Search Result
Results for "
BBB penetrate
" in MedChemExpress (MCE) Product Catalog:
8
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-P10235
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Amylin Receptor
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Neurological Disease
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Cyclic AC253 is an antagonist for amylin receptor, with IC50 of 0.3 μM. Cyclic AC253 exhibits neuroprotective efficacy against Aβ toxicity and abrogates Aβ-induced impairment of hippocampal long-term potentiation. Cyclic AC253 penetrate blood-brain barrier (BBB) .
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- HY-164284
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Sodium Channel
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Neurological Disease
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LK-2 is an antagonist for ASIC1a with a Kd of 1.9 μM. LK-2 reduces glutamate-induced ASIC1a current-enhancement with an IC50 of 6.6 μM. LK-2 exhibits neuroprotective efficacy in mouse ischemic stroke model, with improved motor and coordination skills. LK-2 is blood-brain barrier (BBB) penetrable .
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- HY-162565
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STK33
CDK
RET
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Endocrinology
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CDD-2807 is an inhibitor for serine/threonine kinase 33 (STK33) with IC50 of 9.2 nM. CDD-2807 exhibits no significant toxicity in mice and can cross the blood-testis barrier without accumulating in the brain. CDD-2807 induces a reversible contraceptive effect and has potential for the development of the male contraceptive .
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- HY-134228
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- HY-119624
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PIKfyve
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Cancer
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MOMIPP, a macropinocytosis inducer, is a PIKfyve inhibitor. MOMIPP penetrates the blood-brain barrier (BBB) .
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- HY-153434
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RIP kinase
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Cancer
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RIP1 kinase inhibitor 4 (Example 3) is a BBB-penetrable RIP1 kinase inhibitor (EC50: <100 nM). RIP1 kinase inhibitor 4 can be used for the research of cell programming necrosis-related diseases . RIP1 kinase inhibitor 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-164401
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EAAT
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Cancer
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QBS10072S is a bifunctional chemotherapeutic agent, through combination of a cytotoxin and a selective LAT1 transporter substrate. QBS10072S exhibits cytotoxicity in MDA-MB-231 cell and antitumor efficacy in mice. QBS10072S is blood-brain barrier (BBB) penetrable .
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- HY-162757
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GABA Receptor
Sodium Channel
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Neurological Disease
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Anticonvulsant agent 5 (Compound 5c) exhibits high affinity for GABAA receptors and NaV1.3 receptors. Anticonvulsant agent 5 shows anticonvulsant efficacy in mice psychomotor epilepsy test with an ED50 of 107 mg/kg. Anticonvulsant agent 5 exhibits neuroprotective activity against Kainic acid (HY-N2309) with an IC50 of 113 μM. Anticonvulsant agent 5 is blood-brain barrier (BBB) penetrable .
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- HY-122462
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PNU-159548
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DNA/RNA Synthesis
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Cancer
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Ladirubicin (PNU-159548) is a derivative of Daunorubicin (HY-13062A). Ladirubicin exhibits DNA intercalation and DNA alkylating properties, inhibits DNA replication and transcription, causes DNA damage, and thereby exhibits antitumor efficacy. Ladirubicin exhibits the potential to penetrate the blood-brain barrier (BBB) for its high lipophilicity. Ladirubicin exhibits toxicity through suppression of bone marrow activity .
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- HY-163909
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Cholinesterase (ChE)
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Neurological Disease
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AChE-IN-72 (Compound 13a) is an inhibitor for acetylcholinesterase (AChE) with an IC50 of 0.59 μM. AChE-IN-72 inhibits BChE with an IC50 of 5.02 μM. AChE-IN-72 exhibits radical scavenging with IC50 of 5.88 μM. AChE-IN-72 exhibits iron-chelating property, inhibits Aβ1−42 aggregation, and inhibits NLRP3 inflammasome activation. AChE-IN-72 ameliorates memory impairment in Betaine (HY-B0710)-induced AD mouse model. AChE-IN-72 is blood-brain barrier (BBB) penetrable .
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- HY-P2342
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- HY-121191
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N1,N8-Bisnorcymserine; (-)-Bisnorcymserine
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Cholinesterase (ChE)
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Neurological Disease
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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-P2297
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- HY-P2297A
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- HY-157333
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- HY-164507
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Drug Derivative
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Neurological Disease
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NRMA-7 is a BBB-penetrable small molecule nuclear receptor modulator. NRMA-7 can be used in the study of central nervous system diseases .
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- HY-17383A
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Antifolate
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Neurological Disease
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Levomefolate disodium is an orally active, BBB-penetrable and active form of folic acid. Levomefolate disodium can be used as a food supplement for folic acid and in the research of neural tube defect diseases .
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- HY-149253
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Others
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Neurological Disease
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OY-201 is a potential and BBB-penetrated anti-ischemic stroke agent. OY-201 shows the good safety and neuroprotective activity in both in vitro and in vivo models .
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- HY-125602
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Adenosine Receptor
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Neurological Disease
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MNI-444 is a BBB-penetrable ligand of adenosine 2A receptor (A2AR). A2AR is a potential non-dopaminergic target for the research of Parkinson’s disease .
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- HY-119953
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mAChR
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Neurological Disease
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BIBN-99 is a selective, BBB-penetrable and competitive muscarinic M2 receptor antagonist. BIBN-99 improves cognitive performancein rats with traumatic brain injury .
