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Pathways Recommended: TGF-beta/Smad
Results for "

Beta Receptor

" in MCE Product Catalog:

542

Inhibitors & Agonists

7

Screening Libraries

1

Biochemical Assay Reagents

55

Peptides

4

Inhibitory Antibodies

51

Natural
Products

147

Recombinant Proteins

79

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas
  • HY-150693
    Estrogen receptor β antagonist 2

    Estrogen Receptor/ERR Cancer
    Estrogen receptor β antagonist 2 is a potent and selective estrogen receptor β (ERβ) antagonist with IC50s of 109.10, 0.63 µM for Erα and Erβ, respectively.
  • HY-12452
    DPN

    Diarylpropionitrile

    Estrogen Receptor/ERR Apoptosis Autophagy Neurological Disease
    DPN (Diarylpropionitrile) is a non-steroidal estrogen receptor β (ERβ) selective ligand, with an EC50 of 0.85 nM. DPN has neuroprotective effects in a number of neurological diseases.
  • HY-B0203A
    Nebivolol hydrochloride

    R 065824 hydrochloride

    Adrenergic Receptor Cardiovascular Disease Endocrinology
    Nebivolol (R 065824) hydrochloride is an orally active beta receptor blocker and has the high beta(1)-receptor affinity.Nebivolol hydrochloride has direct vasodilator properties and adrenergic blocking characteristics. Nebivolol hydrochloride can be used for the research of kinds of diseases such as hypertension, coronary artery disease, congestive heart failure and ischemic heart disease.
  • HY-B0203
    Nebivolol

    R 065824

    Adrenergic Receptor Cardiovascular Disease Endocrinology
    Nebivolol (R 065824) is an orally active beta receptor blocker and has the high beta(1)-receptor affinity. Nebivolol has direct vasodilator properties and adrenergic blocking characteristics. Nebivolol can be used for the research of kinds of diseases such as hypertension, coronary artery disease, congestive heart failure and ischemic heart disease.
  • HY-B0432
    Propafenone

    SA-79

    Sodium Channel Adrenergic Receptor Potassium Channel Cancer Cardiovascular Disease
    Propafenone (SA-79), a sodium-channel blocker, acts an antiarrhythmic agent. Propafenone also has high affinity for the β receptor (IC50=32 nM). Propafenone blocks the transient outward current (Ito) and the sustained delayed rectifier K current (Isus) with IC50 values of 4.9 μm and 8.6 μm, respectively. Propafenone suppresses esophageal cancer proliferation through inducing mitochondrial dysfunction and induce apoptosis.
  • HY-B1154
    Penbutolol sulfate

    (-)-Terbuclomine

    Adrenergic Receptor Cardiovascular Disease Endocrinology
    Penbutolol sulfate is able to bind to both beta-1 adrenergic receptors and beta-2 adrenergic receptors (the two subtypes), thus making it a non-selective β blocker.
  • HY-123012
    Lubabegron

    LY-488756

    Adrenergic Receptor Others
    Lubabegron is a potent modulator of β-adrenergic receptor (β -AR). Lubabegron demonstrates antagonistic behavior at the β1 and β2 receptor subtypes and agonistic behavior at the β3 receptor subtype in cattle. Lubabegron reduces NH3 gas emissions from an animal or its waste.
  • HY-117239
    SB-206606

    Adrenergic Receptor Cardiovascular Disease
    SB-206606, a stereoisomer of BRL 37344, is a potentially specific, beta 3-adrenergic receptor (β3-AR) ligand. The affinity of [3H]SB 206606 is 76 times higher for the β3-AR than for the beta 1/beta 2-adrenergic receptors.
  • HY-13951
    ICI 118,551 hydrochloride

    ICI 118551 hydrochloride

    Adrenergic Receptor Neurological Disease Endocrinology
    ICI 118,551 (hydrochloride) is a highly selective β2 adrenergic receptor antagonist, with Kis of 0.7, 49.5 and 611 nM for β2, β1 and β3 receptors, respectively.
  • HY-P99171
    Gevokizumab

    Interleukin Related Inflammation/Immunology
    Gevokizumab is a potent anti-IL-1β antibody, negatively modulates IL-1β signaling through an allosteric mechanism. Gevokizumab selectively decreases the binding affinity of IL-1β for the IL-1 receptor type I (IL-1RI) signaling receptor instead of IL-1 counter-regulatory decoy receptor (IL-1 receptor type II).
  • HY-13713
    LY377604

    Adrenergic Receptor Metabolic Disease Endocrinology
    LY377604 is a human β3-adrenergic receptor agonist with an EC50 of 2.4 nM and also a β1- and β2-adrenergic receptor antagonist.
  • HY-105272A
    Loreclezole hydrochloride

    R 72063 hydrochloride

    GABA Receptor Neurological Disease
    Loreclezole hydrochloride, an antiepileptic compound, is a selective GABAA receptor modulator and acts as a positive allosteric modulator of β2 or β3-subunit containing receptors.
  • HY-B1270
    Isoxsuprine hydrochloride

    Adrenergic Receptor iGluR Neurological Disease Endocrinology
    Isoxsuprine hydrochloride is a beta-adrenergic receptor agonist with Kis of 13.65 μΜ and 3.48 μΜ for myometrial and placcntal beta-adrenergic receptor, respectively. Isoxsuprine hydrochloride is also a NMDA receptor antagonist.
  • HY-105272
    Loreclezole

    R 72063

    GABA Receptor Neurological Disease
    Loreclezole, an antiepileptic compound, is a selective GABAA receptor modulator and acts as a positive allosteric modulator of β2 or β3-subunit containing receptors.
  • HY-19468
    ERB-196

    WAY-202196

    Estrogen Receptor/ERR Inflammation/Immunology Neurological Disease
    ERB-196 is a nonsteroidal selective estrogen receptor-β (ERβ) agonist.
  • HY-B0436
    Salbutamol hemisulfate

    Albuterol hemisulfate; AH-3365 hemisulfate

    Adrenergic Receptor Autophagy Inflammation/Immunology Endocrinology Cancer
    Salbutamol Hemisulfate (Albuterol hemisulfate) is a short-acting β2 adrenergic receptor agonist Target: β2 Adrenergic Receptor Salbutamol Hemisulfate (Albuterol hemisulfate) is a short-acting, selective beta2-adrenergic receptor agonist used in the treatment of asthma and COPD.
  • HY-B0381B
    Levobetaxolol hydrochloride

    (S)-Betaxolol hydrochloride; AL-1577A

    Adrenergic Receptor Neurological Disease Endocrinology
    Levobetaxolol hydrochloride is a beta-adrenergic receptor inhibitor (beta blocker) that can lower the pressure in the eye.
  • HY-103200
    SR59230A hydrochloride

    Adrenergic Receptor Metabolic Disease Cardiovascular Disease
    SR59230A hydrochloride is a potent, selective, and blood-brain barrier penetrating β3-adrenergic receptor antagonist with IC50s of 40, 408, and 648 nM for β3, β1, and β2 receptors, respectively.
  • HY-100672
    SR59230A

    Adrenergic Receptor Metabolic Disease Cardiovascular Disease
    SR59230A is a potent, selective, and blood-brain barrier penetrating β3-adrenergic receptor antagonist with IC50s of 40, 408, and 648 nM for β3, β1, and β2 receptors, respectively.
  • HY-P1868
    α2β1 Integrin Ligand Peptide

    Integrin Infection
    α2β1 Integrin Ligand Peptide interacts with the α2β1 integrin receptor on the cell membrane and mediates extracellular signals into cells. It is a potential antagonist of collagen receptors.
  • HY-B0979
    Lobeline hydrochloride

    α-Lobeline hydrochloride; L-Lobeline hydrochloride

    nAChR Neurological Disease
    Lobeline hydrochloride, a nicotinic receptor agonist, acting as a potent antagonist at both α3β2 and α4β2 neuronal nicotinic receptor subtypes.
  • HY-N1415S
    β-Caryophyllene-d2

    Cannabinoid Receptor Endogenous Metabolite Cancer Infection Neurological Disease
    β-Caryophyllene-d2 is deuterium labeled β-Caryophyllene. β-Caryophyllene is a CB2 receptor agonist.
  • HY-P1868A
    α2β1 Integrin Ligand Peptide TFA

    Integrin Others
    α2β1 Integrin Ligand Peptide TFA interacts with the α2β1 integrin receptor on the cell membrane and mediates extracellular signals into cells. It is a potential antagonist of collagen receptors.
  • HY-B1392
    Esmolol hydrochloride

    Adrenergic Receptor Autophagy Mitophagy Cardiovascular Disease Endocrinology Cancer
    Esmolol hydrochloride is a beta adrenergic receptor blocker.
  • HY-101658
    Pargolol hydrochloride

    Ko 1400 hydrochloride

    Adrenergic Receptor Neurological Disease Endocrinology
    Pargolol hydrochloride is a β adrenergic receptor antagonist.
  • HY-101817
    Spirendolol

    Li 32-468; S 32-468; Substance 32468

    Adrenergic Receptor Neurological Disease Endocrinology
    Spirendolol is a β adrenergic receptor antagonist.
  • HY-101271
    WAY-200070

    Estrogen Receptor/ERR Neurological Disease
    WAY-200070 is a selective estrogen receptor β (ERRβ) agonist with an IC50 of 2.3 nM.
  • HY-103538
    JLK-6

    Amyloid-β Neurological Disease
    JLK-6 markedly reduce the production of amyloid β-peptide (Aβ) by amyloid-β Precursor protein (APP) expressing HEK293 cells by affecting the γ-secretase cleavage of APP, with no effect on the cleavage of the Notch receptor.
  • HY-P1502
    β-Endorphin, human

    Opioid Receptor Neurological Disease
    β-Endorphin, human, a prominent endogenous peptide, existing in the hypophysis cerebri and hypothalamus, is an agonist of opioid receptor, with preferred affinity for μ-opioid receptor and δ-opioid receptor; β-Endorphin, human exhibits antinociception activity.
  • HY-U00016
    Teoprolol

    Adrenergic Receptor Endocrinology
    Teoprolol is a β-adrenergic receptor blocker.
  • HY-B1270S
    Isoxsuprine-d6 hydrochloride

    Adrenergic Receptor iGluR Neurological Disease Endocrinology
    Isoxsuprine-d6 hydrochloride is the deuterium labeled Isoxsuprine hydrochloride. Isoxsuprine hydrochloride is a beta-adrenergic receptor agonist with Kis of 13.65 μΜ and 3.48 μΜ for myometrial and placcntal beta-adrenergic receptor, respectively. Isoxsuprine hydrochloride is also a NMDA receptor antagonist.
  • HY-103394
    TC HSD 21

    Others Cancer
    TC HSD 21 is a potent 17β-hydroxysteroid dehydrogenase type 3 (17β-HSD3) inhibitor with an IC50 of 14 nM. TC HSD 21 shows excellent selectivity over 17β-HSD isoenzymes and nuclear receptors.
  • HY-U00205
    Dopexamine hydrochloride

    FPL60278AR

    Adrenergic Receptor Cardiovascular Disease Endocrinology
    Dopexamine hydrochloride is a β2 adrenergic receptor agonist.
  • HY-101691
    Ecastolol

    Adrenergic Receptor Cardiovascular Disease Endocrinology
    Ecastolol is a beta adrenergic receptor antagonist, with antianginal activities.
  • HY-N1415
    β-Caryophyllene

    (-)-(E)-Caryophyllene; (−)-β-caryophyllene; (−)-trans-Caryophyllene

    Cannabinoid Receptor Endogenous Metabolite Cancer Infection Neurological Disease
    β-Caryophyllene is a CB2 receptor agonist.
  • HY-19307
    SB-273005

    Integrin Inflammation/Immunology
    SB-273005 is a potent nonpeptide and orally active integrin antagonist with Kis of 1.2 nM and 0.3 nM for αvβ3 receptor and αvβ5 receptor, respectively.
  • HY-P1266
    α-Conotoxin EI

    nAChR Neurological Disease
    α-Conotoxin EI is a selective nicotinic acetylcholine α1β1γδ receptor (nAChR) antagonist (IC50=187 nM) and an α3β4 receptor inhibitor. α-Conotoxin EI can block muscle and ganglionic receptors.
  • HY-129029
    Bisoprolol

    Adrenergic Receptor Cancer Inflammation/Immunology Cardiovascular Disease
    Bisoprolol is a potent, selective and orally active β1-adrenergic receptor blocker with little activity on β2-receptor. Bisoprolol has the potential for hypertension, coronary artery disease and stable ventricular dysfunction research.
  • HY-120829
    Bisoprolol fumarate

    Adrenergic Receptor Cancer Inflammation/Immunology Cardiovascular Disease
    Bisoprolol fumarate is a potent, selective and orally active β1-adrenergic receptor blocker with little activity on β2-receptor. Bisoprolol fumarate has the potential for hypertension, coronary artery disease and stable ventricular dysfunction research.
  • HY-14823
    Sobetirome

    GC-1; QRX-431

    Thyroid Hormone Receptor Metabolic Disease Endocrinology
    Sobetirome (GC-1) is a thyroid hormone receptor β (TRβ)-specific agonist which bind selectively to TRβ-1 with an EC50 of 0.16 μM.
  • HY-14652
    Tamibarotene

    Am 80

    RAR/RXR Autophagy Apoptosis Cancer
    Tamibarotene is a retinoic acid receptor α/β (RARα/β) agonist, showing high selectivity over RARγ.
  • HY-B1794
    Thiethylperazine

    Dopamine Receptor Histamine Receptor Bacterial Amyloid-β Infection Neurological Disease
    Thiethylperazine, a phenothiazine derivate, is an orally active and potent dopamine D2-receptor and histamine H1-receptor antagonist. Thiethylperazine is also a selective ABCC1activator that reduces amyloid-β (Aβ) load in mice. Thiethylperazine has anti-emetic, antipsychotic and antimicrobial effects.
  • HY-16316
    Metipranolol hydrochloride

    Adrenergic Receptor Cardiovascular Disease Endocrinology
    Metipranolol hydrochloride is a non-selective β adrenergic receptor blocking agent.
  • HY-B0076
    Bisoprolol hemifumarate

    Adrenergic Receptor Cancer Endocrinology Inflammation/Immunology Cardiovascular Disease
    Bisoprolol hemifumarate is a potent, selective and orally active β1-adrenergic receptor blocker with little activity on β2-receptor. Bisoprolol hemifumarate has the potential for hypertension, coronary artery disease and stable ventricular dysfunction research.
  • HY-138690
    Estrogen receptor modulator 6

    Estrogen Receptor/ERR Endocrinology
    Estrogen receptor modulator 6 (compound 3a) is a selective estrogen receptor (ER) β agonist (Ki=0.44 nM). Estrogen receptor modulator 6 displays 19-fold selectivity for ERβ over ERα(Ki=8.4 nM).
  • HY-B0452S1
    Ritodrine-d3 hydrochloride

    DU21220-d3 hydrochloride

    Adrenergic Receptor Endocrinology
    Ritodrine-d3 (hydrochloride) is the deuterium labeled Ritodrine (hydrochloride). Ritodrine hydrochloride (DU21220 hydrochloride) is a β-2 adrenergic receptor agonist.
  • HY-N6630
    6-Methylflavone

    GABA Receptor Neurological Disease
    6-Methylflavone is an activator of α1β2γ2L and α1β2 GABAA receptors.
  • 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-13783
    BIBF0775

    TGF-β Receptor Cancer
    BIBF0775 is a potent and selective transforming growth factor β (TGFβ) type I receptor (Alk5) inhibitor with an IC50 of 34 nM.
  • HY-12216
    Resmetirom

    MGL-3196; VIA-3196

    Thyroid Hormone Receptor Cardiovascular Disease Endocrinology
    Resmetirom (MGL-3196) is a highly selective thyroid hormone receptor β (THR-β) agonist with an EC50 value of 0.21 μM.
  • HY-108627
    DMPQ dihydrochloride

    PDGFR Others
    DMPQ dihydrochloride is a potent and selective inhibitor of human platelet-derived growth factor receptor β (PDGFRβ) with an IC50 of 80 nM.
  • HY-103211
    L748337

    Adrenergic Receptor Cancer Metabolic Disease Cardiovascular Disease
    L748337 is a potent β3-adrenergic receptor antagonist and displays selectivity over β1 and β2 receptors. The Ki values of L748337 for β3-, β2- and β1-adrenoceptors are 4.0 nM, 204 nM and 390 nM, respectively. L748337 couples predominantly to Gi to activate MAPK signaling and increases phosphorylation of Erk1/2 with pEC50 value of 11.6. L748337 can be used for the research of cancer, nonalcoholic fatty liver disease (NAFLD), and cardiovascular related diseases.
  • HY-B0982
    Pindolol

    LB-46

    5-HT Receptor Adrenergic Receptor Neurological Disease Endocrinology
    Pindolol (LB-46) is a nonselective β-blocker with partial beta-adrenergic receptor agonist activity, also functions as a 5-HT1A receptor weak partial antagonist (Ki=33nM).
  • HY-B1794A
    Thiethylperazine dimaleate

    Dopamine Receptor Histamine Receptor Bacterial Amyloid-β Infection Neurological Disease
    Thiethylperazine dimaleate, a phenothiazine derivate, is an orally active and potent dopamine D2-receptor and histamine H1-receptor antagonist. Thiethylperazine dimaleate is also a selective ABCC1activator that reduces amyloid-β (Aβ) load in mice. Thiethylperazine dimaleate has anti-emetic, antipsychotic and antimicrobial effects.
  • HY-N0175
    Cytisinicline

    Cytisine; Sophorine; Baptitoxine

    nAChR Metabolic Disease Cancer
    Cytisinicline (Cytisine) is an alkaloid. Cytisinicline (Cytisine) is a partial agonist of α4β2 nAChRs, and partial to full agonist at β4 containing receptors and α7 receptors. Has been used medically to help with smoking cessation.
  • HY-101091
    Importazole

    Apoptosis Cancer
    Importazole is a small molecule inhibitor of the nuclear transport receptor importin-β.
  • HY-U00293
    ZK-90055 hydrochloride

    Adrenergic Receptor Inflammation/Immunology Endocrinology
    ZK-90055 hydrochloride is a β2 adrenergic receptor agonist.
  • HY-131145
    Brombuterol hydrochloride

    Bromobuterol hydrochloride

    Adrenergic Receptor Inflammation/Immunology
    Brombuterol hydrochloride (Bromobuterol hydrochloride) is a β-adrenergic receptor agonist.
  • HY-U00391
    β3-AR agonist 2

    Adrenergic Receptor Metabolic Disease Endocrinology
    β3-AR agonist 2 is a potent and selective β3-adrenergic receptor (β3-AR) agonist with an EC50 of 8 nM.
  • HY-N10497
    Dihydro-β-erythroidine

    nAChR Neurological Disease
    Dihydro-β-erythroidine is a a competitive nicotinic receptor antagonist. Dihydro-β-erythroidine blocks the discriminative stimulus properties of nicotine. Dihydro-β-erythroidine inhibits the anxiolytic effect of nicotine induced.
  • HY-10912
    Fexaramine

    FXR Autophagy Others
    Fexaramine is a potent and selective FXR agonist with an EC50 of 25 nM. Fexaramine has no activity against hRXRα, hPPARαγδ, mPXR, hPXR, hLXRα, hTRβ, hRARβ, mCAR, mERRγ, and hVDR receptors.
  • HY-16143
    Cilengitide TFA

    EMD 121974 TFA

    Integrin Autophagy Cancer
    Cilengitide is a potent and selective integrin inhibitor for αvβ3 and αvβ5 receptor, with IC50 values of 4 nM and 79 nM, respectively.
  • HY-103456
    PHTPP

    Estrogen Receptor/ERR Cancer
    PHTPP is a selective estrogen receptor β (ERβ) antagonist with 36-fold selectivity over ERα.
  • HY-103520
    DS2

    GABA Receptor Neurological Disease
    DS2 is a selective positive allosteric modulator of δ-GABAA receptor. DS2 selectively potentiates GABA responses mediated by α4βreceptor. DS2 does not enhance activity at α4β3γ2 and α1β3γ2 receptors. DS2 relieves pain and has the potential for sleep disorders research.
  • HY-P1548
    β-CGRP, human

    Human β-CGRP; CGRP-II (Human)

    CGRP Receptor Inflammation/Immunology Cardiovascular Disease
    β-CGRP, human (Human β-CGRP) is one of calcitonin peptides, acts via the complex of calcitonin-receptor-like receptor (CRLR) and receptor-activity-modifying protein (RAMP), with IC50s of 1 nM and 300 nM for CRLR/RAMP1 and CRLR/RAMP2 in cells.
  • HY-P1548B
    β-CGRP, human acetate

    Human β-CGRP acetate; CGRP-II (Human) (acetate)

    CGRP Receptor Inflammation/Immunology Cardiovascular Disease
    β-CGRP, human acetate (Human β-CGRP acetate) is one of calcitonin peptides, acts via the complex of calcitonin-receptor-like receptor (CRLR) and receptor-activity-modifying protein (RAMP), with IC50s of 1 nM and 300 nM for CRLR/RAMP1 and CRLR/RAMP2 in cells.
  • HY-139727A
    S(-)-Bisoprolol fumarate

    Adrenergic Receptor Cardiovascular Disease
    S(-)-Bisoprolol fumarate is a S(-)-enantiomer of Bisoprolol fumarate. Bisoprolol fumarate is a potent, selective and orally active β1-adrenergic receptor blocker. Bisoprolol has little activity on β2-receptor and has the potential for hypertension, coronary artery disease and stable ventricular dysfunction research.
  • HY-139727
    S(-)-Bisoprolol

    Adrenergic Receptor Cardiovascular Disease
    S(-)-Bisoprolol is a S(-)-enantiomer of Bisoprolol. Bisoprolol is a potent, selective and orally active β1-adrenergic receptor blocker. Bisoprolol has little activity on β2-receptor and has the potential for hypertension, coronary artery disease and stable ventricular dysfunction research.
  • HY-100583
    (-)-(S)-Equol

    Estrogen Receptor/ERR Endogenous Metabolite Cancer Metabolic Disease Neurological Disease
    (-)-(S)-Equol is a high affinity ligand for estrogen receptor β with a Ki of 0.73 nM.
  • HY-P3343A
    hFSH-β-(33-53) (TFA)

    Estrogen Receptor/ERR Cancer
    hFSH-β-(33-53) TFA, a thiol-containing peptide which corresponds to a second FSH receptor-binding domain, is a FSHR (follicle-stimulating hormone receptor) antagonist. hFSH-β-(33-53) TFA inhibits binding of FSH to receptor and is a partial agonist of estradiol synthesis in Sertoli cells.
  • HY-129029S
    Bisoprolol-d5

    Adrenergic Receptor Cardiovascular Disease
    Bisoprolol-d5 is the deuterium labeled Bisoprolol. Bisoprolol is a potent, selective and orally active β1-adrenergic receptor blocker. Bisoprolol has little activity on β2-receptor and has the potential for hypertension, coronary artery disease and stable ventricular dysfunction research.
  • HY-P1548A
    β-CGRP, human TFA

    Human β-CGRP TFA; CGRP-II (Human) (TFA)

    CGRP Receptor Inflammation/Immunology Cardiovascular Disease
    β-CGRP, human TFA (Human β-CGRP TFA) is one of calcitonin peptides, acts via the complex of calcitonin-receptor-like receptor (CRLR) and receptor-activity-modifying protein (RAMP), with IC50s of 1 nM and 300 nM for CRLR/RAMP1 and CRLR/RAMP2 in cells.
  • HY-13338S
    Mabuterol-D9

    Adrenergic Receptor Inflammation/Immunology Cardiovascular Disease
    Mabuterol-D9 is a deuterium labeled Mabuterol. Mabuterol is an agonist of the β2-adrenergic receptor.
  • HY-N0377
    Liquiritigenin

    4',7-Dihydroxyflavanone

    Estrogen Receptor/ERR Cancer Inflammation/Immunology Neurological Disease
    Liquiritigenin, a flavanone isolated from Glycyrrhiza uralensis, is a highly selective estrogen receptor β (ERβ) agonist with an EC50 of 36.5 nM for activation of the ERE tk-Luc.
  • HY-146997
    TRβ agonist 1

    Thyroid Hormone Receptor Metabolic Disease
    TRβ agonist 1 is a selective and mutation-sensitive thyroid hormone receptor β (TRβ) agonist, with an EC50 value of 21 nM. TRβ agonist 1 can be used for researching dyslipidemia, nonalcoholic steatohepatitis (NASH), and resistance to thyroid hormone (RTH).
  • HY-103040
    Zuranolone

    GABA Receptor Neurological Disease
    Zuranolone is an orally active and potent neuroactive steroid positive allosteric modulator of GABAA receptor, with EC50s of 296 and 163 nM for α1β2γ2 and α4β3δ GABAA receptors, respectively.
  • HY-P3517
    β-Endorphin (6-31), human

    β-EP (6-31), human

    Opioid Receptor Endocrinology Neurological Disease
    β-Endorphin, an endogenous opioid neuropeptide, is an opioid receptor agonist. β-Endorphin binds preferentially to μ-opioid receptors and is produced in certain neurons of the central and peripheral nervous system and is one of three endorphins produced in humans. β-Endorphin can be used to reduce stress and maintain homeostasis in the body and is involved in neurological pain perception regulation.
  • HY-136207
    TC-2559 difumarate

    nAChR Neurological Disease
    TC-2559 idifumarate is a CNS-selective, orally active α4β2 subtype of nicotinic acetylcholine receptor (nAChR) partial agonist (EC50=0.18 μM). TC-2559 difumarate shows selectivity for α4β2 over α2β4, α4β4 and α3β4 receptors, with EC50s in the range of 10-30 µM. Antinociceptive effect.
  • HY-103512
    TP003

    GABA Receptor Neurological Disease
    TP003 is a non-selective benzodiazepine site agonist with EC50s of 20.3, 10.6, 3.24, 5.64 nM for α1β2γ2, α2β3γ2, α3β3γ2, α5β2γ2, respectively. TP003 induces anxiolysis via α2GABAA receptors.
  • HY-12704
    ITD-1

    TGF-β Receptor Cardiovascular Disease
    ITD-1 is the first selective TGFβ receptor inhibitor with an IC50 of 460 nM.
  • HY-100327
    MK-6913

    Tetrahydrofluoroene 52

    Estrogen Receptor/ERR Metabolic Disease
    MK-6913 (Tetrahydrofluoroene 52) is a potent and selective estrogen receptor β agonist.
  • HY-14537
    Latrepirdine dihydrochloride

    Dimebolin dihydrochloride

    Amyloid-β Histamine Receptor Adrenergic Receptor 5-HT Receptor Autophagy Neurological Disease Endocrinology
    Latrepirdine dihydrochloride is a neuroactive compound with antagonist activity at histaminergic, α-adrenergic, and serotonergic receptors. Latrepirdine stimulates amyloid precursor protein (APP) catabolism and amyloid-β (Aβ) secretion.
  • HY-N2337
    11beta-Hydroxyprogesterone

    11β-Hydroxyprogesterone

    Endogenous Metabolite Cardiovascular Disease
    11beta-Hydroxyprogesterone is a potent inhibitors of 11β-Hydroxysteroid dehydrogenase; also activates human mineralocorticoid receptor in COS-7 cells with an ED50 of 10 nM.
  • HY-142441
    THR-β agonist 1

    Others Endocrinology
    THRβ Agonist 1 is a potent and selective agonist of THRβ. Thyroid hormone receptor mediates the physiological activity of thyroid hormones which plays a key role in normal growth and development of the body and in maintaining metabolic balance. THRβ Agonist 1 has the potential for the research of thyroid hormone receptor-related diseases (extracted from patent WO2021104288A1, compound 2).
  • HY-117829
    UNC9994

    Dopamine Receptor 5-HT Receptor Histamine Receptor Neurological Disease
    UNC9994, an analog of Aripiprazole, is a functionally selective β-arrestin-biased dopamine D2 receptor (D2R) agonist with EC50 <10 nM for β-arrestin-2 recruitment to D2 receptors. UNC9994 is simultaneously partial agonists of β-arrestin-2 translocation and antagonists of Gi-regulated cAMP production. Antipsychotic Activity.
  • HY-100689
    Propyl pyrazole triol

    PPT

    Estrogen Receptor/ERR Cancer
    Propyl pyrazole triol (PPT) is a selective estrogen receptor alpha (ERα) agonist. The relative binding affinity of Propyl pyrazole triol for ERα (ERα: 49%) around 410 times higher compared with estrogen receptor beta (ERβ: 0.12%).
  • HY-121251
    BI-167107

    Adrenergic Receptor Cancer Neurological Disease Endocrinology
    BI-167107 is a high affinity, full agonist that binds to the β2 adrenergic receptor (β2AR) with a dissociation constant Kd of 84 pM.
  • HY-P1701
    Morphiceptin

