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Results for "

uptake

" in MCE Product Catalog:

146

Inhibitors & Agonists

2

Screening Libraries

4

Dye Reagents

1

Biochemical Assay Reagents

7

Peptides

29

Natural
Products

1

Recombinant Proteins

12

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas
  • HY-138620
    MCU-i4

    Mitochondrial Metabolism Metabolic Disease
    MCU-i4 blocks the IP3-dependent mitochondrial Ca 2+-uptake, maintaining the gatekeeping role of their target.
  • HY-N2368A
    Arecaidine hydrochloride

    GABA Receptor Neurological Disease
    Arecaidine hydrochloride, a pyridine alkaloid, is a potent GABA uptake inhibitor. Arecaidine hydrochloride is a substrate of H +-coupled amino acid transporter 1 (PAT1, SLC36A1) and competitively inhibits L-proline uptake.
  • HY-N2368
    Arecaidine

    GABA Receptor Neurological Disease
    Arecaidine, a pyridine alkaloid, is a potent GABA uptake inhibitor. Arecaidine is a substrate of H +-coupled amino acid transporter 1 (PAT1, SLC36A1) and competitively inhibits L-proline uptake.
  • HY-N8490
    Eicosyl ferulate

    Others Metabolic Disease
    Eicosyl ferulate, a phenolic compound, is isolated from the fresh root and stem of Aristolochia kankauensis. Eicosyl ferulate exhibits glucose uptake stimulatory activity.
  • HY-N5083
    Saponarin

    Others Inflammation/Immunology
    Saponarin is a natural flavonoid isolated from Gypsophila trichotoma, with antioxidant, anti-inflammatory and hepatoprotective activities. Saponarin activates AMPK in a calcium-dependent manner, thus regulating gluconeogenesis and glucose uptake.
  • HY-103341
    UCM707

    Cannabinoid Receptor Neurological Disease
    UCM707, a potent and selective inhibitor of endocannabinoid uptake, potentiates hypokinetic and antinociceptive effects of Anandamide.
  • HY-118166
    Gentisein

    NSC 329491; 1,3,7-Trihydroxyxanthone

    5-HT Receptor Neurological Disease
    Gentisein (NSC 329491), the major metabolite of Mangiferin, shows the most potent serotonin uptake inhibition with an IC50 value of 4.7 µM.
  • HY-100416A
    LY2365109 hydrochloride

    GlyT Neurological Disease
    LY2365109 hydrochloride is a potent and selective GlyT1 inhibitor, with an IC50 of 15.8 nM for glycine uptake in cells over-expressing hGlyT1a.
  • HY-69359
    Nipecotic acid

    (±)-β-Homoproline; Hexahydronicotinic acid; 3-Carboxypiperidine

    GABA Receptor Neurological Disease
    Nipecotic acid ((±)-β-Homoproline) is a potent inhibitor of neuronal and glial-aminobutyric acid (GABA) uptake in vitro. Nipecotic acid can also directly activate GABAA-like chloride channels, with an EC50 of approximately 300 μM.
  • HY-N9407
    Guvacine ethyl ester

    Others Others
    Guvacine ethyl ester (3.1b) is an alkaloid that can be found in betel nut. Guvacine ethyl ester can be used in the synthesis of GABA uptake inhibitor.
  • HY-N7605
    11-epi-mogroside V

    Others Metabolic Disease
    11-epi-mogroside V is a mogroside in the fruit of Siraitia grosvenori. 11-epi-mogroside V exhibits considerable bioactivity in promoting glucose uptake in human HepG2 cells in vitro.
  • HY-101315
    AHN 1-055 hydrochloride

    3α-Bis-(4-fluorophenyl) Methoxytropane hydrochloride

    Dopamine Transporter Neurological Disease
    AHN 1-055 hydrochloride is a dopamine uptake inhibitor, with an IC50 of 71 nM. AHN 1-055 hydrochloride binds with high affinity to the dopamine transporter (DAT) and may serve as leads for the development of agentia to treat cocaine abuse.
  • HY-107522
    DL-TBOA

    EAAT2 Neurological Disease
    DL-TBOA is a potent non-transportable inhibitor of excitatory amino acid transporters with IC50s of 70 μM, 6 μM and 6 μM for excitatory amino acid transporter-1 (EAAT1), EAAT2 and EAAT3, respectively. DL-TBOA inhibits the uptake of [ 14C]glutamate in COS-1 cells expressing the human EAAT1 and EAAT2 with Ki valuesof 42 μM and 5.7 μM, respectively. DL-TBOA blocks EAAT4 and EAAT5 in a competitive manner with Ki values of 4.4 μM and 3.2 μM, respectively.
  • HY-107522B
    DL-TBOA ammonium

    EAAT2 Neurological Disease
    DL-TBOA ammonium is a potent non-transportable inhibitor of excitatory amino acid transporters with IC50s of 70 μM, 6 μM and 6 μM for excitatory amino acid transporter-1 (EAAT1), EAAT2 and EAAT3, respectively. DL-TBOA ammonium inhibits the uptake of [ 14C]glutamate in COS-1 cells expressing the human EAAT1 and EAAT2 with Ki valuesof 42 μM and 5.7 μM, respectively. DL-TBOA ammonium blocks EAAT4 and EAAT5 in a competitive manner with Ki values of 4.4 μM and 3.2 μM, respectively.
  • HY-100957
    Dilazep dihydrochloride

    Others Cardiovascular Disease
    Dilazep dihydrochloride is an inhibitor of adenosine uptake. Dilazep dihydrochloride has cerebral and coronary vasodilating action through enhancement of effect of adenosine. Dilazep dihydrochloride also inhibits the ischemic damage, platelet aggregation, and membrane transport of nucleosides.
  • HY-108510
    Rimcazole dihydrochloride

    BW 234U dihydrochloride

    Sigma Receptor Dopamine Receptor Cancer Neurological Disease
    Rimcazole (BW 234U) dihydrochloride is a carbazole derivative that acts in part as a sigma (σ) receptor antagonist. Rimcazole dihydrochloride also binds with moderate affinity to the dopamine transporter and inhibit dopamine uptake. Rimcazole dihydrochloride can attenuate cocaine-induced locomotor activity and sensitization. Rimcazole dihydrochloride also can be used for the research of cancer.
  • HY-126302
    DMT1 blocker 2

    Others Metabolic Disease
    DMT1 blocker 2 is a direct inhibitor of divalent metal transporter 1 (DMT1), with an IC50 of 0.83 μM. DMT1 blocker 2 can block iron uptake by enterocytes in vivo.
  • HY-135880A
    OMDM-4

    Endogenous Metabolite Neurological Disease
    OMDM-4 is a selective and metabolically stable inhibitor of anandamide cellular uptake (ACU), with a Ki 17.7 μM.
  • HY-135880
    OMDM-3

    Endogenous Metabolite Neurological Disease
    OMDM-3 is a selective and metabolically stable inhibitor of anandamide cellular uptake (ACU), with a Ki of 16.6 μM.
  • HY-121557
    OMDM-1

    Endogenous Metabolite Neurological Disease
    OMDM-1 is a potent, selective and metabolically stable inhibitor of anandamide cellular uptake (ACU), with a Ki of 2.4 μM.
  • HY-103342
    OMDM-2

    Endogenous Metabolite Neurological Disease
    OMDM-2 is a potent, selective and metabolically stable inhibitor of anandamide cellular uptake (ACU), with a Ki of 3.0 μM.
  • HY-N3426
    Kazinol B

    NO Synthase Akt AMPK Metabolic Disease
    Kazinol B, a prenylated flavan with a dimethyl pyrane ring, is an inhibitor of nitric oxide (NO) production. Kazinol B improves insulin sensitivity by enhancing glucose uptake via the insulin-Akt signaling pathway and AMPK activation. Kazinol B has the potential for diabetes mellitus research.
  • HY-B1002
    Oxolinic acid