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- HY-155024
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Parasite
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Infection
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HAT-IN-8 (Compound 38) is a BBB-penetrable T. brucei inhibitor (EC50: 0.18 μM). HAT-IN-8 can be used for the research of Human African trypanosomiasis .
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- HY-13909
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HDAC
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Cancer
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RGFP966 is a highly selective HDAC3 inhibitor with an IC50 of 80 nM and shows no inhibition to other HDACs at concentrations up to 15 μM. RGFP966 can penetrate the blood brain barrier (BBB).
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- HY-P10777
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Peptide-Drug Conjugates (PDCs)
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Cancer
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ANG1009 is a BBB-penetrable anticancer agent. ANG1009 is cytotoxic to a variety of tumor cells and can induce cell cycle arrest. ANG1009 can be used in the study of brain cancer .
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- HY-17383
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Antifolate
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Neurological Disease
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Levomefolate calcium is an orally active, BBB-penetrable and active form of folic acid. Levomefolate calcium can be used as a food supplement for folic acid and in the research of neural tube defect diseases .
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- HY-153432
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Cholinesterase (ChE)
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Neurological Disease
Cancer
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TRV-7019 is a BBB-penetrable radioligand for brain imaging that target butyrylcholinesterase. TRV-7019 can be used for the diagnosis of an amyloid disease, multiple sclerosis, a brain tumor, or butyrylcholinesterase activity .
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- HY-145888
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Amyloid-β
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Neurological Disease
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Antioxidant agent-2 (comp 3c), an BBB-penetrated antioxidant agent and a selective metal ions chelator, presents good neuroprotective effect and hepatoprotective effect for the study of Alzheimer’s disease .
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- HY-147681
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FGFR
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Neurological Disease
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SUN13837 is an orally active, potent and BBB-penetrated FGFR (fibroblast growth factor receptor) modulator. SUN13837 shows neuroprotective activity. SUN13837 can be used for neurodegenerative diseases research .
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- HY-168915
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Akt
PKA
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Cancer
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ML-B01 is the orally active inhibitor for Akt and PKA with the IC50 of 2 nM and 136 nM. ML-B01 exhibits good ability to penetrate the blood-brain barrier (BBB) in the mouse brain .
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- HY-153773
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Z4P
3 Publications Verification
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IRE1
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Cancer
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Z4P is a BBB-penetrable IRE1 inhibitor with an IC50 of 1.13 μM. Z4P in combination with Temozolomide (HY-17364) inhibits the growth and recurrence of glioblastoma and has anti-tumor activity .
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- HY-P1178
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Trk Receptor
p38 MAPK
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Neurological Disease
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Cyclotraxin B is a BBB-penetrable and selective TrkB inhibitor. Cyclotraxin B inhibits BDNF-induced TrkB activity in a non-competitive manner, with an IC50 of 0.30 nM. Cyclotraxin B has analgesic and anxiolytic effects .
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- HY-147668
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α-synuclein
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Neurological Disease
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α-Synuclein inhibitor 6 (compound 3ge) is a potent and BBB-penetrated inhibitor of α-Synuclein (α-Syn) aggregation, with an IC50 of 1.70 μM and inhibition ratio at 30 μM of 94.4% .
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- HY-148787
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SAR443820; DNL788
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RIP kinase
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Neurological Disease
Inflammation/Immunology
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Oditrasertib (SAR443820) is an orally active, BBB-penetrable and selective reversible inhibitor of RIPK1. Oditrasertib can be used in the research of chronic inflammatory central nervous system diseases, such as amyotrophic lateral sclerosis and multiple sclerosis .
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- HY-101059
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GABA Receptor
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Neurological Disease
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FGIN 1-27, an indoleacetamide, is a specific peripheral benzodiazepine receptor (PBR) ligand with a Ki of 5.0 nM. FGIN 1-27 can penetrate the blood brain barrier (BBB). FGIN 1-27 inhibits the onset of Isoniazid-induced convulsions .
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- HY-147666
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α-synuclein
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Neurological Disease
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α-Synuclein inhibitor 4 (compound 3gh) is a potent and BBB-penetrated inhibitor of α-Synuclein (α-Syn) aggregation, with an IC50 of 0.98 μM and inhibition ratio at 30 μM of 91.2% .
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- HY-147669
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α-synuclein
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Neurological Disease
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α-Synuclein inhibitor 7 (compound 3gf) is a potent and BBB-penetrated inhibitor of α-Synuclein (α-Syn) aggregation, with an IC50 of 1.95 μM and inhibition ratio at 30 μM of 85.8% .
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- HY-147667
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α-synuclein
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Neurological Disease
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α-Synuclein inhibitor 5 (compound 4aa) is a potent and BBB-penetrated inhibitor of α-Synuclein (α-Syn) aggregation, with an IC50 of 1.22 μM and inhibition ratio at 30 μM of 94.3% .
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- HY-147683
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FGFR
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Neurological Disease
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FGFR-IN-3 (compound 6) is an orally active, potent and BBB-penetrated FGFR (fibroblast growth factor receptor) modulator. FGFR-IN-3 shows neuroprotective activity. FGFR-IN-3 can be used for neurodegenerative diseases research .
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- HY-N12171
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Bacterial
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Infection
Neurological Disease
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Isoreserpiline is an orally active and BBB-penetrable indole alkaloids with antibacterial and antipsychotic activity. Isoreserpiline is even more effective when used in combination with antibiotics and inhibits the activity of bacterial efflux pumps. Isoreserpiline improves Amphetamine-induced hyperactivity in mice .
