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pharmacologically

" in MCE Product Catalog:

130

Inhibitors & Agonists

7

Screening Libraries

1

Dye Reagents

1

Biochemical Assay Reagents

5

Peptides

52

Natural
Products

10

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas
  • HY-P1298
    Sauvagine

    CRFR Endocrinology Neurological Disease Cardiovascular Disease
    Sauvagine, a 40-amino-acid neuropeptide from the skin of the frog, is a mammalian CRF agonist. Sauvagine is effective at releasing ACTH from rat pituitary cells. Sauvagine possesses a number of pharmacological actions on diuresis, the cardiovascular system and endocrine glands.
  • HY-P1298A
    Sauvagine TFA

    CRFR Endocrinology Neurological Disease Cardiovascular Disease
    Sauvagine TFA, a 40-amino-acid neuropeptide from the skin of the frog, is a mammalian CRF agonist. Sauvagine TFA is effective at releasing ACTH from rat pituitary cells. Sauvagine TFA possesses a number of pharmacological actions on diuresis, the cardiovascular system and endocrine glands.
  • HY-N1377
    Nevadensin

    Bacterial Infection Metabolic Disease Inflammation/Immunology
    Nevadensin is a naturally occurring selective inhibitor of human carboxylesterase 1 (hCE1) with an IC50 of 2.64 μM. Nevadensin has a variety of pharmacological effects such as anti-mycobacterium tuberculosis activities, antitussive, anti-inflammatory and anti-hypertensive.
  • HY-121385
    Hydroxy bosentan

    Ro 48-5033

    Endogenous Metabolite Cardiovascular Disease
    Hydroxy bosentan (Ro 48-5033) is a primary metabolite of Bosentan (BOS) metabolized by the cytochrome P450 system in the liver. Ro 48-5033 assists BOS pharmacologically, retaining 10%-20% activities.
  • HY-B1371
    Spiperone

    Spiroperidol

    Dopamine Receptor 5-HT Receptor Neurological Disease
    Spiperone is a potent dopamine D2, serotonin 5-HT1A, and serotonin 5-HT2A antagonist. Spiperone is a widely used pharmacological tool. Spiperone has the potential for the research of neurology diseases.
  • HY-107712
    TCN 213

    iGluR Neurological Disease
    TCN 213 is a selective, surmountable, glycine-dependentlly GluN1/GluN2A NMDAR antagonist with IC50s of 0.55, 3.5, 40 μM in the presence of 75, 750, 7500 nM glycine, respectively. TCN 213 can be used to monitor, pharmacologically, the switch in NMDAR expression in developing cortical neurones.
  • HY-15895S
    Aprocitentan D4

    ACT-132577 D4

    Endothelin Receptor Endocrinology Cardiovascular Disease
    Aprocitentan D4 (ACT-132577 D4) is a deuterium labeled Aprocitentan. Aprocitentan is a major and pharmacologically active metabolite of Macitentan. Aprocitentan is dual ETA/ETB antagonist with IC50s of 3.4 nM and 987 nM, and pA2 valus of 6.7 and 5.5, respectively.
  • HY-12345
    ML365

    Potassium Channel Cardiovascular Disease
    ML365 is a selective two-pore domain potassium channel KCNK3/TASK1 inhibitor, with an IC50 of 4 nM. ML365 acts as a pharmacological tool that can be used to examine the specific roles of TASK1 channels.
  • HY-142521
    BLT2 probe 1

    Others Metabolic Disease
    BLT2 probe 1 (compound 13) is a fluorescent probe based on the synthetic BLT2 agonist CAY10583. BLT2 is a promising target for diabetic wound healing and gastrointestinal lesions. BLT2 probe 1 is suitable to investigate the pharmacology of BLT2 receptor ligands in a variety of assay systems.
  • HY-B1103
    Hydroxyhexamide

    (±)-Hydroxyhexamid

    Drug Metabolite Cardiovascular Disease
    Hydroxyhexamide is a pharmacologically active metabolite of Acetohexamide, used as a hypoglycemic agents.
  • HY-N2128
    Nigakinone

    Others Inflammation/Immunology
    Nigakinone is one of the most abundant alkaloids responsible for the major pharmacological activities of Kumu.
  • HY-N0850
    Benzoylhypaconine

    Benzoylhypacoitine

    Others Neurological Disease
    Benzoylhypaconine (Benzoylhypacoitine) is a monoester Aconitum alkaloid, is the main pharmacologic and toxic component.
  • HY-108886
    JWG-071

    ERK Cancer
    JWG-071 is the first reported kinase-selective chemical probe for ERK5. JWG-071 improves ERK5 activity and BRD4 selectivity. JWG-071 will be a much-needed chemical probe for deconvoluting ERK5 and BRD4 pharmacology.
  • HY-B0103
    Fluvoxamine

    DU-23000

    Serotonin Transporter Neurological Disease
    Fluvoxamine (DU-23000) is an antidepressant which functions pharmacologically as a selective serotonin reuptake inhibitor.
  • HY-B0103A
    Fluvoxamine maleate

    DU-23000 maleate

    Serotonin Transporter Neurological Disease
    Fluvoxamine maleate (DU-23000 maleate) is an antidepressant which functions pharmacologically as a selective serotonin reuptake inhibitor.
  • HY-N3171A
    (+)-Nortrachelogenin

    Wikstromol

    Apoptosis PI3K Cancer
    (+)-Nortrachelogenin (Wikstromol), a pharmacologically ligand from from wikstroemia indica, possesses antileukemic activity.
  • HY-N5029
    Isofebrifugine

    Parasite Infection
    Isofebrifugine is a natural quinazolinone alkaloid with important physiological activities and good pharmacological effects. Antimalarial effect.
  • HY-76225
    Ammonium glycyrrhizinate

    Monoammonium glycyrrhizinate; Glycyrrhizic acid ammonium salt; Ammonium glycyrrhizate

    Others Inflammation/Immunology
    Ammonium glycyrrhizinate (Monoammonium glycyrrhizinate) has various pharmacological actions such as anti-inflammatory, antiallergic, antigastriculcer, and antihepatitis activities.
  • HY-U00192
    CGP11952

    GABA Receptor Neurological Disease
    CGP11952 is a triazolyl-Benzaphenon resembling the benzodiazepines in its pharmacological action. CGP11952 is an experimental benzodiazepine derivative.
  • HY-B1307
    Zoxazolamine

    Cytochrome P450 Neurological Disease
    Zoxazolamine is widely used for a pharmacologic test that serves as a convenient indicator of changes in cytochrome P-450 activity in rodents.
  • HY-128777
    WEHI-9625