    Bacterial Antibiotic DNA/RNA Synthesis Infection
    Oxolinic acid is an antibiotic against both Gram-negative and Gram-positive bacteria. Oxolinic acid can be used for the research of acute and chronic urinary tract infections. Oxolinic acid is a DNA/RNA synthesis inhibitor. Oxolinic acid acts a dopamine uptake inhibitor and stimulants locomotor effect in mice.
  • HY-128420
    Lobeline sulfate

    α-Lobeline sulfate; L-Lobeline sulfate

    Endogenous Metabolite Neurological Disease
    Lobeline sulfate (α-Lobeline sulfate; L-Lobeline sulfate) is a nonstimulant medication that can alter dopamine uptake in brain. Lobeline sulfate (α-Lobeline sulfate; L-Lobeline sulfate) inhibits nicotine-induced hyperactivity and is effective in smoking cessation.
  • HY-10865
    LY2183240

    FAAH Autophagy Neurological Disease
    LY2183240 is a highly potent blocker of anandamide uptake (IC50= 270 pM; Ki=540 nM). LY2183240 is a potent, covalent inhibitor of the endocannabinoid-degrading enzyme fatty acid amide hydrolase (FAAH) with an IC50 of 12.4 nM. LY2183240 inactivates FAAH by carbamylation of the enzyme's serine nucleophile. LY2183240 also inhibits several other brain serine hydrolases with IC50s of 5.3, 0.09, 8.2 nM for MAG lipase, bh6 and KIAA1363, respectively .
  • HY-143617
    photoCORM-1

    Others Cancer
    photoCORM-1 (compound 8) is a combinatorial carbon monoxide releasing molecule (CORM). photoCORM-1 exhibits good cellular uptake and real-time monitoring ability of CO uncaging by a color change approach. photoCORM-1 has anti-tumor antivity.
  • HY-143618
    photoCORM-2

    Others Cancer
    photoCORM-2 (compound 3) is a single carbon monoxide releasing molecule (CORM). photoCORM-2 exhibits good cellular uptake and real-time monitoring ability of CO uncaging by a color change approach. photoCORM-2 has anti-tumor activity.
  • HY-125990
    SLC13A5-IN-1

    Sodium Channel Metabolic Disease Cardiovascular Disease
    SLC13A5-IN-1 is a selective sodium-citrate co-transporter (SLC13A5) inhibitor. SLC13A5-IN-1 completely blocks the uptake of  14C-citrate with an IC50 value of 0.022 μM in HepG2 cells. SLC13A5-IN-1 has the potential for the treatment of metabolic and/or cardiovascular diseases. SLC13A5-IN-1 is extracted from patent WO2018104220A1, Compound I-5.
  • HY-112683
    V-9302

    Others Cancer
    V-9302 is a competitive antagonist of transmembrane glutamine flux. V-9302 selectively and potently targets the amino acid transporter ASCT2 (SLC1A5) not ASCT1. V-9302 inhibits ASCT2-mediated glutamine uptake (IC50=9.6 µM) in HEK-293 cells.
  • HY-112683A
    V-9302 hydrochloride

    Others Cancer
    V-9302 hydrochloride is a competitive antagonist of transmembrane glutamine flux. V-9302 hydrochloride selectively and potently targets the amino acid transporter ASCT2 (SLC1A5) not ASCT1. V-9302 hydrochloride inhibits ASCT2-mediated glutamine uptake (IC50=9.6 µM) in HEK-293 cells.
  • HY-135882
    OMDM-6

    TRP Channel Cannabinoid Receptor Endogenous Metabolite Neurological Disease
    OMDM-6 is a hybrid agonist of vanilloid receptor type 1 (VR1, TRPV1) (EC50=75 nM) and cannabinoid receptor type 1 (CB1) (Ki=3.2 μM). OMDM-6 inhibits anandamide cellular uptake (ACU) with a Ki of 7.0 μM.
  • HY-135881
    OMDM-5

    TRP Channel Endogenous Metabolite Neurological Disease
    OMDM-5 is a selective inhibitor of anandamide cellular uptake (ACU), with a Ki of 4.8 μM. OMDM-5 is also a potent vanilloid receptor type 1 (VR1, TRPV1) agonist, with an EC50 of 75 nM, and shows weakly active as cannabinoid receptor type 1 (CB1) ligand (Ki=4.9 μM).
  • HY-U00049
    Mioflazine

    Others Neurological Disease Cardiovascular Disease
    Mioflazine is an orally active nucleoside transport inhibitor, has the potential for sleep disorders treatment. Mioflazine inhibits nucleoside uptake.
  • HY-B0696B
    Tiagabine hydrochloride hydrate

    NO050328 hydrochloride hydrate; NO328 hydrochloride hydrate; TGB hydrochloride hydrate

    GABA Receptor Neurological Disease
    Tiagabine hydrochloride hydrate is a potent and selective GABA uptake inhibitor, used as an anticonvulsant agent, with IC50s of 67, 446 and 182 nM for [ 3H]GABA uptake in Synaptosomes, Neurons and Glia, respectively.
  • HY-N0749
    Jatrorrhizine

    AChE 5-HT Receptor Bacterial Neurological Disease
    Jatrorrhizine is an alkaloid isolated from Coptis chinensis with neuroprotective, antimicrobial, antiplasmodial and antioxidant activities. Jatrorrhizine is a potent and orally active inhibitor of AChE (IC50=872 nM) over >115-fold selectivity for BuChE. Jatrorrhizine reduces uptake of serotonin (5-HT) and norepinephrine (NE) via inhibition of uptake-2 transporters.
  • HY-N0740
    Jatrorrhizine chloride

    AChE 5-HT Receptor Bacterial Inflammation/Immunology Neurological Disease
    Jatrorrhizine chloride is an alkaloid isolated from Coptis chinensis with neuroprotective, antimicrobial, antiplasmodial and antioxidant activities. Jatrorrhizine chloride is a potent and orally active inhibitor of AChE (IC50=872 nM) over >115-fold selectivity for BuChE. Jatrorrhizine chloride reduces uptake of serotonin (5-HT) and norepinephrine (NE) via inhibition of uptake-2 transporters.
  • HY-B0444
    Maprotiline hydrochloride

    Autophagy Neurological Disease
    Maprotiline hydrochloride is a selective noradrenalin re-uptake inhibitor and a tetracyclic antidepressant.
  • HY-17553
    Coluracetam

    MKC-231

    iGluR Neurological Disease
    Coluracetam(MKC-231) is a new choline uptake enhancer.
  • HY-N0749A
    Jatrorrhizine hydroxide

    AChE 5-HT Receptor Bacterial Inflammation/Immunology Neurological Disease
    Jatrorrhizine hydroxide is an alkaloid isolated from Coptis chinensis with neuroprotective, antimicrobial, antiplasmodial and antioxidant activities. Jatrorrhizine hydroxide is a potent and orally active inhibitor of AChE (IC50=872 nM) over >115-fold selectivity for BuChE. Jatrorrhizine hydroxide reduces uptake of serotonin (5-HT) and norepinephrine (NE) via inhibition of uptake-2 transporters.
  • HY-B1110A
    Nomifensine maleate

    (±)-Nomifensine maleat

    Dopamine Receptor Neurological Disease
    Nomifensine maleate is a selective inhibitor of dopamine uptake, used in adult attention deficit disorder.
  • HY-B1287
    Citalopram hydrobromide

