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.
| 货号 | 产品名 | Cas | 产品描述 |
|---|---|---|---|
| PL11832 | LP-533401 hydrochloride | 1040526-12-2 | 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。 |
| PL12479 | p-Ethynylphenylalanine | 278605-15-5 | 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。 |
| PL12478 | p-Ethynylphenylalanine hydrochloride | 188640-63-3 | 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。 |
| PL09228 | PCPA methyl ester hydrochloride | 14173-40-1 | 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。 |
| PL12483 | Rodatristat | 1673568-73-4 | Rodatristat (KAR5417) 是一种有效的 tryptophan hydroxylase 1 (TPH1) 和 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。 |
| PL12482 | Rodatristat ethyl | 1673571-51-1 | 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)， |
| PL12480 | Telotristat ethyl | 1033805-22-9 | 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。 |
| PL12481 | Telotristat etiprate | 1137608-69-5 | Telotristat etiprate (LX1606 Hippurate) 是色氨酸羟化酶抑制剂，能够减少血清素的产生。 |
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