Search Result
Results for "
rat blood
" in MedChemExpress (MCE) Product Catalog:
2
Biochemical Assay Reagents
8
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-P0203
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CGRP (83-119), mouse, rat
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CGRP Receptor
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Cardiovascular Disease
Metabolic Disease
Inflammation/Immunology
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α-CGRP (mouse, rat), a neuropeptide (calcitonin gene-related peptide (CGRP)) mainly expressed in neuromuscular junction, is a potent vasodilator. α-CGRP (mouse, 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 (mouse, rat) has the potential in cardiovascular, pro-inflammatory, migraine and metabolic studies .
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- HY-109012
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JNJ-42847922
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Orexin Receptor (OX Receptor)
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Neurological Disease
Endocrinology
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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 .
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- HY-12378
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BQ-123
3 Publications Verification
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Endothelin Receptor
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Cardiovascular Disease
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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 .
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- HY-102064
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5-HT Receptor
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Neurological Disease
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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 .
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- HY-108463
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- HY-106224B
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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 binds and activates two types of G protein-coupled receptors, the orexin-1 receptor (OX1R) and the orexin-2 receptor (OX2R). 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-148195
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NNZ-2591
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Biochemical Assay Reagents
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Neurological Disease
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Ercanetide (NNZ 2591) is a synthetic analogue of a small peptide of cyclic glycine proline (cGP). Ercanetide shows orally active and cross the blood-brain barrier. Ercanetide shows neuroprotective after ischemic brain injury. NNZ 2591 improves motor function in a rat model of Parkinson's disease. Ercanetide has the potential for the research of ischemic brain injury and angelman syndrome .
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- HY-14806
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MP-513
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Dipeptidyl Peptidase
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Cardiovascular Disease
Neurological Disease
Metabolic Disease
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Teneligliptin (MP-513) hydrobromide hydrate is an orally active and selective dipeptidyl peptidase 4 (DPP-4) inhibitor (IC50s: 0.37 and 0.29 nM for the human and rat DPP-4, respectively). Teneligliptin hydrobromide hydrate improves blood glucose levels and can be used in researches related to type 2 diabetes mellitus .
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- HY-150508
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MK-0159
1 Publications Verification
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CD38
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Cardiovascular Disease
Metabolic Disease
Inflammation/Immunology
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MK-0159 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 .
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- HY-W010520
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Environmental Pollutants
MMP
Bacterial
Fungal
Apoptosis
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Infection
Inflammation/Immunology
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Methylothiazolinone is a bacterial and fungal inhibitor and preservative, as well as a sensitizer. Methylisothiazolinone can activate matrix metalloproteinases (MMPs) in human bronchial epithelial cells to induce apoptosis and inflammatory response. Methylisothiazolinone can promote the development of atopic dermatitis in mice by disrupting Th2/Th17 related immune responses. Methylisothiazolinone can cause mitochondrial damage in the endothelium of rat cerebral blood vessels .
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- HY-109012A
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JNJ-42847922 hydrochloride
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Orexin Receptor (OX Receptor)
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Neurological Disease
Metabolic Disease
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Seltorexant hydrochloride (JNJ-42847922 hydrochloride) is an orally active, high-affinity, and selective OX2R antagonist (pKi values of 8.0 and 8.1 for human and rat OX2R). Seltorexant hydrochloride crosses the blood-brain barrier and quickly occupies OX2R binding sites in the rat brain .
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- HY-B2141
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NO Synthase
HIF/HIF Prolyl-Hydroxylase
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Cardiovascular Disease
Others
Metabolic Disease
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Bendazol is an orally effective antihypertensive agent. Bendazol acts directly on vascular smooth muscle to dilate blood vessels and reduce peripheral resistance, thereby improving blood circulation. Bendazol significantly inhibits the development of myopia in rabbit models. Bendazol can regulate kidney function by increasing the activity of NO synthase in the rat model of nephrogenic hypertension. In addition, Bendazol has an effect on sexual behavior and spermatogenesis in male rats .
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- HY-14806A
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- HY-122542B
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Ligands for E3 Ligase
Molecular Glues
IKZF Family
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Cardiovascular Disease
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PPACK TFA is an orally active, selective molecular glue degrader targeting IKZF2. Through a molecular glue mechanism, PPACK TFA binds to CRBN, recruits IKZF2 to form a ternary complex, and promotes its ubiquitination and proteasomal degradation. This further converts inhibitory regulatory T cells (Treg) into effector-like T cells, enhances CD8 + T cell responses, and modulates the Teff:Treg balance. PPACK TFA also increases the production of the inflammatory cytokine IL-2 and reduces the suppressive activity of Treg. PPACK TFA can be used in cancer immunotherapy research, and exhibits a synergistic effect when combined with immune checkpoint inhibitors such as anti-PD1 .
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- HY-114782
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L-Tyrosyl-L-tyrosine
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Angiotensin-converting Enzyme (ACE)
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Cardiovascular Disease
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H-Tyr-Tyr-OH (L-Tyrosyl-L-tyrosine) is an antihypertensive peptide. H-Tyr-Tyr-OH inhibits angiotensin I-converting enzyme (ACE) with an IC50 value of 0.028 mg/mL. H-Tyr-Tyr-OH can be used for the research of high blood pressure .
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- HY-P0203A
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CGRP (83-119), mouse, rat TFA
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CGRP Receptor
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Cardiovascular Disease
Metabolic Disease
Inflammation/Immunology
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α-CGRP (mouse, rat) TFA, a neuropeptide (calcitonin gene-related peptide (CGRP)) mainly expressed in neuromuscular junction, is a potent vasodilator. α-CGRP (mouse, 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 (mouse, rat) TFA has the potential in cardiovascular, pro-inflammatory, migraine and metabolic studies .
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- HY-109968
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CEP-26401
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Histamine Receptor
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Neurological Disease
Metabolic Disease
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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 .
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- HY-14806B
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- HY-113854
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AZD2906
1 Publications Verification
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Glucocorticoid Receptor
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Cardiovascular Disease
Endocrinology
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AZD2906 is a selective glucocorticoid receptor (GR) agonist, increases micronucleated immature erythrocytes in the bone marrow of rats. AZD2906 shows IC50s of 2.2, 0.3, 41.6 and 7.5 nM at GR in human, rat PBMC and human, rat whole blood, respectively .
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- HY-W145497
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Insulin Receptor
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Metabolic Disease
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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 .
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- HY-78086
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3-Methylbenzaldehyde
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Endogenous Metabolite
Bacterial
Cytochrome P450
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Infection
Inflammation/Immunology
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m-Tolualdehyde (3-Methylbenzaldehyde) is an aldehyde metabolite produced by m-xylene metabolism, and it bidirectionally regulates the CYP 2B1, CYP 2E1, and CYP 4B1 isoenzymes in the respiratory tract of rats. m-Tolualdehyde serves as an oxidation substrate and carbon source for Pseudomonas Pxy, and it can be oxidized to m-toluic acid in an NAD + -dependent manner. m-Tolualdehyde exerts a dose-dependent inhibitory effect on CYP 2B1 and CYP 2E1 in the nasal mucosa and lungs of rats, and a dose-dependent activating effect on pulmonary CYP 4B1. m-Tolualdehyde can form aldehyde-heme adducts with the heme group of cytochrome P450. m-Tolualdehyde can be used in studies related to metabolic enzymes in the respiratory tract of rats .
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- HY-N2160
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GABA Receptor
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Neurological Disease
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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 .
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- HY-N7062
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Takeda-25
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FAAH
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Neurological Disease
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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 .
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- HY-122373
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Aldehyde Dehydrogenase (ALDH)
Drug Derivative
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Metabolic Disease
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Coprine is an orally active disulfiram (HY-B0240)-like component and an inhibitor of aldehyde dehydrogenase. Coprine is isolated from Coprinus atranentarius. Coprine inhibits low Km aldehyde dehydrogenase in rat liver and increases blood acetaldehyde levels during in vivo ethanol metabolism. Coprine does not inhibit semi-purified low Km aldehyde dehydrogenase from rat liver in vitro. Coprine can be used in studies related to alcoholism .
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- HY-147403S
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JNJ-61393215
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Orexin Receptor (OX Receptor)
Isotope-Labeled Compounds
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Neurological Disease
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Tebideutorexant is an OX1R-selective inhibitor with oral bioavailability and blood-brain barrier permeability, with human OX1R pKi 8.17 and rat OX1R pKi 8.13.Tebideutorexant selectively modulates OX1R, with no significant functional effect on OX2R. Tebideutorexant can be used for the research of panic and anxiety disorders .
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- HY-101478
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mGluR
Apoptosis
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Neurological Disease
Cancer
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Fenobam is a selective and orally active mGluR5 antagonist (IC50=84 nM) that can penetrate the blood-brain barrier. Fenobam shows the Kd values of 54 nM and 31 nM on rat and human recombinant mGlu5 receptors, respectively. Fenobam has anxiolytic activity, inhibits self-administration behavior in mice, and induces apoptosis in cancer cells. Fenobam can be used for research on neurological diseases, cancer and drug addiction .
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- HY-W010243
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Bacterial
MMP
Apoptosis
Fungal
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Infection
Inflammation/Immunology
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Methylisothiazolinone hydrochloride is a bacterial and fungal inhibitor and preservative, as well as a sensitizer. Methylisothiazolinone hydrochloride can activate matrix metalloproteinases (MMPs) in human bronchial epithelial cells to induce apoptosis and inflammatory response. Methylisothiazolinone hydrochloride can promote the development of atopic dermatitis in mice by disrupting Th2/Th17 related immune responses. Methylisothiazolinone hydrochloride can cause mitochondrial damage in the endothelium of rat cerebral blood vessels .
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- HY-118941
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Prostaglandin Receptor
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Cardiovascular Disease
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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 .
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- HY-W014134
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p-Amidinophenylmethylsulfonylfluoride hydrochloride
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Ser/Thr Protease
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Inflammation/Immunology
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p-APMSF (p-Amidinophenylmethylsulfonylfluoride) hydrochloride is a serine protease and trypsin inhibitor with the characteristic of rapid onset of action. p-APMSF hydrochloride reduces the enzymatic hydrolysis of recombinant human G-CSF in rat pulmonary mucosa. Combined intratracheal treatment with p-APMSF hydrochloride and Laureth-9 significantly enhances its absorption efficiency in rat lungs. Following intranasal administration, p-APMSF hydrochloride does not increase the concentration of recombinant human G-CSF in rat plasma, nor does it alter the effect of G-CSF on inducing an increase in total white blood cell count .
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- HY-121156A
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LF 16-0687 hydrochloride; XY-2405 hydrochloride
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Bradykinin Receptor
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Neurological Disease
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Anatibant (LF 16-0687; XY-2405) hydrochloride is a selective non-peptide bradykinin B2 receptor antagonist. Anatibant hydrochloride binds to the human, rat and guinea-pig recombinant B2 receptor with Ki values of 0.67 nM, 1.74 nM and 1.37 nM, respectively. Anatibant hydrochloride crosses the blood-brain barrier (BBB). Anatibant hydrochloride can be used in research on brain damage diseases .
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- HY-114164D
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Thrombin
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Cardiovascular Disease
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Rat Thrombin is a Na +-activated, allosteric serine protease that plays opposing functional roles in blood coagulation. Thrombin recognition sequence and can be used to digest GST-tagged proteins .
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- HY-W039898
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- HY-U00037
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PLA 725
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Phospholipase
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Inflammation/Immunology
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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.
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- HY-P1323A
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Neuropeptide Y Receptor
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Cardiovascular Disease
Neurological Disease
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[Leu31,Pro34]-Neuropeptide Y(human,rat) TFA is a specific neuropeptide Y Y1 receptor agonist. [Leu31,Pro34]-Neuropeptide Y(human,rat) TFA slao activates Y4, Y5. [Leu31,Pro34]-Neuropeptide Y(human,rat) TFA can increase blood pressure in anesthetized rats and increases food intake .
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![[Leu31,Pro34]-Neuropeptide Y(human,rat,mouse) TFA](//file.medchemexpress.com/product_pic/hy-p1323a.gif)
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- HY-108295
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CXB-722
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GABA Receptor
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Neurological Disease
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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 .
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- HY-W004425
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3,7-Dimethyl-1-propargylxanthine
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Adenosine Receptor
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Neurological Disease
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DMPX (3,7-Dimethyl-1-propargylxanthine) is a selective A2A adenosine receptor (A2A AR) antagonist that crosses the blood-brain barrier, with a Ki of 11 μM for rat A2 adenosine receptor and a Ki of 45 μM for rat A1 adenosine receptor. By blocking A2A receptors in specific brain regions, DMPX protects dopaminergic and GABAergic neurons from mitochondrial dysfunction. DMPX is applicable to research related to depression, Parkinson's disease and Huntington's disease .
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- HY-155642
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Urea Transporter
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Metabolic Disease
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PU-48 is a blood-brain barrier-permeable urea transporter (UT) inhibitor with an IC50 of 0.32 μM against rat UT-A. By functionally inhibiting urea transporters (including UT-A subtypes) in the renal inner medullary collecting ducts, PU-48 induces urea-selective diuresis. PU-48 does not alter blood levels of sodium, potassium or chloride ions, nor does it affect the excretion of non-urea solutes. PU-48 shows no significant toxicity in cell or animal models and can be used in edema-related research .
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- HY-156331
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mGluR
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Neurological Disease
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VU6004909 is a blood-brain barrier penetrated mGlu1 positive allosteric modulator (PAM), with the EC50s of 25.7 nM and 31 nM for human mGlu1 and rat mGlu1, respectively. VU6004909 reduces dorsolateral striatal dopamine (DA) release in vivo and displays antipsychotic efficacy .
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- HY-106934A
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BCX 34 dihydrochloride
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Nucleoside Antimetabolite/Analog
HIV
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Infection
Inflammation/Immunology
Cancer
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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 .
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- HY-123613
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- HY-P1323
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Neuropeptide Y Receptor
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Cardiovascular Disease
Neurological Disease
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[Leu31,Pro34]-Neuropeptide Y(human,rat) is a specific neuropeptide Y Y1 receptor agonist. [Leu31,Pro34]-Neuropeptide Y(human,rat) slao activates Y4, Y5. [Leu31,Pro34]-Neuropeptide Y(human,rat) can increase blood pressure in anesthetized rats and increases food intake .
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![[Leu31,Pro34]-Neuropeptide Y (human,rat)](//file.medchemexpress.com/product_pic/hy-p1323.gif)
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- HY-164412
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Endogenous Metabolite
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Neurological Disease
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Phosphatidylcholine (C18:2,C20:4) is a phosphatidylcholine species containing linoleic acid (C18:2) and arachidonic acid (C20:4) as fatty acid components, that can be isolated from egg yolk, red blood cell membranes of rat, rabbit, human, and dog. Phosphatidylcholine (C18:2,C20:4) can be used as a biomarker for the research of Alzheimer's disease .
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- HY-P3976
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Angiotensin-converting Enzyme (ACE)
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Cardiovascular Disease
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Lactalbumin B (50-53) Alpha [Lactorphin Alpha], bovine is a blood pressure lowering peptide containing 4 amino acids. Lactalbumin B (50-53) Alpha [Lactorphin Alpha], bovine is an angiotensin-converting Enzyme (ACE) inhibitor. Lactalbumin B (50-53) Alpha [Lactorphin Alpha], bovine can be used in research of high blood pressure .
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![Lactalbumin B (50-53) Alpha [Lactorphin Alpha], bovine](//file.medchemexpress.com/product_pic/hy-p3976.gif)
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- HY-125301
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Endogenous Metabolite
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Inflammation/Immunology
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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 .
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- HY-102043
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Phosphodiesterase (PDE)
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Neurological Disease
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PDM-631 is a selective and orally active PDE2A inhibitor with blood-brain barrier penetration. PDM-631 exhibits potent inhibitory activity against human and rat recombinant PDE2A with IC50 values of 1.5 nM and 4.2 nM, respectively. PDM-631 increases cGMP levels in the rat cerebral cortex. PDM-631 can be used for the study of schizophrenia and neurodegenerative disorders .
