Search Result
Results for "
good permeability
" in MedChemExpress (MCE) Product Catalog:
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-136026
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BLU-5937
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P2X Receptor
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Inflammation/Immunology
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Camlipixant (BLU-5937) a potent, selective, non-competitive and orally active P2X3 homotrimeric receptor antagonist with an IC50 of 25 nM against hP2X3 homotrimeric. Camlipixant shows potent anti-tussive effect and no taste alteration. Camlipixant can be used for the research of unexplained, refractory chronic cough .
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- HY-139604
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MARK
Apoptosis
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Cancer
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PCC0208017 is a microtubule affinity regulating kinases (MARK3/MARK4) inhibitor with IC50s of 1.8 and 2.01 nM, respectively. PCC0208017 has much lower inhibitory activity against MARK1 and MARK2, with IC50s of 31.4 and 33.7 nM, respectively. PCC0208017 suppresses glioma progression in vitro and in vivo. PCC0208017 disrupts microtubule dynamics and induces G2/M phase cell cycle arrest and cell apoptosis. PCC0208017 demonstrates robust antitumor activity in vivo and displays good BBB permeability .
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- HY-15023
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Cligosiban
Maximum Cited Publications
6 Publications Verification
PF-3274167
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Oxytocin Receptor
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Endocrinology
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Cligosiban (PF-3274167) is an orally active, highly selective, and centrally permeable oxytocin receptor antagonist with good pharmacokinetics in rats and can inhibit physiological ejaculation in rodents [1][2].
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- HY-122614
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S29434
2 Publications Verification
NMDPEF
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Autophagy
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Neurological Disease
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S29434 (NMDPEF) is a potent, competitive, selective and cell-permeable inhibitor of quinone reductase 2 (QR2), with IC50s ranging from 5 to 16 nM for human QR2 at different organizational levels, and has good selectivity for QR2 over QR1. S29434 induces autophagy and inhibits QR2-mediated ROS production .
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- HY-168046
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Thyroid Hormone Receptor
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Metabolic Disease
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ALG-055009 is a selective and orally active Thyroid Hormone Receptor Beta (THR-β) agonist with an EC50 of 0.063 μM. ALG-055009 binds to the T3 hormone pocket of human THR-β, forming polar interactions with protein residues. ALG-055009 can lower total cholesterol levels in rats on a high-fat diet. ALG-055009 exhibits high metabolic stability, good permeability, a long in vivo half-life, and limited drug-drug interaction liability. ALG-055009 can be used in studies related to metabolic dysfunction-associated fatty liver disease .
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- HY-103234A
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iGluR
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Neurological Disease
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GYKI 52466 dihydrochloride is an orally active, highly selective and noncompetitive AMPA/kainate receptor antagonist with the IC50 values of 7.5 and 11μM, respectively. GYKI 52466 dihydrochloride has good blood brain barrier permeability and anticonvulsant effect. GYKI 52466 dihydrochloride can be used in Parkinson's disease research .
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- HY-119190
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Phosphodiesterase (PDE)
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Neurological Disease
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PF-06445974, a promising positron emission tomography (PET) lead, has exquisite potency at PDE4B with an IC50 <1 nM. The IC50 values are 36, 4.7 and 17 nM for PDE4D, PDE4A and PDE4C, respectively. PF-06445974 has good selectivity over PDE4D, excellent brain permeability, and a high level of specific binding in the "cold tracer" study .
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- HY-155079
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EGFR
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Cancer
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DZD1516 is a potent and selective HER2 inhibitor (IC50=0.56 nM) with good blood-brain permeability. DZD1516 exhibits antitumor activity in CNS and subcutaneous xenograft mouse models .
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- HY-103266
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Aurora Kinase
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Cancer
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TC-A 2317 hydrochloride is an orally active Aurora A kinase inhibitor (Ki=1.2 nM). TC-A 2317 hydrochloride exhibits excellent selectivity to Aurora B kinase (Ki=101 nM) and other 60 kinases, good cell permeability and good PK profile. Antitumor activity .
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- HY-153715
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Mitochondria modulator-1
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Biochemical Assay Reagents
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Metabolic Disease
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NV-354 (Mitochondria modulator-1) (compound 1) is a mitochondrial regulator that stimulates mitochondrial ATP production. NV-354 has good oral bioavailability, blood-brain barrier permeability, and good plasma stability. NV-354 has the potential to study mitochondrial diseases .
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- HY-124638
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MNK
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Cancer
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MNK inhibitor 9 is a potent and selective inhibitor of MNK1/2 with IC50 values of 0.003 µM and 0.003 µM for MNK1 and MNK2 respectively. MNK inhibitor 9 has good cell permeability. MNK inhibitor 9 can be used in tumor related research .
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- HY-13340
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VU152100
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mAChR
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Neurological Disease
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VU0152100 (VU152100) is a highly selective mAChR positive allosteric modulator (permeable to the blood-brain barrier). VU0152100 reverses Amphetamine-induced hypermotility in rats and increased levels of extracellular dopamine in nucleus accumbens and caudate-putamen. VU0152100 has good research potential in psychosis and cognitive impairment associated with mental disorders such as schizophrenia .