    VDAC Apoptosis Cancer
    WEHI-9625 is a tricyclic sulfone, first-in-class inhibitor of apoptosis with an EC50 of 69 nM. WEHI-9625 binds to VDAC2 and promotes its ability to inhibit apoptosis driven by mouse BAK. WEHI-9625 is completely inactive against both human BAK and the closely related apoptosis effector BAX.
  • HY-W106234
    4-(Phenyldiazenyl)benzoic acid

    TRP Channel Others
    4-(Phenyldiazenyl)benzoic acid is a photosensitive and photoswitchable TRPA1 agonist that can be used as pharmacological tools for study of pain signaling.
  • HY-N0657
    Pinoresinol Diglucoside

    Others Others
    Pinoresinol Diglucoside is one of the major lignans with various pharmacological activities which could be isolated from Duzhong and other plant species.
  • HY-14829
    Afegostat

    D-Isofagomine; Isofagomine

    Glucosidase Neurological Disease
    Afegostat is a pharmacological chaperone, which specifically and reversibly binds acid-β-glucosidase (GCase) in the endoplasmic reticulum (ER) with high affinity.
  • HY-U00116
    GP531

    Adenosine Receptor Cardiovascular Disease
    GP531 is a potent, second-generation adenosine regulating agent, is pharmacologically silent under basal conditions but increases localized endogenous adenosine during ischemia.
  • HY-20584
    10-Deacetyl-7-xylosyl paclitaxel

    10-Deacetyl-7-xylosyltaxol; 10-Deacetylpaclitaxel 7-Xyloside; 10-Deacetyltaxol 7-Xyloside

    Microtubule/Tubulin ADC Cytotoxin Cancer
    10-Deacetyl-7-xylosyl paclitaxel is a Paclitaxel (a microtubule stabilizing agent; enhances tubulin polymerization) derivative with improved pharmacological features.
  • HY-N0709
    Coumarin

    Influenza Virus Cancer Infection Inflammation/Immunology
    Coumarin is the primary bioactive ingredient in Radix Glehniae, named Beishashen in China, which possesses many pharmacological activities, including anticancer, anti-inflammation and antivirus activities.
  • HY-N0105
    Rhein

    Rheic Acid; Rhubarb yellow; Monorhein

    Autophagy Reactive Oxygen Species Bacterial Cancer Infection Inflammation/Immunology
    Rhein is a lipophilic anthraquinone extensively found in medicinal herbs, and has many pharmacological effects, including epatoprotective, nephroprotective, anti-inflammatory, antioxidant, anticancer, and antimicrobial activities.
  • HY-14829E
    Afegostat D-Tartrate

    D-Isofagomine D-Tartrate; Isofagomine D-Tartrate

    Glucosidase Neurological Disease
    Afegostat D-Tartrate is a pharmacological chaperone, which specifically and reversibly binds acid-β-glucosidase (GCase) in the endoplasmic reticulum (ER) with high affinity.
  • HY-100032
    PD 117519

    CI947

    Adenosine Receptor Neurological Disease
    PD 117519 (CI947) is an A2A adenosine agonist which has shown oral antihypertensive activity in pharmacological animal models.
  • HY-135331
    N-Desmethyl-Apalutamide

    Androgen Receptor Cytochrome P450 Cancer
    N-Desmethyl Apalutamide is an active metabolite of Apalutamide. N-Desmethyl Apalutamide is a less potent antagonist of the androgen receptor and is responsible for one-third of the activity of Apalutamide. The formation of N-Desmethyl Apalutamide mediated predominantly by CYP2C8 and CYP3A4. N-Desmethyl Apalutamide is moderate to strong CYP3A4 and CYP2B6 inducer and has an excellent plasma-proteins bound concentration.
  • HY-30152
    Xanthotoxol

    8-Hydroxypsoralen

    5-HT Receptor Reactive Oxygen Species Endogenous Metabolite Inflammation/Immunology Neurological Disease
    Xanthotoxol (8-Hydroxypsoralen) is a biologically active linear furocoumarin, shows strong pharmacological activities as anti-inflammatory, antioxidant, 5-HT antagonistic, and neuroprotective effects.
  • HY-N6881
    Gypenoside XIII

    Others Cardiovascular Disease
    Gypenoside XIII is belonging to the gypenosides. Gypenosides, extracted from Gynostemma pentaphyllum, have various pharmacological properties and protect against cardiovascular diseases, especially atherosclerosis.
  • HY-N0697
    Crocin

    Crocin I

    Endogenous Metabolite Cancer Inflammation/Immunology Neurological Disease
    Crocin (Crocin I) is a nutraceutical and the main constituent isolated from the stigmas of Crocus sativus with immense pharmacological properties as anti-inflammatory, anticancer, antidepressant and anticonvulsant.
  • HY-136232
    PSEM 308 hydrochloride

    Others Neurological Disease
    PSEM 308 hydrochloride is a pharmacologically selective actuator module (PSAM) agonist. PSEM 308 Activates PSAML141F-GlyR chimeric ion channels.
  • HY-N2064
    Racanisodamine

    mAChR Neurological Disease
    Racanisodamine is one of the racemic isomers of anisodamine, resembles anisodamine in pharmacological effect. Racanisodamine is a non-selective muscarinic antagonist, used as a component of eye drops for myopic control.
  • HY-N2558
    Murrayone

    Others Cancer
    Murrayone, a coumarin-containing compound extracted from M. paniculata, is the most bioactive substance in this species and is a cancer metastasis chemopreventive agent based on its unique pharmacological properties.
  • HY-101347
    Chlorisondamine diiodide

    nAChR Neurological Disease
    Chlorisondamine (diiodide) is a potent nicotinic acetylcholine receptor (nAChR) antagonist and a ganglion blocker. Chlorisondamine antagonizes some of nicotine's central actions in a potent, long-lasting and pharmacologically selective way.
  • HY-128380
    Dibenamine hydrochloride

    N-​(2-​Chloroethyl)​dibenzylamine hydrochloride

    Adrenergic Receptor Metabolic Disease
    Dibenamine hydrochloride is a competitive and irreversible adrenergic blocking agent and is known to modify the pharmacological effects of epinephrine. Dibenamine hydrochloride cause a significant increase in the rate of destruction of I-epinephrine in the mouse.
  • HY-N4232
    Clematichinenoside AR

    Autophagy Inflammation/Immunology
    Clematichinenoside AR is a major active ingredient that could be extracted from the traditional Chinese herb Clematis chinensis and has potent pharmacological effects on various diseases, including atherosclerosis (AS).
  • HY-D1398
    LtIA-F

    nAChR Neurological Disease
    LtIA-F, a novel fluorescent analogue of LtIA, provides a wealth of pharmacological tools to explore the structure–function relationship, distribution, and ligand binding domain of the α3β2 nAChR subtype.
  • HY-16636
    ML337

    mGluR Neurological Disease
    ML337 is a selective and brain-penetrant negative allosteric modulator of mGlu3, with an IC50 of 593 nM. ML337 possesses a favorable dystrophia myotonica protein kinase (DMPK) and ancillary pharmacology profile.
  • HY-Y1129
    3-Hydroxypyridine

