Search Result
Results for "
rat
" in MCE Product Catalog:
1
Biochemical Assay Reagents
23
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
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- HY-P2416
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- HY-P1349
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- HY-P1532
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- HY-P1296
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Urocortin, rat
Urocortin (rattus norvegicus); rat urocortin;
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CRFR
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Neurological Disease
Endocrinology
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Urocortin, rat (Urocortin (Rattus norvegicus)) is a neuropeptide and a potent endogenous CRFR agonist with Kis of 13 nM, 1.5 nM, and 0.97 nM for human CRF1, rat CRF2α and mouse CRF2β, respectively.
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- HY-P1349A
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Orexin B, rat, mouse TFA
rat orexin B TFA; Orexin B (mouse) (TFA)
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Orexin Receptor (OX Receptor)
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Endocrinology
Neurological Disease
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Orexin B, rat, mouse (Rat orexin B) TFA is an endogenous orexin receptor agonist. Orexin B, rat, mouse TFA binds and activates two closely related orphan G protein-coupled receptors OX1-R and OX2-R. Orexin B, rat, mouse TFA stimulates food intake and energy expenditure and plays a significant role in sleep-wakefulness regulation.
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- HY-P1296A
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Urocortin, rat TFA
Urocortin (rattus norvegicus) (TFA); rat urocortin TFA
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CRFR
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Endocrinology
Neurological Disease
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Urocortin, rat TFA (Urocortin (Rattus norvegicus) TFA) is a neuropeptide and a potent endogenous CRFR agonist with Kis of 13 nM, 1.5 nM, and 0.97 nM for human CRF1, rat CRF2α and mouse CRF2β, respectively.
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- HY-P0209
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- HY-P2457
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rCRAMP (rat)
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Bacterial
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Infection
Inflammation/Immunology
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rCRAMP (rat) is the rat cathelin-related antimicrobial peptide. rCRAMP (rat) contributes to the antibacterial activity in rat brain peptide/protein extracts. rCRAMP (rat) is a potential key player in the innate immune system of rat CNS.
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- HY-P1913
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- HY-P1142
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GLP-2(rat)
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Apoptosis
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Others
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GLP-2(rat) is an intestinal growth factor. GLP-2(rat) stimulates cell proliferation and inhibits apoptosis. GLP-2(rat) enhances mucosal mass and function in residual small intestine after massive small bowel resection (MSBR).
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- HY-P1305
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- HY-P1913A
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- HY-P1090
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Hemopressin(rat)
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Cannabinoid Receptor
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Neurological Disease
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Hemopressin(rat) is a nonapeptide derived from the α1-chain of hemoglobin, is originally isolated from rat brain homogenates. Hemopressin(rat) is orally active, selective and inverse agonist of CB1 cannabinoid receptors. Hemopressin(rat) exerts antinociceptive action in inflammatory pain models.
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- HY-P1142A
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GLP-2(rat) TFA
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Apoptosis
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Others
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GLP-2(rat) TFA is an intestinal growth factor. GLP-2(rat) TFA stimulates cell proliferation and inhibits apoptosis. GLP-2(rat) TFA enhances mucosal mass and function in residual small intestine after massive small bowel resection (MSBR).
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- HY-P1305A
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- HY-106224
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Orexin A (human, rat, mouse)
Hypocretin-1 (human, rat, mouse)
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Orexin Receptor (OX Receptor)
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Neurological Disease
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Orexin A (human, rat, mouse) (Hypocretin-1 (human, rat, mouse)), a 33 amino acid excitatory neuropeptide, orchestrates diverse central and peripheral processes. Orexin A (human, rat, mouse) is a specific, high-affinity agonist for G-protein-coupled receptor OX1R. Orexin A (human, rat, mouse) has a role in the regulation of feeding behavior. Orexin A (human, rat, mouse) is an effective anti-nociceptive and anti-hyperalgesic agent in mice and rats.
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- HY-P1090A
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Hemopressin(rat) TFA
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Cannabinoid Receptor
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Neurological Disease
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Hemopressin(rat) TFA is a nonapeptide derived from the α1-chain of hemoglobin, is originally isolated from rat brain homogenates. Hemopressin(rat) TFA is orally active, selective and inverse agonist of CB1 cannabinoid receptors. Hemopressin(rat) TFA exerts antinociceptive action in inflammatory pain models.
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- HY-P1766
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- HY-P1065
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Apelin-36(rat, mouse)
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HIV
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Infection
Metabolic Disease
Cardiovascular Disease
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Apelin-36(rat, mouse) is an endogenous orphan G protein-coupled receptor APJ agonist. Apelin-36(rat, mouse) binds to APJ receptors with an IC50 of 5.4 nM, and potently inhibits cAMP production with an EC50 of 0.52 nM. Apelin-36(rat, mouse) blocks entry of some HIV-1 and HIV-2 strains into NP-2/CD4 cells expressing APJ.
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- HY-P1306
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Obestatin(rat)
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GHSR
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Inflammation/Immunology
Cardiovascular Disease
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Obestatin(rat), encoded by the Ghrelin gene, is a cpeptide, comprised of 23 amino acids. Obestatin(rat) suppresses food intake, inhibits jejunal contraction, and decreases body-weight gain. Obestatin is an endogenous ligand of G-protein coupled receptor 39 (GPR39). Obestatin(rat) has anti-inflammatory, anti-myocardial infarction and antioxidant activities.
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- HY-P3704
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- HY-P3692
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CART (55-76), rat
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Neuropeptide Y Receptor
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Neurological Disease
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CART (55-76), rat is a neuropeptide (55-76 residues of the CART peptide) and constitutes the N-terminal fragments of CART (55-102). CART (55-76), rat is a rat satiety factor with potent appetite-suppressing activity and is closely associated with leptin and neuropeptide Y. CART (55-76), rat can induce anxiety and stress-related behavior.
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- HY-106224A
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Orexin A (human, rat, mouse) (TFA)
Hypocretin-1 (human, rat, mouse) (TFA)
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Orexin Receptor (OX Receptor)
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Neurological Disease
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Orexin A (human, rat, mouse) (Hypocretin-1 (human, rat, mouse)) TFA, a 33 amino acid excitatory neuropeptide, orchestrates diverse central and peripheral processes. Orexin A (human, rat, mouse) TFA is a specific, high-affinity agonist for G-protein-coupled receptor OX1R. Orexin A (human, rat, mouse) TFA has a role in the regulation of feeding behavior. Orexin A (human, rat, mouse) TFA is an effective anti-nociceptive and anti-hyperalgesic agent in mice and rats.
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- HY-P1065A
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Apelin-36(rat, mouse) TFA
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HIV
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Infection
Metabolic Disease
Cardiovascular Disease
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Apelin-36(rat, mouse) TFA is an endogenous orphan G protein-coupled receptor APJ agonist. Apelin-36(rat, mouse) TFA binds to APJ receptors with an IC50 of 5.4 nM, and potently inhibits cAMP production with an EC50 of 0.52 nM. Apelin-36(rat, mouse) TFA blocks entry of some HIV-1 and HIV-2 strains into NP-2/CD4 cells expressing APJ.
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- HY-P3691
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CART (1-39), Human, Rat
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Neuropeptide Y Receptor
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Neurological Disease
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CART (1-39), Human, Rat is a neuropeptide consisting of 1-39 residues of the CART peptide. CART (1-39), Human, Rat is a rat satiety factor with potent appetite-suppressing activity and is closely associated with leptin and neuropeptide Y. CART (1-39), Human, Rat inhibits both normal and starvation-induced feeding. CART (1-39), Human, Rat can induce anxiety and stress-related behavior.
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- HY-P1473
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Amylin (8-37), rat
Amylin (8-37) (mouse, rat)
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Amylin Receptor
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Metabolic Disease
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Amylin (8-37), rat is a truncated analog of native Amylin that selectively inhibits insulin-related glucose uptake and glycogen deposition in muscle tissue. Amylin (8-37), rat is a weak amylin receptor (AMY) antagonist.
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- HY-P1519B
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- HY-P1519
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- HY-P1438A
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Neuropeptide S(Rat) TFA
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Neuropeptide Y Receptor
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Neuropeptide S(Rat) TFA is a potent endogenous neuropeptide S receptor (NSPR) agonist (EC50=3.2 nM). Neuropeptide S(Rat) TFA increases locomotor activity and wakefulness in mice. Neuropeptide S(Rat) TFA also reduces anxiety-like behavior in mice.
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- HY-P1438
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- HY-P2279A
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- HY-P2279
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- HY-P1747
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Pneumadin, rat
PNM
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Others
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Metabolic Disease
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Pneumadin, rat (PNM) is a decapeptide, which possess a potent stimulating effect on arginine-vasopressin (AVP) release. Pneumadin, rat (PNM) exerts a marked antidiuretic effect in animals with functional AVP system.
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- HY-P1306A
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Obestatin(rat) TFA
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GHSR
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Inflammation/Immunology
Cardiovascular Disease
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Obestatin(rat) TFA, encoded by the Ghrelin gene, is a cpeptide, comprised of 23 amino acids. Obestatin(rat) TFA suppresses food intake, inhibits jejunal contraction, and decreases body-weight gain. Obestatin is an endogenous ligand of G-protein coupled receptor 39 (GPR39). Obestatin(rat) TFA has anti-inflammatory, anti-myocardial infarction and antioxidant activities.
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- HY-P1387
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β-Amyloid (1-40) (rat)
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Amyloid-β
Apoptosis
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Neurological Disease
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β-Amyloid (1-40) (rat) is a rat form of the amyloid β-peptide, which accumulates as an insoluble extracellular deposit around neurons, giving rise to the senile plaques associated with Alzheimer's disease (AD). β-Amyloid (1-40) (rat) increases 45Ca 2+ influx, induces neurodegeneration in the rat hippocampal neurons of the CA1 subfield. β-Amyloid (1-40) (rat) induces apoptosis. β-Amyloid (1-40) (rat) can be used for the research of Alzheimer's disease.
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- HY-P2155
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- HY-P1212
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Cortistatin 14, human, rat
CST-14, human, rat
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Somatostatin Receptor
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Neurological Disease
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Cortistatin 14, human, rat (CST-14, human, rat), a neuropeptide with neuronal depressant and sleep modulating properties, can bind to all five cloned somatostatin receptors (SSTRs) and ghrelin receptor to exert its biological activities and co-exists with GABA within the cortex and hippocampus.
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- HY-P1244
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- HY-P1197
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- HY-P1303
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CART(62-76)(human,rat)
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5-HT Receptor
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Neurological Disease
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CART(62-76)(human,rat) is a neuropeptide (62-76 residues of the CART peptide) with neurotransmitter-like effects. CART(62-76)(human,rat) can modulate the activity of striatal noradrenergic and corticostriatal and hypothalamic serotoninergic (5-HT) system in the rat brain.
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- HY-P1067
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- HY-P0203
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α-CGRP, rat
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CGRP Receptor
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Metabolic Disease
Inflammation/Immunology
Cardiovascular Disease
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α-CGRP, rat, a neuropeptide (calcitonin gene-related peptide (CGRP)) mainly expressed in neuromuscular junction, is a potent vasodilator. α-CGRP, rat can lead to a fall in blood pressure and an increase in heart rate by peripheral administration, also relax colonie smooth muscle. α-CGRP, rat has the potential in cardiovascular, pro-inflammatory, migraine and metabolic studies.
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- HY-P1464
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Amylin, amide, rat
Amylin (rat)
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Amylin Receptor
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Metabolic Disease
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Amylin, amide, rat is a potent and high affinity ligand of Amylin receptor AMY1 and AMY3 receptors and variably of AMY2 receptors; binding studies are generally used for the latter receptor.
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- HY-P2155A
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- HY-P2277
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- HY-P3684
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[DPro5] Corticotropin Releasing Factor, human, rat
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CRFR
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Endocrinology
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[DPro5] Corticotropin Releasing Factor, human, rat is a selective R2 agonist of corticotropin releasing factor/hormone. Corticotropin releasing factor (CRF) is a hypothalamic hormone, stimulates the release of adrenocorticotropic hormone (ACTH) and of β-endorphin. [DPro5] Corticotropin Releasing Factor, human, rat fails to cause the typical anxiogenic effect, but modulates learning and memory processes in rat.
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- HY-106224B
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Orexin A (human, rat, mouse) (acetate)
Hypocretin-1 (human, rat, mouse) (acetate)
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Orexin Receptor (OX Receptor)
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Neurological Disease
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Orexin A (Hypocretin-1) (human, rat, mouse) acetate is a hypothalamic neuropeptide with analgesic properties (crosses the blood-brain barrier). Orexin A (human, rat, mouse) acetate is also an OX1R agonist that induces the expression of BDNF and TH proteins in SH-SY5Y cells in a time- and dose-dependent manner. Orexin A (human, rat, mouse) acetate can be used in studies of appetite regulation, neurodegenerative diseases and modulation of injurious messaging.
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- HY-P1303A
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CART(62-76)(human,rat) TFA
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5-HT Receptor
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Neurological Disease
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CART(62-76)(human,rat) TFA is a neuropeptide (62-76 residues of the CART peptide) with neurotransmitter-like effects. CART(62-76)(human,rat) TFA can modulate the activity of striatal noradrenergic and corticostriatal and hypothalamic serotoninergic (5-HT) system in the rat brain.
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- HY-P1477
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- HY-P1197A
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- HY-P1132
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- HY-P0203A
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α-CGRP, rat TFA
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CGRP Receptor
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Metabolic Disease
Inflammation/Immunology
Cardiovascular Disease
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α-CGRP, rat TFA, a neuropeptide (calcitonin gene-related peptide (CGRP)) mainly expressed in neuromuscular junction, is a potent vasodilator. α-CGRP, rat TFA can lead to a fall in blood pressure and an increase in heart rate by peripheral administration, also relax colonie smooth muscle. α-CGRP, rat TFA has the potential in cardiovascular, pro-inflammatory, migraine and metabolic studies.
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- HY-P3959
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(Tyr0)-Urocortin, rat
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CRFR
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Endocrinology
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(Tyr0)-Urocortin, rat is a high-affinity agonist of corticotropin-releasing factor receptor type 1 (CRF-R1) and type 2 (CRF-R2). (Tyr0)-Urocortin, rat shows inhibitory binding constants (Ki) of 1-2 nM.
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- HY-P1244A
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- HY-P1572
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- HY-P1132A
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- HY-P4856
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pTH-Related Protein (1-40) (human, mouse, rat)
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PKC
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Endocrinology
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pTH-Related Protein (1-40) (human, mouse, rat) stimulates calcium uptake in rat intestinal cells through PTHR1 receptor and PKCα/β signaling pathways. pTH-Related Protein (1-40) up-regulates parathyroid hormone 1 receptor (PTHR1) protein, four transcellular calcium transporters, potential vanillin member 6 (TRPV6), calcium-binding protein-D9K (CaBP-D9k), sodium-calcium Exchanger 1 (NCX1) and plasma membrane calcium ATPase 1 (PMCA1).
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- HY-P1477A
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- HY-P2543
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Neuropeptide Y (3-36) (human, rat)
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Neuropeptide Y Receptor
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Metabolic Disease
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Neuropeptide Y (3-36) (human, rat), a neuropeptide Y (NPY) metabolite formed from dipeptidyl peptidase-4 (DPP4), is a selective Y2 receptor agonist. Neuropeptide Y (3-36) (human, rat) is a NPY metabolite formed from dipeptidyl peptidase-4 (DPP4). Neuropeptide Y (3-36) (human, rat) decreases release of norepinephrine via the Y2 receptor.
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- HY-P1869
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- HY-P1534
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- HY-P3852
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- HY-P1578
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- HY-P1032
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- HY-P1845
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PACAP-38 (31-38), human, mouse, rat
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ERK
EGFR
Reactive Oxygen Species
Calcium Channel
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Neurological Disease
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PACAP-38 (31-38), human, mouse, rat is a PAC1 receptor activator and increases the α-secretase activity. PACAP-38 (31-38), human, mouse, rat elevates cytosolic Ca 2+, increases proliferation and increases phosphorylation of extracellular regulates kinase (ERK) and the epidermal growth factor receptor (EGFR). PACAP-38 (31-38), human, mouse, rat demonstrates potent, efficacious, and sustained stimulatory effects on sympathetic neuronal NPY and catecholamine production. PACAP-38 (31-38), human, mouse, rat can be used for neurotrophic and neuroprotective research.
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- HY-P4672
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(Met(O)27)-Glucagon (1-29) (human, rat, porcine)
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GCGR
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Metabolic Disease
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(Met(O)27)-Glucagon (1-29) (human, rat, porcine) is a modified glucagon. (Met(O)27)-Glucagon (1-29) (human, rat, porcine) has the same maximum glucose-synthesizing activity in rat hepatocytes as native glucagon, but it is less potent, suggesting a crucial role of methionine in the binding of glucagon to its hepatic receptor.
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- HY-107563
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ROS 234
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Histamine Receptor
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Inflammation/Immunology
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ROS 234 is a potent H3 antagonist, with a pKB of 9.46 for Guinea-pig ileum H3-receptor, a pKi of 8.90 for Rat cerebral cortex H3-receptor, and a ED50 of 19.12 mg/kg (ip) in ex vivo of Rat cerebral cortex. ROS 234 diaplays poor central access.
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- HY-P1578A
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- HY-107563A
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ROS 234 dioxalate
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Histamine Receptor
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Inflammation/Immunology
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ROS 234 dioxalate is a potent H3 antagonist, with a pKB of 9.46 for Guinea-pig ileum H3-receptor, a pKi of 8.90 for Rat cerebral cortex H3-receptor, and a ED50 of 19.12 mg/kg (ip) in ex vivo of Rat cerebral cortex. ROS 234 dioxalate diaplays poor central access.
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- HY-P1845A
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PACAP-38 (31-38), human, mouse, rat TFA
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ERK
EGFR
Reactive Oxygen Species
Calcium Channel
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Neurological Disease
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PACAP-38 (31-38), human, mouse, rat TFA is a PAC1 receptor activator and increases the α-secretase activity. PACAP-38 (31-38), human, mouse, rat TFA elevates cytosolic Ca 2+, increases proliferation and increases phosphorylation of extracellular regulates kinase (ERK) and the epidermal growth factor receptor (EGFR). PACAP-38 (31-38), human, mouse, rat TFA demonstrates potent, efficacious, and sustained stimulatory effects on sympathetic neuronal NPY and catecholamine production. PACAP-38 (31-38), human, mouse, rat TFA can be used for neurotrophic and neuroprotective research.
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- HY-P1524
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- HY-P1323
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- HY-101241
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MPPG
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mGluR
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Neurological Disease
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MPPG is a potent and selective L-AP4-sensitive receptor antagonist with an kD value of 9.2 μM, being tested on the neonatal rat spinal cord.
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- HY-P3679
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Neuropeptide Y (1-24) (human)
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Neuropeptide Y Receptor
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Neuropeptide Y (1-24) (human) is a neuropeptide with potencies in inhibiting the electricity stimulated twitch response of rat vas deferens. Neuropeptide Y (1-24) (human) stimulates N-methyl-D-aspartate (NMDA)-induced neuronal activation in the rat CA3 region of the dorsal hippocampus in vivo.
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- HY-P0079
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- HY-P1388
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- HY-P0204A
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Endothelin-3, human, mouse, rabbit, rat TFA
Endothelin 3 (rat,Human) (TFA)
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Endothelin Receptor
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Neurological Disease
Cardiovascular Disease
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Endothelin-3, human, mouse, rabbit, rat TFA is a 21-amino acid vasoactive peptide that binds to G-protein-linked transmembrane receptors, ET-RA and ET-RB.
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- HY-P1205
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MCH(human, mouse, rat)
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MCHR1 (GPR24)
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Neurological Disease
|
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MCH (human, mouse, rat) is a potent peptide agonist of MCH-R and exhibits binding IC50 values of 0.3nM and 1.5 nM for MCH1R and MCH2R, respectively. MCH (human, mouse, rat) is a highly sensitive to MCH-2R in a CHO cell line and monitoring mobilization of intracellular calcium with FLIPR, exhibits functional activation EC50 values of 3.9 nM and 0.1nM for human MCH-1R and MCH-2R, respectively.
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- HY-P1236
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- HY-P1067A
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- HY-P4786
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- HY-P3689
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- HY-P4805
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- HY-P1323A
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- HY-P4680
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- HY-150209
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- HY-D0075
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DHPDS disodium salt
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Fluorescent Dye
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Others
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DHPDS disodium salt is a pH-sensitive fluorescent dye. DHPDS disodium salt is used to measure intracellular pH (pHi) from the surface fluorescence of the isolated perfused rat liver.
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- HY-117962A
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- HY-P1205A
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MCH(human, mouse, rat) TFA
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MCHR1 (GPR24)
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Neurological Disease
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MCH (human, mouse, rat) TFA is a potent peptide agonist of MCH-R and exhibits binding IC50 values of 0.3nM and 1.5 nM for MCH1R and MCH2R, respectively. MCH (human, mouse, rat) is a highly sensitive to MCH-2R in a CHO cell line and monitoring mobilization of intracellular calcium with FLIPR, exhibits functional activation EC50 values of 3.9 nM and 0.1nM for human MCH-1R and MCH-2R, respectively.
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- HY-P1388A
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- HY-P1249
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Neuropeptide SF(mouse,rat)
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Neuropeptide Y Receptor
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Neurological Disease
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Neuropeptide SF (mouse,rat) is a potent neuropeptide FF receptor agonist with Ki values are 48.4 nM and 12.1 nM for NPFF1 and NPFF2, respectively. Neuropeptide SF increases the amplitude of the sustained current of heterologously expressed acid sensing ion channel 3 (ASIC3) .
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- HY-P1236A
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- HY-P3977
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ACTH (3-24) (human, bovine, mouse, ovine, porcine, rabbit, rat)
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Melanocortin Receptor
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Cancer
Inflammation/Immunology
Cardiovascular Disease
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ACTH (3-24) (human, bovine, mouse, ovine, porcine, rabbit, rat) is the 3-24 fragment of adrenocorticotropic hormone (ACTH). ACTH (3-24) (human, bovine, mouse, ovine, porcine, rabbit, rat) can be used for research of a variety of diseases, including cancer, immune diseases, cardiovascular disease.
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- HY-P2562
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- HY-P4860
-
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Adropin (34-76) (human, mouse, rat)
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Akt
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Metabolic Disease
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Adropin (34-76) (human, mouse, rat) regulates fuel selection preferences in skeletal muscle. Adropin increases insulin-induced Akt phosphorylation and cell-surface expression of GLUT4, in diet-induced obesity (DIO) mouse.
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- HY-P1249A
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- HY-111298
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- HY-P3800
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- HY-P4779
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- HY-P4782
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- HY-P4784
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- HY-P4715
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- HY-117962
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(Rac)-BI 703704
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Guanylate Cyclase
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Metabolic Disease
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(Rac)-BI 703704 is a potent soluble guanylyl cyclase (sGC) activator. (Rac)-BI 703704 reduces progression of renal damage in the ZSF1 rat, and highlight the potential of sGC activation as an effective therapy for diabetic nephropathy.
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- HY-103156
-
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NAS-181 dimesylate
|
5-HT Receptor
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Neurological Disease
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NAS181 is a potent and selective antagonist of rat 5-HT1B receptor, with a Ki of 47 nM. NAS181 shows 13-fold selectivity for r5-HT1B over bovine 5-HT1B receptor (Ki=630 nM). NAS181 increases the 5-HT turnover and the synaptic concentration of 5-HT by inhibiting terminal r5-HT1B autoreceptors.
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- HY-P4456
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- HY-P4413
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- HY-P4542
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(D-Phe12,Nle21,38,α-Me-Leu37)-CRF (12-41) (human, rat)
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CRFR
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Endocrinology
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(D-Phe12,Nle21,38,α-Me-Leu37)-CRF (12-41) (human, rat) is a CRF antagonist. (D-Phe12,Nle21,38,α-Me-Leu37)-CRF (12-41) (human, rat) prevents the IL-1a induced Luteinizing hormone (LH) inhibition.
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- HY-13543
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Tretazicar
CB 1954
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DNA Alkylator/Crosslinker
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Cancer
|
|
Tretazicar (CB 1954), an antitumor proagent, is highly selective against the Walker 256 rat tumour line. Tretazicar is enzymatically activated to generate a bifunctional agent, which can form DNA-DNA interstrand cross-links. Tretazicar in rat cells involves the reduction of its 4-nitro group to a 4-hydroxylamine by the enzyme NAD(P)H:quinone oxidoreductase 1 (NQO1).
|
-
- HY-135677
-
-
- HY-135678
-
-
- HY-135679
-
-
- HY-101333
-
|
CPPG
(RS)-CPPG
|
mGluR
|
Neurological Disease
|
|
CPPG ((RS)-CPPG) is a potent group II/III mGlu receptors antagonist. CPPG exhibits some selectivity (approximately 20 fold) for group III (IC50=2.2 nM) over group II (IC50=46.2 nM) mGlu receptors in the rat cerebral cortex. CPPG has weak effects at group I mGlu receptors.
|
-
- HY-117517
-
|
NG-012
|
Others
|
Cancer
|
|
NG-012, potentiator of nerve growth factor (NGF), were isolated from the culture broth of Penicillium verruculosum F-4542. NG-012 potentiates the neurite outgrowth induced by NGF in rat pheochromocytoma cell line (PC12).
|
-
- HY-118463
-
|
Benzomalvin A
|
Neurokinin Receptor
|
Neurological Disease
|
|
Benzomalvin A is a potent antagonist of neurokinin receptor isolated from Penicillium sp. Benzomalvin A shows inhibitory activity against substance P with Ki values of 12, 42 and 43 μM at the guinea pig, rat and human neurokinin NK1 receptors, respectively.
|
-
- HY-P4385
-
-
- HY-129736A
-
|
P32/98
|
Dipeptidyl Peptidase
|
Metabolic Disease
|
|
P32/98 a potent inhibitor of dipeptidyl peptidase IV with a Ki value of 130 nM. P32/98 improves glucose tolerance, insulin sensitivity and β-cell responsiveness in fatty Zucker rat model.
|
-
- HY-107539
-
|
GPR35 agonist 4
|
GPR35
|
Others
|
|
GPR35 agonist 4 (compound 10) is a potent GPR35 agonist with an pEC50 of 5.86. GPR35 agonist 4 shows high potency human and rat GPR35. Mutation of arginine 3.36 eliminates agonist function of GPR35 agonist 4.
|
-
- HY-P1474
-
|
β-Amyloid (22-35)
Amyloid β-Protein (22-35)
|
Amyloid-β
|
Neurological Disease
|
|
β-Amyloid 22-35 (Amyloid β-Protein 22-35), the residues 22-35 fragment ofβ-amyloid protein, has a cytotoxic effect on cultured neurons from the rat hippocampus in serum-free medium. β-Amyloid 22-35 forms aggregates and typical amyloid fibrils resembling those of the β-amyloid protein in neutral buffer solution).
|
-
- HY-129736
-
-
- HY-109114
-
|
Dersimelagon
MT-7117
|
Melanocortin Receptor
|
Metabolic Disease
|
|
Dersimelagon (MT-7117) is an orally active, selective melanocortin 1 receptor (MC1R) agonist with EC50 values of 8.16, 3.91, 1.14 and 0.251 nM for human (h), cynomolgus monkey (cm), mouse (m) and rat (r) MC1R, respectively. Dersimelagon shows good affinity for hMC1R and hMC4R with Ki values of 2.26, 32.9 nM, respectively. Dersimelagon can be used for the research of skin pigmentation[1] [2] .
|
-
- HY-P1474A
-
|
β-Amyloid (22-35) (TFA)
Amyloid β-Protein (22-35) (TFA)
|
Amyloid-β
|
Neurological Disease
|
|
β-Amyloid 22-35 (Amyloid β-Protein 22-35) TFA, the residues 22-35 fragment ofβ-amyloid protein, has a cytotoxic effect on cultured neurons from the rat hippocampus in serum-free medium. β-Amyloid 22-35 TFA forms aggregates and typical amyloid fibrils resembling those of the β-amyloid protein in neutral buffer solution).
|
-
- HY-15404
-
|
Darusentan
Lu-135252
|
Endothelin Receptor
|
Cardiovascular Disease
Endocrinology
|
|
Darusentan (Lu-135252) is a selective endothelin receptor A (ET-A) receptor antagonist, which binds with a Ki of 1.4 nM to the ET-A receptor and a Ki of 184 nM to ET-B receptor, respectively with a 100-fold selectivity for ETA rather than ETB receptors. Darusentan competes for radiolabeled endothelin binding in rat aortic vascular smooth muscle cells (RAVSMs) membranes with single-site kinetics, exhibiting a Ki of 13 nM.
|
-
- HY-P3219
-
-
- HY-W028142
-
|
Quipazine
|
5-HT Receptor
SARS-CoV
|
Neurological Disease
|
|
Quipazine is a 5-HT agonist with a Ki value of 1.4 nM for displaces [3H]GR65630 from 5-HT3R in rat. Quipazine shows antiviral activity against SARS-CoV-2 with an EC50 of 31.64 μM. Quipazine behaves as a 5-HT3R agonist in peripheral models. Quipazine can be used for neurological disease research.
|
-
- HY-101046
-
|
Quipazine dimaleate
|
5-HT Receptor
SARS-CoV
|
Neurological Disease
|
|
Quipazine dimaleate is a 5-HT agonist with a Ki value of 1.4 nM for displaces [3H]GR65630 from 5-HT3R in rat. Quipazine dimaleate shows antiviral activity against SARS-CoV-2 with an EC50 of 31.64 μM. Quipazine dimaleate behaves as a 5-HT3R antagonist in peripheral models. Quipazine dimaleate can be used for neurological disease research.
|
-
- HY-N5067
-
-
- HY-N9480
-
|
Vinaxanthone
SM-345431
|
Phospholipase
|
Cancer
|
|
Vinaxanthone (SM-345431) is a potent and selective semaphorin3A inhibitor. Vinaxanthone exhibits semaphorin3A inhibiting activity with an IC50 of 0.1-0.2 μM. Vinaxanthone shows selective inhibitory activity against phospholipase C (PLC) from rat brain, mutine colon 26 Adenocarcinoma and murine fibroblasts NIH3T3 with IC50s being 5.4, 9.3 and 44 μM, respectively.
|
-
- HY-W010144
-
|
Phenidone
|
COX
Lipoxygenase
|
Inflammation/Immunology
Cardiovascular Disease
|
|
Phenidone, an orally active dual inhibitor of cyclooxygenase (COX) and lipoxygenase (LOX), ameliorates rat paralysis in experimental autoimmune encephalomyelitis. Phenidone is a potent hypotensive agent in the spontaneously hypertensive rat. Phenidone is used as a photographic developer.
|
-
- HY-N2482
-
|
Guvacine
|
GABA Receptor
|
Neurological Disease
|
|
Guvacine, an alkaloid found in the nut of Areca catechu, is a potent GABA uptakp inhibitor. Guvacine inhibits rat GAT-1, rat GAT-2 and rat GAT-3 with IC50 values of 39 μM, 58 μM and 378 μM, respectively.
|
-
- HY-107953
-
|
Chorionic gonadotrophin
hCG; Chorionic gonadotropic hormone
|
Endogenous Metabolite
|
Endocrinology
|
|
Chorionic gonadotrophin (hCG) is a gonadotropin that can be isolated from the anterior pituitary gland. Chorionic gonadotrophin has potential applications in ovarian and follicular development.
|
-
- HY-120944
-
|
BAY-7598
|
MMP
|
Inflammation/Immunology
|
|
BAY-7598 is a potent, orally bioavailable, and selective MMP12 inhibitor probe with IC50s of 0.085, 0.67 and 1.1 nM for human MMP12, murine MMP12, and rat MMP12, respectively.
|
-
- HY-18347A
-
-
- HY-103559
-
|
HexylHIBO
|
mGluR
|
Neurological Disease
|
|
HexylHIBO is a potent group I mGluR antagonist with Kbs of 140 and 110 μM at mGlu1a and mGlu5a receptors, respectively. HexylHIBO decreased sEPSC in rat.
|
-
- HY-U00462
-
|
D-Mannoheptulose
|
Others
|
Metabolic Disease
|
|
D-Mannoheptulose is a major non-structural carbohydrate in avocado. D-mannoheptulose is a specific inhibitor of D-glucose phosphorylation. D-Mannoheptulose can block insulin release and utilization of carbohydrate in rat.
|
-
- HY-100302
-
-
- 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-P1866A
-
-
- HY-119671
-
|
BW 755C
|
COX
Lipoxygenase
|
Endocrinology
|
|
BW 755C is a 5-lipoxygenase (5-LO) inhibitor with an IC50 of 5 μM. BW 755C also inhibits cyclooxygenase (COX) with IC50s of 0.65 and 1.2 μg/mL against COX-1 and COX-2, respectively.
|
-
- HY-N0269
-
|
Echinatin
|
Others
|
Inflammation/Immunology
|
|
Echinatin is a chalcone isolated from the Chinese herbal medicine Gancao with hepatoprotective and anti-inflammatory effects. Echinatin can be quickly absorbed and eliminated and extensively distributed with an absolute bioavailability of approximately 6.81% in Rat.
|
-
- HY-W003445
-
|
4-Bromo-3-hydroxybenzoic acid
|
Endogenous Metabolite
|
Neurological Disease
|
|
4-Bromo-3-hydroxybenzoic acid is a metabolite of Brocresine and a histidine decarboxylase (HDC) inhibitor with IC50s of 1 mM for both rat fetal and rat gastric HDC. 4-Bromo-3-hydroxybenzoic acid also inhibits aromatic-L-amino acid decarboxylase from hog kidney and rat gastric mucosa in vitro with IC50s of 1 mM for both enzymes.
|
-
- HY-15451
-
|
MDA 19
|
Cannabinoid Receptor
|
Neurological Disease
|
|
MDA 19 is a potent and selective agonist of human cannabinoid receptor 2 (CB2), with a Ki of 43.3 nM. MDA 19 has antiallodynic effects in a rat model of neuropathic pain and does not affect rat locomotor activity.
|
-
- HY-124401
-
|
BT-13
|
RET
|
Neurological Disease
|
|
BT-13 is a potent and selective glial cell line-derived neurotrophic factor (GDNF) receptor RET agonist independently of GFLs, promoting neurite growth from sensory neurons in vitro and attenuates experimental neuropathy in the Rat.
|
-
- HY-100809
-
|
Guvacine hydrochloride
|
GABA Receptor
|
Neurological Disease
|
|
Guvacine hydrochloride is an alkaloid from the nut of Areca catechu, acts as an inhibitor of GABA transporter, and dispalys modest selectivity for cloned GABA transporters with IC50s of 14 μM (human GAT-1), 39 μM (rat GAT-1), 58 μM (rat GAT-2), 119 μM (human GAT-3), 378 μM (rat GAT-3), and 1870 μM (human BGT-3).
|
-
- HY-110000
-
-
- HY-121119
-
-
- HY-12942
-
-
- HY-101576
-
-
- HY-N6020B
-
|
Butin
|
Others
|
Inflammation/Immunology
Cardiovascular Disease
|
|
Butin is a major biologically active flavonoid isolated from the heartwood of Dalbergia odorifera, with strong antioxidant, antiplatelet and anti-inflammatory activities. Butin significantly alleviates myocardial infarction and improves heart function, together with prevents diabetes-induced cardiac oxidative damage in rat.
|
-
- HY-N7819
-
|
Pristane
Norphytane
|
Others
|
Inflammation/Immunology
|
|
Pristane (Norphytane) is a naturally occurring hydrocarbon oil found in small quantities in many plants, in various marine organisms, and as the most active component of mineral oil. Pristane is a non-antigenic adjuvant, and induces MHC class II-restricted, arthritogenic T cells in the rat.
|
-
- HY-U00114
-
-
- HY-119674
-
|
Xanthopterin
|
DNA/RNA Synthesis
|
Infection
|
|
Xanthopterin, an unconjugated pteridine compound, is the main component of the yellow granule in the Oriental hornet bear wings, produces a characteristic excitation/emission maximum at 386/456 nm. Xanthopterin (XPT) causes renal growth and hypertrophy in rat.
Xanthopterin inhibits RNA synthesis.
|
-
- HY-10936
-
|
S 18986
|
iGluR
|
Neurological Disease
|
|
S 18986 is a selective, orally active, brain penetrant positive allosteric modulator of AMPA-type receptors. S 18986 shows cognitive enhancing properties in rodents. S 18986 activates the release of noradrenaline and acetylcholine in rat hippocampus and enhances rat memory in object-recognition tests.
|
-
- HY-119674A
-
|
Xanthopterin hydrate
|
DNA/RNA Synthesis
|
Inflammation/Immunology
Cancer
|
|
Xanthopterin hydrate, an unconjugated pteridine compound, is the main component of the yellow granule in the Oriental hornet bear wings, produces a characteristic excitation/emission maximum at 386/456 nm. Xanthopterin hydrate(XPT) causes renal growth and hypertrophy in rat.