    (±)-Citalopram hydrobromide; Lu 10-171

    Serotonin Transporter Autophagy Neurological Disease Cancer
    Citalopram hydrobromide is a selective serotonin reuptake inhibitor (SSRI). Citalopram hydrobromide inhibits 5-HT uptake into synaptosomes with an IC50 of 1.8 nM. Citalopram hydrobromideinhibits the 5-HT uptake in rabbit blood platelets with an IC50 of 14 nM. Antidepressant effect.
  • HY-108322
    NBTGR

    Others Cardiovascular Disease
    NBTGR (p-Nitrobenzylthioguanosine) is a potent inhibitor of nucleoside transport; inhibits adenosine uptake with a Ki of 70 nM.
  • HY-B0312
    Dipyridamole

    Phosphodiesterase (PDE) Cardiovascular Disease
    Dipyridamole (Persantine) is a phosphodiesterase inhibitor that blocks uptake and metabolism of adenosine by erythrocytes and vascular endothelial cells.
  • HY-12392
    Iprindole

    5-HT Receptor Metabolic Disease Neurological Disease
    Iprindole, a tricyclic indole antidepressant, is a weak inhibitor of the uptake of noradrenaline and 5-HT.
  • HY-W008610
    GBR 12783

    Dopamine Receptor Neurological Disease
    GBR 12783 is a specific, potent and selective dopamine uptake inhibitor that inhibits the [ 3H]dopamine uptake by rat and mice striatal synaptosomes with IC50s of 1.8 nM and 1.2 nM, respectively. GBR 12783 can improve memory performance and increase hippocampal acetylcholine release in rats.
  • HY-90003A
    Tianeptine sodium salt

    5-HT Receptor Neurological Disease
    Tianeptine sodium salt is a selective facilitator of 5-HT uptake. Tianeptine sodium salt has no affinity for a wide range of receptors, including 5-HT and dopamine (IC50>10 μM) and has no effect on noradrenalin or dopamine uptake. Tianeptine sodium salt has antidepressant, anxiolytic, analgesic and neuroprotective activities.
  • HY-90003
    Tianeptine

    5-HT Receptor Neurological Disease
    Tianeptine is a selective facilitator of 5-HT uptake. Tianeptine has no affinity for a wide range of receptors, including 5-HT and dopamine (IC50>10 μM) and has no effect on noradrenalin or dopamine uptake. Tianeptine has antidepressant, anxiolytic, analgesic and neuroprotective activities.
  • HY-100968
    GBR 12783 dihydrochloride

    Dopamine Receptor Neurological Disease
    GBR 12783 dihydrochloride is a specific, potent and selective dopamine uptake inhibitor that inhibits the [ 3H]dopamine uptake by rat and mice striatal synaptosomes with IC50s of 1.8 nM and 1.2 nM, respectively. GBR 12783 dihydrochloride can improve memory performance and increase hippocampal acetylcholine release in rats.
  • HY-119468
    Medifoxamine

    Dopamine Receptor Neurological Disease
    Medifoxamine is a monoamine re-uptake inhibiting antidepressive drug which preferentially inhibits dopamine reuptake.
  • HY-B1127
    Betamipron

    N-Benzoyl-β-alanine

    Bacterial Antibiotic Others
    Betamipron is a chemical compound which is used together with Panipenem to inhibit Panipenem uptake into the renal tubule and prevent nephrotoxicity.
  • HY-12390
    Lofepramine

    Lopramine

    Others Neurological Disease
    Lofepramine (Lopramine) is a potent tricyclic antidepressant and is extensively metabolised to Desipramine. The antidepressant activity of Lofepramine stems from the facilitation of noradrenergic neurotransmission by uptake inhibition. Lofepramine may also potentiate serotoninergic neurotransmission by inhibition of the neuronal uptake of serotonin and the enzyme tryptophan pyrrolase. Lofepramine has significant anxiolytic efficacy in addition to its antidepressant properties.
  • HY-10809
    Bitopertin

    RG1678; RO4917838

    GlyT Neurological Disease
    Bitopertin is a potent, noncompetitive glycine reuptake inhibitor, inhibits glycine uptake at human GlyT1 with a concentration exhibiting IC50 of 25 nM.
  • HY-B0937
    Amprolium

    Parasite Infection
    Amprolium is a coccidiostat used in poultry, is a thiamine analogue and blocks the thiamine transporter of Eimeria species by blocking thiamine uptake it prevents carbohydrate synthesis.
  • HY-B0937A
    Amprolium hydrochloride

    Parasite Infection
    Amprolium hydrochloride is a coccidiostat used in poultry, is a thiamine analogue and blocks the thiamine transporter of Eimeria species by blocking thiamine uptake it prevents carbohydrate synthesis.
  • HY-A0275
    Amezinium methylsulfate

    Amezinium metilsulfate; Lu-1631

    Adrenergic Receptor Cardiovascular Disease Endocrinology
    Amezinium metilsulfate has multiple mechanisms, including stimulation of alpha and beta-1 receptors and inhibition ofnoradrenaline and tyramine uptake.
  • HY-B0444S
    Maprotiline-d5 hydrochloride

    Autophagy Neurological Disease
    Maprotiline-d5 hydrochloride is the deuterium labeled Maprotiline hydrochloride. Maprotiline hydrochloride is a selective noradrenalin re-uptake inhibitor and a tetracyclic antidepressant.
  • HY-17385
    Atomoxetine hydrochloride

    Tomoxetine hydrochloride; LY 139603; (R)-Tomoxetine hydrochloride

    Others Neurological Disease
    Atomoxetine hydrochloride is a potent and selective noradrenalin re-uptake inhibitor (Ki values are 5, 77 and 1451 nM for inhibition of radioligand binding to human NET, SERT and DAT respectively).
  • HY-B0211
    Riluzole

    PK 26124

    Sodium Channel GABA Receptor Neurological Disease
    Riluzole is an anticonvulsant drug and belongs to the family of use-dependent Na + channel blocker which can also inhibit GABA uptake with an IC50 of 43 μM.
  • HY-N2209
    Angeloylgomisin H

    PPAR Metabolic Disease
    Angeloylgomisin H, as a major lignin extract of Schisandra rubriflora, has the potential to improve insulin-stimulated glucose uptake by activating PPAR-γ.
  • HY-B0211A
    Riluzole hydrochloride

    PK 26124 hydrochloride

    Sodium Channel GABA Receptor Neurological Disease
    Riluzole hydrochloride is an anticonvulsant drug and belongs to the family of use-dependent Na + channel blocker which can also inhibit GABA uptake with an IC50 of 43 μM.
  • HY-B0312S1
    Dipyridamole-d16

    Phosphodiesterase (PDE) Cardiovascular Disease
    Dipyridamole-d16 is the deuterium labeled Dipyridamole. Dipyridamole (Persantine) is a phosphodiesterase inhibitor that blocks uptake and metabolism of adenosine by erythrocytes and vascular endothelial cells.
  • HY-133033
    COQ7-IN-1

    Others Metabolic Disease
    COQ7-IN-1, a highly potent inhibitor of human coenzyme Q (COQ7), interferes with ubiquinone (UQ) synthesis. COQ7-IN-1 does not disturb physiological cell growth of human normal culture cells. COQ7-IN-1 can be used for the research of the balance between UQ supplementation pathways: de novo UQ synthesis and extracellular UQ uptake.
  • HY-14560C
    Reboxetine mesylate

    FCE20124 mesylate; PNU155950E mesylate

    Adrenergic Receptor Neurological Disease
    Reboxetine mesylate (FCE20124 mesylate) is a potent, selective, and specific noradrenaline reuptake inhibitor (NARI) for the research of depression. Reboxetine mesylate inhibits the uptake of norepinephrine, with a Ki of 8 nM.
  • HY-N0735
    Phellodendrine chloride