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- HY-162663
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ML253
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mAChR
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Neurological Disease
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VU0448088 (ML253) is a potent and cross the blood-brain barrier tricyclic muscarinic acetylcholine receptor subtype 4 (M4) positive allosteric modulator with EC50 values of 56, 176 nM for human and rat, respectively. VU0448088 has the potential for the research of psychotic .
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- HY-170409
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Trk Receptor
Apoptosis
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Neurological Disease
Inflammation/Immunology
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BNN27 is the agonist for TrkA receptor and p75NTR receptor, that exhibits neurotrophic and anti-apoptotic effects. BNN27 increases the levels of glutamate, GABA, and glutamine in the rat hippocampus and prefrontal cortex, improves glutamate turnover. BNN27 exhibits neuroprotective efficacy in mouse amyotrophic lateral sclerosis (ALS) model, exhibits anti-inflammatory efficacy in experimental autoimmune encephalomyelitis (EAE) model, exhibits retinal protective efficacy in rat diabete models. BNN27 is blood-brain barrier penetrable .
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- HY-19165
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Angiotensin Receptor
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Cardiovascular Disease
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CI-996 is a potent, selective, orally active angiotensin II (Ang II) type 1 (AT1) receptor antagonist. In rat liver membranes CI-996 displaces specifically bind [ 125I]Ang II with an IC50 of 0.8 nM. CI-996 has blood pressure-lowering activity .
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- HY-108973A
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CGP-15210G
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5-HT Receptor
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Neurological Disease
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Ifoxetine (CGP 15210G) is an inhibitor of 5-HT reuptake. Ifoxetine specifically and selectively blocks the 5-HT reuptake in the brain without affecting the 5-HT uptake processes in the periphery (blood platelets). Ifoxetine inhibits the uptake of radiolabelled 5-HT into rat brain synaptosomes in vitro or ex vivo. Ifoxetine has antidepressant properties .
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- HY-15008
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Oxytocin Receptor
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Endocrinology
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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 .
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- HY-106934
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BCX 34
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Nucleoside Antimetabolite/Analog
HIV
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Infection
Inflammation/Immunology
Cancer
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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 .
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- HY-122215
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N-696
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Adrenergic Receptor
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Endocrinology
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Tilisolol hydrochloride (N-696) is a non-selective β-adrenergic antagonist with vasodilatory and hypotensive activities. Tilisolol hydrochloride exerts its effects in canine coronary arteries by opening ATP-sensitive K+ channels. Tilisolol hydrochloride exhibits concentration-dependent relaxation in KCl-precontracted rat thoracic aorta. Tilisolol hydrochloride reduces diastolic blood pressure in a dose-dependent manner and slightly increases heart rate in spinal cord stimulated rats .
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- HY-164040
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Somatostatin Receptor
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Metabolic Disease
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Zavolosotine (Compound 1) is an orally active agonist for somatostatin receptor type 5 (SST5) with EC50 <1 nM. Zavolosotine inhibits insulin and glucagon secretion, increases levels of glucagon in blood in rat model .
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- HY-151894
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Epigenetic Reader Domain
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Cancer
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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 .
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- HY-110180
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mGluR
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Neurological Disease
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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) .
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- HY-120321
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Mineralocorticoid Receptor
Carbonic Anhydrase
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Cardiovascular Disease
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DSR-71167 is an orally active mineralocorticoid receptor (MR) antagonist with an IC50 of 0.26 μM. DSR-71167 exhibits weak carbonic anhydrase (CA) inhibitory activity with an IC50 of 19 μM. DSR-71167 can dose-dependently increase urinary sodium excretion in rat models and has a very low risk of hyperkalemia in potassium-loading rat models. DSR-71167 lowers systolic blood pressure in hypertensive rat models. DSR-71167 can be used for research on hypertension and heart failure .
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- HY-15112
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Prolyl Endopeptidase (PREP)
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Infection
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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) .
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- HY-A0113
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Ro 31-3113
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Angiotensin-converting Enzyme (ACE)
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Cardiovascular Disease
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|
Cilazaprilat is an inhibitor of angiotensin-converting enzyme (ACE; IC50=0.7 nM for the rat enzyme) and an active metabolite of Cilazapril (HY-A0043). It decreases creatine kinase release in primary neonatal rat cardiac myocytes in an in vitro model of ischemia-reperfusion injury induced by hypoxia and reoxygenation when used at a concentration of 10 μM.3 Intra-arterial administration of cilazaprilat (3 μg/kg per minute) increases coronary blood flow and fractional shortening in a dog model of coronary hypoperfusion-induced myocardial ischemia.
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-
- HY-158374
-
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IRAK
|
Inflammation/Immunology
|
|
BIO-8169 is a selective inhibitor for interleukin receptor-associated kinase 4 (IRAK 4), with an IC50 of 0.23 nM. BIO-8169 exhibits good pharmacokinetic character, reduces the production of pro-inflammatory cytokines, and attenuates the autoimmune encephalomyelitis in EAE mice model. BIO-8169 exhibits good blood brain penetrant with a rat Kpu,u of 0.7 .
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-
- HY-116680
-
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5-HT Receptor
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Cardiovascular Disease
Neurological Disease
|
|
LY53857 is a potent antagonist of vasoconstriction and serotonin-mediated 5-HT2 receptors. LY53857 did not reduce mean arterial blood pressure in spontaneously hypertensive rats (SHR) at doses that blocked the depressor response to serotonin and blocked central serotonin receptors. In addition, LY53857 was able to enhance neurotransmitter release in rat vas deferens and guinea pig ileal nerves .
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-
- HY-121156
-
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LF 16-0687; XY-2405
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Bradykinin Receptor
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Neurological Disease
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|
Anatibant (LF 16-0687; XY-2405) is a selective non-peptide bradykinin B2 receptor antagonist. Anatibant binds to the human, rat and guinea-pig recombinant B2 receptor with Ki values of 0.67 nM, 1.74 nM and 1.37 nM, respectively. Anatibant crosses the blood-brain barrier (BBB). Anatibant can be used in research on brain damage diseases .
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- HY-165600A
-
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TMB-4
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Cholinesterase (ChE)
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Others
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Trimedoxime (TMB-4) is a blood-brain barrier-permeable cholinesterase reactivator . Trimedoxime reactivates cholinesterase inhibited by paraoxon, sarin, tabun and other agents, restricts the breakdown of acetylcholine and alleviates excessive cholinergic stimulation. Trimedoxime reduces mortality and prolongs survival time. Trimedoxime exhibits reactivation efficacy against AChE in rat tissues. Trimedoxime can be used in research related to organophosphate (paraoxon) poisoning and tabun poisoning .
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- HY-W197533
-
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GABA Receptor
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Cardiovascular Disease
Neurological Disease
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3-Hydroxymethyl-β-carboline is a Benzodiazepine antagonist with a Ki value of ~1470 nM. 3-Hydroxymethyl-β-carboline reverses Flurazepam-induced sleep, cerebrovascular and cerebral metabolic inhibition, and also partially reverses Flurazepam-induced decreases in blood pressure and heart rate. 3-Hydroxymethyl-β-carboline disrupts the anticonvulsant and anxiolytic effects of Diazepam in male mice. 3-Hydroxymethyl-β-carboline has no effect on sodium-dependent high-affinity choline uptake in rat cortical or hippocampal synaptosomes .
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- HY-P5978
-
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ANP 127-150 (rat)
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Natriuretic Peptide Receptor (NPR)
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Cardiovascular Disease
|
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Atriopeptin III (ANP 127-150) (rat), a 24-amino acid atrial peptide, is a potent vasodilator and natriuretic/diuretic agent. Atriopeptin III (rat) improves renal functions and decreases blood pressure in a ureter-obstructed rat kidney model. Atriopeptin III (rat) can be used for research of chronic renal failure .
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- HY-123331
-
|
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Parasite
|
Infection
|
|
S 82-5455 is a floxacrine derivative that exhibits high activity against drug-susceptible strains of Plasmodium berghei induced in mouse and rat blood .
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-
- HY-P5130
-
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Endothelin Receptor
|
Cardiovascular Disease
|
|
Big endothelin-1 (rat 1-39) is a 39-residues peptide. Big endothelin-1 (rat 1-39) induces diuretic and natriuretic response in conscious Sprague-Dawley rats. Big endothelin-1 (rat 1-39) raises blood pressure in mice .
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-
- HY-116638
-
|
|
Lipoxygenase
|
Endocrinology
|
|
AHR-5333 is a selective human blood neutrophil 5-lipoxygenase inhibitor. AHR-5333 exhibits potent, long-acting activity in rat and guinea pig in vivo models of immediate hypersensitivity .
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-
- HY-19155A
-
|
ZD-8731
|
Angiotensin Receptor
|
Cardiovascular Disease
|
|
ICI-D 8731 (compound 5g) is a angiotensin II receptor antagonist with the IC50 of 0.031 μM. ICI-D 8731 shows a rapid and sustained lowering of blood pressure in a renal hypertensive rat model .
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-
- HY-116638A
-
|
|
Lipoxygenase
|
Endocrinology
|
|
AHR-5333 mandelate is a selective human blood neutrophil 5-lipoxygenase inhibitor. AHR-5333 mandelate exhibits potent, long-acting activity in rat and guinea pig in vivo models of immediate hypersensitivity .
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-
- HY-121191
-
|
N1,N8-Bisnorcymserine; (-)-Bisnorcymserine
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
Bisnorcymserine ((-)-Bisnorcymserine) is an inhibitor for butyrylcholinesterase (BChE) with an IC50 of 0.228 nM. Bisnorcymserine reduces the levels of amyloid-β peptide (Aβ), exhibits ameliorates the Alzheimer’s Disease in elderly rat models. Bisnorcymserine is blood-brain barrier penetrate .
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-
- HY-N11691
-
|
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 .
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-
- HY-178153
-
|
|
iGluR
|
Neurological Disease
|
|
BPAM363 is an orally active, selective positive allosteric modulator (PAM) of AMPARs with blood-brain barrier penetration. BPAM363 selectively potentiates AMPAR activity in human and rat models, with an EC2x value of 0.96 μM in rat embryonic cortex primary neurons. BPAM363 upregulates BDNF protein expression in rat primary cortical neuronal cultures. BPAM363 enhances AMPA-mediated excitatory postsynaptic responses in rat and mice. BPAM363 can be used for the study of cognitive disorders .
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-
- HY-78086R
-
|
3-Methylbenzaldehyde (Standard)
|
Reference Standards
Endogenous Metabolite
Bacterial
Cytochrome P450
|
Infection
Inflammation/Immunology
|
|
m-Tolualdehyde (Standard) is the analytical standard of m-Tolualdehyde (HY-78086). This product is intended for research and analytical applications. m-Tolualdehyde (3-Methylbenzaldehyde) is an aldehyde metabolite produced by m-xylene metabolism, and it bidirectionally regulates the CYP 2B1, CYP 2E1, and CYP 4B1 isoenzymes in the respiratory tract of rats. m-Tolualdehyde serves as an oxidation substrate and carbon source for Pseudomonas Pxy, and it can be oxidized to m-toluic acid in an NAD + -dependent manner. m-Tolualdehyde exerts a dose-dependent inhibitory effect on CYP 2B1 and CYP 2E1 in the nasal mucosa and lungs of rats, and a dose-dependent activating effect on pulmonary CYP 4B1. m-Tolualdehyde can form aldehyde-heme adducts with the heme group of cytochrome P450. m-Tolualdehyde can be used in studies related to metabolic enzymes in the respiratory tract of rats .
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-
- HY-W701743
-
|
α-Methyldopamine hydrochloride; α-MeDA hydrochloride
|
Drug Metabolite
|
Cardiovascular Disease
Neurological Disease
|
|
3,4-Dihydroxyamphetamine (α-Methyldopamine) (hydrochloride) is a secondary metabolite of 3,4-Methylenedioxymethamphetamine (MDMA). 3, 4-dihydroxyamphetamine (hydrochloride) is cytotoxic to rat hepatocytes. 3, 4-dihydroxyamphetamine (hydrochloride) is also used in the study of high blood pressure .
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-
- HY-P1694
-
|
|
Bradykinin Receptor
|
Cardiovascular Disease
|
|
B4148 is a selective competitive bradykinin (BK) antagonist that significantly inhibits BK-induced hypotension in rats. In a rat model of endotoxin shock induced by Escherichia coli lipopolysaccharide, B4148 significantly attenuated the decrease in mean arterial blood pressure compared with the control group .
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-
- HY-101478A
-
|
|
mGluR
Apoptosis
|
Neurological Disease
Cancer
|
|
Fenobam hydrate is a selective and orally active mGluR5 antagonist (IC50=84 nM) that can penetrate the blood-brain barrier. Fenobam hydrate shows the Kd values of 54 nM and 31 nM on rat and human recombinant mGlu5 receptors, respectively. Fenobam hydrate has anxiolytic activity, inhibits self-administration behavior in rat, and induces apoptosis in cancer cells. Fenobam hydrate can be used for research on neurological diseases, cancer and drug addiction .
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-
- HY-12378A
-
|
|
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 .
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-
- HY-W419570
-
|
|
P2Y Receptor
|
Cardiovascular Disease
|
|
(Rac)-BX 048 is a BX 048 racemate. BX 048 is a P2Y12 receptor antagonist. BX 048 inhibits ADP-induced platelet aggregation in human, dog and rat whole blood. BX 048 also inhibits Arachidonic acid (HY-109590) induced platelet aggregation (IC50 of 15 μM) .
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-
- HY-19114
-
|
|
Lipoxygenase
|
Inflammation/Immunology
|
|
WY-50295 is an orally active and selective 5-lipoxygenase inhibitor. WY-5029 inhibits LTB4 formation in rat whole blood leukocytes (IC50: 40 μM and oral ED50: 18 mg/kg). WY-50295 can be used in the study of asthma and other leukotriene-dependent diseases .
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-
- HY-125625
-
|
|
Renin
|
Cardiovascular Disease
|
|
ES 6864 is an orally active, competitive inhibitor for human renin, with an IC50 of 6.9 nM and a Ki of 7.3 nM. ES 6864 exhibits high species-specific and enzyme-specific properties. ES 6864 exhibits metabolic stability in rat tissue homogenates. ES 6864 reduces blood pressure in rats and sodium-depleted awake marmosets .
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-
- HY-109968A
-
|
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-106808
-
|
IOS-1.1212
|
Calcium Channel
Chloride Channel
|
Neurological Disease
|
|
Cerebrocrast (IOS-1.1212) is a 1,4-dihydropyridine (DHP) derivative. Cerebrocrast has a high affinity for the membrane lipid bilayer and it can easily penetrate the blood-brain barrier and incorporate into the plasma and organelle membranes, including those of mitochondria. Cerebrocrast promotes the cotransport of H+ and Cl- in rat liver mitochondria. Cerebrocrast also exhibits neuroprotective and cognition enhancer properties .
|
-
- HY-108973
-
|
CGP 15210G hemisulfate
|
5-HT Receptor
|
Neurological Disease
|
|
Ifoxetine (CGP 15210G) hemisulfate is an inhibitor of 5-HT reuptake. Ifoxetine hemisulfate specifically and selectively blocks the 5-HT reuptake in the brain without affecting the 5-HT uptake processes in the periphery (blood platelets). Ifoxetine hemisulfate inhibits the uptake of radiolabelled 5-HT into rat brain synaptosomes in vitro or ex vivo. Ifoxetine hemisulfate has antidepressant properties .
|
-
- HY-118185
-
|
|
Renin
|
Others
|
|
SQ 31844 is a novel renin inhibitor belonging to the imidazolidinol class. This compound, which contains an imidazole ring in its active site binding group, has potent in vitro inhibition of primate renin, but not rat, pig, or dog renin. In conscious, sodium-deprived cynomolgus monkeys, both compounds produced dose-related inhibition of plasma renin activity (PRA) over a dose range of 0.001 to 1.0 μmol/kg, administered intravenously, with complete inhibition observed at the highest dose. However, a reduction in blood pressure was only observed when 10 μmol/kg was administered intravenously or by infusion. In sodium-replete monkeys, SQ 30774 inhibited the increase in arterial blood pressure and PRA following administration of exogenous monkey renin. When the compounds were administered orally at 50 μmol/kg, only SQ 31844 significantly inhibited PRA (80%). In summary, the imidazolidinol renin inhibitors have potent inhibitory effects on renin in vitro and inhibit PRA and reduce arterial blood pressure in vivo.
|
-
- HY-14165A
-
|
(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-174127
-
|
|
P2Y Receptor
|
Neurological Disease
|
|
P2Y1 antagonist 3 (compound 36b) is a blood-brain barrier (BBB)-penetrant P2Y1 antagonist with an IC50 of 0.50 μM. P2Y1 antagonist 3 exhibits protective effects in a rat middle cerebral artery occlusion (MCAO) model and demonstrates neuroprotective activity against oxidative stress by upregulating nuclear Nrf2 protein levels .