    Others Others
    3-Hydroxypyridine is isolated from Bamboo grass. 3-Hydroxypyridine derivatives are structural analogues of vitamin B6 and have a wide range of pharmacological properties, such as antioxidant properties.
  • HY-B0103AS1
    Fluvoxamine-d4 maleate

    DU-23000-d4 maleate

    Serotonin Transporter Neurological Disease
    Fluvoxamine-d4 (DU-23000-d4) maleate is the deuterium labeled Fluvoxamine maleate. Fluvoxamine maleate (DU-23000 maleate) is an antidepressant which functions pharmacologically as a selective serotonin reuptake inhibitor.
  • HY-N6054
    Niranthin

    Parasite Topoisomerase Infection Inflammation/Immunology
    Niranthin, a lignan with a wide spectrum of pharmacological activities. Niranthin is a potent and non-competitive inhibitor of heterodimeric type IB topoisomerase of L. donovani. Niranthin can be used for the research of drug-resistant leishmaniasis treatment.
  • HY-N1422
    Hecogenin

    Fungal Infection Inflammation/Immunology
    Hecogenin is a steroid saponin isolated from Agave sisalana and is a selective inhibitor of human UDP-glucuronosyltransferases. Hecogenin has a wide spectrum of pharmacological activities, including anti-inflammatory, antifungal and gastroprotective effects.
  • HY-121054
    Chalcone

    Bacterial Cancer Inflammation/Immunology
    Chalcone is isolated from Glycyrrhizae inflata and used to synthesize chalcone derivatives. Chalcone derivatives possess varied biological and pharmacological activity, including anti-inflammatory, antioxidative, antibacterial, anticancer, and anti-parasitic activities.
  • HY-105917
    Endovion

    NS3728

    Chloride Channel Others
    Endovion (NS3728) is a pharmacological anion channel inhibitor (like chloride channel) and the specific VRAC/VSOAC blocker. Endovion (NS3728) is also an Anoctamin-1 (ANO 1) channel inhibitor.
  • HY-17642
    Omidenepag

    Prostaglandin Receptor Endocrinology
    Omidenepag,a pharmacologically active form of Omidenepag Isopropyl, is a selective, non-prostanoid EP2 receptor agonist, with an EC50 of 1.1 nM. Omidenepag shows binding affinities (IC50) 10 nM for h-EP2.
  • HY-N2174
    Ophiogenin 3-O-α-L-rhamnopyranosyl-(1→2)-β-D-glucopyranoside

    Others Cardiovascular Disease
    Ophiogenin 3-O-α-L-rhamnopyranosyl-(1→2)-β-D-glucopyranoside, a terpenoid glycoside from Ophiopogon japonicus roots, has good pharmacological effects on the cardiovascular system.
  • HY-B1178A
    R-(+)-Cotinine

    (+)-Cotinine; (R)-Cotinine; (R)-NIH-10498

    Others Neurological Disease
    R-(+)-Cotinine ((+)-Cotinine), a Nicotine metabolite, lacks significant activity across a wide range of pharmacological targets. R-(+)-Cotinine can enhance the Ach-evoked current in human α7 nAChRs.
  • HY-N0709S
    Coumarin-d4

    Influenza Virus Cancer Infection Inflammation/Immunology
    Coumarin-d4 is the deuterium labeled Coumarin. Coumarin is the primary bioactive ingredient in Radix Glehniae, named Beishashen in China, which possesses many pharmacological activities, including anticancer, anti-inflammation and antivirus activities.
  • HY-N2575
    Hypocrellin A

    PKC Bacterial Parasite Cancer Infection
    Hypocrellin A, a naturally occurring PKC inhibitor, has many biological and pharmacological properties, such as antitumour, antiviral, antibacterial, and antileishmanial activities. Hypocrellin A is a promising photosensitizer for anticancer photodynamic therapy (PDT).
  • HY-N0064
    Macelignan

    (+)-Anwulignan; Anwuligan

    COX Cancer Metabolic Disease Inflammation/Immunology Neurological Disease
    Macelignan ((+)-Anwulignan; Anwuligan) is an orally active lignan isolated from Myristica fragrans. Macelignan possesses many pharmacological activities, including anti-inflammatory, anti-cancer, anti-diabetes, and neuroprotective activities.
  • HY-132882
    ARN19689

    Others Inflammation/Immunology
    ARN19689 is a potent, selective, orally active and non-covalent inhibitor of N‑Acylethanolamine-Hydrolyzing Acid Amidase (NAAA), with an IC50 of 42 nM. ARN19689 is a promising pharmacological tool to be further investigated in the field of inflammatory conditions.
  • HY-17599
    Piperazine citrate

    1,4-Diazacyclohexane citrate

    GABA Receptor Infection
    Piperazine (1,4-Diazacyclohexane) citrate is a gamma-aminobutyric acid (GABA) agonist. Piperazine citrate is a vital building block and is an essential core in numerous marketed drugs with diverse pharmacological activities.
  • HY-13633
    Exisulind

    Aldose Reductase Metabolic Disease
    Exisulind is an inactive metabolite of the nonsteroidal, anti-inflammatory agent sulindac. Exisulind inhibits aldose reductase with an IC50 of 367 nM in vitro and may contribute to the beneficial pharmacological effects of sulindac on type 2 diabetic complications.
  • HY-12324
    SB269652

    Dopamine Receptor Neurological Disease
    SB269652 is the first drug-like allosteric modulator of the dopamine D2 receptor (D2R); a new chemical probe that can differentiate D2R monomers from dimers or oligomers depending on the observed pharmacology.
  • HY-N1984
    Artemisic acid

    Qing Hao acid; Artemisinic acid; Arteannuic acid

    Bacterial Cancer Infection Metabolic Disease Inflammation/Immunology
    Artemisinic acid (Qing Hao acid), an amorphane sesquiterpene isolated from Artemisia annua L., possesses a variety of pharmacological activity, such as antimalarial activity, anti-tumor activity, antipyretic effect, antibacterial activity, allelopathy effect and anti-adipogenesis effect.
  • HY-N1214
    Squalene

    Super Squalene; trans-Squalene; AddaVax

    Endogenous Metabolite Reactive Oxygen Species Fungal Infection Cardiovascular Disease
    Squalene is an intermediate product in the synthesis of cholesterol, and shows several pharmacological properties such as hypolipidemic, hepatoprotective, cardioprotective, antioxidant, and antitoxicant activity. Squalene also has anti-fungal activity and can be used for the research of Trichophyton mentagrophytes treatment.
  • HY-103413
    Eticlopride hydrochloride

