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Esterase Inhibitors

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製品番号 製品名 Target 研究分野 構造式
  • HY-18729A
    L-NAME hydrochloride
    Maximum Cited Publications
    78 Publications Verification

    NG-Nitroarginine methyl ester hydrochloride

    		 NO Synthase Infection Neurological Disease Cancer
    L-NAME hydrochloride inhibits NOS with an IC50 of 70 μM. L-NAME is a precursor to NOS inhibitor L-NOARG which has an IC50 value of 1.4 μM. L-NAME hydrochloride requires hydrolysis of the methyl ester by cellular esterases to become a fully functional inhibitor. L-NAME hydrochloride can be used to induce hypertension and preeclampsia models.
    L-NAME hydrochloride
  • HY-B1325
    Cefuroxime axetil

    		Bacterial Antibiotic Infection Inflammation/Immunology
    Cefuroxime axetil is an orally effective broad-spectrum β-lactam antibiotic that targets bacterial penicillin-binding proteins (PBPs, such as PBP3 and PBP1). Cefuroxime axetil inhibits cell wall synthesis, leading to bacterial lysis and death, with a minimum inhibitory concentration (MIC) of 0.12-4 mg/L for non-typeable Haemophilus influenzae (NTHi). Cefuroxime axetil is hydrolyzed by esterase to the active ingredient Cefuroxime (HY-B1256A) after oral absorption. Topical administration of Cefuroxime via bioadhesive nanoparticles (BNPs) can prolong the drug's retention time in the middle ear (≥7 days). Cefuroxime axetil can be used in the study of otitis media (especially NTHi infection). Cefuroxime axetil can achieve precise antibacterial effects through oral or topical nano-delivery systems, reducing systemic exposure and the risk of antibiotic resistance .
    Cefuroxime axetil
  • HY-B0732
    Itopride hydrochloride

    HSR803

    		 Cholinesterase (ChE) Dopamine Receptor Bacterial Neurological Disease
    Itopride (HSR803) hydrochloride is a potent dopamine-2 antagonist and an acetylcholine esterase (AChE) inhibitor. Itopride hydrochloride enhances gastric motility through both antidopaminergic and anti-acetylcholinesterasic actions, can be used as a gastrointestinal prokinetic agent. Itopride can be used for researching gastro-esophageal reflux disease (GERD) .
    Itopride hydrochloride
  • HY-E70562
    Mucinase StcE

    		Bacterial Infection Cancer
    Mucinase StcE is a zinc metalloproteinase belonging to the M66 family, which is secreted by enterohemorrhagic Escherichia coli via the type II general secretion pathway. Mucinase StcE specifically recognizes and cleaves the 'T*XT' motif in mucin-type glycoproteins with α-O-glycans (such as MUC2, Mucin 7, Glycoprotein 340, CD45, CD43, C1 Esterase Inhibitor (HY-P991629), etc.). By degrading the mucus layer to reduce its viscosity, inhibiting complement cascade activation, and localizing complement regulatory factors to the cell membrane, Mucinase StcE helps bacteria penetrate the mucosal barrier, adhere to host cells, and evade immune clearance. Mucinase StcE can serve as a mucin-specific proteolytic tool for research on mucinous carcinomas derived from the colon, esophagus, and salivary glands .
    Mucinase StcE
  • HY-18729
    L-NAME

    NG-Nitroarginine methyl ester

    		 NO Synthase Cancer
    L-NAME inhibits NOS with an IC50 of 70 μM. L-NAME is a precursor to NOS inhibitor L-NOARG which has an IC50 value of 1.4 μM. L-NAME requires hydrolysis of the methyl ester by cellular esterases to become a fully functional inhibitor. L-NAME can be used to induce hypertension and preeclampsia models.
    L-NAME
  • HY-18522
    AA26-9

    		Phospholipase Metabolic Disease
    AA26-9 is a potent and broad spectrum serine hydrolase inhibitor. AA26-9 targets included serine peptidases, lipases, amidases, esterases, and thioesterases. AA26-9 shows inhibitory activity against approximately 1/3 of the 40+ serine hydrolases detected in immortalized T cell lines .
    AA26-9
  • HY-19772
    GSK3117391