Xanthopterin hydrate inhibits RNA synthesis.
|
-
- HY-P3057
-
|
[D-Trp11]-Neurotensin
|
Neurotensin Receptor
|
Neurological Disease
|
|
[D-Trp11]-Neurotensin, an analogue of Neurotensin (NT), is a selective antagonist of NT in perfused rat hearts but behaves as a full agonist in guinea pig atria and rat stomach strips. [D-Trp11]-Neurotensin can inhibit NT-induced hypotension.
|
-
- HY-135507
-
|
NAS-181
|
5-HT Receptor
|
Neurological Disease
|
|
NAS-181 is a potent and selective rat 5-hydroxytryptamine1B (r5-HT1B) antagonist with an Ki value of 47 nM. NAS-181 increases the 5-HTP accumulation in rat brain regions.
|
-
- HY-101641
-
-
- HY-120940A
-
|
AZ13705339 hemihydrate
|
PAK
|
Cancer
|
|
AZ13705339 hemihydrate is a highly potent and selective PAK1 inhibitor with IC50s of 0.33 nM and 59 nM for PAK1 and pPAK1, respectively. AZ13705339 hemihydrate has binding affinities to PAK1 and PAK2, with Kds of 0.28 nM and 0.32 nM, respectively. AZ13705339 hemihydrate can be used in the research of cancers.
|
-
- HY-115890
-
|
Thiocysteine
|
Reactive Oxygen Species
|
Others
|
|
Thiocystine is the trisulfide analog of cysteine, it can modify cysteine in proteins. Thiocystine is an activator for aminolevulinate synthetase. Thiocystine can be used for cysteine metabolism research.
|
-
- HY-135676
-
-
- HY-116808B
-
|
TPN729MA
TPN729 maleate
|
Phosphodiesterase (PDE)
|
Neurological Disease
|
|
TPN729MA (TPN729 maleate) is a selective phosphodiesterase type 5 (PDE5) inhibitor with an IC50 value of 2.28 nM. TPN729MA affects erectile function and it can be used for the research of erectile dysfunction.
|
-
- HY-116808
-
-
- HY-135675
-
-
- HY-120640
-
|
BMS-605541
|
VEGFR
PDGFR
|
Cancer
|
|
BMS-605541 is a selective and orally active inhibitor of VEGFR-2 kinase with an IC50 value of 23 nM and Ki value of 49 nM. BMS-605541 inhibits the activity of Flk-1, VEGFR-1 and PDGFR-β with IC50 values of 40 nM, 400 nM and 200 nM, respectively. BMS-605541 can be used for cancer research.
|
-
- HY-125967
-
|
AM 374
|
FAAH
|
Neurological Disease
|
|
AM 374 is an fatty acid amide hydrolase (FAAH) inhibitor. AM 374 inhibits amidase activity with an IC50 value of 13 nM. AM 374 can be used for the research of neurological disease.
|
-
- HY-110202
-
-
- HY-120940
-
|
AZ13705339
|
PAK
|
Cancer
|
|
AZ13705339 is a highly potent and selective PAK1 inhibitor with IC50s of 0.33 nM and 59 nM for PAK1 and pPAK1, respectively. AZ13705339 has binding affinities to PAK1 and PAK2, with Kds of 0.28 nM and 0.32 nM, respectively. AZ13705339 can be used in the research of cancers.
|
-
- HY-109012A
-
-
- HY-113854
-
-
- HY-12567
-
|
ML375
VU0483253
|
mAChR
|
Neurological Disease
|
|
ML375 (VU0483253) is a potent, highly selective, brain-penetrant and orally active M5 mAChR negative allosteric modulator (NAM) with IC50s of 300 nM and 790 nM for human and rat M5, respectively. ML375 is inactive at human and rat M1-M4.
|
-
- HY-10864
-
|
URB-597
KDS-4103
|
FAAH
Autophagy
Mitophagy
|
Neurological Disease
|
|
URB-597 (KDS-4103) is an orally bioavailable and selective FAAH inhibitor. URB-597 inhibits FAAH activity with an IC50s of approximately 5 nM in rat brain membranes, 0.5 nM in intact rat neurons, 3 nM in human liver microsomes. Antidepressant-like effects. Analgesic activity.
|
-
- HY-121519
-
|
GSK2332255B
|
TRP Channel
|
Cardiovascular Disease
|
|
GSK2332255B is a potent, selective TRPC3 and TRPC6 antagonist with IC50s of 5 nM and 4 nM for rat TRPC3 and rat TRPC6. GSK2332255B shows ≥100-fold selectivity for TRPC3/6 over other calcium-permeable channels.
|
-
- HY-115759
-
-
- HY-P3217
-
|
[Asp5]-Oxytocin
|
Oxytocin Receptor
|
Endocrinology
|
|
[Asp5]-Oxytocin is the first 5-position neurohypophyseal hormone analogue possessing significant biological activity. [Asp5]-Oxytocin causes uterine contractions in vitro, enhanced by Mg 2+. [Asp5]-Oxytocin has the ability of rat uteroconstrictor, avian vasodilator, and rat antidiuretic.
|
-
- HY-P3217A
-
|
[Asp5]-Oxytocin acetate
|
Oxytocin Receptor
|
Endocrinology
|
|
[Asp5]-Oxytocin acetate is the first 5-position neurohypophyseal hormone analogue possessing significant biological activity. [Asp5]-Oxytocin acetate causes uterine contractions in vitro, enhanced by Mg 2+. [Asp5]-Oxytocin acetate has the ability of rat uteroconstrictor, avian vasodilator, and rat antidiuretic.
|
-
- HY-B0817
-
|
Pyridaben
|
Parasite
|
Infection
|
|
Pyridaben is a mitochondrial electron transport inhibitor (METI) acaricide that promotes the formation of damaging oxygen and nitrogen radicals. Pyridaben selectively inhibits complex I (NADH dehydrogenase) with an IC50 value of 2.4 nM (assay sites: rat liver and bovine heart mitochondria). Pyridaben also significantly inhibits rat mitochondrial mtNOS function.
|
-
- HY-N7962
-
-
- HY-120813A
-
-
- HY-N9335
-
-
- HY-111341
-
-
- HY-50675
-
|
GRA Ex-25
|
GCGR
|
Metabolic Disease
|
|
GRA Ex-25 is an inhibitor of glucagon receptor, with IC50 of 56 and 55 nM for rat and human glucagon receptors, respectively.
|
-
- HY-100181
-
-
- HY-N0864
-
|
Macranthoidin B
Macranthoiside I
|
Others
|
Cancer
|
|
Macranthoidin B is a major bioactive saponin in rat plasma after oral administration of extraction of saponins from Flos Lonicerae.
|
-
- HY-D0149
-
-
- HY-123797
-
|
KGA-2727
|
SGLT
|
Metabolic Disease
|
|
KGA-2727 is a first selective, high-affinity and orally active SGLT1 inhibitor with Kis of 97.4 nM and 43.5 nM for human and rat SGLT1, respectively. The selectivity ratios (Ki for SGLT2/Ki for SGLT1) of KGA-2727 are 140 (human) and 390 (rat). KGA-2727 has antidiabetic efficacy.
|
-
- HY-P4580
-
|
Suc-Ala-Ala-Pro-Phe-SBzl
|
Proteasome
|
Others
|
|
Suc-Ala-Ala-Pro-Phe-SBzl can be used as the substrate of rat intestinal mast cell protease (RMCP I), rat skeletal muscle mast cell protease (RMCP II) and Chymotrypsin (HY-108910). Suc-Ala-Ala-Pro-Phe-SBzl can be hydrolyzed by glycine (R208G).
|
-
- HY-116044
-
|
BCATc Inhibitor 2
|
Others
|
Neurological Disease
|
|
BCATc Inhibitor 2 is a selective branched-chain aminotransferase (BCAT) inhibitor for research of neurodegenerative diseases. The IC50s of 0.2 μM, 0.8 μM and 3.0 μM for rat cytosolic isoenzyme rBCATc, human cytosolic isoenzyme hBCATc and rat mitochondrial isoenzyme rBCATm, respectively. BCATc, also called BCAT1, is in the cytoplasm.
|
-
- HY-N7819S
-
|
Pristane-d40
|
Isotope-Labeled Compounds
|
Inflammation/Immunology
|
|
Pristane-d40 is the deuterium labeled Pristane[1]. Pristane (Norphytane) is a naturally occurring hydrocarbon oil found in small quantities in many plants, in various marine organisms, and as the most active component of mineral oil[2]. Pristane is a non-antigenic adjuvant, and induces MHC class II-restricted, arthritogenic T cells in the rat[3].
|
-
- HY-15084
-
-
- HY-N0873A
-
-
- HY-101420
-
-
- HY-14394
-
|
TBB
NSC 231634; Casein Kinase II Inhibitor I
|
Casein Kinase
|
Cancer
|
|
TBB is a cell-permeable and ATP-competitive CK2 inhibitor with an IC50 of 0.15 μM for rat liver CK2.
|
-
- HY-P99148
-
-
- HY-101609
-
-
- HY-101812
-
|
Terbufibrol
|
Others
|
Metabolic Disease
|
|
Terbufibrol has been shown highly active in reducing serum total cholesterol (TC) levels in the normal and hypercholesterolemic male rat.
|
-
- HY-P0198
-
-
- HY-109012
-
|
Seltorexant
JNJ-42847922
|
Orexin Receptor (OX Receptor)
|
Neurological Disease
Endocrinology
|
|
Seltorexant (JNJ-42847922) is an orally active, high-affinity, and selective orexin-2 receptor (OX2R) antagonist (pKi values of 8.0 and 8.1 for human and rat OX2R). Seltorexant (JNJ-42847922) crosses the blood-brain barrier and quickly occupies OX2R binding sites in the rat brain.
|
-
- HY-12959A
-
|
Repinotan hydrochloride
BAY x 3702
|
5-HT Receptor
|
Neurological Disease
|
|
Repinotan hydrochloride (BAY x 3702) is a potent, selective, brain-penetrant and orally active 5-HT1A receptor agonist, with Ki values of 0.19 nM (calf hippocampus), 0.25 nM (rat and human cortex), and 0.59 nM (rat hippocampus Repinotan hydrochloride has a weak affinity for other related receptors. Repinotan hydrochloride has pronounced neuroprotective effects.
|
-
- HY-N0387
-
|
Rhynchophylline
|
NF-κB
|
Others
|
|
Rhyncholphylline, an alkaloid isolated from Uncaria rhynchophylla, shows potent inhibition of lipopolysaccharide (LPS)-induced NO production in rat primary microglial cells.
|
-
- HY-19740
-
-
- HY-111389
-
-
- HY-P0198A
-
-
- HY-P1588
-
-
- HY-100130
-
-
- HY-111914A
-
|
Ferroheme
|
Others
|
Metabolic Disease
|
|
Ferroheme, a complex of ferrous iron and a porphyrin, is an isosteric inhibitor of fatty acid binding to rat liver fatty acid binding protein.
|
-
- HY-P99134
-
-
- HY-U00125
-
-
- HY-P0013
-
|
Antide
D-21074; ORF 23541
|
GnRH Receptor
|
Cancer
|
|
Antide (D-21074) is a potent LHRH antagonist. Antide also can be used for the research of prostatic cancer.
|
-
- HY-101376
-
|
(+)-N-Allylnormetazocine hydrochloride
(+)-SKF 10047 hydrochloride; (+)-N-Allyl-N-normetazocine hydrochloride
|
Opioid Receptor
|
Neurological Disease
|
|
(+)-N-Allylnormetazocine ((+)-SKF 10047) hydrochloride is a benzomorphan opioid with psychotomi metic effects. (+)-N-Allylnormetazocine hydrochloride is an opioid receptor antagonist with Ki values of 300 nM and 27 μM for σ1 and σ2 opioid receptors, respectively. (+)-N-Allylnormetazocine hydrochloride can be used for the research of neurological disease.
|
-
- HY-153120A
-
|
PI3K/mTOR Inhibitor-13 sodium
|
PI3K
mTOR
|
Cancer
|
|
PI3K/mTOR Inhibitor-13 sodium is an orally active dual inhibitor of phosphoinositol 3-kinase (PI3K) and mTOR kinase. PI3K/mTOR Inhibitor-13 sodium has potential applications in sexual diseases, solid tumor and idiopathic pulmonary fibrosis (IPF).
|
-
- HY-108616
-
|
VU 0364739 hydrochloride
|
Phospholipase
|
Cancer
|
|
VU 0364739 hydrochloride is a highly selective phospholipase D2 (PLD2) inhibitor with IC50s of 20 and 1500 nM for PLD2 and PLD1, respectively. VU 0364739 hydrochloride induces apoptosis and it can be used for cancer research.
|
-
- HY-107508
-
|
VU-29
|
mGluR
|
Neurological Disease
|
|
VU-29 is a positive allosteric modulator of metabotropic glutamate 5 (mGlu5) receptor (EC50=9 nM and Ki=244 nM for rmGluR5). VU-29 is selective for mGluR5 relative to other mGluR subtypes (EC50: rmGluR1/rmGluR2=557 nM/1.5 μM; hmGluR4=154 nM).
|
-
- HY-107593
-
|
PS-1145 dihydrochloride
|
IKK
|
Inflammation/Immunology
|
|
PS-1145 (dihydrochloride) is a potent IκB kinase-2 inhibitor with an IC50 value of 88 nM. PS-1145 (dihydrochloride) inhibits activity of NF-κB by blocking IκB kinase phosphorylation in tumor-bearing rats.
|
-
- HY-16688A
-
|
RU 24969 succinate
|
5-HT Receptor
|
Neurological Disease
|
|
RU 24969 succinate is a 5-HT receptor agonist with Ki values of 0.38 and 2.5 nM for 5-HT1B and 5-HT1A, respectively. RU 24969 decreases fluid consumption and increases forward locomotion. RU 24969 succinate can be used for the research of neurological disease.
|
-
- HY-105579
-
-
- HY-105740
-
|
Trenimon
|
DNA/RNA Synthesis
|
Cancer
|
|
Trenimon is a compound with anti-cancer effects. Trenimon shows mutagenic actions in many species by inducing point and chromosomal mutations, sister-chromatid exchanges, recombination phenomena and phage induction. Trenimon can be used for the research of cancer.
|
-
- HY-153120
-
|
PI3K/mTOR Inhibitor-13
|
PI3K
mTOR
|
Cancer
|
|
PI3K/mTOR Inhibitor-13 is an orally active dual inhibitor of phosphoinositol 3-kinase (PI3K) and mTOR kinase. PI3K/mTOR Inhibitor-13 has potential applications in sexual diseases, solid tumor and idiopathic pulmonary fibrosis (IPF).
|
-
- HY-12959
-
|
Repinotan
BAY x 3702 free base
|
5-HT Receptor
|
Neurological Disease
|
|
Repinotan (BAY x 3702 free base) is a potent, selective, brain-penetrant and orally active 5-HT1A receptor agonist, with Ki values of 0.19 nM (calf hippocampus), 0.25 nM (rat and human cortex), and 0.59 nM (rat hippocampus). Repinotan has a weak affinity for other related receptors. Repinotan has pronounced neuroprotective effects.
|
-
- HY-132981
-
|
Lu AF27139
|
P2X Receptor
|
Neurological Disease
|
|
Lu AF27139 is a potent, selective, and orally active antagonist of P2X7 receptor (IC50s of 12 and 2.4 nM for human and rat, Kis of 22, 54, and 13 nM for mouse, human, and rat, respectively). Lu AF27139 has rodent-active and CNS-penetrant character. Lu AF27139 has the potential for the research of CNS diseases.
|
-
- HY-N1457
-
|
Chrysosplenetin
|
P-glycoprotein
Cytochrome P450
Ferroptosis
|
Metabolic Disease
|
|
Chrysosplenetin is one of the polymethoxylated flavonoids in Artemisia annua L. (Compositae) and other several Chinese herbs. Chrysosplenetin inhibits P-gp activity and reverses the up-regulated P-gp and MDR1 levels induced by artemisinin (ART). Chrysosplenetin significantly augments the rat plasma level and anti-malarial efficacy of ART, partially due to the uncompetitive inhibition effect of Chrysosplenetin on rat CYP3A.
|
-
- HY-130246
-
|
NF-56-EJ40
|
Succinate Receptor 1
|
Inflammation/Immunology
|
|
NF-56-EJ40 is a potent, high-affinity, and highly selective human SUCNR1 (GPR91) antagonist with an IC50 of 25 nM and a Ki of 33 nM, and shows almost no activity towards rat SUCNR1. NF-56-EJ40 has high affinity for humanized rat SUCNR1 with a Ki value of 17.4 nM.
|
-
- HY-108614
-
|
GPi688
|
Others
|
Metabolic Disease
|
|
GPi688 is a potent and orally active glycogen phosphorylase (GPa) inhibitor with IC50s of 19 nM, 61 nM and 12 nM for human liver GPa, rat liver GPa and human skeletal muscle GPa, respectively. GPi688 can inhibit glucagons-mediated glucose output in rat primary hepatocytes. GPi688 can be used for researching glucagon-mediated hyperglycaemia.
|
-
- HY-100299
-
-
- HY-13929
-
-
- HY-101020
-
|
Picolinamide
2-Picolinamide
|
PARP
|
Metabolic Disease
|
|
Picolinamide (2-Picolinamide) is an inhibitor of Poly(ADP-ribose) synthetase of nuclei from rat pancreatic islet cells.
|
-
- HY-U00242
-
|
Indacrinone
MK-196; Indacrynic acid
|
Others
|
Metabolic Disease
|
|
Indacrinone (MK196) is an investigational diuretic which has pronounced saluretic activity in the rat and dog as well as both uricosuric and saluretic activity in the chimpanzee.
|
-
- HY-N9737
-
|
(−)-Acutumine
|
Others
|
Neurological Disease
|
|
(−)-Acutumine is a tetracyclic chloroalkaloid that exhibits selective cytotoxicity to cultured human T cells and memory-enhancing properties in the Wistar rat model.
|
-
- HY-A0128
-
-
- HY-A0128A
-
-
- HY-P99124
-
-
- HY-B1151
-
|
Climbazole
BAY-e 6975
|
Fungal
|
Infection
|
|
Climbazole (BAY-e 6975) is a potent antifungal agent. Climbazole also is a potent inducer of rat hepatic cytochrome P450.
|
-
- HY-U00136
-
-
- HY-B0817S
-
|
Pyridaben-d13
|
Parasite
|
Infection
|
|
Pyridaben-d13 is the deuterium labeled Pyridaben[1]. Pyridaben is a mitochondrial electron transport inhibitor (METI) acaricide that promotes the formation of damaging oxygen and nitrogen radicals. Pyridaben selectively inhibits complex I (NADH dehydrogenase) with an IC50 value of 2.4 nM (assay sites: rat liver and bovine heart mitochondria). Pyridaben also significantly inhibits rat mitochondrial mtNOS function[2][3].
|
-
- HY-10016
-
|
E 2012
|
γ-secretase
|
Neurological Disease
|
|
E 2012 is a potent gamma (γ) secretase modulator without affecting Notch processing. E 2012 inhibits 3β-hydroxysterol Δ24-reductase (DHCR24) at the final step in the cholesterol biosynthesis. E 2012 aims at Alzheimer's disease by reduction of amyloid β-42, and induces cataract following repeated doses in the rat.
|
-
- HY-15259
-
|
CP-640186
|
Acetyl-CoA Carboxylase
|
Metabolic Disease
|
|
CP-640186 is an orally active and cell-permeable Acetyl-CoA carboxylase (ACC) inhibitor with IC50s of 53 nM and 61 nM for rat liver ACC1 and rat skeletal muscle ACC2 respectively. Acetyl-CoA carboxylase (ACC) is a key enzyme of fatty acid metabolism that enables the synthesis of malonyl-CoA. CP-640186 can also stimulate muscle fatty acid oxidation.
|
-
- HY-15259A
-
|
CP-640186 hydrochloride
|
Acetyl-CoA Carboxylase
|
Metabolic Disease
|
|
CP-640186 hydrochloride is an orally active and cell-permeable Acetyl-CoA carboxylase (ACC) inhibitor with IC50s of 53 nM and 61 nM for rat liver ACC1 and rat skeletal muscle ACC2 respectively. Acetyl-CoA carboxylase (ACC) is a key enzyme of fatty acid metabolism that enables the synthesis of malonyl-CoA. CP-640186 hydrochloride can also stimulate muscle fatty acid oxidation.
|
-
- HY-118980
-
-
- HY-103575
-
-
- HY-P1276
-
-
- HY-P3702
-
|
CEDAEVFKDSMVPGEK
|
TRP Channel
|
Others
|
|
CEDAEVFKDSMVPGEK is the rat vanilloid receptor subtype 1 (VR1) peptides sequence, can be used to determine the presence and distribution of VR1.
|
-
- HY-103575A
-
-
- HY-100792
-
|
URB602
|
Bacterial
|
Cancer
|
|
URB602 is a selective monoacylglycerol lipase (MGL) inhibitor, which inhibits rat brain MGL with IC50 of 28±4 μM through a noncompetitive mechanism.
|
-
- HY-N0361
-
-
- HY-101222
-
|
SB-203186 hydrochloride
|
5-HT Receptor
|
Neurological Disease
Cardiovascular Disease
|
|
SB-203186 hydrochloride is a potent, selective and competitive 5-HT4 antagonist. SB-203186 hydrochloride antagonizes the 5-HT4 receptor-mediated relaxations of the carbachol-contracted rat isolated oesophagus against 5-HT with pKB values of 10.9 (rat oesophagus), 9.5 (guinea-pig ileum), and 9.0 (human colon) respectively.
|
-
- HY-122099
-
|
Riddelline
|
DNA/RNA Synthesis
|
Others
|
|
Riddelline, a pyrrolizidine alkaloid, is a potent genotoxic agent. Riddelline induces significant elevations in unscheduled DNA synthesis and S-phase synthesis in rat liver.
|
-
- HY-111029
-
|
ALX-1393
|
GlyT
|
Neurological Disease
|
|
ALX-1393, a selective GlyT2 inhibitor, has an antinociceptive effect on thermal, mechanical, and chemical stimulations in a rat acute pain model.
|
-
- HY-W003561
-
|
DHFR-IN-3
|
Antifolate
Parasite
|
Infection
|
|
DHFR-IN-3 is a dihydrofolate reductase (DHFR) inhibitor with the IC50 values of 19 μM and 12 μM in rat liver and P. carinii DHFR, respectively.
|
-
- HY-111804
-
-
- HY-U00133
-
|
HSR6071
|
Others
|
Inflammation/Immunology
|
|
HSR6071, a pyrazinecarboxamide derivative, is an orally active and potent antiallergic agent. HSR6071 potently inhibits the experimental asthma in rat models.
|
-
- HY-14167
-
-
- HY-12363
-
|
U-69593
|
Opioid Receptor
|
Neurological Disease
|
|
U-69593 is a potent and selective κ1-opioid receptor agonist. U-69593 attenuates addictive agent-induced behavioral sensitization in the rat. U-69593 reduces anxiety and enhances spontaneous alternation memory in mice. U-69593 reduces calcium-dependent dialysate levels of dopamine and glutamate in the ventral striatum.
|
-
- HY-117621
-
|
PF-04634817
|
CCR
|
Metabolic Disease
|
|
PF-0463481 is a potent and orally active dual CCR2/CCR5 antagonist with comparable human and rodent CCR2 potency (rat IC50=20.8 nM), and displays 10-20 fold less rodent CCR5 potency (rat IC50=470 nM). PF-0463481 is safe and well-tolerated and has the potential for the study of diabetic nephropathy.
|
-
- HY-P3677
-
|
Neuropeptide Y (2-36) (porcine)
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
Neuropeptide Y (2-36) (porcine) is a porcine-derived neuropeptide with 97.14% homology to rat/human origin. Neuropeptide Y (2-36) (porcine) is also a rat neuropeptide receptor agonist, with EC50 values of 1.2, 1.6 and 3.4 nM for receptor of Y5, Y2 and Y1 respectively. Neuropeptide Y (2-36) (porcine) can be used in studies related to obesity and eating disorders.
|
-
- HY-13414
-
|
Remogliflozin
Remogliflozin A
|
SGLT
|
Metabolic Disease
|
|
Remogliflozin is a potent and selective inhibitor of SGLT2 (sodium-glucose cotransporter 2) with Kis of 12.4 and 26 nM for human and rat SGLT2, respectively.
|
-
- HY-N0435
-
-
- HY-W010451
-
-
- HY-P99119
-
-
- HY-N3710
-
|
Dehydrocrenatidine
Kumujian G; O-Methylpicrasidine I
|
JAK
Apoptosis
|
Cancer
Neurological Disease
|
Dehydrocrenatidine, a natural alkaloid, is a specific JAK inhibitor. Dehydrocrenatidine inhibits voltage-gated sodium channels and ameliorates mechanic allodia in a rat model of neuropathic pain.
|
-
- HY-101736
-
|
AMG9810
|
TRP Channel
|
Neurological Disease
|
|
AMG9810 is a selective and competitive vanilloid receptor 1 (TRPV1) antagonist with IC50 values of 24.5 and 85.6 nM for human and rat TRPV1, repectively.
|
-
- HY-12142
-
-
- HY-P3964
-
-
- HY-111755
-
|
Oral antiplatelet agent 1
|
P2Y Receptor
|
Cardiovascular Disease
|
|
Oral antiplatelet agent 1 is a potent P2Y12 receptor antagonist. Oral antiplatelet agent 1 exhibits excellent antiplatelet aggregation potency with an IC50 value of 2.94 μM as well as antithrombotic efficacy in a rat ferric chloride model. Oral antiplatelet agent 1 shows a superior safety profile than Clopidogrel (HY-15283) in a rat tail-bleeding model. Oral antiplatelet agent 1 can be used to research thromboembolic disorders.
|
-
- HY-17444
-
|
Tesaglitazar
|
PPAR
|
Cancer
Metabolic Disease
|
|
Tesaglitazar is a dual peroxisome proliferator-activated receptor (PPAR) alpha/gamma agonist that is more potent on PPARγ than on PPARα, with EC50s of 13.4 μM and 3.6 μM for rat PPARα and human PPARα, respectively, and approximately 0.2 μM for both rat and human PPARγ. Tesaglitazar induces interstitial mesenchymal cell DNA synthesis and fibrosarcomas in subcutaneous tissues in rats.
|
-
- HY-117621A
-
|
PF-04634817 succinate
|
CCR
|
Metabolic Disease
|
|
PF-0463481 succinate is a potent and orally active dual CCR2/CCR5 antagonist with comparable human and rodent CCR2 potency (rat IC50=20.8 nM), and displays 10-20 fold less rodent CCR5 potency (rat IC50=470 nM). PF-0463481 succinate is safe and well-tolerated and has the potential for the study of diabetic nephropathy.
|
-
- HY-119580
-
|
Leucocyanidin
|
Others
|
Inflammation/Immunology
|
|
Leucocyanidin is an active anti-ulcerogenic ingredient was extracted from Litchi Chinensis. Leucocyanidin demonstrates a significant protective effect against Aspirin-induced erosions in rat models.
|
-
- HY-N6739
-
-
- HY-P1276A
-
-
- HY-120598
-
-
- HY-15687
-
|
SAR407899 hydrochloride
|
ROCK
|
Metabolic Disease
|
|
SAR407899 hydrochloride is a selective, potent and ATP-competitive ROCK inhibitor, with an IC50 of 135 nM for ROCK-2, and Kis of 36 nM and 41 nM for human and rat ROCK-2, respectively.
|
-
- HY-116513
-
-
- HY-13245
-
-
- HY-B0841S
-
|
Acephate-d3
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
Acephate-d3 is the deuterium labeled Acephate. Acephate is an anticholinesterase insecticide that produces cholinotoxicity. Acephate displays weak inhibition of rat AChE but potently inhibits cockroach AChE.
|
-
- HY-N2070
-
-
- HY-112284
-
-
- HY-N6702
-
-
- HY-103500
-
-
- HY-13044
-
-
- HY-101313
-
-
- HY-10716A
-
|
PF-03463275
|
GlyT
|
Neurological Disease
|
|
PF-03463275 is a centrally penetrant, orally available, selective, and competitive GlyT1 (glycine transporter-1) reversible inhibitor, with a Ki of 11.6 nM. PF-03463275 has the potential for Schizophrenia research.
|
-
- HY-153116
-
|
BT8009
|
Others
|
Cancer
|
|
BT8009 is a Nectin-4 targeting toxin conjugate with a Kd value of 2.5 nmol/L for human Nectin-4 (hNectin-4) extra-cellular domain (ECD). BT8009 consists of a Nectin-4-binding bicyclic peptide, a cleavable linker system and monomethylauristatin E (MMAE). BT8009 can be used for the research of advanced and metastatic urothelial cancer.
|
-
- HY-114682A
-
|
Lenperone hydrochloride
AHR 2277
|
Dopamine Receptor
|
Neurological Disease
|
|
Lenperone hydrochloride (AHR 2277) is an antipsychotic compound and a dopamine antagonist. Lenperone hydrochloride reduces gastroesophageal sphincter pressure of healthy dogs. Lenperone hydrochloride can be used for neurological disease research.
|
-
- HY-120088
-
|
PF-06446846
|
Ser/Thr Protease
|
Cardiovascular Disease
|
|
PF-06446846 is an orally active proprotein convertase subtilisin/kexin type 9 (PCSK9) inhibitor. PF-06446846 directly and selectively inhibits translation of PCSK9 by stalling the 80S ribosome in the proximity of codon region.
|
-
- HY-N7147
-
|
Irisquinone
|
Others
|
Cancer
|
|
Irisquinone, a natural product, is an anticancer agent. Irisquinone is also a radiation sensitizer for cancer. Irisquinone reduces GSH level and inhibits the repair of DNA singular strand breaks.
|
-
- HY-W005255
-
-
- HY-103089
-
|
LY393558
|
5-HT Receptor
|
Neurological Disease
|
|
LY393558 is a potent and orally active inhibitor of the 5-HT transporter and an antagonist of 5-HT1B and 5-HT1D receptors. LY393558 increase the extracellular levels of 5-HT in mice model frontal cortex. LY393558 can be used for researching depression.
|
-
- HY-129088
-
-
- HY-109066
-
-
- HY-11034
-
-
- HY-108463
-
|
A-967079
|
TRP Channel
|
Inflammation/Immunology
|
|
A-967079 is a selective TRPA1 receptor antagonist with IC50s of 67 nM and 289 nM at human and rat TRPA1 receptors, respectively, and has good penetration into the CNS.
|
-
- HY-133080
-
|
BAY-784
|
GnRH Receptor
|
Cancer
|
|
BAY-784 is a gonadotropin releasing hormone receptor (GnRH-R) antagonist probe with IC50s of 21 and 24 nM for human and rat GnRH-R, respectively.
|
-
- HY-109542
-
|
Cyclopenthiazide
|
Others
|
Metabolic Disease
|
|
Cyclopenthiazide is a benzothiadiazine diuretic with antihypertensive properties. Cyclopenthiazide exerts a diuretic effect by inhibiting the reabsorption of sodium chloride and water at the distal renal tubules. Cyclopenthiazide increases the excretory capacity of the rat kidney.
|
-
- HY-12332
-
|
JW 642
|
MAGL
|
Neurological Disease
|
|
JW 642 is a potent inhibitor of monoacylglycerol lipase (MAGL) that displays IC50 values of 7.6, 14, and 3.7 nM for inhibition of MAGL in mouse, rat, and human brain membranes, respectively.
|
-
- HY-103207
-
-
- HY-111745
-
|
Tyk2-IN-5
|
JAK
|
Inflammation/Immunology
|
|
Tyk2-IN-5 (compound 6) is a potent, selective and orally active tyrosine kinase 2 (Tyk2) inhibitor that acts on the JH2 structural domain. Tyk2-IN-5 shows a Ki value of 0.086 nM for Tyk2 JH2 and an IC50 value of 25 nM for IFNα. Tyk2-IN-5 efficiently inhibits the production of IFNγ in a pharmacodynamic rat model and is fully efficacious in a rat model of arthritis.
|
-
- HY-136233
-
|
PSB 0777 ammonium
|
Adenosine Receptor
|
Inflammation/Immunology
|
|
PSB 0777 ammonium is a potent and selective adenosine A2A receptor full agonist with Ki values of 44.4 nM, 360 nM for rat and human A2A receptors, respectively. PSB 0777 ammonium has Ki values of ≥10000 nM, 541 nM for rat and human A1 receptors, respectively. PSB 0777 ammonium shows poor brain penetrant and perorally non-absorbable effect. PSB 0777 ammonium has the potential for inflammatory bowel disease (IBS) research research.
|
-
- 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-P0012
-
|
Aviptadil
Vasoactive Intestinal Peptide (human, rat, mouse, rabbit, canine, porcine)
|
SARS-CoV
|
Infection
Inflammation/Immunology
|
|
Aviptadil is an analog vasoactive intestinal polypeptide (VIP) with potent vasodilatory effects. Aviptadil induces pulmonary vasodilation and inhibits vascular SMCs proliferation, platelet aggregation. Aviptadil can be used for the research of pulmonary fibrosis, pulmonary arterial hypertension (PAH) and SARS-CoV-2 caused respiratory failure, et al.
|
-
- HY-P0012A
-
|
Aviptadil acetate
Vasoactive Intestinal Peptide acetate salt (human, rat, mouse, rabbit, canine, porcine)
|
SARS-CoV
|
Infection
Inflammation/Immunology
|
|
Aviptadil acetate is an analog vasoactive intestinal polypeptide (VIP) with potent vasodilatory effects. Aviptadil acetate induces pulmonary vasodilation and inhibits vascular SMCs proliferation, platelet aggregation. Aviptadil acetate can be used for the research of pulmonary fibrosis, pulmonary arterial hypertension (PAH) and SARS-CoV-2 caused respiratory failure, et al.
|
-
- HY-50697
-
-
- HY-124772
-
-
- HY-12190A
-
-
- HY-105634
-
|
Nomegestrol
|
Progesterone Receptor
|
Endocrinology
|
|
Nomegestrol is a potent and orally available progestin, acts as a selective full progesterone receptor agonist, with a Kd of 5.44 nM for rat uterine progesterone receptor, and has moderate antiandrogenic activity and strong antiestrogenic activity.
|
-
- HY-101381
-
|
Otenzepad
AF-DX 116
|
mAChR
|
Metabolic Disease
Neurological Disease
|
|
Otenzepad (AF-DX 116) is a selective and competitive M2 muscarinic acetylcholine receptor antagonist, with IC50 values of 640 nM and 386 nM for rabbit peripheral lung and rat heart, respectively.
|
-
- HY-108479
-
|
Nolpitantium
SR140333
|
Neurokinin Receptor
|
Neurological Disease
|
|
Nolpitantium (SR140333) is a potent, selective, competitive, non-peptide tachykinin NK1 receptor antagonist. Nolpitantium blocks the activation of rat thalamic neurons after nociceptive stimulation.
|
-
- HY-B1486
-
-
- HY-107207
-
-
- HY-12190
-
-
- HY-100747
-
|
PSB-12379
|
CD73
|
Cancer
|
|
PSB-12379, a nucleotide analogue, is a potent Ecto-5'-Nucleotidase (CD73) inhibitor with Kis of 9.03 nM (rat) and 2.21 nM (human).
|
-
- HY-12699
-
-
- HY-P1944A
-
|
Apelin-13 TFA
|
Apelin Receptor (APJ)
|
Metabolic Disease
Cardiovascular Disease
|
|
Apelin-13 TFA is an endogenous ligand for the G-protein coupled receptor angiotensin II protein J (APJ), activating this G protein-coupled receptor with an EC 50 value of 0.37 nM. Apelin-13 TFA has vasodilatory and antihypertensive effects. Apelin-13 TFA also can be used for researching type 2 diabetes and metabolic syndrome.
|
-
- HY-B1505
-
-
- HY-B1151S
-
|
Climbazole-d4
BAY-e 6975-d4
|
Fungal
|
Infection
|
|
Climbazole-d4 is the deuterium labeled Climbazole. Climbazole (BAY-e 6975) is a potent antifungal agent. Climbazole also is a potent inducer of rat hepatic cytochrome P450[2].
|
-
- HY-16654
-
|
ML254
|
mGluR
|
Neurological Disease
|
|
ML254 is a potent mGlu5 potentiator, with EC50 and pEC50 of 9.3 nM and 8.03 nM for rat mGlu5, respectively. ML254 can be used for researching schizophrenia.
|
-
- HY-103316
-
|
trans-Ned 19
|
Calcium Channel
|
Cardiovascular Disease
|
|
trans-Ned 19, a NAADP antagonist and TPC blocker, suppresses the calcium signal in human umbilical vein endothelial cells (HUVEC) and the rat aorta relaxation in response to low histamine concentrations.
|
-
- HY-100747A
-
|
PSB-12379 disodium
|
CD73
|
Cancer
|
|
PSB-12379 disodium, a nucleotide analogue, is a potent Ecto-5'-Nucleotidase (CD73) inhibitor with Kis of 9.03 nM (rat) and 2.21 nM (human).
|
-
- HY-112885B
-
|
nor-NOHA monoacetate
Nω-Hydroxy-nor-L-arginine monoacetate
|
Arginase
|
Metabolic Disease
|
|
nor-NOHA (Nω-Hydroxy-nor-L-arginine) monoacetate is a potent and selective arginase inhibitor. nor-NOHA monoacetate inhibits rat liver arginase with a Ki of 0.5 µM.
|
-
- HY-128585
-
-
- HY-120478
-
|
ASP6432
|
LPL Receptor
|
Infection
|
|
ASP6432 is a potent and selective type 1 lysophosphatidic acid receptor (LPA1) antagonist with IC50s of 11 nM and 30 nM for human LPA1 and rat LPA1, respectively.
|
-
- HY-104003
-
-
- HY-19483
-
-
- HY-16617
-
|
Auglurant
VU0424238
|
mGluR
|
Neurological Disease
|
|
Auglurant (VU0424238) is a novel and selective mGlu5 antagonist with an IC50 value of 11 nM (rat) and an IC50 value of 14 nM (human). Auglurant (VU0424238) has an acceptable CNS penetration.
|
-
- HY-131879
-
|
NS383
|
Sodium Channel
|
Neurological Disease
|
|
NS383 is a potent and uniquely selective inhibitor of rat ASICs containing 1a and/or 3 subunits. NS383 inhibits H(+)-activated currents recorded from rat homomeric ASIC1a, ASIC3, and heteromeric ASIC1a+3 with IC50 values ranging from 0.61 to 2.2 μM. NS383 is well tolerated and capable of reversing pathological painlike behaviors, presumably via peripheral actions, but possibly also via actions within central pain circuits.
|
-
- HY-108006
-
|
Mirogabalin besylate
DS 5565 besylate
|
Calcium Channel
|
Neurological Disease
|
|
Mirogabalin besylate is a selective and orally available ligand for the α2δ subunit of voltage-gated calcium channels, with Kds of 13.5 nM, 22.7 nM, 27 nM, and 47.6 nM for human α2δ-1, human α2δ-2, rat α2δ-1, and rat α2δ-2, respectively.
|
-
- HY-103169
-
|
SCH442416
|
Adenosine Receptor
|
Neurological Disease
|
|
SCH442416 is a potent, selective and brain-penetrant antagonist of adenosine A2A receptor (A2AR), with Kis of 0.048 and 0.5 nM for human and rat A2AR respectively. SCH442416 displays more than 23000-fold selectivity over A1R, A2BR, and A3R (Ki=1111, 10000, and 10000 nM, respectively). SCH442416 can be used for imaging of adenosine A2A receptors in rat and primate brain.
|
-
- HY-100820
-
|
Sarizotan
EMD 128130
|
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
|
Sarizotan (EMD 128130) is an orally active serotonin 5-HT1A receptor and dopamine receptor agonist. Sarizotan (EMD 128130) exhibits IC50 values of 6.5 nM (rat 5-HT1A), 0.1 nM (human 5-HT1A), 15.1 nM (rat D2), 17 nM (human D2), 6.8 nM (human D3) and 2.4 nM (human D4.2), respectively.