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- HY-163563
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Ligands for Target Protein for PROTAC
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Neurological Disease
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JYQ-173, a chemical probe, is a selective inhibitor for human Parkinson disease protein 7 (PARK7), with an IC50 of 19 nM. JYQ-173 exhibits good cell permeability. JYQ-173 is the ligand for target protein PARK7, which can be utilized for synthesis of PROTAC Degrader JYQ-194 (HY-163564) .
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- HY-155478
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Androgen Receptor
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Cancer
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Androgen receptor-IN-6 (compound 16) is an orally available androgen receptor (Androgen Receptor) potent inhibitor (IC50=0.12 μM in vitro), targeting the disordered N-terminal domain (NTD). Androgen receptor-IN-6 has good Caco2 cell membrane permeability and has an oral activity (F/%) of 16% in male CD-1 mice .
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- HY-137016A
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HCN Channel
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Neurological Disease
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8-Pcpt-cGMP sodium is the sodium salt form of 8-Pcpt-cGMP (HY-137016). 8-Pcpt-cGMP sodium is an agonist for cyclic nucleotide-gated (CNG) channel with an EC50 of 0.5 μM. 8-Pcpt-cGMP sodium exhibits good membrane permeability. 8-Pcpt-cGMP sodium can be used in studies about the function of CNG channels in visual signal transduction and olfactory transduction .
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- HY-118858
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EAAT
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Neurological Disease
Cancer
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UCPH-102 is a highly selective EAAT1 inhibitor with an IC50 of 0.43 µM. UCPH-102 exhibits a specific anti-proliferative effect on T-ALL cells. UCPH-102 also shows good blood-brain permeability, which can be used in studies of amyotrophic lateral sclerosis, Alzheimer’s disease, chronic pain and obsessive compulsive disorder .
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- HY-173076A
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HDAC
YAP
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Inflammation/Immunology
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HDAC11-IN-1 (Compound 14-N C6OH) TFA is a selective macrocyclic inhibitor of HDAC11 with a Ki of 40 nM. HDAC11-IN-1 TFA exhibits good cell permeability and can inhibit the expression of YAP1 and SOX2 .
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- HY-156432
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Anaplastic lymphoma kinase (ALK)
mTOR
PARP
Caspase
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Cancer
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ALK-IN-26 is an ALK inhibitor with IC50 value of 7.0 μM for ALK tyrosine kinase. ALK-IN-26 has good pharmacokinetic properties and blood-brain barrier (BBB) permeability. ALK-IN-26 can induce apoptosis, autophagy and necrosis. ALK-IN-26 can be used in glioblastoma studies .
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- HY-170790
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TRP Channel
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Neurological Disease
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HZS60 is a NMDAR/TRPM4 inhibitor with brain permeability that can improve cerebral ischemia. HZS60 has significant neuroprotective effects on primary neuronal ischemic damage caused by NMDA and oxygen-glucose deprivation/reoxygenation. HZS60 exhibits good pharmacokinetic characteristics and can inhibit cerebral ischemia-reperfusion injury. HZS60 can be used as a potential inhibitor of ischemic stroke .
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- HY-161712
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IMPDH
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Cancer
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IMPDH-IN-4 is a derivative of N-pyridinylthiophene carboxamid that exhibits activity against peripheral nerve sheath carcinoma cells. IMPDH-IN-4 is metabolized by NAMPT and NMNAT1 to an adenine dinucleotide (AD) derivative, which is an NAD analog and can inhibit inosine monophosphate dehydrogenase (IMPDH), leading to the accumulation of inosine monophosphate (IMP) in cells. IMPDH-IN-4 has good blood-brain barrier permeability and can be used in the study of central and peripheral nervous system cancers .
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- HY-W338446
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Tau Protein
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Neurological Disease
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BF-170 is a selective tau fibril binding agent with an EC50 of 221 nM. It exhibits good blood-brain barrier permeability, and after intravenous injection in mice, the concentration in brain tissue reaches 9.1% ID/g within 2 minutes (with a brain clearance rate of 0.25% ID/g after 30 minutes). BF-170 can be used as a probe for tau protein pathology imaging in Alzheimer's disease (AD). It plays an important role in early-stage AD research and holds potential for imaging studies of tau-related neurodegenerative diseases .
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- HY-163350
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GPR84
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Inflammation/Immunology
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TUG-2208 (compound 42a) is a GPR84 agonist (pEC50=8.98) with low lipophilicity and good solubility, in vitro permeability and microsomal stability .
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- HY-153241
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Epigenetic Reader Domain
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Cancer
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GSK737 is a BRD4 BD1 and BD2 inhibitor, with pIC50 values of 5.3 and 7.3 respectively. GSK737 has low clearance and good solubility and permeability in rat .
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- HY-D2317
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Fluorescent Dye
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Others
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HaloFlipper 30 is a fluorescent probe that covalently reacts with HaloTag fusion proteins to form an ester bond, which allows the probe to be stably attached to membrane structures. HaloFlipper 30 has high specificity, precision and good cell permeability .
