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Catalog No. Product Name Information Product Use Citations Product Validations
S2173 Telotristat Etiprate (LX 1606 Hippurate) Telotristat Etiprate (LX 1606 Hippurate) is an orally bioavailable, tryptophan hydroxylase (TPH) inhibitor with potential antiserotonergic activity. Phase 3.
Cancers (Basel), 2021, 13(21)5305
S2367 Tetrahydropapaverine HCl Tetrahydropapaverine (Norlaudanosine), one of the TIQs and an analogue of salsolinol and tetrahydropapaveroline, has been reported to have neurotoxic effects on dopamine neurons.
S2695 Nepicastat (SYN-117) HCl Nepicastat (SYN-117) HCl is a potent and selective inhibitor of both bovine and human dopamine-β-hydroxylase with IC50 of 8.5 nM and 9 nM, with negligible affinity for twelve other enzymes and thirteen neurotransmitter receptors. Phase 2.
S3273 Hypericin Hypericin (Hyp, HY) is a naturally occurring substance found in the common St. John's Wort (Hypericum species) with antidepressive, antineoplastic and antiviral (human immunodeficiency and hepatitis C virus) activities. Hypericin has inhibitory effects on MAO (monoaminoxidase), PKC (protein kinase C), dopamine-beta-hydroxylase, reverse transcriptase, telomerase and CYP (cytochrome P450).
Eur J Pharmacol, 2021, 900:174071
S4130 Mildronate Mildronate (Meldonium, MET-88, Quaterin) is an inhibitor of biosynthesis of L-carnitine by gamma-butyrobetaine (GBB) hydroxylase and as a competitive inhibitor of renal carnitine reabsorption.
Cancer Discov, 2020, CD-20-0288
S4586 4-Chloro-DL-phenylalanine 4-Chloro-DL-phenylalanine (Fenclonine, PCPA, CP-10188) is a selective and irreversible inhibitor of tryptophan hydroxylase, a rate-limiting enzyme in the biosynthesis of serotonin (5-HYDROXYTRYPTAMINE). 4-Chloro-DL-phenylalanine acts pharmacologically to deplete endogenous levels of serotonin.
J Anim Sci, 2022, skac065
S4926 (R)-Nepicastat HCl (R)-Nepicastat HCl (RS-25560-198), 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.
S5797 Metyrosine Metyrosine (α-Methyltyrosine), an antihypertensive drug, is a tyrosine hydroxylase inhibitor.
S6044 H-Tyr(3-I)-OH H-Tyr(3-I)-OH (3-Iodo-L-tyrosine) is responsible for catalyzing the first step of the noradrenergic biosynthesis pathway. H-Tyr(3-I)-OH is an effective tyrosine hydroxylase inhibitor.
S7456 Osilodrostat (LCI699) LCI699(Osilodrostat) is a potent inhibitor of 11β-hydroxylase (CYP11B), an enzyme catalyzing the final step of cortisol synthesis.
Drug Metab Dispos, 2022, 50(2):114-127
J Biol Chem, 2021, S0021-9258(21)00587-1
S7483 DMOG DMOG (Dimethyloxalylglycine) is an antagonist of α-ketoglutarate cofactor and inhibitor for HIF prolylhydroxylase, leading to stabilisation and accumulation of HIF-1α protein in the nucleus. DMOG enhances autophagy.
Cell Metab, 2022, 34(2):299-316.e6
Theranostics, 2022, 12(4):1500-1517
Food Funct, 2022, 10.1039/d1fo03909a
S8172 Ro 61-8048 Ro 61-8048 is a high-affinity kynurenine 3-hydroxylase (KMO) inhibitor with IC50 and Ki of 37 nM and 4.8 nM, respectively.
J Neurosci Res, 2020, 98(1):155-167
Invest Ophthalmol Vis Sci, 2019, 60(13):4159-4170
Leukemia, 2019, 10.1038/s41375-019-0558-x
S1379 Isotretinoin Isotretinoin (13-cis retinoic acid) was developed to be used as a chemotherapy medication for the treatment of brain cancer, pancreatic cancer and more.
Sci Adv, 2021, 7(43):eabe0834
Cell Rep, 2020, 32(12):108171
Oncogene, 2020, 39(21):4212-4226
S9568 Sapropterin Dihydrochloride Sapropterin Dihydrochloride (Tetrahydrobiopterin, R-THBP), a synthetic preparation of the dihydrochloride salt of naturally occurring tetrahydrobiopterin (BH4), is a phenylalanine hydroxylase activator.