    Dopamine Receptor Neurological Disease
    Eticlopride hydrochloride, a selective dopamine D2‐like receptor antagonist, exhibits high affinity for dopamine D2, α1‐adrenergic, α2‐adrenergic, 5HT1, 5HT2 receptors with Kis of 0.09, 112, 699, 6220, and 830 nM, respectively. Antipsychotic agent.
  • HY-N6181
    Terrelumamide A

    Others Endocrinology
    Terrelumamide A is a lumazine-containing peptide. Terrelumamide A is isolated from the culture broth of the marine-derived fungus Aspergillus terreus. Terrelumamide A exhibits pharmacological activity by improving insulin sensitivity. Terrelumamide A has the potential in the application of DNA sequence recognition.
  • HY-114412A
    TD-0212 TFA

    Angiotensin Receptor Neprilysin Inflammation/Immunology
    TD-0212 TFA is an orally active dual pharmacology angiotensin II type 1 receptor (AT1) antagonist and neprilysin (NEP) inhibitor, with a pKi of 8.9 for AT1 and a pIC50 of 9.2 for NEP.
  • HY-N7765
    Oenothein B

    HCV Bacterial Apoptosis Fungal Cancer Infection Inflammation/Immunology
    Oenothein B is a dimeric macrocyclic ellagitannin and has widely pharmacological activities, including antioxidant, anti-inflammatory, antifungal, anti-HCV, and antitumor properties. Oenothein B is a potent and specific inhibitor of poly(ADP-ribose) glycohydrolase.
  • HY-15895
    Aprocitentan

    ACT-132577

    Endothelin Receptor Cardiovascular Disease Endocrinology
    Aprocitentan (ACT-132577) is the major and pharmacologically active metabolite of Macitentan. Aprocitentan is dual ETA/ETB antagonist with IC50s of 3.4 nM and 987 nM, and pA2 valus of 6.7 and 5.5, respectively.
  • HY-N0380
    Nardosinone

    Others Neurological Disease
    Nardosinone, isolated from Nardostachys chinensis, is the first enhancer of the neuritogenic action of dbcAMP and staurosporine. Nardosinone may become a useful pharmacological tool for studying the mechanism of action of not only nerve growth factor (NGF) but also both the neuritogenic substances.
  • HY-114412
    TD-0212

    Angiotensin Receptor Neprilysin Inflammation/Immunology Endocrinology
    TD-0212 (compound 35) is an orally active dual pharmacology angiotensin II type 1 receptor (AT1) antagonist and neprilysin (NEP) inhibitor, with a pKi of 8.9 for AT1 and a pIC50 of 9.2 for NEP.
  • HY-N2590
    Lupenone

    Parasite Cancer Infection Inflammation/Immunology
    Lupenone, isolated from Rhizoma Musae, belongs to lupane type triterpenoids. Lupenone shows various pharmacological activities including anti-inflammatory, anti-virus, anti-diabetes, anti-cancer, improving Chagas disease without major toxicity.
  • HY-B1558
    Bifemelane

    MCI-2016 free base

    Calcium Channel Neurological Disease
    Bifemelane is a nootropic compound. Bifemelan causes the first peak by stimulating release from intracellular Ca 2+ stores and the second by capacitive entry through store–operated Ca 2+ channels. Bifemelane will be provided as a pharmacological tool for basic studies on astrocytes.
  • HY-N0013
    Vitexin

    Others Cancer Metabolic Disease Neurological Disease Cardiovascular Disease
    Vitexin is a c-glycosylated flavone, and is found in various medicinal plants species such as Ficus deltoid and Spirodela polyrhiza. Vitexin has a wide range of pharmacological effects, including anti-oxidant, anti-cancer, anti-inflammatory, anti-hyperalgesic, and neuroprotective effects.
  • HY-19675
    Naproxen etemesil

    LT-NS 001; MX 1094

    COX Inflammation/Immunology
    Naproxen etemesil is a lipophilic, non-acidic, inactive prodrug of naproxen that is hydrolysed to pharmacologically active Naproxen once absorbed. Naproxen is a COX-1 and COX-2 inhibitor with IC50s of 8.72 and 5.15 μM, respectively in cell assay.
  • 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-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-F0004
    β-Nicotinamide mononucleotide

    β-NM; NMN

    Endogenous Metabolite Cancer Neurological Disease
    β-nicotinamide mononucleotide (β-NM) is a product of the nicotinamide phosphoribosyltransferase (NAMPT) reaction and a key NAD + intermediate. The pharmacological activities of β-nicotinamide mononucleotide include its role in cellular biochemical functions, cardioprotection, diabetes, Alzheimer's disease, and complications associated with obesity.
  • HY-N7044
    Vitexin arginine

    Others Cancer Metabolic Disease Neurological Disease Cardiovascular Disease
    Vitexin arginine is a c-glycosylated flavone, and is found in various medicinal plants species such as Ficus deltoid and Spirodela polyrhiza. Vitexin arginine has a wide range of pharmacological effects, including anti-oxidant, anti-cancer, anti-inflammatory, anti-hyperalgesic, and neuroprotective effects.
  • HY-12023
    GTx-007

    S-4

    Androgen Receptor Cancer
    GTx-007 (S-4) is an orally active and selective nonsteroidal androgen receptor (AR) modulator (SARM) and a partial agonist, with Ki of 4 nM. GTx-007 (S-4) is identified as SARMs with potent and tissue-selective in vivo pharmacological activity.
  • HY-B1125
    Glucosamine

    D-Glucosamine; Chitosamine

    Endogenous Metabolite Reactive Oxygen Species HIF/HIF Prolyl-Hydroxylase Autophagy Inflammation/Immunology
    Glucosamine (D-Glucosamine) is an amino sugar and a prominent precursor in the biochemical synthesis of glycosylated proteins and lipids, is used as a dietary supplement. Glucosamine also is a natural constituent of glycosaminoglycans in the cartilage matrix and synovial fluid, which when administered exogenously, exerts pharmacological effects on osteoarthritic cartilage and chondrocytes.
  • HY-N0733
    Glucosamine hydrochloride

    D-(+)-Glucosamine hydrochloride; Chitosamine hydrochloride

    Endogenous Metabolite Reactive Oxygen Species HIF/HIF Prolyl-Hydroxylase Autophagy Inflammation/Immunology Cancer
    Glucosamine hydrochloride (D-Glucosamine hydrochloride) is an amino sugar and a prominent precursor in the biochemical synthesis of glycosylated proteins and lipids, is used as a dietary supplement. Glucosamine hydrochloride also is a natural constituent of glycosaminoglycans in the cartilage matrix and synovial fluid, which when administered exogenously, exerts pharmacological effects on osteoarthritic cartilage and chondrocytes.
  • HY-121385S
    Hydroxy Bosentan-d6

