Tryptophan hydroxylase (TPH) is the rate-limiting enzyme in the biosynthesis of the biogenic monoamine serotonin (5-hydroxytryptamine, 5-HT).TPH is a member of the family of aromatic amino acid hydroxylases, along with tyrosine hydroxylase (TH), phenylalanine hydroxylase (PAH), and others. These enzymes are all strictly dependent on dioxygen, non-heme iron (II), and tetrahydrobiopterin (BH4). The phosphorylating conditions (ATP-Mg2+) activate tryptophan hydroxylase in a calcium-dependent, cyclic AMP-independent manner. In vertebrates, two distinct serotonergic systems are produced by the two known TPH isoforms, TPH-1 and TPH-2.
TPH2, which is primarily found in the raphe nuclei of the brain stem, is responsible for the production of 5-HT in the brain, whereas TPH1, which is primarily expressed in the digestive tract and pineal gland, mediates 5-HT biosynthesis in non-neuronal tissues. TPH-1, the key enzyme in peripheral serotonin biosynthesis, offers a brand-new target for the development of anabolic osteoporosis medications. TPH2, a phenotypic marker for serotonin neurons, is well known for being highly oxidation-labile. TPH2, a key regulator of 5-HT neurotransmission and the stress response, is emerging as a new therapeutic target for the treatment of stress disorders due to its pathophysiological and pharmacological significance.
| Structure | Cat No. | Product Name | CAS No. | Product Description |
|---|---|---|---|---|
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V5275 | Fenclonine (PCPA; CP-10188) | 7424-00-2 | Fenclonine [para -chlorophenylalanine (PCPA)], is a selective and irreversible inhibitor of tryptophan hydroxylase, which is a rate-limiting enzyme in the biosynthesis of serotonin. |
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V78349 | Litchinol B | Litchinol B (compound 2) is a noncompetitive tyrosinase inhibitor (antagonist) with an inhibition constant of 5.70 μM. | |
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V18911 | LP-533401 HCl | 1040526-12-2 | LP-533401 HCl is a tryptophan hydroxylase 1 inhibitor that regulates serotonin production in the intestine. |
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V78998 | Piceid 6″-O-azelaic acid ester | Piceid 6″-O-azelaic acid ester has high intracellular tyrosinase inhibitory activity and decolorizing activity. | |
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V3927 | TELOTRISTAT ETHYL (LX1606) | 1033805-22-9 | Telotristat ethyl (formerly LX-1032; LX-1606; LX-1032; LX-1606; trade name:Xermelo), the ethyl ester prodrug form ofTelotristat,is an orally bioavailable tryptophan hydroxylase (TPH) inhibitor (IC50= 0.028 μM) with antiserotonergic and anti-diarrhea activity. |
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V79702 | TPH1-IN-1 | TPH1-IN-1 (compound 40) is a xanthine analogue and an inhibitor (blocker/antagonist) of tryptophan hydroxylase TPH1 (IC50= 110.1 nM). | |
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V79998 | TPT-004 | TPT-004 is a TPH inhibitor. | |
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V81656 | Tyrosinase-IN-13 | Tyrosinase-IN-13 (compound 3c) is an analogue of Flurbiprofen and a potent noncompetitive tyrosinase inhibitor (IC50=68 μM; Ki=36.3 μM). | |
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V81657 | Tyrosinase-IN-14 | Tyrosinase-IN-14 (compound 7m) is a tyrosinase inhibitor that reduces the catalytic activity of tyrosinase by changing its secondary structure. | |
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V80289 | Tyrosinase-IN-15 | Tyrosinase-IN-15 (Compound 39) is a tyrosinase inhibitor (IC50= 7.12 μM, Ki= 11.8 μM). | |
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V80059 | Tyrosinase-IN-18 | Tyrosinase-IN-18 is a potent tyrosinase inhibitor. | |
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V79867 | Tyrosinase-IN-19 | Tyrosinase-IN-19 is a competitive tyrosinase inhibitor. | |
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V80288 | Tyrosinase-IN-8 | Tyrosinase-IN-8 is a potent tyrosinase inhibitor (antagonist) with IC50 of 1.57 µM. |
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