    ESM-HDAC391; CHR-5154; HDAC-IN-3

    		 HDAC c-Fms Inflammation/Immunology
    GSK3117391 (ESM-HDAC391; CHR-5154; HDAC-IN-3) is an orally active HDAC inhibitor with a IC50 of 55 nM. Using esterase-sensitive motif technology, GSK3117391 is selectively converted into its active acid metabolite HDAC189 in cells expressing carboxylesterase-1. GSK3117391 induces sustained global protein acetylation in monocytes, inhibits the production of proinflammatory cytokines, depletes circulating monocytes, downregulates the expression of CSF1R, and inhibits monocyte adhesion and differentiation. GSK3117391 can be used in the research of chronic inflammatory diseases .
    GSK3117391
  • HY-D1078
    5(6)-Carboxy-2',7'-dichlorofluorescein diacetate

    		Fluorescent Dye Reactive Oxygen Species (ROS) P-glycoprotein Others
    5 (6)-Carboxy-2',7'-dichlorofluorescein diacetate is a fluorescein-based reactive oxygen species (ROS) probe and also a MRP2 substrate. 5 (6)-Carboxy-2',7'-dichlorofluorescein diacetate serves as a substrate for intracellular esterases, which cleave its acetate groups to generate a fluorescent product capable of detecting intracellular ROS. 5 (6)-Carboxy-2',7'-dichlorofluorescein diacetate is ATP-dependent and is transported via a single MRP2 binding site; it competes with LTC4 for MRP2 binding sites and inhibits MRP2-mediated LTC4 transport (Ex/Em = 496/525 nm) .
    5(6)-Carboxy-2',7'-dichlorofluorescein diacetate
  • HY-B2029
    Phosalone
    1 Publications Verification

    		 Insecticide Cholinesterase (ChE) Infection Inflammation/Immunology
    Phosalone is an orally active, blood-brain barrier penetrant Insecticide and acaricide. Phosalone inhibits the activity of Acetylcholinesterase. Phosalone acts as a substrate for detoxifying esterases. Phosalone induces symptoms of cholinergic hyperactivity, toxic reactions, mortality, oxidative stress, and changes in pro-inflammatory protein levels, and exerts toxic effects on colonic tissues and cells. Phosalone controls pistachio psyllids. Phosalone can be used in studies related to colitis .
    Phosalone
  • HY-124258
    Valilactone

    (-)-Valilactone

    		 Endogenous Metabolite Metabolic Disease
    Valilactone is a potent and effective inhibitor of esterase, produced by actinomycetes .
    Valilactone
  • HY-17484
    Ampiroxicam
    2 Publications Verification

    CP 65703

    		 Drug Derivative Inflammation/Immunology
    Ampiroxicam is an orally active prodrug of non-steroidal anti-inflammatory drug (NSAID). Ampiroxicam inhibits paw swelling in adjuvant-induced arthritis and acute inflammation models, and suppresses phenylbenzoquinone-induced stretching responses in mice. Ampiroxicam is rapidly and completely converted to Piroxicam (HY-B0253) via non-specific esterases and first-pass metabolism. Ampiroxicam induces contact hypersensitivity and photosensitivity reactions through photoproducts generated by UVA. Ampiroxicam can be used in research related to photosensitivity, adjuvant-induced arthritis, rheumatism, osteoarthritis and other inflammatory diseases .
    Ampiroxicam
  • HY-P991629
    C1 Esterase Inhibitor (Human)

    		Ser/Thr Protease Inflammation/Immunology
    C1 Esterase Inhibitor (Human) is a C1 Esterase inhibitor derived from human plasma. C1 Esterase Inhibitor (Human), a glycoprotein, is a serum protease inhibitor (serpin) that binds covalently and inactivates C1r, C1s, and mannan-binding protein-associated proteases (MASPs). C1 Esterase Inhibitor (Human) has anti-inflammatory effects. C1 Esterase Inhibitor (Human) can be used to prevent angioedema attacks associated with hereditary angioedema .
    C1 Esterase Inhibitor (Human)
  • HY-103610
    4,4'-Dimethoxybenzil

    p-Anisil

    		 Cholinesterase (ChE) Cancer
    4,4'-Dimethoxybenzil is a human intestinal carboxyl esterase (hiCE) inhibitor with Ki of 70 nM.
    4,4'-Dimethoxybenzil
  • HY-126564
    Ebelactone A