    Ro 48-5033-d6

    Endogenous Metabolite Cardiovascular Disease
    Hydroxy Bosentan-d6 is deuterium labeled Hydroxy bosentan. Hydroxy bosentan (Ro 48-5033) is a primary metabolite of Bosentan (BOS) metabolized by the cytochrome P450 system in the liver. Ro 48-5033 assists BOS pharmacologically, retaining 10%-20% activities.
  • HY-121385S1
    Hydroxy Bosentan-d4

    Ro 48-5033-d4

    Endogenous Metabolite Cardiovascular Disease
    Hydroxy Bosentan-d4 is deuterium labeled Hydroxy bosentan. Hydroxy bosentan (Ro 48-5033) is a primary metabolite of Bosentan (BOS) metabolized by the cytochrome P450 system in the liver. Ro 48-5033 assists BOS pharmacologically, retaining 10%-20% activities.
  • HY-117426
    MO-I-500

    Others Cancer
    MO-I-500 is a pharmacological of FTO inhibitor with an IC50 of 8.7 μM for the inhibition of purified FTO demethylase catalyzing demethylation of an artificial small methylated substrate. MO-I-500 can be used for the research of rare panresistant triple-negative inflammatory breast cancer.
  • HY-W033577
    Tricarbonyldichlororuthenium(II) dimer

    CORM-2

    Others Inflammation/Immunology
    Tricarbonyldichlororuthenium(II) dimer is a pharmacological donor of CO releasing. CO releases from Tricarbonyldichlororuthenium(II) dimer prevents gastric mucosal oxidative damage induced by ischemia/reperfusion (I/R) improving gastric blood flow (GBF), decreasing DNA oxidation and inflammatory response on systemic level.
  • HY-103111
    MMPIP hydrochloride

    mGluR Neurological Disease
    MMPIP hydrochloride is an allosteric metabotropic glutamate receptor 7 (mGluR7) selective antagonist (KB values 24 -30 nM). MMPIP hydrochloride acts as a pharmacological tool for elucidating the roles of mGluR7 on central nervous system functions. MMPIP hydrochloride alleviates pain and normalizes affective and cognitive behavior in neuropathic mice.
  • HY-107503
    MMPIP

    mGluR Neurological Disease
    MMPIP is an allosteric metabotropic glutamate receptor 7 (mGluR7) selective antagonist (KB values 24 -30 nM). MMPIP acts as a pharmacological tool for elucidating the roles of mGluR7 on central nervous system functions. MMPIP alleviates pain and normalizes affective and cognitive behavior in neuropathic mice.
  • HY-119917
    Gossypetin

    p38 MAPK MEK Bacterial Cancer Infection
    Gossypetin is a hexahydroxylated flavonoid and is a potent mitogen-activated protein kinase kinase (MKK)3 and MKK6 inhibitor with strongly attenuates the MKK3/6-p38 signaling pathway, has various pharmacological activities, including antioxidant, antibacterial and anticancer activities.
  • HY-N0487
    Glucosamine sulfate

    D-Glucosamine sulfate

    Endogenous Metabolite Reactive Oxygen Species HIF/HIF Prolyl-Hydroxylase Autophagy Inflammation/Immunology Cancer
    Glucosamine sulfate (D-Glucosamine sulfate) is an amino sugar and a prominent precursor in the biochemical synthesis of glycosylated proteins and lipids, is used as a dietary supplement. Glucosamine sulfate also is a natural constituent of glycosaminoglycans in the cartilage matrix and synovial fluid, which when administered exogenously, exerts pharmacological effects on osteoarthritic cartilage and chondrocytes.
  • HY-123054
    BTSA1

    Bcl-2 Family Apoptosis Cancer
    BTSA1 is a potent, high affinity and orally active BAX activator with an IC50 of 250 nM and an EC50 of 144 nM. BTSA1 binds with high affinity and specificity to the N-terminal activation site and induces conformational changes to BAX leading to BAX-mediated apoptosis.
  • HY-W001160
    5-Hydroxyindole

    Endogenous Metabolite Others
    5-Hydroxyindole, a hydroxylated indole, can be found in a vast array of pharmacologically active agents and natural products. 5-Hydroxyindole slows desensitization of the 5-HT3 receptor-mediated ion current in N1E-115 neuroblastoma cells.
  • HY-N2208
    4-Hydroxylonchocarpin

    p38 MAPK Cancer Infection Metabolic Disease Inflammation/Immunology
    4-Hydroxylonchocarpin is a chalcone compound from an extract of Psoralea corylifolia. 4-Hydroxylonchocarpin increases phosphorylation of p38 MAPK, JNK and ERK. 4-Hydroxylonchocarpin has diverse pharmacological activities, including antibacterial, antifungal, anticancer, antireverse transcriptase, antitubercular, antimalarial, anti-inflammatory and antioxidant activities.
  • HY-N2292
    Kinsenoside

    Keap1-Nrf2 Apoptosis Inflammation/Immunology
    Kinsenoside is a main active component isolated from plants of the genus Anoectochilus, and exhibits many biological activities and pharmacological effects. Kinsenoside rescues the nucleus pulposus cells (NPCs) viability under oxidative stress and protects against apoptosis, senescence and mitochondrial dysfunction in a Nrf2-dependent way.
  • HY-N0005S
    Curcumin-d6

    Diferuloylmethane-d6; Natural Yellow 3-d6; Turmeric yellow-d6

    Keap1-Nrf2 Ferroptosis Autophagy Histone Acetyltransferase Epigenetic Reader Domain Mitophagy Influenza Virus Infection Metabolic Disease Inflammation/Immunology
    Curcumin D6 (Diferuloylmethane D6) is a deuterium labeled Curcumin (Turmeric yellow). Curcumin (Turmeric yellow) is a natural phenolic compound with diverse pharmacologic effects including anti-inflammatory, antioxidant, antiproliferative and antiangiogenic activities. Curcumin is an inhibitor of p300 histone acetylatransferase (HATs) and also shows inhibitory effects on NF-κB and MAPKs.
  • HY-N0240
    Herbacetin

    Others Cancer
    Herbacetin is a natural flavonoid from flaxseed, exerts various pharmacological activities, including antioxidant, anti-inflammatory and anticancer effects. Herbacetin is an Ornithine decarboxylase (ODC) allosteric inhibitor, directly binds to Asp44, Asp243, and Glu384 on ODC. Ornithine decarboxylase (ODC) is a rate-limiting enzyme in the first step of polyamine biosynthesis.
  • HY-16023B
    (Rac)-Acolbifene