    Opioid Receptor Neurological Disease Cardiovascular Disease
    Morphiceptin is a potent and specific agonist for morphine (μ) receptors. Morphiceptin, as a synthetic peptide, is the amide of a fragment of the milk protein β-casein. Morphiceptin has morphinelike activities and is highly specific for morphine (μ) receptors but not for enkephalin (⸹) receptors.
  • HY-13715
    Norepinephrine

    Levarterenol; L-Noradrenaline

    Endogenous Metabolite Adrenergic Receptor Autophagy Endocrinology Cardiovascular Disease
    Norepinephrine (Levarterenol; L-Noradrenaline) is a potent adrenergic receptor (AR) agonist. Norepinephrine activates α1, α2, β1 receptors.
  • HY-13715A
    Norepinephrine hydrochloride

    Levarterenol hydrochloride; L-Noradrenaline hydrochloride

    Adrenergic Receptor Autophagy Endogenous Metabolite Cardiovascular Disease Endocrinology Cancer
    Norepinephrine (Levarterenol; L-Noradrenaline) hydrochloride is a potent adrenergic receptor (AR) agonist. Norepinephrine activates α1, α2, β1 receptors.
  • HY-B1486
    Oxprenolol hydrochloride

    Ba 39089

    Adrenergic Receptor Cardiovascular Disease
    Oxprenolol hydrochloride (Ba 39089) is an orally bioavailable β-adrenergic receptor (β-AR) antagonist with a Ki of 7.10 nM in a radioligand binding assay using rat heart muscle.
  • HY-18295
    Erteberel

    LY500307

    Estrogen Receptor/ERR Neurological Disease
    Erteberel (LY500307) is a potent and selective estrogen receptor beta (ERβ) agonist with Ki and EC50 of 1.54 nM and 3.61 nM, respectively. Anti-tumor activities.
  • HY-101656
    Medroxalol

    RMI81968

    Adrenergic Receptor Cardiovascular Disease
    Medroxalol (RMI81968) is an orally active adrenergic receptor antagonist, blocks α- and β-adrenergic receptors. Medroxalol shows antihypertensive and vasodilating effects.
  • HY-130842
    β-Naphthoflavone-CH2-Br

    β-NF-CH2-Br

    Ligands for E3 Ligase Cancer
    β-Naphthoflavone-CH2-Br (β-NF-CH2-Br) is an arylhydrocarbon receptor (AhR) ligand. β-Naphthoflavone-CH2-Br can be used to synthesize the PROTAC β-NF-JQ1(HY-130256).
  • HY-A0295
    (R)-Propranolol hydrochloride

    Adrenergic Receptor Endocrinology Neurological Disease Cardiovascular Disease
    (R)-Propranolol hydrochloride is a less active enantiomer of the β-adrenoceptor antagonist propranolol (HY-B0573). Propranolol is a nonselective β-adrenergic receptor (βAR) antagonist, has high affinity for the β1AR and β2AR with Ki values of 1.8 nM and 0.8 nM, respectively.
  • HY-135103S
    Tauro-β-muricholic acid-d4 sodium

    FXR Cancer
    Tauro-β-muricholic acid-d4 sodium is the deuterium labeled Tauro-β-muricholic acid sodium. Tauro-β-muricholic Acid sodium (T-βMCA sodium), a endogenous metabolite, is a competitive and reversible farnesoid X receptor (FXR) antagonist, with an IC50 of 40 μM.
  • HY-10326
    GW788388

    TGF-β Receptor Cancer
    GW788388 is a potent and selective inhibitor of ALK5 with IC50 of 18 nM, and also inhibits TGF-β type II receptor and activin type II receptor activities, without inhibiting BMP type II receptor.
  • HY-13715B
    Norepinephrine bitartrate monohydrate

    Levarterenol bitartrate monohydrate; L-Noradrenaline bitartrate monohydrate

    Adrenergic Receptor Autophagy Endogenous Metabolite Cardiovascular Disease Endocrinology
    Norepinephrine (Levarterenol; L-Noradrenaline) bitartrate monohydrate is a potent adrenergic receptor (AR) agonist. Norepinephrine activates α1, α2, β1 receptors.
  • HY-B0381A
    Betaxolol hydrochloride

    SL75212

    Adrenergic Receptor Cardiovascular Disease Endocrinology
    Betaxolol Hydrochloride is a selective beta1 adrenergic receptor blocker that can be used for the research of hypertension and glaucoma.
  • HY-B0381
    Betaxolol

    Adrenergic Receptor Cardiovascular Disease Endocrinology
    Betaxolol is a selective beta1 adrenergic receptor blocker that can be used for the research of hypertension and glaucoma.
  • HY-10408
    Ki20227

    c-Fms VEGFR c-Kit PDGFR Inflammation/Immunology
    Ki20227 is an orally active and highly selective c-Fms tyrosine kinase (CSF1R) inhibitor with IC50s of 2 nM, 12 nM, 451 and 217 nM for CSF1R, VEGFR2 (vascular endothelial growth factor receptor-2), c-Kit (stem cell factor receptor) and PDGFRβ (platelet-derived growth factor receptor β). Ki20227 suppresses osteoclast differentiation and osteolytic bone destruction.
  • HY-101514
    β3-AR agonist 1

    Adrenergic Receptor Cardiovascular Disease Endocrinology
    β3-AR agonist 1 (compound 15) is a highly potent, selective, and orally available β3-adrenergic receptor (β3-AR) agonist (EC50=18 nM), being inactive to β1-, β2-, and α1A-AR (β1/β3, β2/β3, and α1A/β3>556-fold).
  • HY-17497A
    Acebutolol hydrochloride

    Adrenergic Receptor Cardiovascular Disease Endocrinology
    Acebutolol hydrochloride is an orally active β1 adrenergic receptor (β1AR) antagonist. Acebutolol hydrochloride is used in the treatment of hypertension, angina pectoris and cardiac arrhythmias.
  • HY-17497
    Acebutolol

    Adrenergic Receptor Cardiovascular Disease
    Acebutolol is an orally active β1 adrenergic receptor (β1AR) antagonist. Acebutolol is used for hypertension, angina pectoris and cardiac arrhythmias research.
  • HY-100449
    AL-8810

    Prostaglandin Receptor Endocrinology
    AL-8810 is an 11β-fluoro analog of PGF and acts as a potent and selective antagonist of the PGFreceptor (FP receptor).
  • HY-110121
    NS3861 fumarate

    nAChR Neurological Disease
    NS3861 fumarate is an agonist of nicotinic acetylcholine receptors (nAChRs) and binds with high affinity to heteromeric α3β4 nAChR. The binding Ki values of 0.62, 25, 7.8, 55 nM for α3β4, α3β2, α4β4, α4β2, respectively.
  • HY-146275
    LXRβ agonist-3

    LXR Cancer
    LXRβ agonist-3 (compound 4-13) is a potent and selective LXRβ (liver X receptor β) agonist, with an EC50 of 0.095 μM. LXRβ agonist-3 efficiently inhibits U87EGFRvIII cell, with an IC50 of 3.75 μM. LXRβ agonist-3 shows antitumor activity, and can inhibit glioblastoma.
  • HY-110121A
    NS3861

    nAChR Neurological Disease
    NS3861 is an agonist of nicotinic acetylcholine receptors (nAChRs) and binds with high affinity to heteromeric α3β4 nAChR. The binding Ki values of 0.62, 25, 7.8, 55 nM for α3β4, α3β2, α4β4, α4β2, respectively.
  • HY-13715C
    Norepinephrine tartrate

    Levarterenol tartrate; L-Noradrenaline tartrate

    Endogenous Metabolite Adrenergic Receptor Autophagy Endocrinology Cardiovascular Disease
    Norepinephrine (Levarterenol; L-Noradrenaline) tartrate is a potent adrenergic receptor (AR) agonist. Norepinephrine tartrate activates α1, α2, β1 receptors.
  • HY-151876
    Glucocorticoid receptor modulator 1

    Glucocorticoid Receptor NF-κB AP-1 Inflammation/Immunology
    Glucocorticoid receptor modulator 1 is a highly potent and orally active non-steroidal selective glucocorticoid receptor modulator with an IC50 value of 9 nM and 130 nM for NF-κB and AP-1, respectively. Glucocorticoid receptor modulator 1 can effectively reduce the expression of inflammatory factors IL-6, IL-1β, TNF-α, also can relieve dermatitis in mice.
  • HY-B1486A
    Oxprenolol

    Ba 39089 free base

    Adrenergic Receptor Cardiovascular Disease
    Oxprenolol (Ba 39089 free base) is an orally bioavailable β-adrenergic receptor (β-AR) antagonist with a Ki of 7.10 nM in a radioligand binding assay using rat heart muscle.
  • HY-U00356
    Tertatolol

    (±)​-​Tertatolol; Racemic Tertatolol; dl-​Tertatolol

    Adrenergic Receptor 5-HT Receptor Cardiovascular Disease Endocrinology
    Tertatolol is a potent antagonist of beta-adrenoceptor and 5-HT receptor, with unique renal vasodilatatory effects.
  • HY-103066
    Br-PBTC

    nAChR Neurological Disease
    Br-PBTC is a potent, 2/4 subtype-selective positive allosteric modulator of nAChRs (nicotinic acetylcholine receptors) with α2β2,α2β4,α4β2,α4β4,(α4β2)2α4 and (α4β2)2β2 EC50 ranges from 0.1~0.6 μM. Br-PBTC acts from the c-tail of an α subunit.
  • HY-110157
    AC-186

    Estrogen Receptor/ERR Neurological Disease
    AC-186 is a selective non-steroidal estrogen receptor β (ERβ) agonist with EC50s of 6 nM and 5000 nM for ERβ and ERα, respectively. AC-186 shows gender specific neuroprotection in a Parkinson’s Disease rat model.
  • HY-100469
    LXRβ agonist-2

    LXR Cardiovascular Disease
    LXRβ agonist-2 is a highly potent and β-selective liver X receptor (LXRβ) agonist with EC50 of 7 nM, displays 28.5-fold selectivity over LXRα (EC50=200 nM) and used in the treatment of atherosclerosis.
  • HY-A0070B
    Liothyronine sodium hydrate

    Triiodothyronine sodium hydrate; 3,3',5-Triiodo-L-thyronine sodium hydrate; T3 sodium hydrate

    Thyroid Hormone Receptor Endogenous Metabolite Cancer Endocrinology
    Liothyronine sodium hydrate is an active form of thyroid hormone. Liothyronine sodium hydrate is a potent thyroid hormone receptors TRα and TRβ agonist with Kis of 2.33 nM for hTRα and hTRβ, respectively.
  • HY-A0070
    Liothyronine sodium

    Triiodothyronine sodium; 3,3',5-Triiodo-L-thyronine sodium; T3 sodium

    Thyroid Hormone Receptor Endogenous Metabolite Cancer Endocrinology
    Liothyronine sodium is an active form of thyroid hormone. Liothyronine sodium is a potent thyroid hormone receptors TRα and TRβ agonist with Kis of 2.33 nM for hTRα and hTRβ, respectively.
  • HY-A0070C
    Liothyronine hydrochloride

    Triiodothyronine hydrochloride; 3,3',5-Triiodo-L-thyronine hydrochloride; T3 hydrochloride

    Thyroid Hormone Receptor Endogenous Metabolite Cancer Endocrinology
    Liothyronine hydrochloride is an active form of thyroid hormone. Liothyronine hydrochloride is a potent thyroid hormone receptors TRα and TRβ agonist with Kis of 2.33 nM for hTRα and hTRβ, respectively.
  • HY-A0070A
    Liothyronine

    Triiodothyronine; 3,3',5-Triiodo-L-thyronine; T3

    Thyroid Hormone Receptor Endogenous Metabolite Cancer Endocrinology
    Liothyronine is an active form of thyroid hormone. Liothyronine is a potent thyroid hormone receptors TRα and TRβ agonist with Kis of 2.33 nM for hTRα and hTRβ, respectively.
  • HY-19888
    GSK-1482160

    P2X Receptor Inflammation/Immunology
    GSK-1482160 is an orally available negative allosteric modulator of the P2X7 receptor. P2X7 receptors are involved in the production of pro-inflammatory cytokines, such as Il-1β, by central and peripheral immune cells. GSK-1482160 has the potential for the research of inflammation diseases.
  • HY-B0141S
    Estradiol-d3

    β-Estradiol-d3; 17β-Estradiol-d3; 17β-Oestradiol-d3

    Estrogen Receptor/ERR Endogenous Metabolite Endocrinology Cancer
    Estradiol-d3 (β-Estradiol-d3) is the deuterium labeled Estradiol. Estradiol is a steroid sex hormone vital to the maintenance of fertility and secondary sexual characteristics in females. Estradiol upregulates IL-6 expression through the estrogen receptor β (ERβ) pathway.
  • HY-B1100
    Estradiol (cypionate)

    Estrogen Receptor/ERR Endocrinology Cancer
    Estradiol cypionate is a 17 β-cyclopentylpropinate ester of estradiol, inhibits ET-1 synthesis via estrogen receptor IC50 value: Target: estrogen receptor Estradiol cypionate is a synthetic ester, is a estrogen.
  • HY-P1866
    β-Endorphin, equine

    Opioid Receptor Neurological Disease
    β-Endorphin, equine is an endogenous opioid peptide, which binds at high affinity to both μ/δ opioid receptors. Analgesic properties.
  • HY-150601
    Estrogen receptor-IN-1

    Estrogen Receptor/ERR Metabolic Disease
    Estrogen receptor-IN-1 (compound 16) is a potent estrogen receptor (ER) inhibitor with IC50s of 13, 5µM for ERα and Erβ, respectively.
  • HY-B1392S
    Esmolol-d7 hydrochloride

    Adrenergic Receptor Autophagy Mitophagy Cardiovascular Disease Endocrinology
    Esmolol-d7 hydrochloride is the deuterium labeled Esmolol hydrochloride. Esmolol hydrochloride is a beta adrenergic receptor blocker.
  • HY-17457
    Levalbuterol tartrate

    Levosalbutamol tartrate

    Adrenergic Receptor Neurological Disease Endocrinology
    Levosalbutamol tartrate(levalbuterol) is the R-enantiomer of the short-acting β2-adrenergic receptor agonist salbutamol.
  • HY-108533
    CD2314

    RAR/RXR Cancer
    CD2314 is a potent and selective RARβ receptor agonist with a Kd of 195 nM in S91 melanoma cells.
  • HY-113960
    ERRα antagonist-1

    Estrogen Receptor/ERR Cancer
    ERRα antagonist-1 (Compound A) is a selective and high affinity estrogen-related receptor α (ERRα) antagonist. ERRα antagonist-1 inhibits interaction of ERRα with Proliferator-activated Receptor γ Coactivator-1α (PGC-1α) and PGC-1β, the IC50 values are 170 nM and 180 nM, respectively. ERRα antagonist-1 does not inhibit the interaction of either ERRβ or ERRγ with PGC-1α and PGC-1β coactivator, and also does not inhibit interaction of ERα or ERβ with PGC-1α or SRC-1.
  • HY-B1276A
    Metaproterenol

    Orciprenaline

    Adrenergic Receptor Inflammation/Immunology Cardiovascular Disease Endocrinology
    Metaproterenol (Orciprenaline) is a direct-acting sympathomimetic and a β2-adrenergic receptor (β2AR) agonist with an IC50 of 68 nM. Metaproterenol also has anti-inflammatory activity.
  • HY-16056
    Arbutamine

    Adrenergic Receptor Cardiovascular Disease
    Arbutamine is a short-acting, potent and nonselective β-adrenoceptor agonist. Arbutamine stimulates cardiac β1-, tracheal β2-, and adiopocyte β3- adrenergic receptors. Arbutamine provides cardiac stress increases heart rate, cardiac contractility, and systolic blood pressure. Arbutamine can be used for cardiac stress agent .
  • HY-16056A
    Arbutamine hydrochloride

    Adrenergic Receptor Cardiovascular Disease
    Arbutamine hydrochloride is a short-acting, potent and nonselective β-adrenoceptor agonist. Arbutamine hydrochloride stimulates cardiac β1-, tracheal β2-, and adiopocyte β3- adrenergic receptors. Arbutamine hydrochloride provides cardiac stress increases heart rate, cardiac contractility, and systolic blood pressure. Arbutamine hydrochloride can be used for cardiac stress agent .
  • HY-B0573A
    (S)-(-)-Propranolol hydrochloride

    Adrenergic Receptor Inflammation/Immunology Cardiovascular Disease
    (S)-(-)-Propranolol hydrochloride is a β-adrenergic receptor antagonist with log Kd values of -8.16, -9.08, and -6.93 for β1, β2, and β3, respectively. (S)-(-)-Propranolol hydrochloride the active enantiomer of propranolol and can be s used for study of hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy.
  • HY-P1866A
    β-Endorphin, equine TFA

    Opioid Receptor Neurological Disease
    β-Endorphin, equine (TFA) is an endogenous opioid peptide, which binds at high affinity to both μ/δ opioid receptors. Analgesic properties.
  • HY-139413
    β-D-Glucan

    Toll-like Receptor (TLR) Cancer
    β-D-glucan is a natural non-digestible polysaccharide and high biocompatibility that can be selectively recognized by recognition receptors such as Dectin-1 and Toll-like receptors as well as being easily internalized by murine or human macrophages, which is likely to attribute to a target delivery. β-d-glucan is an enteric delivery vehicle for probiotics.
  • HY-14649
    Retinoic acid

    Vitamin A acid; all-trans-Retinoic acid; ATRA

    RAR/RXR PPAR Endogenous Metabolite Autophagy Cancer
    Retinoic acid is a metabolite of vitamin A that plays important roles in cell growth, differentiation, and organogenesis. Retinoic acid is a natural agonist of RAR nuclear receptors, with IC50s of 14 nM for RARα/β/γ. Retinoic acid bind to PPARβ/δ with Kd of 17 nM. Retinoic acid acts as an inhibitor of transcription factor Nrf2 through activation of retinoic acid receptor alpha.
  • HY-107790
    5-Methoxyflavone

    DNA/RNA Synthesis Neurological Disease
    5-Methoxyflavone, belonged to Flavonoid family, is a DNA polymerase-beta inhibitor and neuroprotective agent against beta-amyloid toxicity. possess central nervous system (CNS) depressant effect mediated through the ionotropic GABAA receptors.
  • HY-108069
    Iptakalim hydrochloride

    Potassium Channel nAChR Neurological Disease
    Iptakalim hydrochloride, a lipophilic para-amino compound, is a novel ATP-sensitive potassium channel (KATP) opener, as well as an α4β2-containing nicotinic acetylcholine receptor (nAChR) antagonist.
  • HY-111442
    GC 14

    Thyroid Hormone Receptor Metabolic Disease
    GC 14 is a selective thyroid hormone receptor antagonist, with IC50 values of 35 nM and 200 nM for hTRβ and hTRα, respectively.
  • HY-12075
    LY2109761

    TGF-β Receptor Autophagy Cancer
    LY2109761 is an orally active, selective TGF-β receptor type I/II inhibitor with Kis of 38 nM and 300 nM, respectively.
  • HY-13226
    Galunisertib

    LY2157299

    TGF-β Receptor Cancer
    Galunisertib (LY2157299) is an oral and selective TGF-β receptor type I (TGF-βRI) kinase inhibitor with an IC50 of 56 nM.
  • HY-P1980
    A-71915 TFA

    Apoptosis Metabolic Disease
    A-71915 (TFA) is a selective inhibitor of ANP receptor (atrial natriuretic peptide-receptor), induces apoptosis and decreases insulin secretion in RINm5F pancreatic β-cells.
  • HY-B0141S3
    Estradiol-d2

    β-Estradiol-d2; 17β-Estradiol-d2; 17β-Oestradiol-d2

    Estrogen Receptor/ERR Endogenous Metabolite Endocrinology Cancer
    Estradiol-d2 (β-Estradiol-d2) is the deuterium labeled Estradiol. Estradiol is a steroid sex hormone vital to the maintenance of fertility and secondary sexual characteristics in females. Estradiol upregulates IL-6 expression through the estrogen receptor β (ERβ) pathway.
  • HY-B0141S1
    Estradiol-d4

    β-Estradiol-d4; 17β-Estradiol-d4; 17β-Oestradiol-d4

    Estrogen Receptor/ERR Endogenous Metabolite Endocrinology Cancer
    Estradiol-d4 (β-Estradiol-d4) is the deuterium labeled Estradiol. Estradiol is a steroid sex hormone vital to the maintenance of fertility and secondary sexual characteristics in females. Estradiol upregulates IL-6 expression through the estrogen receptor β (ERβ) pathway.
  • HY-N1064
    Xanthoplanine

    nAChR Neurological Disease
    Xanthoplanine, isolated from theroot of Xylopia parviflora, fully inhibits the EC50 ACh responses of both alpha7 and alpha4beta2 nACh receptors with estimated IC50 values of 9 μM (alpha7) and 5 μM (alpha4beta2).
  • HY-P1107
    Antisauvagine-30

    aSvg-30

    CRFR Neurological Disease
    Antisauvagine-30 (aSvg-30) is a potent, competitive and selective CRF2 receptor antagonist with Kd values of 1.4 nM and 153.6 nM for mouse CRF and rat CRF1 receptors, respectively.
  • HY-N7652
    Terminolic acid

    Bacterial Infection Inflammation/Immunology
    Terminolic acid is a pentacyclic triterpenoid glucoside isolated from Combretum racemosum. Terminolic acid can inhibit the pro-inflammatory cytokines by binding to receptor active site of IL-1β and IL-6, and enhance anti-inflammatory cytokines by binding to IL-4 receptor binding sites. Terminolic acid also exhibits moderate antibacterial activity.
  • HY-130553
    β-Spaglumic acid

    β-NAAG; β-N-Acetylaspartylglutamic acid

    Aminopeptidase mGluR Neurological Disease
    β-Spaglumic acid (β-NAAG) is a competitive NAAG peptidase inhibitor (Ki=1 µM) that protects spinal cord neurons from excitotoxicity and hypoxic damage. β-Spaglumic acid is also a selective mGluR3 antagonist (mGluR3 receptor functions to regulate activity-dependent synaptic potentiation in the hippocampus). β-Spaglumic acid can be used in neuroprotection-related studies.
  • HY-131104S
    Brombuterol-d9

    Bromobuterol D9

    Adrenergic Receptor Inflammation/Immunology
    Brombuterol D9 (Bromobuterol D9) is a deuterium labeled Brombuterol. Brombuterol is a β-adrenergic receptor agonist.
  • HY-107675
    Desformylflustrabromine hydrochloride

    Deformylflustrabromine hydrochloride; dFBr hydrochloride

    nAChR Neurological Disease
    Desformylflustrabromine hydrochloride is a selective agonist of α4β2 neuronal nicotinic acetylcholine receptor (nAChR) with a pEC50 of 6.48.
  • HY-15726
    ICI 89406

    Adrenergic Receptor Metabolic Disease
    ICI 89406 is a selective β1 adrenergic receptor antagonist amenable to labelling with positron emitters, for PET.
  • HY-12043
    SB 525334

    TGF-β Receptor Cancer
    SB 525334 is a potent and selective transforming growth factor β1 receptor (ALK5) inhibitor with an IC50 of 14.3 nM.
  • HY-131104AS
    Brombuterol-d9 hydrochloride

    Bromobuterol D9 hydrochloride

    Adrenergic Receptor Inflammation/Immunology
    Brombuterol D9 hydrochloride (Bromobuterol D9 hydrochloride) is a deuterium labeled Brombuterol hydrochloride. Brombuterol hydrochloride is a β-adrenergic receptor agonist.
  • HY-B1276
    Metaproterenol hemisulfate

    Orciprenaline hemisulfate

    Adrenergic Receptor Inflammation/Immunology Cardiovascular Disease Endocrinology
    Metaproterenol hemisulfate (Orciprenaline hemisulfate) is a direct-acting sympathomimetic and a β2-adrenergic receptor (β2AR) agonist with an IC50 of 68 nM. Metaproterenol hemisulfate also has anti-inflammatory activity.
  • HY-103221
    MeBIO

    Aryl Hydrocarbon Receptor GSK-3 CDK Others
    MeBIO is a potent AhR (aryl hydrocarbon receptor) agonist, with IC50 of 44 μM (GSK-3) and 55 μM (CDK1/cyclin B), respectively. MeBIO is inactive on GSK-3β.
  • HY-B1494
    Picrotoxinin

    Chloride Channel GABA Receptor Neurological Disease
    Picrotoxinin, a potent convulsant, is a chloride channel blocker. Picrotoxinin is a noncompetitive GABAA receptor antagonist, which negatively modulates the action of GABA on GABAA receptors. Picrotoxinin inhibits α1β2γ2L GABAA receptor with an IC50 of 1.15 μM.
  • HY-150692
    Estrogen receptor α antagonist 1

    Estrogen Receptor/ERR Cancer
    Estrogen receptor α antagonist 1 (compound 35) is a highly selective antagonist of estrogen receptor α, with IC50s of 0.02, 6.55 and 7.73 μM for estrogen receptor α, estrogen receptor β and MCF-7 cells, respectively. Estrogen receptor α antagonist 1 can be used for the research of cancer.
  • HY-B0982S
    Pindolol-d7

    5-HT Receptor Adrenergic Receptor Neurological Disease Endocrinology
    Pindolol-d7 (LB-46-d7) is the deuterium labeled Pindolol. Pindolol (LB-46) is a nonselective β-blocker with partial beta-adrenergic receptor agonist activity, also functions as a 5-HT1A receptor weak partial antagonist (Ki=33 nM).
  • HY-13715S
    (Rac)-Norepinephrine-d3 (formate)

    Endogenous Metabolite Adrenergic Receptor Autophagy Endocrinology Cardiovascular Disease
    (Rac)-Norepinephrine-d3 (formate) is deuterium labeled Norepinephrine. Norepinephrine (Levarterenol; L-Noradrenaline) is a potent adrenergic receptor (AR) agonist. Norepinephrine activates α1, α2, β1 receptors.
  • HY-P1269
    α-Conotoxin AuIB

    nAChR Neurological Disease
    α-Conotoxin AuIB, a potent and selective α3β4 nicotinic acetylcholine receptor (nAChR) antagonist, blocks α3β4 nAChRs expressed in Xenopus oocytes with an IC50 of 0.75 μM.
  • HY-101327
    Xamoterol

    Corwin; ICI 118587

    Adrenergic Receptor Cardiovascular Disease
    Xamoterol is a selective and potent agonist of beta1-adrenergic receptor. Xamoterol has the potential for the research of arrhythmogenesis. Xamoterol has the potential for the investigating the relationship between β1-adrenergic stimulation and IKr.
  • HY-P1106
    K41498

    CRFR Cardiovascular Disease
    K41498 is a potent and highly selective CRF2 receptor antagonist with Ki values of 0.66 nM, 0.62 nM and 425 nM for human CRF, CRF and CRF1 receptors respectively. K41498 is an analogues of antisauvagine-30 (aSvg-30), inhibits sauvagine-stimulated cAMP accumulation in hCRF- and hCRF-expressing cells. K41498 can be used for hypotension study.
  • HY-105670
    PHA-543613

    nAChR Neurological Disease
    PHA-543613 is a potent, orally active, brain-penetrant and selective α7 nAChR agonist with a Ki of 8.8 nM. PHA-543613 displays selectivity for α7-nAChR over α3β4, α1β1γδ, α4β2 and 5-HT3 receptors. PHA-543613 can be used for the cognitive deficits of Alzheimer's disease and schizophrenia research.
  • HY-B1803A
    Tracazolate hydrochloride

    ICI 136753 hydrochloride

    GABA Receptor Neurological Disease
    Tracazolate (ICI 136753) hydrochloride is a potent GABAA receptor modulator. Tracazolate hydrochloride has selectivity for β3 and potentiates α1β1γ2s (EC50=13.2 μM), α1β3γ2 (EC50=1.5 μM). Tracazolate hydrochloride has the potency (EC50) determined by the nature of the third subunit (γ1-3, δ, ε) within the receptor complex. Tracazolate hydrochloride possesses anxiolytic and anticonvulsant activity.
  • HY-105670B
    PHA-543613 dihydrochloride

    nAChR Neurological Disease
    PHA-543613 dihydrochloride is a potent, orally active, brain-penetrant and selective α7 nAChR agonist with a Ki value of 8.8 nM. PHA-543613 dihydrochloride displays selectivity for α7-nAChR over α3β4, α1β1γδ, α4β2 and 5-HT3 receptors. PHA-543613 dihydrochloride can be used for the cognitive deficits of Alzheimer's disease and schizophrenia research.
  • HY-P2294
    pm26TGF-β1 peptide

