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Pathways Recommended: Membrane Transporter/Ion Channel
Targets Recommended: GlyT

Results for "Anandamide Transporters Inhibitors" in MCE Product Catalog:

146

Inhibitors & Agonists

3

Screening Libraries

4

Dye Reagents

1

Biochemical Assay Reagents

22

Natural
Products

Cat. No. Product Name Target Research Areas
  • HY-10863
    Anandamide

    Cannabinoid Receptor GPR55 Endogenous Metabolite Inflammation/Immunology
    Anandamide is an immune modulator in the central nervous system acts via not only cannabinoid receptors (CB1 and CB2) but also other targets (e.g., GPR18/GPR55).
  • HY-117506
    (S)-SBFI-26

    FABP Neurological Disease
    (S)-SBFI-26 is the (S) enantiomer of SBFI-26, an anti-nociceptive agent binds to anandamide transporters FABP5 and FABP7. (S)-SBFI-26 has anti-nociceptive and anti-inflammatory effects.
  • HY-N7506
    13-Hydroxyisobakuchiol

    Delta3,2-Hydroxylbakuchiol

    Monoamine Transporter Dopamine Transporter Neurological Disease
    Hydroxyisobakuchiol (Delta3,2-Hydroxylbakuchiol), an analog of Bakuchiol (HY-N0235) isolated from Psoralea corylifolia (L.), is a potent monoamine transporter inhibitor. 13-Hydroxyisobakuchiol is more selective for the dopamine transporter (DAT) (IC50=0.58 μM) and norepinephrine transporter (NET) (IC50=0.69 μM) than for the serotonin transporter (SERT) (IC50=312.02 μM). 13-Hydroxyisobakuchiol has the potential for the research of disorders such as Parkinson's disease, depression, and cocaine addiction.
  • HY-117506B
    SBFI-26

    FABP Inflammation/Immunology Neurological Disease
    SBFI-26 is a selective and competitive inhibitor of fatty acid binding proteins FABP5 and FABP7, with Kis of 0.9 µM and 0.4 µM for FABP5 and FABP7, respectively. SBFI-26 produces anti-nociceptive and anti-inflammatory effects.
  • HY-U00439
    Protein kinase inhibitors 1

    DYRK Cancer
    Protein kinase inhibitors 1 is a novel inhibitor of HIPK2 with an IC50 of 74 nM and Kd of 9.5 nM.
  • 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 crosses the blood-brain barrier.
  • HY-18728
    STF-31

    GLUT Autophagy Cancer
    STF-31 is a selective inhibitor of glucose transporter 1 (GLUT1), with an IC50 of 1μM[1][2].
  • 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-B2246A
    D-Carnitine hydrochloride

    (S)-Carnitine hydrochloride

    Endogenous Metabolite Metabolic Disease
    D-Carnitine hydrochloride ((S)-Carnitine Hydrochloride) has been used to study sulfur factor transporter SLC22A4 and carnitine transporter SLC22A5 in ergot. D-Carnitine hydrochloride is also used to get palmitic acid into mitochondria.
  • HY-101190
    Volixibat

    SHP626; LUM002

    Others Metabolic Disease
    Volixibat (SHP626) is a highly selective, minimally absorbed, and competitive apical sodium-dependent bile acid transporter (ASBT) inhibitor. Volixibat has potential for treatment for non-alcoholic steatohepatitis (NASH).
  • HY-119996A
    AR-C141990 hydrochloride

    Monocarboxylate Transporter Inflammation/Immunology
    AR-C141990 hydrochloride is a potent lactate transporters (monocarboxylate transporters; MCTs) inhibitor with pKi values of 7.6, 6.6 for MCT-1 and MCT-2, respectively. AR-C141990 hydrochloride has immunosuppressive properties and inhibits graft versus host response.
  • HY-110101
    ARN272

    Others Neurological Disease
    ARN272 is an anandamide transport inhibitor.
  • HY-W011391
    GPNA hydrochloride

    Apoptosis Cancer
    GPNA hydrochloride is a well known substrate of the enzyme γ-glutamyltransferase (GGT). GPNA hydrochloride is a specific glutamine (Gln) transporter ASCT2 inhibitor. GPNA hydrochloride also inhibit Na +-dependent carriers, such as SNAT family (SNAT1/2/4/5), and the Na +-independent leucine transporters LAT1/2. GPNA reversibly induces apoptosis in A549 cells.
  • HY-109043A
    Solriamfetol hydrochloride

    JZP-110 hydrochloride; ADX-N05 hydrochloride; R228060 hydrochloride

    Dopamine Receptor Neurological Disease
    Solriamfetol hydrochloride (JZP-110 hydrochloride) is an orally active and selective dopamine and norepinephrine reuptake inhibitor with IC50s of 2.9 μM and 4.4 μM for dopamine and norepinephrine transporters, respectively. Solriamfetol hydrochloride has robust wake-promoting effects.
  • HY-109043
    Solriamfetol

    JZP-110; ADX-N05; R228060

    Dopamine Receptor Neurological Disease
    Solriamfetol (JZP-110) is an orally active and selective dopamine and norepinephrine reuptake inhibitor with IC50s of 2.9 μM and 4.4 μM for dopamine and norepinephrine transporters, respectively. Solriamfetol has robust wake-promoting effects.
  • HY-10865
    LY2183240

    FAAH Autophagy Neurological Disease
    LY2183240 is a novel and highly potent blocker of anandamide uptake (IC50 = 270 pM).
  • HY-100017
    BAY-876

    GLUT Cancer
    BAY-876 is an orally active and selective glucose transporter 1 (GLUT1) inhibitor with an IC50 of 2 nM. BAY-876 is >130-fold more selective for GLUT1 than GLUT2, GLUT3, and GLUT4. BAY-876 is also a potent blocker of glycolytic metabolism and ovarian cancer growth.
  • 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-N7433
    4,6-O-Ethylidene-α-D-glucose

    Ethylidene-glucose

    GLUT Endogenous Metabolite Metabolic Disease
    4,6-O-ethylidene-α-D-glucose (Ethylidene-glucose), a glucose derivative, is a competitive exofacial binding-site inhibitor on glucose transporter 1 (GLUT1) with a Ki of 12 mM for wild-type 2-deoxy-D-glucose transport.
  • HY-107641
    α-Cyano-4-hydroxycinnamic acid