    EM-343; (Rac)-EM-652

    Estrogen Receptor/ERR Cancer
    (Rac)-Acolbifene (EM-343; (Rac)-EM-652) is the racemic form of EM652 (estrogen receptor antagonist), has anti-estrogenic and estrogenic activities. (Rac)-Acolbifene (EM-343; (Rac)-EM-652) contains a piperidine ring, shows good pharmacological profile,relative binding affinity (RBA)=380.
  • HY-N2499
    Dehydrotumulosic acid

    Others Metabolic Disease
    Dehydrotumulosic acid is one of the effective constituents of Poria cocos. Poria cocos, a popular Chinese medicinal herb of fungal origin, has been included in many combinations with other CM herbs for its traditionally claimed activities of inducing diuresis, excreting dampness, invigorating the spleen and tranquilizing the mind and its modern pharmacological use of modulating the immune system of the body.
  • HY-114372
    Lycopodine

    Lipoxygenase Caspase Apoptosis Cancer
    Lycopodine, a pharmacologically important bioactive component derived from Lycopodium clavatumspores, triggers apoptosis by modulating 5-lipoxygenase, and depolarizing mitochondrial membrane potential in refractory prostate cancer cells without modulating p53 activity. Lycopodine inhibits proliferation of HeLa cells through induction of apoptosis via caspase-3 activation.
  • HY-N0104
    Curcumol

    (-)-Curcumol

    Apoptosis Cancer
    Curcumol ((-)-Curcumol), a bioactive sesquiterpenoid, possesses numerous pharmacological activities like anticancer, antimicrobial, antifungal, antiviral, and antiinflammatory. Curcumol is a potent inducer of apoptosis in numerous cancer cells via targeting key signaling pathways as MAPK/ERK, PI3K/Akt and NF-κB which are generally deregulated in several cancers.
  • HY-B0387A
    Ibutilide

    U70226E free base

    Potassium Channel Cardiovascular Disease
    Ibutilide (U70226E free base), an action potential-prolonging antiarrhythmic, is a potent blocker of the rapidly activating delayed rectifier K + current (IKr) in AT-1 cells.
  • HY-100359
    CL-82198

    MMP Cancer Inflammation/Immunology
    CL-82198 is a selective inhibitor of MMP-13. CL-82198 binds to the entire S1’ pocket of MMP-13, which is the basis for its selectivity towards MMP-13 and the lack of inhibitory activities against other MMPs. CL-82198 is a pharmacologic treatment for preventing osteoarthritis (OA) progression.
  • HY-13200A
    BRL-15572 hydrochloride

    5-HT Receptor Neurological Disease
    BRL-15572 hydrochloride is a selective antagonist of h5-HT1D, displays high affinity for h5-HT1D receptors. BRL-15572 hydrochloride could be useful pharmacological agents to characterise 5-HT1D receptor mediated responses.
  • HY-115914
    Lipid-lowering agent-1

    Others Others
    Lipid-lowering agent-1 is a potent lipid-lowering agent. Lipid-lowering agent-1 has significant pharmacological effects on the inhibition of low-density lipoprotein cholesterol (LDLC) and promotion of high-density lipoprotein cholesterol (HDLC) production. Lipid-lowering agent-1 shows potent hypolipidemic effect in high-fat diet rats.
  • HY-147547
    SV5

    Amyloid-β Neurological Disease
    SV5 is a potent anti-Alzheimer agent. SV5 can significantly protect SHSY-5Y cells against 1-42-induced death. SV5 shows moderate antioxidant and good neuroprotective activities. SV5 shows the high stability in human plasma and the best pharmacological profile.
  • HY-N9093
    (3R,5R)-3,5-Diacetoxy-1-(3,4-dihydroxyphenyl)-7-(4-hydroxyphenyl)heptane

    Others Cancer Inflammation/Immunology
    (3R,5R)-3,5-Diacetoxy-1-(3,4-dihydroxyphenyl)-7-(4-hydroxyphenyl)heptane, a diarylheptanoid from the rhizomes of Curcuma kwangsiensis, possesses a variety of biological and pharmacological activities including antioxidant, antihepa totoxic, anti-inflammatory, antiproliferative, antiemetic, and antitumor activities.
  • HY-13200
    BRL-15572 dihydrochloride

    5-HT Receptor Neurological Disease
    BRL-15572 dihydrochloride is a selective antagonist of h5-HT1D, displays high affinity for h5-HT1D receptors. BRL-15572 dihydrochloride could be useful pharmacological agents to characterise 5-HT1D receptor mediated responses.
  • HY-N7255
    Cycloartenol

    p38 MAPK Apoptosis Cancer
    Cycloartenol, a phytosterol compound, is one of the key precusor substances for biosynthesis of numerous sterol compounds. Cycloartenol inhibits the migration of glioma cells and suppresses the phosphorylation of the p38 MAP kinase. Cycloartenol has a variety of pharmacological activities such as anti-inflammatory, anti-tumor, antioxidant, antibiosis and anti-alzheimer's disease. Cycloartenol also plays an important role in the process of plant growth and development.
  • HY-76569
    Desfesoterodine

    PNU-200577; 5-Hydroxymethyl Tolterodine

    mAChR Neurological Disease
    Desfesoterodine (PNU-200577) is a potent and selective muscarinic receptor (mAChR) antagonist with a KB and a pA2 of 0.84 nM and 9.14, respectively. Desfesoterodine is a major pharmacologically active metabolite of Tolterodine (PNU-200583; HY-A0024) and Fesoterodine (HY-70053). Desfesoterodine improves cerebral infarction induced detrusor overactivity in rats.
  • HY-123671
    CYM2503

    Neuropeptide Y Receptor Neurological Disease
    CYM2503 is a putative GalR2-positive allosteric modulator. CYM2503 increases the latency to first electrographic seizure and decreases the total time in seizure. CYM2503 also attenuates electroshock-induced seizures in mice. Galanin receptors type 1 (GalR1) and/or type 2 (GalR2) represent unique pharmacological targets for the research of seizures and epilepsy.
  • HY-B0387
    Ibutilide fumarate

    U70226E

    Potassium Channel Cardiovascular Disease
    Ibutilide (U70226E) fumarate, an action potential-prolonging antiarrhythmic, is a potent blocker of the rapidly activating delayed rectifier K + current (IKr) in AT-1 cells.
  • HY-12445
    CDKI-73

    LS-007

    CDK Apoptosis Cancer Inflammation/Immunology
    CDKI-73 (LS-007) is an orally active and highly efficacious CDK9 inhibitor, with Ki values of 4 nM, 4 nM and 3 nM for CDK9, CDK1 and CDK2, respectively. CDKI-73 down-regulates the RNAPII phosphorylation. CDKI-73 is also a novel pharmacological inhibitor of Rab11 cargo delivery and innate immune secretion.
  • HY-101293
    VU0359595

