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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-B1368
    Fenclonine

    芬克洛宁

    Inhibitor 99.92%
    Fenclonine 是一种选择性和不可逆的色氨酸羟化酶 (tryptophan hydroxylase) 抑制剂,它是 5-羟色胺生物合成的限速酶。Fenclonine 可用于类癌综合征的研究。
    Fenclonine
  • HY-101456
    PCPA methyl ester hydrochloride

    4-氯-DL-苯基丙氨酸甲酯盐酸盐

    Inhibitor 99.89%
    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。
    PCPA methyl ester hydrochloride
  • HY-15849A
    LP-533401 hydrochloride Inhibitor 98.02%
    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。
    LP-533401 hydrochloride
  • HY-13055
    Telotristat etiprate

    特罗司他马尿酸盐

    Inhibitor 99.89%
    Telotristat etiprate (LX1606 Hippurate) 是色氨酸羟化酶抑制剂,能够减少血清素的产生。
    Telotristat etiprate
  • HY-13041
    LX-1031 Inhibitor 98.32%
    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。
    LX-1031
  • HY-13055A
    Telotristat ethyl

    特罗司他乙酯

    Inhibitor 99.79%
    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。
    Telotristat ethyl
  • HY-13055B
    Telotristat Inhibitor 99.76%
    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。
    Telotristat
  • HY-W019599
    4-Chloro-L-phenylalanine Inhibitor ≥98.0%
    4-Chloro-L-phenalanine (L-PCPA) 是一种 5-HT 生物合成抑制剂。4-Chloro-L-phenalanine 也是色氨酸羟化酶两种亚型(TPH1TPH2)的非特异性拮抗剂。
    4-Chloro-L-phenylalanine
  • HY-23460
    p-Ethynylphenylalanine Inhibitor 99.93%
    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。p-Ethynylphenylalanine 是一种点击化学试剂。它含有 Alkyne 基团,可以和含有 Azide 基团的分子发生铜催化的叠氮-炔环加成反应 (CuAAc)。
    p-Ethynylphenylalanine
  • HY-15849
    LP-533401 Inhibitor 98.68%
    LP-533401是调节肠道内5-羟色胺产生的色氨酸羟化酶1抑制剂。
    LP-533401
  • 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。p-Ethynylphenylalanine (hydrochloride) 是一种点击化学试剂。它含有 Alkyne 基团,可以和含有 Azide 基团的分子发生铜催化的叠氮-炔环加成反应 (CuAAc)。
    p-Ethynylphenylalanine hydrochloride
  • HY-120083
    Rodatristat Inhibitor 99.11%
    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。
    Rodatristat
  • HY-101124
    Rodatristat ethyl Inhibitor ≥98.0%
    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),
    Rodatristat ethyl
  • HY-W092533
    6-Fluorotryptophan Inhibitor 99.37%
    6-Fluorotryptophan 是一种色氨酸羟化酶 (tryptophan hydroxylase) 的竞争性抑制剂,作用于在长期植入脑电图记录电极的大鼠,可短暂中断睡眠。
    6-Fluorotryptophan
  • HY-19572
    ACT-678689 Inhibitor 99.91%
    ACT-678689 (Compound Example 1.53.4) 是一种色氨酸羟化酶 (TPH) 抑制剂,IC50 为 8 nM。
    ACT-678689
  • HY-156093
    TPH1-IN-1 Inhibitor
    TPH1-IN-1 (compound 40) 是黄嘌呤衍生物,是色氨酸羟化酶 (Tryptophan Hydroxylase) TPH1 抑制剂 (IC50: 110.1 nM)。TPH1-IN-1 具有良好的体外活性和肝微粒体稳定性,有效抑制 T3-L1 细胞的脂肪细胞分化。
    TPH1-IN-1
  • HY-157014
    TPT-004 Inhibitor 99.90%
    TPT-004 是一种 TPH 抑制剂。TPT-004 具有优异的药代动力学和药效学特性。TPT-004 在外周血清素衰减和结直肠肿瘤生长的临床前模型中也具有良好的疗效。
    TPT-004
  • HY-13055BR
    Telotristat (Standard) Inhibitor
    Telotristat (Standard)是 Telotristat 的分析标准品。本产品用于研究及分析应用。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。
    Telotristat (Standard)
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