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- HY-107744
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- HY-143877
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HDAC
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Cancer
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NN-390 is a potent and selective HDAC6 inhibitor, with an IC50 of 9.8 nM. NN-390 penetrates the blood-brain barrier (BBB). NN-390 shows study potential in metastatic Group 3 MB (medulloblastoma) .
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- HY-146313
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Cholinesterase (ChE)
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Neurological Disease
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BChE-IN-7 (compound 13) is a potent, selective, BBB-penetrated and reversible AChE and BChE inhibitor, with an IC50 of 0.06 μM (BChE). BChE-IN-7 can protect neuronal-like cells from toxic Aβ-species .
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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-P1178A
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Trk Receptor
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Neurological Disease
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Cyclotraxin B TFA is a BBB-penetrable and selective TrkB inhibitor. Cyclotraxin B TFA inhibits BDNF-induced TrkB activity in a non-competitive manner, with an IC50 of 0.30 nM. Cyclotraxin B TFA has analgesic and anxiolytic effects .
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- HY-147821
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Cannabinoid Receptor
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Metabolic Disease
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CB1-IN-2 (Compound 4g) is a selective CB1 inhibitor with an IC50 of 0.644 μM. CB1-IN-2 can penetrates BBB and might cause CNS side effect similar with Rimonabant .
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- HY-130630
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mGluR
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Neurological Disease
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mGluR2 modulator 1 (compound 95) is a potent and BBB-penetrated mGluR2 (metabotropic glutamate receptor-2) positive allosteric modulator, with an EC50 of 0.03 μM. mGluR2 modulator 1 can be used for psychosis research .
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- HY-170392
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Drug Derivative
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Cardiovascular Disease
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Vasorelaxant agent-1 (Compound 2j) is a BBB-penetrable vasodilator. Vasorelaxant agent-1 has excellent vasodilator activity with an EC50 of 0.02916 μM. Vasorelaxant agent-1 is non-carcinogenic and can be used in the study of hypertension .
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- HY-151152
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Cholinesterase (ChE)
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Neurological Disease
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AChE-IN-24 is a potent AChE inhibitor and can penetrate the BBB. AChE-IN-24 has the mighty inhibitory activity to hAChE with an IC50 value of 0.053 μM. AChE-IN-24 can be used for the research of Alzheimer s disease (AD) .
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- HY-135714
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EKZ-001
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HDAC
Microtubule/Tubulin
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Neurological Disease
Cancer
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Bavarostat (EKZ-001) is a BBB-penetrable and selective HDAC6 inhibitor (IC50: 0.06 μM). Bavarostat modulates tubulin acetylation selectively over histone acetylation. Bavarostat can be used for research of cancers and central nervous system (CNS) disorders .
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- HY-111136
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GABA Receptor
5-HT Receptor
Dopamine Receptor
Histamine Receptor
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Neurological Disease
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BL-1020 mesylate is the mesylate salt form of BL-1020. BL-1020 mesylate is an antipsychotic agent. BL-1020 mesylate is inhibitor for dopamine receptor and serotonin receptor (5-HT receptor), with Ki of 0.066, 0.062 and 0.21 nM, for D2L, D2S and 5-HT2A receptors, respectively. BL-1020 mesylate is agonist for GABAA receptor with Ki of 3.74 μM, and enhances the GABA release. BL-1020 mesylate exhibits high affinity with histamine receptor (Ki is 0.47 nM). BL-1020 mesylate reduces Amphetamine-induced hyperactivity, with lower catalepsy and sedation. BL-1020 mesylate is blood-brain barrier penetrate .
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- HY-171317
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Bacterial
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Infection
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SMARt751 targets the transcriptional regulatory factor VirS, inhibits its DNA binding ability, upregulates the mymA operon expression, thereby activating Ethionamide (HY-B0276), enhancing the antimicrobial activity of Ethionamide. SMARt751 enhances the antibacterial activity of Ethionamide against M. tuberculosis, reverses the Ethionamide resistance. SMARt751 improves the antibacterial effect of Ethionamide and reduces its effective dose in mouse models. SMARt751 can cross blood brain barrier .
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- HY-173142
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Drug Derivative
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Neurological Disease
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Neuroprotective agent 7 (Compound 13) is a BBB-penetrable neuroprotective agent. Neuroprotective agent 7 has a powerful neuroprotective effect and can reduce the cerebral infarct area in the MCAO rat model. Neuroprotective agent 7 can be used in the research of diseases such as cerebral ischemia .
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- HY-10358
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MK-2206 (2HCl)
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Organoid
Akt
Autophagy
Apoptosis
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Cancer
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MK-2206 dihydrochloride (MK-2206 (2HCl)) is an orally active, BBB-penetrated allosteric AKT inhibitor with IC50s of 5 nM, 12 nM, and 65 nM for AKT1, AKT2, and AKT3, respectively. MK-2206 dihydrochloride induces autophagy .
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- HY-69019A
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NO Synthase
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Cardiovascular Disease
Neurological Disease
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7-Nitroindazole sodium is a selective and BBB-penetrable inhibitor of nitric oxide synthase (NOS). 7-Nitroindazole sodium can inhibit the activity of central NOS with an IC50 of 0.47 μM in the cerebellum of mice. 7-Nitroindazole sodium has anti-injurious and neuroprotective properties .