    α-Cyano-4-hydroxycinnamate

    Monocarboxylate Transporter Metabolic Disease
    α-Cyano-4-hydroxycinnamic acid (α-Cyano-4-hydroxycinnamate) is a potent and non-competitive inhibitor of monocarboxylate transporters (MCTs). α-Cyano-4-hydroxycinnamic acid inhibits mitochondrial pyruvate transporter with a Ki of 6.3 μM. α-Cyano-4-hydroxycinnamic acid is used as a matrix to facilitate peptide ionization in matrix-assisted laser desorption/ionization time-of-flight (MALDI-TOF) mass spectrometry applications.
  • 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-17590
    Radafaxine hydrochloride

    GW-353162A; BW-306U

    Monoamine Transporter Neurological Disease
    Radafaxine hydrochloride (GW-353162A) is a DAT (dopamine transporter) and NET(norepinephrine transporter) transporters inhibitor, and nAChR family modulator.
  • HY-18638
    TCID

    4,5,6,7-Tetrachloroindan-1,3-dione

    Deubiquitinase Neurological Disease
    TCID (4,5,6,7-Tetrachloroindan-1,3-dione) is a potent and selective neuronal ubiquitin C-terminal hydrolase (UCH-L3) inhibitor with an IC50 of 0.6 μM. TCID diminishes glycine transporter GlyT2 ubiquitination in brainstem and spinal cord primary neurons.
  • HY-B0457
    Clomipramine hydrochloride

    Serotonin Transporter Dopamine Receptor Neurological Disease
    Clomipramine hydrochloride is a serotonin transporter (SERT), norepinephrine transporter (NET) and dopamine transporter (DAT) blocker with Ki of 0.14, 54 and 3 nM, respectively.
  • HY-116477
    URB937

    FAAH Inflammation/Immunology Neurological Disease
    URB937 is a FAAH inhibitor and increases anandamide levels, with an IC50 of 26.8 nM. URB937 fails to affect FAAH activity in the brain.
  • HY-B1272
    Desipramine hydrochloride

    Dopamine Transporter Serotonin Transporter Neurological Disease Cancer
    Desipramine hydrochloride is an inhibitor of norepinephrine transporter (NET), 5-HT transporter (SERT) and dopamine transporter (DAT) with Kis of 4, 61 and 78,720 nM, respectively.
  • HY-103334
    MAFP

    Methyl Arachidonyl Fluorophosphonate

    Phospholipase Metabolic Disease Neurological Disease Cardiovascular Disease
    MAFP (Methyl Arachidonyl Fluorophosphonate) is an selective, active-site directed and irreversible inhibitor of cPLA2 and iPLA2. MAFP is also a potent irreversible inhibitor of anandamide amidase.
  • 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). 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). V-9302 hydrochloride inhibits ASCT2-mediated glutamine uptake (IC50=9.6 µM) in HEK-293 cells.
  • HY-16736
    Centanafadine

    EB-1020

    Adrenergic Receptor Dopamine Transporter Serotonin Transporter Neurological Disease Endocrinology
    Centanafadine is dual norepinephrine (NE)/dopamine (DA) transporter inhibitor, also inhibits serotonin transporter, with IC50s of 6 nM, 38 nM and 83 nM for human NE, DA and serotonin transporter , respectively.
  • HY-16736A
    Centanafadine hydrochloride

    EB-1020 hydrochloride

    Adrenergic Receptor Dopamine Transporter Serotonin Transporter Neurological Disease Endocrinology
    Centanafadine (hydrochloride) is dual norepinephrine (NE)/dopamine (DA) transporter inhibitor, also inhibits serotonin transporter, with IC50s of 6 nM, 38 nM and 83 nM for human NE, DA and serotonin transporter , respectively.
  • HY-N0322
    Cholesterol

    Estrogen Receptor/ERR Endogenous Metabolite Metabolic Disease
    Cholesterol is the major sterol in mammals and is makes up 20-25% of structural component of the plasma membrane. Plasma membranes are highly permeable to water but relatively impermeable to ions and protons. Cholesterol plays an important role in determining the fluidity and permeability characteristics of the membrane as well as the function of both the transporters and signaling proteins. Cholesterol is also an endogenous estrogen-related receptor α (ERRα) agonist.
  • HY-B0457AS
    Clomipramine D3

    Serotonin Transporter Dopamine Receptor Neurological Disease
    Clomipramine D3 is the deuterium labeled Clomipramine. Clomipramine is a serotonin transporter (SERT), norepinephrine transporter (NET) dopamine transporter (DAT) blocker with Ki of 0.14, 54 and 3 nM, respectively.
  • HY-B0457S
    Clomipramine D3 hydrochloride

    Serotonin Transporter Dopamine Receptor Neurological Disease
    Clomipramine D3 hydrochloride is a deuterium labeled Clomipramine hydrochloride. Clomipramine hydrochloride is a serotonin transporter (SERT), norepinephrine transporter (NET) dopamine transporter (DAT) blocker with Ki of 0.14, 54 and 3 nM, respectively.
  • HY-B0590A
    Tetrabenazine Racemate

    Ro 1-9569 Racemate

    Monoamine Transporter Neurological Disease
    Tetrabenazine Racemate (Ro 1-9569 Racemate) is a selective and reversible inhibitor of vesicular monoamine transporter-2 (VMAT-2).
  • HY-107794
    Clodronate disodium tetrahydrate

    Disodium clodronate tetrahydrate

    Others Inflammation/Immunology Neurological Disease
    Clodronate disodium tetrahydrate (Disodium clodronate tetrahydrate) is first-generation bisphosphonate, with anti-osteoporotic, anti-inflammatory and analgesic effects. Clodronate disodium tetrahydrate is a selective, potent, reversible and Cl - competitive vesicular nucleotide transporter (VNUT) inhibitor, with an IC50 of 15.6 nM. Clodronate disodium tetrahydrate inhibits vesicular ATP release from neurons and reduces chronic neuropathic and inflammatory pain.
  • HY-131005
    Ehp inhibitor 2