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-
- HY-181094
-
|
|
Glycosidase
|
Metabolic Disease
|
|
α-Glucosidase-IN-110 is a selective and orally active competitive inhibitor of α-Glucosidase with an IC50 of 7.09 μM and a Ki of 6.9 μM. α-Glucosidase-IN-110 can reduce fasting blood glucose levels, improve glucose tolerance, and restore the histomorphology of liver and pancreatic tissues in diabetic rat models. α-Glucosidase-IN-110 can be used for the research of diabetes .
|
-
- HY-P2983A
-
|
|
Angiotensin-converting Enzyme (ACE)
|
Cardiovascular Disease
|
|
Angiotensin Converting Enzyme, Rat (EC 3.4.15.1) indirectly increases blood pressure by causing blood vessels to constrict. Angiotensin Converting Enzyme does that by converting angiotensin I to angiotensin II, which constricts the vessels.
|
-
- HY-181710
-
|
|
mTOR
PI3K
|
Cancer
|
|
LASSBio-2337 is a dual pan-PI3K/mTOR inhibitor with an mTOR IC50 of 5.8 μM.LASSBio-2337 functionally modulates mTOR and all PI3K isoforms.LASSBio-2337 acts as a cytotoxic agent in leukemia cells, including multidrug-resistant populations.LASSBio-2337 spares nontumor human peripheral blood mononuclear cells.LASSBio-2337 displays moderate PAMPA-GIT permeability.LASSBio-2337 shows low metabolic stability in rat liver microsomes.LASSBio-2337 is aqueous insoluble.LASSBio-2337 can be used for the research of acute lymphoblastic leukemia, chronic myelogenous leukemia, breast cancer .
|
-
- HY-181828
-
|
|
iGluR
Dopamine Receptor
|
Neurological Disease
|
|
SePP is a blood-brain barrier-permeable NMDAR antagonist and dopamine/norepinephrine reuptake inhibitor, with a Ki of 28.7 nM for rat NMDAR. SePP exerts anticonvulsant effects. SePP can be used in research related to fragile X syndrome .
|
-
- HY-183954
-
|
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
MDL-19744A is an orally active and selective α1-adrenergic receptor antagonist, with rat α1-adrenergic receptor IC50 of 8 nM. MDL-19744A increases renal blood flow, dose-related decreases mean arterial blood pressure, increases urinary sodium excretion, and mediates renal vasodilation. MDL-19744A can be used for the research of hypertension .
|
-
- HY-109012AR
-
|
JNJ-42847922 hydrochloride (Standard)
|
Reference Standards
Orexin Receptor (OX Receptor)
|
Neurological Disease
Metabolic Disease
|
|
Seltorexant hydrochloride (Standard) is the analytical standard of Seltorexant (hydrochloride) (HY-109012A). This product is intended for research and analytical applications. Seltorexant hydrochloride (JNJ-42847922 hydrochloride) is an orally active, high-affinity, and selective OX2R antagonist (pKi values of 8.0 and 8.1 for human and rat OX2R). Seltorexant hydrochloride crosses the blood-brain barrier and quickly occupies OX2R binding sites in the rat brain .
|
-
- HY-109012R
-
|
JNJ-42847922 (Standard)
|
Reference Standards
Orexin Receptor (OX Receptor)
|
Neurological Disease
Endocrinology
|
|
Seltorexant (Standard) is the analytical standard of Seltorexant (HY-109012). This product is intended for research and analytical applications. 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-108463R
-
|
|
Reference Standards
TRP Channel
|
Neurological Disease
Inflammation/Immunology
|
|
A-967079 (Standard) is the analytical standard of A-967079 (HY-108463). This product is intended for research and analytical applications. 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 blood-brain barrier .
|
-
- HY-182421
-
|
|
Kisspeptin Receptor
|
Endocrinology
Cancer
|
|
GPR54 antagonist‑1 is a GPR54 antagonist with IC50 values of 3.6 nM and 15 nM against human and rat GPR54, respectively. GPR54 antagonist‑1 shows blood‑brain barrier penetration. GPR54 antagonist‑1 blocks the function of human and rat GPR54 receptors. GPR54 antagonist‑1 suppresses plasma luteinizing hormone levels in castrated male rats. GPR54 antagonist‑1 can be used for the study of prostate cancer and endometriosis .
|
-
- HY-181635
-
|
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Azapetine is an α-adrenergic receptor antagonist, with a IC50 of 0.205 μM against rat α1-adrenergic receptors and a IC50 of 1.3 μM against rat α2-adrenergic receptors. Azapetine blocks α1/α2-adrenergic receptor-mediated contraction of blood vessels and vascular smooth muscles. Azapetine can be used for the research of peripheral vascular diseases .
|
-
- HY-106385
-
|
VRX-03011 free base
|
5-HT Receptor
|
Neurological Disease
|
|
PRX-03140 is a selective, blood-brain-barrier permeable 5-HT4 receptor agonist with a Ki value of 110 nM against rat brain 5-HT4 receptor. PRX-03140 can increase cortical ACh and histamine levels. PRX-03140 can be used in the research of Alzheimer's disease .
|
-
- HY-112481
-
|
|
|
Inflammation/Immunology
|
|
IKK2-IN-5 is a selective IKK-2 inhibitor with an IC50 of 0.025 μM. IKK2-IN-5 inhibits the production of TNF-α in LPS (HY-D1056)-stimulated human peripheral blood mononuclear cells. IKK2-IN-5 exhibits extremely low cytotoxicity against human peripheral blood mononuclear cells .
|
-
- HY-W700354
-
|
|
Calcium Channel
|
Cardiovascular Disease
Metabolic Disease
|
|
(S)-(-)-Felodipine is a S-enantiomer of Felodipine. (S)-(-)-Felodipine is an antihypertensive agent. Felodipine is a 1,4-dihydropyridine derivative and a vasoselective calcium antagonist. Felodipine can prevent the activation of the vascular effector cells and interfere with the contractile process in vitro. Felodipine lowers mean arterial blood pressure by 20% in dog model. (S)-(-)-Felodipine shows high metabolic rate in rat and dog liver microsomes .
|
-
- HY-182247
-
|
|
Serotonin Transporter
Dopamine Transporter
|
Neurological Disease
|
|
D-473 is an orally active, blood-brain barrier penetrant and serotonin-preferring reuptake inhibitor. D-473 inhibits serotonin, dopamine and norepinephrine transporters, and significantly elevates the extracellular levels of these three neurotransmitters in rat brain regions. D-473 exhibits definite antidepressant-like activity without inducing motor activation. D-473 is widely used in studies related to major depressive disorder .
|
-
- HY-W153897
-
|
|
Adrenergic Receptor
|
Inflammation/Immunology
|
|
N-Methyltyramine is an orally active α2-adrenoreceptor antagonist with an IC50 value of 5.53 μM against rat targets. N-Methyltyramine blocks α2-adrenoreceptors, while inhibiting lipolysis, hyperactivity responses and small intestinal peristalsis in mice. N-Methyltyramine promotes gastrin release and pancreatic juice secretion, upregulates appetite, blood pressure, myocardial contraction frequency and contraction intensity, and increases renal blood flow, renal vascular resistance and mean peripheral arterial resistance. N-Methyltyramine relaxes mouse small intestinal smooth muscle and undergoes biotransformation in vivo to produce adrenaline. N-Methyltyramine can be used in studies related to gastrointestinal diseases .
|
-
- HY-W153159
-
|
|
Adrenergic Receptor
|
Inflammation/Immunology
|
|
N-Methyltyramine hydrochloride is an orally active α2-adrenoreceptor antagonist with an IC50 value of 5.53 μM against rat targets. N-Methyltyramine hydrochloride blocks α2-adrenoreceptors, while inhibiting lipolysis, hyperactivity responses and small intestinal peristalsis in mice. N-Methyltyramine hydrochloride promotes gastrin release and pancreatic juice secretion, upregulates appetite, blood pressure, myocardial contraction frequency and contraction intensity, and increases renal blood flow, renal vascular resistance and mean peripheral arterial resistance. N-Methyltyramine hydrochloride relaxes mouse small intestinal smooth muscle and undergoes biotransformation in vivo to produce adrenaline. N-Methyltyramine hydrochloride can be used in studies related to gastrointestinal diseases .
|
-
- HY-P11584
-
|
|
Amylin Receptor
CGRP Receptor
|
Metabolic Disease
|
|
KBP-066A is a long-acting dual amylin and calcitonin receptor agonist. KBP-066A can activate the CTR and AMY-R potently, with no off-target activity. KBP-066A reduces fasting blood glucose levels, fasting insulin levels, and body weight in diabetic rat models. KBP-066A can be used for the research of type 2 diabetes mellitus, obesity .
|
-
- HY-15498
-
|
BMS-927711; BHV-3000
|
CGRP Receptor
|
Neurological Disease
|
|
Rimegepant (BMS-927711; BHV-3000) is an orally bioavailable and blood-brain barrier permeable antagonist of CGRP and AMY1 receptors, with a pIC50 of 8.01 and a Ki of 0.027 nM for human CGRP receptors. Rimegepant antagonizes cAMP production induced by αCGRP, βCGRP and amylin at CGRP and AMY1 receptors in humans, rats and mice, as well as at rat AMY3 receptors. Rimegepant can be used in research related to migraine .
|
-
- HY-172419
-
|
GM-1020
|
iGluR
|
Neurological Disease
|
|
Blixeprodil (GM-1020) is an orally active, blood-brain barrier-penetrant NMDA receptor inhibitor with a Ki of 3.25 µM in rat cortical tissues. Blixeprodil binds to the MK-801 ion channel site and blocks NMDA receptor-mediated currents in hyperpolarized states in a voltage-dependent manner. Blixeprodil modulates the power of cortical EEG frequency bands, alters spontaneous motor activity, and induces ataxia at high doses. Blixeprodil can be used in the research of depression .
|
-
- HY-172419A
-
|
GM-1020 hydrochloride
|
iGluR
|
Neurological Disease
|
|
Blixeprodil hydrochloride (GM-1020 hydrochloride) is an orally active, blood-brain barrier-penetrant NMDA receptor inhibitor with a Ki of 3.25 µM in rat cortical tissues. Blixeprodil hydrochloride binds to the MK-801 ion channel site and blocks NMDA receptor-mediated currents in hyperpolarized states in a voltage-dependent manner. Blixeprodil hydrochloride modulates the power of cortical EEG frequency bands, alters spontaneous motor activity, and induces ataxia at high doses. Blixeprodil hydrochloride can be used in the research of depression .
|
-
- HY-180527
-
|
|
SGLT
Dipeptidyl Peptidase
|
Metabolic Disease
|
|
SGLT2-IN-5 (Compound 99) is an orally active SGLT2 inhibitor with IC₅₀ values for SGLT2, SGLT1, and DPP4 of 0.8, 23, and 58 nM respectively. SGLT2-IN-5 controls blood sugar levels in diabetic rat models and increases the levels of active GLP-1. SGLT2-IN-5 can be used for the study of type 2 diabetes .
|
-
- HY-N6951R
-
-
- HY-136625
-
|
|
N-myristoyltransferase
|
Cardiovascular Disease
|
|
LY134046 is an inhibitor of norepinephrine N-methyltransferase (NMT) with cardiovascular activity. LY134046 causes sustained reductions in mean arterial blood pressure and heart rate, but no significant reductions in norepinephrine concentrations in the rat brain. LY134046 does not interact with adrenergic or cholinergic receptors, and its hypotensive and bradycardic effects do not require neurogenic tension. LY134046 (40 mg/kg/day) causes sustained and significant inhibition of hypothalamic and brainstem NMT activity, resulting in central norepinephrine depletion.
|
-
- HY-165600
-
|
TMB-4 dichloride
|
Cholinesterase (ChE)
|
Others
|
|
Trimedoxime dichloride (TMB-4 dichloride) is a blood-brain barrier-permeable cholinesterase reactivator . Trimedoxime dichloride reactivates cholinesterase inhibited by paraoxon, sarin, tabun and other agents, restricts the breakdown of acetylcholine and alleviates excessive cholinergic stimulation. Trimedoxime dichloride reduces mortality and prolongs survival time. Trimedoxime dichloride exhibits reactivation efficacy against AChE in rat tissues. Trimedoxime dichloride can be used in research related to organophosphate (paraoxon) poisoning and tabun poisoning .
|
-
- HY-145512
-
|
NLT
|
Dopamine Receptor
|
Neurological Disease
|
|
N-(α-Linolenoyl) tyrosine (NLT) is a dopaminergic agonist capable of crossing the blood-brain barrier. N-(α-Linolenoyl) tyrosine increases the level, turnover rate and release amount of dopamine in the striatum. N-(α-Linolenoyl) tyrosine modulates rotational behavior in a rat model with unilateral striatal injury and alleviates excessive blinking symptoms in models induced by dopamine-depleting agents. N-(α-Linolenoyl) tyrosine can be used for research on Parkinson's disease and idiopathic blepharospasm .
|
-
- HY-A0114
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RS 10029
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Angiotensin-converting Enzyme (ACE)
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Cardiovascular Disease
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Moexiprilat is an inhibitor of angiotensin-converting enzyme (ACE; IC50=2.1 nM) and an active metabolite of the prodrug Moexipril (HY-117281). It is formed from moexipril in vivo by side chain ester hydrolysis. Moexiprilat (10 nM) prevents the estrone- or angiotensin II-stimulated proliferation of primary neonatal rat cardiac fibroblasts. It reduces mean arterial blood pressure and increases the levels of atrial natriuretic peptide, a marker of hypertension, in ovariectomized mice when administered at a dose of 50 mg/kg per day.
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- HY-17444
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PPAR
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Metabolic Disease
Cancer
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Tesaglitazar is a dual-target PPARα/γ agonist with an EC50 of 13.4 μM for rat PPARα and 3.6 μM for human PPARα. Tesaglitazar affects lipid and glucose metabolism by activating PPARα and PPARγ receptors, and has the potential to improve blood sugar and relieve pain. Tesaglitazar can be used to induce in vivo tumor models and can be used in the study of type 2 diabetes, dyslipidemia, and neuropathic pain .
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- HY-180528
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SGLT
Dipeptidyl Peptidase
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Metabolic Disease
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SGLT2-IN-6 (Compound 101) is an orally active SGLT2 inhibitor with IC₅₀ values for SGLT2, SGLT1, and DPP4 of 0.8, 6.7, and 72 nM respectively. SGLT2-IN-6 controls blood sugar levels in diabetic rat models and increases the levels of active GLP-1. SGLT2-IN-6 can be used for the study of type 2 diabetes .
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- HY-N3807
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Acyltransferase
ERK
NF-κB
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Infection
Cardiovascular Disease
Cancer
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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 .