    CID-53361951; ML-270

    Phospholipase Fungal Cancer Infection Metabolic Disease Inflammation/Immunology Neurological Disease
    VU0359595 (CID-53361951; ML-270) is a potent and selective pharmacological phospholipase D1 (PLD1) inhibitor with an IC50 of 3.7 nM. VU0359595 is >1700-fold selective for PLD1 over PLD2 (IC50 of 6.4 μM). VU0359595 can be used for the research of cancer, diabetes, neurodegenerative and inflammatory diseases.
  • HY-135774
    6-Hydroxybenzbromarone

    Drug Metabolite Phosphatase Cardiovascular Disease
    6-Hydroxybenzbromarone is the major metabolite of Benzbromarone with a longer half-life and greater pharmacological potency than the parent compound. 6-Hydroxybenzbromarone is a protein Eyes Absent 3 (EYA3) inhibitor with an IC50 value of 21.5 μM. 6-Hydroxybenzbromarone is an angiogenic agent, has strong inhibitory effects on cell migration, tubulogenesis, and angiogenic sprouting.
  • HY-P1410
    GsMTx4

    TRP Channel Piezo Channel Inflammation/Immunology Neurological Disease Cardiovascular Disease
    GsMTx4 is a spider venom peptide that selectively inhibits cationic-permeable mechanosensitive channels (MSCs) belonging to the Piezo and TRP channel families. GsMTx4 also blocks cation-selective stretch-activated channels (SACs) , attenuates lysophosphatidylcholine (LPC)-induced astrocyte toxicity and microglial reactivity. GsMTx4 is an important pharmacological tool for identifying the role of these excitatory MSCs in normal physiology and pathology.
  • HY-F0004S
    β-Nicotinamide mononucleotide-d4

    β-NM-d4; NMN-d4

    Endogenous Metabolite Cancer Neurological Disease
    β-Nicotinamide mononucleotide-d4 (β-NM-d4) is the deuterium labeled β-Nicotinamide mononucleotide. β-nicotinamide mononucleotide (β-NM) is a product of the nicotinamide phosphoribosyltransferase (NAMPT) reaction and a key NAD + intermediate. The pharmacological activities of β-nicotinamide mononucleotide include its role in cellular biochemical functions, cardioprotection, diabetes, Alzheimer's disease, and complications associated with obesity.
  • HY-106975
    SCH-42354

    Neprilysin Cardiovascular Disease
    SCH-42354 is a potent, orally active neutral endopeptidase (NEP) inhibitor, is the pharmacologically active form of the prodrug SCH-42495. SCH-42354 inhibits the hydrolysis of NEP to enhance the activity of atrial natriuretic peptide (ANP). SCH-42354 inhibits hydrolysis of leu-enkephalin and ANF with IC50 values of 8.3 nM and 10.0 nM, respectively. SCH-42354 has antihypertensive activity.
  • HY-P1410A
    GsMTx4 TFA

    TRP Channel Piezo Channel Inflammation/Immunology Neurological Disease Cardiovascular Disease
    GsMTx4 TFA is a spider venom peptide that selectively inhibits cationic-permeable mechanosensitive channels (MSCs) belonging to the Piezo and TRP channel families. GsMTx4 TFA also blocks cation-selective stretch-activated channels (SACs) , attenuates lysophosphatidylcholine (LPC)-induced astrocyte toxicity and microglial reactivity. GsMTx4 TFA is an important pharmacological tool for identifying the role of these excitatory MSCs in normal physiology and pathology.
  • HY-124745
    KY-05009

    MAP4K Wnt Apoptosis Cancer
    KY-05009 is an ATP-competitive Traf2- and Nck-interacting kinase (TNIK) inhibitor with a Ki of 100 nM. KY-05009 pharmacologically inhibits TGF-β1-induced epithelial-to-mesenchymal transition (EMT) in human lung adenocarcinoma cells. KY-05009 inhibits the protein expression of TNIK and transcriptional activity of Wnt target genes and induces apoptosis in cancer cells. KY-05009 exerts anti-cancer activity.
  • HY-N0005
    Curcumin

    Diferuloylmethane; Natural Yellow 3; Turmeric yellow

    Histone Acetyltransferase Epigenetic Reader Domain Keap1-Nrf2 Autophagy Mitophagy Influenza Virus Ferroptosis Cancer
    Curcumin (Diferuloylmethane), a natural phenolic compound, is a p300/CREB-binding protein-specific inhibitor of acetyltransferase, represses the acetylation of histone/nonhistone proteins and histone acetyltransferase-dependent chromatin transcription. Curcumin shows inhibitory effects on NF-κB and MAPKs, and has diverse pharmacologic effects including anti-inflammatory, antioxidant, antiproliferative and antiangiogenic activities. Curcumin induces stabilization of Nrf2 protein through Keap1 cysteine modification.
  • HY-103160A
    EHNA hydrochloride

    Adenosine Deaminase Phosphodiesterase (PDE) Influenza Virus Cancer Infection Neurological Disease Cardiovascular Disease
    EHNA hydrochloride is a potent and selective dual inhibitor of cyclic nucleotide phosphodiesterase 2 (PDE2)(IC50=4 μM) and adenosine deaminase (ADA). EHNA hydrochloride exerts a concentration inhibition of the cGMP-stimulated PDE II (cGs-PDE)(IC50:0.8 μM (human), 2 μM (porcine myocardium)), but has smaller inhibitory effect on the unstimulated PDE2 activity. EHNA hydrochloride play roles in mediating diverse pharmacological responses, including antiviral, antitumour and antiarrhythmic effects.
  • HY-N0164
    Matrine

    Matridin-15-one; Vegard; α-Matrine

    Opioid Receptor Autophagy Mitophagy Ferroptosis Apoptosis Cancer Inflammation/Immunology
    Matrine (Matridin-15-one) is an alkaloid found in plants from the Sophora genus that can act as a kappa opioid receptor and u-receptor agonist. Matrine has a variety of pharmacological effects, including anti-cancer, anti-oxidative stress, anti-inflammation and anti-apoptosis effects. Matrine is potential in the research of disease like human non-small cell lung cancer, hepatoma, papillary thyroid cancer and acute kidney injury (AKI).
  • HY-136726
    CGP-82996

    CINK4

    CDK Cancer
    GP-82996 (CINK4) is a pharmacological inhibitor of CDK4/6. GP-82996 has IC50s of 1.5, 5.6 and 25 μM for CDK4/cyclin D1, CDK6/cyclin D1 and Cdk5/p35, respectively. GP-82996 induces the apoptosis of cancer cells U2OS. GP-82996 can be used in the research of cancer.
  • HY-112499
    Menaquinone-7