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- HY-153660
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MC-4R Agonist 2
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Melanocortin Receptor
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Metabolic Disease
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Bivamelagon (MC-4R Agonist 2) is an orally active and BBB-penetrable MC4R agonist with EC50 values of 0.562 nM (Luci assay) and 36.5 nM (cAMP assay), and a Ki of 65 nM. Bivamelagon can be used for the research of diseases such as obesity and diabetes .
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- HY-145833A
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Epoxide Hydrolase
Cholinesterase (ChE)
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Neurological Disease
Cancer
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sEH/AChE-IN-4 (compound (+)-15) is a potent and BBB-penetrated dual inhibitor of sEH (soluble epoxide hydrolase) and AChE (acetylcholinesterase), with IC50 values of 3.1 nM (hsEH), 1660 nM (hAChE), 179 nM (hBChE, human butyrylcholinesterase), 14.5 nM (msEH), and 102 nM (mAChE), respectively .
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- HY-153660A
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MC-4R Agonist 2 hydrochloride
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Melanocortin Receptor
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Metabolic Disease
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Bivamelagon (MC-4R Agonist 2) hydrochloride is an orally active and BBB-penetrable MC4R agonist with EC50 values of 0.562 nM (Luci assay) and 36.5 nM (cAMP assay), and a Ki of 65 nM. Bivamelagon hydrochloride can be used for the research of diseases such as obesity and diabetes .
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- HY-101449
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- HY-117727A
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MIN-102 hydrochloride; Hydroxypioglitazone hydrochloride
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PPAR
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Neurological Disease
Metabolic Disease
Inflammation/Immunology
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Leriglitazone (MIN-102; Hydroxypioglitazone) hydrochloride is an orally active and a BBB-penetrable PPARγ agonist with an EC50 of 9 μM. Leriglitazone hydrochloride, as a regulator of mitochondrial function, has neuroprotective, anti-inflammatory and antioxidant effects. Leriglitazone hydrochloride can be used in the study of neuroinflammatory and neurodegenerative diseases .
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- HY-170798
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Monoamine Oxidase
SOD
Glutathione Peroxidase
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Neurological Disease
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Monoamine Oxidase B inhibitor 6 (Compound BT5) is a BBB-penetrable, highly selective, reversible and competitive MAO-B inhibitor, with an IC50 of 0.11 μM. Monoamine Oxidase B inhibitor 6 has antioxidant and neuroprotective effects and can be used in the research of neurodegenerative diseases .
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- HY-117727
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MIN-102; Hydroxypioglitazone
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PPAR
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Neurological Disease
Metabolic Disease
Inflammation/Immunology
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Leriglitazone (MIN-102; Hydroxypioglitazone) is an orally active and a BBB-penetrable PPARγ agonist with an EC50 of 9 μM. Leriglitazone, as a regulator of mitochondrial function, has neuroprotective, anti-inflammatory and antioxidant effects. Leriglitazone can be used in the study of neuroinflammatory and neurodegenerative diseases .
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- HY-147030
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PARP
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Cancer
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PARP1-IN-8 (compound 11c) is a potent and BBB-penetrated PARP1 inhibitor, with an IC50 of 97 nM. PARP1-IN-8 shows significantly potent anti-proliferative activity against Human lung adenocarcinoma epithelial cell line A549 .
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- HY-P10782
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Peptide-Drug Conjugates (PDCs)
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Cancer
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Pt(IV)-M13 is a BBB-penetrable Platinum (IV) prodrug-perfluoroaryl macrocyclic peptide conjugate. Pt(IV)-M13 is cytotoxic to glioma stem cells and increases uptake of platinum in the brain. Pt(IV)-M13 can be used in the study of glioblastoma .
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- HY-145833
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Epoxide Hydrolase
Cholinesterase (ChE)
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Neurological Disease
Cancer
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sEH/AChE-IN-3 (compound (−)-15) is a potent and BBB-penetrated dual inhibitor of sEH (soluble epoxide hydrolase) and AChE (acetylcholinesterase), with IC50 values of 0.4 nM (hsEH), 1.94 nM (hAChE), 615 (hBChE, human butyrylcholinesterase), 4.3 nM (msEH), and 2.61 nM (mAChE), respectively .
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- HY-169116
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Dopamine Receptor
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Neurological Disease
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D5R agonist 1 (Compound 5j) is a selective, orally active and BBB penetrable D5R partial agonist (EC50: 269.7 nM). D5R agonist 1 enhances the cognition in the Scopolamine (HY-N0296)-induced amnesia model .
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- HY-163369
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HDAC
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Cancer
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HDAC6-IN-35 (compound C4 (ZINC000077541942)) is a potent and BBB-penetrated HDAC6 inhibitor with the IC50 of 4.7 μM. HDAC6-IN-35 shows cell toxicity against MDA-MB-231 with EC50 of 40.6 μM .
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- HY-116820
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Dopamine Receptor
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Neurological Disease
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OS-3-106 is a potent, BBB-penetrated and selective dopamine D3 receptor (D3R) agonist. OS-3-106 binds with high affinity (Ki = 0.2 nM) at the D3R. OS-3-106 can be used for psychoactivator addiction research .