    TGF-β Receptor Inflammation/Immunology
    pm26TGF-β1 peptide is a peptide that mimics a portion of the human TGF-β1 molecule. pm26TGF-β1 peptide shows high affinity for the TGF-β1 receptor. pm26TGF-β1 peptide displays potent anti-inflammatory properties and does not exhibit neutrophils’ chemoattraction.
  • HY-119706
    Barbadin

    Apoptosis Others
    Barbadin is a novel and selective β-arrestin/β2-adaptin interaction inhibitor, has IC50 values of 19.1 μM for β-arrestin1 and 15.6 μM for β-arrestin2. Barbadin blocks agonist-promoted endocytosis of the prototypical β2-adrenergic, V2-vasopressin and angiotensin-II type-1 receptors. Barbadin can induce apoptosis.
  • HY-P3557
    Mibenratide

    Adrenergic Receptor Cardiovascular Disease
    Mibenratide, a small cyclic peptide, is an adrenergic β1 receptor antagonist. Mibenratide can be used for heart failure research.
  • HY-108526
    AC-55649

    RAR/RXR Autophagy Others
    AC-55649 is a potent, highly isoform-selective agonist of human RARβ2 receptor, with a pEC50 of 6.9.
  • HY-103214
    Bucindolol

    Adrenergic Receptor Cardiovascular Disease Endocrinology
    Bucindolol is a β1-adrenergic receptor blocker, with intrinsic sympathomimetic activity, used in the research of heart failure.
  • HY-123813
    CCX-777

    Others Cancer
    CCX-777 is a partial agonist of β-arrestin-2 recruitment to ACKR3 (atypical chemokine receptor 3).
  • HY-B2111
    (R)-(+)-Atenolol

    Adrenergic Receptor Others
    (R)-(+)-Atenolol is the less active enantiomer of the (R,S)-atenolol. (R,S)-atenolol is a β-adrenergic receptor antagonist.
  • HY-B0942
    Benzethonium chloride

    nAChR Bacterial Neurological Disease
    Benzethonium chloride inhibit human recombinant α7 and α4β2 neuronal nicotinic acetylcholine receptors in Xenopus oocytes.
  • HY-121567
    Metipranolol

    Adrenergic Receptor Cardiovascular Disease
    Metipranolol is a nonselective and orally active β-adrenergic receptor antagonist. Metipranolol can be used for hypertension and glaucoma research.
  • HY-147751
    APJ receptor agonist 6

    Apelin Receptor (APJ) Cardiovascular Disease
    APJ receptor agonist 6 (compound 9) is a potent APJ (apelin receptor) agonist, with Ki of 1.3 μM. APJ receptor agonist 6 has EC50 values of 0.070 , 0.097, and 0.063 μM for calcium, cAMP, and β-arrestin, respectively.
  • HY-B1486AS
    Oxprenolol-d7

    Adrenergic Receptor
    Oxprenolol-d7 is the deuterium labeled Oxprenolol. Oxprenolol (Ba 39089 free base) is an orally bioavailable β-adrenergic receptor (β-AR) antagonist with a Ki of 7.10 nM in a radioligand binding assay using rat heart muscle.
  • HY-P1269A
    α-Conotoxin AuIB TFA

    nAChR Neurological Disease
    α-Conotoxin AuIB TFA, a potent and selective α3β4 nicotinic acetylcholine receptor (nAChR) antagonist, blocks α3β4 nAChRs expressed in Xenopus oocytes with an IC50 of 0.75 μM.
  • HY-13954
    A 839977

    P2X Receptor Neurological Disease Inflammation/Immunology
    A 839977 is a P2X7 selective antagonist; it blocks BzATP-evoked calcium influx at recombinant human, rat and mouse P2X7 receptors (IC50 values are 20 nM, 42 nM and 150 nM respectively) and reduces inflammatory and neuropathic pain in animal models; the antihyperalgesic effects of P2X7 receptor blockade are mediated by blocking the release of IL-1beta.
  • HY-122537A
    Arotinolol

    Adrenergic Receptor 5-HT Receptor Cardiovascular Disease
    Arotinolol is a nonselective α/β-adrenergic receptor blocker and a vasodilating β-blocker. Arotinolol also shows potency for inhibiting the binding of the radioligand 125I-ICYP to 5HT1B-serotonergic receptor sites. Arotinolol is an antihypertensive agent for the treatment of a variety of cardiovascular pathologies as well as non-cardiovascular diseases.
  • HY-135594
    4'-Raloxifene-β-D-glucopyranoside

    Estrogen Receptor/ERR Metabolic Disease
    4'-Raloxifene-β-D-glucopyranoside, a metabolite of Raloxifene, is a benzothiophene glucuronidated at the 4' postion. 4'-Raloxifene-β-D-glucopyranoside is a selective and orally active estrogen receptor antagonist. 4'-Raloxifene-β-D-glucopyranoside can be used for inhibiting bone loss and resorption, and lowering lipid levels. 4'-Raloxifene-β-D-glucopyranoside, example 5, is extracted from patent US5567820A.
  • HY-B0573AS
    (S)-(-)-Propranolol-d7 hydrochloride

    Adrenergic Receptor Inflammation/Immunology Cardiovascular Disease
    (S)-(-)-Propranolol-d7 hydrochloride is the deuterium labeled (S)-(-)-Propranolol hydrochloride. (S)-(-)-Propranolol hydrochloride is a β-adrenergic receptor antagonist with log Kd values of -8.16, -9.08, and -6.93 for β1, β2, and β3, respectively. (S)-(-)-Propranolol hydrochloride the active enantiomer of propranolol and can be s used for study of hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy.
  • HY-135595
    6-Raloxifene-β-D-glucopyranoside

    Estrogen Receptor/ERR Drug Metabolite Metabolic Disease
    6-Raloxifene-β-D-glucopyranoside, a derivative of Raloxifene, is a benzothiophene glucuronidated at the 6' postion. 6-Raloxifene-β-D-glucopyranoside is a selective and orally active estrogen receptor antagonist. 6-Raloxifene-β-D-glucopyranoside can be used for inhibiting bone loss and resorption, and lowering lipid levels. 6'-Raloxifene-β-D-glucopyranoside, compound Ia, is extracted from patent US5567820A.
  • HY-B0076S
    Bisoprolol-d7 hemifumarate

    Adrenergic Receptor Inflammation/Immunology Endocrinology
    Bisoprolol-d7 hemifumarate is the deuterium labeled Bisoprolol hemifumarate. Bisoprolol hemifumarate is a selective type β1 adrenergic receptor blocker.
  • HY-112426
    LAU159

    GABA Receptor Neurological Disease
    LAU159 is a functionally selective positive modulator of α1β3 GABA(A) receptor with an EC50 of 2.2 μM.
  • HY-101442
    SR9238

    LXR Metabolic Disease
    SR9238 is a synthetic liver X receptor (LXR) inverse agonist with IC50s of 214 nM and 43 nM for LXRα and LXRβ, respectively.
  • HY-17498
    Atenolol

    (RS)-Atenolol

    Adrenergic Receptor Neurological Disease Endocrinology
    Atenolol ((RS)-Atenolol) is a cardioselective β1-adrenergic receptor blocker, with a Ki of 697 nM atβ1-adrenoceptor in guine pig left ventricle membrane. Atenolol can be used for the research of hypertension and angina pectoris.
  • HY-B0723
    Ospemifene

    FC-1271a

    Estrogen Receptor/ERR Cancer
    Ospemifene is a non-estrogen selective estrogen receptor modulator (SERM), with Kis of 380 and 410 nM for estrogen receptor α (ERα) and ERβ, respectively. Ospemifene can be used for the research of vaginal atrophy and breast cancer.
  • HY-B1833
    Afloqualone

    HQ-495

    GABA Receptor Neurological Disease
    Afloqualone (HQ-495) is a GABAergic agent and has agonist activity at the β subtype of the GABAα receptor. Afloqualone has antivertiginous effects thought to be attributable to the increased sensitivity of GABA receptors of the LVN neuron site.
  • HY-P2294A
    pm26TGF-β1 peptide TFA

    TGF-β Receptor Inflammation/Immunology
    pm26TGF-β1 TFA peptide is a peptide that mimics a portion of the human TGF-β1 molecule. pm26TGF-β1 peptide TFA shows high affinity for the TGF-β1 receptor. pm26TGF-β1 peptide TFA displays potent anti-inflammatory properties and does not exhibit neutrophils’ chemoattraction.
  • HY-B0379A
    Adiphenine hydrochloride

    nAChR Neurological Disease
    Adiphenine hydrochloride is a non-competitive inhibitor of nicotinic acetylcholine receptor (nAChR), with an IC50s of 1.9, 1.8, 3.7, and 6.3 µM for α1, α3β4, α4β2, and α4β4, respectively. Adiphenine hydrochloride has anticonvulsant effects.
  • HY-P1106A
    K41498 TFA

    CFTR Cardiovascular Disease
    K41498 TFA is a potent and highly selective CRF2 receptor antagonist with Ki values of 0.66 nM, 0.62 nM and 425 nM for human CRF, CRF and CRF1 receptors respectively. K41498 TFA is an analogues of antisauvagine-30 (aSvg-30), inhibits sauvagine-stimulated cAMP accumulation in hCRF- and hCRF-expressing cells. K41498 TFA can be used for hypotension study.
  • HY-14933
    Prinaberel

    ERB-041

    Estrogen Receptor/ERR Wnt Apoptosis Cancer
    Prinaberel (ERB-041) is a potent and selective estrogen receptor (ER) β agonist with IC50s of 5.4, 3.1 and 3.7 nM for human, rat and mouse ERβ, respectively. Prinaberel displays >200-fold selectivity for ERβ over ERα. Prinaberel is a potent skin cancer chemopreventive agent that acts by dampening the WNT/β-catenin signaling pathway. Prinaberel induces ovarian cancer apoptosis.
  • HY-W009009
    L-838417

    GABA Receptor Neurological Disease
    L-838417 is a selective partial agonist at the α2, α3 and α5 subtypes of the GABAA receptor and an antagonist at the α1, with binding Ki values of 0.79 nM, 0.67 nM, 1.67 nM, 267 nM, 2.25 nM and 2183 nM for α1β3γ2, α2β3γ2, α3β3γ2, α4β3γ2, α5β3γ2 and α6β3γ2.
  • HY-101327A
    Xamoterol hemifumarate

    Corwin hemifumarate; ICI 118587 hemifumarate

    Adrenergic Receptor Cardiovascular Disease
    Xamoterol hemifumarate is a selective and potent agonist of beta1-adrenergic receptor. Xamoterol hemifumarate has the potential for the research of arrhythmogenesis. Xamoterol hemifumarate has the potential for the investigating the relationship between β1-adrenergic stimulation and IKr.
  • HY-B0141S2
    Estradiol-d5

    β-Estradiol-d5; 17β-Estradiol-d5; 17β-Oestradiol-d5

    Estrogen Receptor/ERR Endogenous Metabolite Endocrinology Cancer
    Estradiol-d5 is deuterium labeled Estradiol. Estradiol is a steroid sex hormone vital to the maintenance of fertility and secondary sexual characteristics in females. Estradiol upregulates IL-6 expression through the estrogen receptor β (ERβ) pathway.
  • HY-131997
    2'MeO6MF

    GABA Receptor Inflammation/Immunology Neurological Disease
    2'MeO6MF is a brain-penetrant positive allosteric modulator at α2β1γ2L and all α1-containing GABAA receptors. 2'MeO6MF also can directly activate α2β2/3 and α2β2/3γ2L GABAA receptors. 2'MeO6MF has anxiolytic and psychomotor stabilizing properties. 2'MeO6MF offers neuroprotection and improved functional recovery and dampens the stroke-induced inflammatory response.
  • HY-19822
    Elacestrant

    RAD1901

    Estrogen Receptor/ERR Cancer
    Elacestrant (RAD1901) is an orally available selective estrogen receptor degrader (SERD) with IC50s of 48 and 870 nM for ERα and ERβ, respectively.
  • HY-B1347
    Clorprenaline hydrochloride

    Adrenergic Receptor Inflammation/Immunology Endocrinology
    Clorprenaline hydrochloride is a β2-adrenergic receptor agonist that is implicated in bronchial expansion. Clorprenaline has the potential for asthma research.
  • HY-19822A
    Elacestrant dihydrochloride

    RAD1901 dihydrochloride

    Estrogen Receptor/ERR Cancer
    Elacestrant dihydrochloride (RAD1901 dihydrochloride) is an orally available selective estrogen receptor degrader (SERD) with IC50s of 48 and 870 nM for ERα and ERβ, respectively.
  • HY-B0381S
    Betaxolol-d5

    Adrenergic Receptor Cardiovascular Disease Endocrinology
    Betaxolol-d5 is the deuterium labeled Betaxolol. Betaxolol is a selective beta1 adrenergic receptor blocker that can be used for the research of hypertension and glaucoma.
  • HY-10407
    SU 5402

    VEGFR FGFR PDGFR Cancer
    SU 5402 is a potent multi-targeted receptor tyrosine kinase inhibitor with IC50 of 20 nM, 30 nM, and 510 nM for VEGFR2, FGFR1, and PDGFRβ, respectively.
  • HY-143259
    BE1218

    LXR Cancer
    BE1218 is a liver X receptor (LXR) inverse agonist with IC50 values of 9 nM and 7 nM against LXRα and LXRβ, respectively.
  • HY-111443
    TR antagonist 1

    Thyroid Hormone Receptor Metabolic Disease Endocrinology
    TR antagonist 1 is a high-affinity thyroid hormone receptor (TR) antagonist with IC50s of 36 and 22 nM for TRα and TRβ, respectively.
  • HY-103241
    Ro 90-7501

    Amyloid-β ATM/ATR Phosphatase Apoptosis Cancer Neurological Disease
    Ro 90-7501 is an amyloid β42 (Aβ42) fibril assembly inhibitor that reduces Aβ42-induced cytotoxicity (EC50 of 2 μM). Ro 90-7501 inhibits ATM phosphorylation and DNA repair. RO 90-7501 selectively enhances toll-like receptor 3 (TLR3) and RIG-I-like receptor (RLR) ligand-induced IFN-β gene expression and antiviral response. Ro 90-7501 also inhibits protein phosphatase 5 (PP5) in a TPR-dependent manner. Ro 90-7501 has significant radiosensitizing effects on cervical cancer cells.
  • HY-130256
    β-NF-JQ1

    PROTACs Epigenetic Reader Domain Cancer
    β-NF-JQ1 is a PROTAC that recruits Aryl Hydrocarbon Receptor E3 ligase to target proteins. β-NF-JQ1 is directed against bromodomain-containing (BRD) proteins using β-NF as an AhR ligand, induces the interaction of AhR and BRD proteins, and displays effective anticancer activity that correlated with protein knockdown activity.
  • HY-B0141S4
    Estradiol-13C6

    β-Estradiol-13C6; E2-13C6; 17β-Estradiol-13C6; 17β-Oestradiol-13C6

    Estrogen Receptor/ERR Endogenous Metabolite Endocrinology Cancer
    Estradiol-13C6 (β-Estradiol-13C6) is the 13C-labeled Estradiol. Estradiol is a steroid sex hormone vital to the maintenance of fertility and secondary sexual characteristics in females. Estradiol upregulates IL-6 expression through the estrogen receptor β (ERβ) pathway.
  • HY-B0141S5
    Estradiol-13C2

    β-Estradiol-13C2; E2-13C2; 17β-Estradiol-13C2; 17β-Oestradiol-13C2

    Estrogen Receptor/ERR Endogenous Metabolite Endocrinology Cancer
    Estradiol-13C2 (β-Estradiol-13C2) is the 13C-labeled Estradiol. Estradiol is a steroid sex hormone vital to the maintenance of fertility and secondary sexual characteristics in females. Estradiol upregulates IL-6 expression through the estrogen receptor β (ERβ) pathway.
  • HY-16579
    Etifoxine hydrochloride

    HOE 36-801 hydrochloride

    GABA Receptor Neurological Disease
    Etifoxine hydrochloride, a non-benzodiazepine GABAergic compound, is a positive allosteric modulator of α1β2γ2 and α1β3γ2 subunit-containing GABAA receptors. Etifoxine hydrochloride reveals anxiolytic and anticonvulsant properties in rodents.
  • HY-P0295
    Gly-Arg-Gly-Asp-Ser

    Integrin Others
    Gly-Arg-Gly-Asp-Ser is a pentapeptide that forms the cell-binding domain of a glycoprotein, osteopontin. Gly-Arg-Gly-Asp-Ser binds to integrin receptors αvβ3 and αvβ5 with estimated IC50 of ∼5 and ∼6.5 μM
  • HY-16579A
    Etifoxine

    HOE 36-801

    GABA Receptor Neurological Disease
    Etifoxine, a non-benzodiazepine GABAergic compound, is a positive allosteric modulator of α1β2γ2 and α1β3γ2 subunit-containing GABAA receptors. Etifoxine reveals anxiolytic and anticonvulsant properties in rodents.
  • HY-P1365
    α-Conotoxin MII

    α-CTxMII

    nAChR Neurological Disease
    α-Conotoxin MII (α-CTxMII), a 16-amino acid peptide from the venom of the marine snail Conus magus, potently blocks nicotinic acetylcholine receptors (nAChRs) composed of α3β2 subunits, with an IC50 of 0.5 nM. α-Conotoxin MII (α-CTxMII) potently blocks β3-containing neuronal nicotinic receptors .
  • HY-116771A
    CL 316243

    Adrenergic Receptor Metabolic Disease
    CL316243 is a highly potent selective β3-adrenoceptor agonist with a EC50 of 3 nM, but is an extremely poor to β1/2- receptors.CL316243 is a effective stimulant of adipocyte lipolysis and increases brown adipose tissue thermogenesis and metabolic rate. CL316243 has the potential for the treatment obesity, diabetes and urge urinary incontinence.
  • HY-P1376A
    G-Protein antagonist peptide TFA

    mAChR Adrenergic Receptor Endocrinology
    G-Protein antagonist peptide TFA is a truncated substance P-related peptide, competes with receptor for G protein binding. G-Protein antagonist peptide TFA inhibits the activation of Gi or Go by M2 muscarinic cholinergic receptor (M2 mAChR) or of Gs by beta-adrenergic receptor in the reconstituted phospholipid vesicles, assayed by receptor-promoted GTP hydrolysis.
  • HY-13225A
    Rivanicline

    RJR-2403; (E)-Metanicotine

    nAChR Neurological Disease
    Rivanicline (RJR-2403; (E)-Metanicotine) is a neuronal nicotinic receptor agonist, showing high selectivity for the α4β2 subtype (Ki=26 nM); > 1,000 fold selectivity than α7 receptors(Ki= 36000 nM).
  • HY-135588
    Raloxifene 6,4'-Bis-β-D-glucuronide

    Drug Metabolite Metabolic Disease
    Raloxifene 6,4'-Bis-β-D-glucuronide (compound IV) is a metabolite of Raloxifene. Raloxifene is a selective estrogen receptor antagonist for the prevention of osteoporosis.
  • HY-135103
    Tauro-β-muricholic acid sodium

    T-βMCA sodium

    FXR Cancer
    Tauro-β-muricholic Acid sodium (T-βMCA sodium), a endogenous metabolite, is a competitive and reversible farnesoid X receptor (FXR) antagonist, with an IC50 of 40 μM.
  • HY-119802
    Practolol

    Adrenergic Receptor Cardiovascular Disease
    Practolol is a potent and selective β1-adrenergic receptor antagonist. Practolol can be used for the research of cardiac arrhythmias.
  • HY-108532
    AC-261066

    RAR/RXR Cancer
    AC-261066 is a potent, orally available and isoform-selective retinoic acid beta2 (RARbeta2) receptor agonist, with a pEC50 of 8.0.
  • HY-W013150
    Alpidem

    Ananxyl

    GABA Receptor Neurological Disease
    Alpidem selectively binds to α1β2γ2 subunit-containing GABAA receptor with an IC50 of 17 nM and exerts anxiolytic effect.
  • HY-B1037
    Salbutamol

    Albuterol; AH-3365

    Adrenergic Receptor Neurological Disease Endocrinology
    Salbutamol is a short-acting β2-adrenergic receptor agonist used for the relief of bronchospasm in conditions such as asthma and chronic obstructive pulmonary disease (COPD).
  • HY-B0141S6
    Estradiol-d2-1

    β-Estradiol-d2-1; E2-d2-1; 17β-Estradiol-d2-1; 17β-Oestradiol-d2-1

    Estrogen Receptor/ERR Endogenous Metabolite Inflammation/Immunology Neurological Disease
    Estradiol-d2-1 is the deuterium labeled Estradiol. Estradiol is a steroid sex hormone vital to the maintenance of fertility and secondary sexual characteristics in females. Estradiol upregulates IL-6 expression through the estrogen receptor β (ERβ) pathway.
  • HY-B1486S
    Oxprenolol-d7 hydrochloride

    Ba 39089-d7

    Adrenergic Receptor Cardiovascular Disease
    Oxprenolol-d7 hydrochloride (Ba 39089-d7) is the deuterium labeled Oxprenolol hydrochloride. Oxprenolol hydrochloride (Ba 39089) is an orally bioavailable β-adrenergic receptor (β-AR) antagonist with a Ki of 7.10 nM in a radioligand binding assay using rat heart muscle.
  • HY-106353
    Smilagenin

    Endogenous Metabolite mAChR Neurological Disease
    Smilagenin (SMI) is a small-molecule steroidal sapogenin from Anemarrhena asphodeloides and Pelargonium hortorum widely used in traditional Chinese medicine for treating chronic neurodegeneration diseases. Smilagenin (SMI) improves memory of aged rats by increasing the muscarinic receptor subtype 1 (M1)-receptor density. Smilagenin (SMI) attenuates Aβ(25-35)-induced neurodegenerationvia stimulating the gene expression of brain-derived neurotrophic factor, may represents a novel therapeutic strategy for AD.
  • HY-121166
    Levobetaxolol

    (S)-Betaxolol

    Adrenergic Receptor Others
    Levobetaxolol is a potent and high affinity β-adrenergic antagonist with IC50 values of 33.2, 2970, 709 nM for guinea pig atrial β1, tracheal β2 and rat colonic β3 receptors, respectively. Levobetaxolol reduces IOP (intraocular pressure). Levobetaxolol exhibits a micromolar affinity for L-type Ca21-channels. Levobetaxolol decreases the effects of ischaemia/reperfusion injury in rats. Levobetaxolol has the potential for the research of glaucoma.
  • HY-P1376
    G-Protein antagonist peptide

    mAChR Adrenergic Receptor Endocrinology
    G-Protein antagonist peptide is the substance P-related peptide that inhibits binding of G proteins to their receptors. G-Protein antagonist peptide competitively and reversibly inhibits M2 muscarinic receptor activation of Gi or Go and inhibits Gs activation by β-adrenoceptors.
  • HY-A0009
    Galanthamine hydrobromide

    Galantamine hydrobromide

    Cholinesterase (ChE) nAChR Neurological Disease
    Galanthamine hydrobromide (Galantamine hydrobromide) is a selective, reversible, competitive, alkaloid AChE inhibitor, with an IC50 of 0.35 µM. Galanthamine hydrobromide is a potent allosteric potentiating ligand (APL) of human α3β4, α4β2, α6β4 nicotinic receptors ( nAChRs). Galanthamine hydrobromide is developed for the research of Alzheimer's disease (AD).
  • HY-N8376
    Fustin

    (±)-Fustin; 3,7,3',4'-Tetrahydroxyflavanone

    Amyloid-β mAChR Cholinesterase (ChE) Neurological Disease
    Fustinis ((±)-Fustin; 3,7,3',4'-Tetrahydroxyflavanone) is a potent amyloid β (Aβ) inhibitor. Fustinis ((±)-Fustin; 3,7,3',4'-Tetrahydroxyflavanone) increases the expression of acetylcholine (ACh) levels, choline acetyltransferase (ChAT) activity, and ChAT gene induced by Aβ (1-42). Fustinis ((±)-Fustin; 3,7,3',4'-Tetrahydroxyflavanone) decreases in acetyl cholinesterase (AChE) activity and AChE gene expression induced by Aβ (1-42). Fustinis ((±)-Fustin; 3,7,3',4'-Tetrahydroxyflavanone) increases muscarinic M1 receptor gene expression and muscarinic M1 receptor binding activity. Fustinis ((±)-Fustin; 3,7,3',4'-Tetrahydroxyflavanone) can be used for Alzheimer's disease research.
  • HY-14564A
    GTS-21 dihydrochloride

    DMXB-A; DMBX-anabaseine

    nAChR 5-HT Receptor Inflammation/Immunology
    GTS-21 dihydrochloride is a selective alpha7 nicotinic acetylcholine receptor (α7-nAChR) agonist with anti‑inflammatory and cognition‑enhancing activities. GTS-21 dihydrochloride is also a α4β2 (Ki=20 nM for humanα4β2) and 5-HT3A receptor (IC50=3.1 μM) antagonist.
  • HY-P1365A
    α-Conotoxin MII TFA

    α-CTxMII TFA

    nAChR Neurological Disease
    α-Conotoxin MII TFA (α-CTxMII TFA), a 16-amino acid peptide from the venom of the marine snail Conus magus, potently blocks nicotinic acetylcholine receptors (nAChRs) composed of α3β2 subunits, with an IC50 of 0.5 nM. α-Conotoxin MII TFA (α-CTxMII TFA) potently blocks β3-containing neuronal nicotinic receptors .
  • HY-111509
    TAK-828F

    ROR Inflammation/Immunology
    TAK-828F is a potent, selective, and orally available retinoic acid receptor-related orphan receptor γt (RORγt) inverse agonist (binding IC50=1.9 nM, reporter gene IC50=6.1 nM). TAK-828F shows excellent RORγt isoforms selectivity (>5000-fold selectivity against human RORα and RORβ).
  • HY-P0118B
    Disitertide diammonium

    P144 diammonium

    TGF-beta/Smad PI3K Apoptosis Cancer
    Disitertide (P144) diammonium is a peptidic transforming growth factor-beta 1 (TGF-β1) inhibitor specifically designed to block the interaction with its receptor. Disitertide diammonium is also a PI3K inhibitor and an apoptosis inducer.
  • HY-P0118
    Disitertide

    P144

    TGF-beta/Smad PI3K Apoptosis Cancer
    Disitertide (P144) is a peptidic transforming growth factor-beta 1 (TGF-β1) inhibitor specifically designed to block the interaction with its receptor. Disitertide (P144) is also a PI3K inhibitor and an apoptosis inducer.
  • HY-P0118A
    Disitertide TFA

    P144 TFA

    TGF-beta/Smad PI3K Apoptosis Cancer
    Disitertide (P144) TFA is a peptidic transforming growth factor-beta 1 (TGF-β1) inhibitor specifically designed to block the interaction with its receptor. Disitertide TFA is also a PI3K inhibitor and an apoptosis inducer.
  • HY-100448A
    Butaprost

    Prostaglandin Receptor TGF-beta/Smad Endocrinology
    Butaprost is a selective prostaglandin E receptor (EP2) agonist with an EC50 of 33 nM and a Ki of 2.4 μM for murine EP2 receptor. Butaprost is less activity against murine EP1, EP3 and EP4 receptors. Butaprost attenuates fibrosis by hampering TGF-β/Smad2 signalling.
  • HY-10432
    A 83-01

    TGF-β Receptor Cancer
    A 83-01 is a potent inhibitor of TGF-β type I receptor ALK5 kinase, type I nodal receptor ALK4 and type I nodal receptor ALK7, with IC50s of 12 nM, 45 nM and 7.5 nM against the transcription induced by ALK5, ALK4 and ALK7, respectively.
  • HY-103524
    Valerenic acid

    (-)-Valerenic Acid

    GABA Receptor 5-HT Receptor Neurological Disease
    Valerenic acid ((-)-Valerenic Acid), a sesquiterpenoid, is an orally active positive allosteric modulator of GABAA receptors. Valerenic acid is also a partial agonist of the 5-HT5a receptor. Valerenic acid mediates anxiolytic activity via GABAA receptors containing the β3 subunit. Valerenic acid also exhibits potent antioxidant properties.
  • HY-114392
    Gly-β-MCA

    FXR Autophagy Metabolic Disease
    Gly-β-MCA, a bile acid, is a potent, sable, intestine-selective and oral bioactive farnesoid X receptor (FXR) inhibitor that may be a candidate for the treatment of metabolic disorders.
  • HY-N2509
    Iristectorigenin B

    Iristectrigenin B

    LXR Cardiovascular Disease
    Iristectorigenin B (Iristectrigenin B) is a liver X receptor (LXR) modulator. Iristectrigenin B stimulates the transcriptional activity of both LXR-α and LXR-β.
  • HY-107586
    Demethylasterriquinone B1