    Ephrin Receptor Cancer
    Ehp inhibitor 2 is a Eph family tyrosine kinase inhibitor.
  • HY-114381
    GT 949

    EAAT2 Neurological Disease
    GT 949 is a selective excitatory amino acid transporter-2 (EAAT2) positive allosteric modulator with an EC50 of 0.26 nM.
  • HY-B1490
    Imipramine hydrochloride

    Serotonin Transporter Neurological Disease
    Imipramine hydrochloride inhibits serotonin transporter with an IC50 value of 32 nM in vitro.
  • HY-N0480A
    Reserpine hydrochloride

    Monoamine Transporter Cancer Neurological Disease
    Reserpine hydrochloride is an inhibitor of the vesicular monoamine transporter 2 (VMAT2).
  • HY-N0480
    Reserpine

    Monoamine Transporter Autophagy Neurological Disease Cancer
    Reserpine is an inhibitor of the vesicular monoamine transporter 2 (VMAT2).
  • HY-121879
    SHP836

    Phosphatase Cancer
    SHP836 is a SHP2 allosteric inhibitor, with an IC50 of 12 μM for the full length SHP2.
  • HY-10716A
    PF-03463275

    GlyT Neurological Disease
    PF-03463275 is a centrally penetrant, orally available, selective, and competitive GlyT1 (glycine transporter-1) reversible inhibitor, with a Ki of 11.6 nM. PF-03463275 has the potential for Schizophrenia research.
  • HY-19887
    Tilapertin

    AMG747

    GlyT Neurological Disease
    Tilapertin is an oral inhibitor of glycine transporter type-1 (GlyT1).
  • HY-110176
    ASP2535

    GlyT Neurological Disease
    ASP2535 is a potent, orally bioavailable, selective, brain permeable and centrally-active glycine transporter-1 (GlyT1) inhibitor. ASP2535 can improve cognitive impairment in animal models of schizophrenia and Alzheimer's disease.
  • HY-128723
    Dapagliflozin impurity

    Others Others
    Dapagliflozin impurity is an enantiomer of Dapagliflozin which is a sodium-glucose transporter 2 inhibitor.
  • HY-10010
    Ko 143

    BCRP Cancer
    Ko 143 is a potent and selective ATP-binding cassette subfamily G member 2 (ABCG2/BCRP) inhibitor. Ko 143 displays >200-fold selectivity over P-gp and MRP-1 transporters.
  • HY-19373
    RWJ-445167

    3DP-10017

    Thrombin Factor Xa Cardiovascular Disease
    RWJ-445167 (3DP-10017) is a dual inhibitor of thrombin and factor Xa with Ki of 4.0 nM and 230 nM, respectively, exhibiting potent antithrombotic activity.
  • HY-16787
    ICA-121431

    Sodium Channel Cardiovascular Disease
    ICA-121431 is a nanomolar potent and broad-spectrum voltage-gated sodium channel (Nav) blocker, shows equipotent selectivity for human Nav1.1 and Nav1.3 subtypes with IC50 values of 13 nM and 23 nM, respectively. ICA-121431 shows less potent inhibition of Nav1.2 (IC50=240 nM) and 1,000 fold selectivity against Nav1.4, Nav1.6, and the TTX-resistant human Nav1.5 and Nav1.8 channels (IC50s >10 µM).
  • 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-101334
    MPDC

    GlyT Neurological Disease
    MPDC is a potent and competitive inhibitor of the Na+-dependent high-affinity glutamate transporter in forebrain synaptosomes.
  • HY-14261
    Vilazodone Hydrochloride

    EMD 68843 Hydrochloride; SB659746A Hydrochloride

    5-HT Receptor Serotonin Transporter Neurological Disease
    Vilazodone Hydrochloride (EMD 68843 Hydrochloride) is a serotonin transporter (SER) inhibitor and 5-HT1A receptor partial agonist.
  • HY-15793
    NBI-98782

    (+)-DTBZ; (+)-α-Dihydrotetrabenazine; (+)-α-DHTBZ

    Monoamine Transporter Neurological Disease
    NBI-98782(alpha-dihydrotetrabenazine) is a vesicular monoamine transporter (VMAT2) inhibtior with an Ki value of 0.97 nM.
  • HY-12850
    Dasotraline

    SEP 225289

    Dopamine Transporter Serotonin Transporter Neurological Disease
    Dasotraline is a triple reuptake inhibitor that blocks dopamine, norepinephrine, and serotonin transporters with IC50 values of 4, 6, and 11 nM, respectively.
  • HY-10914
    UCPH-101

    Others Neurological Disease
    UCPH-101 is an excitatory amino acid transporter subtype 1 (EAAT1) inhibitor with an IC50 of 0.66 μM.
  • HY-U00439A
    Protein kinase inhibitors 1 hydrochloride

    (E)-5-((2-Oxo-6'-(piperazin-1-yl)-1,2-dihydro-[3,3'-bipyridin]-5-yl)methylene)thiazolidine-2,4-dione hydrochloride

    DYRK Cancer
    Protein kinase inhibitors 1 hydrochloride is a potent HIPK2 inhibitor, with IC50s of 136 and 74 nM for HIPK1 and HIPK2, and a Kd of 9.5 nM for HIPK2.
  • HY-107526
    NFPS

    GlyT Neurological Disease
    NFPS is a selective, non-competitive glycine transporter-1 (GlyT1) inhibitor with IC50s of 2.8 nM and 9.8 nM for hGlyT1 and rGlyT1, respectively. NFPS exerts neuroprotection via glyR alpha1 subunit in the rat model of transient focal cerebral ischaemia and reperfusion.
  • HY-100390
    (S)-ML753286

    BCRP Cancer
    (S)-ML753286 is a breast cancer resistance protein (BCRP) inhibitor with an IC50 of 0.6 μM on BCRP efflux transporter.
  • HY-B1110
    Nomifensine

    (±)-Nomifensin

    Dopamine Receptor Neurological Disease
    Nomifensine is a norepinephrine-dopamine reuptake inhibitor, increases the amount of synaptic norepinephrine and dopamine available to receptors by blocking the dopamine and norepinephrine reuptake transporters.
  • HY-124738
    BI 01383298