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- HY-17383R
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Reference Standards
Antifolate
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Neurological Disease
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Levomefolate (calcium) (Standard) is the analytical standard of Levomefolate (calcium). This product is intended for research and analytical applications. Levomefolate (calcium) is an orally active, BBB-penetrable and active form of folic acid. Levomefolate (calcium) can be used as a food supplement for folic acid and in the research of neural tube defect diseases .
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- HY-144765
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NF-κB
Apoptosis
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Neurological Disease
Inflammation/Immunology
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NF-κB-IN-4 (compound 17) is a potent and BBB-penetrated NF-κB pathway inhibitor with blood brain barrier (BBB) permeability. NF-κB-IN-4 exhibits potential anti-neuroinflammatory activity with low toxicity. NF-κB-IN-4 can block the activation and phosphorylation of IκBα, reduce expression of NLRP3, and thus inhibit NF-κB activation. NF-κB-IN-4 can be used for neuroinflammation related diseases research .
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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-P2343
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Apoptosis
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Cancer
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BH3 hydrochloride, a BBB penetrated peptide, provoke apoptosis either by direct activation of pro-apoptotic Bax/Bak or by neutralizing anti-apoptotic Bcl-2 proteins (Bcl-2, Bcl-XL, Bcl-w, Mcl-1 and A-1) via their BH3 domian .
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- HY-170945
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iGluR
Serotonin Transporter
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Neurological Disease
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Antidepressant agent 9 (Compound 24) is an orally active and BBB-penetrable NMDAR and SERT inhibitor with IC50 values of 3.50 μM and 1044 nM, respectively. Antidepressant agent 9 has good metabolic stability and plasma exposure. Antidepressant agent 9 can exert antidepressant-like activity in the mouse forced swim test .
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- HY-132310
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MAGL
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Neurological Disease
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MAGL-IN-4 is an orally active, selective and reversible monoacylglycerol lipase (MAGL) inhibitor with an IC50 of 6.2 nM. MAGL-IN-4 can penetrate the blood-brain barrier (BBB). MAGL-IN-4 enhances endocannabinoid signaling mostly by the increase in the level of 2-AG via selective MAGL inhibition in the brain .
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- HY-P3223
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Opioid Receptor
|
Neurological Disease
|
|
Biphalin TFA, a BBB-penetrable opioid peptide analog, contains two active enkephalin pharmacophores. Biphalin TFA has high affinity for opioid receptors. Biphalin TFA shows analgesic effect in acute, neuropathic, and chronic animal pain models. Biphalin TFA is also an antiviral, antiproliferative, anti-inflammatory, and neuroprotective agent .
|
-
- HY-P99694
-
|
JR-171
|
Transferrin Receptor
|
Neurological Disease
|
|
Lepunafusp alfa (JR-171) is a BBB-penetrable fusion protein consisting of J-Brain Cargo and IDUA (a lysosomal enzyme, α-L-iduronidase). Lepunafusp alfa can reduce concentration of heparan sulfate (HS) and dermatan sulfate (DS). Lepunafusp alfa can be used for research of mucopolysaccharidosis type I .
|
-
- HY-P10861
-
|
|
Tau Protein
|
Neurological Disease
|
|
RI-AG03 is an orally active and a BBB-penetrable Tau aggregation peptide inhibitor. RI-AG03 inhibits Tau aggregation and improves associated neurodegeneration and behavioral phenotypes in both in vivo and in vitro models. RI-AG03 can be used in the study of tauopathies such as Alzheimer's disease .
|
-
- HY-147684
-
|
|
FGFR
|
Neurological Disease
|
|
FGFR-IN-7 (compound 17) is an orally active, potent and BBB-penetrated FGFR (fibroblast growth factor receptor) modulator. FGFR-IN-7 shows neuroprotective activity. FGFR-IN-7 improves brain exposure and reduced risk of phospholidosis. FGFR-IN-7 can be used for neurodegenerative diseases research .
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-
- HY-B1715
-
|
ISF2522
|
GABA Receptor
NO Synthase
|
Neurological Disease
Inflammation/Immunology
|
|
Oxiracetam (ISF2522) is an orally active and a BBB-penetrable cyclic derivative of γ-aminobutyric acid (GABA). Oxiracetam reaches the hippocampus and cerebral cortex in high concentrations. Oxiracetam can promote cognitive function and regulate inflammatory response, with powerful neuroprotective effects. Oxiracetam can be used in the study of central nervous system diseases .
|
-
- HY-157400
-
|
|
Monoamine Oxidase
|
Neurological Disease
|
|
hMAO-B-IN-7 (compound 11n) is a potent and blood–brain barrier (BBB) penetrable inhibitor of human monoamine oxidase-B (hMAO-B), with the IC50 value of 0.79±0.05 μM. hMAO-B-IN-7 can be used for Alzheimer’s disease (AD) and Parkinson’s disease (PD) research .
|
-
- HY-B0553
-
-
- HY-P1146
-
|
|
Amyloid-β
|
Cardiovascular Disease
Neurological Disease
Inflammation/Immunology
|
|
Semax is a BBB-penetrable adrenocorticotropic hormone-like peptide and can form stable complexes with Cu 2+. Semax is a synthetic peptide analog of Adrenocorticotropic hormone (ACTH) (4-10). Semax has immunomodulatory, nootropic and neuroprotective activities. Semax can be used in the research of central nervous system diseases such as Alzheimer's disease and cerebral ischemia .
|
-
- HY-147748
-
|
|
COX
|
Inflammation/Immunology
|
|
COX-2-IN-17 (compound 10) is a potent and BBB-penetrated COX-2 (cyclooxygenase-2) inhibitor, with an IC50 of 0.02 μM. COX-2-IN-17 shows anti-inflammatory and analgesic activities. COX-2-IN-17 attenuates hyperalgesia in the neurogenic phase as well as the inflammatory phase .