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- HY-W010520R
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Reference Standards
Bacterial
MMP
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Infection
Inflammation/Immunology
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Methylisothiazolinone (Standard) is the analytical standard of Methylisothiazolinone. Methylothiazolinone is a fungicide and preservative, as well as a sensitizer. Methylisothiazolinone can activate matrix metalloproteinases (MMPs) in human bronchial epithelial cells to induce cell apoptosis and inflammatory response. Methylisothiazolinone can promote the development of atopic dermatitis in mice by disrupting Th2/Th17 related immune responses. Methylisothiazolinone can cause mitochondrial damage in the endothelium of rat cerebral blood vessels .
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- HY-170499
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BI02982816
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mGluR
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Neurological Disease
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VU6024578 (BI02982816) is a selective, orally active positive allosteric modulator (PAM) for metabotropic glutamate receptor (mGluR1), that activates human mGluR1 and rat mGluR1 with EC50 of 54 nM and 46 nM. VU6024578 exhibits antipsychotic activity in rats amphetamine-induced hyperactivity models and MK-801 (HY-15084B)-induced novel object recognition (NOR) models. VU6024578 is blood brain barrier penetrable .
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- HY-182645
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CRFR
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Neurological Disease
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CRF1 receptor antagonist-2 is an orally active, blood-brain barrier permeable CRF1 receptor antagonist, with an IC50 of 4 nM in CHO-K1 cell membranes and an IC50 of 7 nM in rat brain cell membranes. CRF1 receptor antagonist-2 exerts anxiolytic effects in swim stress-loaded rats. CRF1 receptor antagonist-2 can be used in studies related to stress-induced anxiety .
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- HY-107732
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Neuropeptide Y Receptor
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Neurological Disease
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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 .
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- HY-160959
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nAChR
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Neurological Disease
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AN317 is a selective agonist for α6β2-containing nicotinic acetylcholine receptor (nAChR) with Ki of 6.2 nM and 4.1 nM, for α6/α3β2β3 receptor and α4β2 receptor, respectively. AN317 induces dopamine release in the synaptosomes of the rat striatum, enhances dopaminergic neuronal activity in substantia nigra, and exhibits protective efficacy to rat neurons against dopamine neurotoxin MPP +. AN317 exhibits good pharmacokinetic characteristics in rats. AN317 penetrates the blood-brain barrier (BB) .
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- HY-107915
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(-)-Cobefrin; (-)-α-Methylnoradrenaline; (-)-Nordefrin
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Adrenergic Receptor
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Cardiovascular Disease
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Levonordefrin ((-)-Cobefrin; (-)-α-Methylnoradrenaline; (-)-Nordefrin) is an α-adrenergic receptor agonist with blood pressure regulatory properties. Levonordefrin is a key metabolite responsible for the hypotensive effect of α-methyldopa. By stimulating central α-adrenergic receptors in the nucleus tractus solitarius region of the medulla oblongata, Levonordefrin induces centrally mediated hypotension and bradycardia. When administered intravenously, Levonordefrin increases mean arterial blood pressure in a dose-dependent manner. Levonordefrin is applicable for research on the pathophysiology of hypertension and drug metabolism .
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- HY-111140
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PGE synthase
Lipoxygenase
PPAR
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Inflammation/Immunology
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YS121 is a dual inhibitor of microsomal prostaglandin E2 synthase-1 (mPGES-1; IC50 = 3.4 μM) and 5-lipoxygenase (5-LOX; IC50 = 6.5 μM). YS121 exhibits direct, reversible, and specific binding to mPGES-1 (KD = 10-14 μM) . YS121 dose-dependently reduces PGE2 production with an EC50 of 12 μM in IL-1β-stimulated A549 cells . YS121 (compound 9) activates PPAR-α and -γ (EC50 = 1 and 3.6 μM, respectively) . YS121 exhibits anti-inflammatory efficiency in human whole blood as well as in vivo. YS121 can be used for pleurisy research .
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- HY-W010243S
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Isotope-Labeled Compounds
Bacterial
MMP
Apoptosis
Fungal
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Infection
Inflammation/Immunology
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Methylisothiazolinone-d3 hydrochloride is the deuterium labeled Methylisothiazolinone hydrochloride (HY-W010243). Methylisothiazolinone hydrochloride is a bacterial and fungal inhibitor and preservative, as well as a sensitizer. Methylisothiazolinone hydrochloride can activate matrix metalloproteinases (MMPs) in human bronchial epithelial cells to induce apoptosis and inflammatory response. Methylisothiazolinone hydrochloride can promote the development of atopic dermatitis in mice by disrupting Th2/Th17 related immune responses. Methylisothiazolinone hydrochloride can cause mitochondrial damage in the endothelium of rat cerebral blood vessels .
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- HY-106934AR
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BCX 34 dihydrochloride (Standard)
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Nucleoside Antimetabolite/Analog
HIV
Reference Standards
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Infection
Inflammation/Immunology
Cancer
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Peldesine (dihydrochloride) (Standard) is the analytical standard of Peldesine (dihydrochloride). This product is intended for research and analytical applications. 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 .
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- HY-101478R
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Reference Standards
mGluR
Apoptosis
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Neurological Disease
Cancer
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Fenobam (Standard) is the analytical standard of Fenobam. This product is intended for research and analytical applications. Fenobam is a selective and orally active mGluR5 antagonist (IC50=84 nM) that can penetrate the blood-brain barrier. Fenobam shows the Kd values of 54 nM and 31 nM on rat and human recombinant mGlu5 receptors, respectively. Fenobam has anxiolytic activity, inhibits self-administration behavior in mice, and induces apoptosis in cancer cells. Fenobam can be used for research on neurological diseases, cancer and drug addiction .
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- HY-173396
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VU319
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mAChR
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Neurological Disease
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VU0467319 (Compound VU319) is a highly selective and blood-brain-permeable, orally active M1 positive allosteric modulator (PAM) (EC50: 492 nM). VU0467319 is selective (EC50 > 30 μM) versus M2-5 for both human and rat. VU0467319 improves cognitive impairment in Alzheimer's disease (AD) through central M1 muscarinic receptors. VU0467319 does not induce cholinergic adverse reactions and has potential in AD research .
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- HY-15113
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Prolyl Endopeptidase (PREP)
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Neurological Disease
Cancer
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Y-29794 is a selective, orally active inhibitor for non-peptide prolyl endopeptidase (PREP), with an IC50 of 3 nM and a Ki of 0.95 nM. Y-29794 enhances the effect of thyrotropin-releasing hormone (TRH) on the release of ACh in the rat hippocampus, exhibits potential neuroprotective efficacy. Y-29794 exhibits anticancer activity through inhibition of the IRS1-AKT-mTORC1 pathway. Y-29794 penetrates the brain-blood barrier (BBB) .
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- HY-15113A
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Prolyl Endopeptidase (PREP)
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Neurological Disease
Cancer
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Y-29794 tosylate is a selective, orally active inhibitor for non-peptide prolyl endopeptidase (PREP), with an IC50 of 3 nM and a Ki of 0.95 nM. Y-29794 tosylate enhances the effect of thyrotropin-releasing hormone (TRH) on the release of ACh in the rat hippocampus, exhibits potential neuroprotective efficacy. Y-29794 tosylate exhibits anticancer activity through inhibition of the IRS1-AKT-mTORC1 pathway. Y-29794 tosylate penetrates the brain-blood barrier (BBB) .
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- HY-16276A
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LCI699 phosphate
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Mineralocorticoid Receptor
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Cardiovascular Disease
Cancer
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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) .
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- HY-16276
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LCI699
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Mineralocorticoid Receptor
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Cardiovascular Disease
Inflammation/Immunology
Cancer
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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) .
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- HY-14402
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LPL Receptor
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Infection
Inflammation/Immunology
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AMG 369 is an orally active and potent dual S1P1/S1P5 agonist with limited activity at S1P3 and no activity at S1P2/S1P4. AMG 369 reduces blood lymphocyte counts. AMG 369 delays onset and reduces severity of experimental autoimmune encephalomyelitis in rat .
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- HY-107203
-
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HWA 285
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Phosphodiesterase (PDE)
Adenosine Receptor
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Cardiovascular Disease
Neurological Disease
Cancer
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Propentofylline (HWA 285) is an orally active and brain-penetrant phosphodiesterase inhibitor. Propentofylline blocks adenosine reuptake and prevents cyclic nucleotide degradation. Propentofylline can be used for the research of primary degenerative (Alzheimer's) dementia, vascular dementia, cerebral ischemia, acute stroke, and learning and memory disorders .
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- HY-107203S
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HWA 285-d6
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Isotope-Labeled Compounds
Phosphodiesterase (PDE)
Adenosine Receptor
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Neurological Disease
Cancer
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Propentofylline-d6 (HWA 285-d6) is the deuterium labeled Propentofylline. Propentofylline is an orally active and brain-penetrant phosphodiesterase inhibitor. Propentofylline blocks adenosine reuptake and prevents cyclic nucleotide degradation. Propentofylline can be used for the research of primary degenerative (Alzheimer's) dementia, vascular dementia, cerebral ischemia, acute stroke, and learning and memory disorders .
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- HY-B0130R
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S-9490 (Standard)
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Angiotensin-converting Enzyme (ACE)
NF-κB
STAT
Sirtuin
Reference Standards
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Cardiovascular Disease
Neurological Disease
Cancer
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Perindopril (Standard) is the analytical standard of Perindopril. This product is intended for research and analytical applications. Perindopril (S-9490) is an orally available, long-acting angiotensin-converting enzyme (ACE) inhibitor. Perindopril inhibits inflammatory cell influx and intimal thickening, preserving elastin on the inside of the aorta. Perindopril effectively inhibits experimental abdominal aortic aneurysm (AAA) formation in a rat model and reduces pulmonary vasoconstriction in rats with pulmonary hypertension .
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- HY-B0130
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- HY-13414
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Remogliflozin A
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SGLT
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Metabolic Disease
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Remogliflozin (Remogliflozin A) is an orally active, highly selective sodium-glucose cotransporter 2 (SGLT2) inhibitor, with a Ki of 12.4 nM for human SGLT2 and 26.0 nM for rat SGLT2. Remogliflozin increases urinary glucose excretion by inhibiting renal glucose reabsorption. Without insulin stimulation, remogliflozin suppresses the elevation of plasma glucose, reduces fasting blood glucose and glycated hemoglobin, and improves glycosuria, hyperglycemia, hyperinsulinemia, hypertriglyceridemia and insulin resistance in diabetic rodents. Remogliflozin can be used in research related to type 2 diabetes .
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- HY-181545A
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NO Synthase
IFNAR
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Cancer
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nNOS-IN-2 trihydrochloride is a blood-brain barrier-permeable nitric oxide synthase (nNOS) inhibitor. nNOS-IN-2 trihydrochloride exhibits Ki values of 1.7 nM and 2.3 nM against human and rat nNOS, respectively, and shows high selectivity for human eNOS and iNOS. nNOS-IN-2 trihydrochloride also effectively reduces PD-L1 expression in human melanoma cells under both basal conditions and IFN-γ exposure. nNOS-IN-2 trihydrochloride can be used for the study of melanoma and related signaling pathways .
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- HY-14806S2
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- HY-114947
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9-Deoxy-9-methylene PGE2
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Prostaglandin Receptor
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Cardiovascular Disease
Metabolic Disease
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9-deoxy-9-methylene Prostaglandin E2 (9-deoxy-9-methylene PGE2) is a stable, isosteric analog of PGE2. 9-deoxy-9-methylene PGE2 retains the biological profile of PGE2 with fewer side effects. In the rat 9-deoxy-9-methylene PGE2 is equipotent to PGE2 in decreasing blood pressure. It also stimulates the gerbil colon and primate uterus at the same potency as PGE2.
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- HY-102064R
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Reference Standards
5-HT Receptor
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Neurological Disease
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SR 57227A (Standard) is the analytical standard of SR 57227A (HY-102064). This product is intended for research and analytical applications. 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 .
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- HY-168096
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NO Synthase
Apoptosis
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Cardiovascular Disease
Neurological Disease
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iNOs-IN-5 (Compound BN-4) is an inhibitor for iNOS with an IC50 of 0.1707 μM, and reduces NO levels in LPS (HT-D1056)-induced RAW264.7 cells. iNOs-IN-5 reduces the hypoxic injury stimulated ROS and lactate dehydrogenase expression, and exhibits anti-necrosis and anti-apoptosis efficacy. iNOs-IN-5 exhibits anti-cerebral ischemia and neuroprotective activities in SD rat models. iNOs-IN-5 is blood-brain barrier penetrable .
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- HY-101823A
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Abbott 81282
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Angiotensin Receptor
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Cardiovascular Disease
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A-81282 (Abbott 81282) is an antagonist of angiotensin II's AT1 receptor, with a pA2 value of 9.64 at the AT1 receptor in rabbit aorta. A-81282 also demonstrates significant inhibitory action on the binding of [125i]_Sar1_lle8_Angiotensin_ll to rat liver membranes, with a pKI value of 8.505. A-81282 has antihypertensive activity and can effectively lower blood pressure in renal artery-ligated rats .
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- HY-W153159R
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Reference Standards
Adrenergic Receptor
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Inflammation/Immunology
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N-Methyltyramine (hydrochloride) (Standard) is the analytical standard of N-Methyltyramine (hydrochloride) (HY-W153159). This product is intended for research and analytical applications. N-Methyltyramine hydrochloride is an orally active α2-adrenoreceptor antagonist with an IC50 value of 5.53 μM against rat targets. N-Methyltyramine hydrochloride blocks α2-adrenoreceptors, while inhibiting lipolysis, hyperactivity responses and small intestinal peristalsis in mice. N-Methyltyramine hydrochloride promotes gastrin release and pancreatic juice secretion, upregulates appetite, blood pressure, myocardial contraction frequency and contraction intensity, and increases renal blood flow, renal vascular resistance and mean peripheral arterial resistance. N-Methyltyramine hydrochloride relaxes mouse small intestinal smooth muscle and undergoes biotransformation in vivo to produce adrenaline. N-Methyltyramine hydrochloride can be used in studies related to gastrointestinal diseases .
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- HY-W153897R
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Reference Standards
Adrenergic Receptor
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Inflammation/Immunology
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N-Methyltyramine (Standard) is the analytical standard of N-Methyltyramine (HY-W153897). This product is intended for research and analytical applications. N-Methyltyramine is an orally active α2-adrenoreceptor antagonist with an IC50 value of 5.53 μM against rat targets. N-Methyltyramine blocks α2-adrenoreceptors, while inhibiting lipolysis, hyperactivity responses and small intestinal peristalsis in mice. N-Methyltyramine promotes gastrin release and pancreatic juice secretion, upregulates appetite, blood pressure, myocardial contraction frequency and contraction intensity, and increases renal blood flow, renal vascular resistance and mean peripheral arterial resistance. N-Methyltyramine relaxes mouse small intestinal smooth muscle and undergoes biotransformation in vivo to produce adrenaline. N-Methyltyramine can be used in studies related to gastrointestinal diseases .
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- HY-116062A
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Histone Methyltransferase
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Neurological Disease
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JNJ-7925476 is a triple reuptake inhibitor that selectively and potently inhibits the activity of the serotonin transporter (SERT), norepinephrine transporter (NET), and dopamine transporter (DAT). JNJ-7925476 is rapidly absorbed into the blood and its concentration in the brain is 7-fold higher than that in plasma. The occupancy ED(50) values of JNJ-7925476 for SERT, NET, and DAT in the rat brain are 0.18, 0.09, and 2.4 mg/kg, respectively. JNJ-7925476 rapidly induces a significant increase in the levels of extracellular serotonin, dopamine, and norepinephrine in the rat cerebral cortex in a dose-dependent manner. JNJ-7925476 exhibits potent antidepressant-like activity in the mouse tail suspension test. These results suggest that JNJ-7925476 has in vivo efficacy in biochemical and behavioral models of depression .
