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Metabolism

Acetyl-CoA Carboxylase

Amino Acids and Derivatives

Angiotensin-converting Enzyme (ACE)

Endogenous Metabolite

Glutathione Peroxidase

(73)

Glyoxalase

(17)

HIF/HIF Prolyl-Hydroxylase

Indoleamine 2,3-Dioxygenase (IDO)

(98)

Isocitrate Dehydrogenase (IDH)

Mitochondrial Metabolism

(212)

N-Acetylglucosaminyltransferase

Procollagen C Proteinase

(1)

Prolyl Endopeptidase (PREP)

Reactive Oxygen Species

Serine/threonin kinase

(90)

Stearoyl-CoA Desaturase (SCD)

Hydroxylase

Hydroxylation is a chemical process that introduces a hydroxyl group (-OH) into an organic compound. In biochemistry, hydroxylation reactions are often facilitated by enzymes called hydroxylases. Hydroxylation is the first step in the oxidative degradation of organic compounds in air. It is extremely important in detoxification since hydroxylation converts lipophilic compounds into water-soluble (hydrophilic) products that are more readily removed by the kidneys or liver and excreted. Some drugs (for example, steroids) are activated or deactivated by hydroxylation.

Filter HomeSignaling PathwaysMetabolismHydroxylase

Hypericin

T6S0923548-04-9

Hypericin (Cyclosan) is a natural anthraquinone compound, an extract of Hypericum perforatum, which inhibits PKC, MAO, dopamine-beta-hydroxylase, reverse transcriptase, telomerase, and CYP, etc. Hypericin exhibits antimicrobial, antiviral, antitumor, and antidepressant activities.

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LX-1031

T15796945976-76-1

LX-1031 is an effective inhibitor of tryptophan 5-hydroxylase. LX-1031 decreases serotonin (5-HT) synthesis peripherally.

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4-Hydroxyderricin

T1014655912-03-3

4-Hydroxyderricin, a potent and selective MAO-B inhibitor (IC50: 3.43 μM), is the main active ingredient of Angelica sinensis, which mildly inhibits dopamine β-hydroxylase (DBH) activity and possesses antidepressant activity.

$122

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Telotristat Etiprate

T60441137608-69-5

Telotristat Etiprate (LX 1606 Hippurate) is an orally bioavailable, tryptophan hydroxylase (TPH) inhibitor with potential antiserotonergic activity.

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Diethyl-pythiDC

T151241821370-70-0In house

Diethyl-pythiDC is an collagen prolyl 4-hydroxylase inhibitor.

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Ketoconazole

T067965277-42-1

Ketoconazole (R-41400), a CYP3A4 inhibitor, is an imidazole anti-fungal agent.

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Cited

SU 10603

T28871786-97-0

SU 10603 is a specific inhibitor of 17α-hydroxylase (also known as CYP17A1 and P450c17) used to study steroid hormone synthesis.

$293

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Ro 61-8048

T1896199666-03-0

Ro 61-8048 is a potent and selective inhibitor of kynurenine hydroxylase with an IC50 value of 37 nM.

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Etamicastat hydrochloride

T11238L677773-32-9

Etamicastat hydrochloride (BIA 5-453 hydrochloride) is a peripherally selective dopamine beta-hydroxylase inhibitor that reduces hypertension.

$129

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Sapropterin dihydrochloride

T711769056-38-8

Sapropterin dihydrochloride (6R-BH4 dihydrochloride) is phenylalanine hydroxylase agonist that is approved for the treatment of BH4 responsive PKU.

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Osilodrostat

T4277928134-65-0

Osilodrostat (LCI699) is a potent inhibitor of human 11β-hydroxylase (CYP11B1) and aldosterone synthase (CYP11B2) with IC50 values of 2.5 and 0.7 nM, respectively, and has been approved by the FDA for the treatment of Cushing's disease.

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Telotristat ethyl

T118971033805-22-9

Telotristat ethyl (LX1606) is a orally-delivered inhibitor of tryptophan hydroxylase that reduces serotonin production.

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ACT-678689

T141191783256-96-1

ACT-678689 (Compound Example 1.53.4) is a tryptophan hydroxylase (TPH) inhibitor with an IC50 of 8 nM[1].

$115

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Fenclonine

T14477424-00-2

Fenclonine (CP-10188) is a selective and irreversible inhibitor of tryptophan hydroxylase, a rate-limiting enzyme in the biosynthesis of serotonin (5-HYDROXYTRYPTAMINE). Fenclonine(CP-10188) acts pharmacologically to deplete endogenous levels of serotonin.

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Zamicastat

T133831080028-80-3

Zamicastat (BIA 5-1058) is an inhibitor of dopamine β-hydroxylase (DBH) and a concentration-dependent dual inhibitor of P-gp and BCRP, with IC50 values of 73.8 μM and 17.0 μM, respectively.

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6-fluoro-DL-Tryptophan

T76947730-20-3

6-fluoro-DL-Tryptophan is an inhibitor of serotonin (5-HT) synthesis.

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Casein

T839699000-71-9

Casein is a milk protein with multiple roles in a novel drug delivery system that affects postprandial amino acid delivery in different ways through its intragastric coagulation properties.

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Telotristat

T215061033805-28-5

Telotristat is the active metabolite of LX1606(Telotristat etiprate), which is an orally bioavailable tryptophan hydroxylase (TPH) inhibitor and shows potential antiserotonergic activity.

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Cuprizone

T65013370-81-0

Cuprizone is a copper chelator.Cuprizone is used to induce schizophrenia in mice.Cuprizone induces oligodendrocyte death and induces a demyelination response.

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Mildronate

T326876144-81-5

Mildronate (Meldonium) is an inhibitor of biosynthesis of L-carnitine by gamma-butyrobetaine (GBB) hydroxylase and as a competitive inhibitor of renal carnitine reabsorption.

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4-Chloro-L-phenylalanine

T7822814173-39-8

4-Chloro-L-phenylalanine (L-PCPA) is an inhibitor of 5-HT biosynthesis and a non-specific antagonist of tryptophan hydroxylase (TPH1 and TPH2).

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EWP 815

T6121420231-01-0

EWP 815 is a disulfiram analogue that functions as a powerful inhibitor of Ins(1,4) P 2 phosphatase, Ins(1,4,5) P 3 5-phosphatase, and dopamine β-hydroxylase activity [1] [2].

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p-Ethynylphenylalanine hydrochloride

T10142L188640-63-3

p-Ethynylphenylalanine hydrochloride (4-Ethynyl-L-phenylalanine HCL) is a novel, potent, and specific inhibitor of TPH[1]. Its potential to selectively and reversibly inhibit serotonin biosynthesis may contribute to characterizing the role of serotonin in behavioral and physiological activities[1].

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LP-533401 hydrochloride

T157791040526-12-2

LP-533401 hydrochloride is a peripheral Tph inhibitor that cannot cross the blood-brain barrier that inhibits 5-hydroxytryptamine synthesis and can be used to study periodontal disease and hepatic steatosis.

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