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- HY-149820
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Monoamine Oxidase
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Neurological Disease
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MAO-B-IN-22 (compound 6h) is a potent MAO-B inhibitor with an IC50 of 0.014 μM. MAO-B-IN-22 has high antioxidant activity, good metal chelating ability, proper BBB permeability and significant neuroprotective effect .
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- HY-138648
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ERK
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Neurological Disease
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PB1 is a potent intracellular disulfide reducing agent with several advantages including good cell permeability, the ability to form a high intracellular concentration gradient, and stability. PB1 is a borane-protected TCEP (tris(2-carboxyethyl)phosphine) analogue. PB1 increases retinal ganglion cells survival after axotomy in vitro at nanomolar and picomolar concentrations. PB1 can be used for the research of neuroprotective .
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- HY-11054
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- HY-118147
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Fatty Acid Synthase (FASN)
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Cancer
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ML356 (Compound 16) is an inhibitor for fatty acid synthase (FAS), that inhibits the thioesterase domain of FAS (FAS TE) with an IC50 of 0.334 μM, and blocks the de novo palmitate synthesis in PC-3 cell with an IC50 of 20 μM. ML356 exhibits good membrane permeability, and good stability in human and mouse plasma .
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- HY-173623
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iGluR
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Neurological Disease
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EU 1622-240 is a biased positive allosteric modulator of GluN2B, GluN2C, and GluN2D, with EC50s of 0.57, 0.82, 1.1 μM respectively. EU 1622-240 has good physicochemical properties, in vitro stability, and permeability .
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- HY-137016
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HCN Channel
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Neurological Disease
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8-Pcpt-cGMP is an agonist for cyclic nucleotide-gated (CNG) channel with an EC50 of 0.5 μM. 8-Pcpt-cGMP exhibits good membrane permeability. 8-Pcpt-cGMP can be used in studies about the function of CNG channels in visual signal transduction and olfactory transduction .
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- HY-D2940
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SiR650-BG
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Fluorescent Dye
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Others
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SiR-SNAP (SiR650-BG) is a SiR-labeled SNAP tag near-infrared fluorescent probe (Ex/Em: 645 nm/661 nm). SiR-SNAP combines excellent optical properties, good cell membrane permeability, and environmentally sensitive fluorescence characteristics, providing a powerful tool for the dynamic study of proteins in living cells .
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- HY-P10698
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Peptide-Drug Conjugates (PDCs)
LDLR
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Neurological Disease
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VH-N412 is a vectorized neuropeptide (NT) with good blood-brain barrier permeability. VH-N412 binds to the low-density lipoprotein receptor (LDLR) and neuropeptide receptor 1 (NTSR-1), and acts as a pharmacological-induced hypothermia (PIH) inducer. VH-N412 exhibits anticonvulsant and neuroprotective effects, and can be used in the study of neurological diseases such as epilepsy.
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- HY-156965
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Fluorescent Dye
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Metabolic Disease
Cancer
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BAY-771, a structurally close pyrimidinedione, is a chemical probe with good lead-like properties and high permeability in Caco-2 cells (no hint of efflux). BAY-771 shows very weak inhibitory activity in the BCAT1 biochemical assay and no activity in BCAT2. BAY-771 can be used as a negative control of HY-148242 BAY-069. BAY-771 can be used for the research of tumor metabolism .
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- HY-170491
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GSK-3
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Infection
Neurological Disease
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GSK-3β inhibitor 23 (Compound 11726169) is the inhibitor for glycogen synthase kinase-3, that inhibits GSK-3β and GSK-3α with IC50 of 12.1 nM and 18.8 nM. GSK-3β inhibitor 23 exhibits antiviral activity against HIV 1. GSK-3β inhibitor 23 exhibits good metabolic stablility in mouse/human liver microsomes and plasma, but poor Caco-2 permeability (which predicts low oral bioavailability) .
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- HY-161783
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HDAC
Keap1-Nrf2
Reactive Oxygen Species (ROS)
Apoptosis
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Neurological Disease
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HDAC6-IN-45 (Compound 15) is a selective inhibitor for HDAC6 with IC50 of 15.2 nM. HDAC6-IN-45 exhibits neurotrophic through the upregulation of GAP43 and Beta-3 tubulin markers. HDAC6-IN-45 activates the Nrf2 signaling pathway, reduces H2O2-induced ROS production, inhibits apoptosis in PC12, and exhibits neuroprotective efficacy in SCOP-induced zebrafish Alzheimer's Disease models. HDAC6-IN-45 exhibits antioxidant activity and good blood-brain barrier (BBB) permeability .
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- HY-147285
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mTOR
PI3K
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Neurological Disease
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PI3K/mTOR Inhibitor-9 (Compound 1) is a potent mTOR and PI3K inhibitor with IC50 values of 38 nM, 6.6 μM, 6.6 μM and 0.8 μM against mTOR (phospho-S6 cellular assay), PI3Kα, PI3Kγ and PI3Kδ, respectively .
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- HY-19446
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Phosphodiesterase (PDE)
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Others
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UK-371800 is a highly selective PDE5 inhibitor (IC50 = 4.2 nM). UK-371800 has good permeability and is not affected by the efflux of P-glycoprotein .