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- HY-15498S
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BMS-927711-d4; BHV-3000-d4
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Isotope-Labeled Compounds
CGRP Receptor
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Neurological Disease
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Rimegepant-d4 (BMS-927711-d4) is the deuterium labeled Rimegepant (HY-15498). Rimegepant (BMS-927711) is an orally bioavailable and blood-brain barrier permeable antagonist of CGRP and AMY1 receptors, with a pIC50 of 8.01 and a Ki of 0.027 nM for human CGRP receptors. Rimegepant antagonizes cAMP production induced by αCGRP, βCGRP and amylin at CGRP and AMY1 receptors in humans, rats and mice, as well as at rat AMY3 receptors. Rimegepant can be used in research related to migraine .
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- HY-W714853
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Akt
Src
STAT
EGFR
Drug Isomer
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Neurological Disease
Inflammation/Immunology
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(+)-Theta-cypermethrin is a stereoisomer of Cypermethrin (HY-B0829) that possesses blood-brain barrier penetration ability and binds to AKT1, SRC, STAT3 and EGFR with high affinity. (+)-Theta-cypermethrin reduces the amplitude of delayed rectifier potassium channel currents, shifts the steady-state activation curve to negative potentials, and shifts the steady-state inactivation curve to negative potentials at higher concentrations. (+)-Theta-cypermethrin induces abnormal electrical activity in rat hippocampal neurons. (+)-Theta-cypermethrin causes chronic respiratory system damage and exhibits neurotoxicity .
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- HY-156505A
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iGluR
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Neurological Disease
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R-(+)-EU-1180-453 is a positive allosteric modulator targeting NMDA receptors containing GluN2C and GluN2D subunits, with a pEC50 value of 5.5 for both rat receptor subtypes, and it can cross the blood-brain barrier. R-(+)-EU-1180-453 increases the potency of glutamate, enhances receptor responses to maximally effective concentrations of agonists, and acts only on receptors bound to both co-agonists. R-(+)-EU-1180-453 is applicable to research related to Alzheimer's disease, Parkinson's disease, epilepsy, and neuropathic pain .
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- HY-173221
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NF-κB
p38 MAPK
Reactive Oxygen Species (ROS)
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Neurological Disease
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MJ210 is a modulator of the NF-κB and MAPK pathways with oral activity and the ability to penetrate the blood-brain barrier, and it exhibits neuroprotective activity. In vitro, 5 μM of MJ210 can increase the survival rate of SH-SY5Y cells treated with Rotenone (HY-B1756) to 81.9% and reduce the level of ROS, etc. In vivo, 5 mg/kg of MJ210 can improve the motor impairment in a rat model of Parkinson's disease. MJ210 can be used in the research of neurological diseases, such as Parkinson's disease .
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- HY-122144
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Teroxirone
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Endogenous Metabolite
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Cancer
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α-Triglycidyl isocyanurate (Teroxirone) is an antitumor compound with activity to inhibit DNA replication. α-Triglycidyl isocyanurate exerts its anticancer effect by alkylating and cross-linking DNA. α-Triglycidyl isocyanurate is relatively stable in fresh human plasma and whole blood, showing good biocompatibility. The metabolism of α-Triglycidyl isocyanurate mainly occurs in rat liver and is metabolized through an NADPH-independent pathway. The cytotoxicity of α-Triglycidyl isocyanurate can be partially restored under specific conditions, suggesting the complexity of its metabolic pathway .
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- HY-116450
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Dopamine Receptor
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Neurological Disease
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TISCH is a potent and selective iodinated ligand with high affinity and selectivity for CNS D1 dopamine receptors. TISCH showed a Kd value of 0.205 nM in rat striatal tissue, indicating its effectiveness in biological activity. TISCH is able to easily cross the blood-brain barrier and show distribution in specific areas with D1 receptor density. TISCH is considered to be useful as a pharmacological tool for characterizing D1 dopamine receptors. When labeled with I-123, TISCH has the potential to be used as an in vivo imaging agent for CNS D1 dopamine receptors .
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- HY-P10587
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JNJ-77242113; JNJ-2113; PN-235
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Interleukin Related
STAT
IFNAR
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Inflammation/Immunology
|
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Icotrokinra (JNJ-77242113) is an orally available, selective antagonist of the IL-23 receptor. Icotrokinra inhibits IL-23-induced STAT3 phosphorylation in peripheral blood mononuclear cells (IC50=5.6 pM) and inhibits IL-23-induced interferon IFN-γ production in NK cells with an IC50 of 18.4 pM. Icotrokinra exhibits anti-inflammatory activity in a rat TNBS-induced colitis model. Icotrokinra can be used in the study of psoriasis, psoriatic arthritis, and inflammatory bowel disease .
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- HY-P10587B
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JNJ-77242113 (hydrochloride); JNJ-2113 (hydrochloride); PN-235 (hydrochloride)
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Interleukin Related
STAT
IFNAR
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Inflammation/Immunology
|
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Icotrokinra (JNJ-77242113) hydrochloride is an orally available, selective antagonist of the IL-23 receptor. Icotrokinra hydrochloride inhibits IL-23-induced STAT3 phosphorylation in peripheral blood mononuclear cells (IC50=5.6 pM) and inhibits IL-23-induced interferon IFN-γ production in NK cells with an IC50 of 18.4 pM. Icotrokinra hydrochloride exhibits anti-inflammatory activity in a rat TNBS-induced colitis model. Icotrokinra hydrochloride can be used in the study of psoriasis, psoriatic arthritis, and inflammatory bowel disease .
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- HY-181711
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NO Synthase
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Neurological Disease
Cancer
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nNOS-IN-6 is a human neuronal nitric oxide synthase (hnNOS) inhibitor with a human hnNOS Ki of 16 nM, ~1800-fold selectivity over human eNOS, ~2900-fold selectivity over human iNOS, and a rat nNOS Ki of 34 nM.nNOS-IN-6 exhibits high effective permeability in PAMPA-BBB assays, crosses the blood-brain barrier, and shows sustained systemic exposure, low clearance, and robust brain penetration in mouse in vivo pharmacokinetic studies.nNOS-IN-6 can be used for the research of neurodegenerative diseases, melanoma .
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- HY-P10587A
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JNJ-77242113 acetate; JNJ-2113 acetate; PN-235 acetate
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Interleukin Related
STAT
IFNAR
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Inflammation/Immunology
|
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Icotrokinra (JNJ-77242113) acetate is an orally available, selective antagonist of the IL-23 receptor. Icotrokinra acetate inhibits IL-23-induced STAT3 phosphorylation in peripheral blood mononuclear cells (IC50=5.6 pM) and inhibits IL-23-induced interferon IFN-γ production in NK cells with an IC50 of 18.4 pM. Icotrokinra acetate exhibits anti-inflammatory activity in a rat TNBS-induced colitis model. Icotrokinra acetate can be used in the study of psoriasis, psoriatic arthritis, and inflammatory bowel disease .
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- HY-19210
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Endothelin Receptor
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Cardiovascular Disease
|
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SB-209670 is an extremely potent and highly specific non-peptide, subnanomolar endothelin (ET) receptor antagonist. SB 209670 selectively inhibits binding of 125I-labeled ET-1 to cloned human ET receptor subtypes ETA and ETB (Ki=0.2 and 18 nM, respectively). SB 209670 produces a dose-dependent reduction in blood pressure in hypertensive rats, protects from ischemia-induced neuronal degeneration in a gerbil stroke model, and attenuates neointima formation following rat carotid artery balloon angioplasty .
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- HY-W042301
-
|
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Anion Exchangers
Carbonic Anhydrase
Endothelin Receptor
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Cardiovascular Disease
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Xipamide is an orally active carbonic anhydrase (CA) inhibitor and Na +/Cl --potassium transporter inhibitor with diuretic and antihypertensive effects. Xipamide reduces NaCl reabsorption by inhibiting the Cl -/NaCO3 - anion exchanger, and increases calcium reabsorption while promoting potassium and magnesium excretion. Xipamide is mainly cleared via the renal pathway and causes a temporary decrease in glomerular filtration rate under specific conditions. Xipamide does not affect Ca 2+ signaling induced by endothelin-1 and other factors, nor does it inhibit various ion cotransport or pump activities in red blood cells. Xipamide can be used in researches related to cardiovascular diseases, hypertension (especially with left ventricular hypertrophy), advanced renal failure, and liver cirrhosis with ascites .
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-
- HY-45509
-
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RAD150
|
Androgen Receptor
|
Neurological Disease
|
|
TLB 150 Benzoate (RAD150) is a nonsteroidal androgen receptor modulator with an IC50 value of 0.13 μM. TLB 150 Benzoate spontaneously cyclizes under physiological conditions to form RAD 179, resulting in a persistent, reversible, and slow neuronal conduction blockade. TLB 150 Benzoate can be used for research on neurological diseases .
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-
- HY-100458
-
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NO Synthase
|
Neurological Disease
|
|
SCR-4026 is a neuroprotective agent with blood-brain barrier penetration ability. SCR-4026 exerts neuroprotective effects by disrupting the interaction between neuronal nNOS and PSD9, with an IC50 of 6.3 μM. SCR-4026 alleviates N-methyl-D-aspartate (NMDA)-induced excitotoxic damage in primary cortical neurons, and also protects neurons in the oxygen-glucose deprivation (OGD) model. SCR-4026 can reduce the cerebral infarct volume in the rat middle cerebral artery occlusion (MCAO) reperfusion model. SCR-4026 can be used for the study of stroke .
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-
- HY-N0311
-
|
|
Aldose Reductase
Topoisomerase
SOD
p38 MAPK
|
Neurological Disease
Inflammation/Immunology
|
|
Emodin-8-glucoside is an anthraquinone derivative that can be isolated from Aloe vera. Emodin-8-glucoside is the inhibitor for MAPK with an inhibition constant of 430.14 pM. Emodin-8-glucoside exhibits moderate inhibitory activity against rat lens aldose reductase (ALAR) and topoisomerases II with IC50s of 14.4 μM and 66 μM. Emodin-8-glucoside exhibits antioxidant, anti-inflammatory and anti-fibrotic activities. Emodin-8-glucoside can cross the blood brain barrier .
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-
- HY-182068
-
|
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iGluR
|
Cardiovascular Disease
Neurological Disease
|
|
NFI23 is a blood-brain barrier-penetrant GluN2B-NMDAR inhibitor, with an IC50 of 1.31 μM and a Ki of 5.98 nM against GluN2B-NMDAR. NFI23 reduces NMDA-induced Ca 2+ influx and ROS production, maintains mitochondrial membrane potential, inhibits neuronal apoptosis, and restores the expression of p-ERK1/2. NFI23 exerts neuroprotective effects against NMDA-induced cytotoxicity and in the rat middle cerebral artery occlusion (MCAO) model. NFI23 can be used for the research of ischemic stroke .
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-
- HY-176793
-
|
|
JAK
|
Infection
Inflammation/Immunology
Cancer
|
|
JAK1-IN-18 (Example 2) is a selective JAK1 inhibitor with an IC50 of 0.15 nM for JAK1 over JAK2 and JAK3. JAK1-IN-18 significantly reduces inflammation in DSS (HY-116282C)-induced ulcerative colitis (UC) mouse models and DNBS(HY-W324435)-induced Crohn's disease (CD) rat models. JAK1-IN-18 can be used for autoimmune diseases (such as inflammatory bowel disease), viral infections (such as HBV infection) and cancers (such as blood cancer) research .
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-
- HY-107664A
-
|
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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 .
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-
- HY-107664
-
|
|
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 .
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-
- HY-16276R
-
|
LCI699 (Standard)
|
Mineralocorticoid Receptor
Reference Standards
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Osilodrostat (Standard) is the analytical standard of Osilodrostat. This product is intended for research and analytical applications. 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) .
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-
- HY-N3807S
-
|
|
Isotope-Labeled Compounds
Acyltransferase
ERK
NF-κB
|
Infection
|
|
Enniatin B1- 13C34 is the 13C-labeled Enniatin B1 (HY-N3807). 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-A0168S
-
|
CVT-3146-d3
|
Isotope-Labeled Compounds
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 .
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-
- HY-180406
-
|
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
NPY Y2 antagonist 2 is a modulator targeting the neuropeptide Y (NPY) receptor Y2, with pKi values of 6.8 nM and 7.2 nM in human and rat brains, respectively, and demonstrating blood-brain barrier penetration. NPY Y2 antagonist 2 shows selectivity for the Y1 and Y5 receptors. NPY Y2 antagonist 2 blocks the negative feedback regulation mediated by the NPY Y2 receptor, thereby increasing endogenous NPY release and enhancing Y1 receptor activation, resulting in the modulation of central neurotransmitter release. NPY Y2 antagonist 2 exhibits moderate in vivo clearance, high free fraction in rat brain, and a favorable brain/plasma ratio and brain exposure. NPY Y2 antagonist 2 is applicable for research in conditions such as mood disorders, anxiety induced by alcohol withdrawal, and social anxiety associated with nicotine withdrawal .
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-
- HY-181929
-
|
H018
|
JAK
|
Inflammation/Immunology
|
RAI-20 (H018) is an orally active JAK1/JAK2 dual inhibitor (IC50=15.1 and 22.7 nM). RAI-20 exhibits excellent pharmacokinetic properties, including plasma stability, systemic exposure, and a long half-life. In a collagen-induced arthritis rat model, RAI-20 shows significant anti-inflammatory and anti-arthritic activities, effectively reducing paw swelling volume and arthritis index. RAI-20 can be used for research on the pathogenesis of rheumatoid arthritis .
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-
- HY-N0729D
-
|
|
Glutathione Peroxidase
SOD
|
Cardiovascular Disease
|
|
Linoleic acid is a critical component of polyunsaturated fatty acids. Linoleic acid reduces GSH-PX and T-SOD activities. Linoleic acid functions as a structural component to maintain a certain level of membrane fluidity of the transdermal water barrier of the epidermis. Linoleic acid can cause acute oxidative damage to red blood cells, ultimately leading to partial acute anemia. Linoleic acid can be used in the research of skin diseases associated with linoleic acid deficiency .
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-
- HY-W018475
-
|
MK 462 free base
|
5-HT Receptor
|
Neurological Disease
|
|
Rizatriptan (MK 462 free base) is an orally active 5-HT1B/5-HT1D receptor agonist, with BBB permeability. Rizatriptan exerts significant anti-migraine effects by constricting intracranial and extracranial blood vessels and inhibiting neuropeptide release. Rizatriptan exhibits species- and tissue-specific metabolic characteristics; for example, it undergoes oxidative deamination mainly by MAO-A in the liver of brown rats, so co-administration with MAO-A inhibitors is prohibited. Rizatriptan may also exacerbate nitroglycerin-induced cutaneous allodynia, prolong the duration of central sensitization, and increase anxiety-like behavior and active drug-seeking behavior in mice. Rizatriptan has been widely used in studies related to migraine and medication-overuse headache .
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-
- HY-107664B
-
|
|
Neurotensin Receptor
|
Neurological Disease
|
|
SR 142948 TFA 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 TFA antagonizes NT-induced inositol monophosphate formation in HT-29 cells with an IC50 of 3.9 nM. SR 142948 TFA blocks hypothermia, analgesia and steering behavior induced by NT in vivo. SR 142948 TFA shows blood-brain permeability and can be used in study of psychiatric disorders .
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-
- HY-168366
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
R-6890 is a Brorphine-related opioid receptor antagonist that exhibits differential binding activities toward rat opioid receptors (IC50=4.6 nM (0.05 M Tris; pH 7.4) and 170 nM (0.05 M Tris+0.1 M NaCl)). R-6890 displaces bound labeled opioids from receptors, and its binding affinity is affected by environmental factors, decreasing in the presence of NaCl. R-6890 crosses the blood-brain barrier (BBB) and exerts analgesic effects in the warm water-induced tail-flick reflex model of male Wistar rats .
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-
- HY-144790
-
|
|
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 .
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-
- HY-181884
-
|
|
|
Inflammation/Immunology
|
|
TLR9-IN-3 is a TLR9 antagonist with an IC50 of 0.4 μM. TLR9-IN-3 shows selectivity for TLR4 and TLR8, and inhibits CD69 activation in human whole blood with a corresponding IC50 of 1.1 μM. TLR9-IN-3 can be used in research related to pulmonary fibrosis .