    DAQ B1; L-783281; Dimethylasterriquinone

    Insulin Receptor Akt Endocrinology
    Demethylasterriquinone B1 is a selective insulin receptor activator. Demethylasterriquinone B1 stimulates tyrosine phosphorylation of the IR β subunit, and the activation of PIK3 and AKT.
  • HY-10501
    SU14813

    PDGFR VEGFR c-Kit Cancer
    SU14813 is a multi-targeted receptor tyrosine kinases inhibitor with IC50s of 50, 2, 4, 15 nM for VEGFR2, VEGFR1, PDGFRβ and KIT.
  • HY-Y0313
    p-Hydroxybenzaldehyde

    Endogenous Metabolite GABA Receptor Neurological Disease
    p-Hydroxybenzaldehyde is a one of the major components in vanilla aroma, with antagonistic effect on GABAA receptor of the α1β2γ2S subtype at high concentrations.
  • HY-10501A
    SU14813 maleate

    PDGFR VEGFR c-Kit Cancer
    SU14813 maleate is a multi-targeted receptor tyrosine kinases inhibitor with IC50s of 50, 2, 4, 15 nM for VEGFR2, VEGFR1, PDGFRβ and KIT.
  • HY-17498S2
    (R)-Atenolol-d7

    Adrenergic Receptor Neurological Disease Endocrinology
    (R)-Atenolol-d7 is the deuterium labeled Atenolol. Atenolol ((RS)-Atenolol) is a cardioselective β1-adrenergic receptor blocker, with a Ki of 697 nM atβ1-adrenoceptor in guine pig left ventricle membrane. Atenolol can be used for the research of hypertension and angina pectoris.
  • HY-112813
    TUG-1375

    Free Fatty Acid Receptor Metabolic Disease
    TUG-1375 is an agonist of free fatty acid receptor 2 (FFA2/GPR43), with a pKi of 6.69. TUG-1375 is inactive on FFA3, FFA4, PPARα, PPARγ, PPARδ, LXRα or LXRβ.
  • HY-P0295A
    Gly-Arg-Gly-Asp-Ser TFA

    Integrin Inflammation/Immunology
    Gly-Arg-Gly-Asp-Ser (TFA) is a pentapeptide that forms the cell-binding domain of a glycoprotein, osteopontin. Gly-Arg-Gly-Asp-Ser binds to integrin receptors αvβ3 and αvβ5 with estimated IC50 of ∼5 and ∼6.5 μM.
  • HY-110168
    NS 9283

    nAChR Neurological Disease
    NS9283 is a positive positive allosteric modulator of (α4)3(β2)2 nicotinic ACh receptors. NS9283 can be used in a series of neurological conditions such as attention deficit hyperactivity disorder (ADHD), schizophrenia, Parkinson's disease and Alzheimer's disease.
  • HY-108628
    SU16f

    PDGFR Cancer
    SU16f is a potent and selective PDGFRβ inhibitor with IC50s of 10 nM, 140 nM, 2.29 μM for PDGFRβ, PDGFR1, PDGFR2, respectively. Neutralization of PDGFRβ receptor by SU16f blocks the promoting role of GC-MSCs (gastric cancer-derived mesenchymal stem cells) conditioned medium in gastric cancer cell proliferation and migration.
  • HY-110392
    CMP8

    Estrogen Receptor/ERR Cancer
    CMP8, a selective ligand for estrogen receptor, binds to the mutant estrogen receptor ligand binding domain (ERLBD). CMP8 exhibits IC50 values of 29 nM , 41 nM, 1100 nM and 2200 nM for MGERα, MGRERα, hERα and hERβ, respectively.
  • HY-130269
    β-Naphthoflavone-CH2-OH

    β-NF-CH2-OH

    Ligands for E3 Ligase Cancer
    β-Naphthoflavone-CH2-OH (β-NF-CH2-OH) is a ligand for arylhydrocarbon receptor (AhR) E3 ligase. β-Naphthoflavone-CH2-OH can be connected to the ligand for protein by a linker to form PROTACs or SNIPERs (e.g., β-naphthoflavone-JQ1) that recruit the AhR E3 ligase complex by incorporating AhR ligands into chimeric molecules. PROTACs are inducers of ubiquitination-mediated degradation of cancer-promoting proteins .
  • HY-B0804S
    Nadolol-d9

    SQ-11725-d9

    Adrenergic Receptor Endocrinology Cardiovascular Disease
    Nadolol D9 (SQ-11725 D9) is the deuterium labeled Nadolol. Nadolol is a non-selective and orally active β-adrenergic receptors blocker.
  • HY-N0233
    Bavachin

    Corylifolin

    Estrogen Receptor/ERR Cancer
    Bavachin, a flavonoid first isolated from seeds of P. corylifolia, acts as a phytoestrogen that activates the estrogen receptors ERα and ERβ with EC50s of 320 and 680 nM, respectively.
  • HY-17497S
    Acebutolol D7

    Adrenergic Receptor Endocrinology Cardiovascular Disease
    Acebutolol D7 is a deuterium labeled Acebutolol. Acebutolol is a selective β1 adrenergic receptor antagonist used in the treatment of hypertension, angina pectoris and cardiac arrhythmias.
  • HY-10627A
    GW3965 hydrochloride

    LXR Cardiovascular Disease Cancer
    GW3965 hydrochloride is a potent and selective liver X receptor (LXR) agonist with EC50s of 190 nM and 30 nM for hLXRα and hLXRβ, respectively.
  • HY-10627
    GW3965

    LXR Cardiovascular Disease
    GW3965 is a potent, selective liver X receptor (LXR) agonist with EC50s of 190 nM and 30 nM for hLXRα and hLXRβ, respectively.
  • HY-W011890
    Cridanimod

    Progesterone Receptor IFNAR Inflammation/Immunology
    Cridanimod is a potent progesterone receptor (PR) activator mediated through induction of IFNα and IFNβ expression. Cridanimod is a small-molecule immunomodulator and interferon inducer.
  • HY-78349
    A 77-01

    TGF-β Receptor Cancer
    A 77-01 is a potent inhibitor of transforming growth factor (TGF)-β type I receptor superfamily activin-like kinase ALK5 with an IC50 of 25 nM.
  • HY-U00449
    AGN 193109

    RAR/RXR Autophagy Cancer
    AGN 193109 is a retinoid analog, and acts as a specific and highly effective antagonist of retinoic acid receptors (RARs), with Kds of 2 nM, 2 nM, and 3 nM for RARα, RARβ, and RARγ, respectively.
  • HY-B0379AS
    Adiphenine-d4 hydrochloride

    nAChR Neurological Disease
    Adiphenine-d4 hydrochloride is the deuterium labeled Adiphenine hydrochloride. Adiphenine hydrochloride is a non-competitive inhibitor of nicotinic acetylcholine receptor (nAChR), with an IC50s of 1.9, 1.8, 3.7, and 6.3 µM for α1, α3β4, α4β2, and α4β4, respectively. Adiphenine hydrochloride has anticonvulsant effects.
  • HY-110160
    Pozanicline dihydrochloride

    ABT-089 dihydrochloride

    nAChR Neurological Disease
    Pozanicline dihydrochloride (ABT-089 dihydrochloride) is an orally bioavailable nicotinic acetylcholine receptor (nAChR) agonist with a Ki of 16.7 nM for binding to [ 3H]cytisine sites. Pozanicline is an α4β2-selective nAChR agonist, which binds to rat brain α4β2 nAChR with a Ki of 17 nM while binding to α7 nAChR is insignificant.
  • HY-107436
    LE135

    RAR/RXR TRP Channel Cancer Neurological Disease
    LE135 is a potent RAR antagonist that binds selectively to RARα (Ki of 1.4 μM) and RARβ (Ki of 220 nM), and has a higher affinity to RARβ. LE135 is highly selective over RARγ, RXRα, RXRβ and RXRγ. LE135 is also a potent TRPV1 and TRPA1 receptors activator with EC50s of 2.5 μM and 20 μM, respectively.
  • HY-14649S2
    11-cis-Retinoic Acid-d5

    RAR/RXR PPAR Endogenous Metabolite Autophagy Cancer
    11-cis-Retinoic Acid-d5 is the deuterium labeled Retinoic acid. Retinoic acid is a metabolite of vitamin A that plays important roles in cell growth, differentiation, and organogenesis. Retinoic acid is a natural agonist of RAR nuclear receptors, with IC50s of 14 nM for RARα/β/γ. Retinoic acid bind to PPARβ/δ with Kd of 17 nM. Retinoic acid acts as an inhibitor of transcription factor Nrf2 through activation of retinoic acid receptor alpha.
  • HY-N0166
    Gramine

    Donaxine

    Adiponectin Receptor Adrenergic Receptor Reverse Transcriptase Cancer Infection Metabolic Disease Endocrinology
    Gramine (Donaxine) is a natural alkaloid isolated from giant reed, acts as an active adiponectin receptor (AdipoR) agonist, with IC50s of 3.2 and 4.2 µM for AdipoR2 and AdipoR1, respectively. Gramine is also a human and mouse β2-Adrenergic receptor (β2-AR) agonist. Gramine (Donaxine) has anti-tumor, anti-viral and anti-inflammatory properties.
  • HY-B0802A
    Terbutaline

    Adrenergic Receptor Antibiotic Endocrinology
    Terbutaline is an orally active β2-adrenergic receptor agonist and an active metabolite of bambuterol. Terbutaline can be used in asthma symptom research.
  • HY-101325
    BRL 37344 sodium

    BRL 37344A

    Adrenergic Receptor Metabolic Disease Endocrinology
    BRL 37344 sodium (BRL 37344A) is a specific β3-adrenergic receptor agonist. BRL 37344 sodium treatment significantly lowers the body weight of obese mice.
  • HY-13225
    Rivanicline oxalate

    RJR-2403 oxalate; (E)-Metanicotine oxalate

    nAChR Neurological Disease
    Rivanicline oxalate (RJR-2403 oxalate; (E)-Metanicotine oxalate) is a neuronal nicotinic receptor agonist, showing high selectivity for the α4β2 subtype (Ki=26 nM); > 1,000 fold selectivity than α7 receptors(Ki= 3.6 μM).
  • HY-13225B
    Rivanicline hemioxalate

    RJR-2403 hemioxalate; (E)-Metanicotine hemioxalate

    nAChR Neurological Disease
    Rivanicline hemioxalate (RJR-2403 hemioxalate; (E)-Metanicotine hemioxalate) is a neuronal nicotinic receptor agonist, showing high selectivity for the α4β2 subtype (Ki=26 nM); > 1,000 fold selectivity than α7 receptors(Ki= 3.6 μM).
  • HY-12980
    Batefenterol

    GSK961081; TD-5959

    Adrenergic Receptor mAChR Inflammation/Immunology Endocrinology
    Batefenterol (GSK961081;TD-5959) is a novel muscarinic receptor antagonist and β2-adrenoceptor agonist; displays high affinity for hM2, hM3 muscarinic and hβ2-adrenoceptor with Ki values of 1.4, 1.3 and 3.7 nM, respectively.
  • HY-16579AS2
    Etifoxine-d5

    GABA Receptor Neurological Disease
    Etifoxine-d5 is the deuterium labeled Etifoxine. Etifoxine, a non-benzodiazepine GABAergic compound, is a positive allosteric modulator of α1β2γ2 and α1β3γ2 subunit-containing GABAA receptors. Etifoxine reveals anxiolytic and anticonvulsant properties in rodents.
  • HY-16579AS
    Etifoxine-d3

    GABA Receptor Neurological Disease
    Etifoxine-d3 is the deuterium labeled Etifoxine. Etifoxine, a non-benzodiazepine GABAergic compound, is a positive allosteric modulator of α1β2γ2 and α1β3γ2 subunit-containing GABAA receptors. Etifoxine reveals anxiolytic and anticonvulsant properties in rodents.
  • HY-B0573
    Propranolol hydrochloride

    Adrenergic Receptor Bacterial Neurological Disease Endocrinology Cancer
    Propranolol hydrochloride is a nonselective β-adrenergic receptor (βAR) antagonist, has high affinity for the β1AR and β2AR with Ki values of 1.8 nM and 0.8 nM, respectively. Propranolol hydrochloride inhibits [ 3H]-DHA binding to rat brain membrane preparation with an IC50 of 12 nM. Propranolol hydrochloride is used for study of hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy.
  • HY-B0573B
    Propranolol

    Adrenergic Receptor Bacterial Neurological Disease Cardiovascular Disease Endocrinology Cancer
    Propranolol is a nonselective β-adrenergic receptor (βAR) antagonist, has high affinity for the β1AR and β2AR with Ki values of 1.8 nM and 0.8 nM, respectively. Propranolol inhibits [ 3H]-DHA binding to rat brain membrane preparation with an IC50 of 12 nM. Propranolol is used for the study of hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy.
  • HY-10063
    Ispronicline

    TC-1734; ACD3480

    nAChR Neurological Disease
    Ispronicline (TC-1734), an orally active, brain-selective α4β2 nicotine acetylcholine receptor (nAChR) partial agonist, has shown memory-enhancing properties in rodents and a good tolerability profile. Ispronicline binds to the α4β2 nAChR with high affinity (Ki=11 nM) and is highly selective to other nAChRs such as α7 nAChR and α3β4 nAChR.
  • HY-110246
    Quin C1

    Others Inflammation/Immunology
    Quin C1 is a highly specific and potent agonist for formyl peptide receptor 2 (FPR2/ALX). Quin-C1 significantly reduces the neutrophil and lymphocyte counts in BALF, diminishes expression of TNF-α, IL-1β, KC, and TGF-β1, and decreases collagen deposition in lung tissue. Quin C1 has the potential for the research of lung injury.
  • HY-B1562C
    Bopindolol fumarate

    (±)-Bopindolol fumarate

    Adrenergic Receptor Renin 5-HT Receptor Neurological Disease Cardiovascular Disease
    Bopindolol ((±)-Bopindolol) fumarate is an orally active antagonist of β-adrenoceptors (ARs) with partial agonist activity. Bopindolol fumarate is non-selective for β1- and β2-ARs and has low affinity for β3-AR subtype. Bopindolol fumarate has intrinsic sympathomimetic as well as membrane stabilizing actions, inhibits renin secretion, and interacts with 5-HT receptors. Bopindolol fumarate is a prodrug of Pindolol (HY-B0982). Bopindolol fumarate can be used for essential and renovascular hypertension research.
  • HY-B1562
    Bopindolol

    (±)-Bopindolol

    Adrenergic Receptor Renin 5-HT Receptor Neurological Disease Cardiovascular Disease
    Bopindolol ((±)-Bopindolol) is an orally active antagonist of β-adrenoceptors (ARs) with partial agonist activity. Bopindolol is non-selective for β1- and β2-ARs and has low affinity for β3-AR subtype. Bopindolol has intrinsic sympathomimetic as well as membrane stabilizing actions, inhibits renin secretion, and interacts with 5-HT receptors. Bopindolol is a prodrug of Pindolol (HY-B0982). Bopindolol can be used for essential and renovascular hypertension research.
  • HY-100370
    MRK-016

    GABA Receptor Cancer
    MRK-016 is a selective, orally bioavailable inverse agonist of GABAA α5 receptor, with an EC50 of 3 nM for GABAA α5, and Kis of 0.83, 0.85, 0.77 and 1.4 nM for human GABAA α1β3γ2, GABAA α2β3γ2, GABAA α3β3γ2, and GABAA α5β3γ2, respectively; MRK-016 also readily penetrates the CNS.
  • 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-B0942S
    Benzethonium-d7 chloride

    nAChR Neurological Disease
    Benzethonium-d7 chloride is the deuterium labeled Benzethonium chloride. Benzethonium chloride inhibit human recombinant α7 and α4β2 neuronal nicotinic acetylcholine receptors in Xenopus oocytes.
  • HY-P1504
    β-Melanocyte Stimulating Hormone (MSH), human

    Beta-MSH (1-22) (human)

    Melanocortin Receptor Metabolic Disease Neurological Disease Endocrinology
    β-Melanocyte Stimulating Hormone (MSH), human, a 22-residue peptide, acts as an endogenous melanocortin-4 receptor (MC4-R) agonist.
  • HY-139581
    Ropanicant

    SUVN-911 free base

    nAChR Neurological Disease
    Ropanicant (SUVN-911 free base) is a novel, potent, selective, and orally active neuronal nicotinic acetylcholine α4β2 receptor antagonist for the research of depression.
  • HY-131106S
    Clorprenaline D7

    Adrenergic Receptor Endocrinology Inflammation/Immunology
    Clorprenaline D7 is a deuterium labeled Clorprenaline. Clorprenaline is a β2-adrenergic receptor agonist that is implicated in bronchial expansion. Clorprenaline has the potential for asthma research.
  • HY-123856
    MY10

    Phosphatase Neurological Disease
    MY10 is a potent and orally active receptor protein tyrosine phosphatase (RPTPβ/ζ) inhibitor. MY10 attenuates binge-like ethanol consumption and ethanol reward.
  • HY-10233
    Gaboxadol hydrochloride

    Lu 02-030 hydrochloride; THIP hydrochloride

    GABA Receptor Neurological Disease
    Gaboxadol hydrochloride (Lu 02-030 hydrochloride) is a potent agonist of the GABAA receptor and an antagonist of GABAC receptors (IC50=25 μM). Gaboxadol hydrochloride displays a partial agonist efficacy on subunit α1β2γ2 with an ED50 value of 143 µM, a full agonist efficacy at α5 subunit (ED50=28-129 µM) and a superagonist efficacy at α4β3δ (ED50=6 µM). Gaboxadol hydrochloride is a non-opioid agent.
  • HY-120802
    Navafenterol

    AZD-8871; LAS191351

    mAChR Adrenergic Receptor Inflammation/Immunology
    Navafenterol (AZD-8871) is an inhaled dual-acting, potent, selective, and long-lasting M3-antagonist/β2-agonist (MABA) with long-lasting effects and favorable safety profile. The pIC50 is 9.5 for human M3 receptor, and the pEC50 is 9.5 for β2-adrenoceptor. Navafenterol can be used for the research of chronic obstructive pulmonary disease (COPD). Bronchoprotective and antisialagogue effects. Favorable cardiovascular profile.
  • HY-130252
    YQ128

    NOD-like Receptor (NLR) Interleukin Related Inflammation/Immunology
    YQ128 is a potent and selective second-generation NLRP3 (NOD-like receptor P3) inflammasome inhibitor with an IC50 of 0.30 µM. YQ128 significantly and selectively suppresses the production of IL-1β, but not TNF-α, and it can cross the BBB to reach the CNS. YQ128 has anti-inflammatory activity.
  • HY-10426
    XCT790

    Estrogen Receptor/ERR Autophagy Cancer
    XCT-790 is a potent and selective inverse agonist for ERRα with an IC50 value of 0.37 μM. XCT-790 induces cell death in chemotherapeutic resistant cancer cells. XCT-790 (Compound 12) is inactive against ERRγ and the estrogen receptors ERα and ERβ.
  • HY-13012
    RepSox

    E-616452; SJN 2511

    TGF-β Receptor Metabolic Disease
    RepSox (E-616452) is a potent and selective transforming growth factor-beta receptor I/activin like kinase 5 (TGF-β-RI/ALK5) inhibitor. RepSox inhibits ALK5 autophosphorylation with an IC50 value of 4 nM. RepSox can be used for the research of obesity and associated metabolic diseases such as type 2 diabetes.
  • HY-B1276S
    Metaproterenol-d7 hemisulfate

    Adrenergic Receptor Inflammation/Immunology Cardiovascular Disease Endocrinology
    Metaproterenol-d7 (Orciprenaline-d7) hemisulfate is the deuterium labeled Metaproterenol hemisulfate. Metaproterenol hemisulfate (Orciprenaline hemisulfate) is a direct-acting sympathomimetic and a β2-adrenergic receptor (β2AR) agonist with an IC50 of 68 nM. Metaproterenol hemisulfate also has anti-inflammatory activity.
  • HY-17503S
    Metoprolol-d7

    Adrenergic Receptor Cardiovascular Disease Endocrinology
    Metoprolol-d7 is the deuterium labeled Metoprolol. Metoprolol (Toprol) is a selective β1 receptor blocker used in treatment of several diseases of the cardiovascular system, especially hypertension.
  • HY-P1504A
    β-Melanocyte Stimulating Hormone (MSH), human TFA

    Beta-MSH (1-22) (human) TFA

    Melanocortin Receptor Metabolic Disease Neurological Disease Endocrinology
    β-Melanocyte Stimulating Hormone (MSH), human TFA, a 22-residue peptide, acts as an endogenous melanocortin-4 receptor (MC4-R) agonist.
  • HY-B1517AS
    Alprenolol-d7 hydrochloride

    (RS)-Alprenolol-d7 hydrochloride; dl-Alprenolol-d7(hydrochloride)

    5-HT Receptor Cancer
    Alprenolol-d7 ((RS)-Alprenolol-d7) hydrochloride is the deuterium labeled Alprenolol hydrochloride. Alprenolol hydrochloride is a non-selective beta blocker as well as 5-HT1A receptor antagonist.
  • HY-112071
    Prenalterol

    Adrenergic Receptor Cardiovascular Disease
    Prenalterol is a selective β1-adrenergic receptor agonist. Prenalterol has no effect on gut smooth muscle contractile activity. Prenalterol can be used for researching cardiovascular disease.
  • HY-P1599
    Valorphin

    Opioid Receptor Cancer Neurological Disease
    Valorphin is an endogenous hemoglobin β-chain (33-39) fragment with opioid analgesic activity, binds to rat mu-opioid receptor, with an IC50 of 14 nM; Valorphin also shows anti-tumor activity.
  • HY-B0802
    Terbutaline sulfate

    Terbutaline hemisulfate

    Adrenergic Receptor Antibiotic Endocrinology
    Terbutaline sulfate is an orally active β2-adrenergic receptor agonist and an active metabolite of bambuterol. Terbutaline sulfate can be used in asthma symptom research.
  • HY-B1562B
    Bopindolol (malonate)

    (±)-Bopindolol (malonate)

    Adrenergic Receptor Renin 5-HT Receptor Neurological Disease Cardiovascular Disease
    Bopindolol ((±)-Bopindolol) malonate is an orally active antagonist of β-adrenoceptors (ARs) with partial agonist activity. Bopindolol malonate is non-selective for β1- and β2-ARs and has low affinity for β3-AR subtype. Bopindolol malonate has intrinsic sympathomimetic as well as membrane stabilizing actions, inhibits renin secretion, and interacts with 5-HT receptors. Bopindolol malonate is a prodrug of Pindolol (HY-B0982). Bopindolol malonate can be used for essential and renovascular hypertension research.
  • HY-P1264
    α-Bungarotoxin

    nAChR Neurological Disease
    α-Bungarotoxin is a competitive antagonist at nicotinic acetylcholine receptors (nAChRs). α-Bungarotoxin, a selective α7 receptor blocker, blocks α7 currents with an IC50 of 1.6 nM and has no effects on α3β4 currents at concentrations up to 3 μM.
  • HY-13521
    SB-505124

    TGF-β Receptor Cancer
    SB-505124 is a selective inhibitor of TGF-β Receptor type I receptors (ALK4, ALK5, ALK7), with IC50s of 129 nM and 47 nM for ALK4, ALK5, respectively, but it does not inhibit ALK1, 2, 3, or 6.
  • HY-13521A
    SB-505124 hydrochloride

    TGF-β Receptor Cancer
    SB-505124 hydrochloride is a selective inhibitor of TGF-β Receptor type I receptor (ALK4, ALK5, ALK7), with IC50s of 129 nM and 47 nM for ALK4, ALK5, respectively, but it does not inhibit ALK1, 2, 3, or 6.
  • HY-A0009S
    Galanthamine-d3 hydrobromide

    Galantamine-d3 hydrobromide

    Cholinesterase (ChE) nAChR Neurological Disease
    Galanthamine-d3 (hydrobromide) is deuterium labeled Galanthamine (hydrobromide). Galanthamine hydrobromide (Galantamine hydrobromide) is a selective, reversible, competitive, alkaloid AChE inhibitor, with an IC50 of 0.35 µM. Galanthamine hydrobromide is a potent allosteric potentiating ligand (APL) of human α3β4, α4β2, α6β4 nicotinic receptors ( nAChRs). Galanthamine hydrobromide is developed for the research of Alzheimer's disease (AD).
  • HY-111385
    UNC9994 hydrochloride

    Dopamine Receptor 5-HT Receptor Neurological Disease
    UNC9994 hydrochloride is a functionally selective, β-arrestin–biased dopamine D2 receptor (D2R) agonist that selectively activates β-arrestin recruitment and signaling. UNC9994 hydrochloride shows a binding affinity with a Ki of 79 nM for D2R. UNC9994 hydrochloride is also an antagonist of Gi-regulated cAMP production and partial agonist for D2R/β-arrestin-2 interactions. UNC9994 hydrochloride shows antipsychotic-like activity.
  • HY-13894
    Tyrphostin AG1296

    AG1296

    PDGFR c-Kit FLT3 Apoptosis Cancer Inflammation/Immunology Cardiovascular Disease
    Tyrphostin AG1296 is a potent and selective inhibitor of platelet-derived growth factor receptor (PDGFR), with an IC50 of 0.8 μM. Tyrphostin AG1296 inhibits signaling of human PDGF α- and β-receptors as well as of the related stem cell factor receptor (c-Kit). Tyrphostin AG1296 is also a potent inhibitor of FLT3, with an IC50 in the micromolar range.
  • HY-10020
    Varenicline Hydrochloride

    CP 526555 hydrochloride

    nAChR Neurological Disease
    Varenicline Hydrochloride (CP 526555 hydrochloride) is a high affinity, selective α4β2 nicotine acetylcholine receptor (nAChR) partial agonist and full α7 nAChR agonist. Varenicline Hydrochloride is also a potent partial agonist of α6β2 nAChR in striatum of rats with a Ki value of 0.12 nM.
  • HY-19436
    Solabegron

    GW 427353

    Adrenergic Receptor Metabolic Disease Endocrinology
    Solabegron (GW 427353) is a selective β3-adrenergic receptor agonist, stimulating cAMP accumulation in Chinese hamster ovary cells expressing the human β3-AR, with an EC50 value of 22 nM. Solabegron (GW 427353) is being developed for the treatment of overactive bladder and irritable bowel syndrome.
  • HY-17498S
    Atenolol-d7

    (RS)-Atenolol-d7

    Adrenergic Receptor Neurological Disease Endocrinology
    Atenolol-d7 ((RS)-Atenolol-d7) is the deuterium labeled Atenolol. Atenolol ((RS)-Atenolol) is a cardioselective β1-adrenergic receptor blocker, with a Ki of 697 nM atβ1-adrenoceptor in guine pig left ventricle membrane. Atenolol can be used for the research of hypertension and angina pectoris.
  • HY-103510
    TB-21007

    GABA Receptor Neurological Disease
    TB-21007 is an inverse agonist of α5β3γ2 subunit-containing GABAA receptor with a Ki of 1.6 nM. TB-21007 enhanced spatial memory in rats.
  • HY-P2497
    Exendin (5-39)

    GCGR Neurological Disease
    Exendin (5-39) is a potent glucagon-like peptide 1 (GLP-1) receptor antagonist. Exendin (5-39) improves memory impairment in β-amyloid protein-treated rats.
  • HY-104070
    LG-100064

    RAR/RXR Autophagy Cancer
    LG-100064 is a retinoid-X-receptor (RXR) agonist, with EC50s of 330 nM, 200 nM, and 260 nM for RXRα, RXRβ and RXRγ; LG-100064 can be used in the research of cancer.
  • HY-17503S2
    (S)-Metoprolol-d7

    Adrenergic Receptor Cardiovascular Disease Endocrinology
    (S)-Metoprolol-d7 is the deuterium labeled Metoprolol. Metoprolol (Toprol) is a selective β1 receptor blocker used in treatment of several diseases of the cardiovascular system, especially hypertension.
  • HY-17503S1
    (R)-Metoprolol-d7

    Adrenergic Receptor Cardiovascular Disease Endocrinology
    (R)-Metoprolol-d7 is the deuterium labeled Metoprolol. Metoprolol (Toprol) is a selective β1 receptor blocker used in treatment of several diseases of the cardiovascular system, especially hypertension.
  • HY-19822B
    Elacestrant S enantiomer dihydrochloride

    RAD1901 S enantiomer dihydrochloride

    Estrogen Receptor/ERR Cancer
    Elacestrant S enantiomer dihydrochloride (RAD1901 S enantiomer dihydrochloride) is an low activity enantiomer of elacestrant dihydrochloride. Elacestrant (RAD1901) dihydrochloride is a selective and orally available estrogen receptor (ERR) degrader with IC50 values of 48 and 870 nM for ERα and ERβ, respectively.
  • HY-110241
    Dianicline dihydrochloride

    nAChR Neurological Disease
    Dianicline dihydrochloride is a α4β2 nicotinic acetylcholine receptor partial agonist, a class of drugs that includes varenicline and cytisine for smoking cessation. Dianicline dihydrochloride increases cessation rates in a dose-dependent manner.
  • HY-B0381AS
    Betaxolol-d7 hydrochloride