    		Lipase MetAP Others Inflammation/Immunology
    Ebelactone A is a mycolic acid β-lactone, which exhibits inhibitory activity for esterase, lipase, fMet aminopeptidase (fMet AP) and PNBase, with IC50s of 56, 3, 8 and 7.5 μM, respectively . Ebelactone A inhibits cutinase, exhibits plants protective potency against Erysiphe graminis .
    Ebelactone A
  • HY-B0732A
    Itopride

    HSR803 free base

    		 Cholinesterase (ChE) Dopamine Receptor Bacterial Others
    Itopride (HSR803 free base) is a potent and orally active dopamine-2 antagonist and an acetylcholine esterase (AChE) inhibitor. Itopride enhances gastric motility through both antidopaminergic and anti-acetylcholinesterasic actions, can be used as a gastrointestinal prokinetic agent. Itopride can be used for researching gastro-esophageal reflux disease (GERD) .
    Itopride
  • HY-P10053
    sPLA2-IIA Inhibitor

    		Phospholipase Metabolic Disease
    sPLA2-IIA Inhibitor is a cyclic pentapeptide analog of FLSYK (cyclic 2-Nal-Leu-Ser-2-Nal-Arg (c2)), that binds to hGIIA (human IIA phospholipase A2) and inhibits its hydrolytic ability. sPLA2 is a member of the esterase superfamily that catalyzes the hydrolysis of the ester bond at the sn-2 position of glycerophospholipids, releasing free fatty acids such as arachidonic acid and lysophospholipids .
    sPLA2-IIA Inhibitor
  • HY-16031
    AFP464 free base

    NSC710464 free base

    		 Aryl Hydrocarbon Receptor Integrin Drug Intermediate DNA/RNA Synthesis Cancer
    AFP464 (NSC710464) free base is a prodrug of Aminoflavone (HY-132974) and an agonist of the aryl hydrocarbon receptor (AhR). AFP464 free base downregulates the expression of α6-integrin (α6-integrin), inhibits breast tumor growth, reduces the population of tumor-initiating cells, disrupts mammosphere structure, induces the formation of mucin lake clusters, triggers DNA damage, and exerts antiproliferative activity. AFP464 free base is rapidly converted to Aminoflavone by nonspecific esterases in plasma and cell culture media. AFP464 free base is applicable to research related to breast cancer .
    AFP464 free base
  • HY-106409
    Tefinostat
    1 Publications Verification

    CHR-2845

    		 HDAC Apoptosis Cancer
    Tefinostat (CHR-2845) is a monocyte/macrophage targeted histone deacetylase (HDAC) inhibitor. Tefinostat can be cleaved into active acid CHR-2847 by the intracellular esterase human carboxylesterase-1 (hCE-1). Tefinostat can be used for the research of leukaemias .
    Tefinostat
  • HY-W039923
    β-D-Galactose pentaacetate

    		Insulin Receptor Endocrinology
    β-D-Galactose pentaacetate is a negative regulator of insulin with plasma membrane penetrating ability and can be hydrolyzed by intracellular esterases. β-D-Galactose pentaacetate inhibits Leucine (HY-N0486)-induced insulin release in Wistar rat islets, potentially preventing excessive insulin release in pathological conditions .
    β-D-Galactose pentaacetate
  • HY-16031B
    AFP464 dihydrochloride

    NSC710464 dihydrochloride

    		 Aryl Hydrocarbon Receptor Integrin Drug Intermediate DNA/RNA Synthesis Cancer
    AFP464 (NSC710464) dihydrochloride is a prodrug of Aminoflavone (HY-132974) and an agonist of the aryl hydrocarbon receptor (AhR). AFP464 dihydrochloride downregulates the expression of α6-integrin (α6-integrin), inhibits breast tumor growth, reduces the population of tumor-initiating cells, disrupts mammosphere structure, induces the formation of mucin lake clusters, triggers DNA damage, and exerts antiproliferative activity. AFP464 dihydrochloride is rapidly converted to Aminoflavone by nonspecific esterases in plasma and cell culture media. AFP464 dihydrochloride is applicable to research related to breast cancer .
    AFP464 dihydrochloride
  • HY-P10765
    DTS-108