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-
- HY-101059R
-
|
|
GABA Receptor
Reference Standards
|
Neurological Disease
|
|
FGIN 1-27 (Standard) is the analytical standard of FGIN 1-27. This product is intended for research and analytical applications. FGIN 1-27, an indoleacetamide, is a specific peripheral benzodiazepine receptor (PBR) ligand with a Ki of 5.0 nM. FGIN 1-27 can penetrate the blood brain barrier (BBB). FGIN 1-27 inhibits the onset of Isoniazid-induced convulsions .
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- HY-P1146A
-
|
|
Amyloid-β
|
Cardiovascular Disease
Neurological Disease
Inflammation/Immunology
|
|
Semax acetate is a BBB-penetrable adrenocorticotropic hormone-like peptide and can form stable complexes with Cu 2+. Semax acetate is a synthetic peptide analog of Adrenocorticotropic hormone (ACTH) (4-10). Semax acetate has immunomodulatory, nootropic and neuroprotective activities. Semax acetate can be used in the research of central nervous system diseases such as Alzheimer's disease and cerebral ischemia .
|
-
- HY-170905S
-
-
- HY-124813
-
|
113B7
|
FAK
EGFR
MMP
|
Cancer
|
|
PDZ1i is a potent, BBB-penetrated and specific MDA-9/Syntenin inhibitor. PDZ1i inhibits crucial GBM (glioblastoma multiforme) signaling involving FAK and EGFRvIII. PDZ1i reduces MMP secretion. PDZ1i can improve survival of brain tumor-bearing mice and reduce tumor invasion .
|
-
- HY-12678
-
|
NMS-E628; RXDX-101
|
ROS Kinase
Trk Receptor
Anaplastic lymphoma kinase (ALK)
Autophagy
|
Cancer
|
|
Entrectinib (NMS-E628) is an orally active, BBB-penetrated and centrally active inhibitor of TrkA/B/C, ROS1 and ALK, with IC50 values of 1, 3, 5, 12 and 7 nM, respectively. Entrectinib induces apoptosis and cycle arrest in cancer cells, has antitumor activity, and attenuates bleomycin-induced lung fibrosis in mice .
|
-
- HY-109502S
-
|
|
Isotope-Labeled Compounds
|
Neurological Disease
|
|
10-OH-NBP-d4 is deuterium labeled 10-OH-NBP. 10-OH-NBP is a Butylphthalide (3-n-Butylphthalide; NBP; HY-B0647) hydroxylated metabolite and can penetrates the blood-brain barrier (BBB). Butylphthalide exerts neuroprotective effects and has potential for cerebral ischemia research .
|
-
- HY-D2268
-
|
|
Fluorescent Dye
Amyloid-β
|
Neurological Disease
|
|
QM-FN-SO3 is a BBB-penetrable near-infrared (NIR) aggregation-induced emission (AIE)-active probe for Aβ plaques. QM-FN-SO3 can be used for in vivo detection of Aβ plaques. QM-FN-SO3 has ultra-high S/N ratio, binding affinity, and high-performance NIR emission .
|
-
- HY-B0602
-
|
O-Desmethylvenlafaxine
|
Serotonin Transporter
|
Neurological Disease
|
|
Desvenlafaxine, the succinate salt form of the isolated major active metabolite of Venlafaxine (HY-B0196), is an orally active and BBB penetrated 5-HT and norepinephrine reuptake inhibitor, with IC50 values of 47.3 nM and 531.3 nM for hSERT and hNET, respectively. Desvenlafaxine shows weak binding affinity (62% inhibition at 100 μM) at the human dopamine (DA) transporter .
|
-
- HY-W004425
-
|
3,7-Dimethyl-1-propargylxanthine
|
Adenosine Receptor
|
Neurological Disease
|
|
DMPX (3,7-Dimethyl-1-propargylxanthine) is a BBB-penetrable caffeine analogue. DMPX is A2 selective adenosine receptor (AR) antagonist that strongly and selectively blocks hypothermia and behavioral inhibition induced by A2 adenosine receptor agonists such as NECA (HY-103173). DMPX can be used in the study of Parkinson's disease and other diseases .
|
-
- HY-147697
-
|
|
Histone Demethylase
TNF Receptor
|
Inflammation/Immunology
Cancer
|
|
LSD1-IN-21 (compound 5a) is a potent and BBB-penetrated LSD1 (Lysine specific demethylase-1) inhibitor, with an IC50 of 0.956 µM. LSD1-IN-21 significantly reduces the pro-inflammatory cytokine TNF-α. LSD1-IN-21 shows good anticancer and anti-inflammatory activity .
|
-
- HY-146315
-
|
|
Cholinesterase (ChE)
Monoamine Oxidase
|
Neurological Disease
|
|
AChE/BChE-IN-6 (compound 22) is a potent dual AChE/BChE inhibitor with IC50 values of 0.809 µM, 2.248 µM and > 100 µM for hBChE, hAChE and hMAO-B, respectively. AChE/BChE-IN-6 penetrates the blood-brain barrier (BBB). AChE/BChE-IN-6 can be used for Alzheimer’s disease (AD) research .