|
-
- HY-16751
-
-
- HY-D0845
-
-
- HY-100402
-
|
CFMTI
|
mGluR
|
Cancer
|
|
CFMTI inhibits L-glutamate-induced intracellular Ca 2+ mobilization in CHO cells expressing human and rat mGluR1a, with IC50s of 2.6 and 2.3 nM, respectively.
|
-
- HY-B1486A
-
-
- HY-100208
-
|
HC-067047
|
TRP Channel
|
Cancer
|
|
HC-067047 is a potent and selective TRPV4 antagonist and reversibly inhibits currents through the human, rat, and mouse TRPV4 orthologs with IC50 values of 48 nM, 133 nM, and 17 nM, respectively.
|
-
- HY-14111
-
-
- HY-18610
-
|
Diclofensine hydrochloride
Ro 8-4650 hydrochloride
|
Dopamine Transporter
|
Neurological Disease
|
|
Diclofensine hydrochloride (Ro-8-4650 hydrochloride) is a potent inhibitor of monoamine reuptake, blocking the uptake of dopamine, noradrenaline, and serotonin by rat brain synaptosomes with IC50 values of 0.74, 2.3, and 3.7 nM, respectively.
|
-
- HY-120620
-
|
BMS-195270
|
Others
|
Others
|
|
BMS-195270 is a small molecule that inhibits Carbachol (HY-B1208)-evoked tonicity of isolated rat bladder strips. BMS-195270 inhibits calcium flux.
|
-
- HY-148207
-
|
S-Benzylglutathione
|
Amino Acid Derivatives
|
Metabolic Disease
|
|
S-Benzylglutathione is a competitive glutathionase inhibitor. S-Benzylglutathione is converted to the corresponding cysteine derivatives by rat kidney microsomes. S-Benzylglutathione can be used for the research of metabolic breakdown of glutathione by the glutathionase system.
|
-
- HY-101385
-
-
- HY-14595
-
-
- HY-P1599
-
-
- HY-14185
-
-
- HY-123179
-
|
Mefruside
|
Others
|
Cardiovascular Disease
|
|
Mefruside is an orally active diuretic and has a mild hypotensive effect. Mefruside inhibits the synthesis of urea in an isolated rat liver perfusion model. Mefruside can be used in studies of oedema and hypertension.
|
-
- HY-18610A
-
|
Diclofensine
Ro 8-4650
|
Dopamine Transporter
|
Neurological Disease
|
|
Diclofensine(Ro-8-4650) is a potent inhibitor of monoamine reuptake, blocking the uptake of dopamine, noradrenaline, and serotonin by rat brain synaptosomes with IC50 values of 0.74, 2.3, and 3.7 nM, respectively.
|
-
- HY-103546
-
|
BETP
|
GCGR
|
Metabolic Disease
|
|
BETP is an agonist of glucagon-like peptide-1 (GLP-1) receptor, with EC50s of 0.66 and 0.755 μM for human and rat GLP-1 receptor, respectively.
|
-
- HY-A0151
-
|
Thioproperazine
RP 7843; SKF 5883; Thioperazine
|
Dopamine Receptor
|
Neurological Disease
|
|
Thioproperazine (RP 7843) is an orally active antipsychotic agent with calming, antiemetic activity. Thioproperazine is effective in promoting the release of dopamine in rat striatum. Thioproperazine can be used in studies of schizophrenia and bipolar disorder.
|
-
- HY-148135
-
|
hCAI/II-IN-6
|
Carbonic Anhydrase
|
Neurological Disease
|
|
hCAI/II-IN-6 is an orally active human carbonic anhydrase (CA) inhibitor. hCAI/II-IN-6 selectively inhibits hCA II and hCA VII isoforms with Ki values of 220, 4.9, 6.5 and ＞50000 nM for hCA I, hCA II , hCA VII and hCA XII respectively. hCAI/II-IN-6 shows anticonvulsant activity and anti maximal electroshock (MES) activity in vivo. hCAI/II-IN-6 can be used for the research of epilepsy.
|
-
- HY-W006566
-
|
5-AIQ
5-Aminoisoquinolin-1-one
|
PARP
|
Cancer
|
|
5-AIQ (5-Aminoisoquinolin-1-one) is a water-soluble PARP-1 inhibitor. 5-AIQ is an important functional group in various drugs. 5-AIQ reduces the tissue injury associated with ischemia-reperfusion of the liver, it can be used for the research of the research conditions associated with ischemia-reperfusion of the liver.
|
-
- HY-W354498
-
-
- HY-147719
-
|
COX-2-IN-16
|
COX
|
Inflammation/Immunology
|
|
COX-2-IN-16 (compound 2b) is a potent, selective and orally active COX-2 inhibitor with an IC50 of 102 µM. COX-2-IN-16 inhibits the NO production. COX-2-IN-16 shows anti-inflammatory activity.
|
-
- HY-113161
-
-
- HY-151578
-
|
DPP IV/hCA II-IN-1
|
Dipeptidyl Peptidase
Carbonic Anhydrase
|
Metabolic Disease
|
|
DPP IV/hCA II-IN-1 is a potent and selective dipeptidyl peptidase IV (DPP IV) and carbonic anhydrase (CA) inhibitor with an IC50 value of 0.049 μM for DPP IV and with Ki values of 0.0361, 0.0428, 0.0941, 0.1328, 0.2615, and 3.034 μM for CA II, CA VB, CA VA, CA IX, CA I, and CA IV, respectively.
|
-
- HY-P3169
-
-
- HY-17594
-
|
Oxyclozanide
|
Parasite
Bacterial
Fungal
|
Infection
|
|
Oxyclozanide is an orally active salicylanilide anthelmintic agent that mainly acts by uncoupling oxidative phosphorylation in flukes. Oxyclozanide shows good anti-adenovirus, anti-biofilm, antifungal, and antibacterial activity.
|
-
- HY-P3976
-
-
- HY-N7647
-
-
- HY-W050088
-
|
Isoxepac
HP 549
|
Others
|
Inflammation/Immunology
|
|
Isoxepac (HP 549) is a nonsteroidal anti-inflammatory agent (NSAID) with anti-inflammatory, analgesic and antipyretic activity. Isoxepac has been studied in rat, rabbit, dog, rhesus monkey, etc.
|
-
- HY-19845A
-
-
- HY-N11300
-
-
- HY-N4070
-
|
6"-O-Acetylgenistin
|
Others
|
Others
|
|
6"-O-Acetylgenistin is an isoflavone glycoside isolated from soybeans. 6"-O-Acetylgenistin significantly inhibits lipid peroxidation in rat liver microsome with an IC50 of 10.6 μM.
|
-
- HY-N4071
-
|
6"-O-Acetyldaidzin
|
Others
|
Others
|
|
6"-O-Acetyldaidzin is an isoflavone glycoside isolated from soybeans. 6"-O-Acetyldaidzin significantly inhibits lipid peroxidation in rat liver microsome with an IC50 of 8.2 μM.
|
-
- HY-W010696
-
|
Reverse T3
3′,5′,3-Triiodothyronine
|
Thyroid Hormone Receptor
|
Cardiovascular Disease
|
|
Reverse T3 is a thyroid hormone generated by deiodination of the prohormone thyroxine. Reverse T3 inhibits the increase of sodium current generated by other thyroid hormone analogs in neonatal rat myocytes.
|
-
- HY-103007
-
-
- HY-B1334AS
-
-
- HY-133101
-
|
14-Norpseurotin
|
Others
|
Cancer
|
|
14-Norpseurotin is a compound isolated from the culture of Aspergillus fumigatus. 14-Norpseurotin significantly induces neurite outgrowth of rat pheochromocytoma cells (PC12) at a 10.0 microM concentration.
|
-
- HY-109968A
-
|
Irdabisant hydrochloride
CEP-26401 hydrochloride
|
Histamine Receptor
|
Neurological Disease
|
|
Irdabisant (CEP-26401) hydrochloride is a selective, orally active and blood-brain barrier (BBB) penetrant histamine H3 receptor (H3R) inverse agonist/inverse agonist with Ki values of 7.2 nM and 2.0 nM for rat H3R and human H3R, respectively. Irdabisant hydrochloride has relatively low inhibitory activity against hERG current with an IC50 of 13.8 μM. Irdabisant hydrochloride has cognition-enhancing and wake-promoting activities in the rat social recognition model. Irdabisant hydrochloride can be used to research schizophrenia or cognitive impairment.
|
-
- HY-109968
-
|
Irdabisant
CEP-26401
|
Histamine Receptor
|
Neurological Disease
|
|
Irdabisant (CEP-26401) is a selective, orally active and blood-brain barrier (BBB) penetrant histamine H3 receptor (H3R) inverse agonist/inverse agonist with Ki values of 7.2 nM and 2.0 nM for rat H3R and human H3R, respectively. Irdabisant has relatively low inhibitory activity against hERG current with an IC50 of 13.8 μM. Irdabisant has cognition-enhancing and wake-promoting activities in the rat social recognition model. Irdabisant can be used to research schizophrenia or cognitive impairment.
|
-
- HY-130223
-
-
- HY-122168
-
-
- HY-N0847
-
|
Micheliolide
|
NF-κB
|
Others
|
|
Micheliolide could effectively attenuate the high glucose-stimulated activation of NF-κB, the degradation of IκBα, and the expression of MCP-1, TGF-β1 and FN in rat mesangial cells (MCs).
|
-
- HY-124300
-
|
JNJ-54166060
|
P2X Receptor
|
Others
|
|
JNJ-54166060 is a potent and selective P2X7 receptor antagonist, with IC50s of 4/115/72 nM for human/rat/mouse P2X7 receptor, respectively.
|
-
- HY-N2247A
-
-
- HY-14605
-
-
- HY-14605A
-
|
Rasagiline
(R)-AGN1135; TVP1012
|
Monoamine Oxidase
|
Neurological Disease
|
|
Rasagiline (R-AGN1135) is a highly potent selective irreversible mitochondrial monoamine oxidase (MAO) inhibitor with IC50s of 4.43 nM and 412 nM for rat brain MAO B and A activity, respectively.
|
-
- HY-13077
-
-
- HY-107773
-
|
GSK3004774
|
CaSR
|
Metabolic Disease
|
|
GSK3004774 is a potent, nonabsorbable agonist of CaSR, with an pEC50 of 7.3, 6.6 and 6.5 for human, mouse and rat CaSR, respectively. GSK3004774 shows an EC50 of 50 nM for human CaSR.
|
-
- HY-116663
-
|
(±)20-HDHA
(±)20-HDoHE
|
Endogenous Metabolite
|
Neurological Disease
|
|
(±)20-HDHA ((±)20-HDoHE) is a racemic mixture and is an autoxidation product of Docosahexaenoic acid (DHA). (±)20-HDHA is also formed by peroxidation process in human platelets and rat brain homogenate.
|
-
- HY-U00037
-
|
Ecopladib
PLA 725
|
Phospholipase
|
Inflammation/Immunology
|
|
Ecopladib is a sub-micromolar inhibitor of cytosolic phospholipase A2α (cPLA2α), with IC50s of 0.15 μM and 0.11 μM in the GLU micelle and rat whole blood assays, respectively.
|
-
- HY-14902
-
|
Tofogliflozin
CSG452
|
SGLT
|
Metabolic Disease
|
|
Tofogliflozin(CSG-452) is a potent and highly specific sodium/glucose cotransporter 2(SGLT2) inhibitor with Ki values of 2.9, 14.9, and 6.4 nM for human, rat, and mouse SGLT2.
|
-
- HY-15378
-
-
- HY-P1944
-
|
Apelin-13
|
Apelin Receptor (APJ)
|
Metabolic Disease
Cardiovascular Disease
|
|
Apelin-13 is an endogenous ligand for the G-protein coupled receptor angiotensin II protein J (APJ), activating this G protein-coupled receptor with an EC 50 value of 0.37 nM. Apelin-13 is widely distributed in the central and peripheral nervous systems. Apelin-13 has vasodilatory and antihypertensive effects. Apelin-13 also can be used for researching type 2 diabetes and metabolic syndrome.
|
-
- HY-123377
-
|
Fotagliptin
|
Dipeptidyl Peptidase
|
Metabolic Disease
|
|
Fotagliptin is a Dipeptidyl Peptidase IV (DPP-4) inhibitor (IC50=2.27 nM). Fotagliptin displays great security in rat and dog. Fotagliptin can be used for Type 2 diabetes mellitus research.
|
-
- HY-101516
-
|
CYP17-IN-1
|
Cytochrome P450
|
Cancer
|
|
CYP17-IN-1 (compound 9c) is a potent and orally active CYP17 inhibitor against rat and human CYP17 with IC50s of 15.8 and 20.1 nM.
|
-
- HY-131693
-
-
- HY-N2478
-
|
Taraxasteryl acetate
|
Others
|
Inflammation/Immunology
|
|
Taraxasteryl acetate is isolated from P. sagittalis,and has a broad spectrum of anti-inflammatory activity. Taraxasteryl acetate relieves dextran, zymosan and arachidonic acid induced rat hind-paw edema. Taraxasteryl acetate can be used for the topical inflammation treatment[1] .
|
-
- HY-123481
-
-
- HY-130803
-
|
5-Methyl-5,6-dihydrouridine
|
Others
|
Cancer
|
|
5-Methyl-5,6-dihydrouridine is a minor constituent in the chromosomal RNA of the rat ascites tumor. 5-Methyl-5,6-dihydrouridine can be used for nucleic acid modification.
|
-
- HY-15687A
-
|
SAR407899
|
ROCK
|
Metabolic Disease
|
|
SAR407899 is a selective, potent and ATP-competitive ROCK inhibitor, with an IC50 of 135 nM for ROCK-2, and Kis of 36 nM and 41 nM for human and rat ROCK-2, respectively. SAR407899 shows stable inhibition of migrasome formation.
|
-
- HY-126322
-
|
DVD-445
|
TrxR
|
Cancer
|
|
DVD-445 (Compound 7) is a potent peptidomimetic covalent thioredoxin reductase 1 (TrxR1) inhibitor with an IC50 of 0.60 μM for rat TrxR1. DVD-445 has good anticancer application.
|
-
- HY-12433
-
-
- HY-14471
-
|
Cetilistat
ATL-962
|
Others
|
Metabolic Disease
|
|
Cetilistat (ATL-962), an inhibitor of pancreatic lipase, acts as an effective anti-obesity agent. Cetilistat inhibits rat and human pancreatic lipase activity with IC50s of 54.8 nM, and 5.95 nM, respectively.
|
-
- HY-N6677
-
|
β-Apo-8'-carotenal
Apocarotenal
|
Cytochrome P450
|
Cancer
|
|
β-Apo-8'-carotenal (Apocarotenal), a provitamin A carotenoid, is an inducer of CYPlA1 and CYPlA2 in rat. β-Apo-8'-carotenal is present in many fruits and vegetables.
|
-
- HY-14417
-
|
VU0155041
|
mGluR
|
Neurological Disease
|
|
VU0155041 is a potent, selective positive allosteric modulator (PAM) of mGluR4, with EC50s of 798 nM and 693 nM for human and rat mGluR4, respectively. VU0155041 has potential for the research of Parkinson's disease (PD).
|
-
- HY-100605
-
|
VU0483605
|
mGluR
|
Others
|
|
VU0483605 is a potent and brain-penetrated mGlu1 receptor positive allosteric modulator (PAM). VU0483605 shows excellent mGlu1 PAM activity at both human and rat, with EC50 values of 390 and 356 nM, respectively.
|
-
- HY-101169
-
|
Tetrindole mesylate
|
Monoamine Oxidase
|
Neurological Disease
|
|
Tetrindole mesylate is a selective inhibitor of monoamine oxidase A (MAO A). Tetrindole mesylate inhibits rat brain mitochondrial MAO A in a competitive manner with a Ki value of 0.4 μM and inhibits MAO B with a Ki of 110 μM. Tetrindole mesylate has antidepressant activity.
|
-
- HY-50202
-
|
Etomoxir
(R)-(+)-Etomoxir
|
Apoptosis
|
Cancer
Metabolic Disease
|
|
Etomoxir ((R)-(+)-Etomoxir) is an irreversible inhibitor of carnitine palmitoyltransferase 1a (CPT-1a), inhibits fatty acid oxidation (FAO) through CPT-1a and inhibits palmitate β-oxidation in human, rat and guinea pig.
|
-
- HY-N2080
-
|
Songorine
|
GABA Receptor
|
Cancer
|
|
Songorine is a diterpenoid alkaloid isolated from the genus Aconitum. Songorine is a GABAA receptor antagonist in rat brain and has anti cancer, antiarrhythmic and anti-inflammatory activities. Songorine has the potential for the treatment of Epithelial ovarian cancer (EOC).
|
-
- HY-N2196
-
|
Ajugasterone C
|
Others
|
Inflammation/Immunology
|
|
Ajugasterone C is an ecdysteroid isolated from Leuzea carthamoides. Ajugasterone C shows significant inhibitory effect at 100 mg/kg dose on rat paw oedema development due to Carrageenan-induced inflammation in Sprague Dawley rats.
|
-
- HY-101366
-
-
- HY-14200
-
|
(S)-Rasagiline
TVP1022; S-PAI
|
Monoamine Oxidase
|
Neurological Disease
|
|
(S)-Rasagiline (TVP1022) is the relatively inactive S-enantiomer form of Rasagiline. Rasagiline is a highly potent selective irreversible MAO inhibitor with IC50s of 4.43 nM and 412 nM for rat brain MAO B and A activity, respectively.
|
-
- HY-101316
-
|
TRIM
|
NO Synthase
|
Neurological Disease
|
|
TRIM is a potent nitric oxide synthase inhibitor. TRIM inhibits mouse cerebellar nNOS and rat lung iNOS in vitro with IC50 values of 28.2 and 27.0 µM, respectively. Antidepressant- and anxiolytic-like effects.
|
-
- HY-N11691
-
|
Thapsigargicin
Thapsigargicine
|
Others
|
Inflammation/Immunology
|
|
Thapsigargicin (Thapsigargicine) is a activator of mast cells and leukocytes. Thapsigargicin induces histamine release from rat peritoneal mast cells and human basophil leukocytes. Thapsigargicin increases the cytoplasmic free calcium level in intact human blood platelets.
|
-
- HY-112209
-
|
VU0467154
|
mAChR
|
Neurological Disease
|
|
VU0467154 is a positive allosteric modulator of the M4 muscarinic acetylcholine receptor (mAChR), potentiating the response to ACh with pEC50s of 7.75, 6.2 and 6 for rat, human and cynomolgus monkey M4 receptor, respectively.
|
-
- HY-101281
-
|
VU 6008667
|
mAChR
|
Neurological Disease
|
|
VU 6008667 is a selective negative allosteric modulator of M5 NAM with IC50s of 1.2 μM and 1.6 μM for human M5 and rat M5, respectively. High CNS penetration.
|
-
- HY-120428
-
|
VU0410425
|
mGluR
|
Neurological Disease
|
VU0410425 is an mGlu1 negative allosteric modulator. VU0410425 exhibits potent inhibitory activity for rat mGlu1 with an IC50 value of 140 nM. VU0410425 can be used for the research of central nervous system disorders.
|
-
- HY-14200A
-
|
(S)-Rasagiline mesylate
TVP1022 mesylate; S-PAI mesylate
|
Monoamine Oxidase
|
Neurological Disease
|
|
(S)-Rasagiline (TVP1022) mesylate is the relatively inactive S-enantiomer form of Rasagiline mesylate. Rasagiline mesylate is a highly potent selective irreversible MAO inhibitor with IC50s of 4.43 nM and 412 nM for rat brain MAO B and A activity, respectively.
|
-
- HY-100483
-
|
A-804598
|
P2X Receptor
|
Cancer
|
|
A-804598 is a CNS penetrant, competitive and selective P2X7 receptor antagonist with IC50s of 9 nM, 10 nM and 11 nM for mouse, rat and human P2X7 receptors, respectively.
|
-
- HY-N6777
-
|
Penicillic acid
|
Caspase
Bacterial
Apoptosis
Antibiotic
|
Cancer
Infection
|
|
Penicillic acid is a polyketide mycotoxin produced by several species of Aspergillus and Penicillium. Penicillic acid exhibits cytotoxicity in rat alveolar macrophages (AM) in vitro. Penicillic acid inhibits Fas ligand-induced apoptosis by blocking self-processing of caspase-8.
|
-
- HY-107410
-
|
SC-26196
|
Others
|
Inflammation/Immunology
|
|
SC-26196 is a potent, orally active Delta6 desaturase (D6D, FADS2) inhibitor (IC50=0.2 µM in a rat liver microsomal assay). Antiinflammatory properties.
|
-
- HY-14417B
-
|
VU0155041 sodium
|
mGluR
|
Neurological Disease
|
|
VU0155041 sodium is a potent, selective positive allosteric modulator (PAM) of mGluR4, with EC50s of 798 nM and 693 nM for human and rat mGluR4, respectively. VU0155041 has potential for the research of Parkinson's disease (PD).
|
-
- HY-N1462
-
|
Atractyloside potassium salt
|
Chloride Channel
|
Cardiovascular Disease
|
|
Atractyloside potassium salt is a toxic diterpenoid glycoside that can be isolated from the fruits of Xanthium sibiricum. Atractyloside potassium salt is a powerful and specific inhibitor of mitochondrial ADP/ATP transport. Atractyloside potassium salt inhibits chloride channels from mitochondrial membranes of rat heart.
|
-
- HY-B1404
-
|
Nylidrin hydrochloride
Buphenine hydrochloride
|
Others
|
Inflammation/Immunology
|
|
Nylidrin hydrochloride was an effective inhibitor of IgE-mediated release of histamine from passively sensitized rat peritoneal mast cells and human basophils, and of IgG1-mediated release of histamine from passively sensitized guinea pig lung slices.
|
-
- HY-10715
-
|
SSR504734
|
GlyT
|
Neurological Disease
|
|
SSR504734 is an orally active, selective and reversible inhibitor of human, rat, and mouse GlyT1 (IC50=18, 15, and 38 nM, respectively). SSR504734 shows anti-schizophrenia, anti-anxiety and anti-depression activities.
|
-
- HY-100937
-
|
DPCPX
PD 116948
|
Adenosine Receptor
|
Cardiovascular Disease
|
|
DPCPX (PD 116948), a xanthine derivative, is a highly potent and selective Adenosine A1 receptor antagonist, with a Ki of 0.46 nM in 3H-CHA binding to A1 receptors in rat whole brain membranes.
|
-
- HY-116855
-
|
TASP0433864
|
mGluR
|
Neurological Disease
|
|
TASP0433864 is a selective positive allosteric modulator (PAM) of metabotropic glutamate 2 (mGlu2) receptor with EC50 values of 199 nM and 206 nM against human and rat mGlu2 receptors, respectively. TASP0433864 has antipsychotic activity.
|
-
- HY-18779
-
|
PF-4840154
|
TRP Channel
|
Inflammation/Immunology
|
|
PF-4840154 is a potent, selective agonist of the rat and human TrpA1 channel with EC50s of 97 and 23 nM, respectively. PF-4840154 elicits TrpA1-mediated nocifensive behaviour in mouse.
|
-
- HY-P1010
-
|
Z-LEHD-FMK
|
Caspase
Apoptosis
|
Cancer
Neurological Disease
|
|
Z-LEHD-FMK is a selective and irreversible inhibitor of caspase-9, protects against lethal reperfusion injury and attenuates apoptosis. Z-LEHD-FMK exhibits the neuroprotective effect in a rat model of spinal cord trauma.
|
-
- HY-113767
-
|
Momordin II
|
Others
|
Metabolic Disease
|
|
Momordin II, an oleanane-type triterpene glycoside, is a ribosome inactivating protein. Momordin II inhibits cell-free protein synthesis, releases adenine from rat liver ribosomes and from DNA, and has no RNase activity.
|
-
- HY-123368
-
-
- HY-19889
-
-
- HY-101056
-
-
- HY-148232
-
-
- HY-14806A
-
-
- HY-136124
-
|
Cetilistat impurity 1
|
Drug Metabolite
|
Others
|
|
Cetilistat impurity 1 is an impurity of Cetilistat. Cetilistat, an inhibitor of pancreatic lipase, acts as an effective anti-obesity agent. Cetilistat inhibits rat and human pancreatic lipase activity with IC50s of 54.8 nM, and 5.95 nM, respectively.
|
-
- HY-B0954A
-
|
Oxyphencyclimine
|
mAChR
|
Endocrinology
|
|
Oxyphencyclimine is an orally active muscarinic receptor (mAChR) antagonist. Oxyphencyclimine is effective in reducing ulceration index and increasing pepsin activity in rat gastric ulcer model. Oxyphencyclimine can be used in studies of peptic ulcer disease and gastrointestinal spasm.
|
-
- HY-13070
-
-
- HY-N11304
-
|
Echis Pyramidum Venom
African Carpet Viber Venom
|
Others
|
Metabolic Disease
Inflammation/Immunology
|
|
Echis Pyramidum Venom is a snakevenom that can be obtained from Echis Pyramidum. Echis Pyramidum Venom decreases activities of superoxide dismutase (SOD) and catalase (CAT) in rat livers. Echis Pyramidum Venom causes a lipid peroxidation in organs.
|
-
- HY-121186
-
-
- HY-18732A
-
-
- HY-125301
-
|
Thymoctonan
|
Others
|
Inflammation/Immunology
|
|
Thymoctonan (THF-γ2) is the immunomodulatory octapeptide, thymic humoral factor γ2. Thymoctonan has the half-life less than 6 min at 37 °C in blood from human, rat and mouse.
|
-
- HY-107688A
-
|
UB-165 fumarate
|
nAChR
|
Neurological Disease
|
|
UB-165 fumarate is a nAChR agonist, being a full agonist of the α3β2 isoform and a partial agonist of the α4β2* isoform, with a Ki value of 0.27 nM for nicotine binding in rat brain.
|
-
- HY-14806B
-
-
- HY-142016
-
|
Retinol, palmitate, 9-cis,13-cis-
9-cis,13-cis-Retinyl palmitate; 9-cis,13-cis-Vitamin A palmitate
|
Biochemical Assay Reagents
|
Others
|
|
Retinol, palmitate, 9-cis,13-cis- is the palmitate isomer of vitamin A. Retinol, palmitate, 9-cis,13-cis- can be test bioactivity through rat vaginal smear assays.
|
-
- HY-17610
-
|
Enerisant
TS-091
|
Histamine Receptor
|
Neurological Disease
|
|
Enerisant is a potent, highly selective, competitive and orally active histamine H3 receptor antagonist/inverse agonist with IC50s of 2.89 nM and 14.5 nM against human and rat histamine H3 receptors, respectively.
|
-
- HY-131925
-
|
Diethylamine NONOate diethylammonium salt
DEA NONOate diethylamine
|
Bacterial
|
Infection
|
|
Diethylamine NONOate (DEA NONOate, diethylammonium salt) is a nitric oxide donor. Diethylamine NONOate is a potent antimicrobial agent, which can inhibit Escherichia coli growth. Diethylamine NONOate also can enhance preservation of the donor rat heart.
|
-
- HY-B1486S
-
|
Oxprenolol-d7 hydrochloride
Ba 39089-d7
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Oxprenolol-d7 (hydrochloride) 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[1].
|
-
- HY-N4080
-
|
Cyclobuxine D
|
mAChR
|
Inflammation/Immunology
|
|
Cyclobuxine D is a steroidal alkaloid extracted from Buxus microphylla. Cyclobuxine D has a significant bradycardic effect in the rat heart and an inhibitory action on acetylcholine and Ba ++−induced contraction of the longitudinal muscle isolated from the rabbit jejunum.
|
-
- HY-120184
-
|
VU0467485
AZ13713945
|
mAChR
|
Neurological Disease
|
|
VU0467485 (AZ13713945) is a potent, selective, and orally bioavailable muscarinic acetylcholine receptor 4 (M4) positive allosteric modulator (PAM). VU0467485 (AZ13713945) potentiates activity of ACh at M4 with EC50s of 26.6 nM and 78.8 nM at rat and human M4 receptors, respectively. VU0467485 (AZ13713945) shows selectivity for M4 over human and rat M1/2/3/5. VU0467485 (AZ13713945) displays moderate to high CNS penetration. VU0467485 (AZ13713945) has antipsychotic-like activity.
|
-
- HY-B0822S1
-
|
Fipronil-13C6
|
GABA Receptor
Cytochrome P450
|
Inflammation/Immunology
|
|
Fipronil- 13C6 is the 13C-labeled Fipronil. Fipronil is an insecticide that acts as a selective antagonist of insect GABA receptors (IC50s = 30 nM and 1,600 nM for cockroach and rat receptors, respectively). Fipronil also inhibits desensitizing and non-desensitizing glutamate-induced chloride currents in cockroach neurons (IC50s = 800 nM and 10 nM, respectively). Fipronil induces activity of the cytochrome P450 (CYP) isoforms CYP1A1/2, CYP2B1/2, and CYP3A1/2 in isolated rat liver microsomes.
|
-
- HY-10620
-
|
PI3K-IN-22
|
PI3K
mTOR
|
Cancer
|
|
PI3K-IN-22 is a PI3Kα/mTOR dual kinase inhibitor. PI3K-IN-22 has IC50s of 0.9, 0.6 nM for PI3Kα and mTOR, respectively. PI3K-IN-22 can be used for the research of cancer.
|
-
- HY-103509
-
-
- HY-13736A
-
|
Quinagolide hydrochloride
CV205-502 hydrochloride
|
Dopamine Receptor
Akt
|
Cancer
Neurological Disease
|
|
Quinagolide hydrochloride (CV205-502 hydrochloride) is a selective and orally active dopamine D2 receptor agonist. Quinagolide hydrochloride is an inhibitor of prolactin. Quinagolide hydrochloride down-regulates AKT levels and its phosphorylation. Quinagolide hydrochloride shows antitumor effects, it can be used for the research of cancer.
|
-
- HY-115831
-
|
SAR247799
S1P1 agonist 3
|
LPL Receptor
|
Cardiovascular Disease
|
|
SAR247799 (S1P1 agonist 3) is an oral activity, selective G-protein-biased sphingosine-1 phosphate receptor-1 (S1P1 ) agonist, with EC50s rang from 12.6 to 493 nM in S1P1-overexpressing cells and HUVECs. SAR247799 can be used for the research of endothelial protection, including type-2 diabetes, metabolic syndrome.
|
-
- HY-10711A
-
|
ALX-5407 hydrochloride
(R)-NFPS hydrochloride
|
GlyT
|
Neurological Disease
|
|
ALX-5407 ((R)-NFPS) hydrochloride is a selective and orally active glycine transporter GlyT1 inhibitor with an IC50 value of 3 nM. ALX-5407 hydrochloride can be used the research of N-methyl-D-aspartate-receptor function and schizophrenia.
|
-
- HY-151894
-
|
I-BET432
|
Epigenetic Reader Domain
|
Cancer
|
|
I-BET432 is a BET inhibitor. I-BET432 inhibits BRD4 N-terminal bromodomain (BD1) and the C-terminal bromodomain (BD2) with pIC50 values of 7.5 and 7.2, respectively. I-BET432 can be used as an oral candidate quality molecule for the research of multiple oncology and inflammatory diseases.
|
-
- HY-151962
-
|
JNK3 inhibitor-5
|
JNK
Apoptosis
GSK-3
p38 MAPK
|
Neurological Disease
|
|
JNK3 inhibitor-5 (Compound 22b) is a potent and selective JNK3 inhibitor with an IC50 of 0.379 nM. JNK3 inhibitor-5 effectively protects the neuronal cells against amyloid beta-induced apoptosis. JNK3 inhibitor-5 has a high cell permeability and is predicted as BBB permeable.
|
-
- HY-14256
-
-
- HY-16693
-
|
LDN-27219
|
Others
|
Others
|
|
LDN-27219 is a reversible, slow-binding inhibitor of TGase. LDN-27219 inhibits human TGase with an IC50 value of 0.6 μM. LDN-27219 effectively decreases blood pressure and induces vasodilation, it can be used for the research of cardiovascular disease.
|
-
- HY-N4323
-
-
- HY-W017277
-
|
(+)-Menthol
D-Menthol
|
Others
|
Neurological Disease
|
|
(+)-Menthol (D-Menthol) is one of the optical isomers of Menthol. (+)-Menthol can reduce the electrically evoked contractions of rat phrenic hemidiaphragm in vitro. Local anaesthetic activity. (+)-Menthol can also inhibit the growth of Microcystis aeruginosa cells.
|
-
- HY-101918
-
|
DS-1040 Tosylate
|
Others
|
Cardiovascular Disease
|
|
DS-1040 Tosylate is an orally active, selective inhibitor of activated thrombin-activatable fibrinolysis inhibitor (TAFIa) with IC50s of 5.92 nM and 8.01 nM for human and rat TAFIa. DS-1040 Tosylate is a fibrinolysis enhancer for thromboembolic diseases.
|
-
- HY-125568
-
|
Pyridoxatin
|
Others
|
Others
|
|
Pyridoxatin is a free radical scavenger of microbial origin. Pyridoxatin is isolated from a fungus culture identified as Acremonium sp. BX86. Pyridoxatin inhibits lipid peroxidation induced by free radicals in rat liver microsomes free from vitamin E.
|
-
- HY-123377A
-
-
- HY-P1317
-
-
- HY-106993B
-
-
- HY-103572
-
|
MNI137
|
mGluR
|
Neurological Disease
|
|
MNI137 is a potent and selective negative allosteric modulator for group II mGluRs. MNI137 has IC50s values of 8.3 and 12.6 nM for human and rat mGlu2 inhibition of glutamate-induced calcium mobilization.
|
-
- HY-N8593
-
|
Undecane
|
TNF Receptor
|
Infection
|
|
Undecane has anti-allergic and anti-inflammatory activities on sensitized rat basophilic leukemia (RBL-2H3) mast cells and HaCaT keratinocytes. In sensitized mast cells, Undecane inhibits degranulation and the secretion of histamine and TNF-α[
|
-
- HY-15427
-
|
GDC-0834
|
Btk
|
Inflammation/Immunology
|
|
GDC-0834 is a potent and selective BTK inhibitor. GDC-0834 inhibits BTK with an in vitro IC50 of 5.9 and 6.4 nM in biochemical and cellular assays, respectively, and in vivo IC50 of 1.1 and 5.6 μM in mouse and rat, respectively.
|
-
- HY-P4012
-
-
- HY-N10272
-
|
Avenaciolide
|
Fungal
Bacterial
|
Infection
|
|
Avenaciolide is an antifungal bis-γ-lactone found in Aspergillus avenaceus. Avenaciolide has also antibacterial action. Avenaciolide is a specific inhibitor of glutamate transport in rat liver mitochondria. Avenaciolide interferes with the ability of ADP to stimulate the rate of glutamate oxidation.
|
-
- HY-14886
-
-
- HY-107725
-
|
BIBO3304 TFA
|
Neuropeptide Y Receptor
|
Metabolic Disease
|
|
BIBO3304 TFA is a potent, orally active, and selective neuropeptide Y (NPY) Y1 receptor antagonist, with subnanomolar affinity for both the human and the rat Y1 receptor (IC50=0.38 and 0.72 nM, respectively).
|
-
- HY-50202A
-
|
Etomoxir sodium salt
(R)-(+)-Etomoxir sodium salt
|
Apoptosis
|
Metabolic Disease
Cancer
|
|
Etomoxir((R)-(+)-Etomoxir) sodium salt is an irreversible inhibitor of carnitine palmitoyltransferase 1a (CPT-1a), inhibits fatty acid oxidation (FAO) through CPT-1a and inhibits palmitate β-oxidation in human, rat and guinea pig.
|
-
- HY-130607
-
-
- HY-13632
-
|
Exemestane
FCE 24304; EXE
|
Cytochrome P450
|
Cancer
Endocrinology
|
|
Exemestane (FCE 24304) is a selective, irreversible and orally active steroidal aromatase inhibitor with IC50s of 30 nM and 40 nM for human placental and rat ovarian aromatase, respectively. Exemestane can be used for hormone-dependent breast cancer research.
|
-
- HY-148208
-
|
S-(p-Nitrobenzyl)glutathione
|
Amino Acid Derivatives
|
Metabolic Disease
|
|
S-(p-Nitrobenzyl)glutathione is a competitive glutathionase inhibitor. S-(p-Nitrobenzyl)glutathione is converted to the corresponding cysteine derivatives by rat kidney microsomes. S-(p-Nitrobenzyl)glutathione can be used for the research of metabolic breakdown of glutathione by the glutathionase system.
|
-
- HY-148235
-
|
TP-051
|
Free Fatty Acid Receptor
|
Metabolic Disease
|
|
TP-051 is a potent FFAR1 agonist with an Ki value of 16 nM for human FFAR1. TP-051 can increase insulin secretion in rat insulinoma cells. TP-051 can be used to research type 2 diabetes.
|
-
- 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[1].
|
-
- HY-151947
-
|
ALR2-IN-3
|
Aldose Reductase
|
Metabolic Disease
|
|
ALR2-IN-2 is a potent inhibitor of aldose reductase (ALR2), with IC50s of 22 nM and 116 nM for rat ALR2 and ALR1, respectively. ALR2-IN-2 can be used for the research of diabetic complications.
|
-
- 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 CRF2β and rat CRF1 receptors, respectively.
|
-
- HY-107566
-
|
Conessine
|
Histamine Receptor
Parasite
|
Infection
|
|
Conessine, a steroidal alkaloid, is a potent and selective histamine H3 receptor antagonist with Kis of 5.4, 6.0, 5.7 and 25 nM for human, dog, guinea pig, and rat H H3 receptor, respectively. Anti-malarial activity.
|
-
- HY-P1278A
-
|
GR 64349 TFA
|
Neurokinin Receptor
|
Neurological Disease
|
|
GR 64349 is a potent and highly selective NK2 receptor peptide antagonist, with an EC50 of 3.7 nM in rat colon. GR 64349 exhibits selectivity >1000 and >300-fold with respect to NK1 and NK3 receptors, respectively.
|
-
- HY-110180
-
|
VU0409106
|
mGluR
|
Neurological Disease
|
|
VU0409106 is a potent and selective mGlu5 negative allosteric modulator (NAM) with an IC50 of 24 nM. VU0409106 shows anxiolytic effects in rat models in a concentration-dependent manner. VU0409106 also penetrates the blood-brain barrier (BBB).