    		Peptide-Drug Conjugates (PDCs) Topoisomerase Cancer
    DTS-108 is a prodrug of SN38 (HY-13704) (a Topoisomerase I inhibitor). DTS-108 is a conjugate generated by linking SN38 to a human oligopeptide via an esterase sensitive cross-linker. DTS-108 exhibits anti-tumor activity against colorectal, lung, and mammary cancer .
    DTS-108
  • HY-123120
    SA-152

    		Thrombin Others
    SA-152 is an organophosphorus inhibitor. SA-152 modulates the fibrinogen coagulation and TAME esterase activity of bovine α-thrombin .
    SA-152
  • HY-156984
    Monometacrine

    		Cholinesterase (ChE) CETP Neurological Disease
    Monometacrine is a cholesterol esterase inhibitor. Monometacrine has antidepressant effect .
    Monometacrine
  • HY-19861
    SMP-028

    		Lipase Metabolic Disease
    SMP-028 is an inhibitor of neutral cholesterol esterase (CEase), with an IC50 of 1.01 μM.
    SMP-028
  • HY-143252
    CEase-IN-1

    		Cholinesterase (ChE) Metabolic Disease
    CEase-IN-1 (Compound A1H3) is a potent and selective cholesterol esterase (CEase) inhibitor with an IC50 of 0.36 μM. CEase-IN-1 can be used for the research of hypercholesterolemia .
    CEase-IN-1
  • HY-134451
    Diethylumbelliferyl phosphate

    DEUP

    		 Endogenous Metabolite Metabolic Disease
    Diethylumbelliferyl phosphate (DEUP), a selective and potent inhibitor of cholesterol esterase, does not inhibit protein kinase activity A in vitro, and it effectively disrupts steroidogenesis by blocking the transport of cholesterol into the mitochondria of steroidogenic cells, with an IC50 of 11.6 μM, potentially limiting dietary cholesterol absorption.
    Diethylumbelliferyl phosphate
  • HY-118222
    KBR 2822

    		Cholinesterase (ChE) Neurological Disease
    KBR 2822 is an inhibitor of neurological target esterase (NTE) and has an inhibitory effect on AChE. KBR 2822 can aggravate neurological damage under certain conditions, but does not cause neurological disease when used alone in the absence of direct neurotoxicity or biochemical damage.
    KBR 2822
  • HY-161062
    TAOA AM Ester trimethyl lock

    		EAAT Neurological Disease
    TAOA AM Ester trimethyl lock is a high-affinity fluorescent prodrug-like inhibitor of the excitatory amino acid transporter (EAAT). It can penetrate the cell membrane and be activated by hydrolysis by endogenous cell esterases to form active EAAT inhibitors. TAOA AM Ester trimethyl lock can be used to study neurodegeneration and neuronal cell death .
    TAOA AM Ester trimethyl lock
  • HY-19137
    Pibrozelesin

    KW 2189 free base

    		 Antibiotic Infection Cancer
    Pibrozelesin (KW 2189 free base) is the derivative of antibiotic Duocarmycin B2. Pibrozelesin exhibits antitumor activity, inhibits proliferation of cell H69 with an IC50 of 1.9 μM. Pibrozelesin induces the DNA strand breaks upon activation via carboxyl esterase .
    Pibrozelesin
  • HY-114584
    A-953227

    		Ser/Thr Protease Neurological Disease
    A-953227 is a highly potent and selective inhibitor with the activity of inhibiting calcium-dependent esterase (calpain). A-953227 has enhanced selectivity for related cysteine proteases (cathepsins) and has shown good efficacy in cell experiments. A-953227 has shown broad efficacy in preclinical models for Alzheimer's disease, suggesting that it has potential benefits in inhibiting Alzheimer's disease .
    A-953227
  • HY-172298
    (R,S,S,S)-Orlistat

    (R,S,S,S)-Tetrahydrolipstatin; (R,S,S,S)-Ro-18-0647

    		 Fatty Acid Synthase (FASN) Infection
    (R,S,S,S)-Orlistat is a stereogenic derivative of orlistat (tetrahydrolipstatin; THL) (HY-B0218). (R,S,S,S)-Orlistat inhibits three Mycobacterium tuberculosis lipid esterases, Ag85C (KI: 16.43 μM), Rv3802 (EC50: 16.2 nM), and Pks13-TE .
    (R,S,S,S)-Orlistat
  • HY-B0732R
    Itopride hydrochloride (Standard)