    Others Cancer
    Phellodendrine chloride is a plant alkaloid found in Phellodendron amurense. Phellodendrine chloride suppresses the proliferation of KRAS mutated pancreatic cancer cells through inhibition of nutrients uptake via macropinocytosis .
  • HY-115461
    MID-1

    Insulin Receptor Metabolic Disease
    MID-1 is a disruptor of MG53-IRS-1 (Mitsugumin 53-insulin receptor substrate-1) interaction. MID-1 disrupts molecular association of MG53 with IRS-1 and abolishes MG53-induced IRS-1 ubiquitination and degradation in skeletal muscle, leading to elevated IRS-1 expression level and increased insulin signaling and glucose uptake.
  • HY-14202
    Lazabemide hydrochloride

    Ro 19-6327 hydrochloride

    Monoamine Oxidase Neurological Disease
    Lazabemide hydrochloride (Ro 19-6327 hydrochloride) is a selective, reversible inhibitor of monoamine oxidase B (MAO-B) (IC50=0.03 μM) but less active for MAO-A (IC50>100 μM). Lazabemide  inhibits monoamine uptake at high concentrations, the IC50 values are 86 μM, 123 μM and >500 μM for noradrenalin, serotonin and dopamine uptake, respectively. Lazabemide can be used for the research of parkinson and alzheimer′s disease.
  • HY-14201
    Lazabemide

    Ro 19-6327

    Monoamine Oxidase Neurological Disease
    Lazabemide (Ro 19-6327) is a selective, reversible inhibitor of monoamine oxidase B (MAO-B) (IC50=0.03 μM) but less active for MAO-A (IC50>100 μM). Lazabemide  inhibits monoamine uptake at high concentrations, the IC50 values are 86 μM, 123 μM and >500 μM for noradrenalin, serotonin and dopamine uptake, respectively. Lazabemide can be used for the research of parkinson and alzheimer′s disease.
  • HY-B0312S
    Dipyridamole-d20

    Phosphodiesterase (PDE) Cardiovascular Disease
    Dipyridamole-d20 is the deuterium labeled Dipyridamole. Dipyridamole is a phosphodiesterase inhibitor that blocks uptake and metabolism of adenosine by erythrocytes and vascular endothelial cells.
  • HY-W009208
    Calcium L-Threonate

    Endogenous Metabolite Metabolic Disease
    Calcium L-Threonate is an anti-osteoporosis agent, and widely used as a calcium supplement. Calcium L-Threonate also stimulates the uptake of ascorbic acid.
  • HY-126301
    DMT1 blocker 1

    Others Inflammation/Immunology
    DMT1 blocker 1 is a blocker of divalent metal transporter 1 (DMT1) with an IC50 of 0.64 μM, is expected to block iron uptake by enterocytes in vivo.
  • HY-122272
    Paroxetine

    Serotonin Transporter Adrenergic Receptor Neurological Disease
    Paroxetine, a phenylpiperidine derivative, is a potent and selective serotonin reuptake inhibitor (SSRI). Paroxetine is a very weak inhibitor of norepinephrine (NE) uptake but it is still more potent at this site than the other SSRIs.
  • HY-107203
    Propentofylline

    HWA 285

    Phosphodiesterase (PDE) Inflammation/Immunology Neurological Disease
    Propentofylline is a xanthine-derivative that inhibits adenosine uptake and blocks phosphodiesterase activity. Propentofylline has neuroprotective, antiproliferative, and anti-inflammatory effects that improve cognition and dementia severity in patients with Alzheimer's disease or vascular dementia.
  • HY-134452
    MeAIB

    α-(Methylamino)isobutyric acid

    Others Others
    MeAIB (α-(Methylamino)isobutyric acid) is a specific substrate for amino acid transport system A (ATA1). ATA mediate the uptake of short-chain neutral amino acids in a Na +-dependent manner.
  • HY-101849
    Fasentin

    GLUT Cancer Cardiovascular Disease
    Fasentin, a potent glucose uptake inhibitor, inhibits GLUT-1/GLUT-4 transporters. Fasentin preferentially inhibits GLUT4 (IC50=68 μM) over GLUT1. Fasentin is a death receptor stimuli (FAS) sensitizer and sensitizes cells to FAS-induced cell death. Fasentin is also a tumor necrosis factor (TNF) apoptosis-inducing ligand sensitizer. Fasentin blocks glucose uptake in cancer cell lines and has anti-angiogenic activity.
  • HY-B0696A
    Tiagabine hydrochloride

    NO050328 hydrochloride; NO328 hydrochloride; TGB hydrochloride

    GABA Receptor Neurological Disease
    Tiagabine hydrochloride is a potent and selective GABA reuptake inhibitor, used as an anticonvulsant agent, with IC50s of 67, 446 and 182 nM for [ 3H]GABA uptake in Synaptosomes, Neurons and Glia, respectively.
  • HY-18610
    Diclofensine hydrochloride

    Ro 8-4650 hydrochloride

    Dopamine Transporter Neurological Disease
    Diclofensine hydrochloride (Ro-8-4650 hydrochloride) is a potent inhibitor of monoamine reuptake, blocking the uptake of dopamine, noradrenaline, and serotonin by rat brain synaptosomes with IC50 values of 0.74, 2.3, and 3.7 nM, respectively.
  • HY-15515
    SEA0400

    Na+/Ca2+ Exchanger Cardiovascular Disease
    SEA0400 is a novel and selective inhibitor of the Na +-Ca 2+ exchanger (NCX), inhibiting Na +-dependent Ca 2+ uptake in cultured neurons, astrocytes, and microglia with IC50s of from 5 to 33 nM.
  • HY-10809A
    Bitopertin (R enantiomer)

    RG1678 (R enantiomer); RO4917838 (R enantiomer)

    GlyT Neurological Disease
    Bitopertin R enantiomer (RG1678 R enantiomer; RO4917838 R enantiomer) is the R-enantiomer of Bitopertin. Bitopertin is a potent, noncompetitive glycine reuptake inhibitor, inhibits glycine uptake at human GlyT1 with a concentration exhibiting IC50 of 25 nM.
  • HY-18610A
    Diclofensine

    Ro 8-4650

    Dopamine Transporter Neurological Disease
    Diclofensine(Ro-8-4650) is a potent inhibitor of monoamine reuptake, blocking the uptake of dopamine, noradrenaline, and serotonin by rat brain synaptosomes with IC50 values of 0.74, 2.3, and 3.7 nM, respectively.
  • HY-A0171A
    Benzoctamine hydrochloride

    Ba-30803

    5-HT Receptor Neurological Disease
    Benzoctamine hydrochloride (Ba-30803) is a psychoactive agent with anti-anxiety effect. Benzoctamine hydrochloride blocks the central postsynaptic serotonin receptors and decreases 5-HT turnover in the brain.
  • HY-100769
    Hypidone hydrochloride

    YL0919

    5-HT Receptor Neurological Disease
    Hypidone hydrochloride (YL0919) is an orally active antidepressant agent with dual activity as a highly seletive 5-HT uptake blocker and an effective 5-HT1A receptor agonist (Ki=0.19 nM). Hypidone hydrochloride inhibits the uptake of [ 3H]-5-HT into rat cerebral cortical synaptosomes and HEK293 cells with IC50s of 1.78 nM and 1.93 nM, respectively. Hypidone hydrochloride shows remarkable antidepressant effects in animal models and has the poential for the investigation of depressive disorder.
  • HY-108256
    Melitracen hydrochloride

    5-HT Receptor Neurological Disease
    Melitracen hydrochloride is an orally active biphasic antidepressant and antianxiety agent. Melitracen hydrochloride can inhibit the uptake of Norepinephrine and 5-HT (serotonin) through the presynaptic membrane inducing the increase of monoamine transmitters in synaptic space.
  • HY-W010936
    Nitrobenzylthioinosine