    Sodium Channel Metabolic Disease
    BI 01383298 is a potent inhibitor of the sodium-citrate co-transporter (SLC13A5) that is highly expressed in the liver.
  • HY-B0590S1
    (+)-Tetrabenazine D6

    Monoamine Transporter
    (+)-Tetrabenazine D6 is the deuterium labeled (+)-Tetrabenazine. (+)-Tetrabenazine is a reversible inhibitor of vesicular monoamine transporter 2 (VMAT-2).
  • 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-101037
    Sarcosine

    N-Methylglycine; Sarcosin

    Endogenous Metabolite GlyT Cancer
    Sarcosine is a glycine transporter type 1 (GlyT) inhibitor and an N-methyl-D-aspartate (NMDA) receptor co-agonist at the glycine binding site.
  • HY-13248
    AR-C155858

    Monocarboxylate Transporter Others
    AR-C155858 is a selective monocarboxylate transporter MCT1 and MCT2 inhibitor with Kis of 2.3 nM and 10 nM, respectively.
  • HY-112843
    CNT2 inhibitor-1

    Others Others
    CNT2 inhibitor-1 is a potent concentrative nucleoside transporter 2 Inhibitor (CNT2), with an IC50 of 640 nM for hCNT2.
  • HY-W012037
    8-Hydroxyquinoline hemisulfate

    8-Quinolinol hemisulfate

    Bacterial Antibiotic Infection
    8-Hydroxyquinoline hemisulfate (8-Quinolinol hemisulfate) is a monoprotic bidentate chelating agent, exhibits antiseptic, disinfectant, and pesticide properties, functioning as a transcription inhibitor.
  • HY-B0602
    Desvenlafaxine

    O-Desmethylvenlafaxine

    Serotonin Transporter Neurological Disease
    Desvenlafaxine, the succinate salt form of the isolated major active metabolite of Venlafaxine (HY-B0196), is an orally active and BBB penetrated 5-HT and norepinephrine reuptake inhibitor, with IC50 values of 47.3 nM and 531.3 nM for hSERT and hNET, respectively. Desvenlafaxine shows weak binding affinity (62% inhibition at 100 μM) at the human dopamine (DA) transporter.
  • 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-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-12850A
    Dasotraline hydrochloride

    SEP-225289 hydrochloride

    Serotonin Transporter Dopamine Transporter Neurological Disease
    Dasotraline hydrochloride (SEP-225289 hydrochloride) is a triple reuptake inhibitor that blocks dopamine, norepinephrine, and serotonin transporters with IC50 values of 4, 6, and 11 nM, respectively.
  • HY-B0602A
    Desvenlafaxine succinate hydrate

    O-Desmethylvenlafaxine succinate hydrate

    Serotonin Transporter Neurological Disease
    Desvenlafaxine succinate hydrate, the succinate salt form of the isolated major active metabolite of Venlafaxine (HY-B0196), is an orally active and BBB penetrated 5-HT and norepinephrine reuptake inhibitor, with IC50 values of 47.3 nM and 531.3 nM for hSERT and hNET, respectively. Desvenlafaxine succinate hydrate shows weak binding affinity (62% inhibition at 100 μM) at the human dopamine (DA) transporter.
  • HY-100809
    Guvacine hydrochloride

    GABA Receptor Neurological Disease
    Guvacine hydrochloride is an alkaloid from the nut of Areca catechu, acts as an inhibitor of GABA transporter, and dispalys modest selectivity for cloned GABA transporters with IC50s of 14 μM (human GAT-1), 39 μM (rat GAT-1), 58 μM (rat GAT-2), 119 μM (human GAT-3), 378 μM (rat GAT-3), and 1870 μM (human BGT-3).
  • HY-19331
    WZB117

    GLUT Cancer
    WZB117 is a glucose transporter 1 (Glut1) inhibitor, which downregulates glycolysis, induces cell-cycle arrest, and inhibits cancer cell growth in vitro and in vivo.
  • HY-15258A
    Lesinurad sodium

    RDEA-594 sodium

    URAT1 Metabolic Disease
    Lesinurad sodium is a URAT1 and OAT inhibitor, is determined to be a substrate for the kidney transporters OAT1 and OAT3 with Km values of 0.85 and 2 µM, respectively.
  • HY-15258
    Lesinurad

    RDEA594

    URAT1 Metabolic Disease
    Lesinurad is a URAT1 and OAT inhibitor, is determined to be a substrate for the kidney transporters OAT1 and OAT3 with Km values of 0.85 and 2 µM, respectively.
  • HY-W013093
    Uridine triphosphate trisodium salt

    UTP trisodium salt; Uridine 5'-triphosphate trisodium salt

    Others Cancer Inflammation/Immunology Cardiovascular Disease
    Uridine triphosphate trisodium salt is a nucleotide that regulates the functions of the pancreas in endocrine and exocrine secretion, proliferation, channels, transporters, and intracellular signaling under normal and disease states.
  • HY-135813
    LtaS-IN-1

    Bacterial Infection
    LtaS-IN-1 (compound 1771) is a potent small-molecule inhibitor of Lipoteichoic acid (LTA) synthesis in multidrug-resistant (MDR) E. faecium and by altering the cell wall morphology. LtaS-IN-1 alone inhibits Enterococcus.spp 28 strains with varying MIC values ranging from 0.5 μg/mL to 64 μg/mL. LtaS-IN-1 combination with antibiotics abolishs multidrug-resistant E. faecium growth almost completely.
  • HY-125957
    A-3 hydrochloride

    PKA Casein Kinase CaMK PKC Others
    A-3 hydrochloride is a potent, cell-permeable, reversible, ATP-competitive non-selective antagonist of various kinases. It against PKA (Ki=4.3 µM), casein kinase II (Ki=5.1 µM) and myosin light chain kinase (MLCK) (Ki=7.4 µM). A-3 hydrochloride also inhibits PKC and casein kinase I with Ki values of 47 µM and 80 µM, respectively.
  • HY-128574
    GLUT4 activator 1