    SL75212-d7

    Adrenergic Receptor Cardiovascular Disease Endocrinology
    Betaxolol-d7 hydrochloride (SL75212-d7) is the deuterium labeled Betaxolol hydrochloride. Betaxolol Hydrochloride is a selective beta1 adrenergic receptor blocker that can be used for the research of hypertension and glaucoma.
  • HY-B0316
    Avobenzone

    Estrogen Receptor/ERR Apoptosis Others
    Avobenzone, a dibenzoylmethane compound, is one of the most widely used filters in sunscreens for skin photoprotection in the UVA band. Avobenzone is an endocrine disruptor that directly binds to estrogen receptor β and acts as an estrogen agonist.
  • HY-120802A
    Navafenterol saccharinate

    AZD-8871 saccharinate; LAS191351 saccharinate

    mAChR Adrenergic Receptor Infection Inflammation/Immunology
    Navafenterol (AZD-8871) saccharinate is an inhaled dual-acting, potent, selective, and long-lasting M3-antagonist/β2-agonist (MABA) with long-lasting effects and favorable safety profile. The pIC50 is 9.5 for human M3 receptor, and the pEC50 is 9.5 for β2-adrenoceptor. Navafenterol saccharinate can be used for the research of chronic obstructive pulmonary disease (COPD). Bronchoprotective and antisialagogue effects. Favorable cardiovascular profile.
  • HY-W008859
    Tetrac

    Tetraiodothyroacetic acid; 3,3',5,5'-Tetraiodothyroacetic acid

    Integrin Endogenous Metabolite Cancer
    Tetrac (Tetraiodothyroacetic acid), a derivative of L-thyroxine (T4), is a thyrointegrin receptor antagonist. Tetrac blocks the actions of T4 and 3,5,3'-triiodo-L-thyronine (T3) at the cell surface receptor for thyroid hormone on integrin αvβ3. Tetra has anti-angiogenic and anti-tumor activities.
  • HY-10517
    Orantinib

    SU6668; TSU-68

    PDGFR FGFR VEGFR Apoptosis Cancer
    Orantinib (SU6668; TSU-68) is a multi-targeted receptor tyrosine kinase inhibitor with Kis of 2.1 μM, 8 nM and 1.2 μM for Flt-1, PDGFRβ and FGFR1, respectively.
  • HY-P0318
    Hemorphin-7

    Opioid Receptor Angiotensin-converting Enzyme (ACE) Cardiovascular Disease
    Hemorphin-7 is a hemorphin peptide, an endogenous opioid peptide derived from the β-chain of hemoglobin. Hemorphin peptides exhibits antinociceptive and antihypertensive activities, activating opioid receptors and inhibiting angiotensin-converting enzyme (ACE).
  • HY-B1675A
    Levalbuterol hydrochloride

    (R)-Albuterol hydrochloride; (R)-Salbutamol hydrochloride; Levosalbutamol hydrochloride

    Adrenergic Receptor Inflammation/Immunology
    Levalbuterol ((R)-Albuterol) hydrochloride is a short-acting β2-adrenergic receptor agonist and the active (R)-enantiomer of Salbutamol. Levalbuterol hydrochloride is a more potent bronchodilator than Salbutamol and has the potential for the treatment of COPD.
  • HY-16681
    AGN 194310

    VTP-194310

    RAR/RXR Autophagy Cancer
    AGN 194310 (VTP-194310) is a high affinity, potent and selective retinioic acid receptors (RARs) pan-antagonist with Kd values of 3 nM, 2 nM, 5 nM for RARα, RARβ, RARγ, respectively.
  • HY-113320
    Etiocholanolone

    5β-Androsterone

    GABA Receptor Endogenous Metabolite Neurological Disease
    Etiocholanolone (5β-Androsterone) is the excreted metabolite of testosterone and has anticonvulsant activity. Etiocholanolone is a less potent neurosteroid positive allosteric modulator (PAM) of the GABAAreceptor than its enantiomer form.
  • HY-N0250
    Saikosaponin D

    STAT NF-κB Estrogen Receptor/ERR Bacterial Cancer Infection Inflammation/Immunology
    Saikosaponin D is a triterpene saponin isolated from Bupleurum, with anti-inflammatory, anti-bacterial, anti-tumor, and anti-allergic activities; Saikosaponin D inhibits selectin, STAT3 and NF-kB and activates estrogen receptor-β.
  • HY-14299
    Indacaterol

    Adrenergic Receptor Inflammation/Immunology Cardiovascular Disease
    Indacaterol is an orally active ultra-long-acting β2 adrenergic receptor (ADRB2) agonist. Indacaterol inhibits NF-κB activity in a β-arrestin2-dependent manner, preventing further lung damage and improving lung function in COPD (chronic obstructive pulmonary disorder). Indacaterol can also be used in cardiovascular disease research.
  • HY-B0446
    Naphazoline hydrochloride

    Naphthazoline hydrochloride

    Adrenergic Receptor TNF Receptor Interleukin Related VEGFR Inflammation/Immunology Cardiovascular Disease
    Naphazoline (Naphthazoline) hydrochloride is a potent α-adrenergic receptor agonist. Naphazoline hydrochloride reduces vascular hyperpermeability and promotes vasoconstriction. Naphazoline hydrochloride reduces the levels of inflammatory factors (TNF-α, IL-1β and IL-6), cytokines (IFN-γ and IL-4), IgE, GMCSF, and NGF。Naphazoline hydrochloride can be used for non-bacterial conjunctivitis research.
  • HY-111326
    Naphazoline

    Naphthazoline

    Adrenergic Receptor TNF Receptor Interleukin Related VEGFR Inflammation/Immunology Cardiovascular Disease
    Naphazoline (Naphthazoline) is a potent α-adrenergic receptor agonist. Naphazoline reduces vascular hyperpermeability and promotes vasoconstriction. Naphazoline reduces the levels of inflammatory factors (TNF-α, IL-1β and IL-6), cytokines (IFN-γ and IL-4), IgE, GMCSF, and NGF。Naphazoline can be used for non-bacterial conjunctivitis research.
  • HY-B0573BS
    Propranolol-d7

    Adrenergic Receptor Neurological Disease Cardiovascular Disease Endocrinology
    Propranolol-d7 is the deuterium labeled Propranolol. Propranolol is a nonselective β-adrenergic receptor (βAR) antagonist, has high affinity for the β1AR and β2AR with Ki values of 1.8 nM and 0.8 nM, respectively. Propranolol inhibits [ 3H]-DHA binding to rat brain membrane preparation with an IC50 of 12 nM. Propranolol is used for the study of hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy.
  • HY-B0573S
    Propranolol-d7 hydrochloride

    Adrenergic Receptor Endocrinology Neurological Disease Cardiovascular Disease
    Propranolol D7 hydrochloride is a deuterium labeled Propranolol hydrochloride. Propranolol hydrochloride is a nonselective β-adrenergic receptor (βAR) antagonist, has high affinity for the β1AR and β2AR with Ki values of 1.8 nM and 0.8 nM, respectively. Propranolol hydrochloride inhibits [ 3H]-DHA binding to rat brain membrane preparation with an IC50 of 12 nM. Propranolol hydrochloride is used for the study of hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy.
  • HY-142949
    ALK5-IN-7

    TGF-β Receptor Cancer Inflammation/Immunology
    ALK5-IN-7 is a potent inhibitor of ALK5. Transforming growth factor beta (TGF-β) is a multifunctional cytokine that is involved in regulating cell proliferation, differentiation and apoptosis through complex receptor signaling pathways on the cell surface in an autocrine, paracrine and endocrine manner. ALK5-IN-7 has the potential for the research of TGF-β-related diseases and conditions, including but not limited to tumors, fibrotic diseases, inflammatory diseases, autoimmune diseases, etc (extracted from patent WO2021129621A1, compound 4).
  • HY-142950
    ALK5-IN-6

    TGF-β Receptor Cancer Inflammation/Immunology
    ALK5-IN-6 is a potent inhibitor of ALK5. Transforming growth factor beta (TGF-β) is a multifunctional cytokine that is involved in regulating cell proliferation, differentiation and apoptosis through complex receptor signaling pathways on the cell surface in an autocrine, paracrine and endocrine manner. ALK5-IN-6 has the potential for the research of TGF-β-related diseases and conditions, including but not limited to tumors, fibrotic diseases, inflammatory diseases, autoimmune diseases, etc (extracted from patent WO2021129621A1, compound 1).
  • HY-P1542
    Urotensin I

    Catostomus urotensin I

    CRFR Cardiovascular Disease Endocrinology
    Urotensin I (Catostomus urotensin I), a CRF-like neuropeptide, acts as an agonist of CRF receptor with pEC50s of 11.46, 9.36 and 9.85 for human CRF1, human CRF2 and rat CRF receptors in CHO cells, and Kis of 0.4, 1.8, and 5.7 nM for hCRF1, rCRF and mCRF receptors, respectively.
  • HY-P1542B
    Urotensin I TFA

    Catostomus urotensin I TFA

    CRFR Endocrinology Cardiovascular Disease
    Urotensin I (Catostomus urotensin I) TFA, a CRF-like neuropeptide, acts as an agonist of CRF receptor with pEC50s of 11.46, 9.36 and 9.85 for human CRF1, human CRF2 and rat CRF receptors in CHO cells, and Kis of 0.4, 1.8, and 5.7 nM for hCRF1, rCRF and mCRF receptors, respectively.
  • HY-136146
    SUVN-911

    nAChR Neurological Disease
    SUVN-911 is a potent, selective, brain penetrated and orally bioavailable neuronal nicotinic acetylcholine α4β2 receptor antagonist, with a Ki of 1.5 nM. SUVN-911 has antidepressant activity.
  • HY-114192
    TGFβRI-IN-1

    TGF-β Receptor Cancer
    TGFβRI-IN-1 is an oral active and selective TGFβ receptor type I (TGFβRI) kinase inhibitor, with IC50 values of 2 nM and 7.6 μM for TGFβRI and TGFβRII, respectively .
  • HY-144549
    LXR agonist 1

    LXR Cardiovascular Disease
    LXR (Liver X receptor) agonist 1 is potent LXR agonist with AC50s of 1.5 nM and 12 nM for LXR-α and LXR-β, respectively. LXR agonist 1 has the potential for the research of atherosclerosis.
  • HY-119802S
    Practolol-d7

    Adrenergic Receptor Cardiovascular Disease
    (Rac)-Practolol-d7 is the deuterium labeled Practolol. Practolol is a potent and selective β1-adrenergic receptor antagonist. Practolol can be used for the research of cardiac arrhythmias.
  • HY-19822D
    Elacestrant (S enantiomer)

    RAD1901 S enantiomer

    Estrogen Receptor/ERR Cancer
    Elacestrant S enantiomer (RAD1901 S enantiomer) is an low activity enantiomer of elacestrant. Elacestrant (RAD1901) is a selective and orally available estrogen receptor (ERR) degrader with IC50 values of 48 and 870 nM for ERα and ERβ, respectively.
  • HY-124867
    D3-βArr

    TSH Receptor Endocrinology
    D3-βArr is a positive allosteric modulator for thyrotropin receptor (TSHR), which initiates translocation of β-Arr 1 by direct TSHR activation and potentiates TSH-mediated preosteoblast differentiation in vitro.
  • HY-P1295
    Urocortin, human

    Urocortin (human); Human urocortin; Human urocortin 1; Human urocortin I

    CRFR Neurological Disease Endocrinology
    Urocortin, human, a 40-aa neuropeptide, acts as a selective agonist of endogenous CRF2 receptor, with Kis of 0.4, 0.3, and 0.5 nM for hCRF1, rCRF and mCRF, respectively.
  • HY-13223
    Crenolanib

    CP-868596

    FLT3 PDGFR Autophagy Cancer
    Crenolanib is a potent and selective inhibitor of wild-type and mutant isoforms of the class III receptor tyrosine kinases FLT3 and PDGFRα/β with Kds of 0.74 nM and 2.1 nM/3.2 nM, respectively.
  • HY-N0020
    Echinacoside

    Wnt Reactive Oxygen Species Neurological Disease
    Echinacoside, one of the phenylethanoids isolated from the stems of Cistanche deserticola, effectively inhibits Wnt/β-catenin signaling. Echinacoside elicits neuroprotection by activating Trk receptors and their downstream signal pathways. Antiosteoporotic activity.
  • HY-B0723S
    Ospemifene D4

    FC-1271a D4

    Estrogen Receptor/ERR Cancer
    Ospemifene D4 (FC-1271a D4) is a deuterium labeled Ospemifene. Ospemifene is a selective and orally active estrogen receptor modulator for the prevention of osteoporosis with IC50 values of 827 nM and 1633 nM for estrogen receptor α (ERα) and ERβ, respectively. Ospemifene has bone-sparing, antitumor, and cholesterol-lowering effects.
  • HY-100369A
    DMCM hydrochloride

    GABA Receptor Neurological Disease
    DMCM hydrochloride is a nonselective full inverse agonist of benzodiazepine. DMCM shows bnding afinity at human recombinant GABAA αxβ3γ2 receptor subtypes with Kis of 10 nM, 13 nM, 7.5 nM, 2.2 nM for α1, α2, α3, and α5  receptors, respectively.
  • HY-111326A
    Naphazoline nitrate

    Naphthazoline nitrate

    Adrenergic Receptor TNF Receptor Interleukin Related VEGFR Inflammation/Immunology Cardiovascular Disease
    Naphazoline (Naphthazoline) nitrate is an α-adrenergic receptor agonist. Naphazoline nitrate reduces vascular hyperpermeability and promotes vasoconstriction. Naphazoline nitrate reduces the levels of inflammatory factors (TNF-α, IL-1β and IL-6), cytokines (IFN-γ and IL-4), IgE, GMCSF, and NGF。Naphazoline nitrate can be used for non-bacterial conjunctivitis research.
  • HY-14299A
    Indacaterol maleate

    QAB149

    Adrenergic Receptor Endocrinology
    Indacaterol maleate (QAB149) is an orally active ultra-long-acting β2 adrenergic receptor (ADRB2) agonist. Indacaterol maleate inhibits NF-κB activity in a β-arrestin2-dependent manner, preventing further lung damage and improving lung function in COPD (chronic obstructive pulmonary disorder). Indacaterol maleate can also be used in cardiovascular disease research.
  • HY-108652
    α,β-Methylene ATP trisodium

    P2X Receptor Inflammation/Immunology
    α,β-Methylene ATP trisodium, a phosphonic analog of ATP, is a P2X3 and P2X7 receptor ligand. α,β-Methylene ATP trisodium is a highly selective agonist for P2X1 and P2X3, with practically no activity at P2X2,4-7.
  • HY-134440
    α,β-Methylene-ATP dilithium

    P2X Receptor Inflammation/Immunology
    α,β-Methylene ATP dilithium, a phosphonic analog of ATP, is a P2X3 and P2X7 receptor ligand. α,β-Methylene ATP dilithium is a highly selective agonist for P2X1 and P2X3, with practically no activity at P2X2,4-7.
  • HY-B0203BS
    (rac)-Nebivolol-d8

    Adrenergic Receptor Cardiovascular Disease Endocrinology
    (Rac)-Nebivolol-d8 ((rac)-R 065824-d8) is a labelled racemic Nebivolol. Nebivolol selectively inhibits β1- adrenergic receptor with IC50 of 0.8 nM.
  • HY-121186
    Bevantolol hydrochloride

    Adrenergic Receptor Calcium Channel Metabolic Disease Neurological Disease
    Bevantolol hydrochloride is a selective β1 and α1-adrenergic receptor antagonist with pKi values of 7.83, 6.9 in rat cerebral cortex, respectively. Bevantolol hydrochloride is a potent Ca 2+ antagonist.
  • HY-B1675
    Levalbuterol

    (R)-Albuterol; (R)-Salbutamol; Levosalbutamol

    Adrenergic Receptor Inflammation/Immunology
    Levalbuterol ((R)-Albuterol; (R)-Salbutamol) is a short-acting β2-adrenergic receptor agonist and the active (R)-enantiomer of Salbutamol. Levalbuterol is a more potent bronchodilator than Salbutamol and has the potential for the treatment of COPD.
  • HY-B0203BS1
    (rac)-Nebivolol-d4

    Adrenergic Receptor Cardiovascular Disease Endocrinology
    (Rac)-Nebivolol-d4 ((Rac)-R 065824-d4) is a labelled racemic Nebivolol. Nebivolol selectively inhibits β1- adrenergic receptor with IC50 of 0.8 nM.
  • HY-147699
    FRα-IN-1

    Antifolate Cancer
    FRα-IN-1 (Compound 4) is a tumor-targeting agent. FRα-IN-1 shows selective anticancer activity towards folate receptors (FRα and FRβ) expression cells.
  • HY-B0573S1
    Propranolol-d7 (ring-d7)

    Adrenergic Receptor Neurological Disease Endocrinology
    Propranolol-d7 (ring-d7) is the deuterium labeled Propranolol hydrochloride. Propranolol hydrochloride is a nonselective β-adrenergic receptor (βAR) antagonist, has high affinity for the β1AR and β2AR with Ki values of 1.8 nM and 0.8 nM, respectively. Propranolol hydrochloride inhibits [ 3H]-DHA binding to rat brain membrane preparation with an IC50 of 12 nM. Propranolol hydrochloride is used for study of hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy.
  • HY-14565
    Pozanicline

    ABT-089

    nAChR Neurological Disease
    Pozanicline (ABT-089) selectively activate neuronal nicotinic acetylcholine receptor (nAChR) subtypes, is a novel cholinergic agent that is a partial agonist at α4β2* nAChRs (Ki=16 nM) and shows high selectivity for α6β2* and α4α5β2 nAChR subtypes, the binding affinity (Ki, rat) for Pozanicline to [ 3H] cytisine sites is 16.7 nM. Pozanicline reverses nicotine withdrawal-induced cognitive deficits, may be an effective component of novel therapeutic strategies for nicotine addiction.
  • HY-107684
    3-Bromocytisine

    3-Br-cytisine

    nAChR Neurological Disease
    3-Bromocytisine (3-Br-cytisine) is a potent nACh receptors agonist, with IC50s are 0.28, 0.30 and 31.6 nM for hα4β4, hα4β2, and hα7-nACh, respectively. 3-Bromocytisine (3-Br-cytisine) shows different effects on high (HS) and low (LS) ACh sensitivity α4β2 nAChRs with EC50s are 8 and 50 nM, respectively.
  • HY-B0723S1
    Ospemifene-d4-1

    FC-1271a-d4-1

    Estrogen Receptor/ERR Cancer
    Ospemifene-d4-1 (FC-1271a-d4-1) is the deuterium labeled Ospemifene. Ospemifene is a non-estrogen selective estrogen receptor modulator (SERM), with Kis of 380 and 410 nM for estrogen receptor α (ERα) and ERβ, respectively. Ospemifene can be used for the research of vaginal atrophy and breast cancer.
  • HY-103457
    Y134

    Estrogen Receptor/ERR Cancer
    Y134 is a selective and orally active oestrogen receptor (ER) modulator (SERM), exhibits potent antagonist activity at ERα and ERβ. Y134 shows 121.1-fold selectivity for ERα (Ki=0.09 nM) over ERβ (Ki=11.31 nM). Y134 inhibits oestrogen-stimulated proliferation of ER-positive human breast cancer cells.
  • HY-117378
    N-5984

    KRP-204

    Adrenergic Receptor Cancer Inflammation/Immunology
    N-5984 (KRP-204) is a potent and selective agonist of β3-adrenergic receptor. N-5984 has the potential for developing as one of the clinically effective drugs for obesity and diabetes mellitus.
  • HY-P2197
    ELA-11(human)

    Apelin Receptor (APJ) Inflammation/Immunology
    ELA-11(human), a peptide, is a full agonist of human apelin receptor, with a pKi of 7.85. ELA-11(human) completely inhibits Forskolin-induced cAMP production and stimulates β-arrestin recruitment.
  • HY-B1662
    Hexestrol

    Estrogen Receptor/ERR Endocrinology
    Hexestrol is a nonsteroidal synthetic estrogen, with a Ki of 0.06 and 0.06 nM for estrogen receptor alpha (ERα) and ERβ. Hexestrol can be used for the research of the diseases caused by estrogen deficiencym, and it also can increase the weight of cattle.
  • HY-B1037S
    Salbutamol-d3

    Albuterol-d3; AH-3365-d3

    Adrenergic Receptor Neurological Disease Endocrinology
    Salbutamol-d3 (Albuterol-d3) is the deuterium labeled Salbutamol. Salbutamol is a short-acting β2-adrenergic receptor agonist used for the relief of bronchospasm in conditions such as asthma and chronic obstructive pulmonary disease (COPD).
  • HY-100506
    GLPG0187

    Integrin Cancer
    GLPG0187 is a broad spectrum integrin receptor antagonist with antitumor activity; inhibits αvβ1-integrin with an IC50 of 1.3 nM. GLPG0187 inhibits migrasome biogenesis without cytotoxicity.
  • HY-121383
    Labetalol

    AH5158; Sch-15719W free base

    Adrenergic Receptor Inflammation/Immunology Cardiovascular Disease
    Labetalol (AH5158) is an orally active selective α1- and non-selective β-adrenergic receptors competitive antagonist. Labetalol, an anti-hypertensive agent, can be used for the research of cardiovascular disease, such as hypertension in pregnancy.
  • HY-B1035A
    Levobunolol

    l-Bunolol

    Adrenergic Receptor Others
    Levobunolol (l-Bunolol) is a potent and nonselective β-adrenergic receptor antagonist. Levobunolol is an ocular hypotensive agent and lowers mean intraocular pressure (IOP). Levobunolol can be used for glaucoma and superior oblique myokymia (SOM) research.
  • HY-B1037S2
    Salbutamol-d9

    Albuterol-d9; AH-3365-d9

    Adrenergic Receptor Neurological Disease Endocrinology
    Salbutamol-d9 (Albuterol-d9) is the deuterium labeled Salbutamol. Salbutamol is a short-acting β2-adrenergic receptor agonist used for the relief of bronchospasm in conditions such as asthma and chronic obstructive pulmonary disease (COPD).
  • HY-B1035
    Levobunolol hydrochloride

    l-Bunolol hydrochloride

    Adrenergic Receptor Others
    Levobunolol (l-Bunolol) hydrochloride is a potent and nonselective β-adrenergic receptor antagonist. Levobunolol hydrochloride is an ocular hypotensive agent and lowers mean intraocular pressure (IOP). Levobunolol hydrochloride can be used for glaucoma and superior oblique myokymia (SOM) research.
  • HY-125703
    Ferutinin

    Estrogen Receptor/ERR Apoptosis Cancer Infection Endocrinology Inflammation/Immunology
    Ferutinin, a natural terpenoid compound, is an estrogen receptor ERα agonist and estrogen ERβ-receptor agonist/antagonist with IC50s of 33.1 nM and 180.5 nM, respectively. Ferutinin acts as an electrogenic Ca 2+-ionophore that increases calcium permeability of lipid bilayer membranes, mitochondria. Ferutinin possesses estrogenic, antitumor, antibacterial and antiinflammatory activities.
  • HY-100634
    4-Hydroxypropranolol hydrochloride

    (±)-4-hydroxy Propranolol hydrochloride

    Adrenergic Receptor Neurological Disease
    4-Hydroxypropranolol hydrochlorid is an active metabolite of Propranolol. 4-Hydroxypropranolol hydrochlorid is of comparable potency to Propranolol. 4-Hydroxypropranolol hydrochlorid inhibits β1- and β2-adrenergic receptors with pA2 values of 8.24 and 8.26, respectively. 4-Hydroxypropranolol hydrochlorid has intrinsic sympathomimetic activity, membrane stabilizing activity and potent antioxidant properties.
  • HY-10019
    Varenicline

    CP 526555

    nAChR Inflammation/Immunology Neurological Disease Cancer
    Varenicline (CP 526555) is a potent partial agonist for α4β2 nicotinic acetylcholine receptor (nAChR) with an EC50 value of 2.3 μM. Varenicline is a full agonist for α3β4 and α7 nAChRs with EC50 values of 55 μM and 18 μM, respectively. Varenicline is a nicotinic ligand based on the structure of cytosine, and has the potential for smoking cessation treatment.
  • HY-10019A
    Varenicline dihydrochloride

    CP 526555 dihydrochloride

    nAChR Inflammation/Immunology Neurological Disease
    Varenicline (CP 526555) dihydrochloride is a potent partial agonist for α4β2 nicotinic acetylcholine receptor (nAChR) with an EC50 value of 2.3 μM. Varenicline dihydrochloride is a full agonist for α3β4 and α7 nAChRs with EC50 values of 55 μM and 18 μM, respectively. Varenicline dihydrochloride is a nicotinic ligand based on the structure of cytosine, and has the potential for smoking cessation treatment.
  • HY-N4201
    β-Hydroxyisovalerylshikonin

    EGFR Src Cancer
    Beta-hydroxyisovalerylshikonin is a natural product isolated from Lithospermum erythrorhizon, acts as a potent inhibitor of protein tyrosine kinases (PTK), with IC50s of 0.7μM and 1μM for EGFR and v-Src receptor, respectively. Beta-hydroxyisovalerylshikonin is effective against a wide variety of tumor cell lines, and most efficiently induces cell-death in NCI-H522 and DMS114 cells.
  • HY-Y0313S
    p-Hydroxybenzaldehyde-d4

    Endogenous Metabolite GABA Receptor Neurological Disease
    p-Hydroxybenzaldehyde-d4 is the deuterium labeled p-Hydroxybenzaldehyde. p-Hydroxybenzaldehyde is a one of the major components in Dendrocalamus asper bamboo shoots, with antagonistic effect on GABAA receptor of the α1β2γ2S subtype at high concentrations.
  • HY-N2589
    Isosaponarin

    TGF-β Receptor Others
    Isosaponarin is a flavone glycoside isolated from wasabi leaves. Isosaponarin increases collagen synthesis, caused by up-regulated TGF-β type II receptor (TβR-II) and prolyl 4-hydroxylase (P4H) proteins production.
  • HY-108353
    Isoprenaline

    Adrenergic Receptor Endogenous Metabolite Endocrinology Cardiovascular Disease
    Isoprenaline is a non-selective, orally active β-adrenergic receptor agonist. Isoprenaline has potent peripheral vasodilator, bronchodilator, and cardiac stimulating activities. Isoprenaline can be used for the research of bradycardia and bronchial asthma.
  • HY-111014
    VK-II-36

    Calcium Channel Cardiovascular Disease
    VK-II-36 is a carvedilol analog that suppresses sarcoplasmic reticulum Ca 2+release but does not block the β-receptor.VK-II-36 inhibits triggered activities evoked by both early and delayed after depolarizations.
  • HY-U00449S
    AGN 193109-d7

    RAR/RXR Autophagy Cancer
    AGN 193109-d7 is the deuterium labeled AGN 193109. AGN 193109 is a retinoid analog, and acts as a specific and highly effective antagonist of retinoic acid receptors (RARs), with Kds of 2 nM, 2 nM, and 3 nM for RARα, RARβ, and RARγ, respectively.
  • HY-146561
    S-HP210

    Glucocorticoid Receptor NF-κB Inflammation/Immunology
    S-HP210 is a potent and selective glucocorticoid receptor (GR) with an IC50 value of 1.92 μM for NF-κB transrepression (TR). S-HP210 represses the LPS-induced transcription of a variety of proinflammatory genes such as IL-1β, IL-6 and COX-2. S-HP210 is nontoxic at effective doses against mouse fibroblasts 3T3 cells.
  • HY-10431
    SB-431542

    TGF-β Receptor Apoptosis Cancer
    SB-431542 is a TGF-β receptor kinase inhibitor (TRKI). SB-431542 has inhibitory activity for ALK4, ALK5 and ALK7 with IC50 values of 1 μM, 0.75 μM and 2 μM, respectively. SB-431542 also inhibits TGF-β-induced transcription, gene expression, apoptosis, and growth suppression. SB-431542 can be used for the research of cancer and signal transduction pathways.
  • HY-147660
    IMMH001

    LPL Receptor Inflammation/Immunology
    IMMH001, also called SYL930, is an orally active, potent and selective S1P1 (sphingosine-1-phosphate receptor 1) agonist. IMMH001 decreased levels of both chemokines and proinflammatory cytokines, including IL-1β, IL-5, IL-18, IP10, CCL3, and CCL5. IMMH001 can be used for rheumatoid arthritis (RA) research.
  • HY-119486A
    (Rac)-Tavapadon