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-
- HY-161104
-
|
|
Potassium Channel
Apoptosis
|
Cardiovascular Disease
Neurological Disease
|
|
Kv2.1-IN-1 is an orally active and blood-brain barrier penetrant Kv2.1 inhibitor with an IC50 of 0.07 μM. Kv2.1-IN-1 exhibits a selectivity >130 fold over other K +, Na +, and Ca 2+ ion channels. Kv2.1-IN-1 decreases the apoptosis of HEK293 cells induced by H2O2. Kv2.1-IN-1 produces significant neuroprotection efficacy in middle cerebral artery occlusion (MCAO) rat. Kv2.1-IN-1 can be used for the study of ischemic stroke .
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-
- HY-B0742
-
|
17α-Hydroxyprogesterone hexanoate; 17α-Hydroxyprogesterone caproate
|
Progesterone Receptor
|
Endocrinology
|
|
Hydroxyprogesterone caproate (17α-Hydroxyprogesterone hexanoate; 17α-Hydroxyprogesterone caproate) is a progesterone receptor (progesterone receptor) ligand and steroid hormone transcription inhibitor. Hydroxyprogesterone caproate downregulates estrogen receptors in target tissues and activates their metabolic pathways, and exhibits equivalent affinity for progesterone receptor A and progesterone receptor B. Hydroxyprogesterone caproate shows no consistent teratogenicity or developmental toxicity in rat, mouse and monkey models, but induces resorption or abortion in rhesus monkeys at human-equivalent doses. Hydroxyprogesterone caproate promotes the production of TNF-α in lipopolysaccharide-stimulated whole blood from non-pregnant women. Hydroxyprogesterone caproate can be used in scientific research related to preterm birth .
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-
- HY-182300
-
|
|
Dipeptidyl Peptidase
GLP Receptor
|
Metabolic Disease
|
|
FE 999011 is an orally active dipeptidyl peptidase IV (DPP-IV) inhibitor with IC50 values of 7 nM and 3 nM against human and rat sources, respectively. FE 999011 acts as a glucose tolerance-improving agent and a GLP-1 receptor activator, which reduces blood glucose fluctuation, promotes GLP-1 release and decreases the insulin-glucose ratio. FE 999011 regulates lipid metabolism, delays the onset of diabetes, stabilizes food and water intake, reduces hypertriglyceridemia, prevents the elevation of free fatty acids, and delays the progression of impaired glucose tolerance to disease. FE 999011 can be used in relevant studies of type 2 diabetes .
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-
- HY-162677
-
|
|
Adrenergic Receptor
5-HT Receptor
|
Cardiovascular Disease
|
|
MT-1207 is an orally active and selective adrenergic α1 and 5-HT2A receptor antagonist. MT-1207 shows IC50<0.1 nM, 0.15 nM, 1.40 nM and 0.27 nM for α1A, α1B, α1D and 5-HT2A, respectively. MT-1207 achieves an effective blood pressure (BP) reduction in the 2K2C rat model without damaging renal function. MT-1207 is a potent multitarget inhibitor with the potential for vasodilatation research .
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- HY-123189
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
LY 171859 is a D2 receptor agonist with significant reductase activity. LY 171859 exhibits enzymatic activity in the cytoplasm of liver, lung, and kidney, and also contains significant reductase activity in rat and human blood. LY 171859 has higher hepatic reductase activity in guinea pigs, followed by hamsters, rabbits, rats, and mice. The substrate of LY 171859 shows an apparent Km of 5.6 μM. The reduction reaction of LY 171859 is NADPH-dependent with an apparent Km of 14.8 μM. Only the A-side hydrogen of NADPH is incorporated in the reduction product of LY 171859. The reaction of LY 171859 is inhibited by cyanide and thiol reagents, and phenobarbital does not induce its activity in rats .
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- HY-116673
-
|
|
Histone Acetyltransferase
|
Neurological Disease
|
|
TTK21 is an activator of the histone acetyltransferases CBP/p300. TTK21 passes the blood–brain barrier, induces no toxicity, and reaches different parts of the brain when conjugated to glucose-based carbon nanosphere (CSP). TTK21 has beneficial implications for the brain functions of neurogenesis and long-term memory .CSP-TTK21 can ameliorate Aβ-impaired long-term potentiation (LTP). CSP-TTK21 may enhance the transcription of genes that promote synaptic health and cognitive function . CSP-TTK21 is orally effective and leads to improvements in motor functions, histone acetylation dynamics in a spinal injury rat model .
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-
- HY-B0596
-
|
TA-0910
|
Thyroid Hormone Receptor
Apoptosis
|
Neurological Disease
Endocrinology
|
|
Taltirelin (TA-0910) is an orally effective analogue of thyrotropin releasing hormone (TRH) and a TRH receptor (TRH-R) superagonist (IC50 at 910 nM). Taltirelin can cross the blood-brain barrier. Taltirelin stimulates an increase in cytosolic Ca 2+ concentration (Ca 2+ release) with an EC50 value of 36 nM. Taltirelin increases cell viability and reduces apoptosis in SH-SY5Y cells and primary rat mesencephalic neurons treated with MPP+ (HY-W008719) or Rotenone (HY-B1756). Taltirelin has neuroprotective effects in both cellular and animal models of Parkinson's disease. Taltirelin alleviates fatigue-like behavior in mouse models of cancer-related fatigue .
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-
- HY-107664R
-
|
|
Reference Standards
Neurotensin Receptor
|
Neurological Disease
|
|
SR 142948 (Standard) is the analytical standard of SR 142948 (HY-107664). This product is intended for research and analytical applications. 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-N0311R
-
|
|
Reference Standards
Aldose Reductase
Topoisomerase
SOD
p38 MAPK
|
Neurological Disease
Inflammation/Immunology
|
|
Emodin-8-glucoside (Standard) is the analytical standard of Emodin-8-glucoside. This product is intended for research and analytical applications. Emodin-8-glucoside is an anthraquinone derivative that can be isolated from Aloe vera. Emodin-8-glucoside is the inhibitor for MAPK with an inhibition constant of 430.14 pM. Emodin-8-glucoside exhibits moderate inhibitory activity against rat lens aldose reductase (ALAR) and topoisomerases II with IC50s of 14.4 μM and 66 μM. Emodin-8-glucoside exhibits antioxidant, anti-inflammatory and anti-fibrotic activities. Emodin-8-glucoside can cross the blood brain barrier .
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-
- HY-19888
-
|
|
P2X Receptor
Interleukin Related
|
Neurological Disease
Inflammation/Immunology
|
|
GSK-1482160 is an orally active and blood-brain barrier penetrant P2X7 receptor (P2X7R) negative allosteric modulator with pIC50s of 8.5 (human) and 6.5 (rat). GSK-1482160 reduces the efficacy of ATP at the P2X7 receptor without affecting its affinity, thereby inhibiting the release of IL-1β. GSK-1482160 is an effective radioligand and can be labeled with radioactive isotopes like 11C or 18F to image P2X7R. GSK-1482160 can be used for the studies of chronic joint pain and chronic constriction injury (CCI) .
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-
- HY-59201
-
|
|
nAChR
5-HT Receptor
ERK
Epigenetic Reader Domain
|
Neurological Disease
|
|
A-582941 is a selective, orally active, blood-brain barrier-permeable α7 nAChR agonist, with Ki values of 10.8 nM and 17 nM in rat brain and human frontal cortex, respectively. A-582941 exhibits agonistic activity at 5-HT3 receptors, with a Ki of 150 nM. A-582941 triggers phosphorylation of ERK1/2 and CREB, inhibits GSK-3β via Ser-9 phosphorylation, increases acetylcholine release, induces the expression of Arc and c-Fos, activates brain regions associated with working memory and attention, and reduces cell death caused by nerve growth factor (NGF) deprivation. A-582941 is applicable for the research of Alzheimer's disease and schizophrenia .
|
-
- HY-59201A
-
|
|
ERK
5-HT Receptor
Epigenetic Reader Domain
nAChR
|
Neurological Disease
Metabolic Disease
|
|
A-582941 dihydrochloride is a selective, orally active, blood-brain barrier-permeable α7 nAChR agonist, with Ki values of 10.8 nM and 17 nM in rat brain and human frontal cortex, respectively. A-582941 dihydrochloride exhibits agonistic activity at 5-HT3 receptors, with a Ki of 150 nM. A-582941 dihydrochloride triggers phosphorylation of ERK1/2 and CREB, inhibits GSK-3β via Ser-9 phosphorylation, increases acetylcholine release, induces the expression of Arc and c-Fos, activates brain regions associated with working memory and attention, and reduces cell death caused by nerve growth factor (NGF) deprivation. A-582941 dihydrochloride is applicable for the research of Alzheimer's disease and schizophrenia .
|
-
- HY-180824
-
|
|
p38 MAPK
|
Neurological Disease
|
|
P38-α MAPK-IN-11 (Compound 4C) is a selective inhibitor of P38α MAPK that can cross the blood-brain barrier with an IC50 value of 43 nM. P38-α MAPK-IN-11 has extremely low inhibitory activity against other MAPK subtypes, namely p38β, p38γ, and p38δ, with IC50 values of > 100 nM, > 100 nM, and 48.6 mM respectively. P38-α MAPK-IN-11 exhibits outstanding neuroprotective effects and anti-neuroinflammatory effects in Alzheimer's disease-like rat models. P38-α MAPK-IN-11 can be used for the study of Alzheimer's disease .
|
-
- HY-175824
-
|
|
iGluR
NO Synthase
Apoptosis
Reactive Oxygen Species (ROS)
|
Neurological Disease
|
|
PSD-95/nNOS PPI-IN-1 is a inhibitor targeting the PSD-95/nNOS interaction with potential blood-brain barrier penetration. PSD-95/nNOS PPI-IN-1 binds to the PSD-95 PDZ2 domain with high affinity (Ki = 19.45 μM). PSD-95/nNOS PPI-IN-1 inhibits glutamate-induced excitotoxicity by reducing intracellular ROS levels and inhibiting apoptosis. PSD-95/nNOS PPI-IN-1 significantly reduces cerebral infarct volume in rat tMCAO models. PSD-95/nNOS PPI-IN-1 can be used for the study of acute ischemic stroke .
|
-
- HY-168906
-
|
|
Bradykinin Receptor
PI3K
Akt
TNF Receptor
ERK
|
Neurological Disease
Inflammation/Immunology
|
|
BI-113823 is an orally active, blood-brain barrier-permeable bradykinin B1 receptor antagonist, with a Ki value of 5.3 nM for human receptors and 13.3 nM for rat receptors. BI-113823 reduces inflammation-induced mechanical hyperalgesia, as well as the mechanical sensitivity of peripheral afferent nerves and spinal nociceptive-specific neurons. BI-113823 alleviates liver fibrosis and portal hypertension, and improves survival in chronic liver disease models. BI-113823 inhibits the activities of monocytes, neutrophils and hepatic stellate cells, as well as the PI3K/Akt signaling pathway. BI-113823 can be used in research related to inflammatory pain, liver fibrosis and portal hypertension .
|
-
- HY-136903
-
|
|
Calcium Channel
Proteasome
Reactive Oxygen Species (ROS)
|
Cardiovascular Disease
Neurological Disease
Inflammation/Immunology
|
|
SNJ-1945 is an orally active Calpain inhibitor that can cross the blood-brain barrier. SNJ-1945 protects rat hearts against cardiac arrest-reperfusion injury by inhibiting the hydrolysis of α-fodrin. SNJ-1945 inhibits VEGF-induced angiogenesis in retinal endothelial cells. SNJ-1945 also protects SH-SY5Y cells from damage induced by MPP+ (HY-W008719) and Rotenone (HY-B1756). SNJ-1945 exhibits anti-inflammatory and neuroprotective activities in a mouse model of multiple sclerosis. SNJ-1945 can be used for the research of cardiovascular, nervous system and inflammatory diseases .
|
-
- HY-181646
-
|
|
Phosphodiesterase (PDE)
TNF Receptor
|
Inflammation/Immunology
|
|
PDE4-IN-34 is a phosphodiesterase 4 (PDE4) inhibitor, with IC50 values of 19 pM and 14 pM against PDE4B1 and PDE4D2, respectively. PDE4-IN-34 shows weak inhibitory activity against PDE8A1, with an IC50 value of 4.092 μM, and exhibits significant selectivity over other subtypes (IC50 > 10 μM). PDE4-IN-34 improves pulmonary function, reduces inflammatory responses and alleviates lung tissue damage in a rat model induced by cigarette smoke combined with LPS (HY-D1056). PDE4-IN-34 can be used for research related to chronic obstructive pulmonary disease .
|
-
- HY-183925
-
|
|
HIV
Dihydroorotate Dehydrogenase
|
Infection
|
|
Redoxal is a dihydroorotate dehydrogenase (DHODH) inhibitor and anti-HIV-1 agent. Redoxal induces intracellular pyrimidine depletion by inhibiting the de novo pyrimidine biosynthesis pathway, enhances the protein stability of APOBEC3G (A3G), upregulates the abundance of A3G protein in cells and progeny viral particles, thereby strengthening the host endogenous antiviral restriction mediated by A3G . Redoxal selectively targets DHOdehase at the mitochondrial level, with an IC50 of 430 nM for inhibiting DHO oxidation in human mitochondria and an IC50 of 910 nM in rat mitochondria . Redoxal can be used in studies related to HIV-1 infection .
|
-
- HY-B0742R
-
|
17α-Hydroxyprogesterone hexanoate(Standard); 17α-Hydroxyprogesterone caproate (Standard)
|
Reference Standards
Progesterone Receptor
|
Others
|
|
Hydroxyprogesterone caproate (Standard) is the analytical standard of Hydroxyprogesterone caproate. This product is intended for research and analytical applications. Hydroxyprogesterone caproate (17α-Hydroxyprogesterone hexanoate; 17α-Hydroxyprogesterone caproate) is a progesterone receptor (progesterone receptor) ligand and steroid hormone transcription inhibitor. Hydroxyprogesterone caproate downregulates estrogen receptors in target tissues and activates their metabolic pathways, and exhibits equivalent affinity for progesterone receptor A and progesterone receptor B. Hydroxyprogesterone caproate shows no consistent teratogenicity or developmental toxicity in rat, mouse and monkey models, but induces resorption or abortion in rhesus monkeys at human-equivalent doses. Hydroxyprogesterone caproate promotes the production of TNF-α in lipopolysaccharide-stimulated whole blood from non-pregnant women. Hydroxyprogesterone caproate can be used in scientific research related to preterm birth .
|
-
- HY-186105A
-
|
|
Opioid Receptor
Apoptosis
|
Neurological Disease
|
|
(-)-P7C3-S243 is an orally active, blood-brain barrier permeable neuroprotective agent. (-)-P7C3-S243 binds to μ-opioid Receptor and TSPO. (-)-P7C3-S243 inhibits the premature apoptosis death of newborn hippocampal neurons, protects mature nigral dopaminergic neurons, promotes neuronal survival and prevents cognitive impairment. (-)-P7C3-S243 ameliorates depression-like behaviors in rat models. (-)-P7C3-S243 is applicable to research related to Parkinson's disease and Alzheimer's disease .
|
-
- HY-B0596A
-
|
TA-0910 acetate
|
Thyroid Hormone Receptor
Apoptosis
|
Neurological Disease
Endocrinology
|
|
Taltirelin acetate (TA-0910) is an acetate form of Taltirelin (TA-0910). Taltirelin (TA-0910) is an orally effective analogue of thyrotropin releasing hormone (TRH) and a TRH receptor (TRH-R) superagonist (IC50 at 910 nM). Taltirelin can cross the blood-brain barrier. Taltirelin stimulates an increase in cytosolic Ca 2+ concentration (Ca 2+ release) with an EC50 value of 36 nM. Taltirelin increases cell viability and reduces apoptosis in SH-SY5Y cells and primary rat mesencephalic neurons treated with MPP+ (HY-W008719) or Rotenone (HY-B1756). Taltirelin has neuroprotective effects in both cellular and animal models of Parkinson's disease. Taltirelin alleviates fatigue-like behavior in mouse models of cancer-related fatigue .