    GLUT Metabolic Disease
    GLUT4 activator 1 (Compound 26b) is a potent glucose transporter type 4 (GLUT4) translocation activator with an EC50 of 0.14 μM.
  • HY-107625A
    SNAP 94847 hydrochloride

    MCHR1 (GPR24) Neurological Disease
    SNAP 94847 hydrochloride is a novel, high affinity selective melanin-concentrating hormonereceptor1 (MCHR1) antagonist with (Ki= 2.2 nM, Kd=530 pM), it displays >80-fold and >500-fold selectivity over MCHα1A and MCHD2 receptors respectively. SNAP 94847 hydrochloride binds with high affinity to the mouse and rat MCHR1 with minimal cross-reactivity to other GPCR, ion channels, enzymes, and transporters.
  • HY-107625
    SNAP 94847

    MCHR1 (GPR24) Neurological Disease Endocrinology
    SNAP 94847 is a novel, high affinity selective melanin-concentrating hormonereceptor1 (MCHR1) antagonist with (Ki= 2.2 nM, Kd=530 pM), it displays >80-fold and >500-fold selectivity over MCHα1A and MCHD2 receptors respectively. SNAP 94847 binds with high affinity to the mouse and rat MCHR1 with minimal cross-reactivity to other GPCR, ion channels, enzymes, and transporters.
  • HY-107372
    Uridine triphosphate

    UTP; Uridine 5'-triphosphate

    Endogenous Metabolite Cancer Inflammation/Immunology Cardiovascular Disease
    Uridine triphosphate (UTP;Uridine 5'-triphosphate) is a nucleotide that regulates the functions of the pancreas in endocrine and exocrine secretion, proliferation, channels, transporters, and intracellular signaling under normal and disease states.
  • HY-112807
    SGLT inhibitor-1

    SGLT Metabolic Disease
    SGLT inhibitor-1 is a potent dual inhibitor of sodium glucose co-transporter proteins (SGLTs), inhibits hSGLT1 and hSGLT2 with IC50s of 43 nM and 9 nM, respectively.
  • HY-114309
    URAT1 inhibitor 1

    URAT1 Inflammation/Immunology
    URAT1 inhibitor 1 (1g) is a uric acid transporter 1 (URAT1) inhibitor, with an IC50 of 32 nM. URAT1 inhibitor 1 has potential to treat hyperuricemia associated with gout.
  • 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-15790
    Elobixibat

    A 3309; AZD 7806

    Others Metabolic Disease
    Elobixibat is a potent ileal bile acid transporter (IBAT) inhibitor with IC50 values of 0.53 ± 0.17 nM, 0.13 ± 0.03 nM, and 5.8 ± 1.6 nM for human IBAT, mouse IBAT, and canine IBAT.
  • HY-12741
    LDN-212320

    LDN/OSU-0212320; LDN-0212320; OSU-0212320

    EAAT2 Neurological Disease
    LDN-212320(OSU-0212320) is a glutamate transporter EAAT2 activator; enhances EAAT2 levels by > 6 fold at concentrations < 5 μM after 24 h.
  • HY-19264
    264W94

    Others Metabolic Disease
    264W94 is a potent ileal bile acid transporter (IBAT) inhibitor and a new cholesterol lowering agent. 264W94 has CYP7A1 induction, and antilipemic action.
  • HY-111419
    DSP-1053

    Serotonin Transporter Neurological Disease
    DSP-1053 is a potent Serotonin Transporter (SERT) (Ki=1.02 nM) inhibitor with partial 5-HT1A receptor (Ki=5.05 nM) agonistic activity.
  • HY-101918
    DS-1040 Tosylate

    Others Cardiovascular Disease
    DS-1040 Tosylate is an orally active, selective inhibitor of activated thrombin-activatable fibrinolysis inhibitor (TAFIa) with IC50s of 5.92 nM and 8.01 nM for human and rat TAFIa. DS-1040 Tosylate is a fibrinolysis enhancer for thromboembolic diseases.
  • HY-126302
    DMT1 blocker 2

    Others Inflammation/Immunology
    DMT1 blocker 2, Compound 12f, is a direct inhibitor of divalent metal transporter 1 (DMT1) with an IC50 of 0.83 μM, is expected to block iron uptake by enterocytes in vivo.
  • HY-13217
    Vanoxerine dihydrochloride

    GBR-12909 dihydrochloride; I893 dihydrochloride

    Dopamine Transporter Neurological Disease
    Vanoxerine dihydrochloride (GBR-12909 dihydrochloride) is a competitive, potent, and highly selective dopamine reuptake inhibitor (Ki=1 nM). Vanoxerine dihydrochloride (GBR-12909 dihydrochloride) binds to the target site on the dopamine transporter (DAT).
  • HY-13217A
    Vanoxerine

    GBR 12909; I893

    Dopamine Transporter Neurological Disease
    Vanoxerine (GBR-12909) is a competitive, potent, and highly selective dopamine reuptake inhibitor (Ki=1 nM). Vanoxerine (GBR-12909) binds to the target site on the dopamine transporter (DAT).
  • HY-12501A
    ITI-214

    Phosphodiesterase (PDE) Neurological Disease
    ITI-214 is a picomolar PDE1 inhibitor with excellent selectivity against other PDE family members and against a panel of enzymes, receptors, transporters, and ion channels, exhibits potent PDE1 inhibitory activity (Ki = 58 pM).
  • HY-16191
    ELR510444

    Microtubule/Tubulin Apoptosis Cancer
    ELR510444 is a novel microtubule disruptor; inhibits MDA-MB-231 cell proliferation with IC50 of 30.9 nM; not a substrate for the P-glycoprotein drug transporter and retains activity in βIII-tubulin-overexpressing cell lines.
  • HY-12501
    ITI214 free base

    Phosphodiesterase (PDE) Neurological Disease
    ITI-214 (free base) is a picomolar PDE1 inhibitor with excellent selectivity against other PDE family members and against a panel of enzymes, receptors, transporters, and ion channels, exhibits potent PDE1 inhibitory activity (Ki = 58 pM).
  • 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-B0486
    Lonidamine