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- HY-155992
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Sigma Receptor
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Neurological Disease
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WLB-89462 (Compound 20c) is a selective σ2 receptor ligand (Ki: 13 nM). WLB-89462 has neuroprotective activity. WLB-89462 improves short-term memory impairment induced by Aβ peptide in rats. WLB-89462 has good ADMET profile (good solubility, no CYP inhibition, good metabolic stability, high permeability, brain penetration, and high oral exposure in rodents) .
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- HY-W299574A
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Others
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Cancer
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(Rac)-HfLeu hydrochloride is an anticancer agent with good cell membrane permeability. (Rac)-HfLeu hydrochloride has excellent proliferation inhibition ability for cancer cells. (Rac)-HfLeu hydrochloride can be used for research on various types of cancer .
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- HY-169194
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Parasite
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Infection
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Antimalarial agent 44 (Compound 3) is an antimalarial agent against parasite. Antimalarial agent 44 has a good permeability across MDCK-MDR1 cell monolayers and a high clearance by mouse liver microsomes .
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- HY-163797
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DNA/RNA Synthesis
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Cancer
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WRN inhibitor 10 (Compound P24) is an inhibitor for the Werner helicase WRN with an IC50 of 1.1 nM. WRN inhibitor 10 inhibits the proliferation of cancer cell SW48 with IC50 of 39 nM. WRN inhibitor 10 exhibits good liver microsomal stability and film permeability. WRN inhibitor 10 exhibits good pharmacokinetic characteristics in CD-1 mice .
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- HY-134406
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Phosphodiesterase (PDE)
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Neurological Disease
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6-Cl-cPuMP (sodium) is a cAMP analog with active chlorine function. 6-Cl-cPuMP (sodium) has good membrane permeability and phosphodiesterase (PDE) stability. 6-Cl-cPuMP (sodium) can be used for nervous system research .
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- HY-147726
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Microtubule/Tubulin
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Cancer
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Microtubule inhibitor 5 (compound 17f) is a potent microtubule inhibitor. Microtubule inhibitor 5 shows cytotoxicity with an IC50 value of 154.5 nM for NCI-H460 cells. Microtubule inhibitor 5 shows good cell permeability .
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- HY-148850
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Cannabinoid Receptor
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Metabolic Disease
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AZD-2207 is a cannabinoid receptor CB1 antagonist, known for its high lipophilicity. AZD-2207 has good intestinal permeability in the Caco-2 model and can be used in research related to type 2 diabetes and obesity .
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- HY-15023R
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PF-3274167 (Standard)
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Oxytocin Receptor
Reference Standards
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Endocrinology
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Cligosiban (Standard) is the analytical standard of Cligosiban. This product is intended for research and analytical applications. Cligosiban (PF-3274167) is an orally active, highly selective, and centrally permeable oxytocin receptor antagonist with good pharmacokinetics in rats and can inhibit physiological ejaculation in rodents .
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- HY-173076
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HDAC
YAP
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Inflammation/Immunology
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HDAC11-IN-1 (Compound 14-N C6OH) is a selective macrocyclic inhibitor of HDAC11 with a Ki of 40 nM. HDAC11-IN-1 exhibits good cell permeability and can inhibit the expression of YAP1 and SOX2 .
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- HY-161380
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Fungal
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Infection
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Antifungal agent 96 (Compound WZ-2) is an antifungal agent with good blood-brain barrier permeability and brain penetration. Antifungal agent 96 inhibits the growth of C. neoformans H99 and C. albicans 0304103 with MIC values of 0.016 and 32 μg/mL, respectively .
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- HY-P4135
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Fluorescent Dye
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Others
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FITC-LC-Antennapedia Peptide is a FITC labeled Antennapedia Peptide (HY-P0307). Antennapedia Peptide is a cellular-membrane permeable peptides (CPP). FITC-LC-Antennapedia Peptide has good penetration in 3T3 cell line, which was rapidly accumulated into nuclei .
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- HY-103234
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iGluR
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Neurological Disease
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GYKI 52466 is an orally active, highly selective and noncompetitive AMPA/kainate receptor antagonist with the IC50 values of 7.5 and 11μM, respectively. GYKI 52466 has good blood brain barrier permeability and anticonvulsant effect. GYKI 52466 can be used in Parkinson's disease research .
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- HY-161381
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- HY-103234B
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iGluR
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Neurological Disease
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GYKI 52466 hydrochloride is an orally active, highly selective and noncompetitive AMPA/kainate receptor antagonist with the IC50 values of 7.5 and 11μM, respectively. GYKI 52466 hydrochloride has good blood brain barrier permeability and anticonvulsant effect. GYKI 52466 hydrochloride can be used in Parkinson's disease research .
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- HY-149242
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Monoamine Oxidase
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Neurological Disease
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MAO-B-IN-20 (Compound C14) is a potent MAO-B inhibitor with an IC50 of 0.037 μM. MAO-B-IN-20 displays good metabolic stability and brain-blood barrier permeability. MAO-B-IN-20 can be used for the research of Parkinson's disease .