    NBMPR

    Adenosine Receptor Neurological Disease
    Nitrobenzylthioinosine is an ENT1 transporter inhibitor that binds to ENT1 transporter with high affinity. Nitrobenzylthioinosine is a photoaffinity probe for adenosine uptake sites in brain. Nitrobenzylthioinosine can cross the blood-brain barrier.
  • HY-B0696
    Tiagabine

    NO050328; NO328; TGB

    GABA Receptor Neurological Disease
    Tiagabine (NO050328) is a potent and selective GABA reuptake inhibitor, used as an anticonvulsant agent, with IC50s of 67, 446 and 182 nM for [ 3H]GABA uptake in Synaptosomes, Neurons and Glia, respectively.
  • HY-N6258
    Kahweol

    AMPK Apoptosis Metabolic Disease
    Kahweol is one of the consituents of the coffee from Coffea Arabica with anti-inflammatory anti-angiogenic, and anti-cancerous activities. Kahweol inhibits adipogenesis and increase glucose uptake by AMP-activated protein kinase (AMPK) activation. Kahweol induces apoptosis.
  • HY-N0647
    Silychristin

    Others Endocrinology
    Silychristin is an abundant flavonolignan present in the fruits of Silybum marianum, with antioxidant properties. Silychristin is a potent inhibitor of the thyroid hormone transporter MCT8, and elicits a strong inhibition of T3 uptake with an IC50 of 110 nM.
  • HY-132898
    PI3K-IN-23

    PI3K Others
    PI3K-IN-23 is an (E)-9-oxooctadec-10-en-12-ynoic acid analogue to promote glucose uptake with an EC50 value of 7.00 μM.
  • HY-107658
    SN 6

    Na+/Ca2+ Exchanger Cardiovascular Disease
    SN 6 is a selective Na +/Ca 2+ exchanger (NCX) inhibitor, and inhibits 45Ca 2+ uptake by NCX1, NCX2, and NCX3, with IC50s of 2.9, 16, and 8.6 μM, respectively.
  • HY-16137
    Cefaloglycin

    Cephaloglycin

    Bacterial Infection
    Cefaloglycin (Cephaloglycin) is an orally active nephrotoxic β-lactam cephalosporin antibiotic with antibacterial activity. Cefaloglycin is activity against Gram-Positive cocci other than enterococci. Cefaloglycin is toxic to mitochondrial substrate uptake and respiration.
  • HY-14542
    Ziprasidone

    CP-88059

    5-HT Receptor Dopamine Receptor Neurological Disease
    Ziprasidone, an antipsychotic agent, is a combined 5-HT (serotonin) and dopamine receptor antagonist. Ziprasidone has high affinity for rat (Ki: 3.4 nM)/human (2.5 nM) 5-HT1A receptors, 5-HT2A (0.42 nM), and dopamine D2 receptors (4.8 nM). Ziprasidone is an inhibitor of norepinephrine reuptake.
  • HY-101903A
    BMS-309403 sodium

    FABP Metabolic Disease Cardiovascular Disease
    BMS-309403 sodium is a potent, orally active, and selective adipocyte fatty acid binding protein (also known as FABP4, aP2) inhibitor, with Kis of <2, 250, and 350 nM for FABP4, FABP3, and FABP5, respectively. BMS-309403 sodium interacts with the fatty-acid-binding pocket within the interior of the protein and competitively inhibits the binding of endogenous fatty acids. BMS-309403 sodium improves endothelial function in apolipoprotein E-deficient mice and in cultured human endothelial cells.
  • HY-101903
    BMS-309403

    FABP Metabolic Disease Cardiovascular Disease
    BMS-309403 is a potent, orally active and selective adipocyte fatty acid binding protein (also known as FABP4, aP2) inhibitor with Kis of <2, 250, and 350 nM for FABP4, FABP3, and FABP5, respectively. BMS-309403 interacts with the fatty-acid-binding pocket within the interior of the protein and competitively inhibits the binding of endogenous fatty acids. BMS-309403 improves endothelial function in apolipoprotein E-deficient mice and in cultured human endothelial cells.
  • HY-14542A
    Ziprasidone hydrochloride

    CP-88059 hydrochloride

    5-HT Receptor Dopamine Receptor Neurological Disease
    Ziprasidone (CP-88059) hydrochloride, an antipsychotic agent, is a combined 5-HT (serotonin) and dopamine receptor antagonist. Ziprasidone hydrochloride has high affinity for rat (Ki: 3.4 nM)/human (2.5 nM) 5-HT1A receptors, 5-HT2A (0.42 nM), and dopamine D2 receptors (4.8 nM). Ziprasidone hydrochloride is an inhibitor of norepinephrine reuptake.
  • HY-P2231A
    Cotadutide acetate

    MEDI0382 acetate

    Glucagon Receptor Metabolic Disease
    Cotadutide acetate (MEDI0382 acetate) is a potent peptide dual agonist of glucagon-like peptide-1 (GLP-1) and glucagon receptor with EC50 values of 6.9 pM and 10.2 pM, respectively. Cotadutide acetate (MEDI0382 acetate) exhibits ability to facilitate both weight loss and glycaemic control, has the potential for obesity and type 2 diabetes (T2D) treatment.
  • HY-17407
    Ziprasidone hydrochloride monohydrate

    CP 88059 hydrochloride monohydrate

    5-HT Receptor Dopamine Receptor Neurological Disease
    Ziprasidone (CP 88059) hydrochloride monohydrate, an antipsychotic agent, is an orally active combined 5-HT (serotonin) and dopamine receptor antagonist. Ziprasidone hydrochloride monohydrate has high affinity for rat (Ki: 3.4 nM)/human (2.5 nM) 5-HT1A receptors, 5-HT2A (0.42 nM), and dopamine D2 receptors (4.8 nM). Ziprasidone hydrochloride monohydrate is an inhibitor of norepinephrine reuptake.
  • HY-144793
    Deac-SS-Biotin

    Others Cancer
    Deac-SS-Biotin is a potent antitumor agent. Deac-SS-Biotin uptakes into the cells through biotin-mediated internalization. Deac-SS-Biotin combined with DTT (Glutathione mimetic) can effectively inhibit microtubule assembly and displays greater antitumor activity.
  • HY-100800
    TACA

    trans-4-Aminocrotonic acid

    GABA Receptor Neurological Disease
    TACA (trans-4-Aminocrotonic acid) is a potent agonist of GABAA and GABAC receptors (KD= 0.6 μM). TACA also is GABA uptake inhibitor and substrate for GABA-T. TACA produces late biphasic responses in the MPG neurons.
  • HY-23999
    BI-0115

    Others Cardiovascular Disease
    BI-0115 is a selective inhibitor of LOX-1 (IC50=5.4 µM) that blocks cellular uptake of oxLDL. BI-0115 binding triggers receptor inhibition by formation of dimers of the homodimeric ligand binding domain.
  • HY-18610S
    Diclofensine-d3 hydrochloride

    Dopamine Transporter Neurological Disease
    Diclofensine-d3 hydrochloride is the deuterium labeled Diclofensine hydrochloride. Diclofensine hydrochloride (Ro-8-4650 hydrochloride) is a potent inhibitor of monoamine reuptake, blocking the uptake of dopamine, noradrenaline, and serotonin by rat brain synaptosomes with IC50 values of 0.74, 2.3, and 3.7 nM, respectively.
  • HY-108540
    LAT1-IN-1

    BCH

    Apoptosis Cancer
    LAT1-IN-1 (BCH) is a selective and competitive inhibitor of large neutral amino acid transporter 1 (LAT1) significantly inhibit cellular uptake of amino acids and mTOR phosphorylation, which induces the suppression of cancer growth and apoptosis.
  • HY-A0160
    Indalpine