    Vitamin K2-7; Vitamin K2(35); Vitamin MK-7

    Others Cardiovascular Disease
    Menaquinone-7 (Vitamin K2-7), belongs to a class of K2-vitamin homologs, is originally discovered as the anti-hemorrhagic factors. Menaquinone-7 (Vitamin K2-7) is identified as the most bioactive cofactor for the carboxylation reaction of Gla-proteins . Supplementation with Menaquinone-7 (Vitamin K2-7) is a pharmacological option for activating matrix Gla protein and intervening in the progression of calcific aortic valve stenosis (CAVS).
  • HY-N0103A
    Sophocarpine monohydrate

    Autophagy Apoptosis PI3K Akt Influenza Virus Cancer Infection Inflammation/Immunology
    Sophocarpine (monohydrate) is one of the significant alkaloid extracted from the traditional herb medicine Sophora flavescens which has many pharmacological properties such as anti-virus, anti-tumor, anti-inflammatory. Sophocarpine (monohydrate) significantly inhibits the growth of gastric cancer (GC) cells through multiple mechanisms such as induction of autophagy, activation of cell apoptosis and down-regulation of cell survival PI3K/AKT signaling pathway. Sophocarpine (monohydrate) has been demonstrated to have anti-tumor activity in various cancer cells, including hepatocellular carcinoma, prostate cancer and colorectal cancer.
  • HY-N0103
    Sophocarpine

    Autophagy Apoptosis PI3K Akt Influenza Virus Cancer Infection Inflammation/Immunology
    Sophocarpine is one of the significant alkaloid extracted from the traditional herb medicine Sophora flavescens which has many pharmacological properties such as anti-virus, anti-tumor, anti-inflammatory. Sophocarpine significantly inhibits the growth of gastric cancer (GC) cells through multiple mechanisms such as induction of autophagy, activation of cell apoptosis and down-regulation of cell survival PI3K/AKT signaling pathway. Sophocarpine has been demonstrated to have anti-tumor activity in various cancer cells, including hepatocellular carcinoma, prostate cancer and colorectal cancer.
  • HY-10965
    Rolofylline

    KW-3902

    Adenosine Receptor Neurological Disease
    Rolofylline (KW-3902) is a potent, selective adenosine A1 receptor antagonist that is under development for the treatment of patients with acute congestive heart failure and renal impairment. Rolofylline is metabolized primarily to the pharmacologically active M1-trans and M1-cis metabolites by cytochrome P450 (CYP450). Rolofylline is alleviating the presynaptic dysfunction and restores neuronal activity as well as dendritic spine levels in vitro, is an interesting candidate to combat the hypometabolism and neuronal dysfunction associated with Tau-induced neurodegenerative diseases.
  • HY-N0408
    Picroside II

    NF-κB Reactive Oxygen Species Apoptosis Influenza Virus Cancer Infection Inflammation/Immunology Neurological Disease
    Picroside II, an iridoid compound extracted from Picrorhiza, exhibits anti-inflammatory and anti-apoptotic activities. picroside II alleviates the inflammatory response in sepsis and enhances immune function by inhibiting the activation of NLRP3 inflammasome and NF-κB pathways. Picroside II is an antioxidant, exhibits a significant neuroprotective effect through reducing ROS production and protects the blood-brain barrier (BBB) after cerebral ischemia-reperfusion (CI/R) injury. Picroside II has antioxidant, anti-inflammatory, immune regulatory, anti-virus and other pharmacological activities.
  • HY-N3127
    Orobol

    Casein Kinase PI3K Metabolic Disease
    Orobol is one of the major soy isoflavones and has various pharmacological activities, including anti-skin-aging and anti-obesity effects. Orobol inhibits CK1ε, VEGFR2, MAP4K5, MNK1, MUSK, TOPK, and TNIK (IC50=1.24-4.45 μM). Orobol also inhibits PI3K isoforms (IC50=3.46-5.27 μM for PI3K α/β/γ/K/δ).
  • HY-N1940
    β-Anhydroicaritin

    Interleukin Related TNF Receptor MMP Inflammation/Immunology
    β-Anhydroicaritin is isolated from Boswellia carterii Birdware, has important biological and pharmacological effects, such as antiosteoporosis, estrogen regulation and antitumor properties. β-Anhydroicaritin ameliorates the degradation of periodontal tissue and inhibits the synthesis and secretion of TNF-α and MMP-3 in diabetic rats. β-Anhydroicaritin decreases the overproduction of NO, IL-10, TNF-α, MCP-1 and IL-6 in inperitonitis mice. β-Anhydroicaritin inhibits the elevation of intracellular Ca 2+, and markedly decreases iNOS protein expression.
  • HY-149008
    α-Amylase-IN-3

    Others Cancer Metabolic Disease
    α-Amylase-IN-3 (Compound 4) is a none-competitive type of α-Amylase inhibitor with an IC50 value of 18.04 μM, which also has radical scavenging activities (DPPH and ABTS) with IC50 values of 16.04 μM (DPPH) and 16.99 μM (ABTS), respectively. α-Amylase-IN-3 has good protein–ligand interactions profile against α-Amylase. α-Amylase-IN-3 may have pharmacological activities such as anti-oxidative, anti-inflammatory inhibitory, which is helpful for the development of diabetes and oxidative stress associated disease.
  • HY-124322
    NB-360

    Beta-secretase Inflammation/Immunology Neurological Disease
    NB-360 is a potent, brain penetrable, and orally bioavailable dual BACE1/BACE2 inhibitor (IC50: mouse and human BACE1=5 nM; BACE2=6 nM). NB-360 shows a superior pharmacological profile and robust reduction of amyloid-β and neuroinflammation in amyloid precursor protein(APP) transgenic mice. NB-360 can completely block the progression of Aβ deposition in the brains of APP transgenic mice. NB-360 shows excellent selectivity over the related aspartyl proteases pepsin, cathepsin D and cathepsin E.
  • HY-131574
    Heliosupine N-oxide

    mAChR Neurological Disease
    Heliosupine N-oxide, Heliosupin metabolite, inhibits muscarinic acetylcholine receptor (mAChR) with the IC50 of 350 μM. Heliosupine N-oxide is a pyrrolizidine alkaloid (PA).
  • HY-146201
    PDE4B/7A-IN-1

    Phosphodiesterase (PDE) Others
    1 a /5-hydroxynitrile rubber 7 receptor antagonist (5-HT1 a k i = 8 nm, kb= 0.04 nm; 5-nitrile rubber 7K I = 451 nm, kb= 460 nm) has pde4b/pde7a inhibitory activity (PDE4B ic50= 80.4 μ M; Pde7a chip 50= 151.3 μ M)。 Compound 22 has a very good ability of passive penetration of biofilm and high metabolic stability in vitro. In addition, 22's pharmacological evaluation showed its pre cognitive and antidepressant properties in rat behavioral tests.