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- HY-147738
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Fluorescent Dye
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Others
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SQM-NBD is a potent and selectiveAIE fluorescent probe. SQM-NBD exhibits excellent sensitivity to Cys and Hcy with the LOD of 54 nM and 72 nM, respectively.SQM-NBD has good cell permeability and low cytotoxicity. SQM-NBD has the potential for Cys/Hcy identification under physiological and pathological conditions .
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- HY-161643
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Cholinesterase (ChE)
Keap1-Nrf2
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Neurological Disease
Inflammation/Immunology
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S21-1011 is a selective inhibitor for butyrylcholinesterase (BChE), with IC50 of 0.059 and 0.162 μM, for eqBChE and hBChE, respectively. S21-1011 exhibits good blood-brain barrier (BBB) permeability and good pharmacokinetic characters. S21-1011 exhibits anti-inflammatory activity through activation of keap1-Nrf2-ARE pathway (EC50 is 23.48 μM for antioxidant element ARE activation), ameliorates cognitive impairment in murine Alzheimer’s disease model .
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- HY-159091
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HIV Integrase
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Infection
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HIV-1 integrase inhibitor 12 (Compound 17) is an inhibitor for HIV-1 integrase with an IC50 of 1.4 nM. HIV-1 integrase inhibitor 12 inhibits the HIV-1 WT and HIV-1 T125A, with IC50 of 7.4 and 120 nM, respectively. HIV-1 integrase inhibitor 12 exhibits metabolic stability and Caco-2 permeability, and good pharmacokinetic characteristics with good bioavailability (64%) and low clearance (0.16 L/hr/kg) in rats .
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- HY-160656
-
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5-HT Receptor
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Neurological Disease
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5-HT/NA Reuptake inhibitor-1 (compound 9) is a selective dual 5-HT and NA reuptake inhibitor with IC50 of 660 nM and 70 nM respectively. . 5-HT/NA Reuptake inhibitor-1 has good in vitro human metabolic stability, hERG selectivity and passive membrane permeability .
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- HY-144660
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Cholinesterase (ChE)
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Neurological Disease
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AChE-IN-7 (Compound 16) is a selective and potent inhibitor of acetylcholinesterase (eeAChE IC50 = 0.045 μM; eeBuChE IC50 = 19.68 μM). AChE-IN-7 is safe in vivo and in vitro, and shows good overall pharmacokinetic performance and high bioavailability (F = 55.5%). AChE-IN-7 also has high BBB permeability .
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- HY-100855
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Histone Methyltransferase
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Cancer
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DC_C66 is a cell-permeable, selective coactivator associated arginine methyltransferase 1 (CARM1) inhibitor with an IC50 of 1.8 μM. DC_C66 has a good selectivity for CARM1 against PRMT1 (IC50=21 μM), PRMT6 (IC50= 47μM), and PRMT5 .
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- HY-147397
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Pyruvate Kinase
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Cancer
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PKM2 activator 3 is a potent PKM2 activator with an AC50 value of 90 nM. PKM2 activator 3 has good Caco-2 permeability, a low efflux ratio and high microsomal stability. PKM2 activator 3 can be used for researching anticancer .
(AC50: the concentration which gives 50% activation of enzyme.)
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- HY-151368
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Cholinesterase (ChE)
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Neurological Disease
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AChE/BChE-IN-10 (Compound 7b) is a potent dual AChE and BChE inhibitor with IC50 values of 0.176, and 0.47 μM, respectively. AChE/BChE-IN-10 shows good blood brain barrier permeability. AChE/BChE-IN-10 can inhibit Aβ-aggregation and be used in Alzheimer’s disease (AD) research .
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- HY-152614
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Parasite
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Infection
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Antimalarial agent 19 (compound 6e) is an antimalarial active agent. Antimalarial agent 19 has antimalarial activity for the blood stage of P. falciparum K1 and P. berghei with EC50 values of 0.3 µM, 15.3 µM, respectively. Antimalarial agent 19 has good aqueous solubility, intestinal permeability and microsomal stability compared to gamhepathiopine .
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- HY-161663
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Phosphodiesterase (PDE)
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Cardiovascular Disease
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Phosphodiesterase-IN-2 (Compound C7) is a selective, orally active inhibitor for phosphodiesterase 10A (PDE10A), with an IC50 of 11.9 nM. Phosphodiesterase-IN-2 improves the stability of liver microsomes, and lowers BBB permeability. Phosphodiesterase-IN-2 exhibits good pharmacokinetic characters, and attenuates isoprenaline (HY-108353)-induced cardiac hypertrophic in mouse models .
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- HY-163799
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Histone Methyltransferase
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Cancer
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PRMT5-MTA-IN-1 (Compound A9a) is an inhibitor for protein arginine methyltransferase PRMT5-MTA. PRMT5-MTA-IN-1 inhibits the proliferation of colorectal cancer cell HCT116 wildtype and MTAP del mutant, with an IC50 of 16 nM and 2.47 μM. PRMT5-MTA-IN-1 exhibits good liver microsomal stability and film permeability. PRMT5-MTA-IN-1 exhibits good pharmacokinetic characteristics in CD-1 mice .
