Hydroxylases

Hydroxylase inhibitors block enzymes that add hydroxyl groups to amino acids, amines, steroids or proteins. The section is a mixed set that covers several unrelated enzymes. Tryptophan hydroxylase (TPH) starts serotonin synthesis, with TPH1 in the gut and TPH2 in the brain; LP-533401 and telotristat etiprate inhibit it. Dopamine beta-hydroxylase (DBH) converts dopamine to norepinephrine and is blocked by nepicastat HCl. Hypoxia-inducible factor (HIF) prolyl hydroxylases are oxygen-dependent dioxygenases that mark HIF for degradation; DMOG inhibits this group. Ro 61-8048 targets kynurenine 3-monooxygenase (KMO), and metyrapone inhibits steroid 11-beta-hydroxylase in cortisol synthesis.

25 Items

  • Nepicastat HCl
    Cat. No.
    A11172

    Nepicastat HCl

    Synonyms: RS-25560-197; SYN117

    Nepicastat hydrochloride is an inhibitor of dopamine beta-hydroxylase, an enzyme that catalyzes the conversion of dopamine to norepinephrine.

    5 mg
    $45.00
    10 mg
    $80.00
    All 7 sizes
  • Metyrapone
    Cat. No.
    A13363

    Metyrapone

    Metyrapone is an inhibitor of cytochrome P450-mediated ω/ω-1 hydroxylase activity and CYP11B1.

    50 mg
    $25.00
    100 mg
    $40.00
    All 5 sizes
  • Ro 61-8048
    Cat. No.
    A12833

    Ro 61-8048

    Ro 61-8048 is a potent and competitive kynurenine 3-hydroxylase inhibitor (Ki = 4.8 nM, IC50 = 37 nM).

    2 mg
    $25.00
    5 mg
    $45.00
    All 9 sizes
  • DMOG
    Cat. No.
    A13998

    DMOG

    Synonyms: Dimethyloxaloyl glycine

    DMOG is a cell permeable, competitive inhibitor of HIF-PH. It acts to stabilize HIF-1α expression at normal oxygen tensions in cultured cells, at concentrations between 0.1 and 1 mM.

    25 mg
    $30.00
    50 mg
    $50.00
    All 6 sizes
  • Tetrahydropapaverine HCl
    Cat. No.
    A10920

    Tetrahydropapaverine HCl

    Tetrahydropapaverine, one of the TIQs and an analogue of salsolinol and tetrahydropapaveroline, has been reported to have neurotoxic effects on dopamine neurons.

    5 mg
    $30.00
    10 mg
    $40.00
    All 7 sizes
  • LX-1031
    Cat. No.
    A11479

    LX-1031

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

    1 mg
    $60.00
    2 mg
    $80.00
    All 8 sizes
  • Osilodrostat
    Cat. No.
    A14013

    Osilodrostat (LCI-699)

    Synonyms: LCI-699

    Osilodrostat (LCI699) is a potent inhibitor of human 11β-hydroxylase and aldosterone synthase with IC50 values of 2.5 and 0.7 nM, respectively.

    1 mg
    $35.00
    2 mg
    $50.00
    All 8 sizes
  • Telotristat
    Cat. No.
    A14054

    Telotristat

    Synonyms: LP-778902

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

    1 mg
    $25.00
    2 mg
    $40.00
    All 10 sizes
  • ACT-678689
    Cat. No.
    A15846

    ACT-678689

    ACT-678689 is a potent inhibitor of tryptophan hydroxylase (TPH), exhibiting an IC50 value of 8 nM. This compound plays a critical role in the modulation of serotonin synthesis, making it valuable for research in neuropharmacology and the study of mood disorders. Its selective inhibition of TPH allows for in-depth investigation into serotonin-related pathways and their physiological implications.

    1 mg
    $90.00
    5 mg
    $225.00
    All 7 sizes
  • 4-Chloro-DL-phenylalanine
    Cat. No.
    A16424

    4-Chloro-DL-phenylalanine

    Synonyms: Fenclonine; PCPA; CP-10188

    4-Chloro-DL-phenylalanine is a selective and irreversible inhibitor of tryptophan hydroxylase, a rate-limiting enzyme in the biosynthesis of serotonin (5-HYDROXYTRYPTAMINE).