    AF-1890; Diclondazolic Acid; DICA

    Hexokinase Mitochondrial Metabolism Apoptosis Cancer
    Lonidamine (AF-1890), an antitumor agent, is a hexokinase, mitochondrial pyruvate carrier (Ki 2.5 μM in isolated rat liver mitochondria) and plasma membrane monocarboxylate transporters inhibitor, which also inhibits mitochondrial complex II.
  • HY-15583
    Auristatin F

    Microtubule/Tubulin ADC Cytotoxin Cancer
    Auristatin F is a potent cytotoxin. Auristatin F, a potent microtubule inhibitor and vascular damaging agent (VDA), can be used in antibody-drug conjugates (ADC).
  • HY-15084A
    (-)-Dizocilpine maleate

    (-)-MK-801 maleate

    iGluR Neurological Disease
    (-)-Dizocilpine maleate ((-)-MK-801 maleate) is a less active (-)-enantiomer of Dizocilpine. (-)-Dizocilpine maleate is a selective and non-competitive N-methyl-D-aspartate (NMDA) receptor antagonist with a Ki of 211.7 nM. (-)-Dizocilpine maleate has antidepressant effects.
  • HY-B1190A
    Cefadroxil hydrate

    BL-S 578 hydrate

    Bacterial Antibiotic Infection
    Cefadroxil hydrate (BL-S 578 hydrate) is an orally active and first-generation cephalosporin with a broad spectrum antibacterial activity. Cefadroxil hydrate (BL-S 578 hydrate) also acts as a substrate of the peptide transporter PEPT1 and PEPT2.
  • HY-N0406
    2"-O-beta-L-galactopyranosylorientin

    Others Metabolic Disease
    2"-O-beta-L-galactopyranosylorientin is extracted from the flowers of Trollius ledebouri. 2"-O-beta-L-galactopyranosylorientin involves transporter mediated efflux in addition to passive diffusion and is the substrate of multidrug resistance protein 2 (MRP2).
  • HY-19753
    KS176

    BCRP Cancer
    KS176 is a potent and selective inhibitor of the breast cancer resistance protein (BCRP) multidrug transporter (IC50 values are 0.59 and 1.39 μM in Pheo A and Hoechst 33342 assays respectively). Displays no inhibitory activity against P-gp or MRP1.
  • HY-124658
    G0507

    Bacterial Infection
    G0507, a pyrrolopyrimidinedione compound, is a potent LolCDE ABC Transporter inhibitor. G0507 is a inhibitor of Escherichia coli growth and induces the extracytoplasmic σE stress response. G0507 acts as a chemical probe to dissect lipoprotein trafficking in Gram-negative bacteria.
  • 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-D0067
    7ACC1

    DEAC; Coumarin D 1421; D 1421

    Monocarboxylate Transporter Cancer
    7ACC1(DEAC; Coumarin D 1421; D 1421) selectively interfere with lactate fluxes in the lactate-rich tumor microenvironment; inhibits lactate influx but not efflux in tumor cells expressing MCT1 and MCT4 transporters.
  • HY-15793A
    Trans (2,3)-Dihydrotetrabenazine

    (2R,3R,11bR)-rel-Dihydrotetrabenazine; (2R,3R,11bR)-rel-DHTBZ

    Drug Metabolite Monoamine Transporter Neurological Disease
    Trans (2,3)-Dihydrotetrabenazine ((2R,3R,11bR)-rel-Dihydrotetrabenazine), a metabolite of Tetrabenazine, shows remarkable inhibition activity on vesicular monoamine transporter (VMAT2).
  • HY-114395
    NVS-ZP7-4

    Others Inflammation/Immunology
    NVS-ZP7-4 is a Zinc transporter SLC39A7 (ZIP7) inhibitor that is also the first reported chemical tool to probe the impact of modulating ER zinc levels and investigate ZIP7 as a novel druggable node in the Notch pathway.
  • HY-N6936
    Sennidin A

    HCV Akt GLUT Infection
    Sennidin A, isolated from the leaves of Cassia angustifolia, inhibits HCV NS3 helicase, with an IC50 of 0.8 μM. Sennidin A induces phosphorylation of Akt and glucose transporter 4 (GLUT4) translocation. Sennidin A stimulates the glucose incorporation.
  • HY-100228A
    SKF89976A hydrochloride

    d,l-SKF89976A hydrochloride

    GABA Receptor Neurological Disease
    SKF89976A hydrochloride is a selective GABA transporter (GAT-1) inhibitor with IC50s of 0.28 μM, 137.34 μM and 202.8 μM for GAT-1, GAT-2 and GAT-3 in CHO cells, respectively.
  • HY-122470
    Stampidine

    Reverse Transcriptase HIV Infection
    Stampidine is a nucleoside reverse transcriptase inhibitor (NRTI) with potent and broad-spectrum anti-HIV activity. Stampidine inhibits the laboratory HIV-1 strain HTLVIIIB (B-envelope subtype) and primary clinical isolates with IC50s of 1 nM and 2 nM, respectively. Stampidine also inhibits NRTI-resistant primary clinical isolates and NNRTI-resistant clinical isolates with IC50s of 8.7 nM and 11.2 nM, respectively.
  • HY-N4137
    Tormentic acid

    Others Inflammation/Immunology Cardiovascular Disease
    Tormentic acid, a triterpene isolated from Rosa rugosa, exerts anti-inflammatory, antihyperlipidemic, and anti-atherogenic properties.
  • HY-122312
    BAY-8002

    Monocarboxylate Transporter Cancer
    BAY-8002 is a potent, selective, orally active inhibitor of monocarboxylate transporter 1 (MCT1), with an IC50 of 85 nM in the MCT1-expressing DLD-1 cells, displays excellent selectivity against MCT4. Anti-tumor activity.
  • HY-N2003
    D-Tetrahydropalmatine

    Dopamine Receptor Metabolic Disease
    D-Tetrahydropalmatine is an isoquinoline alkaloid, mainly in the genus Corydalis. D-Tetrahydropalmatine is a Dopamine (DA) receptor antagonist with preferential affinity toward the D1 receptors. D-Tetrahydropalmatine is a potent organic cation transporter 1 (OCT1) inhibitor.
  • HY-109120
    Odevixibat