|
-
- HY-117727S
-
|
MIN-102-d4; Hydroxypioglitazone-d4
|
Isotope-Labeled Compounds
PPAR
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
|
|
Leriglitazone-d4 (MIN-102-d4; Hydroxypioglitazone-d4) is deuterium labeled Leriglitazone. Leriglitazone is an orally active and a BBB-penetrable PPARγ agonist with an EC50 of 9 μM. Leriglitazone, as a regulator of mitochondrial function, has neuroprotective, anti-inflammatory and antioxidant effects. Leriglitazone can be used in the study of neuroinflammatory and neurodegenerative diseases .
|
-
- HY-16170
-
|
O-Desmethylvenlafaxine succinate; Wy-45233 succinate
|
Serotonin Transporter
|
Neurological Disease
Metabolic Disease
|
|
Desvenlafaxine succinate, the succinate salt form of the isolated major active metabolite of Venlafaxine (HY-B0196), is an orally active and BBB penetrated 5-HT and norepinephrine reuptake inhibitor, with IC50 values of 47.3 nM and 531.3 nM for hSERT and hNET, respectively. Desvenlafaxine succinate (DVS) shows weak binding affinity (62% inhibition at 100 μM) at the human dopamine (DA) transporter .
|
-
- HY-137262
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
Protein deglycase DJ-1 against-1, a DJ-1-binding compound, dependently targets DJ1. Protein deglycase DJ-1 against-1 penetrates through the blood brain barrier (BBB). Protein deglycase DJ-1 against-1 is used as a neuroprotective agent and has the potential for Parkinson's disease research .
|
-
- HY-N1501
-
|
|
α-synuclein
|
Cardiovascular Disease
Neurological Disease
Inflammation/Immunology
|
|
Beta-asarone is an orally active and BBB-penetrable anti-inflammatory agent and neuroprotective agent, which is the major ingredient of Acorus tatarinowii Schott. Beta-asarone can protect nerve cells from apoptosis and autophagy, inhibit expression of α-synuclein, as well as myocardial protection. Beta-asarone can be used in the study of neurological and cardiovascular diseases .
|
-
- HY-144898
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
SB-216 is an BBB-penetrable tubulin polymerization inhibitor. SB-216 can inhibit the proliferation and migration, and induce apoptosis and cell cycle arrest of tumor cells. SB-216 has good in vivo metabolic stability and low toxicity, but its oral bioavailability is limited. SB-216 has antitumor activity and can be used in the research of tumors such as melanoma .
|
-
- HY-146347
-
|
|
Monoamine Oxidase
Amyloid-β
|
Neurological Disease
|
|
MAO-B-IN-10 (compound 4f) is a potent, selective, BBB-penetrated MAO-B (monoamine oxidase-B) inhibitor, with IC50 of 5.3 μM. MAO-B-IN-10 can inhibit (58.2%) and disaggregate (43.3%) self-mediated Aβ (amyloid β) aggregation. MAO-B-IN-10 can be use for Alzheimer’s disease research .
|
-
- HY-B0602A
-
|
O-Desmethylvenlafaxine succinate hydrate; Desvenlafaxine succinate monohydrate
|
Serotonin Transporter
|
Neurological Disease
|
|
Desvenlafaxine succinate hydrate, the succinate salt form of the isolated major active metabolite of Venlafaxine (HY-B0196), is an orally active and BBB penetrated 5-HT and norepinephrine reuptake inhibitor, with IC50 values of 47.3 nM and 531.3 nM for hSERT and hNET, respectively. Desvenlafaxine succinate hydrate shows weak binding affinity (62% inhibition at 100 μM) at the human dopamine (DA) transporter .
|
-
- HY-147027
-
|
|
PARP
Caspase
Apoptosis
|
Cancer
|
|
PARP-1-IN-2 (compound 11g) is a potent and BBB-penetrated PARP1 inhibitor, with an IC50 of 149 nM. PARP1-IN-2 shows significantly potent anti-proliferative activity against Human lung adenocarcinoma epithelial cell line A549. PARP1-IN-2 can induce A549 cells apoptosis .
|
-
- HY-107531
-
|
|
GSK-3
|
Neurological Disease
Cancer
|
|
A 1070722 is a potent and selective glycogen synthase kinase 3 (GSK-3) inhibitor, with a Ki of 0.6 nM for both GSK-3α and GSK-3β. A 1070722 can penetrate the blood-brain barrier (BBB) and accumulates in brain regions, thus potential for PET radiotracer for the quantification of GSK-3 in brain. A 1070722 decreases spontaneous locomotion .
|
-
- HY-168494
-
|
|
iGluR
|
Neurological Disease
|
|
GluN2A Allosteric modulator 1 (Compound 11) is an orally active, BBB-penetrable and highly selective GluN2A negative allosteric modulator. GluN2A Allosteric modulator 1 has IC50 values of 0.042 μM and 13 μM for GluN2A and GluN2B, respectively. GluN2A Allosteric modulator 1 can be used for the research of nervous system diseases .
|
-
- HY-19939S
-
VX-984
4 Publications Verification
M9831
|
DNA-PK
|
Cancer
|
|
VX-984 is an orally active, potent, selective and BBB-penetrated DNA-PK inhibitor. VX-984 efficiently inhibits NHEJ (non-homologous end joining) and increases DSBs (DNA double-strand breaks). VX-984 can be used for glioblastomas (GBM) and non-small cell lung cancer (NSCLC) research. VX-984 is a de novo deuterium .