|
-
- HY-123382
-
|
|
Drug Isomer
|
Neurological Disease
Inflammation/Immunology
|
|
GSK-1482160 isomer is the isomer of GSK-1482160 (HY-19888). GSK-1482160 is an orally active and blood-brain barrier penetrant P2X7 receptor (P2X7R) negative allosteric modulator with pIC50s of 8.5 (human) and 6.5 (rat). GSK-1482160 reduces the efficacy of ATP at the P2X7 receptor without affecting its affinity, thereby inhibiting the release of IL-1β. GSK-1482160 is an effective radioligand and can be labeled with radioactive isotopes like 11C or 18F to image P2X7R. GSK-1482160 can be used for the studies of chronic joint pain and chronic constriction injury (CCI).
|
-
- HY-183997
-
|
|
E1/E2/E3 Enzyme
Interleukin Related
|
Cancer
|
|
Cbl-b-IN-33 is an orally active, selective inhibitor of Casitas B-lineage lymphoma-b (Cbl-b) with an IC50 of 7 nM and a Kd of 1.2 nM. Cbl-b-IN-33 inhibits non-phosphorylated E3 ubiquitin ligase Cbl-b, induces IL-2 activation in peripheral blood mononuclear cells, and exerts tumor growth inhibitory effects in a mouse colon cancer model. Cbl-b-IN-33 can be used for the research of colon cancer .
|
-
- HY-B1829
-
|
Dexamethasone 21-phosphate
|
Glucocorticoid Receptor
TGF-β Receptor
Interleukin Related
|
Neurological Disease
Inflammation/Immunology
|
|
Dexamethasone phosphate (Dexamethasone 21-phosphate) is a prodrug form of the glucocorticoid Dexamethasone (HY-14648). Dexamethasone phosphate is prepared by introducing a phosphate ester group to the hydroxyl group at position 21 of the Dexamethasone molecule. Dexamethasone phosphate inhibits LPS (HY-D1056)-induced degradation of IRAK-1 and IRAK-4, and blocks LPS-induced activation of TRAF6, p-TAK1 and p-JNK. Dexamethasone phosphate inhibits the secretion of RANTES, TGF-β1 and NO, promotes the production of MIP-1α and IL-10, and blocks microglial migration. Dexamethasone phosphate is almost completely converted to Dexamethasone in rat blood, and supports transdermal delivery via iontophoresis. Dexamethasone phosphate can be used in research related to steroid-dependent ulcerative colitis, chemotherapy-induced vomiting, allergic asthma and acute colitis (inflammatory bowel disease) .
|
-
- HY-147294
-
|
ACT-539313
|
Orexin Receptor (OX Receptor)
Cytochrome P450
|
Neurological Disease
|
|
Nivasorexant (ACT-539313) is an orally active, blood-brain barrier penetrant, selective orexin OX1R inhibitor. Nivasorexant specifically blocks central OX1Rs without affecting OX2Rs, and exhibits competitive inhibitory activity against CYP2C8, CYP2C9, CYP2C19 and CYP3A4 (IC50 values are 25 μM, 8.6 μM, 1.6 μM, 19 μM/44 μM, respectively). Nivasorexant significantly reduces binge-like eating behavior of highly palatable food in rat models and has long-acting properties. Nivasorexant shows no relevant off-target activity against over 130 selected proteins, exhibits favorable safety profiles, and can be used for studies related to binge eating disorder .
|
-
- HY-B0742S1
-
|
17α-Hydroxyprogesterone hexanoate-d8; 17α-Hydroxyprogesterone caproate-d8
|
Isotope-Labeled Compounds
Progesterone Receptor
|
Others
|
|
Hydroxyprogesterone caproate-d8 (17α-Hydroxyprogesterone hexanoate-d8) is the deuterium labeled Hydroxyprogesterone caproate (HY-B0742). Hydroxyprogesterone caproate (17α-Hydroxyprogesterone hexanoate; 17α-Hydroxyprogesterone caproate) is a progesterone receptor (progesterone receptor) ligand and steroid hormone transcription inhibitor. Hydroxyprogesterone caproate downregulates estrogen receptors in target tissues and activates their metabolic pathways, and exhibits equivalent affinity for progesterone receptor A and progesterone receptor B. Hydroxyprogesterone caproate shows no consistent teratogenicity or developmental toxicity in rat, mouse and monkey models, but induces resorption or abortion in rhesus monkeys at human-equivalent doses. Hydroxyprogesterone caproate promotes the production of TNF-α in lipopolysaccharide-stimulated whole blood from non-pregnant women. Hydroxyprogesterone caproate can be used in scientific research related to preterm birth .
|
-
- HY-124529
-
|
|
11β-HSD
Endogenous Metabolite
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Lunularin is an inhibitor of 11β-hydroxysteroid dehydrogenase 1, with an IC50 of 45.44 μM and a Ki of 35.8 μM against human 11β-HSD1, and an IC50 of 17.39 μM and a Ki of 10.31 μM against rat 11β-HSD1. Lunularin upregulates the transcription levels of Sirt1 and Hmox1 genes in the liver. Lunularin reduces food intake and body weight gain, and decreases blood glucose levels in mice fed a high-fat diet. Lunularin inhibits LPS-induced TLR4-mediated NF-κB pathway activation and nitric oxide production. Lunularin inhibits the proliferation and colony formation of renal cancer and colon cancer cells, and exhibits cancer cell-specific cytotoxicity. Lunularin binds to the steroid-binding site of human 11β-HSD1 and the steroid/NADPH-binding region of rat 11β-HSD1, but does not inhibit 11β-HSD2 or mouse 11β-HSD1. Lunularin can be used in research related to diet-induced obesity, renal cancer, colorectal cancer, inflammatory diseases and metabolic syndrome .
|
-
- HY-B1829A
-
|
Dexamethasone 21-phosphate disodium
|
Glucocorticoid Receptor
TGF-β Receptor
Interleukin Related
|
Neurological Disease
Inflammation/Immunology
|
|
Dexamethasone phosphate (Dexamethasone 21-phosphate) disodium is a prodrug form of the glucocorticoid Dexamethasone (HY-14648). Dexamethasone phosphate disodium is produced by introducing a phosphate ester group at the 21-position of the Dexamethasone molecule, forming a salt with sodium ions, thereby significantly improving water solubility. Dexamethasone phosphate disodium inhibits LPS (HY-D1056)-induced degradation of IRAK-1 and IRAK-4, and blocks LPS-induced activation of TRAF6, p-TAK1 and p-JNK. Dexamethasone phosphate disodium inhibits the secretion of RANTES, TGF-β1 and NO, promotes the production of MIP-1α and IL-10, and blocks microglial migration. Dexamethasone phosphate disodium is almost completely converted to Dexamethasone in rat blood, and supports transdermal delivery via iontophoresis. Dexamethasone phosphate disodium can be used in research related to steroid-dependent ulcerative colitis, chemotherapy-induced vomiting, allergic asthma and acute colitis (inflammatory bowel disease) .
|
-
- HY-B1829R
-
|
Dexamethasone 21-phosphate (Standard)
|
Glucocorticoid Receptor
Reference Standards
TGF-β Receptor
Interleukin Related
|
Neurological Disease
Inflammation/Immunology
|
|
Dexamethasone phosphate (Standard) (Dexamethasone 21-phosphate (Standard)) is the analytical standard of Dexamethasone phosphate (HY-B1829). This product is intended for research and analytical applications. Dexamethasone phosphate (Dexamethasone 21-phosphate) is a prodrug form of the glucocorticoid Dexamethasone (HY-14648). Dexamethasone phosphate is prepared by introducing a phosphate ester group to the hydroxyl group at position 21 of the Dexamethasone molecule. Dexamethasone phosphate inhibits LPS (HY-D1056)-induced degradation of IRAK-1 and IRAK-4, and blocks LPS-induced activation of TRAF6, p-TAK1 and p-JNK. Dexamethasone phosphate inhibits the secretion of RANTES, TGF-β1 and NO, promotes the production of MIP-1α and IL-10, and blocks microglial migration. Dexamethasone phosphate is almost completely converted to Dexamethasone in rat blood, and supports transdermal delivery via iontophoresis. Dexamethasone phosphate can be used in research related to steroid-dependent ulcerative colitis, chemotherapy-induced vomiting, allergic asthma and acute colitis (inflammatory bowel disease).
|
-
- HY-B1829AR
-
|
Dexamethasone 21-phosphate disodium (Standard)
|
Glucocorticoid Receptor
Reference Standards
Interleukin Related
TGF-β Receptor
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
|
|
Dexamethasone phosphate (Dexamethasone 21-phosphate) disodium (Standard) is the analytical standard of Dexamethasone phosphate disodium (HY-B1829A). This product is intended for research and analytical applications. Dexamethasone phosphate (Dexamethasone 21-phosphate) disodium is a prodrug form of the glucocorticoid Dexamethasone (HY-14648). Dexamethasone phosphate disodium is produced by introducing a phosphate ester group at the 21-position of the Dexamethasone molecule, forming a salt with sodium ions, thereby significantly improving water solubility. Dexamethasone phosphate disodium inhibits LPS (HY-D1056)-induced degradation of IRAK-1 and IRAK-4, and blocks LPS-induced activation of TRAF6, p-TAK1 and p-JNK. Dexamethasone phosphate disodium inhibits the secretion of RANTES, TGF-β1 and NO, promotes the production of MIP-1α and IL-10, and blocks microglial migration. Dexamethasone phosphate disodium is almost completely converted to Dexamethasone in rat blood, and supports transdermal delivery via iontophoresis. Dexamethasone phosphate disodium can be used in research related to steroid-dependent ulcerative colitis, chemotherapy-induced vomiting, allergic asthma and acute colitis (inflammatory bowel disease).
|
-
- HY-118156
-
|
|
Others
|
Others
|
|
L-699333 is a 5-lipoxygenase (5-LO) inhibitor belonging to the thieno[2,3,4-cd]indole class. This compound has a 2-ethoxybutyric acid side chain and is a potent inhibitor of the biosynthesis of 5-HPETE and LTB4 produced from human 5-LO, with ICm values of 22 nM, 7 nM, and 3.8 pM for human neutrophils and whole blood, respectively. L-699333 has shown anti-inflammatory and antiasthmatic effects in a variety of animal models, including rat pleurisy models, antigen-induced wheezing models, and awake macaque and sheep asthma models. Its inhibition of 5-LO is highly selective, with higher ICm values or stronger competitive inhibition in FLAP binding assays compared to inhibition of human 15-LO, porcine 12-LO, and ram epididymal cyclooxygenase. The racemic enantiomer 14g of L-699333 is the most potent enantiomer to date, with inhibitory effects similar to those of the known MK-0591, which has been shown in clinical trials to inhibit the biochemical effects of LTB4 biosynthesis in vitro and LTE4 excretion in urine.
|
-
- HY-186072
-
|
|
NOD-like Receptor (NLR)
Interleukin Related
Cytochrome P450
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
|
|
NT-0527 is a selective, orally active, and brain-permeable NLRP3 inflammasome inhibitor. NT-0527 can specifically block the formation of the NLRP3 inflammasome, resulting in the reduction in the maturation and release of IL-1β, exhibit inhibition on CYP2C19. NT-0527 displays anti-inflammatory activity in the mouse LPS (HY-D1056) /ATP (HY-B2176)-induced peritonitis model. NT-0527 can be used for the research of neuroinflammatory disorders (Parkinson's disease, Alzheimer's disease, amyotrophic lateral sclerosis) and peripheral inflammatory disorders (type II diabetes, atherosclerosis, gout, etc.) associated with NLRP3 inflammasome .
|
-
| Cat. No. |
Product Name |
Type |
-
- HY-N0729D
-
|
|
Biochemical Assay Reagents
|
|
Linoleic acid is a critical component of polyunsaturated fatty acids. Linoleic acid reduces GSH-PX and T-SOD activities. Linoleic acid functions as a structural component to maintain a certain level of membrane fluidity of the transdermal water barrier of the epidermis. Linoleic acid can cause acute oxidative damage to red blood cells, ultimately leading to partial acute anemia. Linoleic acid can be used in the research of skin diseases associated with linoleic acid deficiency .
|
-
- HY-W039898
-
|
1,2,3,4,6-Penta-O-acetyl-α-D-mannopyranose
|
Biochemical Assay Reagents
|
|
α-D-Mannose pentaacetate (1,2,3,4,6-Penta-O-acetyl-α-D-mannopyranose) acts as a lactate promoter. It increases lactate production in rat red blood cells .
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P0203
-
|
CGRP (83-119), mouse, rat
|
CGRP Receptor
|
Cardiovascular Disease
Metabolic Disease
Inflammation/Immunology
|
|
α-CGRP (mouse, rat), a neuropeptide (calcitonin gene-related peptide (CGRP)) mainly expressed in neuromuscular junction, is a potent vasodilator. α-CGRP (mouse, 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 (mouse, rat) has the potential in cardiovascular, pro-inflammatory, migraine and metabolic studies .
|
-
- HY-P10587
-
|
JNJ-77242113; JNJ-2113; PN-235
|
Interleukin Related
STAT
IFNAR
|
Inflammation/Immunology
|
|
Icotrokinra (JNJ-77242113) is an orally available, selective antagonist of the IL-23 receptor. Icotrokinra inhibits IL-23-induced STAT3 phosphorylation in peripheral blood mononuclear cells (IC50=5.6 pM) and inhibits IL-23-induced interferon IFN-γ production in NK cells with an IC50 of 18.4 pM. Icotrokinra exhibits anti-inflammatory activity in a rat TNBS-induced colitis model. Icotrokinra can be used in the study of psoriasis, psoriatic arthritis, and inflammatory bowel disease .
|
-
- HY-12378
-
BQ-123
3 Publications Verification
|
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-106224B
-
|
Hypocretin-1 (human, rat, mouse) acetate
|
Orexin Receptor (OX Receptor)
|
Neurological Disease
|
|
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 binds and activates two types of G protein-coupled receptors, the orexin-1 receptor (OX1R) and the orexin-2 receptor (OX2R). Orexin A (human, rat, mouse) acetate can be used in studies of appetite regulation, neurodegenerative diseases and modulation of injurious messaging .
|
-
- HY-148195
-
|
NNZ-2591
|
Biochemical Assay Reagents
|
Neurological Disease
|
|
Ercanetide (NNZ 2591) is a synthetic analogue of a small peptide of cyclic glycine proline (cGP). Ercanetide shows orally active and cross the blood-brain barrier. Ercanetide shows neuroprotective after ischemic brain injury. NNZ 2591 improves motor function in a rat model of Parkinson's disease. Ercanetide has the potential for the research of ischemic brain injury and angelman syndrome .
|
-
- HY-122542B
-
|
|
Ligands for E3 Ligase
Molecular Glues
IKZF Family
|
Cardiovascular Disease
|
|
PPACK TFA is an orally active, selective molecular glue degrader targeting IKZF2. Through a molecular glue mechanism, PPACK TFA binds to CRBN, recruits IKZF2 to form a ternary complex, and promotes its ubiquitination and proteasomal degradation. This further converts inhibitory regulatory T cells (Treg) into effector-like T cells, enhances CD8 + T cell responses, and modulates the Teff:Treg balance. PPACK TFA also increases the production of the inflammatory cytokine IL-2 and reduces the suppressive activity of Treg. PPACK TFA can be used in cancer immunotherapy research, and exhibits a synergistic effect when combined with immune checkpoint inhibitors such as anti-PD1 .
|
-
- HY-P0203A
-
|
CGRP (83-119), mouse, rat TFA
|
CGRP Receptor
|
Cardiovascular Disease
Metabolic Disease
Inflammation/Immunology
|
|
α-CGRP (mouse, rat) TFA, a neuropeptide (calcitonin gene-related peptide (CGRP)) mainly expressed in neuromuscular junction, is a potent vasodilator. α-CGRP (mouse, 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 (mouse, rat) TFA has the potential in cardiovascular, pro-inflammatory, migraine and metabolic studies .