    (Rac)-PF-06649751; (Rac)-CVL-751

    Dopamine Receptor Neurological Disease
    (Rac)-Tavapadon ((Rac)-PF-06649751) is a potent and selective noncatechol dopamine D1 receptor agonist. (Rac)-Tavapadon displays potent full agonism in the GS activation assay as well as partial agonism in the β-arrestin2 recruitment assay (GS-cAMP, EC50=0.8 nM; β-arrestin2, EC50=68 nM). (Rac)-Tavapadon has antiparkinsonian activity.
  • HY-P2106
    Elabela(19-32)

    Apelin Receptor (APJ) Cardiovascular Disease
    Elabela(19-32) is an active fragment of ELABELA (ELA) that binds to apelin receptor (APJ). Elabela(19-32) activates the Gαi1 and β-arrestin-2 signaling pathways with EC50s of 8.6 nM and 166 nM. Elabela(19-32) induces receptor internalization and reduces arterial pressure, exerts positive inotropic effects on the heart.
  • HY-14171
    Bexarotene

    LGD1069

    RAR/RXR Autophagy Cancer
    Bexarotene (LGD1069) is a high-affinity and selective retinoid X receptors (RXR) agonist with EC50s of 33, 24, 25 nM for RXRα, RXRβ, and RXRγ, respectively. Bexarotene shows limited affinity for RAR receptors (EC50 >10000 nM). Bexarotene can be used for the research of cutaneous T-cell lymphoma.
  • HY-108675
    PPNDS tetrasodium

    MMP P2X Receptor Cancer Infection
    PPNDS tetrasodium is a selective and competitive meprin β inhibitor (IC50: 80 nM, Ki: 8 nM), and also inhibits ADAM10 (IC50: 1.2 μM). PPNDS tetrasodium is also a P2X1 receptor antagonist. PPNDS is an agonist for the ATP receptor of Paramecium. PPNDS tetrasodium potently inhibits polymerases from viruses. PPNDS tetrasodium can be used in the research of infection and cancers.
  • HY-108353A
    Isoprenaline hemisulfate

    Adrenergic Receptor Endogenous Metabolite Endocrinology Cardiovascular Disease
    Isoprenaline hemisulfate is a non-selective, orally active β-adrenergic receptor agonist. Isoprenaline has potent peripheral vasodilator, bronchodilator, and cardiac stimulating activities. Isoprenaline can be used for the research of bradycardia and bronchial asthma.
  • HY-B0468
    Isoprenaline hydrochloride

    Isoproterenol hydrochloride

    Adrenergic Receptor Endogenous Metabolite Cardiovascular Disease Endocrinology
    Isoprenaline (Isoproterenol) hydrochloride is a non-selective, orally active β-adrenergic receptor agonist. Isoprenaline has potent peripheral vasodilator, bronchodilator, and cardiac stimulating activities. Isoprenaline can be used for the research of bradycardia and bronchial asthma.
  • HY-10432A
    A 83-01 sodium

    TGF-β Receptor Cancer
    A 83-01 sodium is a potent inhibitor of TGF-β type I receptor ALK5 kinase, ALK4 and ALK7, with IC50s of 12 nM, 45 nM and 7.5 nM against the transcription induced by ALK5, ALK4 and ALK7, respectively.
  • HY-113320S
    Etiocholanolone-d5

    GABA Receptor Endogenous Metabolite Neurological Disease
    Etiocholanolone-d5 is the deuterium labeled Etiocholanolone. Etiocholanolone (5β-Androsterone) is the excreted metabolite of testosterone and has anticonvulsant activity. Etiocholanolone is a less potent neurosteroid positive allosteric modulator (PAM) of the GABAAreceptor than its enantiomer form.
  • HY-145600
    Tegileridine

    Opioid Receptor Neurological Disease
    Tegileridine is the potent agonist of opioid receptor (MOR). Tegileridine is an oxa spiro derivative which reduces the side effects mediated by β-arrestin. Tegileridine has the potential for the research of pains and pains-related diseases (extracted from patent WO2017063509A1).
  • HY-N0366
    Sennoside B

    PDGFR Cancer
    Sennoside B is an anthraquinone glycoside, found in large quantities in leaves and pods of Senna (Cassia angustifolia). Sennoside B can inhibit PDGF-stimulated cell proliferation by binding to PDGF-BB and its receptor and by down-regulating the PDGFR-beta signaling pathway.
  • HY-103021
    LY3200882

    TGF-β Receptor Cancer Inflammation/Immunology
    LY3200882 is a potent, highly selective, ATP-competitive and orally active TGF-β receptor type 1 (ALK5) inhibitor with an IC50 of 38.2 nM. LY3200882 inhibits various pro-tumorigenic activities and is also used as an immune modulatory agent.
  • HY-103454B
    MPP hydrochloride

    Estrogen Receptor/ERR Apoptosis Cancer
    MPP hydrochloride is a potent and selective ER (estrogen receptor) modulator. MPP hydrochloride induces significant apoptosis in the endometrial cancer and oLE cell lines. MPP hydrochloride reverses the positive effects of beta-estradiol. MPP hydrochloride has mixed agonist/antagonist action on murine uterine ERalpha in vivo.
  • HY-P2106A
    Elabela(19-32) TFA

    Apelin Receptor (APJ) Cardiovascular Disease
    Elabela(19-32) TFA is an active fragment of ELABELA (ELA) that binds to apelin receptor (APJ). Elabela(19-32) TFA activates the Gαi1 and β-arrestin-2 signaling pathways with EC50s of 8.6 nM and 166 nM. Elabela(19-32) TFA induces receptor internalization and reduces arterial pressure, exerts positive inotropic effects on the heart.
  • HY-137862
    1-Oleoyl lysophosphatidic acid

    1-Oleoyl-sn-glycero-3-phosphate; 1-Oleoyl-LPA

    LPL Receptor Neurological Disease
    1-Oleoyl lysophosphatidic acid (1-Oleoyl-sn-glycero-3-phosphate) is an abundant lysophosphatidic acid (LPA) species with high biological activity due to its strong affinity for the LPA receptors. 1-Oleoyl lysophosphatidic acid is commonly used in most laboratories as a reagent for LPA receptor activation. 1-Oleoyl lysophosphatidic acid increases SRE-driven β-galactosidase activity.
  • HY-P0198B
    [D-Arg25]-Neuropeptide Y (human)

    Neuropeptide Y Receptor Metabolic Disease Neurological Disease
    [D-Arg25]-Neuropeptide Y (human) ([D-Arg25] NPY) is a Y1 receptor selective agonist. Neuropeptide Y (human) is involved in Alzheimer's disease (AD) and protects rat cortical neurons against β-Amyloid toxicity.
  • HY-P1107A
    Antisauvagine-30 TFA

    aSvg-30 TFA

    CRFR Neurological Disease
    Antisauvagine-30 TFA (aSvg-30 TFA) is a potent, highly selective and competitive CRF2 receptor peptidic antagonist. Antisauvagine-30 TFA exhibits a Kd of 1.4 nM and 150 nM for mCRFR2β and CRFR1, respectively.
  • HY-113320S1
    Etiocholanolone-d2

    5β-Androsterone-d2

    GABA Receptor Endogenous Metabolite
    Etiocholanolone-d2 is the deuterium labeled Etiocholanolone. Etiocholanolone (5β-Androsterone) is the excreted metabolite of testosterone and has anticonvulsant activity. Etiocholanolone is a less potent neurosteroid positive allosteric modulator (PAM) of the GABAA receptor than its enantiomer form.
  • HY-Y0313S1
    p-Hydroxybenzaldehyde-13C

    Endogenous Metabolite GABA Receptor Neurological Disease
    p-Hydroxybenzaldehyde-13C is the 13C-labeled p-Hydroxybenzaldehyde. p-Hydroxybenzaldehyde is a one of the major components in Dendrocalamus asper bamboo shoots, with antagonistic effect on GABAA receptor of the α1β2γ2S subtype at high concentrations.
  • HY-10019S
    Varenicline-d4

    CP 526555-d4

    nAChR Neurological Disease
    Varenicline-d4 is deuterium labeled Varenicline. Varenicline (CP 526555) is a potent partial agonist for α4β2 nicotinic acetylcholine receptor (nAChR) with an EC50 value of 2.3 μM. Varenicline is a full agonist for α3β4 and α7 nAChRs with EC50 values of 55 μM and 18 μM, respectively. Varenicline is a nicotinic ligand based on the structure of cytisine, has the potential for smoking cessation treatment.
  • HY-114263
    NXT629

    PPAR Cancer
    NXT629 is a potent, selective, and competitive PPAR-α antagonist, with an IC50 of 77 nM for human PPARα, shows high selectivity over other nuclear hormone receptor, such as PPARδ, PPARγ, ERβ, GR and TRβ, IC50s are 6.0, 15, 15.2, 32.5 and >100 μM, respectively. NXT629 has potent anti-tumor activity and inhibits experimental metastasis of cancer cell in animal models.
  • HY-N2326
    (±)-Anatoxin A fumarate

    nAChR Neurological Disease
    (±)-Anatoxin A fumarate is a natural alkaloid isolated from freshwater cyanobacterium.(±)-Anatoxin A fumarate is a potent nicotinic receptor agonist and exhibits Ki values of 1.25 nM and 1.84 μM for binding to putative α4β2-type nAChR and α7-type nAChR in rat brain membranes, respectively. (±)-Anatoxin A fumarate stimulates [ 3H]-dopamine release from rat striatal synaptosomes (EC50=134 nM).
  • HY-151129
    nAChR-IN-1

    2,2,6,6-Tetramethylpiperidin-4-yl heptanoate

    nAChR Neurological Disease
    nAChR-IN-1 (2,2,6,6-Tetramethylpiperidin-4-yl heptanoate) is a tetramethylpiperidine heptanoate, a selective nicotinic acetylcholine receptor (nAChR) inhibitor that inhibits nAChRs lacking α5, α6, or β3 subunits. nAChR-IN-1 has the effect of preventing nerve disorder, can be used for nicotinic acetylcholine receptor dysfunction or neurological disorders research.
  • HY-123489
    3α,21-Dihydroxy-5α-pregnan-20-one

    THDOC

    GABA Receptor Neurological Disease
    3α,21-Dihydroxy-5α-pregnan-20-one (THDOC), an endogenous neurosteroid, is a positive modulator of GABAA receptors. 3α,21-Dihydroxy-5α-pregnan-20-one potentiates neuronal response to low concentrations of GABA at α4β1δ GABAA receptors in vitro.
  • HY-122304
    Adrenaline sulfate

    Endogenous Metabolite Adrenergic Receptor Endocrinology Neurological Disease
    Adrenaline sulfate is a orally active hormone secreted by the medulla of the adrenal glands. Adrenaline sulfate is an α-adrenergic and β-adrenergic receptor agonist. Adrenaline sulfate can be used in the treatment of anaphylaxis. Adrenaline sulfate has the potential for the research of cardiac arrest.
  • HY-103454
    MPP dihydrochloride

    Estrogen Receptor/ERR Apoptosis Cancer
    MPP dihydrochloride is a potent and selective ER (estrogen receptor) modulator. MPP dihydrochloride induces significant apoptosis in the endometrial cancer and oLE cell lines. MPP dihydrochloride reverses the positive effects of beta-estradiol. MPP dihydrochloride has mixed agonist/antagonist action on murine uterine ERalpha in vivo.
  • HY-N7715
    Ferulic acid acyl-β-D-glucoside

    Ferulic acid glucoside

    Drug Metabolite Others
    Ferulic acid acyl-β-D-glucoside is a metabolite of Ferulic Acid (HY-N0060). Ferulic acid is a novel fibroblast growth factor receptor 1 (FGFR1) inhibitor with IC50s of 3.78 and 12.5 μM for FGFR1 and FGFR2, respectively.
  • HY-B0151S2
    Pregnenolone-d4-1

    3β-Hydroxy-5-pregnen-20-one-d4-1

    Cannabinoid Receptor TRP Channel Endogenous Metabolite Autophagy Neurological Disease
    Pregnenolone-d4-1 (3β-Hydroxy-5-pregnen-20-one-d4-1) is the deuterium labeled Pregnenolone. Pregnenolone (3β-Hydroxy-5-pregnen-20-one) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone can protect the brain from cannabis intoxication. Pregnenolone is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels.
  • HY-135581
    Raloxifene 6-glucuronide

    Estrogen Receptor/ERR Endocrinology
    Raloxifene 6-glucuronide is a primary metabolite of Raloxifene. Raloxifene 6-glucuronide is mediated mostly by UGT1A1 and UGT1A8. Raloxifene 6-glucuronide binds to estrogen receptor with an IC50 of 290 μM. Raloxifene is a selective and nonsteroidal estrogen receptor modulator. Raloxifene activates TGFβ3 promoter as a full agonist at nanomolar concentrations, and inhibits the estrogen response element-containing vitellogenin promoter expression.
  • HY-118140
    ZCZ011

    Cannabinoid Receptor Inflammation/Immunology Neurological Disease
    ZCZ011 is a potent and brain penetrant cannabinoid 1 (CB1) receptor positive allosteric modulator. ZCZ011 potentiates binding of CP55,940 to the CB1 receptor, enhances anandamide (AEA)-stimulated GTPγS binding in mouse brain membranes. ZCZ011 increases β-arrestin recruitment and ERK phosphorylation in hCB1 cells. ZCZ011 can be used for researching neuropathic and inflammatory pain.
  • HY-101170
    BU224 hydrochloride

    Imidazoline Receptor Apoptosis TNF Receptor Inflammation/Immunology Neurological Disease
    BU224 hydrochloride is a selective and high affinity imidazoline I2 receptor ligand, with a Ki of 2.1 nM. BU224 hydrochloride is sometimes used as an I2 receptor antagonist. BU224 hydrochloride exerts neuroprotective effects, with anti-inflammatory and anti-apoptotic properties. BU224 hydrochloride improves memory in 5XFAD mice, enlarging dendritic spines and reducing Aβ-induced changes in NMDARs. BU224 hydrochloride can be used for Alzheimer's disease research.
  • HY-116553
    FzM1

    Wnt β-catenin Cancer
    FzM1 is a negative allosteric modulator (NAM) of Frizzled receptor FZD4. FzM1 reduces WNT5A-dependent WNT responsive element (WRE) activity (log EC50inh=−6.2). FzM1 binds to an allosteric binding site located in intracellular loop 3 (ICL3) of FZD4 and alters the conformation of the receptor, ultimately inhibiting the WNT/β-catenin cascade.
  • HY-135582
    Raloxifene 4'-glucuronide

    Estrogen Receptor/ERR Endocrinology
    Raloxifene 4'-glucuronide is a primary metabolite of Raloxifene. Raloxifene 4'-glucuronide formation is mediated mostly by UGT1A10 and UGT1A8. Raloxifene 4'-glucuronide binds to estrogen receptor with an IC50 of 370 μM. . Raloxifene is a selective estrogen receptor modulator. Raloxifene activates TGFβ3 promoter as a full agonist at nanomolar concentrations, and inhibits the estrogen response element-containing vitellogenin promoter expression.
  • HY-110302
    6'-GNTI dihydrochloride

    Opioid Receptor Neurological Disease
    6'-GNTI dihydrochloride, a κ-opioid receptor (KOR) agonist, displays bias toward the activation of G protein-mediated signaling over β-arrestin2 recruitment. 6'-GNTI 6'-GNTI dihydrochloride only activates the Akt pathway in striatal neurons.
  • HY-126236
    3,5-Diiodothyropropionic acid

    Thyroid Hormone Receptor Cardiovascular Disease Endocrinology
    3,5-Diiodothyropropionic acid is a thyroid hormone analog, induces α-myosin heavy chain mRNA expression, binds to thyroid hormone receptor (TR), with Ka of 2.40 and 4.06 M -1 for TRα1 and TRβ1, respectively.
  • HY-138879
    CP-601927

    nAChR Neurological Disease
    CP-601927 is a selective α4β2 nicotinic acetylcholine receptor (nAChR) partial agonist (Ki=1.2 nM; EC50=2.6 μM). CP-601927 shows good brain penetration and antidepressant-like properties.
  • HY-P2249
    ELA-21 (human)

    Apelin Receptor (APJ) Cardiovascular Disease
    ELA-21 (human) is an apelin receptor agonist with a pKi of 8.52. ELA-21 (human) completely inhibits Forskolin-induced cAMP production and stimulates β-arrestin recruitment with subnanomolar potencies. ELA-21 (human) is an agonist in G-protein-dependent and -independent pathways.
  • HY-B0804
    Nadolol

    SQ-11725

    Adrenergic Receptor Cardiovascular Disease
    Nadolol (SQ-11725) is a non-selective and orally active β-adrenergic receptors blocker and is a substrate of organic anion transporting polypeptide 1A2 (OATP1A2). Nadolol has the the potential for high blood pressure, angina pectoris and vascular headaches research.
  • HY-10255A
    Sunitinib

    SU 11248

    VEGFR PDGFR IRE1 Mitophagy Autophagy Apoptosis Cancer
    Sunitinib (SU 11248) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively. Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation.
  • HY-100634S
    4-Hydroxypropranolol-d7 hydrochloride

    (±)-4-Hydroxy Propranolol-d7 hydrochloride

    Adrenergic Receptor Neurological Disease
    4-Hydroxypropranolol D7 hydrochloride ((±)-4-hydroxy Propranolol D7 hydrochloride) is a deuterium labeled 4-Hydroxypropranolol hydrochloride. 4-Hydroxypropranolol hydrochlorid is an active metabolite of Propranolol, with potency comparable to Propranolol. 4-Hydroxypropranolol hydrochlorid inhibits β1- and β2-adrenergic receptors with pA2 values of 8.24 and 8.26, respectively. 4-Hydroxypropranolol hydrochlorid has intrinsic sympathomimetic activity, membrane stabilizing activity and potent antioxidant properties.
  • HY-137976
    Penehyclidine hydrochloride

    Penequinine hydrochloride

    mAChR NF-κB Inflammation/Immunology
    Penehyclidine (Penequinine) hydrochloride, a anticholinergic drug, is a selective antagonist of M1 and M3 receptors. Penehyclidine hydrochloride activates NF-kβ in lung tissue and inhibits the release of inflammatory factors. Penehyclidine hydrochloride can alleviate the pulmonary inflammatory response in rats with chronic obstructive pulmonary disease (COPD) undergoing mechanical ventilation.
  • HY-142119
    Penehyclidine

    mAChR NF-κB Inflammation/Immunology
    Penehyclidine, a anticholinergic agent, is a selective antagonist of M1 and M3 receptors. Penehyclidine activates NF-kβ in lung tissue and inhibits the release of inflammatory factors. Penehyclidine can alleviate the pulmonary inflammatory response in rats with chronic obstructive pulmonary disease (COPD) undergoing mechanical ventilation.
  • HY-10431G
    SB-431542

    TGF-β Receptor Cancer Neurological Disease
    SB-431542 (GMP) is SB-431542 (HY-10431) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. SB-431542 is a TGF-β receptor kinase inhibitor (TRKI) in SMAD signaling.
  • HY-B1481A
    Isoetharine

    Isoetarine

    Adrenergic Receptor Inflammation/Immunology Cardiovascular Disease
    Isoetharine (Isoetarine) is an orally active selective agonist of β-adrenergic receptors. Isoetharine is a catechol-like drug and catechol O-methyltransferase (COMT) mediates its methylation. Isoetharine can promote the production of cAMP which stimulates the relaxation of smooth muscle cells and can be used as an emphysema, bronchitis and bronchodilator.
  • HY-B0316S
    Avobenzone-13C,d3

    Estrogen Receptor/ERR Apoptosis Others
    Avobenzone-13C,d3 is the 13C- and deuterium labeled Avobenzone. Avobenzone, a dibenzoylmethane compound, is one of the most widely used filters in sunscreens for skin photoprotection in the UVA band. Avobenzone is an endocrine disruptor that directly binds to estrogen receptor β and acts as an estrogen agonist.
  • HY-B1481
    Isoetharine mesylate

    Isoetarine mesylate

    Adrenergic Receptor Inflammation/Immunology Cardiovascular Disease
    Isoetharine (Isoetarine) mesylate is an orally active selective agonist of β-adrenergic receptors. Isoetharine mesylate is a catechol-like drug and catechol O-methyltransferase (COMT) mediates its methylation. Isoetharine mesylate can promote the production of cAMP which stimulates the relaxation of smooth muscle cells and can be used as an emphysema, bronchitis and bronchodilator.
  • HY-B1517A
    Alprenolol hydrochloride

    (RS)-Alprenolol hydrochloride; dl-Alprenolol hydrochloride

    5-HT Receptor Cancer
    Alprenolol ((RS)-Alprenolol; dl-Alprenolol) hydrochloride is an orally active non-selective β-adrenoceptor antagonist and an antagonist of 5-HT1A and 5-HT1B receptors. Alprenolol hydrochloride is used as an anti-hypertensive, anti-anginal and anti-arrhythmic agent.
  • HY-108847
    Etanercept

    TNF Receptor Bacterial Inflammation/Immunology Cancer
    Etanercept, a dimeric fusion protein that binds TNF, acts as a TNF inhibitor. Etanercept competitively inhibits the binding of both TNF-α and TNF-β to cell surface TNF receptors, rendering TNF biologically inactive. Etanercept shows efficacy against rheumatoid arthritis, juvenile idiopathic arthritis, and plaque psoriasis.
  • HY-12753A
    Debutyldronedarone hydrochloride

    SR35021 hydrochloride

    Thyroid Hormone Receptor Cardiovascular Disease
    Debutyldronedarone (SR35021) hydrochloride, the main metabolite of Dronedarone, is a selective thyroid hormone receptor α1 (TRα1) inhibitor. Debutyldronedarone hydrochloride inhibits T3 binding to TRα1 and TRβ1 by 77% and 25%, respectively. Debutyldronedarone hydrochloride can be used for the research of arrhythmic.
  • HY-116790
    (-)-Penbutolol

    (S)-Penbutolol; (-)-Isopenbutolol

    Adrenergic Receptor 5-HT Receptor Endocrinology Neurological Disease
    (-)-Penbutolol ((S)-Penbutolol) is a potent β-adrenoceptor and 5-HT receptor antagonist with Ki values of 11.6 nM and 11.9 nM for 5-HT in rat cornu ammonis 1 (CA1) and human CA3. (-)-Penbutolol can increase hippocampal 5-HT output.
  • HY-P1072
    PHM-27 (human)

    CGRP Receptor Metabolic Disease Cardiovascular Disease
    PHM-27 (human) is a human prepro-vasoactive intestinal polypeptide (27 amino acid). PHM-27 (human) is a potent the human calcitonin receptor agonist with an EC50 of 11 nM. PHM-27 (human) efficiently enhances glucose-induced insulin secretion from beta cells by an autocrine mechanism.
  • HY-10255
    Sunitinib Malate

    SU 11248 Malate

    PDGFR VEGFR IRE1 Mitophagy Autophagy Apoptosis Cancer
    Sunitinib Malate (SU 11248 Malate) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively. Sunitinib Malate, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation.
  • HY-B1517
    Alprenolol

    (RS)-Alprenolol; dl-Alprenolol

    5-HT Receptor Cancer
    Alprenolol ((RS)-Alprenolol; dl-Alprenolol) is an orally active non-selective β-adrenoceptor antagonist and an antagonist of 5-HT1A and 5-HT1B receptors. Alprenolol is used as an anti-hypertensive, anti-anginal and anti-arrhythmic agent.
  • HY-123984
    LTβR-IN-1

    Others Metabolic Disease
    LTβR-IN-1 is a potent, selective lymphotoxin β receptor (LTβR) inhibitor with an IC50 of 10 μM. LTβR-IN-1 is potent in TWEAK-stimulated p52 translocation assays with an IC50 of 10 μM and did not alter TNF-α–induced p65 nuclear translocation.
  • HY-10473
    Eprotirome

    KB2115

    Thyroid Hormone Receptor Endocrinology Metabolic Disease
    Eprotirome (KB2115) is a liver-selective thyroid hormone receptor (TR) agonist. KB2115 has modestly higher affinity for TRβ than for TRα. Eprotirome reduces low-density lipoprotein (LDL) cholesterol concentrations. Eprotirome can be used for dyslipidemias and obesity research.
  • HY-15340
    LG100268

    LG268

    RAR/RXR Autophagy Metabolic Disease
    LG100268 (LG268) is a potent, selective and orally active retinoid X receptor (RXR) agonist with EC50 values of 4 nM, 3 nM, and 4 nM for RXR-α, RXR-β, and RXR-γ, respectively. LG100268 displays >1000-fold selectivity for RXR over RAR, the Ki values are 3.4 nM, 6.2 nM and 9.2 nM for RXR-α, RXR-β, and RXR-γ, respectively. LG100268 activates RXR homodimers to induce transcriptional activation. LG100268 can be used for the study of lung carcinogenesisy.
  • HY-10330
    Toceranib

    SU11654; PHA 291639E

    PDGFR VEGFR c-Kit Cancer
    Toceranib phosphate (SU11654 phosphate) is an orally active receptor tyrosine kinase (RTK) inhibitor, and it potently inhibits PDGFR, VEGFR, and Kit with Kis of 5 and 6 nM for PDGFRβ and Flk-1/KDR, respectively. Toceranib phosphate (SU11654 phosphate) has antitumor and antiangiogenic activity, and used in the treatment of canine mast cell tumors.
  • HY-144653
    PDGFR-IN-1

    PDGFR Apoptosis Cancer
    PDGFR-IN-1 (compound 7m) is a potent and orally active PDGFR (platelet-derived growth factor receptor) inhibitor, with IC50 values of 2.4 and 0.9 nM for PDGFRα and PDGFRβ, respectively. PDGFR-IN-1 displays robust antitumor effects and low toxicity, and can be used to study osteosarcoma.
  • HY-P2197A
    ELA-11(human) TFA

    Apelin Receptor (APJ)
    ELA-11(human) TFA is a high affinity apelin receptor agonist (Ki=14 nM). ELA-11(human) TFA is a bioactive fragment of ELA-32. ELA-11(human) TFA inhibits forskolin-induced cAMP production and stimulates β-arrestin recruitment in vitro.
  • HY-P2264
    KYL peptide

    Ephrin Receptor Inflammation/Immunology
    KYL peptide, an antagonistic peptide, selectively targets EphA4 receptor. KYL peptide binds to the ligand-binding domain of EphA4, effectively alleviates Aβ-induced synaptic dysfunction and synaptic plasticity defects in AD mice. KYL peptide can promote nerve regeneration after injury and modulating immune responses.
  • HY-10330A
    Toceranib phosphate

    SU11654 phosphate; PHA 291639E phosphate

    PDGFR VEGFR c-Kit Cancer
    Toceranib phosphate (SU11654 phosphate) is an orally active receptor tyrosine kinase (RTK) inhibitor, and it potently inhibits PDGFR, VEGFR, and Kit with Kis of 5 and 6 nM for PDGFRβ and Flk-1/KDR, respectively. Toceranib phosphate (SU11654 phosphate) has antitumor and antiangiogenic activity, and used in the treatment of canine mast cell tumors .
  • HY-146780
    TGFβRI-IN-4

    TGF-β Receptor Cancer
    TGFβRI-IN-4 is a highly potent and orally active TGFβ receptor type I (TGFβRI) inhibitor, with IC50s of 44 nM and 42.5 nM for ALK5 and NIH3T3. TGFβRI-IN-4 can suppress tumor growth and tumor weight in tumor xenograft model.
  • HY-W063968
    RO8191

    CDM-3008; RO4948191

    IFNAR JAK STAT HCV HBV Infection
    RO8191 (CDM-3008), an imidazonaphthyridine compound, is an orally active and potent interferon (IFN) receptor agonist. RO8191 directly binds to IFNα/β receptor 2 (IFNAR2) and activates IFN-stimulated genes (ISGs) expression and JAK/STAT phosphorylation. RO8191 shows antiviral activity against both HCV and EMCV with an IC50 of 200 nM for HCV replicon. RO8191 is a cccDNA modulator (CDM) through interferon-like activity and has anti-HBV activity.
  • HY-14171S1
    Bexarotene-d3

    RAR/RXR Autophagy Cancer
    Bexarotene-d3 (LGD1069-d3) is the deuterium labeled Bexarotene. Bexarotene (LGD1069) is a high-affinity and selective retinoid X receptors (RXR) agonist with EC50s of 33, 24, 25 nM for RXRα, RXRβ, and RXRγ, respectively. Bexarotene shows limited affinity for RAR receptors (EC50 >10000 nM). Bexarotene can be used for the research of cutaneous T-cell lymphoma.
  • HY-B0151
    Pregnenolone

    3β-Hydroxy-5-pregnen-20-one

    Cannabinoid Receptor TRP Channel Endogenous Metabolite Autophagy Neurological Disease
    Pregnenolone (3β-Hydroxy-5-pregnen-20-one) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone can protect the brain from cannabis intoxication. Pregnenolone is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels.
  • HY-100991
    FG 7142