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- HY-155541
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Apoptosis
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Cancer
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Antitumor agent-110 (compound 13) is an anticancer imidazotetrazine with good permeability properties. Antitumor agent-110 arrests cell cycel at G2/M phase, and induces apoptosis . Antitumor agent-110 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-103234AR
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Reference Standards
iGluR
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Neurological Disease
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GYKI 52466 (dihydrochloride) (Standard) is the analytical standard of GYKI 52466 (dihydrochloride). This product is intended for research and analytical applications. GYKI 52466 dihydrochloride is an orally active, highly selective and noncompetitive AMPA/kainate receptor antagonist with the IC50 values of 7.5 and 11μM, respectively. GYKI 52466 dihydrochloride has good blood brain barrier permeability and anticonvulsant effect. GYKI 52466 dihydrochloride can be used in Parkinson's disease research .
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- HY-144272
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- HY-168152
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SARS-CoV
Virus Protease
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Infection
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SARS-CoV-2 3CLpro-IN-26 (Compound (S,R)-4y) is an allosteric inhibitor for SARS-CoV-2 3CLpro with an IC50 of 0.43 μM. SARS-CoV-2 3CLpro-IN-26 exhibits good cell permeability and is able to effectively cross the cell membrane, after co-incubation with Vero-E6 cells .
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- HY-146049
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Parasite
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Infection
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Antitrypanosomal agent 4 (compound 19) is a potent and blood-brain barrier permeable antitrypanosomal agent. Antitrypanosomal agent 4 has good activity against Trypanosoma cruzi (T. cruzi) and Trypanosoma brucei brucei (T. b. brucei) with IC50s of 1.2 μM and 70 nM, respectively . Antitrypanosomal agent 4 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-13340R
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VU152100 (Standard)
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mAChR
Reference Standards
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Neurological Disease
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VU0152100 (Standard) is the analytical standard of VU0152100. This product is intended for research and analytical applications. VU0152100 (VU152100) is a highly selective mAChR positive allosteric modulator (permeable to the blood-brain barrier). VU0152100 reverses Amphetamine-induced hypermotility in rats and increased levels of extracellular dopamine in nucleus accumbens and caudate-putamen. VU0152100 has good research potential in psychosis and cognitive impairment associated with mental disorders such as schizophrenia .
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- HY-175524
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Monoamine Oxidase
Cholinesterase (ChE)
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Neurological Disease
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BChE/MAO-B-IN-2 is a dual inhibitor of BChE (IC50 = 0.05 μM, Ki = 0.01 μM) and MAO-B (IC50 = 0.45 μM, Ki = 0.08 μM) with good blood-brain barrier permeability. BChE/MAO-B-IN-2 exhibits antioxidant activity, including DPPH radical scavenging, CUPRAC copper ion reduction, and superoxide anion scavenging. BChE/MAO-B-IN-2 can be used for the study of Alzheimer's disease (AD) .
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- HY-155061
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Cytochrome P450
Aryl Hydrocarbon Receptor
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Cancer
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hCYP1B1-IN-1 (compound B18) is a hCYP1B1 inhibitor (IC50=3.6 nM)，as well as an antagonist of Aryl Hydrocarbon Receptor. hCYP1B1-IN-1 exhibtis suitable metabolic stability and good cell-permeability. hCYP1B1-IN-1 inhibits migration of MCF-7 cells .
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- HY-155735
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iGluR
Cholinesterase (ChE)
Amyloid-β
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Neurological Disease
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AChE/Aβ-IN-2 (compound 33) is a potent and orally active inhibitor of acetylcholinesterase (AChE) with IC50 of 135 nM, as well as an antagonist of NMDA receptor (GluN1-1b/GluN2B subunit combination) with IC50 of 5.054 μM. AChE/Aβ-IN-2 also inhibits Aβ aggregation and shows good blood-brain barrier permeability. AChE/Aβ-IN-2 improves cognitive and spatial memory impairment in rats model .
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- HY-155733
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iGluR
Cholinesterase (ChE)
Amyloid-β
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Neurological Disease
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AChE/Aβ-IN-1 (compound 32) is a potent and orally active inhibitor of acetylcholinesterase (AChE) with an IC50 of 86 nM, as well as an antagonist of NMDA receptor (GluN1-1b/GluN2B subunit combination) with IC50 of 3.876 μM. AChE/Aβ-IN-1 also inhibits Aβ aggregation and shows good blood-brain barrier permeability and neuroprotection. AChE/Aβ-IN-1 improves cognitive and spatial memory impairment in rats model .
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- HY-16731
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EVT 302; RG1577; RO4602522
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Monoamine Oxidase
Reactive Oxygen Species (ROS)
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Neurological Disease
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Sembragiline (EVT 302) is a potent, selective and reversible monoamine oxidase B (MAO-B) inhibitor. Sembragiline reduces the metabolism of dopamine and other amine neurotransmitters by inhibiting the activity of the MAO-B enzyme, thereby potentially increasing the concentration of these neurotransmitters in the brain. Inhibition of the MAO-B enzyme also reduces the formation of toxic reactive oxygen species (ROS) that play a role in the pathological process of AD. Sembragiline has good oral activity and blood-brain barrier permeability. Sembragiline can be used in studies of AD, especially in patients with AD who show increased MAO-B activity .