|
-
- HY-138953A
-
|
Epiboxidine hydrochloride
|
nAChR
|
Neurological Disease
|
|
Epiboxidine hydrochloride is a potent and selective neural nAChR agonist with Kis of 0.46 nM and 1.2 nM for rat and human α4β2 nAChRs, respectively. Epiboxidine hydrochloride is a methylisoxazole analog of the alkaloid Epibatidine, and is also an analog of another nAChR agonist, ABT 418.
|
-
- HY-P1010A
-
|
Z-LEHD-FMK TFA
|
Caspase
Apoptosis
|
Cancer
Neurological Disease
|
|
Z-LEHD-FMK TFA is a selective and irreversible inhibitor of caspase-9, protects against lethal reperfusion injury and attenuates apoptosis. Z-LEHD-FMK TFA exhibits the neuroprotective effect in a rat model of spinal cord trauma.
|
-
- HY-148290
-
|
KTX-951
|
PROTACs
IRAK
|
Cancer
|
|
KTX-951 is a PROTAC targeting IRAK4 degradation (DC50=18 nM). KTX-951 (10 mg/kg) shows the oral bioavailability (F%) of 22% in a rat model. KTX-951 has good anticancer potential.
|
-
- HY-103226
-
|
SC-57461A
|
Aminopeptidase
|
Inflammation/Immunology
|
|
SC-57461A is a potent, orally active, nonpeptide, and selective inhibitor of Leukotriene A4 (LTA4) hydrolase with IC50s of 2.5 nM, 3 nM, and 23 nM for recombinant human, mouse, and rat LTA4 hydrolase, respectively.
|
-
- HY-P2706
-
|
Granuliberin R
|
Histamine Receptor
|
Endocrinology
|
|
Granuliberin R is a new mast cell degranulating peptide comes from amphibian, can be isolated from the skin of frog Rana rugosa. Granuliberin R is a dodecapeptide, can act on rat peritoneal mast cell to liberate granules and release histamine.
|
-
- HY-P0049
-
-
- HY-151946
-
|
ALR2-IN-2
|
Aldose Reductase
|
Metabolic Disease
|
|
ALR2-IN-2 is a potent inhibitor of aldose reductase (ALR2), with IC50s of 27 nM and 228 nM for rat ALR2 and ALR1, respectively. ALR2-IN-2 can be used for the research of diabetic complications.
|
-
- HY-18734
-
-
- HY-P1278
-
|
GR 64349
|
Neurokinin Receptor
|
Neurological Disease
|
|
GR 64349 is a potent and highly selective NK2 receptor peptide antagonist, with an EC50 of 3.7 nM in rat colon. GR 64349 exhibits selectivity >1000 and >300-fold with respect to NK1 and NK3 receptors, respectively.
|
-
- HY-N4193
-
|
Glabrol
|
Acyltransferase
|
Cardiovascular Disease
|
|
Glabrol (Compound 1), One isoprenyl flavonoid was isolated from ethanol extract of licorice roots, is a potent and non-competitive Acyl-coenzyme A: cholesterol acyltransferase (ACAT) inhibitor with an IC50 value of 24.6 μM for rat liver microsomal ACAT activity.
|
-
- HY-138953
-
|
Epiboxidine
|
nAChR
|
Neurological Disease
|
|
Epiboxidine is a potent and selective neural nAChR agonist with Kis of 0.46 nM and 1.2 nM for rat and human α4β2 nAChRs, respectively. Epiboxidine is a methylisoxazole analog of the alkaloid Epibatidine, and is also an analog of another nAChR agonist, ABT 418.
|
-
- HY-108682
-
-
- HY-118941
-
|
BAY 73-1449
|
Prostaglandin Receptor
|
Cardiovascular Disease
|
|
BAY 73-1449 is a selective antagonist of prostacyclin receptor (IP), with high potency (IC50 of less than 0.1 nM) in cAMP assays in Human HEL cells and rat DRG. BAY 73-1449 can be used in the research of lowering blood pressure.
|
-
- HY-U00064
-
|
AZD2098
|
CCR
|
Inflammation/Immunology
Endocrinology
|
|
AZD2098 is a potent and selective CC-chemokine receptor 4 (CCR4) inhibitor with pIC50s of 7.8, 8.0, 8.0 and 7.6 for human, rat, mouse and dog respectively, used for asthma research.
|
-
- HY-P1317A
-
-
- HY-14364
-
-
- HY-100405
-
|
FTIDC
|
mGluR
|
Neurological Disease
|
|
FTIDC is an orally active, noncompetitive, selective allosteric metabotropic glutamate receptor (mGluR) 1 antagonist with an IC50 of 5.8 nM for human mGluR1a. FTIDC has no species differences in its antagonistic activity on recombinant human, mouse, and rat mGluR1.
|
-
- HY-P1770
-
|
Adrenomedullin (16-31), human
|
CGRP Receptor
|
Cardiovascular Disease
|
|
Adrenomedullin (16-31), human is amino acid residues 16-31 fragment of human adrenomedullin (hADM). Adrenomedullin has appreciable affinity for the CGRP1 receptor. Adrenomedullin (16-31), human possesses pressor activity in the systemic vascular bed of the rat, but not the cat.
|
-
- 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-18734A
-
-
- HY-135976
-
|
P2X3 antagonist 34
|
P2X Receptor
|
Inflammation/Immunology
Neurological Disease
|
|
P2X3 antagonist 34 is a potent, selective and orally active P2X3 homotrimeric receptor antagonist with IC50s of 25 nM, 92 nM and 126 nM for human P2X3, rat P2X3 and guinea pig P2X3 receptors, respectively. P2X3 antagonist 34 is less active against human, rat and guinea pig P2X2/3 heterotrimeric receptors. P2X3 antagonist 34 has strong anti-tussive effect.
|
-
- HY-N1957
-
|
Gamma-Mangostin
γ-Mangostin
|
5-HT Receptor
|
Metabolic Disease
|
|
Gamma-Mangostin is a novel competitive 5-hydroxytryptamine 2A (5-HT2A) receptors antagonist, purified from the fruit hull of the medicinal plant Garcinia mangostana. Gamma-Mangostin is a inhibitor of Transthyretin (TTR) fibrillization, it binds to the thyroxine (T4)-binding sites and stabilized the TTR tetramer. Gamma-Mangostin inhibits [3 H] spiperone binding to cultured rat aortic myocytes (IC50=3.5 nM) and reduces The perfusion pressure response of rat coronary artery to 5-HT2A (IC50=0.32 µM) .
|
-
- HY-N1733
-
|
2′-Hydroxydaidzein
|
Others
|
Inflammation/Immunology
|
|
2′-Hydroxydaidzein is a metabolite. 2′-Hydroxydaidzein inhibits the release of chemical mediator from inflammatory cells. 2′-Hydroxydaidzein significantly inhibits lysozyme and β-glucuronidase release from rat neutrophils, which is stimulated with fMLP/CB, respectively.
|
-
- HY-130248B
-
|
(R)-BAY-899
|
GnRH Receptor
|
Others
|
|
(R)-BAY-899 is the R-enantiomer of BAY-899. BAY-899 is an orally active and selective luteinizing hormone receptor (LH-R) antagonist with IC50s of 185 nM and 46nM for hLH (human LH) and rLH (rat LH), respectively.
|
-
- HY-18992
-
|
AS2444697
|
IRAK
|
Inflammation/Immunology
|
|
AS2444697 is an orally active IRAK-4 inhibitor with an IC50 of 21 nM. AS2444697 potently inhibits human and rat IRAK-4 activity. AS2444697 exhibits renoprotective effects through anti-inflammatory action.
|
-
- HY-135034
-
|
UMB68 sodium
|
Others
|
Neurological Disease
|
|
UMB68 sodium is a selective GHB receptor ligand. UMB68 sodium displaces [ 3H]NCS-382 with an IC50 of 38 nM in rat cerebrocortical membranes. UMB68 sodium has no significant affinity at GABAB receptors, cannot be metabolized to GABA-active compounds.
|
-
- HY-130248
-
|
BAY-899
|
GnRH Receptor
|
Endocrinology
|
|
BAY-899 is an orally active and selective luteinizing hormone receptor (LH-R) antagonist with IC50s of 185 nM and 46nM for hLH (human LH) and rLH (rat LH), respectively. BAY-899 can reduce sex hormone levels.
|
-
- HY-117604
-
|
THPP-1
|
Phosphodiesterase (PDE)
|
Neurological Disease
|
|
THPP-1, a SGC chemical probe, is a potent and orally bioavailable phosphodiesterase 10A (PDE10A) inhibitor, with Ki values of 1 nM and 1.3 nM for human and rat PDE10A, respectively. THPP-1 has excellent pharmacokinetic properties in preclinical species.
|
-
- HY-W145497
-
|
D-(+)-Sorbose
|
Insulin Receptor
|
Metabolic Disease
|
|
D-(+)-Sorbose, an active enantiomer of D-Sorbose, which inhibits disaccharidase activity and demonstrates suppressive action on postprandial blood levels of glucose and insulin in the rat. D-sorbose acts as a sweetener may contribute to the prevention of lifestyle-related diseases, such as type 2 diabetes mellitus.
|
-
- HY-103166
-
|
PSB-603
|
Adenosine Receptor
|
Inflammation/Immunology
|
|
PSB-603 is a potent and highly selective A2B adenosine receptor antagonist exhibiting a Ki value of 0.553 nM and virtually no affinity for the human and rat A1 and A2A and the human A3 receptors up to a concentration of 10 μM.
|
-
- HY-B1559
-
|
Allethrin
|
Apoptosis
|
Cancer
|
|
Allethrin, a pyrethroid insecticide is a major mosquito repellent agent. Allethrin induces oxidative stress, apoptosis and calcium release in rat testicular carcinoma cells (LC540). Allethrin induces BCL-2, caspase-3 activation and release of intracellular calcium.
|
-
- HY-10198
-
|
Navarixin
SCH 527123; MK-7123
|
CXCR
|
Inflammation/Immunology
Endocrinology
|
|
Navarixin (SCH 527123) is a potent, allosteric and orally active antagonist of both CXCR1 and CXCR2, with Kd values of 41 nM for cynomolgus CXCR1 and 0.20 nM, 0.20 nM, 0.08 nM for mouse, rat and cynomolgus monkey CXCR2, respectivelly.
|
-
- HY-146457
-
-
- HY-132841A
-
|
Sucunamostat hydrochloride
SCO-792 hydrochloride
|
Others
|
Metabolic Disease
|
|
Sucunamostat (SCO-792) hydrochloride is an orally active and reversible enteropeptidase inhibitor with IC50s of 4.6 nM and 5.4 nM for rat enteropeptidase and human enteropeptidase, respectively. Sucunamostat hydrochloride can slowly dissociate from enteropeptidase in vitro and inhibit protein digestion in vivo.
|
-
- HY-18780
-
|
RR6
|
Others
|
Cancer
|
|
RR6 is a potent, selective, reversible, competitive and orally active vanin inhibitor with an IC50 of 540 nM for recombinant vanin-1. RR6 also potently inhibits human, bovine and rat serum pantetheinase with IC50 values of 40 nM, 41 nM and 87 nM, respectively.
|
-
- HY-P3528
-
|
GPR
|
Caspase
Apoptosis
|
Neurological Disease
|
|
GPR is a three amino acid peptide. GPR can rescue cultured rat hippocampal neurons from Aβ-induced neuronal death by inhibiting caspase-3/p53 dependent apoptosis. GPR can be used for the research of Alzheimer's disease (AD).
|
-
- HY-107688
-
|
UB-165
|
nAChR
|
Neurological Disease
|
|
UB-165 is a nAChR agonist, being a full agonist of the α3β2 isoform and a partial agonist of the α4β2* isoform, with a Ki value of 0.27 nM for [ 3H]-nicotine binding in rat brain.
|
-
- HY-101839
-
|
ML381
VU0488130
|
mAChR
|
Neurological Disease
|
|
ML381 (VU0488130) is a highly selective, central nervous system penetrant mAChR M5 orthogonal antagonist (IC50 = 450 nM; Ki = 340 nM). ML381 is unstable in rat plasma and can be mainly used as a molecular probe for in vitro and electrophysiological studies.
|
-
- HY-100834
-
|
5,7-Dichlorokynurenic acid
5,7-DCKA
|
iGluR
|
Neurological Disease
|
|
5,7-Dichlorokynurenic acid (5,7-DCKA) is a selective and competitive antagonist of the glycine site on NMDA receptor with a KB of 65 nM. 5,7-Dichlorokynurenic acid, a derivative of kynurenic acid, reduced NMDA-induced neuron injury in rat cortical cell cultures.
|
-
- HY-N2228
-
|
(-)-Epigallocatechin-3-(3''-O-methyl) gallate
(-)-EGCG-3''-O-ME
|
Others
|
Cancer
|
|
(-)-Epigallocatechin-3-(3''-O-methyl) gallate is a natural product isolated from the tea leaf, with strong antioxidative activity. (-)-Epigallocatechin-3-(3''-O-methyl) gallate has a strong cytotoxic activity for rat cancer cells.
|
-
- HY-10679A
-
|
PF-03049423
|
Phosphodiesterase (PDE)
|
Neurological Disease
|
|
PF-03049423 (Compound PF-5) is a potent and highly selective phosphodiesterase-5A inhibitor with an IC50 of about 0.2 nM for rat and human platelet enzyme. PF-03049423 can be used for the research of acute ischaemic stroke.
|
-
- HY-130126
-
|
Sucunamostat hydrate
SCO-792
|
Others
|
Others
|
|
Sucunamostat hydrate (SCO-792) is an orally active and reversible enteropeptidase inhibitor with IC50s of 4.6 nM and 5.4 nM for rat enteropeptidase and human enteropeptidase, respectively. Sucunamostat hydrate can slowly dissociate from enteropeptidase in vitro and inhibit protein digestion in vivo.
|
-
- HY-14450
-
-
- HY-N2160
-
|
6'''-Feruloylspinosin
|
GABA Receptor
|
Neurological Disease
|
|
6'''-Feruloylspinosin is a flavonoid isolated from seeds of Ziziphus jujuba. 6'''-Feruloylspinosin can across the blood-brain barrier and enhance the expression of GABAAα1, GABAAα5, and GABABR1 mRNA in rat hippocampal neurons.
|
-
- HY-117575A
-
-
- HY-108295
-
|
Pivagabine
CXB-722
|
GABA Receptor
|
Neurological Disease
|
|
Pivagabine (CXB 722) is a hydrophobic 4-aminobutyric acid derivative with neuromodulatory activity. Pivagabine penetrates the blood-brain barrier in rats. Pivagabine antagonizes the effects of foot shock on both GABAA receptor function and corticotropin-releasing factor (CRF) concentrations in rat brain.
|
-
- HY-44157
-
|
ALS-I
|
Biochemical Assay Reagents
|
Neurological Disease
|
|
ALS-I, an acid-Liable surfactant, is adopted for in-solution enzymatic digestions, can help to solubilize hydrophobic proteins. ALS-I is significantly enhanced peptide recovery for mass spectrometry (MS) mapping in the study of the proteomes of regenerating rat retina and mouse brain.
|
-
- HY-113974
-
|
trans-AUCB
t-AUCB
|
Epoxide Hydrolase
|
Cancer
|
|
trans-AUCB (t-AUCB) is a potent, orally active and selective soluble epoxide hydrolase (sEH) inhibitor with IC50s of 1.3 nM, 8 nM, 8 nM for hsEH, mouse sEH and rat sEH, respectively. trans-AUCB has anti-glioma activity.
|
-
- HY-P1174
-
-
- HY-113936
-
-
- HY-107605
-
|
UBP296
|
iGluR
|
Neurological Disease
|
|
UBP296 is a potent and selective antagonist of GLUK5-containing kainate receptor in the spinal cord. UBP296 reversibly blocks ATPA-induced depressions of synaptic transmission, and affects AMPA receptor-mediated synaptic transmission directly in rat hippocampal slices.
|
-
- HY-15084B
-
|
Dizocilpine
MK-801
|
iGluR
|
Neurological Disease
|
|
Dizocilpine (MK-801), a potent anticonvulsant, is a selective and non-competitive NMDA receptor antagonist, with a Kd of 37.2 nM in rat brain membranes. Dizocilpine acts by binding to a site located within the NMDA associated ion channel and thus prevents Ca 2+ flux.
|
-
- HY-P3498
-
|
Elsiglutide
ZP1846
|
GCGR
|
Others
|
|
Elsiglutide (ZP1846) is a GLP-2 analogue, an orally active and selective GLP-2 receptor agonist, increases cell proliferation and reduces apoptosis in the intestine. Elsiglutide improves Lapatinib (HY-50898)-induced diarrhoea in rat model.
|
-
- HY-100371
-
|
(RS)-MCPG
alpha-MCPG
|
mGluR
|
Neurological Disease
|
|
(RS)-MCPG (alpha-MCPG) is a competitive and selective group I/group II metabotropic glutamate receptor (mGluR) antagonist. (RS)-MCPG blocks theta-burst stimulation (TBS)-induced shifts in both juvenile and neonatal rat hippocampal neurons.
|
-
- HY-P1770A
-
|
Adrenomedullin (16-31), human TFA
|
CGRP Receptor
|
Cardiovascular Disease
|
|
Adrenomedullin (16-31), human TFA is amino acid residues 16-31 fragment of human adrenomedullin (hADM). Adrenomedullin has appreciable affinity for the CGRP1 receptor. Adrenomedullin (16-31), human TFA possesses pressor activity in the systemic vascular bed of the rat, but not the cat.
|
-
- HY-108677
-
|
L-368,899 hydrochloride
|
Oxytocin Receptor
|
Endocrinology
|
|
L-368,899 hydrochloride is a potent, selective, orally bioavailable, non-peptide oxytocin receptor antagonist, with IC50s of 8.9 nM and 26 nM for rat uterus and human uterus oxytocin receptor, respectively. L-368,899 hydrochloride used as a tocolytic agent.
|
-
- HY-108015
-
-
- HY-13755A
-
|
(R)-Sulforaphane
L-Sulforaphane
|
Keap1-Nrf2
|
Cancer
|
|
(R)-Sulforaphane (L-Sulforaphane) is a highly potent inducer of the Keap1/Nrf2/ARE pathway. (R)-Sulforaphane is a far more potent inducer of the carcinogen-detoxifying enzyme systems in rat liver and lung than the S-isomer.
|
-
- HY-14806
-
|
Teneligliptin
MP-513
|
Dipeptidyl Peptidase
|
Metabolic Disease
|
|
Teneligliptin (MP-513) is a potent, orally available, competitive, and long-lasting DPP-4 inhibitor. Teneligliptin competitively inhibits human plasma, rat plasma, and human recombinant DPP-4 in vitro, with IC50s of approximately 1 nM.
|
-
- HY-100554
-
|
BMY 7378
|
Adrenergic Receptor
5-HT Receptor
|
Cardiovascular Disease
|
|
BMY 7378 is a selective antagonist of α1D-adrenoceptor (α1D-AR). BMY 7378 binds to membranes expressing the cloned rat α1D-AR with a >100-fold higher affinity (Ki=2 nM) than binding to either the cloned rat α1A-AR (Ki=800 nM) or the hamster α1B-AR (Ki=600 nM). BMY 7378 is a 5-HT1A receptor partial agonist.
|
-
- HY-N2566
-
|
Euscaphic acid
|
DNA/RNA Synthesis
PI3K
Apoptosis
|
Cancer
|
|
Euscaphic acid, a DNA polymerase inhibitor, is a triterpene from the root of the R. alceaefolius Poir. Euscaphic inhibits calf DNA polymerase α (pol α) and rat DNA polymerase β (pol β) with IC50 values of 61 and 108 μM. Euscaphic acid induces apoptosis.
|
-
- HY-13213
-
-
- HY-A0171
-
|
Benzoctamine
Ba-30803 free base
|
Others
|
Neurological Disease
|
|
Benzoctamine is an orally active and potent psychoactive agent which possesses tranquillizing properties. Benzoctamine increases the turnover rate of catecholamines. Benzoctamine enhances the [3H]noradrenaline uptake in the rat heart. Benzoctamine also accelerated the disappearance of intracisternally injected [3H]noradrenaline.
|
-
- 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-P0198B
-
-
- 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-14335
-
|
Ro 04-6790
|
5-HT Receptor
|
Neurological Disease
|
|
Ro 04-6790 is a potent, competitive and selective 5-HT6 receptor antagonist with pKi values of 7.26, 7.35 for rat and human 5-HT6 receptors, respectively. Ro 04-6790 has no affinity at other receptors.
|
-
- HY-116522
-
|
AR420626
|
Free Fatty Acid Receptor
|
Others
|
|
AR420626 is a selective agonist of free fatty acid receptor 3 (FFAR3, GPR41) with IC50 of 117 nM. AR420626 inhibits nicotine and serotonin-induced changes in motility of isolated muscle strips from rat colon and suppresses serotonin-induced fecal output in rats.
|
-
- HY-122635A
-
|
T-448
|
Histone Demethylase
|
Neurological Disease
|
|
T-448 is a specific, orally active and irreversible inhibitor of lysine-specific demethylase 1 (LSD1, an H3K4 demethylase), with an IC50 of 22 nM. T-448 enhances H3K4 methylation in primary cultured rat neurons.
|
-
- HY-154831
-
|
C22-Ceramide
N-Behenoyl-D-erythro-sphingosine; Cer d18:1/22:0
|
Others
|
Metabolic Disease
|
|
C22-Ceramide (Cer d18:1/22:0) is an endogenous bioactive sphingolipid. C22-Ceramide reduces the propensity of C16-ceramide channel formation in isolated rat liver mitochondria and in liposomes.
|
-
- HY-N7665
-
|
Prosaikogenin G
|
Others
|
Metabolic Disease
|
|
Prosaikogenin G, isolated from the roots of Bupleurum chinensis DC., exhibits significant inhibitory effects on rat mesangial cell proliferation induced by Ang II. Prosaikogenin G has protective action on the kidney. Prosaikogenin G is a derivative of Saikosaponin d in the gastrointestinal tract.
|
-
- HY-125934
-
|
Allocholic acid
|
Others
|
Cancer
|
|
Allocholic acid is a typically fetal bile acid found in vertebrates and reappears during liver regeneration and carcinogenesis, besides it is also a conjugate acid of allocholate and an isomer of cholic acid. Allocholic acid is a potent and specific stimulant of the adult olfactory system, it has a role as a marine metabolite, a rat metabolite and a human metabolite.
|
-
- HY-113074
-
-
- HY-103234
-
|
GYKI 52466
|
iGluR
|
Neurological Disease
|
|
GYKI 52466 is an orally active, highly selective and noncompetitive AMPA/kainate receptor antagonist with the IC50 values of 7.5 and 11μM, respectively. GYKI 52466 has good blood brain barrier permeability and anticonvulsant effect. GYKI 52466 can be used in Parkinson's disease research.
|
-
- HY-N2021
-
-
- HY-17613
-
|
Evocalcet
KHK7580
|
CaSR
|
Metabolic Disease
|
|
Evocalcet (KHK7580) is an orally active calcium sensing receptor (CaSR) agonist. Evocalcet inhibits the secretion of parathyroid hormone (PTH) from parathyroid gland cells. Evocalcet can be used for the research of hyperparathyroidism.
|
-
- HY-103502
-
|
CGP7930
|
GABA Receptor
|
Neurological Disease
|
|
CGP7930 (3-(3’,5’-Di-tert-butyl-4’-hydroxy) phenyl-2, 2-dimethylpropanol) is a positive metabotropic GABAB receptor allosteric modulator. CGP7930 enhances the inhibitory effect of l-baclofen on the oscillatory activity of cultured cortical neurons.
|
-
- HY-122812
-
-
- HY-146421
-
|
Anti-inflammatory agent 21
|
NO Synthase
NF-κB
Reactive Oxygen Species
|
Inflammation/Immunology
|
|
Anti-inflammatory agent 21 (compound 9o) is an orally active and low cytotoxic anti-inflammatory agent, with an IC50 value of 0.76 μM for NO. Anti-inflammatory agent 21 acts via accumulation ROS and blocks the NF-κB/MAPK signaling pathway. Anti-inflammatory agent 21 can ameliorate cartilage destruction and inflammatory cell infiltration in arthritis rats model.
|
-
- HY-107416
-
|
RHC 80267
U-57908
|
Acyltransferase
mAChR
COX
Phospholipase
|
Metabolic Disease
Neurological Disease
|
|
RHC 80267 (U-57908) is a potent and selective inhibitor of diacylglycerol lipase (DAGL) (with IC50 of 4 μM in canine platelets). RHC-80267 inhibits cholinesterase activity with an IC50 of 4 μM, thereby enhancing the relaxation evoked by acetylcholine. RHC 80267 also inhibits COX and the hydrolysis of phosphatidylcholine (PC).
|
-
- HY-N9113
-
|
1,3,5,6-Tetrahydroxyxanthone
|
Others
|
Cardiovascular Disease
|
|
1,3,5,6-Tetrahydroxyxanthone is a natural xanthone that can be isolated from Garcinia achachairu Rusby (Clusiaceae) branches. 1,3,5,6-Tetrahydroxyxanthone induces diuresis and saluresis in normotensive and hypertensive rats.
|
-
- HY-129143
-
|
Delphinidin-3-sambubioside chloride
Dp3‐Sam chloride
|
Others
|
Metabolic Disease
Inflammation/Immunology
|
|
Delphinidin-3-sambubioside (Dp3‐Sam) chloride is an anthocyanin that has orally active anti-inflammatory activity. Delphinidin-3-sambubioside chloride inhibits LPS-induced inflammatory factors release. Delphinidin-3-sambubioside chloride also alleviates hepatic lipid accumulation in HFD rats. Delphinidin-3-sambubioside chloride can be isolated from Hibiscus sabdariffa L..
|
-
- HY-103234A
-
|
GYKI 52466 dihydrochloride
|
iGluR
|
Neurological Disease
|
|
GYKI 52466 dihydrochloride is an orally active, highly selective and noncompetitive AMPA/kainate receptor antagonist with the IC50 values of 7.5 and 11μM, respectively. GYKI 52466 dihydrochloride has good blood brain barrier permeability and anticonvulsant effect. GYKI 52466 dihydrochloride can be used in Parkinson's disease research.
|
-
- HY-16635
-
|
Setipiprant
ACT-129968; KYTH-105
|
Prostaglandin Receptor
|
Inflammation/Immunology
Endocrinology
|
|
Setipiprant (ACT-129968) is an orally active and selective CRTH2 antagonist. Setipiprant interacts with hCRTH2 receptor with an IC50 value of 6 nM. Setipiprant inhibits prostanoid receptors hDP1 and hEP2 with IC50 values of 1290 and 2600 nM, respectively. Setipiprant can be used for the research of asthma and rhinitis.
|
-
- HY-116301
-
|
CAY10502
|
Phospholipase
|
Inflammation/Immunology
|
|
CAY10502 is a potent, calcium-dependent cytosolic phospholipase A2 α (cPLA2α) inhibitor with an IC50 of 4.3 nM for isolated enzyme. CAY10502 can be used in the research of retinopathy and inflammatory diseases.
|
-
- HY-N10587
-
|
Catechin 7-O-β-D-glucopyranoside
|
Others
|
Inflammation/Immunology
|
|
Catechin 7-O-beta-D-glucopyranoside is an orally active natural product found in Ulmus davidiana and Paeonia obovata. Catechin 7-O-β-D-glucopyranoside shows antioxidant and anti-inflammatory activities, and attenuates mitochondrial dysfunction. Catechin 7-O-beta-D-glucopyranoside can be used in intestinal inflammatory disease research.
|
-
- HY-N2021A
-
-
- HY-11011
-
|
A-770041
|
Src
|
Inflammation/Immunology
|
|
A-770041 is a selective and orally active Src-family Lck inhibitor. A-770041 inhibits Lck with an IC50 value of 147 nM with the presence of 1 mM ATP. A-770041 shows 300-fold selective to Lck over Fyn, the other Src family kinase involved in T-cell signaling. A-770041 can be used for the research of acute rejection.
|
-
- HY-139667
-
|
PKM2-IN-3
|
Pyruvate Kinase
|
Neurological Disease
|
|
PKM2-IN-3 is an inhibitor of PKM2 kinase with an IC50 value of 4.1 μM. PKM2-IN-3 exhibits an anti-neuroinflammatory effect by inhibiting PKM2-mediated glycolysis and NLRP3 activation.
|
-
- HY-W040030
-
|
Hematin
|
Others
|
Cancer
Metabolic Disease
|
|
Hematin, an iron-containing porphyrin, inhibits the activity of clotting factors and also fibrin clot lysis through the mechanism of binding to and inactivation of hemostatic proteins. Hematin can be used for the research of acute porphyrias and cancer.
|
-
- HY-137978A
-
|
Ezurpimtrostat hydrochloride
GNS561 hydrochloride
|
Others
|
Cancer
Metabolic Disease
Inflammation/Immunology
|
|
Ezurpimtrostat hydrochloride (compound 2-3) is a potent and orally active anti-fibrotic agent. Ezurpimtrostat hydrochloride reduces significantly the liver fibrosis in DEN (diethyl nitrosamine) cirrhotic rat model. Ezurpimtrostat hydrochloride can be used for the research of fibrosis, cancer, autophagy and cathepsins B (CTSB), L (CTSL) and D (CTSD) related diseases .
|
-
- HY-12066
-
-
- HY-15834A
-
|
Eprosartan mesylate
SKF-108566J
|
Angiotensin Receptor
|
Cardiovascular Disease
Endocrinology
|
|
Eprosartan mesylate (SKF-108566J) is a selective, competitive, nonpeptid and orally active angiotensin II receptor antagonist, used as an antihypertensive. Eprosartan mesylate binds angiotensin II receptor with IC50s of 9.2 nM and 3.9 nM in rat and human adrenal cortical membranes, respectively.
|
-
- HY-A0119
-
|
Nitroprusside disodium dihydrate
Sodium nitroprusside dihydrate; Sodium Nitroferricyanide(III) Dihydrate
|
Autophagy
|
Cardiovascular Disease
Cancer
|
|
Nitroprusside disodium dehydrate (Sodium nitroprusside dihydrate) is a vasodilator that available for the research of acute hypertension, heart failure. Nitroprusside disodium dehydrate induces autophagy in glutathione-depleted osteoblasts. Nitroprusside disodium dehydrate acts as a nitric oxide (NO) donor in a rat intestinal ischemia reperfusion model.
|
-
- HY-128584
-
|
VU6005806
AZN-00016130
|
mAChR
|
Neurological Disease
|
|
VU6005806 (AZN-00016130) is a potent muscarnic acethylcholine receptor subtype 4 (M4) positive allosteric modulator (PAM), with EC50s of 94 nM, 28 nM, 87 nM and 68 nM for human, rat, dog and cyno M4, respectively. Used in the research of neuropsychiatric disorders.
|
-
- HY-N3806
-
-
- HY-111926
-
-
- HY-108583
-
|
Psora-4
5-(4-Phenylbutoxy)psoralen
|
Potassium Channel
|
Inflammation/Immunology
|
|
Psora-4 is a potent and selective inhibitor of Kv1.3 (voltage-gated potassium channels) with an EC50 of 3 nM. Psora-4 has immunosuppressive activity and inhibits proliferation of human and rat myelin-specific effector memory T cells in vitro.
|
-
- HY-P1091
-
|
Hemopressin (human, mouse)
|
Cannabinoid Receptor
|
Neurological Disease
|
|
Hemopressin is a nonapeptide derived from the α1-chain of hemoglobin, is originally isolated from rat brain homogenates. Hemopressin is orally active, selective and inverse agonist of CB1 cannabinoid receptors. Hemopressin exerts antinociceptive action in inflammatory pain models.
|
-
- HY-113906
-
|
GSK1614343
|
GHSR
|
Metabolic Disease
|
|
GSK1614343 is the potent antagonist of growth hormone secretagogues type 1a (GHS1a) receptors. GSK1614343 inhibits the calcium response induced by ghrelin with a pIC50 value of 7.90. GSK1614343 represents a useful tool to investigate the physiological relevance of the ghrelin system in rat models.
|
-
- HY-P1214
-
-
- HY-10679
-
-
- HY-P1316
-
|
Ac-RYYRWK-NH2
|
Opioid Receptor
|
Neurological Disease
|
|
Ac-RYYRWK-NH2 is a potent and selective partial agonist for the nociceptin receptor (NOP), [ 3H]Ac-RYYRWK-NH2 binds to rat cortical membranes ORL1 with a Kd of 0.071 nM, but has no affinity for µ-, κ- or δ-opioid receptors.
|
-
- HY-114739
-
|
MA-0204
|
PPAR
|
Metabolic Disease
|
|
MA-0204 is a potent, highly selective and orally available peroxisome proliferator activated receptor δ (PPARδ) modulator with EC50s of 0.4 nM, 7.9 nM and 10 nM for human, mouse and rat PPARδ, respectively. Potential treatment for Duchene Muscular Dystrophy (DMD).
|
-
- HY-148844
-
|
GCGR antagonist 2
|
GCGR
|
Metabolic Disease
|
|
GCGR antagonist 2, a Furan-2-carbohydrazide, is an orally active glucagon receptor antagonist. GCGR antagonist 2 binds to hGluR with an Kd value of 2.3 nM, and inhibits rat receptor with an IC50 value of 0.43 nM. GCGR antagonist 2 inhibits glucagon-stimulated glycogenolysis.
|
-
- HY-W062836
-
|
BAY 41-8543
|
Guanylate Cyclase
|
Cardiovascular Disease
|
|
BAY 41-8543 is an orally active, nitric oxide (NO)-independent stimulator of soluble guanylyl cyclase (sGC). BAY 41-8543 has vasodilator activity in the pulmonary and systemic vascular beds in the rat. BAY 41-8543 has antiplatelet effects and has the potential for cardiovascular diseases research.
|
-
- HY-117743
-
|
Eprosartan
SKF-108566J free base
|
Angiotensin Receptor
|
Cardiovascular Disease
|
|
Eprosartan (SKF-108566J free base) is a selective, competitive, nonpeptid and orally active angiotensin II receptor antagonist, used as an antihypertensive. Eprosartan binds angiotensin II receptor with IC50s of 9.2 nM and 3.9 nM in rat and human adrenal cortical membranes, respectively .
|
-
- HY-W539944
-
-
- HY-N10881
-
|
Dihydrocurcumenone
|
Others
|
Cardiovascular Disease
|
|
Dihydrocurcumenone is a carabrane-type sesquiterpene. Dihydrocurcumenone can be isolated from Curcuma zedoaria, and the common form is 4-dihydrocurcumenone. Curcuma zedoaria sesquiterpene has vascular relaxation activity. 4-dihydrocurcumenone can inhibit the high concentration of K + induced constriction of isolated rat aortic strips.
|
-
- HY-119615
-
|
Mezilamine
|
Adrenergic Receptor
|
Endocrinology
Neurological Disease
|
|
Mezilamine is a potent antidopaminergic agent. Mezilamine induces a concentration dependent increase in the electrically stimulated overflow of 3H-noradrenaline from rat cortical slices, without affecting the basal overflow. Mezilamine acts as a presynaptic α-adrenoceptor antagonist and a postsynaptic α-adrenoceptor agonist.
|
-
- HY-P1316A
-
|
Ac-RYYRWK-NH2 TFA
|
Opioid Receptor
|
Neurological Disease
|
|
Ac-RYYRWK-NH2 is a potent and selective partial agonist for the nociceptin receptor (NOP), [ 3H]Ac-RYYRWK-NH2 binds to rat cortical membranes ORL1 with a Kd of 0.071 nM, but has no affinity for µ-, κ- or δ-opioid receptors.
|
-
- HY-146456
-
|
A1AR antagonist 3
|
Adenosine Receptor
|
Neurological Disease
|
|
A1AR antagonist 3 (compound 13) is a selective adenosine 1 (A1) receptor antagonist with Kis of 9.69 nM and 0.529 nM for human A1 and rat A1, respectively. A1AR antagonist 3 can be used for researching neurological diseases.
|
-
- HY-108670
-
|
AZ 11645373
|
P2X Receptor
|
Inflammation/Immunology
|
|
AZ11645373 is a highly selective and potent antagonist at human but not rat P2X7 receptors，AZ11645373 inhibits ATP-evoked IL-1β release from lipopolysaccharide-activated THP-1 cells , with an IC50 value of 90 nM.
|
-
- HY-100459
-
|
GSK3179106
|
RET
|
Metabolic Disease
Inflammation/Immunology
|
|
GSK3179106 is an orally active and selective RET kinase inhibitor with IC50s of 0.4 nM, 0.2 nM for human RET and rat RET, respectively. GSK3179106 has the potential for irritable bowel syndrome (IBS) through the attenuation of post-inflammatory and stress-induced visceral hypersensitivity.
|
-
- HY-N7062
-
|
JNJ-1661010
Takeda-25
|
FAAH
|
Neurological Disease
|
|
JNJ-1661010 (Takeda-25) a potent and selective fatty acid amide hydrolase (FAAH) inhibitor with IC50s of 34 and 33 nM for rat FAAH and human FAAH, respectively. JNJ-1661010 can cross the blood-brain barrier and used as broad-spectrum analgesics.
|
-
- HY-N0539
-
|
Calceolarioside B
|
Aldose Reductase
|
Cancer
|
|
Calceolarioside B is a natural product isolated from Akebia quinata leaves. Calceolarioside B exhibits significant inhibitory activity against rat lens aldose reductase (RLAR) with an IC50 of 23.99 μM. Calceolarioside B displays inhibitory effect on DPPH radical scavenging activity with an IC50 of 94.60 μM .
|
-
- HY-120986
-
|
(S)-Bromoenol lactone
(S)-BEL; (S,E)-Bromoenol lactone
|
Phospholipase
|
Inflammation/Immunology
|
|
(S)-Bromoenol lactone ((S)-BEL) is an irreversible, chiral, mechanism-based inhibitor of calcium-independent phospholipase A2β (iPLA2β) that inhibits the vasopressin-induced release of arachidonate from cultured rat aortic smooth muscle (A10) cells with an IC50 of 2 µM.
|
-
- HY-126326
-
|
SWE101
|
Epoxide Hydrolase
|
Metabolic Disease
|
|
SWE101 (compound 22 b) is a potent soluble epoxide hydrolase (sEH)-P inhibitor with IC50s of 4 μM and 2.8 μM for human and rat sEH-P, respectively. SWE101 does not inhibit neither hydrolase nor phosphatase activity of the mouse sEH.