    HSR803 (Standard)

    		 Reference Standards Cholinesterase (ChE) Dopamine Receptor Bacterial Neurological Disease
    Itopride (hydrochloride) (Standard) is the analytical standard of Itopride (hydrochloride). This product is intended for research and analytical applications. Itopride (HSR803) hydrochloride is a potent dopamine-2 antagonist and an acetylcholine esterase (AChE) inhibitor. Itopride hydrochloride enhances gastric motility through both antidopaminergic and anti-acetylcholinesterasic actions, can be used as a gastrointestinal prokinetic agent. Itopride can be used for researching gastro-esophageal reflux disease (GERD) .
    Itopride hydrochloride (Standard)
  • HY-19651A
    Zanapezil

    TAK-147

    		 Cholinesterase (ChE) Neurological Disease
    Zanapezil (TAK-147) is a potent, reversible and selective acetylcholine esterase (AChE) inhibitor. Zanapezil shows a potent and reversible inhibition of AChE activity in homogenates of the rat cerebral cortex (IC50=51.2 nM). Zanapezil shows a moderate inhibition of muscarinic M1 and M2 receptor binding with Ki values of 234 and 340 nM, respectively. Zanapezil can be used for the research of early stages of Alzheimer's disease (AD) .
    Zanapezil
  • HY-19651B
    Zanapezil fumarate

    TAK-147 fumarate

    		 Cholinesterase (ChE) Neurological Disease
    Zanapezil (TAK-147) fumarate is a potent, reversible and selective acetylcholine esterase (AChE) inhibitor. Zanapezil fumarate shows a potent and reversible inhibition of AChE activity in homogenates of the rat cerebral cortex (IC50=51.2 nM). Zanapezil fumarate shows a moderate inhibition of muscarinic M1 and M2 receptor binding with Ki values of 234 and 340 nM, respectively. Zanapezil fumarate can be used for the research of early stages of Alzheimer's disease (AD) .
    Zanapezil fumarate
  • HY-B0732AS
    Itopride-d6

    HSR803-d6 free base

    		 Isotope-Labeled Compounds Dopamine Receptor Bacterial Cholinesterase (ChE) Others
    Itopride-d6 (HSR803-d6 (free base)) is deuterium labeled Itopride. Itopride (HSR803 free base) is a potent and orally active dopamine-2 antagonist and an acetylcholine esterase (AChE) inhibitor. Itopride enhances gastric motility through both antidopaminergic and anti-acetylcholinesterasic actions, can be used as a gastrointestinal prokinetic agent. Itopride can be used for researching gastro-esophageal reflux disease (GERD) .
    Itopride-d6
  • HY-19651
    Zanapezil free base

    TAK-147 free base

    		 Cholinesterase (ChE) Neurological Disease
    Zanapezil (TAK-147) free base is a potent, reversible and selective acetylcholine esterase (AChE) inhibitor. Zanapezil free base shows a potent and reversible inhibition of AChE activity in homogenates of the rat cerebral cortex (IC50=51.2 nM). Zanapezil free base shows a moderate inhibition of muscarinic M1 and M2 receptor binding with Ki values of 234 and 340 nM, respectively. Zanapezil free base can be used for the research of early stages of Alzheimer's disease (AD) .
    Zanapezil free base
  • HY-174450
    KMT9-IN-1

    		Epigenetic Reader Domain Cancer
    KMT9-IN-1 (Compound 8) is a KMT9 inhibitor and the ethyl ester prodrug of compound 7b. KMT9-IN-1 releases the active form 7b via esterases in cells. KMT9-IN-1 targets KMT9 in cells and reduces H4K12me1 levels. KMT9-IN-1 has antitumor activity against colon cancer. KMT9-IN-1 can be used in the research of prostate cancer and hepatocellular carcinoma .
    KMT9-IN-1
  • HY-17484R
    Ampiroxicam (Standard)

    CP 65703 (Standard)