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- HY-159492
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5-HT Receptor
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Neurological Disease
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5-HT7 receptor ligand 2 (compound 32) is an arylpiperazinehydrazine ligand for 5-HT7R (Ki=178 nM). 5-HT7 receptor ligand 2 has good membrane permeability, low hepatotoxicity and cardiotoxicity, and high plasma protein binding. 5-HT7 receptor ligand 2 shows neuroprotective effects in SH-SY5Y cells and can be used for the study of central nervous system related diseases .
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- HY-162760
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COMT
Monoamine Oxidase
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Neurological Disease
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COMT-IN-1 (compound C12), a nitrophenolic analogue, is an orally active dopamine metabolic enzyme catechol-O-methyltransferase (COMT) inhibitor with IC50s of 0.37 μM, 95.58 μM and 58.82 μM for COMT, MAO-A and MAO-B, respectively. COMT-IN-1 exhibits chelation with a variety of metal ions. COMT-IN-1 exhibits good BBB permeability. COMT-IN-1 improves dopamine levels and ameliorates MPTP (HY-15608)-induced Parkinson's disease (PD) symptoms in mice .
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- HY-149090
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Cholinesterase (ChE)
Monoamine Oxidase
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Neurological Disease
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AChE/BuChE/MAO-B-IN-2 (compound 4b) is a potent AChE/BuChE inhibitor and showed good blood brain barrier (BBB) permeability in vitro with an IC50 value of 5.3 μM, 12.4 μM, 1.9±0.08 μM, for AChE, BuChE, huMAO-B, respectively. AChE/BuChE/MAO-B-IN-2 (compound 4b) can inhibit excess AChE/BuChE in Alzheimer's disease (AD) brain. AChE/BuChE/MAO-B-IN-2 (compound 4b) can be used in anti-Alzheimer's research .
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- HY-181047
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Dopamine Receptor
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Neurological Disease
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FMJ-01-042 is a blood-brain barrier-permeable, low-efficacy partial agonist with high affinity (Kᵢ = 4.33 nM) and exceptional subtype selectivity for the dopamine D4 receptor. FMJ-01-042 exhibits good metabolic stability and is suitable for research on neurological and psychiatric disorders .
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- HY-174454
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P-glycoprotein
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Infection
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Antitrypanosomal agent 24 is a benzothiazole amidoxime with strong and selective antitrypanosomal activity (IC50 = 0.92 μM). Antitrypanosomal agent 24 is a substrate of the P-glycoprotein efflux pump. Antitrypanosomal agent 24 has high membrane permeability and good metabolic stability. Antitrypanosomal agent 24 binds to DNA/RNA by intercalation .
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- HY-143330
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Monoamine Oxidase
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Neurological Disease
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MAO-B-IN-4 (Compound 26) is an orally active and reversible MAO-B inhibitor with an IC50 of 9 nM. MAO-B-IN-4 has good metabolic stability, safety profile and brain permeability. MAO-B-IN-4 shows antidepressant activity in rats and mice. MAO-B-IN-4 can be used in studies related to Alzheimer's disease .
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HY-L141
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2,904 compounds
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Drug repurposing (also called drug repositioning, reprofiling, or re‑tasking) offers various advantages over developing an entirely new drug for a given indication, for example, lower risk of failure, less investment, and shorter development timelines. But drug repositioning projects are also subject to several risks, including regulatory and intellectual property issues. So the off-patent drugs are optimal for repositioning because of their immediate availability for clinical studies, with high feasibility and relatively low risk.
MCE carefully prepared a unique collection of 2,904 off-patent drugs, which is a good choice for drug repurposing.
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HY-L901P
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80,000 compounds
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A Lead-like, diverse library is the foundation for achieving biological activity diversity. The MCE Lead-like Diverse Library Plus is a further supplement to the 50K Lead-like Compound Library (HY-L901), consisting of over 80,000 lead-like compounds, with an additional 30,000 structurally novel lead-like molecules. These compounds occupy a broader "chemical space", making it a powerful tool for new drug discovery.
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HY-L906
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647 compounds
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On May 15, 2024, "Dimerization and antidepressant recognition at noradrenaline transporter" was published online by Nature. The research findings were an effort from Shanghai Institute of Materia Medica, Chinese Academy of Sciences. This study unraveled the important neural system target - the noradrenaline transporter (NET), obtaining the binding modes of human NET homodimers with the natural substrate norepinephrine (NE) and six selective antidepressants. It laid an important theoretical foundation for understanding the physiological regulation mechanisms of NET and other monoamine transporters.
The Norepinephrine Transporter (NET) Compound Library is obtained by computer-aided virtual screening based on the HY-L901 compound library . The specific screening process includes molecular docking screening, key pharmacophore screening, and CNS-MPO screening, which can be used for new drug discovery targeting the noradrenaline transporter.