|
-
- HY-N1517
-
|
Ganoderic acid C2
|
Aldose Reductase
|
Cancer
|
|
Ganoderic acid C2 is a bioactive triterpenoid in Ganoderma lucidum. Ganoderic acid C2 possesses the potential anti-tumor bioactivity, antihistamine, anti-aging and cytotoxic effects. Ganoderic acid C2 exhibits high inhibitory activity against the rat lens aldose reductase (RLAR) with an IC50 of 3.8 µM.
|
-
- HY-N3007A
-
|
(E)-Naringenin chalcone
|
Others
|
Inflammation/Immunology
|
|
(E)-Naringenin chalcone is an orally active anti-allergic agent. (E)-Naringenin chalcone also has antioxidant, anti-inflammatory activities. (E)-Naringenin chalcone can improve adipocyte functions. (E)-Naringenin chalcone inhibits histamine release from rat peritoneal mast cell.
|
-
- HY-W020468
-
|
Linopirdine
DuP 996
|
Potassium Channel
TRP Channel
|
Neurological Disease
|
|
Linopirdine (DuP 996) is an orally active, selective M-type K + current (IM; Kv7; KCNQ Channels) inhibitor with an IC50 of 2.4 μM. Linopirdine is a TRPV1 agonist. Linopirdine, a putative cognition enhancing agent, increases acetylcholine release in rat brain tissue.
|
-
- HY-13632S
-
|
Exemestane-d2
FCE 24304-d2; EXE-d2
|
Cytochrome P450
Isotope-Labeled Compounds
|
Cancer
Endocrinology
|
|
Exemestane-d2 is the deuterium labeled Exemestane. Exemestane (FCE 24304) is a selective, irreversible and orally active steroidal aromatase inhibitor with IC50s of 30 nM and 40 nM for human placental and rat ovarian aromatase, respectively. Exemestane can be used for hormone-dependent breast cancer research[1][2].
|
-
- HY-130249
-
|
BAY-298
|
GnRH Receptor
|
Endocrinology
|
|
BAY-298 is an orally active and selective luteinizing hormone receptor (LH-R) antagonist with IC50s of 96 nM, 23 nM and 78 nM for hLH (human LH) and rLH (rat LH) and cLH (cynomolgus monkey LH), respectively. BAY-298 can reduce sex hormone levels.
|
-
- HY-108671
-
|
NF110
|
P2X Receptor
|
Neurological Disease
|
|
NF110 is a P2X3 receptor antagonist (Ki = 36 nM) and inactive toward P2Y receptors stably expressed (IC50s > 10 M). NF110 blocks alphabeta-methylene-ATP-induced currents (IC50 = 527 nM) in rat dorsal root ganglia neurons.
|
-
- HY-13632S2
-
|
Exemestane-d3
FCE 24304-d3; EXE-d3
|
Cytochrome P450
Isotope-Labeled Compounds
|
Cancer
Endocrinology
|
|
Exemestane-d3 is the deuterium labeled Exemestane. Exemestane (FCE 24304) is a selective, irreversible and orally active steroidal aromatase inhibitor with IC50s of 30 nM and 40 nM for human placental and rat ovarian aromatase, respectively. Exemestane can be used for hormone-dependent breast cancer research[1][2].
|
-
- HY-P3799
-
-
- HY-128976
-
-
- HY-101388
-
|
AM404
|
Others
|
Neurological Disease
|
|
AM404, an inhibitor of endocannabinoid reuptake, blocks anandamide transport with IC50 values in the low micromolar range. AM404 is able to relax rat isolated hepatic arteries contracted with Phenylephrine, with a pEC50 value of 7.4 (corresponding to an EC50 of 0.04 µM). Neuroprotective Effect.
|
-
- HY-18663B
-
|
CP-465022 hydrochloride
|
iGluR
|
Neurological Disease
|
|
CP-465022 hydrochloride is a potent, and selective noncompetitive AMPA receptor antagonist with anticonvulsant activity. CP-465022 is against Kainate-induced response with an IC50 of 25 nM in rat cortical neurons. CP-465022 provides a new tool to investigate the role of AMPA receptors in physiological and pathophysiological processes.
|
-
- HY-18663
-
|
CP-465022
|
iGluR
|
Neurological Disease
|
|
CP-465022 is a potent, and selective noncompetitive AMPA receptor antagonist with anticonvulsant activity. CP-465022 is against Kainate-induced response with an IC50 of 25 nM in rat cortical neurons. CP-465022 provides a new tool to investigate the role of AMPA receptors in physiological and pathophysiological processes.
|
-
- HY-118256
-
|
LSN2814617
|
mGluR
|
Neurological Disease
|
|
LSN2814617 is an orally active, potent, brain-penetrant, and selective mGlu5 (metabotropic glutamate 5) positive allosteric modulator (PAM), with EC50 values of 52 nM (Human mGlu5) and 42 nM (rat mGlu5). LSN2814617 shows wake-promoting effect. LSN2814617 can be used for schizophrenia research.
|
-
- HY-16434
-
|
DGAT1-IN-3
|
Acyltransferase
|
Metabolic Disease
|
|
DGAT1-IN-3 is a potent, selective and orally bioavailable inhibitor of DGAT-1, with IC50s of 38 nM for human DGAT-1 and 120 nM for rat DGAT-1. DGAT1-IN-3 could be used to research of obesity, dyslipidemia, and metabolic syndrome.
|
-
- HY-12378
-
|
BQ-123
|
Endothelin Receptor
|
Cardiovascular Disease
|
|
BQ-123 is a potent and selective endothelin A (ETA) receptor antagonist with an IC50 of 7.3 nM and a Ki of 25 nM. BQ-123 inhibits endothelin-1-mediated proliferation of human pulmonary artery smooth muscle cells and lowers blood pressure in different rat models of hypertension.
|
-
- HY-W008610
-
|
GBR 12783
|
Dopamine Receptor
|
Neurological Disease
|
|
GBR 12783 is a specific, potent and selective dopamine uptake inhibitor that inhibits the [ 3H]dopamine uptake by rat and mice striatal synaptosomes with IC50s of 1.8 nM and 1.2 nM, respectively. GBR 12783 can improve memory performance and increase hippocampal acetylcholine release in rats.
|
-
- HY-105327
-
|
P11149
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
P11149 is a competitive, BBB-penetarated weakly, orally active and selective inhibitor of AChE. P11149 exhibits an IC50 of 1.3 μM for rat BChE/AChE. P11149, a Galanthamine derivative, demonstrates central cholinergic activity, behavioral efficacy and safety. P11149 is used in the study for Alzheimer's disease.
|
-
- HY-100547
-
|
IEM-1754
|
iGluR
|
Neurological Disease
|
|
IEM-1754, a dicationic adamantane derivative, is a potent blocker of open channels of native ionotropic glutamate receptors including quisqualate-sensitive receptors in insect muscles, NMDAR in cultured rat cortical neurons, and AMPAR in freshly isolated hippocampal cells. IEM-1754 shows anticonvulsant potency in vivo.
|
-
- HY-18663A
-
|
CP-465022 maleate
|
iGluR
|
Neurological Disease
|
|
CP-465022 Maleate is a potent, and selective noncompetitive AMPA receptor antagonist with anticonvulsant activity. CP-465022 is against Kainate-induced response with an IC50 of 25 nM in rat cortical neurons. CP-465022 provides a new tool to investigate the role of AMPA receptors in physiological and pathophysiological processes.
|
-
- HY-151627
-
-
- HY-101854
-
-
- HY-100804
-
|
L-Cysteinesulfinic acid
|
mGluR
Endogenous Metabolite
|
Neurological Disease
|
|
L-Cysteinesulfinic acid is a potent agonist at several rat metabotropic glutamate receptors (mGluRs) with pEC50s of 3.92, 4.6, 3.9, 2.7, 4.0, and 3.94 for mGluR1, mGluR5, mGluR2, mGluR4, mGluR6, and mGluR8, respectively.
|
-
- HY-18977
-
|
KML29
|
MAGL
|
Metabolic Disease
Inflammation/Immunology
|
|
KML29 is an extremely selective, orally active and irreversible MAGL inhibitor, with IC50 values of 15 nM, 43 nM and 5.9 nM for mouse, rat and human MAGL, respectively. KML29 exhibits minimal cross-reactivity toward other central and peripheral serine hydrolases, including no detectable activity against FAAH.
|
-
- HY-W017230
-
|
L-Cysteinesulfinic acid monohydrate
|
mGluR
Endogenous Metabolite
|
Neurological Disease
|
|
L-Cysteinesulfinic acid monohydrate is a potent agonist at several rat metabotropic glutamate receptors (mGluRs) with pEC50s of 3.92, 4.6, 3.9, 2.7, 4.0, and 3.94 for mGluR1, mGluR5, mGluR2, mGluR4, mGluR6, and mGluR8, respectively.
|
-
- HY-18759
-
|
BMS-751324
|
p38 MAPK
TNF Receptor
|
Inflammation/Immunology
|
|
BMS-751324 is a p38α MAPK inhibitor. BMS-751324 equips a precursor of carbamyl-methyl linkage, containing esters and phosphate functional groups derived from hydroxyphenylacetic acid (HPA). BMS-751324 effectively inhibits foot swelling and LPS-induced TNFα production in an arthritic rat model.
|
-
- HY-14894
-
|
Ipragliflozin
ASP1941
|
SGLT
|
Metabolic Disease
|
|
Ipragliflozin (ASP1941) is an orally active and selective SGLT2 inhibitor with IC50s of 7.38 and 1876 nM, 6.73 and 1166 nM, 5.64 and 1380 nM for human SGLT2 and SGLT1, rat SGLT2 and SGLT1, mouse SGLT2 and SGLT1, respectively. Antidiabetic agent.
|
-
- HY-13632S1
-
|
Exemestane-13C3
|
Cytochrome P450
Isotope-Labeled Compounds
|
Cancer
Endocrinology
|
|
Exemestane- 13C3 is the 13C-labeled Exemestane. Exemestane (FCE 24304) is a selective, irreversible and orally active steroidal aromatase inhibitor with IC50s of 30 nM and 40 nM for human placental and rat ovarian aromatase, respectively. Exemestane can be used for hormone-dependent breast cancer research[1][2].
|
-
- HY-P1091A
-
|
Hemopressin(human, mouse) TFA
|
Cannabinoid Receptor
|
Neurological Disease
|
|
Hemopressin TFA is a nonapeptide derived from the α1-chain of hemoglobin, is originally isolated from rat brain homogenates. Hemopressin TFA is orally active, selective and inverse agonist of CB1 cannabinoid receptors. Hemopressin TFA exerts antinociceptive action in inflammatory pain models.
|
-
- HY-116790
-
-
- HY-N0745
-
|
Senkyunolide I
|
Caspase
|
Inflammation/Immunology
|
|
Senkyunolide I, isolated from Ligusticum chuanxiong Hort, is an anti-migraine compound. Senkyunolide I protects rat brain against focal cerebral ischemia-reperfusion injury by up-regulating p-Erk1/2, Nrf2/HO-1 and inhibiting caspase 3.
|
-
- HY-120170
-
-
- HY-50688
-
|
SB-265610
|
CXCR
|
Inflammation/Immunology
|
|
SB-265610 is a selective, competitive, nonpeptide and allosteric CXCR2 antagonist. SB-265610 blocks rat cytokine-induced neutrophil chemoattractant-1 (CINC-1)-induced calcium mobilization and neutrophil chemotaxis with IC50s of 3.7 nM and 70 nM, respectively.
|
-
- HY-110199
-
|
TC-I 2014
|
TRP Channel
|
Neurological Disease
|
|
TC-I 2014 (compound 5) is a potent and orally active Benzimidazole-containing transient receptor potential melastatin 8 (TRPM8) antagonist, with IC50 values of 0.8 nM, 3.0 nM and 4.4 nM for canine, human and rat channels respectively. TC-I 2014 exhibits antiallodynic properties in pain models.
|
-
- HY-122635
-
|
T-448 free base
|
Histone Demethylase
|
Neurological Disease
|
|
T-448 free base is a specific, orally active and irreversible inhibitor of lysine-specific demethylase 1 (LSD1, an H3K4 demethylase), with an IC50 of 22 nM. T-448 free base enhances H3K4 methylation in primary cultured rat neurons.
|
-
- HY-N0033
-
-
- HY-B0182
-
|
Carmofur
HCFU
|
Nucleoside Antimetabolite/Analog
SARS-CoV
Virus Protease
|
Cancer
|
|
Carmofur (HCFU), a derivative of 5-Fluorouracil, is an antineoplastic agent. Carmofur is an inhibitor of acid ceramidase with an IC50 of 79 nM for the rat enzyme. Carmofur inhibits the SARS-CoV-2 main protease (Mpro). Carmofur Inhibits SARS-CoV-2 in Vero E6 cell with an EC50 of 24.3 μM.
|
-
- HY-100968
-
|
GBR 12783 dihydrochloride
|
Dopamine Receptor
|
Neurological Disease
|
|
GBR 12783 dihydrochloride is a specific, potent and selective dopamine uptake inhibitor that inhibits the [ 3H]dopamine uptake by rat and mice striatal synaptosomes with IC50s of 1.8 nM and 1.2 nM, respectively. GBR 12783 dihydrochloride can improve memory performance and increase hippocampal acetylcholine release in rats.
|
-
- HY-111191A
-
|
(R)-ONO-2952
|
Others
|
Neurological Disease
|
|
(R)-ONO-2952 is a R-enantiomer of ONO-2952. ONO-2952 is a potent, selective and orally active TSPO antagonist with Kis of 0.33-9.30 nM for rat and human TSPO. ONO-2952 is more selective for TSPO than other receptors, transporters, ion channels and enzymes.
|
-
- HY-119226
-
|
VU0152099
|
mAChR
|
Neurological Disease
|
|
VU0152099 is a potent, selective and brain-penetrant mAChR M4 positive allosteric modulator with an EC50 of 0.4 µM for rat M4 receptor. VU0152099 is inactive for other mAChR subtypes or other GPCRs. VU0152099 has no agonist activity but potentiated responses of M4 to acetylcholine.
|
-
- HY-103327
-
|
MJ15
|
Cannabinoid Receptor
|
Metabolic Disease
|
|
MJ15 is a potent and selective CB1 receptor antagonist with a Ki of 27.2 pM and an IC50 of 118.9 pM for rat CB1 receptors. MJ15 exhibits potency in obesity and hyperlipidemia models. MJ15 inhibits food intake and increases in body weight in diet-induced obese rats and mice.
|
-
- HY-100125
-
|
Timegadine
SR1368
|
COX
|
Inflammation/Immunology
|
|
Timegadine, a new antiinflammatory agent, is found to be a potent, competitive inhibitor of cyclo-oxygenase (COX) and lipo-oxygenase, with IC50s ranging from 5 nM (washed rabbit platelets) to 20 μM (rat brain) for COX and 100 μM for lipo-oxygenase both in the cytosol fraction of horse platelet homogenates, and in washed rabbit platelets.
|
-
- HY-108669
-
|
AZ10606120 dihydrochloride
|
P2X Receptor
|
Cancer
Neurological Disease
|
|
AZ10606120 dihydrochloride is a selective, high affinity antagonist for P2X7 receptor (P2X7R) at human and rat with an IC50 of ~10 nM. AZ10606120 dihydrochloride is little or no effect at other P2XR subtypes. AZ10606120 dihydrochloride has anti-depressant effects and reduces tumour growth.
|
-
- HY-112102
-
|
(22S,23S)-Homobrassinolide
SSHB
|
Others
|
Metabolic Disease
|
|
(22S,23S)-Homobrassinolide is one of the most active brassinosteroids in inducing plant growth in various plant bioassay systems. (22S,23S)-Homobrassinolide shows Akt-dependent anabolic activity in rat skeletal muscle cells. Orally active.
|
-
- HY-P1214A
-
-
- HY-145387
-
|
MRT-81
|
Smo
|
Cancer
|
|
MRT-81 is a potent antagonist of human and rodent smoothened (Smo) receptors, with an IC50 value of 41 nM in the Shh-light2 cells. MRT-81 has potent hedgehog inhibiting activity. MRT-81 can be used for the research of cancer.
|
-
- HY-B0919
-
|
Azaserine
CI-337; O-Diazoacetyl-L-serine; P-165
|
Bacterial
Antibiotic
DNA/RNA Synthesis
|
Cancer
Infection
|
|
Azazerine (CI-337) is a competitive inhibitor of glutamine amidotransferase. Azaserine is an antibiotic, it shows antibacterial activities. Azazerine shows anti-tumor activities and it may also act as a tumor inducer. Azazerine can be used for the research of cancer and infection.
|
-
- HY-N9182
-
|
Zeaxanthin dipalmitate
Physalien
|
Adiponectin Receptor
P2X Receptor
Autophagy
|
Inflammation/Immunology
|
|
Zeaxanthin dipalmitate (Physalien) is a wolfberry-derived carotenoid, has anti-inflammatory and anti-oxidative stress effects. Zeaxanthin dipalmitate directly interact with p2X7 receptor (Kd=81.2 nM) and adiponectin receptor 1 (AdipoR1; Kd=533 nM) in a positive dose-dependent manner. Zeaxanthin dipalmitate restores mitochondrial autophagy functions suppressed by ethanol intoxication. Zeaxanthin dipalmitate can be used in the research of alcoholic fatty liver disease (AFLD) and retinitis pigmentosa (RP).
|
-
- HY-121383
-
-
- HY-P2813
-
|
Hirudin
|
Thrombin
Apoptosis
|
Cancer
Cardiovascular Disease
|
|
Hirudin is a thrombin inhibitor with blood anticoagulant property. Hirudin has potent anti-thrombotic, wound repair, anti-fibrosis, anti-tumor and anti-hyperuricemia effects. Hirudin also affects diabetic complications, cerebral hemorrhage, and others.
|
-
- HY-132126
-
|
SPHINX
|
SRPK
|
Others
|
|
SPHINX is a selective SRPK1 inhibitor with an IC50 value of 0.58 μM. SPHINX effectively reduces Choroidal Neovascularization (CNV) in vivo. SPHINX can be used for the research of (age-related macular degenaration) AMD.
|
-
- HY-114782
-
-
- HY-18137
-
|
PF-04995274
|
5-HT Receptor
|
Neurological Disease
|
|
PF-04995274 is a potent, high-affinity, orally active and partial serotonin 4 receptor (5-HT4R) agonist. PF-04995274 has an EC50 range of 0.26-0.47 nM for human 5-HT4A/4B/4D/4E (Ki range of 0.15-0.46 nM), and has an EC50 range of 0.59-0.65 nM for rat 5-HT4S/4L/4E (Ki of 0.30 nM for rat 5-HT4S). PF-04995274 is brain penetrant and can be used for cognitive disorders associated with Alzheimer's disease.
|
-
- HY-P1428A
-
|
RFRP-1(human) TFA
|
Neuropeptide Y Receptor
|
|
|
RFRP-1(human) TFA is a potent endogenous NPFF receptor agonist (EC50 values are 0.0011 and 29 nM for NPFF2 and NPFF1, respectively). Attenuates contractile function of isolated rat and rabbit cardiac myocytes. Reduces heart rate, stroke volume, ejection fraction and cardiac output, and increases plasma prolactin levels in rats.
|
-
- HY-18698
-
|
L-701324
|
iGluR
|
Neurological Disease
|
|
L-701324 is a potent, orally active NMDA receptor antagonist that antagonizes the activity of the NMDA receptor by blocking its glycine B binding site. L-701324 binds with high affinity to rat brain membranes (IC50=2 nM). L-701324 has antidepressant activity.
|
-
- HY-122051
-
|
AC1903
|
TRP Channel
|
Metabolic Disease
|
|
AC1903 is a specific and selective inhibitor of TRPC5 and has podocyte-protective properties. AC1903 does no effects on TRPC4 or TRPC6 currents and shows no off-target effects in kinase profiling assays. AC1903 suppresses severe proteinuria and prevents podocyte loss in focal segmental glomerulosclerosis (FSGS) rat model.
|
-
- HY-106301
-
|
Devazepide
L-364,718; MK-329
|
Cholecystokinin Receptor
|
Metabolic Disease
|
|
Devazepide (L-364,718) is a potent, competitive, selective and orally active nonpeptide antagonist of cholecystokinin (CCK) receptor, with IC50s of 81 pM, 45 pM and 245 nM for rat pancreatic, bovine gallbladder and guinea pig brain CCK receptors, respectively. Devazepide (L-364,718) is effective for gastrointestinal disorders.
|
-
- HY-110161
-
-
- HY-113149
-
|
Argininosuccinic acid
|
Endogenous Metabolite
Reactive Oxygen Species
|
Inflammation/Immunology
|
|
Argininosuccinic acid participates in the fourth step of the urea cycle, with being cleaved to arginine and fumaric acid by argininosuccinic acid lyase (ASL). Argininosuccinic acid reduces reduced glutathione (GSH) level, and increases the production of reactive oxygen species in cerebral cortex and striatum. Argininosuccinic acid causes lipid peroxidation and protein oxidation, and induces oxidative stress in the developing rat brain.
|
-
- HY-100675
-
|
JTE-013
|
LPL Receptor
Apoptosis
|
Cancer
|
|
JTE-013 is a potent and specific S1P2 (Sphingosine-1-Phosphate 2; EDG-5) antagonist. JTE-013 inhibits the specific binding of radiolabeled S1P to human and rat S1P2 with IC50s of 17 nM and 22 nM, respectively.
|
-
- HY-107526
-
|
(Rac)-ALX 5407
(Rac)-NFPS
|
GlyT
|
Neurological Disease
|
|
NFPS is a selective, non-competitive glycine transporter-1 (GlyT1) inhibitor with IC50s of 2.8 nM and 9.8 nM for hGlyT1 and rGlyT1, respectively. NFPS exerts neuroprotection via glyR alpha1 subunit in the rat model of transient focal cerebral ischaemia and reperfusion.
|
-
- HY-119152
-
|
CMX-2043
|
Insulin Receptor
Tyrosinase
Akt
|
Others
|
|
CMX-2043 is a novel analogue of α-Lipoic Acid (HY-N0492). CMX-2043 is effective in antioxidant effect, activation of insulin receptor kinase, soluble tyrosine kinase, and Akt phosphorylation. CMX-2043 shows protection against ischemia-reperfusion injury (IRI) in rat model.
|
-
- HY-B1816
-
-
- HY-135671
-
-
- HY-12143
-
-
- HY-151360
-
|
NHE3-IN-3
|
Sodium Channel
|
Metabolic Disease
|
|
NHE3-IN-3 (Compound 1) is a Na +/H + exchanger isoform 3 (NHE3) inhibitor with pIC50 of 6.2 and 6.6 against human and rat NHE3, respectively. NHE3-IN-3 shows high (98%) oral bioavailability in Sprague–Dawley rats.
|
-
- HY-13104
-
-
- HY-N8593S
-
|
Undecane-d24
|
TNF Receptor
|
Infection
|
|
Undecane-d24 is the deuterium labeled Undecane[1]. Undecane has anti-allergic and anti-inflammatory activities on sensitized rat basophilic leukemia (RBL-2H3) mast cells and HaCaT keratinocytes. In sensitized mast cells, Undecane inhibits degranulation and the secretion of histamine and TNF-α[2].
|
-
- HY-U00322
-
-
- HY-123812
-
-
- HY-145086
-
|
R-PSOP
|
Others
|
Metabolic Disease
|
|
R-PSOP is highly potent and selective nonpeptidic NMUR2 antagonist. R-PSOP binds to NMUR2 with the Kis of 52 and 32 nM for the human and rat NMUR2, respectively. R-PSOP shows moderate CNS penetration. R-PSOP can be used for the research of the eating disorders, obesity, pain, and stress-related disorders.
|
-
- HY-118482
-
|
Sauristolactam
Saurolactam
|
Others
|
Neurological Disease
|
|
Sauristolactam, a natural aristolactam isolated from aerial portions of Saururus chinensis, has significant neuroprotective activity against glutamate-induced toxicity in primary cultured rat cortical cells. Sauristolactam also inhibits the receptor activator of nuclear factor-κB ligand (RANKL)-induced osteoclastogenesis and has the potential to inhibit osteoclast differentiation.
|
-
- HY-144110
-
|
HCV-IN-37
|
HCV
|
Infection
|
|
HCV-IN-37 (Compound 3d) is a potent inhibitor of HCV. HCV-IN-37 is orally available and long-lasting in rat plasma after oral administration to rats by a single dose of 15 mg/kg. The high potency of active derivative HCV-IN-37 is primarily driven by the inhibitory effect on the virus entry stage.
|
-
- HY-12378A
-
|
BQ-123 TFA
|
Endothelin Receptor
|
Cardiovascular Disease
|
|
BQ-123 TFA is a potent and selective endothelin A (ETA) receptor antagonist with an IC50 of 7.3 nM and a Ki of 25 nM. BQ-123 TFA inhibits endothelin-1-mediated proliferation of human pulmonary artery smooth muscle cells and lowers blood pressure in different rat models of hypertension.
|
-
- HY-15112
-
|
JTP-4819
|
Prolyl Endopeptidase (PREP)
|
|
|
JTP-4819 is a potent and specific inhibitor of prolyl endopeptidase (PREP) with IC50s of 0.83 nM (in rat brain supernatant) and 5.43 nM (in Flavobacterium meningosepticum). JTP-4819 has blood-brain penetration, also improves the retention time of amnesia rats induced by Scopolamine (HY-N2096).
|
-
- HY-14806S1
-
|
Teneligliptin-d4
MP-513-d4
|
Dipeptidyl Peptidase
|
Metabolic Disease
|
|
Teneligliptin-d4 is deuterium labeled Teneligliptin. Teneligliptin (MP-513) is a potent, orally available, competitive, and long-lasting DPP-4 inhibitor. Teneligliptin competitively inhibits human plasma, rat plasma, and human recombinant DPP-4 in vitro, with IC50s of approximately 1 nM[1].
|
-
- HY-111615
-
|
J-2156
|
Somatostatin Receptor
|
Neurological Disease
|
|
J-2156 is a high potent, selective somatostatin receptor type 4 (SST4 receptor) agonist with IC50s of 0.05 nM and 0.07 nM for human and rat SST4 receptors, respectively. J-2156 is used for the relief of mechanical allodynia and mechanical hyperalgesia in the ipsilateral hindpaws in rats.
|
-
- HY-142088
-
|
Beauverolide Ka
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Beauverolide Ka, a cyclotetradepsipeptide, is a metabolite of Beauveria bassiana fungus. Beauverolide Ka stimulates glucose uptake in cultured rat L6 myoblasts at 50 μM. Beauverolide Ka exhibits protecting effects on HEI-OC1 cells at 10 μM and shows dose-dependent activity in both L6 myoblasts and myotubes.
|
-
- HY-101418
-
|
JNJ-47965567
|
P2X Receptor
|
Neurological Disease
|
|
JNJ-47965567 is a centrally permeable, high-affinity, selective P2X7 antagonist, with pKis of 7.9 and 8.7 for human and rat P2X7, respectively. JNJ-47965567 can be used to probe the role of central P2X7 in rodent models of CNS pathophysiology.
|
-
- HY-15314
-
|
Ranirestat
AS-3201
|
Aldose Reductase
|
Metabolic Disease
Neurological Disease
|
|
Ranirestat (AS-3201) potent and orally active aldose reductase (AR) inhibitor with IC50s of 11 nM and 15 nM for rat lens AR and recombinant human AR, respectively, and a Ki of 0.38 nM for recombinant human AR. Ranirestat has the potential for diabetic sensorimotor polyneuropathy treatment. Ranirestat also has a neuroprotective effect on diabetic retinas.
|
-
- HY-101075
-
|
L-690330
|
Phosphatase
|
Others
|
|
L-690330 is a competitive inhibitor of inositol monophosphatase (IMPase) with Kis of 0.27 and 0.19 μM for recombinant human and bovine IMPase, 0.30 and 0.42 μM for human and bovine frontal cortex IMPase, respectively. L-690330 exhibits 10-fold more sensitive than mouse and rat IMPase.
|
-
- HY-103133
-
|
WAY208466 dihydrochloride
|
5-HT Receptor
|
Neurological Disease
|
|
WAY 208466 dihydrochloride is a potent and selective 5-HT6 receptor agonist (EC50=7.3 nM for the human 5-HT6 receptor). WAY-208466 dihydrochloride elevates cortical GABA levels in rat frontal cortex. WAY 208466 dihydrochloride exhibits antidepressant and anxiolytic-like effects.
|
-
- HY-16210
-
|
Forodesine
BCX-1777; Immucillin-H
|
Nucleoside Antimetabolite/Analog
Apoptosis
|
Cancer
|
|
Forodesine (BCX-1777) is a highly potent and orally active purine nucleoside phosphorylase (PNP) inhibitor with IC50 values ranging from 0.48 to 1.57 nM for human, mouse, rat, monkey and dog PNP. Forodesine is a potent human lymphocyte proliferation inhibitor. Forodesine could induce apoptosis in leukemic cells by increasing the dGTP levels.
|
-
- HY-P2501
-
|
Amylin (8-37), human
|
Amylin Receptor
|
Metabolic Disease
|
|
Amylin (8-37), human is a fragment of human Amylin. Amylin (8-37), human has direct vasodilator effects in the isolated mesenteric resistance artery of the rat. Human Amylin is a small hormone secreted by pancreatic β-cells that forms aggregates under insulin deficiency metabolic conditions, and it constitutes a pathological hallmark of type II diabetes mellitus.
|
-
- HY-18662
-
|
RQ-00203078
|
TRP Channel
|
Cancer
Neurological Disease
|
|
RQ-00203078 is a highly selective, potent and orally active TRPM8 antagonist with IC50s of 5.3 nM and 8.3 nM for rat and human TRPM8 channels, respectively. RQ-00203078 shows little inhibitory action against TRPV1, TRPA1, TRPV4, or TRPM2 channels.
|
-
- HY-117743S
-
|
Eprosartan-d3
|
Angiotensin Receptor
|
Cardiovascular Disease
|
|
Eprosartan-d3 is the deuterium labeled Eprosartan. Eprosartan (SKF-108566J free base) is a selective, competitive, nonpeptid and orally active angiotensin II receptor antagonist, used as an antihypertensive. Eprosartan binds angiotensin II receptor with IC50s of 9.2 nM and 3.9 nM in rat and human adrenal cortical membranes, respectively [1].
|
-
- HY-142723
-
-
- HY-101478
-
|
Fenobam
|
mGluR
|
Neurological Disease
|
|
Fenobam is a selective, orally active, and brain-penetrant mGluR5 antagonist acting at an allosteric modulatory site (Kds of 54 and 31 nM for rat and human recombinant mGlu5 receptors, respectively). Fenobam displays inverse agonist activity which blocks the mGlu5 receptor basal activity with an IC50 of 84 nM. Fenobam exerts anxiolytic activity.
|
-
- HY-101075A
-
|
L-690330 hydrate
|
Phosphatase
|
Others
|
|
L-690330 hydrate is a competitive inhibitor of inositol monophosphatase (IMPase) with Kis of 0.27 and 0.19 μM for recombinant human and bovine IMPase, 0.30 and 0.42 μM for human and bovine frontal cortex IMPase, respectively. L-690330 hydrate exhibits 10-fold more sensitive than mouse and rat IMPase.
|
-
- HY-14418
-
|
VU0361737
ML-128
|
mGluR
|
Neurological Disease
|
|
VU0361737 (ML-128) is a potent, selective and CNS penetrant positive allosteric modulator of metabotropic glutamate receptor 4 (mGluR4 PAM), with EC50s of 240 nM and 110 nM for human and rat mGluR4 receptors, respectively. VU0361737 has neuroprotective effect. VU0361737 is potential for Parkinson's disease research.
|
-
- HY-N6704
-
|
Enniatin A1
|
ERK
Apoptosis
|
Cancer
|
|
Enniatin A1 isolated from Fusarium mycotoxins is a cyclic hexadepsipeptide consisting of alternating D-α-hydroxyisovaleric acids and N-methyl-L-amino acids. Enniatin A1 possesses anticarcinogenic properties by induction of apoptosis and disruption of ERK signalling pathway. Enniatin A1 inhibits ACAT with an IC50 of 49 μM in rat liver microsomes.
|
-
- HY-N0061
-
|
Ethyl ferulate
|
Reactive Oxygen Species
|
Neurological Disease
|
|
Ethyl ferulate, a naturally lipophilic derivative of ferulic acid originally derived from Rhizoma Chuanxiong, induces heme oxygenase-1 (HO-1) and protects rat neurons against oxidative stress. Ethyl ferulate also protects neurons against amyloid β peptide (1-42)-induced oxidative stress and neurotoxicity.
|
-
- HY-16209
-
|
Forodesine hydrochloride
BCX-1777 hydrochloride; Immucillin-H hydrochloride
|
Nucleoside Antimetabolite/Analog
Apoptosis
|
Cancer
|
|
Forodesine hydrochloride (BCX-1777 hydrochloride) is a highly potent and orally active purine nucleoside phosphorylase (PNP) inhibitor with IC50 values ranging from 0.48 to 1.57 nM for human, mouse, rat, monkey and dog PNP. Forodesine hydrochloride is a potent human lymphocyte proliferation inhibitor. Forodesine hydrochloride could induce apoptosis in leukemic cells by increasing the dGTP levels.
|
-
- HY-13706
-
|
CAY10471 Racemate
TM30089 Racemate
|
Prostaglandin Receptor
|
Cancer
Endocrinology
|
|
CAY10471 Racemate (TM30089 Racemate) is a potent and highly selective prostaglandin D2 receptor CRTH2 antagonist, with a Ki of 0.6 nM for hCRTH2, selective over human thromboxane A2 receptor TP (Ki, >10000 nM) or PGD2 receptor DP (Ki, 1200 nM). CAY10471 Racemate also has effect on mouse and rat orthologs of CRTH2.
|
-
- HY-P3801
-
|
[Glp5,(Me)Phe8,Sar9] Substance P (5-11)
DiMe-C7
|
Neurokinin Receptor
|
Metabolic Disease
Neurological Disease
Others
|
|
[Glp5,(Me)Phe8,Sar9] Substance P (5-11) (DiMe-C7) is a Substance P (HY-P0201) analogue that has approximately the same effects as Substance P (HY-P0201) on neurokinin 1 receptor (NK1R) in rat brain, but with a much longer duration of action. [Glp5,(Me)Phe8,Sar9] Substance P (5-11) selectively activates dopamine metabolism in the mesencephalon and midbrain cortex of the rat brain. [Glp5,(Me)Phe8,Sar9] Substance P (5-11) also increases motor activity and induces recovery of addictive agent-seeking behavior in rats.
|
-
- HY-148258
-
-
- HY-136939
-
-
- HY-D1635
-
|
Sulfo-NHS-LC-LC-Biotin
Biotin-XX-SSE
|
Fluorescent Dye
|
Infection
|
|
Sulfo-NHS-LC-LC-Biotin (Biotin-XX-SSE), a biotin reagent, is used to label the proteins exposed to the external leaflet of intact exosomes and contains a larger spacer arm between the biotin and amine reactive linker. The size of this linker helps to overcome steric hindrance and increases labeling efficiency at the crowded exosome surface.
|
-
- HY-14218
-
|
Ditolylguanidine
1,3-Di-o-tolylguanidine; DTG
|
Sigma Receptor
|
Neurological Disease
|
|
Ditolylguanidine (1,3-Di-o-tolylguanidine) is an agonist of sigma receptor (σ1/σ2 receptor) with Ki values of 69 and 21 nM for σ1 and σ2 receptors, respectively. Ditolylguanidine effectively inhibits the growth of small cell lung cancer cells. Ditolylguanidine can be used for the research of lung cancer.
|
-
- HY-146662
-
|
HPGDS inhibitor 3
|
PGE synthase
|
Inflammation/Immunology
|
|
HPGDS inhibitor 3 is an orally active and highly potent peripherally restricted hematopoietic prostaglandin D synthase (H-PGDS) inhibitor with IC50 value of 9.4 nM and EC50 of 42 nM, respectively. HPGDS inhibitor 3 exhibits good selectivity, good pharmacokinetic parameters in mouse, rat, and dog, and no CNS toxicity. HPGDS inhibitor 3 has anti-inflammatory activity.
|
-
- HY-P3355
-
|
p-fin4
|
iGluR
|
Neurological Disease
|
|
p-fin4 is a peptide inhibitor of STEP Phosphatase-GluA2 AMPA receptor interaction with a Ki of 0.4 μM. p-fin4 restores the memory deficits and displays anxiolytic and antidepressant effects in a scopolamine-treated rat model. p-fin4 is a promising lead compound for novel cognitive enhancers and/or behavioral modulators.
|
-
- HY-N7056
-
|
4'-Hydroxychalcone
|
Proteasome
|
Cancer
Inflammation/Immunology
|
|
4'-Hydroxychalcone is a chalcone isolated from licorice root, with hepatoprotective activity. 4'-Hydroxychalcone inhibits TNFα-induced NF-κB activation via proteasome inhibition. 4'-Hydroxychalcone induces a rapid potassium release from mitochondrial vesicles and causes deterioration of respiratory control and oxidative phosphorylation of isolated rat liver mitochondria.
|
-
- HY-101250
-
-
- HY-106993A
-
|
Cipralisant maleate
GT-2331 maleate
|
Histamine Receptor
|
Neurological Disease
|
|
Cipralisant (GT-2331) (maleate) is an orally active, low-toxicity, potent, selective, high affinity histamine H3 receptor full antagonist in vivo, and an agonist in vitro, with a pKi of 9.9 for histamine H3 receptor and a Ki of 0.47 nM for rat histamine H3 receptor. Cipralisant (maleate) has the potential for attention-deficit hyperactivity disorder research.
|
-
- HY-106961
-
|
ONO 1301
ONO-AP 500-02
|
Prostaglandin Receptor
|
Cardiovascular Disease
|
|
ONO 1301 (ONO-AP 500-02), a prostaglandin (PG) I2 mimetic, is an orally active, long-acting prostacyclin agonist with thromboxane-synthase inhibitory activity. ONO 1301 promotes production of hepatocyte growth factor (HGF) from various cell types and ameliorates ischemia-induced left ventricle dysfunction in the mouse, rat and pig.
|
-
- HY-13413
-
|
Tofogliflozin (hydrate)
CSG-452 hydrate
|
SGLT
Reactive Oxygen Species
|
Metabolic Disease
|
|
Tofogliflozin hydrate (CSG-452 hydrate) is a potent and highly specific sodium/glucose cotransporter 2 (SGLT2) inhibitor with an IC50 of 2.9 nM and Ki values of 2.9 nM, 14.9 nM, and 6.4 nM for human, rat, and mouse SGLT2. Tofogliflozin partially inhibits high glucose-induced reactive oxyen species (ROS) generation in tubular cells.