|
-
- HY-145512
-
|
NLT
|
Dopamine Receptor
|
Neurological Disease
|
|
N-(α-Linolenoyl) tyrosine (NLT) is a dopaminergic agonist capable of crossing the blood-brain barrier. N-(α-Linolenoyl) tyrosine increases the level, turnover rate and release amount of dopamine in the striatum. N-(α-Linolenoyl) tyrosine modulates rotational behavior in a rat model with unilateral striatal injury and alleviates excessive blinking symptoms in models induced by dopamine-depleting agents. N-(α-Linolenoyl) tyrosine can be used for research on Parkinson's disease and idiopathic blepharospasm .
|
-
- HY-137874
-
|
|
Peptides
|
Metabolic Disease
Cancer
|
|
L-Glutamic γ-monohydroxamate is an antitumor agent, inhibits cell proliferation. L-Glutamic γ-monohydroxamate selectively inhibits the uptake of L-histidine into microvascular endothelial cell. L-Glutamic γ-monohydroxamate, as a vanadium ligand, activates glucose uptake and metabolism, thus decreases the blood glucose levels in vivo .
|
-
- HY-P1323A
-
|
|
Neuropeptide Y Receptor
|
Cardiovascular Disease
Neurological Disease
|
|
[Leu31,Pro34]-Neuropeptide Y(human,rat) TFA is a specific neuropeptide Y Y1 receptor agonist. [Leu31,Pro34]-Neuropeptide Y(human,rat) TFA slao activates Y4, Y5. [Leu31,Pro34]-Neuropeptide Y(human,rat) TFA can increase blood pressure in anesthetized rats and increases food intake .
|
-
- HY-P10153
-
|
|
Peptides
|
Others
|
|
gH625 is a cell-penetrating viral peptide which is a part of glycoprotein H of Herpes simplex virus type I. gH625 is able to cross the cell membrane and to transport many conjugated cargoes into the cytosol. gH625 is permeable to the blood-brain barrier (BBB) and can enter the rat brain in vivo without toxic effects. gH625 can be used for siRNA delivery research .
|
-
- HY-P1323
-
|
|
Neuropeptide Y Receptor
|
Cardiovascular Disease
Neurological Disease
|
|
[Leu31,Pro34]-Neuropeptide Y(human,rat) is a specific neuropeptide Y Y1 receptor agonist. [Leu31,Pro34]-Neuropeptide Y(human,rat) slao activates Y4, Y5. [Leu31,Pro34]-Neuropeptide Y(human,rat) can increase blood pressure in anesthetized rats and increases food intake .
|
-
- HY-P3976
-
|
|
Angiotensin-converting Enzyme (ACE)
|
Cardiovascular Disease
|
|
Lactalbumin B (50-53) Alpha [Lactorphin Alpha], bovine is a blood pressure lowering peptide containing 4 amino acids. Lactalbumin B (50-53) Alpha [Lactorphin Alpha], bovine is an angiotensin-converting Enzyme (ACE) inhibitor. Lactalbumin B (50-53) Alpha [Lactorphin Alpha], bovine can be used in research of high blood pressure .
|
-
- HY-P10587A
-
|
JNJ-77242113 acetate; JNJ-2113 acetate; PN-235 acetate
|
Interleukin Related
STAT
IFNAR
|
Inflammation/Immunology
|
|
Icotrokinra (JNJ-77242113) acetate is an orally available, selective antagonist of the IL-23 receptor. Icotrokinra acetate inhibits IL-23-induced STAT3 phosphorylation in peripheral blood mononuclear cells (IC50=5.6 pM) and inhibits IL-23-induced interferon IFN-γ production in NK cells with an IC50 of 18.4 pM. Icotrokinra acetate exhibits anti-inflammatory activity in a rat TNBS-induced colitis model. Icotrokinra acetate can be used in the study of psoriasis, psoriatic arthritis, and inflammatory bowel disease .
|
-
- HY-P5978
-
|
ANP 127-150 (rat)
|
Natriuretic Peptide Receptor (NPR)
|
Cardiovascular Disease
|
|
Atriopeptin III (ANP 127-150) (rat), a 24-amino acid atrial peptide, is a potent vasodilator and natriuretic/diuretic agent. Atriopeptin III (rat) improves renal functions and decreases blood pressure in a ureter-obstructed rat kidney model. Atriopeptin III (rat) can be used for research of chronic renal failure .
|
-
- HY-P5130
-
|
|
Endothelin Receptor
|
Cardiovascular Disease
|
|
Big endothelin-1 (rat 1-39) is a 39-residues peptide. Big endothelin-1 (rat 1-39) induces diuretic and natriuretic response in conscious Sprague-Dawley rats. Big endothelin-1 (rat 1-39) raises blood pressure in mice .
|
-
- HY-P1694
-
|
|
Bradykinin Receptor
|
Cardiovascular Disease
|
|
B4148 is a selective competitive bradykinin (BK) antagonist that significantly inhibits BK-induced hypotension in rats. In a rat model of endotoxin shock induced by Escherichia coli lipopolysaccharide, B4148 significantly attenuated the decrease in mean arterial blood pressure compared with the control group .
|
-
- HY-P11584
-
|
|
Amylin Receptor
CGRP Receptor
|
Metabolic Disease
|
|
KBP-066A is a long-acting dual amylin and calcitonin receptor agonist. KBP-066A can activate the CTR and AMY-R potently, with no off-target activity. KBP-066A reduces fasting blood glucose levels, fasting insulin levels, and body weight in diabetic rat models. KBP-066A can be used for the research of type 2 diabetes mellitus, obesity .
|
-
- HY-P10587B
-
|
JNJ-77242113 (hydrochloride); JNJ-2113 (hydrochloride); PN-235 (hydrochloride)
|
Interleukin Related
STAT
IFNAR
|
Inflammation/Immunology
|
|
Icotrokinra (JNJ-77242113) hydrochloride is an orally available, selective antagonist of the IL-23 receptor. Icotrokinra hydrochloride inhibits IL-23-induced STAT3 phosphorylation in peripheral blood mononuclear cells (IC50=5.6 pM) and inhibits IL-23-induced interferon IFN-γ production in NK cells with an IC50 of 18.4 pM. Icotrokinra hydrochloride exhibits anti-inflammatory activity in a rat TNBS-induced colitis model. Icotrokinra hydrochloride can be used in the study of psoriasis, psoriatic arthritis, and inflammatory bowel disease .
|
-
- HY-175824
-
|
|
iGluR
NO Synthase
Apoptosis
Reactive Oxygen Species (ROS)
|
Neurological Disease
|
|
PSD-95/nNOS PPI-IN-1 is a inhibitor targeting the PSD-95/nNOS interaction with potential blood-brain barrier penetration. PSD-95/nNOS PPI-IN-1 binds to the PSD-95 PDZ2 domain with high affinity (Ki = 19.45 μM). PSD-95/nNOS PPI-IN-1 inhibits glutamate-induced excitotoxicity by reducing intracellular ROS levels and inhibiting apoptosis. PSD-95/nNOS PPI-IN-1 significantly reduces cerebral infarct volume in rat tMCAO models. PSD-95/nNOS PPI-IN-1 can be used for the study of acute ischemic stroke .
|
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-B0130
-
-
-
- HY-124529
-
|
|
Structural Classification
Human Gut Microbiota Metabolites
other families
Conocephalum conicum (L.) Dumort.
Phenols
Polyphenols
Plants
Endogenous metabolite
Source Classification
|
11β-HSD
Endogenous Metabolite
|
|
Lunularin is an inhibitor of 11β-hydroxysteroid dehydrogenase 1, with an IC50 of 45.44 μM and a Ki of 35.8 μM against human 11β-HSD1, and an IC50 of 17.39 μM and a Ki of 10.31 μM against rat 11β-HSD1. Lunularin upregulates the transcription levels of Sirt1 and Hmox1 genes in the liver. Lunularin reduces food intake and body weight gain, and decreases blood glucose levels in mice fed a high-fat diet. Lunularin inhibits LPS-induced TLR4-mediated NF-κB pathway activation and nitric oxide production. Lunularin inhibits the proliferation and colony formation of renal cancer and colon cancer cells, and exhibits cancer cell-specific cytotoxicity. Lunularin binds to the steroid-binding site of human 11β-HSD1 and the steroid/NADPH-binding region of rat 11β-HSD1, but does not inhibit 11β-HSD2 or mouse 11β-HSD1. Lunularin can be used in research related to diet-induced obesity, renal cancer, colorectal cancer, inflammatory diseases and metabolic syndrome .
|
-
-
- HY-N0311
-
-
-
- HY-78086
-
-
-
- HY-N2160
-
-
-
- HY-N3807
-
-
-
- HY-W153159
-
|
|
Structural Classification
Alkaloids
Monophenols
Other Alkaloids
Gramineae
Phenols
Plants
Hordeum distichon L.
Source Classification
|
Adrenergic Receptor
|
|
N-Methyltyramine hydrochloride is an orally active α2-adrenoreceptor antagonist with an IC50 value of 5.53 μM against rat targets. N-Methyltyramine hydrochloride blocks α2-adrenoreceptors, while inhibiting lipolysis, hyperactivity responses and small intestinal peristalsis in mice. N-Methyltyramine hydrochloride promotes gastrin release and pancreatic juice secretion, upregulates appetite, blood pressure, myocardial contraction frequency and contraction intensity, and increases renal blood flow, renal vascular resistance and mean peripheral arterial resistance. N-Methyltyramine hydrochloride relaxes mouse small intestinal smooth muscle and undergoes biotransformation in vivo to produce adrenaline. N-Methyltyramine hydrochloride can be used in studies related to gastrointestinal diseases .
|
-
-
- HY-W153897
-
-
-
- HY-N11691
-
-
-
- HY-78086R
-
|
3-Methylbenzaldehyde (Standard)
|
Structural Classification
Ketones, Aldehydes, Acids
Labiatae
Plants
Vachellia nilotica (L.) P. J. H. Hurter & Mabb.
Source Classification
|
Reference Standards
Endogenous Metabolite
Bacterial
Cytochrome P450
|
|
m-Tolualdehyde (Standard) is the analytical standard of m-Tolualdehyde (HY-78086). This product is intended for research and analytical applications. m-Tolualdehyde (3-Methylbenzaldehyde) is an aldehyde metabolite produced by m-xylene metabolism, and it bidirectionally regulates the CYP 2B1, CYP 2E1, and CYP 4B1 isoenzymes in the respiratory tract of rats. m-Tolualdehyde serves as an oxidation substrate and carbon source for Pseudomonas Pxy, and it can be oxidized to m-toluic acid in an NAD + -dependent manner. m-Tolualdehyde exerts a dose-dependent inhibitory effect on CYP 2B1 and CYP 2E1 in the nasal mucosa and lungs of rats, and a dose-dependent activating effect on pulmonary CYP 4B1. m-Tolualdehyde can form aldehyde-heme adducts with the heme group of cytochrome P450. m-Tolualdehyde can be used in studies related to metabolic enzymes in the respiratory tract of rats .
|
-
-
- HY-N6951R
-
-
-
- HY-W153897R
-
-
-
- HY-N0311R
-
-
-
- HY-W153159R
-
|
|
Structural Classification
Alkaloids
Monophenols
Other Alkaloids
Gramineae
Phenols
Plants
Hordeum distichon L.
Source Classification
|
Reference Standards
Adrenergic Receptor
|
|
N-Methyltyramine (hydrochloride) (Standard) is the analytical standard of N-Methyltyramine (hydrochloride) (HY-W153159). This product is intended for research and analytical applications. N-Methyltyramine hydrochloride is an orally active α2-adrenoreceptor antagonist with an IC50 value of 5.53 μM against rat targets. N-Methyltyramine hydrochloride blocks α2-adrenoreceptors, while inhibiting lipolysis, hyperactivity responses and small intestinal peristalsis in mice. N-Methyltyramine hydrochloride promotes gastrin release and pancreatic juice secretion, upregulates appetite, blood pressure, myocardial contraction frequency and contraction intensity, and increases renal blood flow, renal vascular resistance and mean peripheral arterial resistance. N-Methyltyramine hydrochloride relaxes mouse small intestinal smooth muscle and undergoes biotransformation in vivo to produce adrenaline. N-Methyltyramine hydrochloride can be used in studies related to gastrointestinal diseases .
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- HY-147403S
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Tebideutorexant is an OX1R-selective inhibitor with oral bioavailability and blood-brain barrier permeability, with human OX1R pKi 8.17 and rat OX1R pKi 8.13.Tebideutorexant selectively modulates OX1R, with no significant functional effect on OX2R. Tebideutorexant can be used for the research of panic and anxiety disorders .
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- HY-W010243S
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Methylisothiazolinone-d3 hydrochloride is the deuterium labeled Methylisothiazolinone hydrochloride (HY-W010243). Methylisothiazolinone hydrochloride is a bacterial and fungal inhibitor and preservative, as well as a sensitizer. Methylisothiazolinone hydrochloride can activate matrix metalloproteinases (MMPs) in human bronchial epithelial cells to induce apoptosis and inflammatory response. Methylisothiazolinone hydrochloride can promote the development of atopic dermatitis in mice by disrupting Th2/Th17 related immune responses. Methylisothiazolinone hydrochloride can cause mitochondrial damage in the endothelium of rat cerebral blood vessels .
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- HY-107203S
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Propentofylline-d6 (HWA 285-d6) is the deuterium labeled Propentofylline. Propentofylline is an orally active and brain-penetrant phosphodiesterase inhibitor. Propentofylline blocks adenosine reuptake and prevents cyclic nucleotide degradation. Propentofylline can be used for the research of primary degenerative (Alzheimer's) dementia, vascular dementia, cerebral ischemia, acute stroke, and learning and memory disorders .
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- HY-14806S2
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Teneligliptin-d5 (MP-513-d5) is deuterium labeled Teneligliptin. Teneligliptin (MP-513) hydrobromide hydrate is an orally active and selective dipeptidyl peptidase 4 (DPP-4) inhibitor (IC50s: 0.37 and 0.29 nM for the human and rat DPP-4, respectively). Teneligliptin hydrobromide hydrate improves blood glucose levels and can be used in researches related to type 2 diabetes mellitus .
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- HY-A0168S
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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 .
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- HY-15498S
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Rimegepant-d4 (BMS-927711-d4) is the deuterium labeled Rimegepant (HY-15498). Rimegepant (BMS-927711) is an orally bioavailable and blood-brain barrier permeable antagonist of CGRP and AMY1 receptors, with a pIC50 of 8.01 and a Ki of 0.027 nM for human CGRP receptors. Rimegepant antagonizes cAMP production induced by αCGRP, βCGRP and amylin at CGRP and AMY1 receptors in humans, rats and mice, as well as at rat AMY3 receptors. Rimegepant can be used in research related to migraine .
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- HY-N3807S
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Enniatin B1- 13C34 is the 13C-labeled Enniatin B1 (HY-N3807). 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 .
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- HY-B0742S1
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Hydroxyprogesterone caproate-d8 (17α-Hydroxyprogesterone hexanoate-d8) is the deuterium labeled Hydroxyprogesterone caproate (HY-B0742). Hydroxyprogesterone caproate (17α-Hydroxyprogesterone hexanoate; 17α-Hydroxyprogesterone caproate) is a progesterone receptor (progesterone receptor) ligand and steroid hormone transcription inhibitor. Hydroxyprogesterone caproate downregulates estrogen receptors in target tissues and activates their metabolic pathways, and exhibits equivalent affinity for progesterone receptor A and progesterone receptor B. Hydroxyprogesterone caproate shows no consistent teratogenicity or developmental toxicity in rat, mouse and monkey models, but induces resorption or abortion in rhesus monkeys at human-equivalent doses. Hydroxyprogesterone caproate promotes the production of TNF-α in lipopolysaccharide-stimulated whole blood from non-pregnant women. Hydroxyprogesterone caproate can be used in scientific research related to preterm birth .
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