    LM 5008

    Serotonin Transporter Neurological Disease
    Indalpine (LM 5008) is a potent and selective 5-HT uptake blocker. Indalpine is potent in displacing 3H-5-HT bound to brain membranes with the IC50 of 36 μM. Indalpine, two antidepressant agent.
  • HY-137331
    FAPI-46

    Others Cancer
    FAPI-46 is a quinoline-based fibroblast activation protein (FAP)-targeted radiotracer. FAPI-46 has higher tumor uptake and prolonged tumor accumulation. FAPI-46 can be used for tumor imaging of a multitude of different cancers.
  • HY-16974
    Afoxolaner

    GABA Receptor Chloride Channel Parasite Infection
    Afoxolaner is an orally active isoxazoline insecticide/acaricide against Ixodes scapularis in dogs. Afoxolaner acts on the insect γ-aminobutyric acid receptor (GABA) and glutamate receptors, inhibiting GABA & glutamate-regulated uptake of chloride ions, resulting in excess neuronal stimulation and death of the arthropod.
  • HY-142955
    Dual photoCORM 1

    Others Cancer
    Dual photoCORM 1 (compound 5) is metal-free, photochemically active dual CORM. Dual photoCORM 1 exhibits good cellular uptake and real-time monitoring ability of CO uncaging by a color change approach in cancerous B16F10 cells.
  • HY-114334
    Glutaminase-IN-1

    CB839 derivative

    Glutaminase Cancer
    Glutaminase-IN-1 (CB839 derivative), a CB839 derivative, is an allosteric inhibitor of 1,3,4-selenadiazole-containing kidney-type glutaminase (KGA), with an IC50 of 1 nM. Glutaminase-IN-1 (CB839 derivative) shows improved cellular uptake and antitumor activity.
  • HY-10446
    Pralatrexate

    Antifolate Apoptosis Cancer
    Pralatrexate is an antifolate and is a potent dihydrofolate reductasean (DHFR) inhibitor with a Ki of 13.4 pM. Pralatrexate is a substrate for folylpolyglutamate synthetase with improved cellular uptake and retention. Pralatrexate has antitumor activities and has the potential for relapsed/refractory T-cell lymphoma treatment.
  • HY-108256S
    Melitracen-d6 hydrochloride

    5-HT Receptor Neurological Disease
    Melitracen-d6 hydrochloride is the deuterium labeled Melitracen hydrochloride. Melitracen hydrochloride is an orally active biphasic antidepressant and antianxiety agent. Melitracen hydrochloride can inhibit the uptake of Norepinephrine and 5-HT (serotonin) through the presynaptic membrane inducing the increase of monoamine transmitters in synaptic space.
  • HY-N3513
    Mulberrin

    Kuwanon C

    Others Cardiovascular Disease
    Mulberrin is a strong inhibitor of organic anion-transporting polypeptide 2B1 (OATP2B1)-mediated estrone-3-sulfate (E3S) uptake with an IC50 value being 1.8 ±1.5 μM.
  • HY-132603
    AB-729

    HBV Infection
    AB-729, a nucleoside analogue, is a RNA interference (RNAi). AB-729 conjugates to a trimer of N-acetylgalactosamine (GalNAc) ligand that promotes uptake into hepatocytes via the asialoglycoprotein receptor (ASGR). AB-729 inhibits viral replication and reduces HBV antigens.
  • HY-B1396
    Nefazodone hydrochloride

    BMY-13754; MJ-13754-1

    5-HT Receptor Adrenergic Receptor Neurological Disease Endocrinology
    Nefazodone hydrochloride (BMY-13754) is a potent and selective 5HT2A (Ki=5.8 nM) antagonist with moderate inhibition of 5-HT and noradrenaline uptake (IC50 of 290 and 300 nM, respectively). Nefazodone hydrochloride is a phenylpiperazine antidepressant with less alpha-adrenergic blocking activity.
  • HY-139409
    2-Deoxy-D-glucose 6-phosphate

    Others Metabolic Disease
    2-Deoxy-D-glucose 6-phosphate is an intermediate of 2-deoxy-D-glucose (2-DG) . 2-Deoxy-D-glucose is incorporated into glycogen.
  • HY-N6780
    Ophiobolin B

    Fungal Infection
    Ophiobolin B, a sesterterpene metabolite of Helminthosporium oryzae, inhibits proton extrusion from maize coleoptiles. Ophiobolin B inhibits fusicoccin (FC) promoted proton extrusion, potassium uptake and cell enlargement. The MIC values with the antifungal effect of Ophiobolins B on different zygomycetes is 25–50 μg/mL.
  • HY-N0401A
    (Z)-Ligustilide

    Bacterial Infection Metabolic Disease
    (Z)-Ligustilide is extracted from Ligusticum chuanxiong Hort, has antimicrobial and antifungal activity, exhibits an average antifungal score of 5.6. (Z)-Ligustilide inhibits the expression of FATP5 and DGAT, inhibits fatty acid uptake and esterification in mice and has potential as therapeutics for nonalcoholic fatty liver disease (NAFLD) .
  • HY-107203S
    Propentofylline-d6

    HWA 285-d6

    Phosphodiesterase (PDE) Inflammation/Immunology Neurological Disease
    Propentofylline-d6 (HWA 285-d6) is the deuterium labeled Propentofylline. Propentofylline is a xanthine-derivative that inhibits adenosine uptake and blocks phosphodiesterase activity. Propentofylline has neuroprotective, antiproliferative, and anti-inflammatory effects that improve cognition and dementia severity in patients with Alzheimer's disease or vascular dementia.
  • HY-133018
    HCV-IN-7

    HCV Infection
    HCV-IN-7 is an orally active and potent pan-genotypic HCV NS5A inhibitor with IC50s of 3-47 pM. HCV-IN-7 shows a superior pan-genotypic profile and a good pharmacokinetic profile coupled with a favorable liver uptake. HCV-IN-7 has anti-viral activity.
  • HY-107521
    TFB-TBOA

    CF3-Bza-TBOA

    EAAT2 Neurological Disease
    TFB-TBOA (CF3-Bza-TBOA) is a potent glutamate transporter blocker that potently suppresses the activity of glial transporters. TFB-TBOA shows IC50 values of 22, 17, and 300 nM for glutamate transporters EAAT1, EAAT2, and EAAT3 respectively in an uptake assay using cells transiently expressing EAATs.
  • HY-133116
    4-Hydroxyatomoxetine

    Others Neurological Disease
    4-Hydroxyatomoxetine is an active metabolite of Atomoxetine. 4-Hydroxyatomoxetine is metabolized by the enzyme cytochrome P450 2D6 (CYP2D6). Atomoxetine hydrochloride is a potent and selective noradrenalin re-uptake inhibitor (Ki values are 5 nM, 77 nM and 1451 nM for inhibition of radioligand binding to human NET, SERT and DAT respectively).
  • HY-133018A
    HCV-IN-7 hydrochloride

    HCV Cancer
    HCV-IN-7 hydrochloride is an orally active and potent pan-genotypic HCV NS5A inhibitor with IC50s of 3-47 pM. HCV-IN-7 hydrochloride shows a superior pan-genotypic profile and a good pharmacokinetic profile coupled with a favorable liver uptake. HCV-IN-7 hydrochloride has anti-viral activity.
  • HY-B0520A
    Benztropine mesylate