|
-
- HY-P1022
-
|
Kisspeptin-54(human)
Metastin(human)
|
GnRH Receptor
|
Cancer
Endocrinology
|
|
Kisspeptin-54(human) (Metastin(human)) is an endogenous ligand for kisspeptin receptor (KISS1, GPR54). Kisspeptin-54(human) binds to rat and human GPR54 receptors with Ki values of 1.81 nM and 1.45 nM, respectively. Kisspeptin-54(human) hinders tumor metastasis and stimulates gonadotropin secretion.
|
-
- HY-103193
-
|
NKH477
Colforsin dapropate hydrochloride
|
Adenylate Cyclase
|
Cardiovascular Disease
|
|
NKH477 (Colforsin dapropate hydrochloride) directly activates the catalytic unit of adenylate cyclase and increases intracellular cAMP. NKH477 is a forskolin derivative that improves cardiac failure mainly through its beneficial effects on diastolic cardiac function. NKH477 exerts an antiproliferative effect in vivo with an altered cytokine profile to inhibit the acute rejection of rat orthotopic lung allografts.
|
-
- HY-W013712
-
|
GI-530159
|
Potassium Channel
|
Neurological Disease
|
|
GI-530159 is a selective opener of TREK1 and TREK2 potassium channels. GI-530159 displays selectivity for TREK1/2 over TRAAK, TASK3 and other potassium channels, with an EC50 of 0.76 μM for TREK1. GI-530159 reduces rat dorsal root ganglion neuron excitability and shows potential analgesic effect.
|
-
- HY-153091
-
-
- HY-138793
-
|
2-(2,6-Dioxopiperidin-3-yl)phthalimidine
EM-12
|
Others
|
Cancer
|
|
2-(2,6-Dioxopiperidin-3-yl)phthalimidine (EM-12), a teratogenic Thalidomide analogue, is more active than Thalidomide and is much more stable for hydrolysis. 2-(2,6-Dioxopiperidin-3-yl)phthalimidine enhances 1,2-dimethylhydrazine-induction of rat colon adenocarcinomas.
|
-
- HY-115553
-
|
DETQ
|
Dopamine Receptor
|
Neurological Disease
|
|
DETQ is a selective, allosteric and orally active dopamine D1 receptor (Dopamine Receptor) potentiator. In HEK293 cells expressing the human D1 receptor, DETQ increases cAMP with an EC50 of 5.8 nM and a Kb of 26 nM. DETQ shows ~30-fold less potent at rat and mouse D1 receptors and is inactive at the human D5 receptor.
|
-
- HY-105115
-
|
Abecarnil
ZK 112119
|
GABA Receptor
|
Neurological Disease
|
|
Abecarnil (ZK 112119) is a ligand or a partial agonist for benzodiazepine (BZ) receptor. Abecarnil possesses anxiolytic and anticonvulsant properties. Abecarnil can act as a positive allosteric modulator of GABAA receptor. Abecarnil inhibits the binding of the BZ [3H]lormetazepam to rat cerebral cortex membranes, with an IC50 of 0.82 nM. Abecarnil can be used for epilepsy research.
|
-
- HY-103445
-
|
SSR69071
|
Elastase
|
Cardiovascular Disease
|
|
SSR69071 is a potent, orally active and selective inhibitor of neutrophil elastase. SSR69071 reduces myocardial infarct size following ischemia-reperfusion injury. SSR69071 displays a higher affinity for human elastase (Ki=0.0168 nM) than for rat (Ki=3 nM), mouse (Ki=1.8 nM), and rabbit (Ki= 58 nM) elastases.
|
-
- HY-103104
-
|
Fananserin
RP 62203
|
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
|
Fananserin (RP 62203) is an orally bioavailable, potent and selective 5-hydroxytryptamine2 (5-HT2) receptor antagonist, with a Ki of 0.37 nM for the rat 5-HT2A receptor. Fananserin also is a selective dopamine D4 receptor antagonist, with a Ki of 2.93 nM for the human dopamine D4 receptor.
|
-
- HY-152118
-
|
CYP1B1-IN-4
|
Cytochrome P450
|
Cancer
|
|
CYP1B1-IN-4 is a 2,4-diarylthiazole compound with selectively CYP1B1 inhibition (IC50=0.2 nM). CYP1B1-IN-4 has little cytotoxicity and high stability in both human and rat liver microsomes.
|
-
- HY-P4052
-
|
Pinealon
|
ROS Kinase
|
Neurological Disease
|
|
Pinealon is a 3-amino acid peptide and shows neuroprotective properties. Pinealon prevents reactive oxygenspecies (ROS) accumulation and supressesthe activation of ERK 1/2. Pinealon has the ability to stimulate the functional activity of the main cellular elements of brain tissue, reduce the level of spontaneous cell death. Pinealon protects the rat offspring from prenatal hyperhomocysteinemia.
|
-
- HY-126419
-
|
Kobophenol A
|
SARS-CoV
PKC
|
Infection
|
|
Kobophenol A, an oligomeric stilbene, blocks the interaction between the ACE2 receptor and S1-RBD with an IC50 of 1.81 μM and inhibits SARS-CoV-2 viral infection in cells with an EC50 of 71.6 μM. Kobophenol A inhibits the activity of partially purified rat brain protein kinase C (PKC) with an IC50 of 52 µM.
|
-
- HY-112603A
-
|
AP5 sodium
|
Free Fatty Acid Receptor
|
Metabolic Disease
|
|
AP5 sodium is a potent, orall active, and selective GPR40 receptor agonist with a positive allosteric modulation of endogenous ligand (AgoPAM). AP5 sodium demonstrates rat and human inositol monophosphate (IP1) EC50 values of 0.49 nM and 0.8 nM against the GPR40 receptor, respectively. AP5 sodium has the potential for type II diabetes research.
|
-
- HY-103263
-
-
- HY-147927
-
|
Human enteropeptidase-IN-1
|
Others
|
Metabolic Disease
|
|
Human enteropeptidase-IN-1 (compound 6b) is a highly potent, orally active and low systemic exposure enteropeptidase inhibitor. Human enteropeptidase-IN-1 boosts the increase in fecal protein output, and exhibits potent body weight loss in diet-induced obese (DIO) rat model. Human enteropeptidase-IN-1 can be used for anti-obesity research.
|
-
- HY-106993
-
|
Cipralisant
GT-2331
|
Histamine Receptor
|
Neurological Disease
Endocrinology
|
|
Cipralisant (GT-2331) is an orally active, low-toxicity, potent, selective, high affinity histamine H3 receptor full antagonist in vivo, and an agonist in vitro, with a pKi of 9.9 for histamine H3 receptor and a Ki of 0.47 nM for rat histamine H3 receptor. Cipralisant has the potential for attention-deficit hyperactivity disorder research.
|
-
- HY-112603
-
|
AP5
|
Free Fatty Acid Receptor
|
Metabolic Disease
|
|
AP5 is a potent, orlly active, and selective GPR40 receptor agonist with a positive allosteric modulation of endogenous ligand (AgoPAM). AP5 demonstrates rat and human inositol monophosphate (IP1) EC50 values of 0.49 nM and 0.8 nM against the GPR40 receptor, respectively. AP5 has the potential for type II diabetes research.
|
-
- HY-19644
-
|
GSK2256294A
GSK 2256294
|
Epoxide Hydrolase
|
Cardiovascular Disease
|
|
GSK2256294A (GSK 2256294) is a selective and orally active inhibitor of soluble epoxide hydrolase (sEH). GSK2256294A inhibits recombinant human sEH, rat sEH orthologs and murine sEH orthologs with IC50s of 27, 61 and 189 pM, respectively. GSK2256294A can be used for the research of chronic obstructive pulmonary disease (COPD) and cardiovascular disease.
|
-
- HY-111615A
-
|
J-2156 TFA
|
Somatostatin Receptor
|
Inflammation/Immunology
Neurological Disease
|
|
J-2156 TFA is a high potent, selective somatostatin receptor type 4 (SST4 receptor) agonist with IC50s of 0.05 nM and 0.07 nM for human and rat SST4 receptors, respectively. J-2156 TFA has anti-inflammatory activity and it is used for the relief of mechanical allodynia and mechanical hyperalgesia in the ipsilateral hindpaws in rats.
|
-
- HY-12439
-
|
ML380
|
mAChR
|
Neurological Disease
|
|
ML380 is a potent, subtype-selective, and brain-penetrant positive allosteric modulator (PAM) of M5 mAChR, with EC50s of 190 and 610 nM for human and rat M5, respectively. ML380 exhibits moderate selectivity versus the M1 and M3 mAChR subtypes. ML380 could increase the affinity of ACh for the M5 mAChR.
|
-
- HY-13402A
-
|
Varespladib sodium
LY315920 sodium
|
Phospholipase
|
Inflammation/Immunology
|
|
Varespladib sodium (LY315920 sodium) is a potent and selective group IIA, secretory phospholipase A2 (sPLA2) inhibitor with an IC50 of 9 nM. Varespladib sodium exhibits the significant inhibitory effect on sPLA2 activity in serum from various species including rat, rabbit, guinea pig and human with IC50s of 8.1 nM, 5.0 nM, 3.2 nM and 6.2 nM, respectively.
|
-
- HY-12811
-
|
PF-04856264
|
Sodium Channel
|
Neurological Disease
|
|
PF-04856264 is a potent and selective Nav1.7 inhibitor, with IC50s of 28, 131, 19, and 42 nM for human, mouse, cynomolgus monkey and dog Nav1.7, respectively. PF-04856264 has low potency against the rat Nav1.7 channel. PF-04856264 shows analgesic effect.
|
-
- 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-40136
-
|
cis-4-Hydroxy-L-proline
|
Endogenous Metabolite
|
Cancer
Metabolic Disease
|
|
cis-4-Hydroxy-L-proline, a proline analogue, is an inhibitor of collagen production. cis-4-Hydroxy-L-proline could inhibit fibroblast growth by preventing the deposition of triple-helical collagen on the cell layer. cis-4-Hydroxy-L-proline also depresses the growth of primary N-nitrosomethylurea-induced rat mammary tumors.
|
-
- HY-13402
-
|
Varespladib
LY315920
|
Phospholipase
|
Inflammation/Immunology
|
|
Varespladib (LY315920) is a potent and selective group IIA, secretory phospholipase A2 (sPLA2) inhibitor with an IC50 of 9 nM. Varespladib exhibits the significant inhibitory effect on sPLA2 activity in serum from various species including rat, rabbit, guinea pig and human with IC50s of 8.1 nM, 5.0 nM, 3.2 nM and 6.2 nM, respectively.
|
-
- HY-N0665
-
|
Specnuezhenide
(8E)-Nuezhenide
|
NF-κB
Wnt
|
Inflammation/Immunology
|
|
Specnuezhenide ((8E)-Nuezhenide) is isolated from the fruits of Ligustrum lucidum. Specnuezhenide ((8E)-Nuezhenide) can inhibit IL-1β-induced inflammation in chondrocytes via inhibition of NF-κB and wnt/β-catenin signaling. Specnuezhenide ((8E)-Nuezhenide) exerts anti-inflammatory effects in a rat model of osteoarthritis (OA).
|
-
- HY-14542A
-
-
- HY-122028
-
|
HSD-016
|
11β-HSD
|
Metabolic Disease
|
|
HSD-016 is a potent, selective and orally active 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor with IC50 values of 11, 1 and 8 nM against human, mouse and rat 11β-HSD1, respectively. HSD-016 can be used for type 2 diabetes research.
|
-
- HY-142735
-
|
KCa2 channel modulator 2
|
Potassium Channel
|
Neurological Disease
|
|
KCa2 channel modulator 2 (compound 2q) is a potent subtype-selective positive modulator of KCa2 channel. KCa2 channel modulator 2 exhibits similar potency on the rat KCa2.2a and human KCa2.3 channel subtypes, with EC50s of 0.64 μM and 0.60 μM, respectively
|
-
- HY-13290
-
|
KN-62
|
CaMK
P2X Receptor
|
Metabolic Disease
Cancer
|
|
KN-62 is a selective and reversible inhibitor of calmodulin-dependent protein kinase II (CaMK-II) with a Ki of 0.9 μM for rat brain CaMK-II. KN-62 directly binds to the calmodulin binding site of CaMK-II. KN-62 displays noncompetitive antagonism at P2X7 receptors in HEK293 cells, with an IC50 value of approximately 15 nM.
|
-
- HY-118700
-
|
2-Iminobiotin
Guanidinobiotin
|
NO Synthase
|
Neurological Disease
|
|
2-Iminobiotin (Guanidinobiotin) is a biotin (vitamin H or B7) analog. 2-Iminobiotin is a reversible nitric oxide synthases inhibitor with Kis of 21.8 and 37.5μM for murine iNOS and rat n-cNOS, respectively. 2-Iminobiotin superimposes on hypothermia protects human neuronal cells from hypoxia-induced cell damage.
|
-
- HY-14542C
-
-
- HY-N0482
-
-
- HY-146241
-
|
SN40
|
Others
|
Cancer
|
|
SN40 is a potent amino acid transport (AAT) inhibitor with Kis of 7.29 μM, 2.42 μM, 2.94 μM, 5.55 μM, 24.43 μM and 5.55 μM for rat ASCT2, human ASCT2, EAAT1, EAAT2, EAAC1 and EAAT5, respectively. SN40 can be used for researching anticancer.
|
-
- HY-136501
-
|
MRS2395
|
P2Y Receptor
|
Cardiovascular Disease
|
|
MRS2395, an dipivaloyl derivative, is a potent P2Y12 receptor antagonist. MRS2395 inhibits ADP-induced platelet activation with a Ki of 3.6 μM. MRS2395 inhibits cAMP induced by ADP in rat platelets in the presence of PGE1 with an IC50 of 7 µM. MRS2395 enhances platelet dense granule release in response to TRAP-6.
|
-
- HY-10656
-
|
SB-657510
|
Urotensin Receptor
|
Inflammation/Immunology
|
|
SB-657510 is a selective urotensin II (UII) receptor (UT) antagonist. The Ki values are 61, 17, 30, 65 and 56 nM for human, monkey, cat, rat and mouse receptors, respectively. SB-657510 exerts anti-inflammatory effects by inhibiting UII-induced upregulation of inflammatory mediators such as adhesion molecules, cytokines, and tissue factor in human vascular endothelial cells.
|
-
- HY-P1597
-
|
Malantide
|
PKA
PKC
|
Cancer
|
|
Malantide is a synthetic dodecapeptide derived from the site phosphorylated by cAMP-dependent protein kinase (PKA) on the β-subunit of phosphorylase kinase. Malantide is a highly specific substrate for PKA with a Km of 15 μM and shows protein inhibitor (PKI) inhibition >90% substrate phosphorylation in various rat tissue extracts. Malantide is also an efficient substrate for PKC with a Km of 16 μM.
|
-
- HY-17407
-
-
- HY-18166
-
|
NIBR0213
|
LPL Receptor
|
Inflammation/Immunology
|
|
NIBR-0213 is a potent and selective S1P1 antagonist with efficacy in experimental autoimmune encephalomyelitis. NIBR-0213 displays potent and comparable potency on human and rat S1P1 (IC50 of 2.0 nM and 2.3 nM, respectively) in GTPγ 35S assays.
|
-
- 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-100594
-
|
EUK-134
|
NF-κB
|
Cardiovascular Disease
|
|
EUK-134, a synthetic superoxide dismutase and catalase mimetic, protects rat kidneys from ischemia-reperfusion-induced damage. EUK-134 is a superoxide dismutase (SOD) mimetics (SODm) with catalase activity. EUK-134 is a mitoprotective antioxidant. EUK-134 reduces the expression of NF-κB, MDA level, and protein carbonylation in H9C2 cells.
|
-
- HY-103080
-
|
CMF019
|
Apelin Receptor (APJ)
|
Cardiovascular Disease
|
|
CMF019 is a potent and small molecule agonist at Apelin receptor (APJ) with G protein bias. CMF019 binds to APJ with pKi values of 8.58, 8.49 and 8.71 for human, rat, and mouse, respectively. CMF019 mimics the beneficial cardiovascular actions of apelin in rodents. Apelin receptor (APJ) is a G protein-coupled receptor (GPCR) activated by the endogenous peptide apelin.
|
-
- HY-146429
-
|
NaPi2b-IN-3
|
Others
|
Metabolic Disease
|
|
NaPi2b-IN-3 (compound 5) is a potent sodium-dependent transport protein 2b (SLC34A2, NaPi2b) inhibitor with IC50s of 71 nM and 28 nM for human NaPi2b and rat NaPi2b, respectively. NaPi2b-IN-3 can be used for researching hyperphosphatemia.
|
-
- HY-15008
-
|
L-368,899
|
Oxytocin Receptor
|
Endocrinology
|
|
L-368,899 is an orally active and selective OT (oxytocin ) receptor antagonist, with IC50s of 8.9 and 26 nM for uterus of rat and human, respectively. L-368,899 can cross the blood-brain barrier (BBB). L-368,899 inhibits oxytocin-stimulated uterine contractions in rats and can be used in study of preterm labor.
|
-
- HY-P3883
-
-
- HY-14542
-
-
- HY-P1022A
-
|
Kisspeptin-54(human) TFA
Metastin(human) TFA
|
GnRH Receptor
|
Cancer
Endocrinology
|
|
Kisspeptin-54(human) TFA (Metastin(human) TFA) is an endogenous ligand for kisspeptin receptor (KISS1, GPR54). Kisspeptin-54(human) TFA binds to rat and human GPR54 receptors with Ki values of 1.81 nM and 1.45 nM, respectively. Kisspeptin-54(human) TFA hinders tumor metastasis and stimulates gonadotropin secretion.
|
-
- HY-14899
-
|
Taprenepag
CP-544326
|
Prostaglandin Receptor
|
Endocrinology
|
|
Taprenepag (CP-544326) is a potent and selective prostaglandin EP(2) agonist with IC50s of 10 and 15 nM for human and rat EP2, respectively. Taprenepag shows selectivity for EP2 over other EP receptors (IC50s>3200 nM for EP1, EP3, and EP4) and a panel of 37 G protein-coupled receptors.
|
-
- HY-144456
-
|
Xanthine oxidase-IN-5
|
Xanthine Oxidase
|
Metabolic Disease
|
|
Xanthine oxidase-IN-5 is an effective and orally active xanthine oxidase (XO) inhibitor with IC50 value of 0.70 μM. Xanthine oxidase-IN-5 displays favorable agent-like properties with ligand efficiency (LE) and lipophilic ligand efficiency (LLE) values of 0.33 and 3.41, respectively. Xanthine oxidase-IN-5 shows potent hypouricemic effects in hyperuricemic rat model.
|
-
- HY-N1735
-
|
2′-Hydroxygenistein
|
Others
|
Inflammation/Immunology
|
|
2′-Hydroxygenistein is a natural product that can be isolated from Crotalaria pallida and C. assamica. 2′-Hydroxygenistein shows anti-inflammatory activity. 2′-Hydroxygenistein shows significant concentration-dependent inhibitory effects on the release of β-glucuronidase and lysozyme from rat neutrophils, with IC50 values of 5.9 ± 1.4 and 9.7 ± 3.5 μM, respectively.
|
-
- HY-W008344
-
|
2-Chloroadenosine
|
Nucleoside Antimetabolite/Analog
|
Others
|
|
2-Chloroadenosine, a stable adenosine analogue, protects against long term development of ischaemic cell loss in the rat hippocampus. 2-Chloroadenosine is an apparent competitive inhibitor of uridine influx (apparent Ki=33 μM) and high-affinity nitrobenzylthioinosine binding (apparent Ki=0.18 mM). 2-Chloroadenosine is a transported permeant for the nucleoside transporter in human erythrocytes.
|
-
- HY-14542B
-
-
- HY-10061
-
|
Lesogaberan
AZD-3355
|
GABA Receptor
|
Metabolic Disease
|
|
Lesogaberan (AZD-3355) is a potent and selective GABAB receptor agonist with an EC50 of 8.6 nM for human recombinant GABAB receptors. The affinity (Kis) of Lesogaberan for rat GABAB and GABAA receptors, as measured by displacement of [ 3H]GABA binding in brain membranes: 5.1 nM and 1.4 μM, respectively. Lesogaberan inhibits transient lower esophageal sphincter relaxation through a peripheral mode of action.
|
-
- HY-10435
-
|
SKF-82958
(±)-SKF-82958; Chloro-APB
|
Dopamine Receptor
|
Neurological Disease
|
|
SKF-82958 ((±)-SKF 82958) is a dopamine D1 receptor full agonist (K0.5=4 nM), displays selective for D1 over D2 receptors (K0.5=73 nM). SKF-82958 induces dopamine D1 receptor-dependent adenylate cyclase activity in rat striatal membranes (EC50=491 nM).
|
-
- HY-P1597A
-
|
Malantide TFA
|
PKA
PKC
|
Cancer
|
|
Malantide TFA is a synthetic dodecapeptide derived from the site phosphorylated by cAMP-dependent protein kinase (PKA) on the β-subunit of phosphorylase kinase. Malantide TFA is a highly specific substrate for PKA with a Km of 15 μM and shows protein inhibitor (PKI) inhibition >90% substrate phosphorylation in various rat tissue extracts. Malantide TFA is also an efficient substrate for PKC with a Km of 16 μM.
|
-
- HY-101368A
-
|
WIN 64338 hydrochloride
|
Bradykinin Receptor
mAChR
|
Neurological Disease
|
|
WIN 64338 hydrochloride is a potent, selective, nonpeptide competitive antagonist of bradykinin B2 receptor. WIN 64338 hydrochloride inhibits [ 3H]-Bradykinin binding to the bradykinin B2 receptor on human IMR-90 cells with a Ki of 64 nM. WIN 64338 hydrochloride also can inhibits [ 3H]Quinuclidinyl benzilate binding to the rat brain muscarinic receptor (Ki=350 nM).
|
-
- HY-133036
-
|
APJ receptor agonist 1
|
Apelin Receptor (APJ)
|
Cardiovascular Disease
|
|
APJ receptor agonist 1, a biphenyl acid derivative, is a potent APJ receptor (APJ-R) agonist (EC50s 0.093 and 0.12 nM for human and rat APJ-R, respectively). APJ receptor agonist 1 displays in vitro potency to apelin-13, the endogenous peptidic ligand for the APJ receptor. APJ receptor agonist 1 has the potential for the research of heart failure.
|
-
- HY-102064
-
|
SR 57227A
|
5-HT Receptor
|
Neurological Disease
|
|
SR 57227A is a potent, orally active and selective 5-HT3 receptor agonist, with ability to cross the blood brain barrier. SR 57227A has affinities (IC50) varying between 2.8 and 250 nM for 5-HT3 receptor binding sites in rat cortical membranes and on whole NG 108-15 cells or their membranes. Anti-depressant effects.
|
-
- HY-108044
-
|
ONO-5334
|
Cathepsin
SARS-CoV
|
Metabolic Disease
|
|
ONO-5334 is a potent, selective and orally active cathepsin K inhibitor with Ki values of 0.10 nM, 0.049 nM and 0.85 nM for human, rabbit and rat cathepsin K, respectively. ONO 5334 is an effective antiviral compound against SAR-COV-2 virus activity with an EC50 value of 500 nM. ONO-5334 has the potential for the study of osteoporosis and COVID-19 disease.
|
-
- HY-103428
-
|
LE 300
|
Dopamine Receptor
5-HT Receptor
|
Neurological Disease
|
|
LE 300 is a potent and selective dopamine D1-like receptor antagonist with Kis of 1.9 nM and 7.5 nM in CHO cell membranes expressing human dopamine D1 and D5 receptors, respectively. LE 300 is an antagonist of the 5-HT2A receptor with a pA2 of 8.32 in a rat tail artery assay.
|
-
- HY-10061B
-
|
Lesogaberan hydrochloride
AZD-3355 hydrochloride
|
GABA Receptor
|
Metabolic Disease
|
|
Lesogaberan (AZD-3355) hydrochloride is a potent and selective GABAB receptor agonist with an EC50 of 8.6 nM for human recombinant GABAB receptor. The affinity (Kis) of Lesogaberan hydrochloride for rat GABAB and GABAA receptors, as measured by displacement of [ 3H]GABA binding in brain membranes: 5.1 nM and 1.4 μM, respectively. Lesogaberan hydrochloride inhibits transient lower esophageal sphincter relaxation through a peripheral mode of action.
|
-
- HY-12914
-
|
V116517
|
TRP Channel
|
Inflammation/Immunology
Neurological Disease
|
|
V116517 is a potent, orally active transient receptor potential vanilloid (TRPV1) antagonist. V116517 shows potent activity in inhibiting both capsaicin (CAP)- and acid (pH 5)-induced currents in rat DRG neurons expressing native TRPV (IC50=423.2 nM for CAP; IC50=180.3 nM for acid). V116517 can be used for the research of pain.
|
-
- HY-B0358
-
-
- HY-16079
-
|
AZD3514
|
Androgen Receptor
|
Cancer
|
|
AZD3514 is an orally activie and selective androgen receptor (AR) inhibitor. AZD3514 androgen-dependently and -independently inhibits AR signal. AZD351 down-regulates nuclear AR levels in human LNCaP prostate cancer cells in the absence of androgen with an pIC50 value of 5.75. AZD3514 can be used for the research of prostate cancer.
|
-
- HY-120596
-
-
- HY-145814
-
|
HSP90-IN-9
|
HSP
Fungal
|
Infection
|
|
HSP90-IN-9 is a potent and selective HSP90 inhibitor. HSP90-IN-9 displays a fungicidal effect in a dose-dependent manner. HSP90-IN-9 inhibits fungal biofilm formation and fungal morphological changes after being combined with FLC. HSP90-IN-9 recovers FLC resistance by down-regulating the expression of related genes (ERG11, CDR1 and CDR2).
|
-
- HY-B0358A
-
-
- HY-151392
-
-
- HY-10037
-
|
Quiflapon
MK-591
|
FLAP
Apoptosis
|
Inflammation/Immunology
|
|
Quiflapon (MK-591) is a selective and specific 5-lipoxygenase-activating protein (FLAP) inhibitor with an IC50 of 1.6 nM in a FLAP binding assay. Quiflapon is also a potent and orally active Leukotriene biosynthesis (LT) inhibitor, shows IC50 values of 3.1 and 6.1 nM in intact human and elicited rat PMNLs, respectively. Quiflapon induces cell apoptosis.
|
-
- HY-106827
-
|
Trimegestone
RU 27987
|
Progesterone Receptor
Androgen Receptor
Phosphatase
|
Endocrinology
|
|
Trimegestone (RU 27987) is an orally active 19-norpregnane progestin. Trimegestone binds to progesterone receptor (PR) with an IC50 value of 3.3 nM (rat PR). Trimegestone increases alkaline phosphatase activity (EC50=0.1 nM) but not luciferase activity. Trimegestone also shows a weak antiandrogenic activity (weak androgen receptor affinity). Trimegestone can be used in studies of contraception or menopausal syndromes.
|
-
- HY-101016
-
|
17-ODYA
|
Cytochrome P450
Apoptosis
|
Cardiovascular Disease
|
|
17-ODYA is a CYP450 ω-hydroxylase inhibitor. 17-ODYA is also a potent inhibitor (IC50<100 nM) of the formation of 20-hydroxyeicosatetraenoic acid (20-HETE), epoxyeicosatrienoic acids and dihydroxyeicosatrienoic acids by rat renal cortical microsomes incubated with arachidonic acid. 17-ODYA completely attenuates the isoproterenol (ISO)-induced apoptosis, and necrosis in cultured cardiomyocytes.
|
-
- HY-13863
-
|
Hydroxy-Dynasore
Dyngo-4a
|
Dynamin
|
Neurological Disease
|
|
Hydroxy Dynasore (Dyngo-4a), a structural analog of Dynasore (HY-15304), is an potency improved, low cytotoxicity and non‐specific binding dynamin inhibitor with IC50 values of 0.38 μM and 2.3 μM for brain dynamin I and recombinant rat dynamin II, respectively. Hydroxy Dynasore inhibits dynamin‐dependent endocytosis of transferrin with an IC50 of 5.7 μM in vitro.
|
-
- HY-153095
-
|
PF-6870961
|
GHSR
|
Metabolic Disease
|
|
PF-6870961 is an inverse agonist of GHSR1a with Ki values of 73.6 nM (human GHSR), 239 nM (rat GHSR), and 217 nM (dog GHSR), respectively. PF-6870961 inhibits the constitutive GHSR1a-induced IP accumulation with an IC50 value of 300 nM. PF-6870961 also inhibits constitutive GHSR1a β-arrestin mobilization with an IC50 value of 1.10 nM.
|
-
- HY-107422A
-
|
Lenumlostat hydrochloride
PAT-1251 hydrochloride; GB2064 hydrochloride
|
Monoamine Oxidase
|
Inflammation/Immunology
|
|
PAT-1251 Hydrochloride is a potent, selective and oral lysyl oxidase-like 2 (LOXL2) inhibitor, with IC50s of 0.71 and 1.17 μM for hLOXL2 and hLOXL3, respectively, and also potently inhibits mouse, rat, and dog LOXL2 (IC50s, 0.10, 0.12, and 0.16 μM, respectively). PAT-1251 Hydrochloride is used in the research of fibrotic diseases.
|
-
- HY-122255
-
|
LY487379
|
mGluR
|
Neurological Disease
|
|
LY487379 is a selective human mGluR2 positive allosteric modulator (PAM). LY487379 potentiates glutamate-stimulated [ 35S]GTPγS binding with EC50 values of 1.7 μM and >10 μM for mGlu2 and mGlu3 receptors respectively. LY487379 promotes cognitive flexibility and facilitates behavioral inhibition in a rat model. LY487379 can be used for schizophrenia research.
|
-
- HY-P1318
-
|
Ac-RYYRIK-NH2
|
Opioid Receptor
|
Neurological Disease
|
|
Ac-RYYRIK-NH2 is a potent and partial agonist on ORL1 transfected in CHO cells (Kd=1.5 nM) and behaves as a endogenous ligand of ORL1. Ac-RYYRIK-NH2 is a specific antagonist for the activation of G protein and competitively antagonizes the stimulation of [ 35S]-GTPgS binding to G proteins by nociceptin/orphanin FQ (noc/OFQ) in membranes and sections of rat brain.
|
-
- HY-P1163
-
|
D[LEU4,LYS8]-VP
|
Vasopressin Receptor
|
Neurological Disease
Cardiovascular Disease
|
|
D[LEU4,LYS8]-VP is a selective agonist of vasopressin V1b receptor, with the Kis of 0.16 nM, 0.52 nM, and 0.1.38 nM for rat, human and mouse V1b receptor, respectively. D[LEU4,LYS8]-VP has weak antidiuretic, vasopressor, and in vitro oxytocic activities.
|
-
- HY-111313
-
|
JNJ-26070109
|
Cholecystokinin Receptor
|
Metabolic Disease
|
|
JNJ-26070109 is a high-affinity, competitive, orally bioactive, and selective cholecystokinin 2 (CCK2) receptor antagonist with good pharmacokinetic properties, with pKis of 8.49, 7.99, and 7.70 for human, rat, and dog CCK2 receptors, respectively. The dual function of CCK2 receptors in regulating gastric acid secretion and growth of the gastrointestinal mucosa make this an attractive and novel target for the research of gastroesophageal reflux disease.
|
-
- HY-14174
-
|
MRK-560
|
γ-secretase
|
Cancer
Neurological Disease
|
|
MRK-560 is an orally active, brain barrier-penetrating γ-Secretase inhibitor, can potently reduces Aβ peptide in rat brain and cerebrospinal fluid. MRK-560 also decreases mutant NOTCH1 processing by selectively inhibiting PSEN1. MRK-560 can be used in studies of Alzheimer's disease and T-cell acute lymphoblastic leukaemia (T-ALL).
|
-
- HY-109509
-
|
Enoxaparin
PK 10169; Enoxaparin sodium; Lovenox
|
Factor Xa
Thrombin
SARS-CoV
|
Infection
Inflammation/Immunology
Neurological Disease
Cardiovascular Disease
|
|
Enoxaparin (PK 10169), a low-molecular-weight heparin (LMWH) derivative. Enoxaparin exerts anticoagulant activity through antithrombin III, an endogenous inhibitor of factor Xa and thrombin IIa. Enoxaparin protect the rat hippocampus against TBI (traumatic brain injury) via antioxidant and anti-inflammatory properties. Enoxaparin can be used for the research of deep vein thrombosis (DVT), pulmonary embolism, TBI and COVID-19.
|
-
- HY-153095A
-
|
PF-6870961 hydrochloride
|
GHSR
|
Metabolic Disease
|
|
PF-6870961 hydrochloride is an inverse agonist of GHSR1a with Ki values of 73.6 nM (human GHSR), 239 nM (rat GHSR), and 217 nM (dog GHSR), respectively. PF-6870961 hydrochloride inhibits the constitutive GHSR1a-induced IP accumulation with an IC50 value of 300 nM. PF-6870961 hydrochloride also inhibits constitutive GHSR1a β-arrestin mobilization with an IC50 value of 1.10 nM.
|
-
- HY-118700A
-
|
2-Iminobiotin hydrobromide
Guanidinobiotin hydrobromide
|
NO Synthase
|
Neurological Disease
|
|
2-Iminobiotin hydrobromide (Guanidinobiotin hydrobromide) is a biotin (vitamin H or B7) analog. 2-Iminobiotin hydrobromide is a reversible nitric oxide synthases inhibitor with Kis of 21.8 and 37.5 μM for murine iNOS and rat n-cNOS, respectively. 2-Iminobiotin hydrobromide superimposes on hypothermia protects human neuronal cells from hypoxia-induced cell damage.
|
-
- HY-10435A
-
|
SKF-82958 hydrobromide
(±)-SKF-82958 hydrobromide; Chloro-APB hydrobromide
|
Dopamine Receptor
|
Neurological Disease
|
|
SKF-82958 ((±)-SKF 82958) hydrobromide is a dopamine D1 receptor full agonist (K0.5=4 nM), displays selective for D1 over D2 receptors (K0.5=73 nM). SKF-82958 hydrobromide induces dopamine D1 receptor-dependent adenylate cyclase activity in rat striatal membranes (EC50=491 nM).
|
-
- HY-106934
-
|
Peldesine
BCX 34
|
Nucleoside Antimetabolite/Analog
HIV
|
Cancer
Infection
Inflammation/Immunology
|
|
Peldesine (BCX 34) is a potent, competitive, reversible and orally active purine nucleoside phosphorylase (PNP) inhibitor with IC50s of 36 nM, 5 nM, and 32 nM for human, rat, and mouse red blood cell (RBC) PNP, respectively. Peldesine is also a T-cell proliferation inhibitor with an IC50 of 800 nM. Peldesine has the potential for cutaneous T-cell lymphoma, psoriasis and HIV infection research.
|
-
- HY-106934A
-
|
Peldesine dihydrochloride
BCX 34 dihydrochloride
|
Nucleoside Antimetabolite/Analog
HIV
|
Cancer
Infection
Inflammation/Immunology
|
|
Peldesine (BCX 34) dihydrochloride is a potent, competitive, reversible and orally active purine nucleoside phosphorylase (PNP) inhibitor with IC50s of 36 nM, 5 nM, and 32 nM for human, rat, and mouse red blood cell (RBC) PNP, respectively. Peldesine dihydrochloride is also a T-cell proliferation inhibitor with an IC50 of 800 nM. Peldesine dihydrochloride has the potential for cutaneous T-cell lymphoma, psoriasis and HIV infection research.
|
-
- HY-103110
-
|
ST1936
|
5-HT Receptor
Adrenergic Receptor
|
Neurological Disease
|
|
ST1936 is a selective, nanomolar affinity 5-HT6 receptor agonist with Ki values of 13 nM, 168 nM and 245 nM for human 5-HT6, 5-HT7 and 5-HT2B receptors, respectively. ST1936 also shows moderate affinity (Ki of 300 nM) for human and rat α2 adrenergic receptor.
|
-
- HY-150508
-
|
MK-0159
|
CD38
|
Metabolic Disease
Cardiovascular Disease
|
|
MK-0159 (compound 37) is an orally active, potent and selective CD38 inhibitor, with IC50 values of 22, 3, and 70 nM for human, mouse and rat CD38, respectively. MK-0159 also shows good microsomal stability for human and rodent liver microsomes. MK-0159 increases NAD + (nicotinamide adenine dinucleotide) and reduces ADPR (adenosine diphosphate ribose) in whole blood and heart.
|
-
- HY-14165A
-
|
(S)-Veliflapon
(S)-BAY X 1005; (S)-DG-031
|
Leukotriene Receptor
FLAP
|
Inflammation/Immunology
|
|
(S)-Veliflapon ((S)-BAY X 1005) is an orally active inhibitor of leukotriene biosynthesis and 5-lipoxygenase activating protein (FLAP). (S)-Veliflapon inhibits the formation of leukotriene B4 (LTB4) in rat, mouse and human leukocytes with IC50 values of 0.026 µM, 0.039 µM and 0.22 µM respectively. (S)-Veliflapon showes enantioselectivity in human whole blood.
|
-
- HY-103135
-
-
- HY-151140
-
|
CYP11B1-IN-2
|
Cytochrome P450
|
Others
|
|
CYP11B1-IN-2 (compound 7aa) is an orally active, potent and selective CYP11B1 inhibitor, with IC50 values of 9 nM and 25 nM for human CYP11B1 and rat CYP11B1, respectively. CYP11B1-IN-2 can be used for the research of diseases caused by excessive cortisol.
|
-
- HY-111767
-
|
BAY-545
|
Adenosine Receptor
|
Inflammation/Immunology
|
|
BAY-545 is a potent and selective A2B adenosine receptor antagonist, with an IC50 of 59 nM. BAY-545 also exhibits IC50s of 66, 400, 280 nM for human, mouse, rat A2B adenosine receptor in cells, respectively, and a Ki of 97 nM for human A2B adenosine receptor, with more selectivity over A1, A2A, and A3 adenosine receptor.
|
-
- HY-108467
-
|
GGsTop
Nahlsgen
|
Others
|
Cardiovascular Disease
|
|
GGsTop (Nahlsgen) is a potent, non-toxic, highly selective and irreversible γ−glutamyl transpeptidase (GGT) inhibitor, with a Ki of 170 μM for Human GGT. GGsTop shows a pKa of 9.71, also exhibits Kons of 150±10 and 51±3 M -1 s -1 against E.coli GGT and human GGT, respectively. GGsTop protects hepatic ischemia-reperfusion injury in rat model.