    ZK 39106; LSU-65

    GABA Receptor Neurological Disease
    FG 7142 (ZK 39106; LSU-65), a non-selectively benzodiazepine inverse agonist, has high affinity for the α1 subunit-containing GABAA receptor (Ki=91 nM). FG 7142 (ZK 39106; LSU-65) also modulates GABA-induced chloride flux at GABAA receptors expressing the α1 subunit (EC50= 137 nM). FG 7142 (ZK 39106; LSU-65) can increase tyrosine hydroxylation and cause upregulation of β-adrenoceptors in mouse cerebral cortex.
  • HY-100634SA
    4-Hydroxypropranolol-d7

    (±)-4-Hydroxy Propranolol-d7

    Adrenergic Receptor Neurological Disease
    4-Hydroxypropranolol-d7 ((±)-4-Hydroxy Propranolol-d7) is the deuterium labeled 4-Hydroxypropranolol hydrochloride. 4-Hydroxypropranolol hydrochlorid is an active metabolite of Propranolol. 4-Hydroxypropranolol hydrochlorid is of comparable potency to Propranolol. 4-Hydroxypropranolol hydrochlorid inhibits β1- and β2-adrenergic receptors with pA2 values of 8.24 and 8.26, respectively. 4-Hydroxypropranolol hydrochlorid has intrinsic sympathomimetic activity, membrane stabilizing activity and potent antioxidant properties.
  • HY-19744
    T6167923

    MyD88 Inflammation/Immunology
    T6167923 is a selective inhibitor of MyD88-dependent signaling pathways. T6167923 directly binds to Toll/IL1 receptor (TIR) domain of MyD88 and disrupts MyD88 homodimeric formation. T6167923 inhibits NF-κB driven Staphylococcus enterotoxin AP (SEAP) activity, and improves anti-inflammatory activity with IC50s of 2.7  μM, 2.9 μM, 2.66 μM and 2.66 μM for IFN-γ, IL-1β, IL-6 and TNF-α, respectively.
  • HY-150741
    ODN 2216

    Toll-like Receptor (TLR) IFNAR Interleukin Related Cancer Infection Inflammation/Immunology
    ODN 2216 is a TLR9 (toll-like receptor 9) ligand or agonist. ODN 2216 induces high amounts of IFN-α and IFN-β. ODN 2216 induces IFN-α by pDC (plasmacytoid DC) and IL-12 (p40) production by DC (dendritic cells). ODN 2216 stimulates IFN-γ production in peripheral blood mononuclear cells (PBMC), which is indirect and mediated by IFN-α/β. ODN 2216 can activate NK cells and promote IFN-γ production of TCR-triggered CD4 + T cells.
  • HY-N10403
    4-Hydroxyestradiol

    4-Hydroxy-17β-estradiol

    Drug Metabolite Endogenous Metabolite Cancer
    4-Hydroxyestradiol (4-Hydroxy-17β-estradiol) is an endogenous metabolite of Estradiol (HY-B0141). 4-Hydroxyestradiol is carcinogenic and shows mutagenic activity in breast epithelial cells. 4-Hydroxyestradiol inhibits the binding of Estradiol to the estrogen receptor in a competitive manner, with a Ki of 0.48 nM.
  • HY-107397
    Ch55

    RAR/RXR Cancer
    Ch55 is a potent synthetic retinoid. Ch55 binds to RAR-α and RAR-β receptors with high affinity. Ch55 displays low affinity for cellular retinoic acid binding protein (CRABP). Ch55 is a potent inducer of the differentiation of HL60 cells with an EC50 of 200 nM. Ch55 can be used for cancer research.
  • HY-B0203B
    (Rac)-Nebivolol

    (Rac)-R 065824

    Adrenergic Receptor NADPH Oxidase Cardiovascular Disease
    (Rac)-Nebivolol ((Rac)-R 065824) is a racemic isomer of Nebivolol. Nebivolol is a selective β1-adrenergic receptor antagonist with an IC50 value of 0.8 nM. Nebivolol can prevent up-regulation of Nox2/NADPH oxidase and lipoperoxidation in the early stages of ethanol-induced cardiac toxicity. Vasodilatory activity.
  • HY-10407G
    SU 5402

    VEGFR EGFR PDGFR Cancer
    SU 5402 (GMP) is SU 5402 (HY-10407) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. SU 5402 is a potent multi-targeted receptor tyrosine kinase inhibitor with IC50 of 20 nM, 30 nM, and 510 nM for VEGFR2, FGFR1, and PDGFRβ, respectively.
  • HY-W012123
    3,4,5-Trimethoxycinnamic acid

    GABA Receptor Endogenous Metabolite Neurological Disease
    3,4,5-Trimethoxycinnamic acid is a phenylpropanoid isolated from the roots of Polygala tenuifolia WILLD, with anti-stress effect, prolonging the sleeping time in animals. 3,4,5-Trimethoxycinnamic acid increases expression of GAD65 and γ-subunit of GABAA receptor, but shows no effect on the amounts of α-, β-subunits.
  • HY-P1119
    WRW4

    Formyl Peptide Receptor (FPR) Neurological Disease
    WRW4, a specific formyl peptide receptor-like 1 (FPRL1) antagonist, inhibits WKYMVm binding to FPRL1 with an IC50 of 0.23 μM. WRW4 specifically inhibits the increase in intracellular calcium by the FPRL1 agonists MMK-1, amyloid beta42 (Abeta42) peptide, and F peptide.
  • HY-14653
    Amsilarotene

    TAC-101; Am 555S

    RAR/RXR Apoptosis Cancer
    Amsilarotene (TAC-101; Am 555S), an orally active synthetic retinoid, has selective affinity for retinoic acid receptor α (RAR-α) binding with Ki of 2.4, 400 nM for RAR-α and RAR-β. Amsilarotene induces the apoptotic of human gastric cancer, hepatocellular carcinoma and ovarian carcinoma cells. Amsilarotene can be used for the research of cancer.
  • HY-124270
    Sibenadet hydrochloride

    AR-C68397AA

    Dopamine Receptor Adrenergic Receptor Inflammation/Immunology
    Sibenadet hydrochloride (AR-C68397AA) is a dual D2 dopamine receptor, beta2-adrenoceptor agonist with bronchodilator activity. Investigation in animal models of key chronic obstructive pulmonary disease (COPD) symptoms has demonstrated that Sibenadet hydrochloride effectively inhibits sensory nerve activity, thereby reducing reflex cough, mucus production and tachypnoea.
  • HY-10331
    Regorafenib

    BAY 73-4506

    VEGFR Autophagy PDGFR Raf RET c-Kit FGFR Cancer
    Regorafenib (BAY 73-4506) is an orally active and potent multi-targeted receptor tyrosine kinase inhibitor, with IC50 values of 13/4.2/46, 22, 7, 1.5 and 2.5 nM for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1, respectively. Regorafenib shows very robust antitumor and antiangiogenic activity.
  • HY-107676
    SIB-1553A

    nAChR Neurological Disease
    SIB-1553A is an orally bioavailable nicotinic acetylcholine receptors (nAChRs) agonist, with selectivity for β4 subunit-containing nAChRs. SIB-1553A is also a selective neuronal nAChR ligand. SIB-1553A is a cognitive enhancer, and has therapeutic potential for the symptomatic treatment of Alzheimer’s disease and other cognitive disorders.
  • HY-14930A
    Mirodenafil dihydrochloride

    SK-3530 dihydrochloride

    Phosphodiesterase (PDE) Glucocorticoid Receptor Wnt β-catenin Apoptosis Endocrinology Inflammation/Immunology Neurological Disease
    Mirodenafil (SK3530) dihydrochloride is an orally active, potent, reversible, and selective phosphodiesterase 5 (PDE5) inhibitor. Mirodenafil dihydrochloride is a glucocorticoid receptor (GR) modulator Mirodenafil dihydrochloride activates the Wnt/β-catenin signaling pathway by downregulating Dkk1 expression. Mirodenafil dihydrochloride can be used for the research of erectile dysfunction (ED), Alzheimer’s disease (AD) and systemic sclerosis (SSc).
  • HY-14930
    Mirodenafil

    SK3530

    Phosphodiesterase (PDE) Glucocorticoid Receptor Wnt β-catenin Apoptosis Endocrinology Inflammation/Immunology Neurological Disease
    Mirodenafil (SK3530) is an orally active, potent, reversible, and selective phosphodiesterase 5 (PDE5) inhibitor. Mirodenafil is a glucocorticoid receptor (GR) modulator Mirodenafil activates the Wnt/β-catenin signaling pathway by downregulating Dkk1 expression. Mirodenafil can be used for the research of erectile dysfunction (ED), Alzheimer’s disease (AD) and systemic sclerosis (SSc).
  • HY-10331B
    Regorafenib mesylate

    BAY 73-4506 mesylate

    VEGFR PDGFR RET Raf c-Kit FGFR Autophagy Cancer
    Regorafenib (BAY 73-4506) mesylate is an orally active and potent multi-targeted receptor tyrosine kinase inhibitor, with IC50 values of 13/4.2/46, 22, 7, 1.5 and 2.5 nM for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1, respectively. Regorafenib mesylate shows very robust antitumor and antiangiogenic activity.
  • HY-120087
    KG-548

    HIF/HIF Prolyl-Hydroxylase Cancer
    KG-548 is an ARNT/TACC3 disruptor and a HIF-1α inhibitor. KG-548 directly interferes with ARNT/TACC3 complex formation by competing with TACC3 for binding to the ARNT PAS-B domain. ARNT is the aryl hydrocarbon receptor nuclear translocator, also known as HIF-β.
  • HY-N6052
    (+)-Medicarpin

    Estrogen Receptor/ERR Cancer
    (+)-Medicarpin, a pterocarpan, is a type of isoflavonoid isolated from several medicinal plant species with various biological effects, including Sophora japonica, Zollernia paraensis and Platymiscium yucatamun, Machaerium aristulatum, Platymiscium floribundum, and so on. (+)-Medicarpin potently inhibits osteoclastogenesis and promotes bone healing and increases bone mass by osteoblast differentiation with estrogen receptor (ER) β-mediated osteogenic action.
  • HY-W008634
    Bropirimine

    Toll-like Receptor (TLR) Cancer
    Bropirimine is a synthetic agonist for toll-like receptor 7 (TLR7). Bropirimine inhibits differentiation of osteoclast precursor cells into osteoclasts via TLR7-mediated production of IFN-β. Bropirimine is an orally active immunomodulator that has demonstrated anticancer activity in transitional cell carcinoma in situ (CIS) in both the bladder and upper urinary tract.
  • HY-10331A
    Regorafenib monohydrate

    BAY 73-4506 monohydrate

    VEGFR Autophagy PDGFR Raf RET FGFR c-Kit Cancer
    Regorafenib (BAY 73-4506) monohydrate is an orally active and potent multi-targeted receptor tyrosine kinase inhibitor, with IC50 values of 13/4.2/46, 22, 7, 1.5 and 2.5 nM for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1, respectively. Regorafenib monohydrate shows very robust antitumor and antiangiogenic activity.
  • HY-P1119A
    WRW4 TFA

    Formyl Peptide Receptor (FPR) Neurological Disease
    WRW4 TFA, a specific formyl peptide receptor-like 1 (FPRL1) antagonist, inhibits WKYMVm binding to FPRL1 with an IC50 of 0.23 μM. WRW4 TFA specifically inhibits the increase in intracellular calcium by the FPRL1 agonists MMK-1, amyloid beta42 (Abeta42) peptide, and F peptide.
  • HY-10255AS
    Sunitinib-d10

    SU 11248-d10

    VEGFR PDGFR IRE1 Mitophagy Autophagy Apoptosis Cancer
    Sunitinib D10 (SU 11248 D10) is a deuterium labeled Sunitinib. Sunitinib is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively. Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation.
  • HY-B1739
    Pregnenolone monosulfate

    3β-Hydroxy-5-pregnen-20-one monosulfate

    Cannabinoid Receptor TRP Channel Endogenous Metabolite Autophagy Neurological Disease
    Pregnenolone monosulfate (3β-Hydroxy-5-pregnen-20-one monosulfate) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone monosulfate acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone monosulfate can protect the brain from cannabis intoxication. Pregnenolone monosulfate is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels.
  • HY-100434
    PD-161570

    FGFR PDGFR EGFR Src TGF-β Receptor Cancer Cardiovascular Disease
    PD-161570 is a potent and ATP-competitive human FGF-1 receptor inhibitor with an IC50 of 39.9 nM and a Ki of 42 nM. PD-161570 also inhibits the PDGFR, EGFR and c-Src tyrosine kinases with IC50 values of 310 nM, 240 nM, and 44 nM, respectively. PD-161570 inhibits PDGF-stimulated autophosphorylation and FGF-1 receptor phosphorylation with IC50s of 450 nM and 622 nM, respectively. PD-161570 is also a bone morphogenetic proteins (BMPs) and TGF-β signaling inhibitor.
  • HY-135581S
    Raloxifene 6-glucuronide-d4

    Estrogen Receptor/ERR Endocrinology
    Raloxifene 6-glucuronide-d4 is the deuterium labeled Raloxifene 6-glucuronide. Raloxifene 6-glucuronide is a primary metabolite of Raloxifene. Raloxifene 6-glucuronide is mediated mostly by UGT1A1 and UGT1A8. Raloxifene 6-glucuronide binds to estrogen receptor with an IC50 of 290 μM. Raloxifene is a selective and nonsteroidal estrogen receptor modulator. Raloxifene activates TGFβ3 promoter as a full agonist at nanomolar concentrations, and inhibits the estrogen response element-containing vitellogenin promoter expression.
  • HY-110189
    Pregnenolone monosulfate sodium

    3β-Hydroxy-5-pregnen-20-one monosulfate sodium

    Cannabinoid Receptor TRP Channel Endogenous Metabolite Autophagy Neurological Disease
    Pregnenolone monosulfate sodium (3β-Hydroxy-5-pregnen-20-one monosulfate sodium) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone monosulfate sodium acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone monosulfate sodium can protect the brain from cannabis intoxication. Pregnenolone monosulfate sodium is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels.
  • HY-16561
    Resveratrol

    trans-Resveratrol; SRT501

    IKK Autophagy Mitophagy Sirtuin Apoptosis Bacterial Fungal Antibiotic Keap1-Nrf2 Cancer Infection Inflammation/Immunology
    Resveratrol (trans-Resveratrol; SRT501), a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol (SRT 501) has a wide spectrum of targets including mTOR, JAK, β-amyloid, Adenylyl cyclase, IKKβ, DNA polymerase. Resveratrol also is a specific SIRT1 activator. Resveratrol is a potent pregnane X receptor (PXR) inhibitor. Resveratrol is an Nrf2 activator, ameliorates aging-related progressive renal injury in mice model. Resveratrol increases production of NO in endothelial cells.
  • HY-120645
    BMS-986122

    Opioid Receptor Neurological Disease
    BMS-986122 is a selective, potent positive allosteric modulator of the mu-opioid receptor (µ-OR). BMS-986122 shows potentiation of orthosteric agonist-mediated β-arrestin recruitment, adenylyl cyclase inhibition, and G protein activation. BMS-986122 potentiates DAMGO-mediated [ 35S]GTPγS binding in mouse brain membranes.
  • HY-19578B
    Isamoltane hemifumarate

    5-HT Receptor Adrenergic Receptor Neurological Disease
    Isamoltane hemifumarate is a selective antagonist of 5-HT1B receptor, with an IC50 of 39 nM for inhibits the binding of [ 125I]ICYP to 5-HT1B recognition sites in rat brain membranes. Isamoltane hemifumarate is also a β-adrenoceptor ligand, with an IC50 of 8.4 nM. Isamoltane hemifumarate shows anxiolytic activity.
  • HY-N0761
    Isoferulic acid

    3-Hydroxy-4-methoxycinnamic acid

    Adrenergic Receptor Influenza Virus Infection Endocrinology Metabolic Disease
    Isoferulic acid (3-Hydroxy-4-methoxycinnamic acid) is a cinnamic acid derivative that has antidiabetic activity. Isoferulic acid binds to and activates α1-adrenergic receptors (IC50=1.4 µM) to enhance secretion of β-endorphin (EC50=52.2 nM) and increase glucose use. Isoferulic acid also has anti-influenza virus activities.
  • HY-A0036
    Bazedoxifene acetate

    TSE-424 acetate

    Estrogen Receptor/ERR Cancer
    Bazedoxifene acetate (TSE-424 acetate) is an oral, nonsteroidal selective estrogen receptor modulator (SERM), with IC50s of 23 nM and 99 nM for ERα and ERβ, respectively. Bazedoxifene acetate can be used for the research of osteoporosis. Bazedoxifene acetate also acts as an inhibitor of IL-6/GP130 protein-protein interactions and can be used for the research of pancreatic cancer.
  • HY-10331S1
    Regorafenib-13C,d3

    BAY 73-4506-13C,d3

    VEGFR Autophagy PDGFR Raf RET Cancer
    Regorafenib-13C,d3 is the 13C- and deuterium labeled Regorafenib. Regorafenib (BAY 73-4506) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 13/4.2/46, 22, 7, 1.5 and 2.5 nM for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1, respectively.
  • HY-135581S1
    Raloxifene 6-glucuronide-d4 lithium

    Estrogen Receptor/ERR Endocrinology
    Raloxifene 6-glucuronide-d4 (lithium) is deuterium labeled Raloxifene 6-glucuronide. Raloxifene 6-glucuronide is a primary metabolite of Raloxifene. Raloxifene 6-glucuronide is mediated mostly by UGT1A1 and UGT1A8. Raloxifene 6-glucuronide binds to estrogen receptor with an IC50 of 290 μM. Raloxifene is a selective and nonsteroidal estrogen receptor modulator. Raloxifene activates TGFβ3 promoter as a full agonist at nanomolar concentrations, and inhibits the estrogen response element-containing vitellogenin promoter expression.
  • HY-B0151S
    Pregnenolone-d4

    3β-Hydroxy-5-pregnen-20-one-d4

    Cannabinoid Receptor TRP Channel Endogenous Metabolite Autophagy Neurological Disease
    Pregnenolone-d4 is the deuterium labeled Pregnenolone. Pregnenolone (3β-Hydroxy-5-pregnen-20-one) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone can protect the brain from cannabis intoxication. Pregnenolone is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels.
  • HY-135582S1
    Raloxifene 4'-glucuronide-d4 lithium

    Estrogen Receptor/ERR Endocrinology
    Raloxifene 4'-glucuronide-d4 (lithium) is deuterium labeled Raloxifene 4'-glucuronide. Raloxifene 4'-glucuronide is a primary metabolite of Raloxifene. Raloxifene 4'-glucuronide formation is mediated mostly by UGT1A10 and UGT1A8. Raloxifene 4'-glucuronide binds to estrogen receptor with an IC50 of 370 μM. . Raloxifene is a selective estrogen receptor modulator. Raloxifene activates TGFβ3 promoter as a full agonist at nanomolar concentrations, and inhibits the estrogen response element-containing vitellogenin promoter expression.
  • HY-A0031
    Bazedoxifene

    TSE-424

    Estrogen Receptor/ERR Cancer
    Bazedoxifene (TSE-424) is an oral, BBB-penetrant nonsteroidal selective estrogen receptor modulator (SERM), with IC50s of 23 nM and 99 nM for ERα and ERβ, respectively. Bazedoxifene can be used for the research of osteoporosis. Bazedoxifene also acts as an inhibitor of IL-6/GP130 protein-protein interactions and can be used for the research of pancreatic cancer.
  • HY-123966
    MY33-3

    Phosphatase
    MY33-3 is a potent and selective inhibitor of receptor protein tyrosine phosphatase (RPTP)β/ζ, with an IC50 of ~0.1 μM. MY33-3 also inhibits PTP-1B (IC50 ~0.7 μM). MY33-3 can reduce ethanol consumption and alleviate Sevoflurane-induced neuroinflammation and cognitive dysfunction.
  • HY-123966A
    MY33-3 hydrochloride

    Phosphatase Neurological Disease
    MY33-3 hydrochloride is a potent and selective inhibitor of receptor protein tyrosine phosphatase (RPTP)β/ζ, with an IC50 of ~0.1 μM. MY33-3 hydrochloride also inhibits PTP-1B (IC50 ~0.7 μM). MY33-3 hydrochloride can reduce ethanol consumption and alleviate Sevoflurane-induced neuroinflammation and cognitive dysfunction.
  • HY-10185
    TG 100572 Hydrochloride

    Src VEGFR FGFR PDGFR Inflammation/Immunology
    TG 100572 Hydrochloride is a multi-targeted kinase inhibitor which inhibits receptor tyrosine kinases and Src kinases; has IC50s of 2, 7, 2, 16, 13, 5, 0.5, 6, 0.1, 0.4, 1, 0.2 nM for VEGFR1, VEGFR2, FGFR1, FGFR2, PDGFRβ, Fgr, Fyn, Hck, Lck, Lyn, Src, Yes, respectively.
  • HY-10255AS1
    Sunitinib-d4

    VEGFR PDGFR IRE1 Mitophagy Autophagy Apoptosis Cancer
    Sunitinib-d4 (SU 11248-d4) is the deuterium labeled Sunitinib. Sunitinib (SU 11248) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively. Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation.
  • HY-A0016
    Dronedarone

    SR 33589

    mAChR Sodium Channel Calcium Channel Adrenergic Receptor Cytochrome P450 Autophagy Cardiovascular Disease
    Dronedarone (SR 33589), a derivative of amiodarone (HY-14187), is a class III antiarrhythmic agent for the study of atrial fibrillation (AF) and atrial flutter. Dronedarone is a potent blocker of multiple ion currents, including potassium current, sodium current, and L-type calcium current, and exhibits antiadrenergic effects by noncompetitive binding to β-adrenergic receptors. Dronedarone is a substrate for and a moderate inhibitor of CYP3A4.
  • HY-A0031A
    Bazedoxifene hydrochloride

    TSE-424 hydrochloride

    Estrogen Receptor/ERR Cancer
    Bazedoxifene hydrochloride (TSE-424 hydrochloride) is an oral active, BBB-penetrant nonsteroidal selective estrogen receptor modulator (SERM), with IC50s of 23 nM and 99 nM for ERα and ERβ, respectively. Bazedoxifene hydrochloride can be used for the research of osteoporosis. Bazedoxifene hydrochloride acts as an inhibitor of IL-6/GP130 protein-protein interactions. Bazedoxifene hydrochloride can be used for the research of pancreatic cancer.
  • HY-10184
    TG 100572

    Src VEGFR PDGFR FGFR Cancer
    TG 100572 is a multi-targeted kinase inhibitor which inhibits receptor tyrosine kinases and Src kinases; has IC50s of 2, 7, 2, 16, 13, 5, 0.5, 6, 0.1, 0.4, 1, 0.2 nM for VEGFR1, VEGFR2, FGFR1, FGFR2, PDGFRβ, Fgr, Fyn, Hck, Lck, Lyn, Src, Yes, respectively.
  • HY-136390
    ML417

    Dopamine Receptor Neurological Disease
    ML417 is a selective and brain penetrant D3 dopamine receptor (D3R) agonist, with an EC50 of 38 nM. ML417 potently promotes D3R-mediated β-arrestin translocation, G protein mediated signaling, and pERK phosphorylation with minimal effects on other GPCR-mediated signaling. ML417 exhibits neuroprotection against toxin-induced neurodegeneration of dopaminergic neurons.
  • HY-108742A
    Abaloparatide TFA

    BA 058 TFA; BIM 44058 TFA

    Thyroid Hormone Receptor Metabolic Disease Endocrinology
    Abaloparatide TFA (BA 058 TFA) is a parathyroid hormone receptor 1 (PTHR1) analogue selected to be a potent and selective activator of the PTHR1 signaling pathway. Abaloparatide TFA enhances Gs/cAMP signaling (EC50 of 0.3 nM) and β-arrestin recruitment (EC50 of 0.9 nM) in MC3T3-E1 osteoblast cells.
  • HY-16023A
    Acolbifene

    EM-652; SCH 57068

    Estrogen Receptor/ERR Cancer
    Acolbifene (EM-652), the active metabolite of EM800, is an orally active pure antiestrogen and selective estrogen receptor antagonist. Acolbifene (EM-652) inhibits estradiol (E2)-induced transcriptional activity of ERα (IC50 = 2 nM) and ERβ (IC50 = 0.4 nM). Acolbifene (EM-652) possesses potent and pure anticarcinogenic properties.
  • HY-18725
    P2X7-IN-2

    P2X Receptor Interleukin Related Inflammation/Immunology Cardiovascular Disease
    P2X7-IN-2 (compound 58) is a P2X7 receptor inhibitor. P2X7-IN-2 inhibits IL-Iβ release with an IC50 value of 0.01 nM. P2X7-IN-2 can be used for the research of autoimmunity, inflammation and cardiovascular disease.
  • HY-144705
    GAT564

    Cannabinoid Receptor Neurological Disease
    GAT564 (Compound 15d) is a potent allosteric modulator of cannabinoid 1 receptor (CB1R) with EC50s of 87 and 320 nM respectively for cAMP and β-arrestin2. GAT564 markedly promotes orthosteric ligand binding to hCB1R. GAT564 is efficacious as a topical agent that significantly reduces intraocular pressure (IOP) in the ocular normotensive murine model of glaucoma.
  • HY-16673
    PSN632408

    GPR119 Metabolic Disease
    PSN632408, a selective, orally active GPR119 agonist, shows similar potency to OEA at both recombinant mouse and human GPR119 receptors (EC50=5.6 and 7.9 uM, respectively). PSN632408 can stimulate β-cell replication and improve islet graft function. PSN632408 has the potential for the research of obesity and related metabolic disorders.
  • HY-122816
    HLY78

    Wnt β-catenin Apoptosis Cancer Neurological Disease Cardiovascular Disease
    HLY78, a Lycorine (HY-N0288) derivative, is a potent activator of the Wnt/β-catenin signaling pathway. HLY78 targets the DIX domain of Axin and promotes the Axin-LRP6 (lipoprotein receptor-related protein 6) association, thus promoting LRP6 phosphorylation and Wnt signal transduction. HLY78 can be used for subarachnoid hemorrhage (SAH) research.
  • HY-110189S1
    Pregnenolone monosulfate-d4 sodium

    3β-Hydroxy-5-pregnen-20-one monosulfate-d4 sodium

    Cannabinoid Receptor TRP Channel Endogenous Metabolite Autophagy
    Pregnenolone monosulfate-d4 (sodium) is the deuterium labeled Pregnenolone monosulfate. Pregnenolone monosulfate sodium (3β-Hydroxy-5-pregnen-20-one monosulfate sodium) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone monosulfate sodium acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone monosulfate sodium can protect the brain from cannabis intoxication. Pregnenolone monosulfate sodium is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels.
  • HY-112461A
    NF449 octasodium

    P2X Receptor Cardiovascular Disease
    NF449 octasodium is a highly potent P2X1 receptor antagonist, with IC50s of 0.28, 0.69, and 120 nM for rP2X1, rP2X1+5, P2X2+3, respectively. NF449 octasodium is a G-selective G Protein antagonist. NF449 octasodium suppresses the rate of GTP[γS] binding to Gsα-s, inhibits the stimulation of adenylyl cyclase activity, and blocks the coupling of β-adrenergic receptors to Gs.
  • HY-151198
    CHF-6366

    mAChR Adrenergic Receptor Calcium Channel Endocrinology Inflammation/Immunology
    CHF-6366 is a potent M3 muscarinic antagonist and β2-adrenergic receptors agonist with pKi values of 10.4 and 11.4, respectively. CHF-6366 is also a weak calcium channel inhibitor (IC50~50 μM). CHF-6366 inhibits bronchoconstriction in guinea pigs. CHF-6366 can be used to research chronic obstructive pulmonary disease (COPD).
  • HY-124748A
    ENMD-1068 hydrochloride

    Protease Activated Receptor (PAR) Apoptosis Inflammation/Immunology
    ENMD-1068 hydrochloride is a selective protease-activated receptor 2 (PAR2) antagonist. ENMD-1068 hydrochloride reduces hepatic stellate cell activation and collagen expression by inhibiting TGF-β1/Smad signaling. ENMD-1068 hydrochloride also inhibits the proliferation of endometrial cells and induces apoptosis of epithelial cells in the lesion. ENMD-1068 hydrochloride can be used in the study of endometriosis and liver fibrosis.
  • HY-16561S
    Resveratrol-d4

    trans-Resveratrol-d4; SRT501-d4

    IKK Autophagy Mitophagy Sirtuin Apoptosis Bacterial Fungal Antibiotic Keap1-Nrf2 Cancer Infection Inflammation/Immunology
    Resveratrol-d4 (trans-Resveratrol-d4) is the deuterium labeled Resveratrol. Resveratrol (trans-Resveratrol; SRT501), a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol (SRT 501) has a wide spectrum of targets including mTOR, JAK, β-amyloid, Adenylyl cyclase, IKKβ, DNA polymerase. Resveratrol also is a specific SIRT1 activator. Resveratrol is a potent pregnane X receptor (PXR) inhibitor. Resveratrol is an Nrf2 activator, ameliorates aging-related progressive renal injury in mice model. Resveratrol increases production of NO in endothelial cells.
  • HY-P2141
    TRV-120027