    Benzatropine mesylate; Benzotropine mesylate; Benztropine methanesulfonate

    Dopamine Receptor mAChR Histamine Receptor Cancer Neurological Disease
    Benztropine mesylate (Benzatropine mesylate) is an orally active centrally acting anticholinergic agent that can be used for Parkinson's disease research. Benztropine mesylate is an anti-histamine agent and a dopamine re-uptake inhibitor. Benztropine mesylate is also a human D2 dopamine receptor allosteric antagonist. Benztropine mesylate also has anti-CSCs (cancer stem cells) effects.
  • HY-P2048A
    MOTS-c(human) acetate

    AMPK GLUT Metabolic Disease
    MOTS-c(human) acetate is a mitochondrial-derived peptide. MOTS-c(human) acetate induces the accumulation of AMP analog AICAR, increases activation of AMPK and expression of its downstream GLUT4. MOTS-c(human) acetate induces glucose uptake and improves insulin sensitivity. MOTS-c(human) acetate has implications in the regulation of obesity, diabetes, exercise, and longevity.
  • HY-115762
    4-Hydroxytryptamine creatinine sulfate

    Endogenous Metabolite Neurological Disease
    4-Hydroxytryptamine creatinine sulfate, a tryptamine derivative, is a neurotransmitter agonist.
  • HY-120139
    KMH-233

    Others Cancer
    KMH-233, a potent, reversible and selective l-type amino acid transporter 1 (LAT1) inhibitor, inhibits the uptake of LAT1 substrate, l-leucin (IC50=18 μM) as well as cell growth. KMH-233 significantly potentiates the efficacy of Bestatin and Cisplatin even at low concentrations (25 μM).
  • HY-124418
    SBI-477

    Others Metabolic Disease
    SBI-477 is a chemical probe stimulated insulin signaling by deactivating the transcription factor MondoA, leading to reduced expression of the insulin pathway suppressors thioredoxin-interacting protein (TXNIP) and arrestin domain–containing 4 (ARRDC4). SBI-477 coordinately inhibits triacylglyceride (TAG) synthesis and enhances basal glucose uptake in human skeletal myocytes.
  • HY-B1002S
    Oxolinic acid-d5

    Bacterial Antibiotic DNA/RNA Synthesis Infection
    Oxolinic acid-d5 is the deuterium labeled Oxolinic acid. Oxolinic acid is an antibiotic against both Gram-negative and Gram-positive bacteria. Oxolinic acid can be used for the research of acute and chronic urinary tract infections. Oxolinic acid is a DNA/RNA synthesis inhibitor. Oxolinic acid acts a dopamine uptake inhibitor and stimulants locomotor effect in mice.
  • HY-12203
    PFK-158

    Autophagy Apoptosis Cancer
    PFK-158 is a potent and selective PFKFB3 inhibitor with an IC50 value 137 nM. PFK-158 reduces glucose uptake, ATP production, lactate release, and induces apoptosis and autophagy in cancer cells. PFK-158 has broad anti-tumor activity. PFK-158 can also enhance Colistin's resistance to bacteria.
  • HY-B0528A
    Octopamine hydrochloride

    (±)-p-Octopamine hydrochloride

    Adrenergic Receptor Endogenous Metabolite Neurological Disease Endocrinology
    Octopamine ((±)-p-Octopamine) hydrochloride, a biogenic monoamine structurally related to noradrenaline, acts as a neurohormone, a neuromodulator and a neurotransmitter in invertebrates. Octopamine hydrochloride can stimulate alpha2-adrenoceptors (ARs) in Chinese hamster ovary cells transfected with human alpha2-ARs. Octopamine hydrochloride increased glycogenolysis, glycolysis, oxygen uptake, gluconeogenesis and the portal perfusion pressure.
  • HY-106100
    Roxindole

    EMD 49980

    Dopamine Receptor Serotonin Transporter Neurological Disease
    Roxindole (EMD 49980), an indot-alkyl-pipenidine, is a potent agonist at dopamine autoreceptors, with an affinity for the D2-like subtype in the low nanomolar range. Roxindole can be used for the research of positive and negative schizophrenic symptoms. Roxindole is a 5-HT1A agonist and 5-HT uptake inhibitor. Antipsychotic and antidepressant activities.
  • HY-B1396S
    Nefazodone-d6 hydrochloride

    BMY-13754-d6; MJ-13754-1-d6

    5-HT Receptor Adrenergic Receptor Neurological Disease Endocrinology
    Nefazodone-d6 hydrochloride (BMY-13754-d6) is the deuterium labeled Nefazodone hydrochloride. Nefazodone hydrochloride (BMY-13754) is a potent and selective 5HT2A (Ki=5.8 nM) antagonist with moderate inhibition of 5-HT and noradrenaline uptake (IC50 of 290 and 300 nM, respectively). Nefazodone hydrochloride is a phenylpiperazine antidepressant with less alpha-adrenergic blocking activity.
  • HY-14472
    Tesofensine

    NS-2330

    Dopamine Transporter Serotonin Transporter Metabolic Disease
    Tesofensine (NS-2330) is a triple monoamine reuptake inhibitor inducing a potent inhibition of the re-uptake process in the synaptic cleft of the neurotransmitters dopamine (DA; IC50=6.5 nM), norepinephrine (NE;IC50=1.7 nM), and serotonin (5-HT;IC50=11 nM), and with potentials as an anti-obesity agent. Tesofensine is a CNS acting anti-obesity agent.
  • HY-143906
    URAT1 inhibitor 2

    URAT1 Inflammation/Immunology
    URAT1 inhibitor 2 is an orally active and potent URAT1 and CYP isozyme inhibitor, with IC50 values of 1.36 μM, 16.97 μM, 5.22 μM for URAT1-mediated 14C-UA uptake, CYP1A2 and CYP2C9, respectively. URAT1 inhibitor 2 is a promising drug candidate in the study of hyperuricemia and gout.
  • HY-B1704A
    Nisoxetine hydrochloride

    Monoamine Transporter Sodium Channel Neurological Disease
    Nisoxetine hydrochloride is a potent and selective inhibitor of noradrenaline transporter (NET), with a Kd of 0.76 nM. Nisoxetine hydrochloride is an antidepressant and local anesthetic, it can block voltage-gated sodium channels.
  • HY-19824
    3PO

    Autophagy Cancer
    3PO is a novel small-molecule inhibitor of the PFKFB3 isozyme, 3PO markedly attenuates the proliferation of several human malignant hematopoietic and adenocarcinoma cell lines (IC50, 1.4-24 μM) IC50 value Target: PFKFB3 isozyme in vitro: 3PO inhibits recombinant PFKFB3 activity, suppresses glucose uptake, and decreases the intracellular concentration of Fru-2,6-BP, lactate, ATP, NAD+, and NADH.
  • HY-N1511
    Ganoderic acid D

    Sirtuin Apoptosis Cancer
    Ganoderic acid D, a highly oxygenated tetracyclic triterpenoid, is the major active component of Ganoderma lucidum. Ganoderic acid D upregulates the protein expression of SIRT3 and induces the deacetylated cyclophilin D (CypD) by SIRT3. Ganoderic acid D inhibits the energy reprogramming of colon cancer cells including glucose uptake, lactate production, pyruvate and acetyl-coenzyme production in colon cancer cells. Ganoderic acid D induces HeLa human cervical carcinoma apoptosis.
  • HY-103430
    SKF-83566 hydrobromide

    Dopamine Receptor 5-HT Receptor Adenylate Cyclase Neurological Disease
    SKF-83566 hydrobromide is a potent, blood-brain permeable and orally active D1-like dopamine receptor (D1DR) antagonist and a weaker competitive antagonist at the vascular 5-HT2 receptor (Ki=11 nM). SKF-83566 is a competitive DAT (dopamine transporter) inhibitor with an IC50 of 5.7 μM. SKF-83566 also shows selective inhibition for adenylyl cyclase 2 (AC2) over AC1 and AC5 in the isolated rabbit thoracic aorta. SKF-83566 can be used for the research of parkinson’s disease and nicotine craving alleviation.
  • HY-W014421
    AP-18