    		 Reference Standards Inflammation/Immunology
    Ampiroxicam (Standard) is the analytical standard of Ampiroxicam. This product is intended for research and analytical applications. Ampiroxicam is an orally active prodrug of non-steroidal anti-inflammatory drug (NSAID). Ampiroxicam inhibits paw swelling in adjuvant-induced arthritis and acute inflammation models, and suppresses phenylbenzoquinone-induced stretching responses in mice. Ampiroxicam is rapidly and completely converted to Piroxicam (HY-B0253) via non-specific esterases and first-pass metabolism. Ampiroxicam induces contact hypersensitivity and photosensitivity reactions through photoproducts generated by UVA. Ampiroxicam can be used in research related to photosensitivity, adjuvant-induced arthritis, rheumatism, osteoarthritis and other inflammatory diseases.
    Ampiroxicam (Standard)
  • HY-182402
    Notum-IN-2

    		Carboxylesterase (CES) Wnt
    Notum-IN-2 is a partially brain-penetrant Notum carboxyl-esterase inhibitor with an IC50 of 18 nM. Notum-IN-2 can be used as a chemical tool for exploring Wnt signalling in cells .
    Notum-IN-2
  • HY-103610R
    4,4'-Dimethoxybenzil (Standard)

    p-Anisil (Standard)

    		 Cholinesterase (ChE) Reference Standards Cancer
    4,4'-Dimethoxybenzil (Standard) is the analytical standard of 4,4'-Dimethoxybenzil (HY-103610). This product is intended for research and analytical applications. 4,4'-Dimethoxybenzil is a human intestinal carboxyl esterase (hiCE) inhibitor with Ki of 70 nM.
    4,4'-Dimethoxybenzil (Standard)
  • HY-137357
    5-Monobutyl methotrexate

    NSC 305986; γ-MBMTX

    		 Dihydrofolate reductase (DHFR) Cancer
    5-Monobutyl methotrexate (NSC 305986; γ-MBMTX) is a dihydrofolate reductase (DHFR) inhibitor and esterase substrate. 5-Monobutyl methotrexate is hydrolyzed by esterases to produce methotrexate. In rhesus monkeys, 5-Monobutyl methotrexate clears more slowly from cerebrospinal fluid than from serum, and its serum protein binding rate exceeds 99%. At the same dose rate, 5-Monobutyl methotrexate achieves cerebrospinal fluid concentrations comparable to those of Methotrexate (HY-14519), and exhibits activity against Methotrexate-resistant cells (with transport defects) that is comparable to that against sensitive parental cells. 5-Monobutyl methotrexate can be used in studies related to Methotrexate-resistant tumors .
    5-Monobutyl methotrexate
  • HY-106409R
    Tefinostat (Standard)

    CHR-2845 (Standard)

    		 Reference Standards HDAC Apoptosis Cancer
    Tefinostat (Standard) is the analytical standard of Tefinostat (HY-106409). This product is intended for research and analytical applications. Tefinostat (CHR-2845) is a monocyte/macrophage targeted histone deacetylase (HDAC) inhibitor. Tefinostat can be cleaved into active acid CHR-2847 by the intracellular esterase human carboxylesterase-1 (hCE-1). Tefinostat can be used for the research of leukaemias .
    Tefinostat (Standard)
  • HY-16031A
    AFP464

    NSC710464

    		 Aryl Hydrocarbon Receptor Integrin Drug Intermediate DNA/RNA Synthesis Cancer
    AFP464 (NSC710464) is a prodrug of Aminoflavone (HY-132974) and an agonist of the aryl hydrocarbon receptor (AhR). AFP464 downregulates the expression of α6-integrin (α6-integrin), inhibits breast tumor growth, reduces the population of tumor-initiating cells, disrupts mammosphere structure, induces the formation of mucin lake clusters, triggers DNA damage, and exerts antiproliferative activity. AFP464 is rapidly converted to Aminoflavone by nonspecific esterases in plasma and cell culture media. AFP464 is applicable to research related to breast cancer .
    AFP464
  • HY-W275793
    Tripropionin

    Glycerol tripropionate

    		 Carboxylesterase (CES) Others
    Tripropionin (Glycerol tripropionate) is a triglyceride that can be hydrolyzed by carboxylic esterase from carrots. Tripropionin can serve as the oil phase for constructing high-performance lipid nanoemulsion droplets, enabling efficient encapsulation of Combretastatin A4 (HY-N2146) to achieve its stable storage and controlled release .
    Tripropionin

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