    A4250

    Others Metabolic Disease
    Odevixibat (A4250) is a potent, selective and orally active inhibitor of the ileal bile acid transporter (IBAT). Odevixibat (A4250)decreases cholestatic liver and bile duct injury in mice model. Odevixibat (A4250) has the potential for the treatment of primary biliary cirrhosis.
  • HY-128974
    N-Dodecyl-β-D-maltoside

    Lauryl Maltoside

    Others Others
    N-Dodecyl-β-D-maltoside (Lauryl Maltoside) is a derivatives of pyrene (Py), and it is a alkyl maltopyranoside detergent, especially in transporters and respiratory complexes. N-Dodecyl-β-D-maltoside has also been employed in applications such as in the purification and stabilization of RNA polymerase and detection of protein-lipid interactions.
  • HY-111678
    ML230

    CID44640177; SID 88095709

    Others Cancer
    ML230 (CID44640177; SID 88095709) is a selective inhibitor of ATP-binding cassette (ABC) transporter ABCG2, and 36-fold selective for ABCG2 over ABCB1 with EC50s values of 0.13 μM and 4.65 μM, respectively.
  • HY-G0025
    Tetrabenazine Metabolite

    (-)-β-Dihydrotetrabenazine; (-)-β-HTBZ

    Monoamine Transporter Drug Metabolite Neurological Disease
    Tetrabenazine Metabolite is an active metabolite of Tetrabenazine. Tetrabenazine Metabolite is a vesicular monoamine transporter 2 (VMAT2) inhibitor with a high affinity (Ki=13.4 nM). Tetrabenazine Metabolite is be developed for the treatment of chorea associated with Huntington’s disease and other hyperkinetic disorders.
  • HY-16643
    Linerixibat

    GSK2330672

    Others Metabolic Disease Inflammation/Immunology
    Linerixibat (GSK2330672) is a highly potent, nonabsorbable and orally active apical sodium-dependent bile acid transporter (ASBT) inhibitor with an IC50 of 42 nM human ASBT. Linerixibat can be used as lipid-lowering agent. Linerixibat has the potential for type 2 diabetes and Primary Biliary Cholangitis treatment.
  • HY-125176
    G907

    Bacterial Infection
    G907 is a selective small-molecule antagonist of ATP-binding cassette (ABC) transporter, MsbA. It inhibits purified E. coli MsbA in amphipols with an IC50 of 18 nM. G907 traps MsbA in an inward-facing, lipopolysaccharide-bound conformation by wedging into an architecturally conserved transmembrane pocket. Bactericidal activity.
  • HY-11007
    GNF-2

    Bcr-Abl SARS-CoV Cancer
    GNF-2 is a highly selective, allosteric, non-ATP competitive inhibitor of Bcr-Abl. GNF-2 inhibits Ba/F3.p210 proliferation with an IC50 of 138 nM .
  • HY-B0590B
    (+)-Tetrabenazine

    (+)-TBZ; (3R,11bR)-TBZ; (3R,11bR)-Tetrabenazine

    Monoamine Transporter Cancer
    (+)-Tetrabenazine ((+)-TBZ; (3R,11bR)-TBZ; (3R,11bR)-Tetrabenazine) is a reversible inhibitor of vesicular monoamine transporter 2 (VMAT-2), inhibits transport by VMAT2 with 10-fold greater potency than transport by VMAT1.
  • HY-N6935
    Sennidin B

    HCV Akt GLUT Infection Metabolic Disease
    Sennidin B, a stereoisomer isolated from the leaves of Cassia angustifolia, has lower activity than Sennidin A. Sennidin A inhibits HCV NS3 helicase, with an IC50 of 0.8 μM. Sennidin A induces phosphorylation of Akt and glucose transporter 4 (GLUT4) translocation. Sennidin A stimulates the glucose incorporation .
  • HY-103430
    SKF-83566 hydrobromide

    Dopamine Receptor Neurological Disease
    SKF-83566 hydrobromide is a potent, blood-brain permeable and orally active dopamine D1/D5 receptor antagonist. SKF-83566 is a competitive DAT (dopamine transporter) inhibitor with an IC50 of 5.7 μM and attenuates cocaine effects in vivo.
  • HY-N0749
    Jatrorrhizine

    Others Neurological Disease
    Jatrorrhizine is a potent and orally active uptake-2 transporter inhibitor, it can be isolated from various Chinese medicinal plants. Jatrorrhizine exhibits a critical neuroprotective role in H2O2-induced apoptosis via inhibition of MAPK pathway in HT22 hippocampal neurons.
  • HY-N0740
    Jatrorrhizine chloride

    Others Neurological Disease
    Jatrorrhizine chloride is a potent and orally active uptake-2 transporter inhibitor, it can be isolated from various Chinese medicinal plants. Jatrorrhizine chloride exhibits a critical neuroprotective role in H2O2-induced apoptosis via inhibition of MAPK pathway in HT22 hippocampal neurons.
  • HY-135482
    GABAA receptor agent 2 TFA

    GABA Receptor Neurological Disease
    GABAA receptor agent 2 TFA is a potent and high-affinity GABAA receptor antagonist with an IC50 of 24 nM (human α1β2γ2 GABAA-expressing tsA201 cells) and a Ki of 28 nM (rat GABAA receptors). GABAA receptor agent 2 TFA is inactive against four human GABA transporters (hGAT-1, hBGT-1, hGAT-2, and hGAT-3).
  • HY-117203A
    CDK12-IN-E9

    CDK Cancer
    CDK12-IN-E9 is a potent and selective covalent CDK12 inhibitor and a non-covalent CDK9 inhibitor, while avoiding ABC transporter-mediated efflux. CDK12-IN-E9 has weak binding ability to CDK7/CyclinH complex with an IC50> 1 μM.
  • HY-114395A
    (R)-NVS-ZP7-4

    Others Inflammation/Immunology
    (R)-NVS-ZP7-4 is the R-isomer of NVS-ZP7-4. NVS-ZP7-4 is a Zinc transporter SLC39A7 (ZIP7) inhibitor that is also the first reported chemical tool to probe the impact of modulating ER zinc levels and investigate ZIP7 as a novel druggable node in the Notch pathway.
  • HY-N0755
    Rhoifolin