    Angiotensin Receptor Cardiovascular Disease
    TRV120027, a β-arrestin-1-biased agonist of the angiotensin II receptor type 1 (AT1R), engages ß-arrestins while blocking G-protein signaling. TRV120027 induces acute catecholamine secretion through cation channel subfamily C3 (TRPC3) coupling, promotes the formation of a macromolecular complex composed of AT1R–β-arrestin-1–TRPC3–PLCγ at the plasma membrane. TRV120027 inhibits angiotensin II–mediated vasoconstriction and increases cardiomyocyte contractility. TRV120027 has the potential for the acute decompensated heart failure (ADHF) treatment.
  • HY-P2141A
    TRV-120027 TFA

    Angiotensin Receptor Cardiovascular Disease
    TRV120027 TFA, a β-arrestin-1-biased agonist of the angiotensin II receptor type 1 (AT1R), engages ß-arrestins while blocking G-protein signaling. TRV120027 TFA induces acute catecholamine secretion through cation channel subfamily C3 (TRPC3) coupling, promotes the formation of a macromolecular complex composed of AT1R–β-arrestin-1–TRPC3–PLCγ at the plasma membrane. TRV120027 TFA inhibits angiotensin II–mediated vasoconstriction and increases cardiomyocyte contractility. TRV120027 TFA has the potential for the acute decompensated heart failure (ADHF) treatment.
  • HY-A0031S1
    Bazedoxifene-d4 N-Oxide

    Estrogen Receptor/ERR Cancer
    Bazedoxifene-d4 N-Oxide is the deuterium labeled Bazedoxifene. Bazedoxifene (TSE-424) is an oral, BBB-penetrant nonsteroidal selective estrogen receptor modulator (SERM), with IC50s of 23 nM and 99 nM for ERα and ERβ, respectively. Bazedoxifene can be used for the research of osteoporosis. Bazedoxifene also acts as an inhibitor of IL-6/GP130 protein-protein interactions and can be used for the research of pancreatic cancer.
  • HY-B1671
    (+)-Kavain

    GABA Receptor Sodium Channel Calcium Channel Metabolic Disease Neurological Disease
    (+)-Kavain, a main kavalactone extracted from Piper methysticum, has anticonvulsive properties, attenuating vascular smooth muscle contraction through interactions with voltage-dependent Na + and Ca 2+ channels. (+)-Kavain is shown to bind at the α4β2δ GABAA receptor and potentiate GABA efficacy. (+)-Kavain is used as a treatment for inflammatory diseases, its anti-inflammatory action has been widely studied.
  • HY-135794
    11-Ketodihydrotestosterone

    11-KDHT; 5α-Dihydro-11-keto testosterone

    Androgen Receptor Endocrinology
    11-Ketodihydrotestosterone (11-KDHT; 5α-Dihydro-11-keto testosterone) is an endogenous steroid and a metabolite of 11β-Hydroxyandrostenedione. 11-Ketodihydrotestosterone is an active androgen and is also a potent androgen receptor (AR) agonist with a Ki of 20.4 nM and an EC50 of 1.35 nM for human AR. 11-Ketodihydrotestosterone drives gene regulation, protein expression and cell growth in androgen-dependent prostate cancer cells.
  • HY-A0083
    Methacholine chloride

    Acetyl-β-methylcholine chloride

    mAChR Others
    Methacholine (Acetyl-β-methylcholine) choride is a potent muscarinic-3 (M3) agonist. Methacholine choride acts directly on acetylcholine receptors on smooth muscle causing bronchoconstriction and airway narrowing. Methacholine choride shows a high sensitivity to identify bronchial hyperresponsiveness (BHR). Methacholine choride can be used to measure airway hyperresponsiveness (AHR) as a diagnostic aid in the assessment of individuals with asthma-like symptoms and normal resting expiratory flow rates.
  • HY-A0031S
    Bazedoxifene-d4

    TSE-424-d4

    Estrogen Receptor/ERR Cancer
    Bazedoxifene-d4 is deuterium labeled Bazedoxifene. Bazedoxifene (TSE-424) is an oral, BBB-penetrant nonsteroidal selective estrogen receptor modulator (SERM), with IC50s of 23 nM and 99 nM for ERα and ERβ, respectively. Bazedoxifene can be used for the research of osteoporosis. Bazedoxifene also acts as an inhibitor of IL-6/GP130 protein-protein interactions and can be used for the research of pancreatic cancer.
  • HY-10330S
    Toceranib-d8

    PDGFR VEGFR c-Kit Cancer
    Toceranib-d8 (SU11654-d8) is the deuterium labeled Toceranib. Toceranib (SU11654) is an orally active receptor tyrosine kinase (RTK) inhibitor, and it potently inhibits PDGFR, VEGFR, and Kit with Kis of 5 and 6 nM for PDGFRβ and Flk-1/KDR, respectively. Toceranib (SU11654) has antitumor and antiangiogenic activity, and used in the treatment of canine mast cell tumors.
  • HY-P1682
    Balixafortide

    POL6326

    CXCR Cancer
    Balixafortide (POL6326) is a potent, selective, well-tolerated peptidic CXCR4 antagonist with an IC50 < 10 nM. Balixafortide shows 1000-fold selective for CXCR4 than a large panel of receptors including CXCR7. Balixafortide blocks β-arrestin recruitment and calcium flux with IC50s < 10 nM. Balixafortide is also a potent hematopoietic stem and progenitor cell (HSPC) mobilizing agent. Anti-cancer effects.
  • HY-A0016S
    Dronedarone D6 hydrochloride

    mAChR Sodium Channel Calcium Channel Adrenergic Receptor Cytochrome P450 Autophagy Cardiovascular Disease
    Dronedarone D6 hydrochloride is the deuterium labeled Dronedarone. Dronedarone hydrochloride, a derivative of Amiodarone (HY-14187), is a class III antiarrhythmic agent for the study of atrial fibrillation (AF) and atrial flutter. Dronedarone hydrochloride is a potent blocker of multiple ion currents, including potassium current, sodium current, and L-type calcium current, and exhibits antiadrenergic effects by noncompetitive binding to β-adrenergic receptors. Dronedarone hydrochloride is a substrate for and a moderate inhibitor of CYP3A4.
  • HY-A0083B
    Methacholine bromide

    Acetyl-β-methylcholine bromide

    mAChR Cardiovascular Disease
    Methacholine (Acetyl-β-methylcholine) bromide is a potent muscarinic-3 (M3) agonist. Methacholine bromide acts directly on acetylcholine receptors on smooth muscle causing bronchoconstriction and airway narrowing. Methacholine bromide shows a high sensitivity to identify bronchial hyperresponsiveness (BHR). Methacholine bromide can be used to measure airway hyperresponsiveness (AHR) as a diagnostic aid in the assessment of individuals with asthma-like symptoms and normal resting expiratory flow rates.
  • HY-W011266
    JNJ-10198409

    PDGFR Cancer
    JNJ-10198409 is a relatively selective, orally active, and ATP competitive PDGF-RTK (platelet-derived growth factor receptor tyrosine kinase) inhibitor (IC50=2 nM). It is a dual-mechanism, antiangiogenic, and tumor cell antiproliferative agent. JNJ-10198409 has good activity against PDGFR-β kinase (IC50=4.2 nM) and PDGFR-α kinase (IC50=45 nM).
  • HY-147428
    Zolunicant

    MM-110

    nAChR Parasite Infection Neurological Disease
    Zolunicant (MM-110) is a potent inhibitor against nicotinic α3β4 receptors with an IC50 of 0.90 μM to combat addiction. Zolunicant can decrease the self-administration of several addictive agents including morphine, cocaine, methamphetamine, nicotine, and ethanol in rat model. Zolunicant can be studied as a potential treatment for multiple forms of drug abuse. Zolunicant also reveals a potent leishmanicide effect against Leishmania amazonensis.
  • HY-100277
    Mifobate

    SR-202

    PPAR Metabolic Disease
    Mifobate (SR-202) is a potent and specific PPARγ antagonist. Mifobate (SR-202) selectively inhibits Thiazolidinedione (TZD)-induced PPARγ transcriptional activity (IC50=140 μM). Mifobate (SR-202) does not affect basal or ligand-stimulated transcriptional activity of PPARα, PPARβ, or the farnesoid X receptor (FXR). Mifobate (SR-202) shows antiobesity and antidiabetic effects.
  • HY-P1454
    Fz7-21

    Ac-LPSDDLEFWCHVMY-NH2

    Wnt Cancer
    Fz7-21 (Ac-LPSDDLEFWCHVMY-NH2) is a potent peptide antagonist of FZD7 receptors , selectively binds to FZD7 CRD subclass and alters the conformation of the CRD and the architecture of its lipid-binding groove. The EC50 values are 58 and 34 nM for human and mouse FZD7 CRD, respectively. Fz7-21 impairs the function of FZD7 in Wnt–β-catenin signalling and stem cell function in intestinal organoids.
  • HY-16561S1
    Resveratrol-13C6

    trans-Resveratrol-13C6; SRT501-13C6

    IKK Autophagy Mitophagy Sirtuin Apoptosis Bacterial Fungal Antibiotic Keap1-Nrf2 Cancer Infection Inflammation/Immunology
    Resveratrol-13C6 (trans-Resveratrol-13C6) is the 13C-labeled Resveratrol. Resveratrol (trans-Resveratrol; SRT501), a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol (SRT 501) has a wide spectrum of targets including mTOR, JAK, β-amyloid, Adenylyl cyclase, IKKβ, DNA polymerase. Resveratrol also is a specific SIRT1 activator. Resveratrol is a potent pregnane X receptor (PXR) inhibitor. Resveratrol is an Nrf2 activator, ameliorates aging-related progressive renal injury in mice model. Resveratrol increases production of NO in endothelial cells.
  • HY-128121
    MLS1547

    Dopamine Receptor Neurological Disease
    MLS1547 is a highly efficacious G protein-biased dopamine D2 receptor (D2R) agonist (Ki=1.2 μM). MLS1547 stimulates D2R G protein-mediated signaling (EC50=0.37 μM in a calcium mobilization assay). MLS1547 acts as an antagonist for dopamine (DA)-stimulated β-arrestin recruitment to the D2R (IC50=9.9 μM).
  • HY-P99410
    Ordesekimab

    AMG 714; PRV-015

    Interleukin Related Inflammation/Immunology
    Ordesekimab (AMG 714; PRV-015) is a fully human IgG1κ anti-IL-15 (Interleukin Related) monoclonal antibody. The binding of Ordesekimab to IL-15 inhibits the interaction of IL-15 with the IL-2Rβ and common γ chain of the IL-15 receptor complex, but not with the IL-15Rα chain. Ordesekimab has the potential for study of nonresponsive celiac disease (NRCD).
  • HY-146289
    LXR antagonist 2

    LXR Metabolic Disease
    LXR antagonist 2 (compound 10rr) is a potent LXR (liver X receptor) inverse agonist, with IC50 values of 0.36 and 2.25 μM for LXRβ and LXRα, respectively. LXR antagonist 2 is a lipogenesis inhibitor through down-regulating LXR target genes SREBP-1c, ACC, FAS and SCD-1. LXR antagonist 2 shows lipid-lowering effects in mice with Triton WR-1339-induced hyperlipidemia.
  • HY-P1454A
    Fz7-21 TFA

    Ac-LPSDDLEFWCHVMY-NH2 TFA

    Wnt Cancer
    Fz7-21 (Ac-LPSDDLEFWCHVMY-NH2) TFA is a potent peptide antagonist of FZD7 receptors , selectively binds to FZD7 CRD subclass and alters the conformation of the CRD and the architecture of its lipid-binding groove. The EC50 values are 58 and 34 nM for human and mouse FZD7 CRD, respectively. Fz7-21 TFA impairs the function of FZD7 in Wnt-β-catenin signalling and stem cell function in intestinal organoids.
  • HY-P1682A
    Balixafortide TFA

    POL6326 TFA

    CXCR Cancer
    Balixafortide TFA (POL6326 TFA) is a potent, selective, well-tolerated peptidic CXCR4 antagonist with an IC50 < 10 nM. Balixafortide TFA shows 1000-fold selective for CXCR4 than a large panel of receptors including CXCR7. Balixafortide TFA blocks β-arrestin recruitment and calcium flux with IC50s < 10 nM. Balixafortide TFA is also a potent hematopoietic stem and progenitor cell (HSPC) mobilizing agent. Anti-cancer effects.
  • HY-120026
    KB130015

    KB015

    Thyroid Hormone Receptor Neurological Disease
    KB130015 (KB015) is an orally active and potent ThRα and ThRβ (Thyroid Hormone Receptor) inhibitor, with IC50 values of 4.5 and 5.1 μM, respectively. KB130015 has antiarrhythmic properties. KB130015 markedly slows the kinetics of inactivation of Na + channels. KB130015 opens large-conductance Ca 2+-activated K + channels and relaxes vascular smooth muscle.
  • HY-16023
    Acolbifene hydrochloride

    EM-652 hydrochloride; SCH 57068 hydrochloride

    Estrogen Receptor/ERR Cancer
    Acolbifene (EM-652) hydrochloride, an active metabolite of EM800, is an orally active, cancer-preventing selective estrogen receptor modulator (SERM). Acolbifene (EM-652) hydrochloride inhibits estradiol (E2)-induced transcriptional activity of ERα (IC50=2 nM) and ERβ (IC50=0.4 nM). Acolbifene (EM-652) hydrochloride exerts a potent and pure antiestrogenic action in the mammary gland and uterus. Anticarcinogenic properties.
  • HY-10564
    Sarpogrelate hydrochloride

    MCI-9042

    5-HT Receptor Cardiovascular Disease
    Sarpogrelate hydrochloride (MCI-9042) is a selective 5-HT2R antagonist, with pKis of 8.52, 6.57, and 7.43 for 5-HT2A, 5-HT2B, and 5-HT2C receptors, respectively. Sarpogrelate hydrochloride displays selectivity over 5-HT1, 5-HT3, 5-HT4, α1-, α2- and β-adrenoreceptor, histamine H1, H2 and muscarinic M3 receptors. Sarpogrelate hydrochloride can be used for the research of vascular disease associated with thrombosis.
  • HY-123489S
    3α,21-Dihydroxy-5α-pregnan-20-one-d3

    THDOC-d3

    GABA Receptor Neurological Disease
    3α,21-Dihydroxy-5α-pregnan-20-one-d3 (THDOC-d3) is the deuterium labeled 3α,21-Dihydroxy-5α-pregnan-20-one. 3α,21-Dihydroxy-5α-pregnan-20-one (THDOC), an endogenous neurosteroid, is a positive modulator of GABAA receptors. 3α,21-Dihydroxy-5α-pregnan-20-one potentiates neuronal response to low concentrations of GABA at α4β1δ GABAA receptors in vitro.
  • HY-110189S
    Pregnenolone monosulfate sodium-13C2,d2

    3β-Hydroxy-5-pregnen-20-one monosulfate sodium-13C2,d2

    Cannabinoid Receptor TRP Channel Endogenous Metabolite Autophagy Neurological Disease
    Pregnenolone monosulfate sodium-13C2,d2 is the 13C- and deuterium labeled Pregnenolone monosulfate sodium. Pregnenolone monosulfate sodium (3β-Hydroxy-5-pregnen-20-one monosulfate sodium) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone monosulfate sodium salt acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone monosulfate sodium salt can protect the brain from cannabis intoxication. Pregnenolone monosulfate sodium salt is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels.
  • HY-131404
    TPBM

    Estrogen Receptor/ERR Cancer
    TPBM is a potent estrogen receptor α (ERα) inhibitor with an IC50 value of 9 μM for 17β-estradiol (E2)-ERα. TPBM reduces E2·ERα recruitment to an endogenous estrogen-responsive gene. TPBM inhibits E2-dependent growth of ERα-positive cancer cells (IC50=5 μM). TPBM is not toxic to cells and does not affect estrogen-independent cell growth.
  • HY-10187
    TG 100801 Hydrochloride

    VEGFR FGFR PDGFR Src Cancer
    TG 100801 Hydrochloride is a prodrug that generates TG 100572 by de-esterification in development to treat age-related macular degeneration. TG 100572 is a multi-targeted kinase inhibitor which inhibits receptor tyrosine kinases and Src kinases; has IC50s of 2, 7, 2, 16, 13, 5, 0.5, 6, 0.1, 0.4, 1, 0.2 for VEGFR1, VEGFR2, FGFR1, FGFR2, PDGFRβ, Fgr, Fyn, Hck, Lck, Lyn, Src, Yes, respectively.
  • HY-P1844
    Chemerin-9 (149-157)

    Akt ERK Reactive Oxygen Species Amyloid-β Inflammation/Immunology
    Chemerin-9 (149-157) is a potent agonist of chemokine-like receptor 1 (CMKLR1) . Chemerin-9 (149-157) has anti-inflammatory activity. Chemerin-9 (149-157) stimulates phosphorylation of Akt and ERK as well as ROS production. Chemerin-9 (149-157) ameliorates Aβ1-42-induced memory impairmen. Chemerin-9 (149-157) regulates immune responses, adipocyte differentiation, and glucose metabolism.
  • HY-N1584
    Halofuginone

    RU-19110

    DNA/RNA Synthesis TGF-beta/Smad Parasite Sodium Channel Calcium Channel Cancer Infection Inflammation/Immunology Cardiovascular Disease
    Halofuginone (RU-19110), a Febrifugine derivative, is a competitive prolyl-tRNA synthetase inhibitor with a Ki of 18.3 nM. Halofuginone is a specific inhibitor of type-I collagen synthesis and attenuates osteoarthritis (OA) by inhibition of TGF-β activity. Halofuginone is also a potent pulmonary vasodilator by activating Kv channels and blocking voltage-gated, receptor-operated and store-operated Ca 2+ channels. Halofuginone has anti-malaria, anti-inflammatory, anti-cancer, anti-fibrosis effects.
  • HY-10186
    TG 100801

    VEGFR FGFR PDGFR Src Cancer
    TG 100801 is a prodrug that generates TG 100572 by de-esterification in development to treat age-related macular degeneration. TG 100572 is a multi-targeted kinase inhibitor which inhibits receptor tyrosine kinases and Src kinases; has IC50s of 2, 7, 2, 16, 13, 5, 0.5, 6, 0.1, 0.4, 1, 0.2 for VEGFR1, VEGFR2, FGFR1, FGFR2, PDGFRβ, Fgr, Fyn, Hck, Lck, Lyn, Src, Yes, respectively.
  • HY-P1844A
    Chemerin-9 (149-157) (TFA)

    Akt ERK Reactive Oxygen Species Amyloid-β Inflammation/Immunology
    Chemerin-9 (149-157) TFA is a potent agonist of chemokine-like receptor 1 (CMKLR1) . Chemerin-9 (149-157) TFA has anti-inflammatory activity. Chemerin-9 (149-157) TFA stimulates phosphorylation of Akt and ERK as well as ROS production. Chemerin-9 (149-157) TFA ameliorates Aβ1-42-induced memory impairmen. Chemerin-9 (149-157) TFA regulates immune responses, adipocyte differentiation, and glucose metabolism.
  • HY-N0755
    Rhoifolin

    Insulin Receptor GLUT NF-κB p38 MAPK Autophagy Metabolic Disease Endocrinology Cancer
    Rhoifolin is a flavone glycoside can be isolated from Rhus succedanea. Rhoifolin has anti-diabetic effect acting through enhanced adiponectin secretion, tyrosine phosphorylation of insulin receptor-β and glucose transporter 4 (GLUT 4) translocation. Rhoifolin has an anti-inflammatory action via multi-level regulation of inflammatory mediators. Rhoifolin ameliorates titanium particle-stimulated osteolysis and attenuates osteoclastogenesis via RANKL-induced NF-κB and MAPK pathways. Rhoifolin also has cytotoxic activity against different cancer cell lines.
  • HY-18758
    IN-1130

    TGF-β Receptor Cancer Inflammation/Immunology
    IN-1130 is a highly selective transforming growth factor-β type I receptor kinase (ALK5) inhibitor with an IC50 of 5.3 nM for ALK5-mediated Smad3 phosphorylation. IN-1130 inhibits ALK5 phosphorylation of casein (IC50=36 nM) and p38α mitogen-activated protein kinase (IC50=4.3 μM). IN-1130 suppresses renal fibrosis in obstructive nephropathy and blocks breast cancer lung metastasis.
  • HY-112345
    PD-089828

    FGFR PDGFR EGFR Src Cancer
    PD-089828 is an ATP competitive inhibitor of FGFR-1, PDGFR-β and EGFR (IC50s=0.15, 1.76, and 5.47 µM, respectively) and a noncompetitive inhibitor of c-Src tyrosine kinase (IC50=0.18 µM). PD-089828 also inhibits MAPK with an IC50 of 7.1 µM. PD-089828 inhibits PDGF-, EGF- and bFGF-mediated tyrosine kinase receptor autophosphorylation in vitro. PD-089828 has a long-lasting cellular activity.
  • HY-N1584A
    Halofuginone hydrobromide

    RU-19110 hydrobromide

    DNA/RNA Synthesis TGF-beta/Smad Parasite Sodium Channel Calcium Channel Cancer Infection Inflammation/Immunology Cardiovascular Disease
    Halofuginone (RU-19110) hydrobromid, a Febrifugine derivative, is a competitive prolyl-tRNA synthetase inhibitor with a Ki of 18.3 nM. Halofuginone hydrobromid is a specific inhibitor of type-I collagen synthesis and attenuates osteoarthritis (OA) by inhibition of TGF-β activity. Halofuginone hydrobromid is also a potent pulmonary vasodilator by activating Kv channels and blocking voltage-gated, receptor-operated and store-operated Ca 2+ channels. Halofuginone hydrobromid has anti-malaria, anti-inflammatory, anti-cancer, anti-fibrosis effects.
  • HY-10564S
    Sarpogrelate-d3 hydrochloride

    MCI-9042-d3

    5-HT Receptor Cardiovascular Disease
    Sarpogrelate-d3 hydrochloride (MCI-9042-d3) is the deuterium labeled Sarpogrelate hydrochloride. Sarpogrelate hydrochloride (MCI-9042) is a selective 5-HT2R antagonist, with pKis of 8.52, 6.57, and 7.43 for 5-HT2A, 5-HT2B, and 5-HT2C receptors, respectively. Sarpogrelate hydrochloride displays selectivity over 5-HT1, 5-HT3, 5-HT4, α1-, α2- and β-adrenoreceptor, histamine H1, H2 and muscarinic M3 receptors. Sarpogrelate hydrochloride can be used for the research of vascular disease associated with thrombosis.
  • HY-120878
    CXCR2-IN-2

    CXCR Inflammation/Immunology
    CXCR2-IN-2 is a selective, brain penetrant, and orally bioavailable CXCR2 antagonist (IC50=5.2 nM/1 nM in β-arrestin assay/CXCR2 Tango assay, respectively). CXCR2-IN-2 displays ~730-fold selectivity over CXCR1 and >1900-fold selectivity over all other chemokine receptors. CXCR2-IN-2 inhibits human whole blood Gro-α induced CD11b expression with an IC50 of 0.04 μM.
  • HY-135794S
    11-Ketodihydrotestosterone-d3

    11-KDHT-d3; 5α-Dihydro-11-keto testosterone-d3

    Androgen Receptor Endocrinology
    11-Ketodihydrotestosterone-d3 (11-KDHT-d3) is the deuterium labeled 11-Ketodihydrotestosterone. 11-Ketodihydrotestosterone (11-KDHT; 5α-Dihydro-11-keto testosterone) is an endogenous steroid and a metabolite of 11β-Hydroxyandrostenedione. 11-Ketodihydrotestosterone is an active androgen and is also a potent androgen receptor (AR) agonist with a Ki of 20.4 nM and an EC50 of 1.35 nM for human AR. 11-Ketodihydrotestosterone drives gene regulation, protein expression and cell growth in androgen-dependent prostate cancer cells.
  • HY-101392
    Harmane

    Imidazoline Receptor Monoamine Oxidase Adrenergic Receptor Cancer Neurological Disease
    Harmane, a β-Carboline alkaloid (BCA), is a potent neurotoxin that causes severe action tremors and psychiatric manifestations. Harmane shows 1000-fold selectivity for I1-Imidazoline receptor (IC50=30 nM) over α2-adrenoceptor (IC50=18 μM). Harmane is also a potent and selective inhibitor of monoamine oxidase (MAO) (IC50s=0.5 and 5 μM for human MAO A/B, respectively). Harmane exhibits comutagenic effect.
  • HY-101392S1
    Harmane-d2

    Imidazoline Receptor Monoamine Oxidase Adrenergic Receptor Cancer Neurological Disease
    Harmane-d2 is the deuterium labeled Harmane. Harmane, a β-Carboline alkaloid (BCA), is a potent neurotoxin that causes severe action tremors and psychiatric manifestations. Harmane shows 1000-fold selectivity for I1-Imidazoline receptor (IC50=30 nM) over α2-adrenoceptor (IC50=18 μM). Harmane is also a potent and selective inhibitor of monoamine oxidase (MAO) (IC50s=0.5 and 5 μM for human MAO A/B, respectively).
  • HY-101392S
    Harmane-d1

    Imidazoline Receptor Monoamine Oxidase Adrenergic Receptor Cancer Neurological Disease
    Harmane-d1 is the deuterium labeled Harmane. Harmane, a β-Carboline alkaloid (BCA), is a potent neurotoxin that causes severe action tremors and psychiatric manifestations. Harmane shows 1000-fold selectivity for I1-Imidazoline receptor (IC50=30 nM) over α2-adrenoceptor (IC50=18 μM). Harmane is also a potent and selective inhibitor of monoamine oxidase (MAO) (IC50s=0.5 and 5 μM for human MAO A/B, respectively).
  • HY-N4267
    Yangambin

    Calcium Channel Infection Cardiovascular Disease
    Yangambin, a furofuran lignan, is already isolated from plants such as member of the Annonaceae family, including species of the genus Rollinia: R. pickeli, R. exalbidaand R. mucosa, as well from the Magnolia biondii. Yangambin, a selective PAF receptor antagonist, inhibits Ca 2+ influx through voltage-gated Ca 2+ channels, leading to the reduction in [Ca 2+]i in vascular smooth muscle cells and consequent peripheral vasodilation. Yangambin exhibits the antiallergic activity against β-hexosaminidase release with an IC50 of 33.8 μM and for anti-inflammatory activity with an IC50 of 37.4 μM.
  • HY-123450
    S116836

    Bcr-Abl Apoptosis PDGFR Cancer
    S116836, a potent, orally active BCR-ABL tyrosine kinase inhibitor, blocks both wild-type as well as T315I Bcr-Abl. S116836 arrests the cells in the G0/G1 phase of cell cycle, induces apoptosis, increases ROS production, and decreases GSH production in BaF3/WT and BaF3/T315I cells. S116836 also inhibits SRC, LYN, HCK, LCK and BLK, and receptor tyrosine kinases such as FLT3, TIE2, KIT, PDGFR-β. Antitumor activies.
  • HY-P2196A
    ELA-32(human) TFA

    Apelin Receptor (APJ)
    ELA-32(human) TFA is a potent, high affinity apelin receptor agonist (IC50=0.27 nM; Kd=0.51 nM). ELA-32(human) TFA exhibits no binding GPR15 and GPR25. ELA-32(human) TFA activates the PI3K/AKT pathway and promotes self-renewal of hESCs via cell-cycle progression and protein translation. ELA-32(human) TFA also potentiates the TGFβ pathway, priming hESCs toward the endoderm lineage. ELA-32(human) TFA stimulates angiogenesis in HUVEC cells.
  • HY-15310
    Ivermectin

    MK-933

    Parasite HIV Mitophagy HSV SARS-CoV Antibiotic Autophagy Bacterial Infection Cancer
    Ivermectin (MK-933) is a broad-spectrum anti-parasite agent. Ivermectin (MK-933) is a specific inhibitor of Impα/β1-mediated nuclear import and has potent antiviral activity towards both HIV-1 and dengue virus. It is a positive allosteric effector of P2X4 and the α7 neuronal nicotinic acetylcholine receptor (nAChRs). Ivermectin also inhibits bovine herpesvirus1 (BoHV-1) replication and inhibits BoHV-1 DNA polymerase nuclear import. Ivermectin is a candidate therapeutic against SARS-CoV-2/COVID-19.