    TRP Channel Neurological Disease
    AP-18, a potent and selective TRPA1 inhibitor, blocks activation of TRPA1 by 50 μM Cinnamaldehyde with an IC50 of 3.1 μM and 4.5 μM for human and mouse TRPA1, respectively. AP-18 reverses complete Freund's adjuvant (CFA)-induced mechanical hyperalgesia in mice. AP-18 attenuated 30 μM AITC-induced Yo-Pro uptake in a concentration-dependent manner, with an IC50 of 10.3 μM.
  • HY-106100A
    Roxindole hydrochloride

    EMD 38362

    Dopamine Receptor Serotonin Transporter Neurological Disease
    Roxindole hydrochloride (EMD 38362), an indot-alkyl-pipenidine, is a potent agonist at dopamine autoreceptors, with an affinity for the D2-like subtype in the low nanomolar range. Roxindole can be used for the research of positive and negative schizophrenic symptoms. Roxindole is a 5-HT1A agonist and 5-HT uptake inhibitor with high affinity for 5-HT1A (IC50=0.9 nM). Antipsychotic and antidepressant activities.
  • HY-B0528AS
    Octopamine-d4 hydrochloride

    (±)-p-Octopamine-d4 hydrochloride

    Adrenergic Receptor Endogenous Metabolite Neurological Disease Endocrinology
    Octopamine-d4 ((±)-p-Octopamine-d4) hydrochloride is the deuterium labeled Octopamine hydrochloride. Octopamine ((±)-p-Octopamine) hydrochloride, a biogenic monoamine structurally related to noradrenaline, acts as a neurohormone, a neuromodulator and a neurotransmitter in invertebrates. Octopamine hydrochloride can stimulate alpha2-adrenoceptors (ARs) in Chinese hamster ovary cells transfected with human alpha2-ARs. Octopamine hydrochloride increased glycogenolysis, glycolysis, oxygen uptake, gluconeogenesis and the portal perfusion pressure.
  • HY-N6924
    Zingibroside R1

    HIV Infection Metabolic Disease
    Zingibroside R1 is dammaranae-type triterpenoid saponin, isolated from rhizomes, taproots, and lateral roots of Panax japonicas C. A. Meyer, shows excellent anti-tumor effects as well as anti-angiogenic activity. Zingibroside R1 possesses some anti-HIV-1 activity. Zingibroside R1 has inhibitory effects on the 2-deoxy-D-glucose (2-DG) uptake by EAT cells (IC50=91.3 μM).
  • HY-N2118
    Bilobetin

    PPAR PKA Metabolic Disease
    Bilobetin, an active component of Ginkgo biloba, can reduce blood lipids and improve the effects of insulin. Bilobetin ameliorated insulin resistance, increased the hepatic uptake and oxidation of lipids, reduced very-low-density lipoprotein triglyceride secretion and blood triglyceride levels, enhanced the expression and activity of enzymes involved in β-oxidation and attenuated the accumulation of triglycerides and their metabolites in tissues. Bilobetin also increased the phosphorylation, nuclear translocation and activity of PPARα accompanied by elevated cAMP level and PKA activity.
  • HY-P1723A
    Spexin TFA

    Neuropeptide Q TFA

    Neuropeptide Y Receptor
    Spexin TFA is a potent galanin receptor 2/3 (GAL2/GAL3) agonist (EC50 values are 45.7 and 112.2 nM, respectively). Spexin TFA exhibits no significant activity at galanin receptor 1. Spexin TFA is an endogenous satiety-inducing peptide; Spexin TFA inhibits long chain fatty acid uptake by adipocytes and decreases food consumption in diet-induced obese mice and rats. Spexin TFA attenuates LH secretion in goldfish. Spexin TFA exhibits anxiolytic effects in vivo.
  • HY-N6791
    KT5823

    PKA PKC Bacterial Apoptosis Antibiotic Infection Inflammation/Immunology
    KT5823, a selective the cGMP-dependent protein kinase (PKG) inhibitor with an Ki value of 0.23 μM, it also inhibits PKA and PKC with Ki values of 10 μM and 4 μM, respectively. KT5823 is a staurosporine-related protein kinase inhibitor, increases thyroid-stimulating hormone-induced (Na +/I - symporter) NIS expression, and iodide uptake in thyroid cells. KT5823 arrests cells after the G0/G1 boundary and causes increases in the levels of apoptotic DNA fragmentation.
  • HY-108464A
    Phenamil methanesulfonate

    Sodium Channel TRP Channel Metabolic Disease Inflammation/Immunology
    Phenamil methanesulfonate, an analog of Amiloride (HY-B0285), is a more potent and less reversible epithelial sodium channel (ENaC) blocker with an IC50 of 400 nM. Phenamil methanesulfonate is also a competive inhibitor of TRPP3 and inhibits TRPP3-mediated Ca 2+ transport with an IC50 of 140 nM in a Ca 2+ uptake assay. Phenamil methanesulfonate is an intriguing small molecule to promote bone repair by strongly activating BMP signaling pathway. Phenamil methanesulfonate is used for the research of cystic fibrosis lung disease.
  • HY-N7676
    Marein

    AMPK HDAC Metabolic Disease Neurological Disease Cardiovascular Disease
    Marein has the neuroprotective effect due to a reduction of damage to mitochondria function and activation of the AMPK signal pathway. Marein improves insulin resistance induced by high glucose in HepG2 cells through CaMKK/AMPK/GLUT1 to promote glucose uptake, through IRS/Akt/GSK-3β to increase glycogen synthesis, and through Akt/FoxO1 to decrease gluconeogenesis. Marein is a HDAC inhibitor with an IC50 of 100 µM. Marein has beneficial antioxidative, antihypertensive, antihyperlipidemic and antidiabetic effects.
  • HY-118567
    Bis(maltolato)oxovanadium(IV)

    BMOV

    Phosphatase Metabolic Disease
    Bis(maltolato)oxovanadium(IV) (BMOV) is a potent, reversible, competitive and orally active pan-PTP (protein tyrosine phosphatases) inhibitor. Bis(maltolato)oxovanadium(IV) inhibits HCPTPA, PTP1B, HPTPβ and SHP2 with IC50s of 126 nM, 109 nM, 26 nM and 201 nM, respectively. Bis(maltolato)oxovanadium(IV) is a potent insulin sensitizer.
  • HY-W020111
    7-Chloro-4-(piperazin-1-yl)quinoline

    Sirtuin Parasite Infection
    7-Chloro-4-(piperazin-1-yl)quinolone is an important scaffold in medicinal chemistry. 7-Chloro-4-(piperazin-1-yl)quinolone is a potent sirtuin inhibitor and also inhibits the serotonin uptake (IC50 of 50 μM). 7-Chloro-4-(piperazin-1-yl)quinolone exhibits antimalarial activity on D10 and K1 strains of P. falciparum with IC50s of 1.18 μM and 0.97 μM, respectively.
  • HY-103430A
    SKF-83566

    Dopamine Receptor 5-HT Receptor Adenylate Cyclase Neurological Disease
    SKF-83566 is a potent, blood-brain permeable and orally active D1-like dopamine receptor (D1DR) antagonist and a weaker competitive antagonist at the vascular 5-HT2 receptor (Ki=11 nM). SKF-83566 is a competitive DAT (dopamine transporter) inhibitor with an IC50 of 5.7 μM. SKF-83566 also shows selective inhibition for adenylyl cyclase 2 (AC2) over AC1 and AC5 in the isolated rabbit thoracic aorta. SKF-83566 can be used for research of parkinson’s disease and nicotine craving alleviation.