    Insulin Receptor GLUT NF-κB p38 MAPK Autophagy Metabolic Disease Endocrinology Cancer
    Rhoifolin is a flavone glycoside isolated from Citrus grandis (L.) Osbeck leaves. Rhoifolin is beneficial for diabetic complications through enhanced adiponectin secretion, tyrosine phosphorylation of insulin receptor-β and glucose transporter 4 (GLUT 4) translocation. Rhoifolin ameliorates titanium particle-stimulated osteolysis and attenuates osteoclastogenesis via RANKL-induced NF-κB and MAPK pathways.
  • HY-W008344
    2-Chloroadenosine

    Others Others
    2-Chloroadenosine, a stable adenosine analogue, protects against long term development of ischaemic cell loss in the rat hippocampus. 2-Chloroadenosine is an apparent competitive inhibitor of uridine influx (apparent Ki=33 μM) and high-affinity nitrobenzylthioinosine binding (apparent Ki=0.18 mM). 2-Chloroadenosine is a transported permeant for the nucleoside transporter in human erythrocytes.
  • HY-N0173
    Cinchonidine

    α-Quinidine

    Serotonin Transporter Parasite Infection
    Cinchonidine (α-Quinidine) is a cinchona alkaloid found in Cinchona officinalis and Gongronema latifolium. A building block used in asymmetric synthesis in organic chemistry. Weak inhibitor of serotonin transporter (SERT) with Kis of 330, 4.2, 36, 196, 15 μM for dSERT, hSERT, hSERT I172M, hSERT S438T, hSERT Y95F, respectively. Antimalarial activities.
  • HY-100619
    BMS-986020

    LPL Receptor Metabolic Disease Inflammation/Immunology
    BMS-986020 is a high-affinity and selective lysophosphatidic acid receptor 1 (LPA1) antagonist. BMS-986020 inhibits bile acid and phospholipid transporters with IC50s of 4.8 µM, 6.2 µM, and 7.5 µM for BSEP, MRP4, and MDR3, respectively. BMS-986020 has the potential for the treatment of idiopathic pulmonary fibrosis (IPF).
  • HY-100619A
    BMS-986020 sodium

    LPL Receptor Metabolic Disease Inflammation/Immunology
    BMS-986020 sodium is a high-affinity lysophosphatidic acid receptor 1 (LPA1) antagonist. BMS-986020 sodium inhibits bile acid and phospholipid transporters with IC50s of 4.8 µM, 6.2 µM, and 7.5 µM for BSEP, MRP4, and MDR3, respectively. BMS-986020 sodium has the potential for the treatment of idiopathic pulmonary fibrosis (IPF).
  • HY-116594A
    OPC-14523 hydrochloride

    Sigma Receptor 5-HT Receptor Neurological Disease
    OPC-14523 hydrochloride is an orally active sigma and 5-HT1A receptor agonist, with high affinity for sigma receptors (σ1/2 IC50=47/56 nM), the 5-HT1A receptor (IC50=2.3 nM), and the 5-HT transporter (IC50=80 nM). OPC-14523 hydrochloride shows antidepressant-like activity.
  • HY-109067
    Opiranserin

    GlyT 5-HT Receptor P2X Receptor Neurological Disease
    Opiranserin, a non-opioid and non-NSAID analgesic candidate, is a dual antagonist of glycine transporter type 2 (GlyT2) and serotonin receptor 2A (5HT2A), with IC50s of 0.86 and 1.3 μM, respectively. Opiranserin shows antagonistic activity on rP2X3 (IC50=0.87 μM). Opiranserin is development as an injectable agent for the treatment of postoperative pain.
  • HY-111191
    ONO-2952

    Others Neurological Disease
    ONO-2952 is a potent, selective and orally active translocator protein 18 kDa (TSPO) antagonist with Ki of 0.33-9.30 nM for rat and human TSPO. ONO-2952 is more selective for TSPO than other receptors, transporters, ion channels and enzymes. ONO-2952 exerts its anti-stress effects through inhibition of excessive activation of noradrenergic system in the brain without the amnesic effect. ONO-2952 has the potential for irritable bowel syndrome treatment.
  • HY-13779
    J-147

    Monoamine Oxidase Dopamine Transporter Neurological Disease
    J-147 is an exceptionally potent, orally active, neuroprotective agent for cognitive enhancement. J-147 can readily pass the blood brain barrier (BBB). J-147 can inhibit monoamine oxidase B (MAO B) and the dopamine transporter with EC50 values of 1.88 μM and 0.649 μM, respectively. J-147 has potential for the treatment of Alzheimer’s disease (AD).
  • HY-116594
    OPC-14523 free base

    Sigma Receptor 5-HT Receptor Neurological Disease
    OPC-14523 free base is an orally active sigma and 5-HT1A receptor agonist, with high affinity for sigma receptors (σ1/2 IC50=47/56 nM), the 5-HT1A receptor (IC50=2.3 nM), and the 5-HT transporter (IC50=80 nM). OPC-14523 free base shows antidepressant-like activity.
  • HY-122872
    MKK7-COV-9

    p38 MAPK Cancer
    MKK7-COV-9 is a potent and selective covalent inhibitor of MKK7 and targets a specific protein–protein interaction of MKK7. MKK7-COV-9 blocks primary B cell activation in response to LPS with an EC50 of 4.98 μM.
  • 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-124619
    GPI-1046

    FKBP HIV Infection Neurological Disease
    GPI-1046 is a immunophilin ligand without antibiotic action and attenuates ethanol intake in part through the upregulation of glutamate transporter 1 (GLT1) in PFC and NAc-core. GPI-1046 is an analog of FK506, which is an immunophilin ligand that has been shown neuroprotective effects in neurodegenerative disease models. GPI-1046 readily crosses the blood-brain barrier and promotes the regeneration of dopamine (DA) cells in the CNS in association with functional recovery in rodent models. GPI-1046 improves HIV-associated injury of peripheral nerves.
  • HY-120944
    BAY-7598

    MMP Inflammation/Immunology
    BAY-7598 is a potent, orally bioavailable, and selective MMP12 inhibitor probe with IC50s of 0.085, 0.67 and 1.1 nM for human MMP12, murine MMP12, and rat MMP12, respectively.