S2173 Telotristat Etiprate (LX 1606 Hippurate) Telotristat Etiprate (LX 1606 Hippurate) is an orally bioavailable, tryptophan hydroxylase (TPH) inhibitor with potential antiserotonergic activity. Phase 3.
Cancers (Basel), 2021, 13(21)5305
S2367 Tetrahydropapaverine HCl Tetrahydropapaverine (Norlaudanosine), one of the TIQs and an analogue of salsolinol and tetrahydropapaveroline, has been reported to have neurotoxic effects on dopamine neurons.
S2695 Nepicastat (SYN-117) HCl Nepicastat (SYN-117) HCl is a potent and selective inhibitor of both bovine and human dopamine-β-hydroxylase with IC50 of 8.5 nM and 9 nM, with negligible affinity for twelve other enzymes and thirteen neurotransmitter receptors. Phase 2.
S3273 Hypericin Hypericin (Hyp, HY) is a naturally occurring substance found in the common St. John's Wort (Hypericum species) with antidepressive, antineoplastic and antiviral (human immunodeficiency and hepatitis C virus) activities. Hypericin has inhibitory effects on MAO (monoaminoxidase), PKC (protein kinase C), dopamine-beta-hydroxylase, reverse transcriptase, telomerase and CYP (cytochrome P450).
Eur J Pharmacol, 2021, 900:174071
S4130 Mildronate Mildronate (Meldonium, MET-88, Quaterin) is an inhibitor of biosynthesis of L-carnitine by gamma-butyrobetaine (GBB) hydroxylase and as a competitive inhibitor of renal carnitine reabsorption.
Cancer Discov, 2020, CD-20-0288
S4586 4-Chloro-DL-phenylalanine 4-Chloro-DL-phenylalanine (Fenclonine, PCPA, CP-10188) is a selective and irreversible inhibitor of tryptophan hydroxylase, a rate-limiting enzyme in the biosynthesis of serotonin (5-HYDROXYTRYPTAMINE). 4-Chloro-DL-phenylalanine acts pharmacologically to deplete endogenous levels of serotonin.
J Anim Sci, 2022, skac065
S4926 (R)-Nepicastat HCl (R)-Nepicastat HCl (RS-25560-198), 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.
S5797 Metyrosine Metyrosine (α-Methyltyrosine), an antihypertensive drug, is a tyrosine hydroxylase inhibitor.
S6044 H-Tyr(3-I)-OH H-Tyr(3-I)-OH (3-Iodo-L-tyrosine) is responsible for catalyzing the first step of the noradrenergic biosynthesis pathway. H-Tyr(3-I)-OH is an effective tyrosine hydroxylase inhibitor.
S7456 Osilodrostat (LCI699) LCI699(Osilodrostat) is a potent inhibitor of 11β-hydroxylase (CYP11B), an enzyme catalyzing the final step of cortisol synthesis.
Drug Metab Dispos, 2022, 50(2):114-127
J Biol Chem, 2021, S0021-9258(21)00587-1
S7483 DMOG DMOG (Dimethyloxalylglycine) is an antagonist of α-ketoglutarate cofactor and inhibitor for HIF prolylhydroxylase, leading to stabilisation and accumulation of HIF-1α protein in the nucleus. DMOG enhances autophagy.
Cell Metab, 2022, 34(2):299-316.e6
Theranostics, 2022, 12(4):1500-1517
Food Funct, 2022, 10.1039/d1fo03909a
S8172 Ro 61-8048 Ro 61-8048 is a high-affinity kynurenine 3-hydroxylase (KMO) inhibitor with IC50 and Ki of 37 nM and 4.8 nM, respectively.
J Neurosci Res, 2020, 98(1):155-167
Invest Ophthalmol Vis Sci, 2019, 60(13):4159-4170
Leukemia, 2019, 10.1038/s41375-019-0558-x
S1379 Isotretinoin Isotretinoin (13-cis retinoic acid) was developed to be used as a chemotherapy medication for the treatment of brain cancer, pancreatic cancer and more.
Sci Adv, 2021, 7(43):eabe0834
Cell Rep, 2020, 32(12):108171
Oncogene, 2020, 39(21):4212-4226
S9568 Sapropterin Dihydrochloride Sapropterin Dihydrochloride (Tetrahydrobiopterin, R-THBP), a synthetic preparation of the dihydrochloride salt of naturally occurring tetrahydrobiopterin (BH4), is a phenylalanine hydroxylase activator.
Tags: Hydroxylase activity | Dopamine-β-Hydroxylase activity | Hydroxylase inhibitor review