    100 mg
    $20.00
    250 mg
    $35.00
    All 4 sizes
  • Rodatristat
    Cat. No.
    A18820

    Rodatristat

    Synonyms: KAR5417

    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.

    1 mg
    $315.00
    5 mg
    $605.00
    All 6 sizes
  • Enarodustat
    Cat. No.
    A19214

    Enarodustat

    Synonyms: JTZ-951

    Enarodustat is a potent and orally active factor prolyl hydroxylase inhibitor, with an EC50 of 0.22 μM; Enarodustat has entered clinical trial for renal anemia.

    1 mg
    $25.00
    2 mg
    $40.00
    All 8 sizes
  • Rodatristat ethyl
    Cat. No.
    A20593

    Rodatristat ethyl

    Synonyms: KAR5585

    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).

    1 mg
    $315.00
    5 mg
    $875.00
    All 6 sizes
  • PCPA methyl ester hydrochloride
    Cat. No.
    A45815

    PCPA methyl ester hydrochloride

    Synonyms: 4-Chloro-DL-phenylalanine methyl ester hydrochloride

    PCPA methyl ester hydrochloride is a reversible inhibitor of tryptophan hydroxylase, an enzyme critical for serotonin (5-HT) synthesis. This compound effectively crosses the blood-brain barrier, leading to a reduction in central 5-HT availability. It is widely utilized in research to investigate the role of serotonin in various physiological and pathological processes.

    200 mg
    $25.00
    1 g
    $60.00
    All 4 sizes
  • LP-533401 hydrochloride
    Cat. No.
    A78000

    LP-533401 hydrochloride

    LP-533401 hydrochloride is an inhibitor of tryptophan hydroxylase 1, a key enzyme in serotonin biosynthesis. By modulating serotonin production in the gut, this compound serves as a valuable tool for investigating the role of serotonin in gastrointestinal physiology and associated disorders. Its applications extend to understanding the pathophysiology of conditions related to serotonin dysregulation, including mood disorders and gastrointestinal diseases.

    1 mg
    $25.00
    5 mg
    $65.00
    All 6 sizes
  • 6-Fluorotryptophan
    Cat. No.
    A78002

    6-Fluorotryptophan

    6-Fluorotryptophan is a competitive inhibitor of tryptophan hydroxylase, an enzyme crucial for serotonin synthesis. This compound has demonstrated significant effects on sleep disruption in animal models, particularly in rats with chronic EEG electrode implantation. Its application in research includes studies on serotonin-related disorders and the modulation of sleep patterns, providing insights into the neurochemical mechanisms underlying these processes.

    5 mg
    $20.00
    10 mg
    $25.00
    All 4 sizes
  • TPT-004
    Cat. No.
    A78004

    TPT-004

    TPT-004 is a selective inhibitor of tryptophan hydroxylases (TPH), demonstrating IC50 values of 77 nM and 16 nM for TPH1 and TPH2, respectively. This compound exhibits strong selectivity for TPH1, targeting the production of serotonin. TPT-004 has been shown to effectively reduce peripheral serotonin levels and inhibit colorectal tumor growth in preclinical mouse models, making it a valuable tool in cancer and serotonin-related research.

    5 mg
    $330.00
    10 mg
    $540.00
    All 4 sizes
  • TPH1-IN-1
    Cat. No.
    A78006

    TPH1-IN-1

    TPH1-IN-1 is a xanthine derivative that functions as a specific inhibitor of tryptophan hydroxylase 1 (TPH1), exhibiting an IC50 value of 110.1 nM. This compound demonstrates robust in vitro activity and is stable in liver microsomes, making it a valuable tool for studies targeting serotonin biosynthesis. TPH1-IN-1 effectively inhibits adipocyte differentiation in T3-L1 cells, highlighting its potential applications in metabolic research and related therapeutic investigations.

    Out of stock

    All 3 sizes
  • Telotristat besilate
    Cat. No.
    A78007

    Telotristat besilate

    Telotristat besilate is a potent inhibitor of tryptophan hydroxylase, exhibiting an in vivo IC50 of 0.028 μM. This compound effectively modulates serotonin synthesis, making it a valuable tool for research on serotonin-related disorders and other neurochemical pathways. Its application extends to studies investigating the regulation of mood, gastrointestinal function, and tumor activity in carcinoid syndrome.

    25 mg
    $1,275.00
    50 mg
    $1,625.00
    All 3 sizes

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