|
-
- 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-14336A
-
|
SB 271046 Hydrochloride
SB 271046A
|
5-HT Receptor
|
Neurological Disease
|
|
SB 271046 Hydrochloride (SB 271046A) is a potent, selective and orally active 5-HT6 receptor antagonist with pKi of 9.02, 8.55, and 8.81 for rat, pig and human, respectively. SB 271046 Hydrochloride is over 200 fold selective for the 5-HT6 receptor vs 55 other receptors, binding sites and ion channels. Anticonvulsant activity (EC50=0.16 μM).
|
-
- 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 CRF2α receptors in CHO cells, and Kis of 0.4, 1.8, and 5.7 nM for hCRF1, rCRF2α and mCRF2β receptors, respectively.
|
-
- HY-10456
-
|
TAK-715
|
p38 MAPK
Casein Kinase
|
Inflammation/Immunology
|
|
TAK-715 is an orally active and potent p38 MAPK inhibitor with IC50s of 7.1 nM, 200 nM for p38α and p38β, respectively. TAK-715 inhibits casein kinase I (CK1δ/ε) to regulate activation of Wnt/β-catenin signaling. TAK-715 shows good significant efficacy in a rat arthritis model.
|
-
- HY-P1163A
-
|
D[LEU4,LYS8]-VP TFA
|
Vasopressin Receptor
|
Neurological Disease
Cardiovascular Disease
|
|
D[LEU4,LYS8]-VP TFA is a selective agonist of vasopressin V1b receptor, with the Kis of 0.16 nM, 0.52 nM, and 0.1.38 nM for rat, human and mouse V1b receptor, respectively. D[LEU4,LYS8]-VP TFA has weak antidiuretic, vasopressor, and in vitro oxytocic activities.
|
-
- HY-19835
-
|
LY2922470
|
Free Fatty Acid Receptor
|
Metabolic Disease
|
|
LY2922470 is a potent, selective and orally available agonist of the G protein-coupled receptor 40 (GPR40), with EC50s of 7 nM, 1 nM and 3 nM for human GPR40, mouse GPR40 and rat GPR40, respectively. LY2922470 reduces glucose levels along with significant increases in insulin and GLP-1, is potential for the treatment of type 2 diabetes mellitus (T2DM).
|
-
- HY-103110A
-
|
ST1936 oxalate
|
5-HT Receptor
Adrenergic Receptor
|
Neurological Disease
|
|
ST1936 oxalate is a selective, nanomolar affinity 5-HT6 receptor agonist with Ki values of 13 nM, 168 nM and 245 nM for human 5-HT6, 5-HT7 and 5-HT2B receptors, respectively. ST1936 oxalate also shows moderate affinity (Ki of 300 nM) for human and rat α2 adrenergic receptor.
|
-
- HY-146012
-
|
HIV-1 protease-IN-4
|
HIV
|
Infection
|
|
HIV-1 protease-IN-4 (Compound II-22) is a potent HIV-1 protease inhibitor. HIV-1 protease-IN-4 is a proagent of atazanavir. HIV-1 protease-IN-4 as a proagent that delivers the parent 1 to rat plasma with a 5-fold higher AUC and 67-fold higher C24 when compared to oral administration of the parent agent.
|
-
- HY-107422
-
|
Lenumlostat
PAT-1251; GB2064
|
Monoamine Oxidase
|
Inflammation/Immunology
|
|
PAT-1251 is a potent, selective and oral lysyl oxidase-like 2 (LOXL2) inhibitor, with IC50s of 0.71 and 1.17 μM for hLOXL2 and hLOXL3, respectively, and also potently inhibits mouse, rat, and dog LOXL2 (IC50s, 0.10, 0.12, and 0.16 μM, respectively); PAT-1251 is used in the research of fibrotic diseases.
|
-
- HY-59201A
-
|
A-582941 dihydrochloride
|
nAChR
5-HT Receptor
|
Neurological Disease
|
|
A-582941 dihydrochloride is a potent, selective and brain-penetrant partial agonist of α7 nAChR, with Kis of 10.8 and 16.7 nM in rat brain membranes and human frontal cortex, respectively. A-582941 dihydrochloride also binds to human 5-HT3 receptor with a Ki of 150 nM. A-582941 has the potential for cognitive deficits associated with various neurodegenerative and psychiatric disorders research.
|
-
- HY-148259
-
|
SF-1 antagonist-1
|
Others
|
Cancer
|
|
SF-1 antagonist-1 (compound 11) is a antagonist of steroidogenic factor 1 (SF-1). SF-1 antagonist-1 affects SF-1 transcriptional activity with an EC50 value of ＜200 nM. SF-1 antagonist-1 inhibits the proliferation of Rat Leydig tumor cells. SF-1 antagonist-1 can be used for the research of cancer.
|
-
- HY-10061A
-
|
Lesogaberan napadisylate
AZD-3355 napadisylate
|
GABA Receptor
|
Metabolic Disease
|
|
Lesogaberan (AZD-3355) napadisylate is a potent and selective GABAB receptor agonist with an EC50 of 8.6 nM for human recombinant GABAB receptors. The affinity (Kis) of Lesogaberan napadisylate for rat GABAB and GABAA receptors, as measured by displacement of [ 3H]GABA binding in brain membranes: 5.1 nM and 1.4 μM, respectively. Lesogaberan napadisylate inhibits transient lower esophageal sphincter relaxation through a peripheral mode of action.
|
-
- HY-142295
-
|
GNF2133
|
DYRK
|
Metabolic Disease
|
|
GNF2133 is a potent, selective and orally active DYRK1A inhibitor with IC50s of 0.0062, >50 µM for DYRK1A and GSK3β, respectively. GNF2133 shows good proliferation potency and efficacy on rat and human primary β-cell. GNF2133 significantly improves glucose disposal capacity and increases insulin secretion. GNF2133 has the potential for the research of type 1 diabetes.
|
-
- HY-105184
-
|
YM511
|
Cytochrome P450
|
Endocrinology
|
|
YM511 is a highly specific non-steroidal aromatase inhibitor. YM511 inhibits aromatase activities in microsomes from rat ovary and human placenta competitively (IC50s of 0.4 and 0.12 nM, respectively). YM511 slightly inhibits production of other steroid hormones. YM511 has the potential for suppressing estrogen-dependent action research without affecting serum levels of other steroid hormones.
|
-
- 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-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 CRF2α receptors in CHO cells, and Kis of 0.4, 1.8, and 5.7 nM for hCRF1, rCRF2α and mCRF2β receptors, respectively.
|
-
- HY-P1318A
-
|
Ac-RYYRIK-NH2 TFA
|
Opioid Receptor
|
Neurological Disease
|
|
Ac-RYYRIK-NH2 TFA is a potent and partial agonist on ORL1 transfected in CHO cells (Kd=1.5 nM) and behaves as a endogenous ligand of ORL1. Ac-RYYRIK-NH2 is a specific antagonist for the activation of G protein and competitively antagonizes the stimulation of [ 35S]-GTPgS binding to G proteins by nociceptin/orphanin FQ (noc/OFQ) in membranes and sections of rat brain.
|
-
- HY-129624A
-
|
Bisindolylmaleimide VIII acetate
Ro 31-7549 acetate; Bis VIII acetate
|
PKC
Apoptosis
|
Cancer
Inflammation/Immunology
|
|
Bisindolylmaleimide VIII acetate (Ro 31-7549 acetate) is a potent and selective protein kinase C (PKC) inhibitor with an IC50 of 158 nM for rat brain PKC. Bisindolylmaleimide VIII acetate has IC50s of 53, 195, 163, 213, and 175 nM for PKC-α, PKC-βI, PKC-βII, PKC-γ, PKC-ε, respectively. Bisindolylmaleimide VIII acetate facilitates Fas-mediated apoptosis and inhibits T cell-mediated autoimmune diseases.
|
-
- HY-146242
-
|
SN05
|
Others
|
Cancer
|
|
SN05 is a potent amino acid transport (AAT) inhibitor with Kis of 2.77 μM, 0.73 μM, 0.87 μM, 3.7 μM, 7.25 μM, 7.23 μM and 2.22 μM for human ASCT1, rat ASCT2, human ASCT2, EAAT1, EAAT2, EAAC1 and EAAT5, respectively. SN05 can be used for researching anticancer.
|
-
- HY-14483
-
|
AF-353
Ro-4
|
P2X Receptor
|
Cancer
|
|
AF-353 (Ro-4) is a potent, selective and orally bioavailable P2X3/P2X2/3 receptor antagonist, with a pIC50 of 8.0 for both human and rat P2X3, and with a pIC50 of 7.3 for human P2X2/3.
|
-
- HY-142295A
-
|
GNF2133 hydrochloride
|
DYRK
|
Metabolic Disease
|
|
GNF2133 hydrochloride is a potent, selective and orally active DYRK1A inhibitor with IC50s of 0.0062, >50 µM for DYRK1A and GSK3β, respectively. GNF2133 hydrochloride shows good proliferation potency and efficacy on rat and human primary β-cell. GNF2133 hydrochloride significantly improves glucose disposal capacity and increases insulin secretion. GNF2133 hydrochloride has the potential for the research of type 1 diabetes.
|
-
- 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-146410
-
|
AT2R antagonist 1
|
Angiotensin Receptor
|
Others
|
|
AT2R antagonist 1 (compound 21) is a potent and high selective AT2R (angiotensin II AT2 receptor) ligand. AT2R antagonist 1 exhibits a fair AT2R affinity, with a Ki of 29 nM. AT2R antagonist 1 also inhibits common agent-metabolizing CYP enzymes. AT2R antagonist 1 shows high stability in human, rat and mouse liver microsomes.
|
-
- HY-120516
-
|
CDE-096
|
PAI-1
|
Cardiovascular Disease
|
|
CDE-096 is a potent inhibitor of PAI-1. CDE-096 prevents PAI-1 from inactivating tPA and uPA with similar potency (IC50=30 and 25 nM, respectively) and is active against glycosylated PAI-1, as well as PAI-1 derived from several species (IC50=19, 22 and 18 nM for murine, rat, and Porcine PAI-1, respectively).
|
-
- HY-110129
-
|
Eplivanserin hemifumarate
SR-46349 hemifumarate; SR 46349B
|
5-HT Receptor
|
Neurological Disease
|
|
Eplivanserin (SR-46349) hemifumarate is a potent, selective and orally active 5-HT2A receptor antagonist, with an IC50 of 5.8 nM in rat cortical membrane, and a Kd of 1.14 nM. Eplivanserin hemifumarate displays >20-fold selectivity more selective for 5-HT2A than 5-HT2B and 5-HT2C.
|
-
- HY-107678
-
|
SEN12333
WAY-317538
|
nAChR
|
Neurological Disease
|
|
SEN 12333 (WAY-317538) is a potent, selective and orally active α7 nAChR agonist. SEN12333 displays high affinity for the rat α7 nAChRs expressed in GH4C1 cells (K>i=260 nM) and acts as full agonist in functional Ca 2+ flux studies (EC50=1.6 μM). SEN 12333 is used for AD and schizophrenia research.
|
-
- HY-103552
-
|
LY487379 hydrochloride
|
mGluR
|
Neurological Disease
|
|
LY487379 hydrochloride is a selective human mGluR2 positive allosteric modulator (PAM). LY487379 hydrochloride potentiates glutamate-stimulated [ 35S]GTPγS binding with EC50 values of 1.7 μM and >10 μM for mGlu2 and mGlu3 receptors respectively. LY487379 hydrochloride promotes cognitive flexibility and facilitates behavioral inhibition in a rat model. LY487379 hydrochloride can be used for schizophrenia research.
|
-
- HY-117133
-
|
SF0166
|
Integrin
|
Metabolic Disease
|
|
SF0166 is a potent and selective αvβ3 antagonist with IC50 values of 0.6 nM, 8 nM, and 13 nM for αvβ3, αvβ6, and αvβ8, respectively. SF0166 inhibits cellular adhesion to vitronectin across human, rat, rabbit, and dog cell lines with IC50 values of 7.6 pM to 76 nM. SF0166 decreases neovascularization in the oxygen-induced retinopathy mouse model.
|
-
- HY-101986A
-
|
BIIE-0246 hydrochloride
AR-H 053591 hydrochloride
|
Neuropeptide Y Receptor
|
Metabolic Disease
|
|
BIIE-0246 hydrochloride (AR-H 053591 hydrochloride) is a potent and selective NPY2R (neuropeptide Y receptor 2) antagonist with an IC50 value of 15 nM for rat [ 125I]PYY3-36. BIIE-0246 hydrochloride decreases the expression of p-AKT S473, P-p44/42 MAPK under the NPY-stimulated. BIIE-0246 hydrochloride reduces albuminuria in ADR nephropathy.
|
-
- HY-137307
-
|
Cholest-5-ene-3ß,22(S)-diol
(22S)-Hydroxycholesterol
|
Others
|
Inflammation/Immunology
|
|
Cholest-5-ene-3ß,22(S)-diol ((22S)-Hydroxycholesterol) is an orally active oxysterol with no significant cytotoxic, oxidative, or inflammatory effects on human prokaryotic leukemia cells. Cholest-5-ene-3ß,22(S)-diol inhibits weight gain and increased serum triacylglycerol (TAG) levels in rat models.
|
-
- HY-100403
-
|
Ro 67-7476
|
mGluR
|
Cancer
|
|
Ro 67-7476 is a potent positive allosteric modulator of mGluR1 and potentiates glutamate-induced calcium release in HEK293 cells expressing rat mGluR1a with an EC50 of 60.1 nM. Ro 67-7476 is a potent P-ERK1/2 agonist and activates ERK1/2 phosphorylation in the absence of exogenously added glutamate (EC50=163.3 nM).
|
-
- HY-10792
-
|
Eplivanserin
SR-46349
|
5-HT Receptor
|
Neurological Disease
|
|
Eplivanserin (SR-46349) is a potent, selective and orally active 5-HT2A receptor antagonist, with an IC50 of 5.8 nM in rat cortical membrane, and a Kd of 1.14 nM. Eplivanserin displays >20-fold selectivity more selective for 5-HT2A than 5-HT2B and 5-HT2C.
|
-
- 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-12119A
-
|
GW274150 phosphate
|
NO Synthase
|
Inflammation/Immunology
Neurological Disease
|
|
GW274150 phosphate is a potent, selective, orally active and NADPH-dependent inhibitor of human inducible nitric oxide synthase (iNOS) (IC50=2.19 μM; Kd=40 nM) and rat iNOS (ED50=1.15 μM). GW274150 phosphate displays less potency for both humans or rats endothelial NOS (eNOS) and neuronal NOS (nNOS). GW274150 phosphate exerts a protective role in an acute model of lung injury inflammation.
|
-
- HY-11052A
-
|
Trap-101 hydrochloride
|
Opioid Receptor
|
Neurological Disease
|
|
Trap-101 hydrochloride is a potent, selective and competitive antagonist of NOP receptors over classical opioid receptors. Trap-101 stimulates GTPγ 35S binding to CHOhNOP membranes with pKi values of 8.65, 6.60, 6.14 and <5 for NOP, μ-, κ-, and δ-opioid receptors, respectively. Trap-101 attenuates motor deficits in a rat model of parkinson's disease and can be used for the research of nervous system diseases.
|
-
- 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-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-P3354
-
|
p3Ysh-3
|
iGluR
|
Neurological Disease
|
|
p3Ysh-3 is a peptide inhibitor of STEP Phosphatase-GluA2 AMPA receptor interaction with a Ki of 1.09 μM. p3Ysh-3 restores the memory deficits and displays anxiolytic and antidepressant effects in a scopolamine-treated rat model. p3Ysh-3 is a promising lead compound for novel cognitive enhancers and/or behavioral modulators.
|
-
- HY-110207
-
|
SM-324405
|
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
|
SM-324405 is a TLR7 agonistic antedrug (EC50 = 50 nM), with pEC50 values of 7.3 and 6.6 for human TLR7 and Rat TLR7, respectively. SM-324405 is used for immunoresearch of allergic diseases. An antedrug is defined as a locally active compound that is designed to be rapidly metabolized to an inactive form upon entry into the circulation and prevents systemic toxicity by losing its agonistic activity in a plasmatic environment.
|
-
- HY-106481
-
|
Bufrolin
|
GPR35
Histamine Receptor
|
Inflammation/Immunology
|
|
Bufrolin is a Cromoglycate (histamine release inhibitor) analog and a high potency agonist of GPR35. Bufrolin promotes interactions between β-arrestin-2 and either human GPR35a or rat GPR35. Bufrolin also serves as antiallergic mast cell stabilizer and inhibit an anti-inflammatory response inducible by the internalization peptide. Bufrolin acts as an anti-inflammatory agent to be used in research of delivering pharmacol linked with internalization peptide.
|
-
- HY-147428
-
|
Zolunicant
MM-110; (±)-18-Methoxycoronaridine
|
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, methamphetamine, nicotine, and ethanol in rat model. Zolunicant can be studied as a potential research for multiple forms of agent abuse. Zolunicant also reveals a potent leishmanicide effect against Leishmania amazonensis.
|
-
- HY-107732
-
|
JNJ-5207787
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
JNJ-5207787 is a nonpeptidic, selective and penetrate the blood-brain barrier neuropeptide Y Y2 receptor (Y2) antagonist. JNJ-5207787 inhibits the binding of peptide YY (PYY) with pIC50s of 7.0 and 7.1 for human Y2 receptor and rat Y2 receptor, respectively. JNJ-5207787 is >100-fold selective versus human Y1, Y4, and Y5 receptors.
|
-
- HY-P3678
-
-
- HY-100743
-
|
DL-AP4
2-Amino-4-phosphonobutyric acid
|
Others
|
Metabolic Disease
Neurological Disease
|
|
DL-AP4 (2-Amino-4-phosphonobutyric acid) is a glutamate antagonist. DL-AP4 behaves as a competitive inhibitor of glutamate binding with an apparent Kd of 66 μM. DL-AP4 can be used for the research of central nervous system and visual system.
|
-
- HY-100978
-
|
(±)-Hexanoylcarnitine chloride
DL-Hexanoylcarnitine chloride
|
Endogenous Metabolite
|
Metabolic Disease
|
|
(±)-Hexanoylcarnitine chloride is a fatty acid metabolite that breaks down fatty acids into energy that can be used by the body. (±)-Hexanoylcarnitine chloride also serves as a specific and easily detectable biomarker for rat skeletal muscle toxicity. Cerivastatin (HY-129458) and TMPD (HY-W012145) induce an increase in Hexanoylcarnitine in rats in a metabolomic analysis of the rectus femoris muscle. In type 2 diabetes, Hexanoylcarnitine is also significantly associated with and improves prediction of all-cause mortality. Hexanoylcarnitine is a biomarker for the identification of novel pathogenic pathways.
|
-
- HY-107691
-
|
GR 159897
|
Neurokinin Receptor
|
Cancer
Endocrinology
Neurological Disease
|
|
GR 159897 is a highly potent, selective, competitive, brain-penetrated non-peptide neurokinin 2 (NK2) receptor antagonist. GR 159897 has little or no affinity for NK1 and NK3 receptors. GR 159897 inhibits binding of [ 3H]GR100679 to human NK2 (hNK2)-CHO cells and rat colon membranes with pKis of 9.51 and 10, respectively. Antagonizes bronchoconstriction. Anxiolytic-like and anti-tumor effects.
|
-
- HY-111191
-
|
ONO-2952
|
Adrenergic Receptor
|
Neurological Disease
|
|
ONO-2952 is a potent, selective and orally active translocator protein 18 kDa (TSPO) antagonist with Ki of 0.33-9.30 nM for rat and human TSPO. ONO-2952 is more selective for TSPO than other receptors, transporters, ion channels and enzymes. ONO-2952 exerts its anti-stress effects through inhibition of excessive activation of noradrenergic system in the brain without the amnesic effect. ONO-2952 has the potential for irritable bowel syndrome treatment.
|
-
- HY-116749
-
|
Ethaselen
BBSKE
|
TrxR
|
Cancer
|
|
Ethaselen (BBSKE) is an orally active, selective thioredoxin reductase (TrxR) inhibitor with IC50s of 0.5 and 0.35 μM for the wild-type human TrxR1 and rat TrxR1, respectively. Ethaselen specifically binds to the unique selenocysteine-cysteine redox pair in the C-terminal active site of mammalian TrxR1. Ethaselen, an organoselenium compound, is a potent antitumor candidate that exerts potent inhibition on non-small cell lung cancer (NSCLC) by targeting TrxR.
|
-
- HY-19996
-
|
AH-7614
|
Free Fatty Acid Receptor
|
Metabolic Disease
|
|
AH-7614 is a potent and selective FFA4 (GPR120) antagonist, with pIC50s of 7.1, 8.1, and 8.1 for human, mouse, and rat FFA4, respectively. AH-7614 has selectivity for FFA4 over FFA1 (pIC50<4.6). AH-7614 is able to block effects of both the polyunsaturated ω-6 fatty acid linoleic acid and the synthetic FFA4 agonist.
|
-
- HY-15342
-
|
Timapiprant
OC000459
|
Prostaglandin Receptor
|
Inflammation/Immunology
Endocrinology
|
|
Timapiprant (OC000459) is a potent, selective, and orally active D prostanoid receptor 2 (DP2, also known as CRTH2) antagonist. Timapiprant (OC000459) potently displaces [ 3H] PGD2 from human recombinant DP2 (Ki=13 nM), rat recombinant DP2 (Ki=3 nM), and human native DP2 (Ki=4 nM). Timapiprant (OC000459) inhibits mast cell activation of Th2 lymphocytes and eosinophils.
|
-
- HY-131972
-
|
PF-06843195
|
PI3K
|
Cancer
|
|
PF-06843195 is a highly selective PI3Kα inhibitor with an IC50 of 18 nM in Rat1 fibroblasts. The Kis of PF-06843195 for PI3Kα and PI3Kδ in biochemical kinase assay are less than 0.018 nM and 0.28 nM, respectively. PF-06843195 has great suppression of the PI3K/mTOR signaling pathway and durable antitumor efficacy.
|
-
- HY-107625A
-
|
SNAP 94847 hydrochloride
|
MCHR1 (GPR24)
|
Neurological Disease
|
|
SNAP 94847 hydrochloride is a novel, high affinity selective melanin-concentrating hormonereceptor1 (MCHR1) antagonist with (Ki= 2.2 nM, Kd=530 pM), it displays >80-fold and >500-fold selectivity over MCHα1A and MCHD2 receptors respectively. SNAP 94847 hydrochloride binds with high affinity to the mouse and rat MCHR1 with minimal cross-reactivity to other GPCR, ion channels, enzymes, and transporters.
|
-
- HY-19411
-
|
SSR180711 hydrochloride
|
nAChR
|
Neurological Disease
|
|
SSR180711 hydrochloride is an orally active, selective and reversible α7 acetylcholine nicotinic receptor (n-AChRs) partial agonist. SSR180711 hydrochloride can act on rat α7 n-AChR (Ki=22 nM; IC50=30 nM) and human α7 n-AChR (Ki=14 nM; IC50=18 nM). SSR180711 hydrochloride increases glutamatergic neurotransmission, ACh release and long-term potentiation (LTP) in the hippocampus.
|
-
- HY-N0930B
-
|
Galegine hydrochloride
|
AMPK
Bacterial
|
Infection
Metabolic Disease
|
|
Galegine hydrochloride, a guanidine derivative, contributes to weight loss in mice. Guanidine hydrochloride is the compound derived from G. officinalis, which gave rise to the biguanides, metformin and phenformin. Galegine hydrochloride activates AMPK in 3T3-L1 adipocytes and L6 myotubes, as well as in the H4IIE rat hepatoma and HEK293 human kidney cell lines. Galegine hydrochloride has antibacterial activity, with minimum inhibitory concentration of 4 mg/L against Staphylococcus aureus strains.
|
-
- HY-16276A
-
|
Osilodrostat phosphate
LCI699 phosphate
|
Mineralocorticoid Receptor
|
Cancer
|
|
Osilodrostat (LCI699) phosphate is a potent, orally active11β-hydroxylase (CYP11B1) inhibitor with an IC50 value of 35 nM. Osilodrostat phosphate is a potent, orally aldosterone synthase (CYP11B2) inhibitor with IC50 values of 0.7 nM and 160 nM for human aldosterone synthase and rat aldosterone synthase, respectively. Osilodrostat phosphate inhibits aldosterone and corticosterone synthesis. Osilodrostat phosphate has blood pressure lowering ability. Osilodrostat phosphate can be used for research of Cushing syndrome (CS).
|
-
- HY-108611
-
|
AACOCF3
Arachidonyl trifluoromethyl ketone
|
Phospholipase
|
Cardiovascular Disease
|
|
AACOCF3 (Arachidonyl trifluoromethyl ketone) is a cell-permeant trifluoromethyl ketone analog of arachidonic acid. AACOCF3 is a potent and selective slow binding inhibitor of the 85-kDa cytosolic phospholipase A2 (cPLA2). AACOCF3 blocks production of arachidonate and 12-hydroxyeicosatetraenoic acid by calcium ionophore-challenged platelets. AACOCF3 inhibits glucose-induced insulin secretion from isolated rat islets. AACOCF3 has the potential for the research of cardiovascular disease.
|
-
- HY-15342A
-
|
Timapiprant sodium
OC000459 sodium
|
Prostaglandin Receptor
|
Inflammation/Immunology
Endocrinology
|
|
Timapiprant sodium (OC000459 sodium) is a potent, selective, and orally active D prostanoid receptor 2 (DP2, also known as CRTH2) antagonist. Timapiprant sodium (OC000459 sodium) potently displaces [ 3H] PGD2 from human recombinant DP2 (Ki=13 nM), rat recombinant DP2 (Ki=3 nM), and human native DP2 (Ki=4 nM). Timapiprant sodium (OC000459 sodium) inhibits mast cell activation of Th2 lymphocytes and eosinophils.
|
-
- HY-107625
-
|
SNAP 94847
|
MCHR1 (GPR24)
|
Neurological Disease
Endocrinology
|
|
SNAP 94847 is a novel, high affinity selective melanin-concentrating hormonereceptor1 (MCHR1) antagonist with (Ki= 2.2 nM, Kd=530 pM), it displays >80-fold and >500-fold selectivity over MCHα1A and MCHD2 receptors respectively. SNAP 94847 binds with high affinity to the mouse and rat MCHR1 with minimal cross-reactivity to other GPCR, ion channels, enzymes, and transporters.
|
-
- HY-16276
-
|
Osilodrostat
LCI699
|
Mineralocorticoid Receptor
|
Cancer
Inflammation/Immunology
|
|
Osilodrostat (LCI699) is a potent, orally active11β-hydroxylase (CYP11B1) inhibitor with an IC50 value of 35 nM. Osilodrostat is a potent, orally aldosterone synthase (CYP11B2) inhibitor with IC50 values of 0.7 nM and 160 nM for human aldosterone synthase and rat aldosterone synthase, respectively. Osilodrostat inhibits aldosterone and corticosterone synthesis. Osilodrostat has blood pressure lowering ability. Osilodrostat can be used for research of Cushing syndrome (CS).
|
-
- HY-12119
-
|
GW274150
|
NO Synthase
|
Inflammation/Immunology
Neurological Disease
|
|
GW274150 is a potent, selective, orally active and NADPH-dependent inhibitor of human inducible nitric oxide synthase (iNOS) (IC50=2.19 μM; Kd=40 nM) and rat iNOS (ED50=1.15 μM). GW274150 also displays less potency for both humans or rats endothelial NOS (eNOS) and neuronal NOS (nNOS). GW274150 exerts a protective role in an acute model of lung injury inflammation.
|
-
- HY-N1942
-
|
5-O-Demethylnobiletin
5-Demethylnobiletin
|
Lipoxygenase
Leukotriene Receptor
|
Inflammation/Immunology
Neurological Disease
Cancer
|
|
5-O-Demethylnobiletin (5-Demethylnobiletin), a polymethoxyflavone isolated from Citrus jambhiri Lush., is a direct inhibition of 5-LOX (IC50=0.1 μM), without affecting the expression of COX-2. 5-O-Demethylnobiletin (5-Demethylnobiletin) has anti-inflammatory activity, inhibits leukotriene B (4)(LTB4) formation in rat neutrophils and elastase release in human neutrophils with an IC50 of 0.35 μM.
|
-
- HY-107479
-
|
(R)-JNJ-31020028
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
(R)-JNJ-31020028 is a high affinity, selective brain penetrant neuropeptide Y Y2 receptor antagonist, with pIC50 values of 8.07, 8.22 and 8.21 for human, rat, and mouse Y2 receptor, respectively. (R)-JNJ-31020028 shows >100-fold selective versus human Y1, Y4, and Y5 receptors. (R)-JNJ-31020028 has antidepressant like effects.
|
-
- HY-N3807
-
|
Enniatin B1
|
Acyltransferase
ERK
NF-κB
|
Cancer
Infection
Cardiovascular Disease
|
|
Enniatin B1 is a Fusarium mycotoxin. Enniatin B1 inhibits acyl-CoA: cholesterol acyltransferase (ACAT) activity with an IC50 of 73 μM in an enzyme assay using rat liver microsomes. Enniatin B1 crosss the blood-brain barrier. Enniatin B1 decreases the activation of ERK (p44/p42). Enniatin B1 inhibits moderately TNF-α-induced NF-κB activation.
|
-
- HY-P1321
-
|
GR231118
1229U91; GW1229
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
GR231118, an analogue of the C-terminus of neuropeptide Y, is a potent , competitive and relative seletive antagonist at human neuropeptide Y Y receptor with a pKi of 10.4. GR231118 a potent agonist at the human neuropeptide Y Y4 receptor (pEC50=8.6; pKi=9.6) and a weak agonist at the human and rat neuropeptide YY2 and Y5 receptors. GR231118 also has high affinity for the mouse neuropeptide Y Y6 receptor (pKi= 8.8).
|
-
- HY-19651
-
|
Zanapezil free base
TAK-147 free base
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
Zanapezil (TAK-147) free base is a potent, reversible and selective acetylcholine esterase (AChE) inhibitor. Zanapezil free base shows a potent and reversible inhibition of AChE activity in homogenates of the rat cerebral cortex (IC50=51.2 nM). Zanapezil free base shows a moderate inhibition of muscarinic M1 and M2 receptor binding with Ki values of 234 and 340 nM, respectively. Zanapezil free base can be used for the research of early stages of Alzheimer's disease (AD).
|
-
- HY-10932
-
|
Aniracetam
Ro 13-5057
|
nAChR
iGluR
|
Neurological Disease
|
|
Aniracetam (Ro 13-5057) is an orally active neuroprotective agent, possessing nootropics effects. Aniracetam potentiates the ionotropic quisqualate (iQA) responses in the CA1 region of rat hippocampal slices. Aniracetam also potentiates the excitatory post synaptic potentials (EPSPs) in Schaffer collateral-commissural synapses. Aniracetam can prevents the CO2-induced impairment of acquisition in hypercapnia model rats. Aniracetam can be used to research cerebral dysfunctional disorders.
|
-
- HY-P0262
-
|
Galantide
|
Neuropeptide Y Receptor
|
Metabolic Disease
Inflammation/Immunology
Neurological Disease
Endocrinology
|
|
Galantide, a non-specific galanin receptor antagonist, is a peptide consisting of fragments of galanin and substance P. Galantide recognizes two classes of galanin binding sites (KD<0.1 nM and ~6 nM) in the rat hypothalamus. Galantide dose dependently (IC50=1.0 nM) antagonizes the galanin-mediated inhibition of the glucose-induced insulin secretion from mouse pancreatic islets. Galantide appears to bind to a single population of SP receptors (KD~40 nM).
|
-
- HY-146478
-
|
A1/A3 AR antagonist 1
|
Adenosine Receptor
|
Inflammation/Immunology
Neurological Disease
|
|
A1/A3 AR antagonist 1 (compound 10) is a potent adenosine 1 (A1) and adenosine 3 (A3) receptor dual antagonist with Kis of 36.7 nM, 25.4 nM and 1.47 nM for human A1, human A3 and rat A1, respectively. A1/A3 AR antagonist 1 can be used for researching kidney failure, inflammatory pulmonary diseases, and Alzheimer’s disease.
|
-
- HY-P1321A
-
|
GR231118 TFA
1229U91 TFA; GW1229 TFA
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
GR231118 TFA, an analogue of the C-terminus of neuropeptide Y, is a potent , competitive and relative seletive antagonist at human neuropeptide YY receptor with a pKi of 10.4. GR231118 a potent agonist at the human neuropeptide YY4 receptor (pEC50=8.6; pKi=9.6) and a weak agonist at the human and rat neuropeptide Y Y2 and Y5 receptors. GR231118 also has high affinity for the mouse neuropeptide YY6 receptor (pKi= 8.8).
|
-
- HY-B0822
-
|
Fipronil
|
GABA Receptor
Cytochrome P450
Apoptosis
|
Neurological Disease
|
|
Fipronil is a broad-spectrum insecticide effective against Lepidoptera species as well as thrips, locusts, ants, cockroaches, fleas and ticks. Fipronil selectively inhibits GABA receptor with IC50s of 30 nM and 1600 nM for cockroach and rat GABA receptors, respectively. Glutamate-gated chloride channels (GluCls), which are present in cockroaches but not in mammals, are sensitive to the blocking effect of Fipronil. Fipronil also induces apoptosis in HepG2 cells and promotes the expression of CYP1A1 and CYP3A4 mRNA in human hepatocytes.
|
-
- HY-144827
-
|
AM8936
|
Cannabinoid Receptor
|
Neurological Disease
Metabolic Disease
|
|
AM8936 acts as a balanced and potent cannabinoid receptor type-1 (CB1) agonist in functional assays (EC50s of 8.6 and 1.4 nM for rCB1 and hCB1, respectively). AM8936 exhibits high affinity for rat CB1 (rCB1) with Ki of 0.55 nM. AM8936 is a potent and efficacious CB1 agonist in vivo. AM8936 can be used for the research of CNS and metabolic disorders, pain, glaucoma, etc.
|
-
- HY-120124
-
|
Samelisant
SUVN-G3031
|
Histamine Receptor
|
Neurological Disease
|
|
Samelisant (SUVN-G3031) is a potent and selective histamine H3 receptor (H3R) inverse agonist with good brain penetration and oral bioavailability. Samelisant has a similar binding affinity towards human (hH3R; Ki=8.7 nM) and rat (rH3R;Ki=9.8 nM) H3R indicating no inter-species differences. Samelisant can be used for the research of sleep-related disorders.
|
-
- 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-40136S
-
|
cis-4-Hydroxy-L-proline-d3
|
Endogenous Metabolite
|
|
|
cis-4-Hydroxy-L-proline-d3 is the deuterium labeled cis-4-Hydroxy-L-proline. cis-4-Hydroxy-L-proline, a proline analogue, is an inhibitor of collagen production. cis-4-Hydroxy-L-proline could inhibit fibroblast growth by preventing the deposition of triple-helical collagen on the cell layer. cis-4-Hydroxy-L-proline also depresses the growth of primary N-nitrosomethylurea-induced rat mammary tumors[1][2][3][4].
|
-
- HY-100588
-
|
VU0364770
|
mGluR
|
Neurological Disease
|
|
VU0364770 is a selective and potent positive allosteric modulator (PAM) of mGlu4. VU0346770 exhibits EC50s of 290 nM and 1.1 μM at rat mGlu4 and human mGlu4 receptor, respectively. VU0364770 exhibits antagonist activity at mGlu5 with a potency of 17.9 μM and PAM activity at mGlu6 with a potency of 6.8 μM. VU0364770 also possesses activity at MAO with Ki values of 8.5 and 0.72 μM for human MAO-A and human MAO-B, respectively.
|
-
- HY-13866
-
|
Ro 31-8220 mesylate
Ro 31-8220 methanesulfonate; Bisindolylmaleimide IX mesylate
|
PKC
|
Neurological Disease
Cardiovascular Disease
Cancer
|
|
Ro 31-8220 mesylate is a potent PKC inhibitor, with IC50s of 5, 24, 14, 27, 24 and 23 nM for PKCα, PKCβI, PKCβII, PKCγ, PKCε and rat brain PKC, respectively. Ro 31-8220 also significantly inhibits MAPKAP-K1b, MSK1, S6K1 and GSK3β (IC50s, 3, 8, 15, and 38 nM, respectively), with no effect on MKK3, MKK4, MKK6 and MKK7.
|
-
- HY-130344
-
|
SKF83959
|
Dopamine Receptor
Sigma Receptor
|
Neurological Disease
|
|
SKF83959 is a potent and selective dopamine D1-like receptor partial agonist. SKF83959 Ki values for rat D1, D5, D2 and D3 receptors are 1.18, 7.56, 920 and 399 nM, respectively. SKF83959 is a potent allosteric modulator of sigma (σ)-1 receptor. SKF83959 belongs to benzazepine family and has improvements on cognitive dysfunction. SKF83959 can be used for the research of Alzheimer's disease and depression.
|
-
- HY-101249
-
|
L-732138
|
Neurokinin Receptor
|
Cancer
Neurological Disease
|
|
L-732138 is a selective, potent and competitive neurokinin-1 (NK-1) receptor antagonist with an IC50 of 2.3 nM. L-732138 has 200-fold more potent in cloned human NK-1 receptors than cloned rat NK-1 receptors, and has > 1000-fold more potent than human NK-2 and NK-3 receptors. L-732138 can reduce hyperalgesia and has antitumor action.
|
-
- 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[1]. Propranolol inhibits [3H]-DHA binding to rat brain membrane preparation with an IC50 of 12 nM[2]. Propranolol is used for the study of hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy[3].
|
-
- 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[1]. Propranolol hydrochloride inhibits [3H]-DHA binding to rat brain membrane preparation with an IC50 of 12 nM[2]. Propranolol hydrochloride is used for the study of hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy[3].
|
-
- HY-122608
-
|
Samelisant free base
SUVN-G3031 free base
|
Histamine Receptor
|
Neurological Disease
|
|
Samelisant (SUVN-G3031) free base is a potent and selective histamine H3 receptor (H3R) inverse agonist with good brain penetration and oral bioavailability. Samelisant free base has a similar binding affinity towards human (hH3R; Ki=8.7 nM) and rat (rH3R;Ki=9.8 nM) H3R indicating no inter-species differences. Samelisant free base can be used for the research of sleep-related disorders.
