) 是一种高效、选择性的,可逆、竞争性的色氨酸羟化酶 (TPH) 抑制剂,其 Ki 值为 32.6 μM。
  • HY-15849
    LP-533401 Inhibitor ≥98.0%
  • HY-13041
    LX-1031 Inhibitor 99.58%
    LX-1031 是一种有效的,可口服的 tryptophan 5-hydroxylase (TPH) 抑制剂,能够减少5-羟色胺的合成。
  • HY-23460A
    p-Ethynylphenylalanine hydrochloride Inhibitor 99.42%
    p-Ethynylphenylalanine hydrochloride (4-Ethynyl-L-phenylalanine hydrochloride) 是一种高效、选择性的,可逆、竞争性的色氨酸羟化酶 (TPH) 抑制剂,其 Ki 值为 32.6 μM。
  • HY-120083
    Rodatristat Inhibitor
    Rodatristat (KAR5417) 是一种有效的 tryptophan hydroxylase 1 (TPH1)TPH2 抑制剂,其 IC50 值分别为 33 nM 和 7 nM,并显著降低小鼠肠道中的血清素 (5-HT) 水平。
  • HY-101124
    Rodatristat ethyl Inhibitor
    Rodatristat ethyl (KAR5585) 是一种首创的,具有口服活性的 tryptophan hydroxylase 1 (TPH1) 抑制剂,具有体外纳摩尔浓度,可降低 5-hydroxytryptamine (5-HT) 的水平并显着降低肺动脉高压 (PAH),
  • HY-19572
    ACT-678689 Inhibitor
    ACT-678689 (Compound Example 1.53.4) 是一种色氨酸羟化酶 (TPH) 抑制剂,IC50 为 8 nM。
  • HY-101456
    PCPA methyl ester hydrochloride Inhibitor 99.67%
    PCPA methyl ester hydrochloride (4-Chloro-DL-phenylalanine methyl ester hydrochloride) 是一种可逆的色氨酸羟化酶 (tryptophan hydroxylase) 抑制剂,是 5-羟色胺 (5-HT) 合成抑制剂。PCPA methyl ester hydrochloride 可穿过血脑屏障,并降低 5-HT 的中枢利用率。
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