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Metabolism

ATP Citrate Lyase

(11)

Acetyl-CoA Carboxylase

Amino Acids and Derivatives

Angiotensin-converting Enzyme (ACE)

Endogenous Metabolite

Glutathione Peroxidase

(36)

HIF/HIF Prolyl-Hydroxylase

Indoleamine 2,3-Dioxygenase (IDO)

(33)

Isocitrate Dehydrogenase (IDH)

Mitochondrial Metabolism

(85)

N-Acetylglucosaminyltransferase

Procollagen C Proteinase

(1)

Prolyl Endopeptidase (PREP)

Reactive Oxygen Species

Serine/threonin kinase

(47)

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

Diethyl-pythiDC

T151241821370-70-0In house

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

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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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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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Telotristat ethyl

T118971033805-22-9

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

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Nepicastat hydrochloride

T6604170151-24-3

Nepicastat hydrochloride (RS-25560-197 hydrochloride) is an effective and specific inhibitor, which is used for bovine and human dopamine-β-hydroxylase with IC50 of 8.5 nM and 9 nM, respectively.The affinity of Nepicastat for twelve other enzymes and thirteen neurotransmitter receptors is negligible.

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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

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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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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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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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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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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p-Ethynylphenylalanine

T10142278605-15-5In house

p-Ethynylphenylalanine (4-Ethynyl-L-phenylalanine), a selective, effective, and reversible tryptophan hydroxylase (TPH) inhibitor, exhibits competitive inhibition with a Ki of 32.6 μM.

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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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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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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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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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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].

$129

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Tetrahydropapaverine hydrochloride

T60046429-04-5

Tetrahydropapaverine hydrochloride (Norlaudanosine HCl) , an analogue of salsolinol and tetrahydropapaveroline, has neurotoxicity on dopamine neurons.

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p-Fluoro-L-phenylalanine

T412741132-68-9

p-Fluoro-L-phenylalanine is a substrate for tyrosine hydroxylase (TH) that can be used to study the regulation of that enzyme. p-Fluoro-L-phenylalanine binds to the L-leucine specific receptor of Escherichia coli with an KD of 0.26 μM.

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Bupicomide

T3061522632-06-0In house

Bupicomide is a dopamine beta hydroxylase inhibitor with antihypertensive and vasodilatory activity that reduces 14C-norepinephrine biosynthesis of 14C-dopamine and can be used to study hypertension.

$293

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pCPA methyl ester hydrochloride

T4114314173-40-1

pCPA methyl ester hydrochloride (4-Chloro-DL-phenylalanine methyl ester hydrochloride) is an inhibitor of tryptophan hydroxylase inhibitor and 5-HT synthesis. pCPA methyl ester hydrochloride is permeable across the blood-brain barrier and reduces 5-HT central availability.

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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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(R)-Nepicastat HCl

T6356195881-94-8

(R)-Nepicastat HCl (RS-25560-198 HCl), the R-enantiomer of Nepicastat HCl, is a potent and selective inhibitor with IC50 of 25.1 nM and 18.3 nM for bovine and human dopamine-β-hydroxylase, with negligible affinity for twelve other enzymes and thirteen neurotransmitter receptors.

$135

6-8 weeks

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GSK180

T154261799725-26-0

GSK180 is a selective competitive inhibitor of kynurenine 3-monooxygenase (KMO; IC50: ~6 nM), an enzyme involved in tryptophan metabolism.

5 days

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GSK 366

T114701953157-39-5

GSK 366 is a potent kynurenine-3-monooxygenase (KMO) inhibitor with IC50 values of 0.7 nM for P. fluorescens-KMO and 2.3 nM for human KMO.

$2,420

10-14 weeks

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LPA2 antagonist 1

T157861017606-66-4

LPA2 antagonist 1 is an LPA2 antagonist (IC50: 17 nM).

$590

35 days

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LP-533401

T15778945976-43-2

LP-533401 is an inhibitor of Tryptophan hydroxylase 1. It is used for regulates serotonin production in the gut.

$770

35 days

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Rodatristat ethyl

T167791673571-51-1

Rodatristat ethyl (KAR5585) is a groundbreaking, orally active, and potent inhibitor of tryptophan hydroxylase 1 (TPH1) that significantly reduces 5-hydroxytryptamine (5-HT) levels and decreases pulmonary arterial hypertension (PAH) at low concentrations.

$2,390

10-14 weeks

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