|
-
- HY-14571
-
|
E7820
ER68203-00
|
Molecular Glues
Integrin
|
Cancer
|
|
E7820 (ER68203-00), an orally active aromatic sulfonamide derivative, is a unique angiogenesis inhibitor suppressing an expression of integrin alpha2 subunit on endothelium. E7820 inhibits rat aorta angiogenesis with an IC50 of 0.11 μg/ml. E7820 modulates α-1, α-2, α-3, and α-5 integrin mRNA expression. Antiangiogenic and antitumor activity.
|
-
- HY-100588A
-
|
VU0364770 hydrochloride
|
mGluR
|
Neurological Disease
|
|
VU0364770 hydrochloride is a selective and potent positive allosteric modulator (PAM) of mGlu4. VU0346770 hydrochloride exhibits EC50s of 290 nM and 1.1 μM at rat mGlu4 and human mGlu4 receptor, respectively. VU0364770 hydrochloride exhibits antagonist activity at mGlu5 with a potency of 17.9 μM and PAM activity at mGlu6 with a potency of 6.8 μM. VU0364770 hydrochloride also possesses activity at MAO with Ki values of 8.5 and 0.72 μM for human MAO-A and human MAO-B, respectively.
|
-
- HY-12765
-
|
Losartan Carboxylic Acid
E-3174; EXP-3174
|
Angiotensin Receptor
|
Cardiovascular Disease
|
|
Losartan Carboxylic Acid (E-3174), an active carboxylic acid metabolite of Losartan, is an angiotensin II receptor type 1 (AT1) antagonist. The Ki values are 0.97, 0.57, 0.67 nM for rat AT1B/AT1A and human AT1, respectively. Losartan Carboxylic Acid blocks the angiotensin II-induced responses in vascular smoothmuscle cells (VSMC). Losartan Carboxylic Acid elevates plasma renin activities and reduces mean arterial pressure.
|
-
- HY-103409
-
|
ABT-724 trihydrochloride
|
Dopamine Receptor
|
Neurological Disease
|
|
ABT-724 trihydrochloride is a potent and highly selective dopamine D4 receptor agonist with an EC50 of 12.4 nM for human dopamine D4 receptor. ABT-724 trihydrochloride is a potent partial agonist at the rat D4 (EC50 of 14.3 nM) and the ferret D4 receptor (EC50 of 23.2 nM), and has no effect on dopamine D1, D2, D3, or D5 receptors. ABT-724 trihydrochloride could be useful for the treatment of erectile dysfunction and has favorable side-effect profile.
|
-
- HY-13866A
-
|
Ro 31-8220
Bisindolylmaleimide IX
|
PKC
|
Neurological Disease
Cardiovascular Disease
|
|
Ro 31-8220 is a potent PKC inhibitor, with IC50s of 5, 24, 14, 27, 24 and 23 nM for PKCα, PKCβI, PKCβII, PKCγ, PKCε and rat brain PKC, respectively. Ro 31-8220 also significantly inhibits MAPKAP-K1b, MSK1, S6K1 and GSK3β (IC50s, 3, 8, 15, and 38 nM, respectively), with no effect on MKK3, MKK4, MKK6 and MKK7.
|
-
- HY-103286
-
|
PD176252
|
Bombesin Receptor
|
Cancer
|
|
PD176252 is a potent antagonist of neuromedin-B preferring (BB1) and gastrin-releasing peptide-preferring (BB2) receptor with Kis of 0.17 nM and 1 nM for human BB1 and BB2 receptors, and 0.66 nM, 16 nM for Rat BB1 and BB2 receptors, respectively; PD176252 is also an agonist of N-Formyl peptide receptor1/2 (FPR1/FPR2), with EC50s of 0.31 and 0.66 μM in HL-60 cells.
|
-
- HY-18071A
-
|
BI-9627 hydrochloride
|
Na+/H+ Exchanger (NHE)
|
Cardiovascular Disease
|
|
BI-9627 hydrochloride is potent sodium-hydrogen exchanger isoform 1 (NHE1) inhibitor, with IC50s of 6 and 31 nM in intracellular pH recovery (pHi) and human platelet swelling assays, respectively. BI-9627 hydrochloride displays >30-fold selectivity against NHE2 and with no measurable inhibitory activity against the NHE3 isoform. BI-9627 hydrochloride shows low DDI (agent-agent interaction) potential, excellent pharmacokinetics in rat and dog, and remarkably potent activity in the isolated heart model of ischemia-reperfusion injury.
|
-
- HY-107428
-
|
PD-166793
|
MMP
|
Cardiovascular Disease
|
|
PD-166793 is a potent, selective, orally active and wide‐broad spectrum inhibitor of MMP, exhibiting nanomolar potency against MMP-2, MMP-3 and MMP-13 (IC50=4, 7, and 8 nM, respectively) and micromolar potency vs MMP-1, -7 and -9 (IC50=6.0, 7.2, and 7.9 μM, respectively). PD-166793 can attenuate left ventricular remodeling and dysfunction in a rat model of progressive heart failure.
|
-
- HY-14330
-
|
ABT-724
|
Dopamine Receptor
|
Neurological Disease
|
|
ABT-724 is a potent and highly selective dopamine D4 receptor agonist with an EC50 of 12.4 nM for human dopamine D4 receptor. ABT-724 is a potent partial agonist at the rat D4 (EC50 of 14.3 nM) and the ferret D4 receptor (EC50 of 23.2 nM). ABT-724 has no effect on dopamine D1, D2, D3, or D5 receptors. ABT-724 could be useful for the treatment of erectile dysfunction and has favorable side-effect profile.
|
-
- HY-109139
-
|
Taminadenant
NIR178; PBF509
|
Adenosine Receptor
|
Cancer
Neurological Disease
|
|
Taminadenant (NIR178; PBF509) is a highly potent and orally active adenosine A2A receptor (A2AR) antagonist. Taminadenant can antagonize A2AR agonist-mediated cAMP accumulation and impedance responses with KB values of 72.8 nM and 8.2 nM, respectively. Taminadenant reverses motor impairments in several rat models of movement disorders, including catalepsy, tremor, and hemiparkinsonism. Taminadenant can also inhibit tumor growth when combined with Spartalizumab (HY-P9972). Taminadenant reactivate the antitumor immune response.
|
-
- HY-W324243
-
|
11β-HSD1-IN-9
|
11β-HSD
|
Metabolic Disease
|
|
11β-HSD1-IN-9 (compound c4a) is a potent 11β-HSD1 inhibitor with IC50 values of 0.48 and 1.3 µM for human and murine 11β-HSD1, respectively. 11β-HSD1-IN-9 competitively interacts with rat 11β-HSD1. 11β-HSD1-IN-19 can be used in studies of obesity, hyperglycemia and cognitive impairment.
|
-
- HY-14604
-
|
Xaliproden hydrochloride
SR57746A; SR57746 hydrochloride
|
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
|
Xaliproden hydrochloride (SR57746A) is a potent, selective and orally active agonist of 5-HT1A receptor, shows a high affinity for 5-HT1A specific binding sites in the rat hippocampus (IC50=3 nM). Xaliproden hydrochloride is also a selective antagonist of dopamine D2 receptor, has moderate affinity (IC50=0.1-1 μM). Xaliproden hydrochloride exhibits anti-depression and anti-anxiety effects, and it may possess therapeutic potential for the research of neurodegenerative diseases.
|
-
- 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[1]. Propranolol hydrochloride inhibits [3H]-DHA binding to rat brain membrane preparation with an IC50 of 12 nM[2]. Propranolol hydrochloride is used for study of hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy[3].
|
-
- HY-P2161B
-
|
TAK-683 acetate
|
Kisspeptin Receptor
|
Cancer
|
|
TAK-683 acetate is a potent full KISS1 receptor (KISS1R) agonist (IC50=170 pM) with improved metabolic stability. TAK-683 acetate is a nonapeptide metastin analog, exhibits agonistic activities to KISS1R with EC50 values of 0.96 nM and 1.6 nM for human and rat, respectively. TAK-683 acetate depletes GnRH in the hypothalamus and reduces plasma FSH, LH, and testosterone levels in vivo, it has the potential for the study of hormone-dependent prostate cancer.
|
-
- 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-P1424A
-
|
Lei-Dab7 TFA
|
Potassium Channel
|
|
|
Lei-Dab7 TFA is a high affinity, selective KCa2.2 (SK2) channel blocker (Kd=3.8 nM). Lei-Dab7 TFA exhibits >200-fold selectivity for KCa2.2 over KCa2.1, KCa2.3, KCa3.1, Kv and Kir2.1. Lei-Dab7 TFA increases theta-burst responses and increases LTP in rat hippocampal slices in vitro.
|
-
- HY-P2161A
-
|
TAK-683 TFA
|
Kisspeptin Receptor
|
Cancer
|
|
TAK-683 TFA is a potent full KISS1 receptor (KISS1R) agonist (IC50=170 pM) with improved metabolic stability. TAK-683 TFA is a nonapeptide metastin analog, exhibits agonistic activities to KISS1R with EC50 values of 0.96 nM and 1.6 nM for human and rat, respectively. TAK-683 TFA depletes GnRH in the hypothalamus and reduces plasma FSH, LH, and testosterone levels in vivo, it has the potential for the study of hormone-dependent prostate cancer.
|
-
- HY-19995
-
|
GSK137647A
GSK 137647
|
Free Fatty Acid Receptor
|
Metabolic Disease
|
|
GSK137647A (GSK 137647) is a potent, selective free fatty acid receptor 4 (FFA4) agonist with pEC50 values of 6.3, 6.2, and 6.1 for human, mouse and rat FFA4, and pEC50 values < 4.5 for all three species for FFA1, FFA2, and FFA3, respectively. GSK137647A has anti-inflammatory activity. GSK137647A induces insulin secretion and inhibits epithelial ion transport, GSK137647A is related to regulation of glucose homeostasis and anti-inflammatory response.
|
-
- HY-14850
-
|
Sograzepide
Netazepide; YF 476; YM-220
|
Cholecystokinin Receptor
|
Metabolic Disease
Endocrinology
|
|
Sograzepide (Netazepide; YF 476; YM-220) is an extremely potent , highly selective and orally active Gastrin/CCK-B antagonist with an IC50 value of 0.1 nM, has inhibitory effect on Gastrin/CCK-A activity with an IC50 of 502 nM. Sograzepide (Netazepide; YF 476; YM-220) replaces the specific binding of [125I]CCK-8 to the rat brain, cloned canine and cloned human Gastrin/CCK-B receptors, with Ki values of 0.068, 0.62 and 0.19 nM, respectively.
|
-
- HY-100769
-
|
Hypidone hydrochloride
YL0919
|
5-HT Receptor
|
Neurological Disease
|
|
Hypidone hydrochloride (YL0919) is an orally active antidepressant agent with dual activity as a highly seletive 5-HT uptake blocker and an effective 5-HT1A receptor agonist (Ki=0.19 nM). Hypidone hydrochloride inhibits the uptake of [ 3H]-5-HT into rat cerebral cortical synaptosomes and HEK293 cells with IC50s of 1.78 nM and 1.93 nM, respectively. Hypidone hydrochloride shows remarkable antidepressant effects in animal models and has the poential for the investigation of depressive disorder.
|
-
- HY-118152
-
|
Org-12962
|
5-HT Receptor
|
Neurological Disease
|
|
Org-12962 is a potent, selective and orally active 5-HT2C receptor agonist with a pEC50 value of 7.01. Org-12962 also exhibits high effacy for the 5-HT2A and 5-HT2B receptor with pEC50s of 6.38 and 6.28, respectively.Org-12962 displays antiaversive effects in a rat model of panic-like anxiety.
|
-
- HY-B0847S1
-
|
Propiconazole-d3 nitrate
|
Fungal
Reactive Oxygen Species
|
Infection
|
|
Propiconazole-d3 (nitrate) is the deuterium labeled Propiconazole nitrate. Propiconazole is a broad-spectrum triazole fungicide that inhibits the conversion of lanosterol to ergosterol, leading to fungal cell membrane disruption. Propiconazole inhibits S. cerevisiae, but not rat liver, microsomal cytochrome P450 (IC50s=0.04 and >200 µM, respectively). Propiconazole inhibits the growth of T. deformans and R. stolonifer (ED50s=0.073 and 4.6 µg/mL, respectively). Propiconazole increases production of reactive oxygen species (ROS).
|
-
- HY-B0847S
-
|
Propiconazole-d7
|
Fungal
Reactive Oxygen Species
|
Infection
|
|
Propiconazole-d7 is the deuterium labeled Propiconazole. Propiconazole is a broad-spectrum triazole fungicide that inhibits the conversion of lanosterol to ergosterol, leading to fungal cell membrane disruption. Propiconazole inhibits S. cerevisiae, but not rat liver, microsomal cytochrome P450 (IC50s=0.04 and >200 µM, respectively). Propiconazole inhibits the growth of T. deformans and R. stolonifer (ED50s=0.073 and 4.6 µg/mL, respectively). Propiconazole increases production of reactive oxygen species (ROS)[1].
|
-
- HY-P1210
-
|
Lys-γ3-MSH(human)
|
Melanocortin Receptor
|
Endocrinology
|
|
Lys-γ3-MSH(human) is a melanocortin peptide derived from the C-terminal of the fragment of pro-opiomelanocortin (POMC). Lys-γ3-MSH(human) potentiates the steroidogenic response of the rat adrenal to adrenocorticotrophin (ACTH). Lys-γ3-MSH(human) is a potent stimulator of lipolysis with an apparent EC50 of 3.56 nM. Lys-γ3-MSH(human) can activate hormone sensitive lipase (HSL) and Perilipin A resulting in lipolysis.
|
-
- HY-P2161
-
|
TAK-683
|
Kisspeptin Receptor
|
Cancer
|
|
TAK-683 is a potent full KISS1 receptor (KISS1R) agonist (IC50=170 pM) with improved metabolic stability. TAK-683 is a nonapeptide metastin analog, exhibits agonistic activities to KISS1R with EC50 values of 0.96 nM and 1.6 nM for human and rat, respectively. TAK-683 depletes GnRH in the hypothalamus and reduces plasma FSH, LH, and testosterone levels in vivo, it has the potential for the study of hormone-dependent prostate cancer.
|
-
- HY-18071
-
|
BI-9627
|
Na+/H+ Exchanger (NHE)
|
Cardiovascular Disease
|
|
BI-9627 is potent sodium-hydrogen exchanger isoform 1 (NHE1) inhibitor, with IC50s of 6 and 31 nM in intracellular pH recovery (pHi) and human platelet swelling assays, respectively. BI-9627 displays >30-fold selectivity against NHE2 and with no measurable inhibitory activity against the NHE3 isoform. BI-9627 shows low DDI (agent-agent interaction) potential, excellent pharmacokinetics in rat and dog, and remarkably potent activity in the isolated heart model of ischemia-reperfusion injury.
|
-
- HY-P1210A
-
|
Lys-γ3-MSH(human) TFA
|
Melanocortin Receptor
|
Endocrinology
|
|
Lys-γ3-MSH(human) TFA is a melanocortin peptide derived from the C-terminal of the fragment of pro-opiomelanocortin (POMC). Lys-γ3-MSH(human) TFA potentiates the steroidogenic response of the rat adrenal to adrenocorticotrophin (ACTH). Lys-γ3-MSH(human) TFA is a potent stimulator of lipolysis with an apparent EC50 of 3.56 nM. Lys-γ3-MSH(human) TFA can activate hormone sensitive lipase (HSL) and Perilipin A resulting in lipolysis.
|
-
- HY-14993
-
|
SCH79797
|
Protease Activated Receptor (PAR)
Apoptosis
|
Cardiovascular Disease
|
|
SCH79797 is a highly potent, selective nonpeptide protease activated receptor 1 (PAR1) antagonist. SCH79797 inhibits binding of a high-affinity thrombin receptor-activating peptide to PAR1 with an IC50 of 70 nM and a Ki of 35 nM. SCH79797 inhibits thrombin-induced platelet aggregation with an IC50 of 3 μM. SCH79797 has antiproliferative and pro-apoptotic effects, and limits myocardial ischemia/reperfusion injury in rat hearts. SCH79797 also potently prevents PAR1 activation in vascular smooth muscle cells, endothelial cells, and astrocytes.
|
-
- HY-117427
-
|
D5D-IN-326
|
Others
|
Metabolic Disease
|
|
D5D-IN-326 is a selective, orally active delta-5 desaturase (D5D) inhibitor, with IC50s of 72 and 22 nM for rat and human D5D in enzymic and cell-based assays, respectively, has no effect on D6D or D9D activity. D5D-IN-326 reduces insulin resistance and decreases body weight in diet-induced obese C57BL/6J mice.
|
-
- HY-12765S1
-
|
Losartan carboxylic acid-d4 hydrochloride
|
Angiotensin Receptor
|
Cardiovascular Disease
|
|
Losartan carboxylic acid-d4 (hydrochloride) is deuterium labeled Losartan Carboxylic Acid. Losartan Carboxylic Acid (E-3174), an active carboxylic acid metabolite of Losartan, is an angiotensin II receptor type 1 (AT1) antagonist. The Ki values are 0.97, 0.57, 0.67 nM for rat AT1B/AT1A and human AT1, respectively. Losartan Carboxylic Acid blocks the angiotensin II-induced responses in vascular smoothmuscle cells (VSMC). Losartan Carboxylic Acid elevates plasma renin activities and reduces mean arterial pressure[1][2][3][4].
|
-
- HY-107664A
-
|
SR 142948 dihydrochloride
|
Neurotensin Receptor
|
Neurological Disease
|
|
SR 142948 dihydrochloride is an orally active and selective non-peptide neurotensin receptor (NT) antagonist with IC50s of 1.19 nM, 0.32 nM, 3.96 nM in h-NTR1-CHO cells, HT-29 cells, and adult rat brain, respectively. SR 142948 dihydrochloride antagonizes NT-induced inositol monophosphate formation in HT-29 cells with an IC50 of 3.9 nM. SR 142948 dihydrochloride blocks hypothermia, analgesia and steering behavior induced by NT in vivo. SR 142948 dihydrochloride shows blood-brain permeability and can be used in study of psychiatric disorders.
|
-
- HY-107664
-
|
SR 142948
|
Neurotensin Receptor
|
Neurological Disease
|
|
SR 142948 is an orally active and selective non-peptide neurotensin receptor (NT) antagonist with IC50s of 1.19 nM, 0.32 nM, 3.96 nM in h-NTR1-CHO cells, HT-29 cells, and adult rat brain, respectively. SR 142948 antagonizes NT-induced inositol monophosphate formation in HT-29 cells with an IC50 of 3.9 nM. SR 142948 blocks hypothermia, analgesia and steering behavior induced by NT in vivo. SR 142948 shows blood-brain permeability and can be used in study of psychiatric disorders.
|
-
- HY-103412
-
|
SKF 83959 hydrobromide
|
Dopamine Receptor
Sigma Receptor
|
Neurological Disease
|
|
SKF83959 hydrobromide is a potent and selective dopamine D1-like receptor partial agonist. SKF83959 hydrobromide Ki values for rat D1, D5, D2 and D3 receptors are 1.18, 7.56, 920 and 399 nM, respectively. SKF83959 hydrobromide is a potent allosteric modulator of sigma (σ)-1 receptor. SKF83959 hydrobromide belongs to benzazepine family and has improvements on cognitive dysfunction. SKF83959 hydrobromide can be used for the research of Alzheimer's disease and depression.
|
-
- HY-14994
-
|
SCH79797 dihydrochloride
|
Protease Activated Receptor (PAR)
Apoptosis
|
Cardiovascular Disease
|
|
SCH79797 dihydrochloride is a highly potent, selective nonpeptide protease activated receptor 1 (PAR1) antagonist. SCH79797 dihydrochloride inhibits binding of a high-affinity thrombin receptor-activating peptide to PAR1 with an IC50 of 70 nM and a Ki of 35 nM. SCH79797 dihydrochloride inhibits thrombin-induced platelet aggregation with an IC50 of 3 μM. SCH79797 dihydrochloride has antiproliferative and pro-apoptotic effects, and limits myocardial ischemia/reperfusion injury in rat hearts. SCH79797 dihydrochloride also potently prevents PAR1 activation in vascular smooth muscle cells, endothelial cells, and astrocytes.
|
-
- HY-14280A
-
|
Entacapone sodium salt
|
COMT
|
Neurological Disease
|
|
Entacapone sodium salt is a potent, reversible, peripherally acting and orally active catechol-O-methyltransferase (COMT) inhibitor. Entacapone sodium salt inhibits COMT from rat brain, erythrocytes and liver with IC50 values of 10 nM, 20 nM, and 160 nM, respectively. Entacapone sodium salt is selective for COMT over other catecholamine metabolizing enzymes, including MAO-A, MAO-B, phenolsulphotransferase M (PST-M) and PST-P (IC50s>50 µM). Entacapone sodium salt can be used for the research of Parkinson's disease. Entacapone sodium salt serves as as a inhibit of FTO demethylation with an IC50 of 3.5 μM, can be used for the research of metabolic disorders.
|
-
- HY-151562
-
|
AChE/BuChE/MAO-B-IN-1
|
Cholinesterase (ChE)
Monoamine Oxidase
|
Neurological Disease
|
|
AChE/BuChE/MAO-B-IN-1 (compound 19) is an inhibitor of human acetyl- (hAChE), butyrylcholinesterase (hBuChE) and monoamine oxidase-B (hMAO-B) with IC50s of 4.8 μM, 13.7 μM, and 1.11 μM, respectively. AChE/BuChE/MAO-B-IN-1 also exhibits high affinity to both the σ1 and σ2 receptors with Ki values of 42.8 nM (human σ1 receptor) and 191 nM (rat σ2 receptor), respectively. AChE/BuChE/MAO-B-IN-1 can be used for Alzheimer’s disease research.
|
-
- HY-144790
-
|
AChE-IN-12
|
Amyloid-β
Cholinesterase (ChE)
Monoamine Oxidase
|
Neurological Disease
|
|
AChE-IN-12 is a potent and blood-brain barrier (BBB) penetrant acetylcholinesterase (AChE) with IC50s of 0.41 μM and 1.88 μM for rat AChE and electric eel AChE. AChE-IN-12 is also a good antioxidant (ORAC = 3.3 eq), selective metal chelator and huMAO-B inhibitor (IC50 = 8.8 µM). AChE-IN-12 has remarkable inhibition of self- and Cu 2+-induced Aβ1-42 aggregation, as well as exhibits a good neuroprotective effect. AChE-IN-12 can be used for researching Alzheimer’s disease.
|
-
- HY-A0168S
-
|
Regadenoson-d3
CVT-3146-d3
|
Adenosine Receptor
|
Cardiovascular Disease
Cancer
|
|
Regadenoson-d3 is the deuterium labeled Regadenoson. Regadenoson (CVT-3146) is a potent and selective A2A adenosine receptor agonist, with Kis of 290 and 1120 nM for rat and pig adenosine A2A receptor, respectively. Regadenoson is selective for the adenosine A2A receptor over adenosine A1 and A2B receptors, and shows 13-fold selectivity over the human adenosine A1 receptor. Regadenoson is a vasodilator stress agent has shifted the landscape of vasodilator myocardial perfusion imaging. Regadenoson increases blood-brain barrier (BBB) permeability in rodents[1][2][3].
|
-
- HY-14280
-
|
Entacapone
|
COMT
|
Neurological Disease
|
|
Entacapone is a potent, reversible, peripherally acting and orally active catechol-O-methyltransferase (COMT) inhibitor. Entacapone inhibits COMT from rat brain, erythrocytes and liver with IC50 values of 10 nM, 20 nM, and 160 nM, respectively. Entacapone is selective for COMT over other catecholamine metabolizing enzymes, including MAO-A, MAO-B, phenolsulphotransferase M (PST-M) and PST-P (IC50s>50 µM). Entacapone can be used for the research of Parkinson's disease. Entacapone serves as a inhibitor of FTO demethylation with an IC50 of 3.5 μM, can be used for the research of metabolic disorders.
|
-
- HY-Q40175
-
|
Antitrypanosomal agent 9
|
Parasite
|
Infection
|
|
Antitrypanosomal agent 9 (compound 1) is a potent antitrypanosomal agent. Antitrypanosomal agent 9 shows inhibitory activity against T. b. brucei, with an IC50 of 1.15 μM. Antitrypanosomal agent 9 can be used for human African trypanosomiasis (HAT) research.
|
-
- HY-108648
-
|
2-Methylthioadenosine diphosphate trisodium
2-Methylthio-ADP trisodium
|
P2Y Receptor
|
Neurological Disease
|
|
2-Methylthioadenosine diphosphate trisodium is a potent purinergic P2Y receptors agonist, with EC50s of 19, 6.2, and 5 nM for human P2Y13, mouse P2Y13 and human P2Y12, respectively. 2-Methylthioadenosine diphosphate trisodium has pEC50s of 8.29 and 5.75 for human P2Y1 and rat P2Y6, respectively. 2-Methylthioadenosine diphosphate trisodium induces platelet aggregation and shape change, and inhibits cyclic AMP accumulation in platelets exposed to prostaglandin E1.
|
-
- HY-14280S
-
|
Entacapone-d10
|
COMT
|
Neurological Disease
|
|
Entacapone-d10 is the deuterium labeled Entacapone. Entacapone is a potent, reversible, peripherally acting and orally active catechol-O-methyltransferase (COMT) inhibitor. Entacapone inhibits COMT from rat brain, erythrocytes and liver with IC50 values of 10 nM, 20 nM, and 160 nM, respectively. Entacapone is selective for COMT over other catecholamine metabolizing enzymes, including MAO-A, MAO-B, phenolsulphotransferase M (PST-M) and PST-P (IC50s>50 µM). Entacapone can be used for the research of Parkinson's disease[1]. Entacapone serves as a inhibitor of FTO demethylation with an IC50 of 3.5 μM, can be used for the research of metabolic disorders[2].
|
-
- HY-16677A
-
|
Mofegiline hydrochloride
MDL72974A
|
Monoamine Oxidase
|
Neurological Disease
|
|
Mofegiline hydrochloride (MDL72974A) is an orally active and selective enzyme-activated irreversible inhibitor of MAO-B, with marked selectivity on the MAO-B over MAO-A with IC50s of 3.6 nM (MAO-B) and 680 nM (MAO-A), respectively. Mofegiline hydrochloride is also an inhibitor of semicarbazide-sensitive amine oxidase (SSAO).
|
-
- HY-100604
-
|
JNJ-40418677
|
γ-secretase
Amyloid-β
|
Neurological Disease
|
|
JNJ-40418677 is an orally active modulator of γ-secretase, can cross the blood-brain barrier. JNJ-40418677 inhibits Aβ42 and NS2B-NS3 protease, with IC50s of 200 nM and 3.9 μM, respectively. JNJ-40418677 displays good biological tolerance, can be use for Alzheimer’s disease research.
|
-
- HY-136254
-
|
BzATP triethylammonium salt
|
P2X Receptor
|
Cancer
Inflammation/Immunology
|
|
BzATP triethylammonium salt acts as a P2X receptor agonist with pEC50s of 8.74, 5.26, 7.10, 7.50, 6.19, 6.31, 5.33 for P2X1, P2X2, P2X3, P2X2/3, P2X4 and P2X7, respectively. BzATP triethylammonium salt is potent at P2X7 receptors with EC50s of 3.6 μM and 285 μM for rat P2X7 and mouse P2X7, respectively.
|
-
- HY-14280S2
-
|
(E)-Entacapone-d10
|
COMT
|
Neurological Disease
|
|
(E)-Entacapone-d10 is the deuterium labeled Entacapone. Entacapone is a potent, reversible, peripherally acting and orally active catechol-O-methyltransferase (COMT) inhibitor. Entacapone inhibits COMT from rat brain, erythrocytes and liver with IC50 values of 10 nM, 20 nM, and 160 nM, respectively. Entacapone is selective for COMT over other catecholamine metabolizing enzymes, including MAO-A, MAO-B, phenolsulphotransferase M (PST-M) and PST-P (IC50s>50 µM). Entacapone can be used for the research of Parkinson's disease[1]. Entacapone serves as a inhibitor of FTO demethylation with an IC50 of 3.5 μM, can be used for the research of metabolic disorders[2].
|
-
- 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.
|
-
- HY-148682
-
|
18β-Glycyrrhetyl-3-O-sulfate
Glycyrrhetic acid 3-O-hydrogen sulfate
|
11β-HSD
Drug Metabolite
|
Metabolic Disease
Inflammation/Immunology
|
|
18β-Glycyrrhetyl-3-O-sulfate (Glycyrrhetic acid 3-O-(hydrogen sulfate)) is a potent type 2 11β-hydroxysteroid dehydrogenase (11β-HSD2) inhibitor with an IC50 of 0.10 µM using rat kidney microsome. 18β-Glycyrrhetyl-3-O-sulfate is the major metabolite of Glycyrrhetinic acid (GA). 18β-Glycyrrhetyl-3-O-sulfate is the substrate of organic anion transporter (OAT) 1 and OAT3. 18β-Glycyrrhetyl-3-O-sulfate has anti-inflammatory effects and has the potential for pseudohyperaldosteronism research.
|
-
- HY-150079
-
|
HIV-1 integrase inhibitor 10
|
HIV Integrase
|
Infection
|
|
HIV-1 integrase inhibitor 10 is an orally active HIV-1 allosteric integrase inhibitor (ALLINI). HIV-1 integrase inhibitor 10 can inhibit viral outgrowth of the NLRepRluc virus in MT-2 cells with EC50 values of 3-5 nM. HIV-1 integrase inhibitor 10 can be used for the research of Human immunodeficiency virus-1 (HIV-1).
|
-
- HY-10341
-
|
Fasudil Hydrochloride
HA-1077 Hydrochloride; AT-877 Hydrochloride
|
ROCK
Calcium Channel
Autophagy
PKA
PKC
HIV
|
Cancer
|
|
Fasudil (HA-1077; AT877) Hydrochloride is a nonspecific RhoA/ROCK inhibitor and also has inhibitory effect on protein kinases, with an Ki of 0.33 μM for ROCK1, IC50s of 0.158 μM and 4.58 μM, 12.30 μM, 1.650 μM for ROCK2 and PKA, PKC, PKG, respectively. Fasudil Hydrochloride is also a potent Ca 2+ channel antagonist and vasodilator.
|
-
- HY-10341C
-
|
Fasudil dihydrochloride
HA-1077 dihydrochloride; AT-877 dihydrochloride
|
Calcium Channel
ROCK
PKA
PKC
Autophagy
HIV
|
Cancer
|
|
Fasudil (HA-1077; AT877) dihydrochloride is a nonspecific RhoA/ROCK inhibitor and also has inhibitory effect on protein kinases, with an Ki of 0.33 μM for ROCK1, IC50s of 0.158 μM and 4.58 μM, 12.30 μM, 1.650 μM for ROCK2 and PKA, PKC, PKG, respectively. Fasudil dihydrochloride is also a potent Ca 2+ channel antagonist and vasodilator.
|
-
- HY-10341B
-
|
Fasudil hydrochloride semihydrate
HA-1077 hydrochloride semihydrate; AT877 hydrochloride semihydrate
|
ROCK
Calcium Channel
Autophagy
HIV
PKA
PKC
|
Cancer
|
|
Fasudil (HA-1077; AT877) hydrochloride semihydrate is a nonspecific RhoA/ROCK inhibitor and also has inhibitory effect on protein kinases, with an Ki of 0.33 μM for ROCK1, IC50s of 0.158 μM and 4.58 μM, 12.30 μM, 1.650 μM for ROCK2 and PKA, PKC, PKG, respectively. Fasudil hydrochloride semihydrate is also a potent Ca 2+ channel antagonist and vasodilator.
|
-
- HY-10341A
-
|
Fasudil
HA-1077; AT877
|
ROCK
Calcium Channel
Autophagy
PKA
PKC
|
Cancer
|
|
Fasudil (HA-1077; AT877) is a nonspecific RhoA/ROCK inhibitor and also has inhibitory effect on protein kinases, with an Ki of 0.33 μM for ROCK1, IC50s of 0.158 μM and 4.58 μM, 12.30 μM, 1.650 μM for ROCK2 and PKA, PKC, PKG, respectively. Fasudil is also a potent Ca 2+ channel antagonist and vasodilator.
|
-
- HY-W127391
-
|
1,2-Dilaurin
(Rac)-1,2-Didodecanoylglycerol
|
Biochemical Assay Reagents
|
Others
|
|
1,2-Dilaurin is a diacylglycerol containing lauric acid at the sn-1 and sn-2 positions. It has been used as an internal standard for the quantification of diglycerides in rat desheathed sciatic nerves. [1] Monomolecular films containing 1,2-dilauroyl-rac-glycerol have been used as substrates to measure surface pressure and the effect of pancreatic procolipase and colipase on porcine pancreatic lipase activity. [2] References: [1]. Zhu, X. and Eichberg, J. 1,2-Diacylglycerol content and its arachidonyl-containing molecular species are reduced in the sciatic nerve of streptozotocin-induced diabetic rats. J. Neurochemistry. 55(3), 1087-1090 (1990).[2]. Wieloch, T., Borgstr?m, B., Piéroni, G. et al. Porcine trypsinogen and its trypsin-activated form: lipid binding and lipase activation on monomolecular membranes. FEBS Express. 128(2), 217-220 (1981).
|
-
- HY-12764
-
|
6-OAU
GTPL5846
|
GPR84
ERK
Bacterial
Antibiotic
|
Inflammation/Immunology
|
|
6-OAU (GTPL5846) (6-n-octylaminouracil) is an GPR84 (G protein-coupled receptor 84) agonist, with an EC50 value of 105 nM. 6-OAU works as a chemoattractant to both PMNs and macrophages, and amplifies the proinflammatory cytokine IL-8, shows proinflammatory function. 6-OAU also displays anti-bacterial function.
|
-
- HY-B0384
-
-
- HY-100713
-
-
- HY-151093
-
| Cat. No. |
Product Name |
Type |
| Cat. No. |
Product Name |
Type |
-
- HY-W127391
-
|
1,2-Dilaurin
(Rac)-1,2-Didodecanoylglycerol
|
Biochemical Assay Reagents
|
|
1,2-Dilaurin is a diacylglycerol containing lauric acid at the sn-1 and sn-2 positions. It has been used as an internal standard for the quantification of diglycerides in rat desheathed sciatic nerves. [1] Monomolecular films containing 1,2-dilauroyl-rac-glycerol have been used as substrates to measure surface pressure and the effect of pancreatic procolipase and colipase on porcine pancreatic lipase activity. [2] References: [1]. Zhu, X. and Eichberg, J. 1,2-Diacylglycerol content and its arachidonyl-containing molecular species are reduced in the sciatic nerve of streptozotocin-induced diabetic rats. J. Neurochemistry. 55(3), 1087-1090 (1990).[2]. Wieloch, T., Borgstr?m, B., Piéroni, G. et al. Porcine trypsinogen and its trypsin-activated form: lipid binding and lipase activation on monomolecular membranes. FEBS Express. 128(2), 217-220 (1981).
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| Cat. No. |
Product Name |
Target |
Research Area |
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- HY-P2416
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-
- HY-P1349
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-
- HY-P1532
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-
- HY-P1296
-
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Urocortin, rat
Urocortin (rattus norvegicus); rat urocortin;
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CRFR
|
Neurological Disease
Endocrinology
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|
Urocortin, rat (Urocortin (Rattus norvegicus)) is a neuropeptide and a potent endogenous CRFR agonist with Kis of 13 nM, 1.5 nM, and 0.97 nM for human CRF1, rat CRF2α and mouse CRF2β, respectively.
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-
- HY-P4814
-
|
Proadrenomedullin (1-20) (rat)
rat PAMP
|
Peptides
|
Others
|
|
Proadrenomedullin (1-20, rat) (Rat PAMP) is a polypeptide that can be found by peptide screening. Peptide screening is a research tool that pools active peptides primarily by immunoassay. Peptide screening can be used for protein interaction, functional analysis, epitope screening, especially in the field of agent research and development.
|
-
- HY-P1349A
-
|
Orexin B, rat, mouse TFA
rat orexin B TFA; Orexin B (mouse) (TFA)
|
Orexin Receptor (OX Receptor)
|
Endocrinology
Neurological Disease
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|
Orexin B, rat, mouse (Rat orexin B) TFA is an endogenous orexin receptor agonist. Orexin B, rat, mouse TFA binds and activates two closely related orphan G protein-coupled receptors OX1-R and OX2-R. Orexin B, rat, mouse TFA stimulates food intake and energy expenditure and plays a significant role in sleep-wakefulness regulation.
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-
- HY-P1296A
-
|
Urocortin, rat TFA
Urocortin (rattus norvegicus) (TFA); rat urocortin TFA
|
CRFR
|
Endocrinology
Neurological Disease
|
|
Urocortin, rat TFA (Urocortin (Rattus norvegicus) TFA) is a neuropeptide and a potent endogenous CRFR agonist with Kis of 13 nM, 1.5 nM, and 0.97 nM for human CRF1, rat CRF2α and mouse CRF2β, respectively.
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-
- HY-P0209
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-
- HY-P1238
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|
Neuromedin U, rat
Neuromedin U (rat); rat neuromedin U-23
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Peptides
|
Neurological Disease
|
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Neuromedin U, rat is a 23-amino acid brain-gut peptide. Neuromedin U (NMU), through its cognate receptor NMUR2 in the central nervous system, regulates several important physiological functions, including energy balance, stress response, and nociception.
|
-
- HY-P1238A
-
|
Neuromedin U, rat TFA
Neuromedin U (rat) (TFA); rat neuromedin U-23 TFA
|
Peptides
|
Neurological Disease
|
|
Neuromedin U, rat TFA is a 23-amino acid brain-gut peptide. Neuromedin U (NMU), through its cognate receptor NMUR2 in the central nervous system, regulates several important physiological functions, including energy balance, stress response, and nociception.
|
-
- HY-P2457
-
|
rCRAMP (rat)
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Bacterial
|
Infection
Inflammation/Immunology
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rCRAMP (rat) is the rat cathelin-related antimicrobial peptide. rCRAMP (rat) contributes to the antibacterial activity in rat brain peptide/protein extracts. rCRAMP (rat) is a potential key player in the innate immune system of rat CNS.
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-
- HY-P3603
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-
- HY-P3534
-
|
EILDV (human, bovine, rat)
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Peptides
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Cancer
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EILDV (human, bovine, rat) is an analogue of the active pentapeptide. EILDV (human, bovine, rat) has active tripeptide amino acid sequence LDV that is conserved in human, bovine, rat. EILDV (human, bovine, rat) can be used for the research of cell adhesion.
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-
- HY-P1573
-
-
- HY-P1913
-
-
- HY-P1142
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