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HY-L0121V
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10,000 compounds
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Natural products are an attractive source with varied structures that exhibit potent biological activities, and desirable pharmacological profiles. The core scaffold of a natural product can also provide a biologically validated framework upon which to display diverse functional groups. Inspired by bioactive natural products, natural product-like compounds, occupying the same chemical space, are ideally suited to explore and to facilitate understanding of biological pathways.
MCE 10K Natural Product-like Compound Library consists of 10,000 natural product-like compounds. Each compound has scaffold of natural products or Tanimoto coefficient >0.6 with natural products. The natural-likeness scoring of these compounds is >-2. What’s more, compounds in the library are drug-like and readily available for re-supply, making it a powerful tool for new drug research and development. It can be widely applied in high-throughput screening (HTS) and high-content screening (HCS).
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HY-L905
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4,803 compounds
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Natural products are an attractive source with varied structures that exhibit potent biological activities, and desirable pharmacological profiles. The core scaffold of a natural product can also provide a biologically validated framework upon which to display diverse functional groups. Inspired by bioactive natural products, natural product-like compounds, occupying the same chemical space, are ideally suited to explore and to facilitate understanding of biological pathways.
MCE 5K Natural Product-like Compound Library consists of 5,000 natural product-like compounds. Each compound has scaffold of natural products or Tanimoto coefficient >0.6 with natural products. The natural-likeness scoring of these compounds is >-2. What’s more, compounds in the library are drug-like and readily available for re-supply, making it a powerful tool for new drug research and development. It can be widely applied in high-throughput screening (HTS) and high-content screening (HCS).
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| Cat. No. |
Product Name |
Type |
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- HY-D2317
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Fluorescent Dyes
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HaloFlipper 30 is a fluorescent probe that covalently reacts with HaloTag fusion proteins to form an ester bond, which allows the probe to be stably attached to membrane structures. HaloFlipper 30 has high specificity, precision and good cell permeability .
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- HY-D2940
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SiR650-BG
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Fluorescent Dyes
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SiR-SNAP (SiR650-BG) is a SiR-labeled SNAP tag near-infrared fluorescent probe (Ex/Em: 645 nm/661 nm). SiR-SNAP combines excellent optical properties, good cell membrane permeability, and environmentally sensitive fluorescence characteristics, providing a powerful tool for the dynamic study of proteins in living cells .
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| Cat. No. |
Product Name |
Target |
Research Area |
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- HY-173076A
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HDAC
YAP
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Inflammation/Immunology
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HDAC11-IN-1 (Compound 14-N C6OH) TFA is a selective macrocyclic inhibitor of HDAC11 with a Ki of 40 nM. HDAC11-IN-1 TFA exhibits good cell permeability and can inhibit the expression of YAP1 and SOX2 .
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- HY-P10698
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Peptide-Drug Conjugates (PDCs)
LDLR
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Neurological Disease
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VH-N412 is a vectorized neuropeptide (NT) with good blood-brain barrier permeability. VH-N412 binds to the low-density lipoprotein receptor (LDLR) and neuropeptide receptor 1 (NTSR-1), and acts as a pharmacological-induced hypothermia (PIH) inducer. VH-N412 exhibits anticonvulsant and neuroprotective effects, and can be used in the study of neurological diseases such as epilepsy.
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- HY-173076
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HDAC
YAP
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Inflammation/Immunology
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HDAC11-IN-1 (Compound 14-N C6OH) is a selective macrocyclic inhibitor of HDAC11 with a Ki of 40 nM. HDAC11-IN-1 exhibits good cell permeability and can inhibit the expression of YAP1 and SOX2 .
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- HY-P4135
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Fluorescent Dye
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Others
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FITC-LC-Antennapedia Peptide is a FITC labeled Antennapedia Peptide (HY-P0307). Antennapedia Peptide is a cellular-membrane permeable peptides (CPP). FITC-LC-Antennapedia Peptide has good penetration in 3T3 cell line, which was rapidly accumulated into nuclei .
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| Cat. No. |
Product Name |
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Classification |
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- HY-155541
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Alkynes
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Antitumor agent-110 (compound 13) is an anticancer imidazotetrazine with good permeability properties. Antitumor agent-110 arrests cell cycel at G2/M phase, and induces apoptosis . Antitumor agent-110 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-168152
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Alkynes
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SARS-CoV-2 3CLpro-IN-26 (Compound (S,R)-4y) is an allosteric inhibitor for SARS-CoV-2 3CLpro with an IC50 of 0.43 μM. SARS-CoV-2 3CLpro-IN-26 exhibits good cell permeability and is able to effectively cross the cell membrane, after co-incubation with Vero-E6 cells .
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- HY-175524
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Alkynes
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BChE/MAO-B-IN-2 is a dual inhibitor of BChE (IC50 = 0.05 μM, Ki = 0.01 μM) and MAO-B (IC50 = 0.45 μM, Ki = 0.08 μM) with good blood-brain barrier permeability. BChE/MAO-B-IN-2 exhibits antioxidant activity, including DPPH radical scavenging, CUPRAC copper ion reduction, and superoxide anion scavenging. BChE/MAO-B-IN-2 can be used for the study of Alzheimer's disease (AD) .
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