|
-
- HY-B1715R
-
|
ISF2522 (Standard)
|
Reference Standards
GABA Receptor
NO Synthase
|
Neurological Disease
Inflammation/Immunology
|
|
Oxiracetam (Standard) is the analytical standard of Oxiracetam. This product is intended for research and analytical applications. Oxiracetam (ISF2522) is an orally active and a BBB-penetrable cyclic derivative of γ-aminobutyric acid (GABA). Oxiracetam reaches the hippocampus and cerebral cortex in high concentrations. Oxiracetam can promote cognitive function and regulate inflammatory response, with powerful neuroprotective effects. Oxiracetam can be used in the study of central nervous system diseases .
|
-
- HY-107566
-
|
|
Histamine Receptor
Parasite
MDM-2/p53
NF-κB
FOXO
Bacterial
|
Infection
Neurological Disease
|
|
Conessine is an orally active and BBB-penetrable selective histamine H3 receptor antagonist. The pKi values of Conessine for rat and human H3 receptors are 7.61 and 8.27, respectively. Conessine is an inhibitor of the multidrug efflux pump system in Pseudomonas aeruginosa and can enhance the activity of antibiotics. Conessine has antimalarial activity. Conessine can also be used in the research of muscle atrophy .
|
-
- HY-D2268A
-
|
|
Amyloid-β
Fluorescent Dye
|
Neurological Disease
|
|
QM-FN-SO3 ammonium is a BBB-penetrable near-infrared (NIR) aggregation-induced emission (AIE)-active probe for Aβ plaques. QM-FN-SO3 ammonium can be used for in vivo detection of Aβ plaques. QM-FN-SO3 ammonium has ultra-high S/N ratio, binding affinity, and high-performance NIR emission .
|
-
- HY-B0553R
-
-
- HY-115681
-
|
6-Prenylnaringenin; (±)-6-Prenylnaringenin
|
Calcium Channel
|
Neurological Disease
|
|
(2R/S)-6-PNG (6-Prenylnaringenin) is a potent and reversible Cav3.2 T-type Ca 2+ channels (T-channels) blocker. (2R/S)-6-PNG can penetrate the blood-brain barrier (BBB). (2R/S)-6-PNG suppresses neuropathic and visceral pain in mice .
|
-
- HY-69019
-
|
|
NO Synthase
|
Cardiovascular Disease
Neurological Disease
|
|
7-Nitroindazole is a selective and BBB-penetrable inhibitor of nitric oxide synthase (NOS) (IC50 = 0.47 μM in mouse cerebellum). 7-Nitroindazole does not affect blood pressure or endothelium-dependent relaxation while inhibiting nNOS in experimental animals. 7-Nitroindazole has anti-injurious and neuroprotective properties, and can be studied in research for neurological diseases such as Parkinson’s disease .
|
-
- HY-B0602S3
-
|
|
Isotope-Labeled Compounds
Serotonin Transporter
|
Neurological Disease
|
|
Desvenlafaxine-d10 is deuterium labeled Desvenlafaxine. Desvenlafaxine, the succinate salt form of the isolated major active metabolite of Venlafaxine (HY-B0196), is an orally active and BBB penetrated 5-HT and norepinephrine reuptake inhibitor, with IC50 values of 47.3 nM and 531.3 nM for hSERT and hNET, respectively. Desvenlafaxine shows weak binding affinity (62% inhibition at 100 μM) at the human dopamine (DA) transporter .
|
-
- HY-B0602S2
-
|
|
Isotope-Labeled Compounds
Serotonin Transporter
|
Neurological Disease
|
|
Desvenlafaxine-d6 is deuterium labeled Desvenlafaxine. Desvenlafaxine, the succinate salt form of the isolated major active metabolite of Venlafaxine (HY-B0196), is an orally active and BBB penetrated 5-HT and norepinephrine reuptake inhibitor, with IC50 values of 47.3 nM and 531.3 nM for hSERT and hNET, respectively. Desvenlafaxine shows weak binding affinity (62% inhibition at 100 μM) at the human dopamine (DA) transporter .
|
-
- HY-12678R
-
|
|
ROS Kinase
Trk Receptor
Anaplastic lymphoma kinase (ALK)
Autophagy
|
Cancer
|
|
Entrectinib (Standard) is the analytical standard of Entrectinib. This product is intended for research and analytical applications. Entrectinib (NMS-E628) is an orally active, BBB-penetrated and centrally active inhibitor of TrkA/B/C, ROS1 and ALK, with IC50 values of 1, 3, 5, 12 and 7 nM, respectively. Entrectinib induces apoptosis and cycle arrest in cancer cells, has antitumor activity, and attenuates bleomycin-induced lung fibrosis in mice .
|
-
- HY-160761
-
|
|
Opioid Receptor
|
Inflammation/Immunology
|
|
K-Opioid receptor agonist-1 (Compound 5a) is an agonist for κ-Opioid receptor with Ki of 0.25 nM and EC50 of 2 nM. K-Opioid receptor agonist-1 is blood brain barrier (BBB) penetrate (brain/plasma ratios of 0.50 to 0.65). K-Opioid receptor agonist-1 exhibits anti-inflammatory activity in dermatitis models induced by Arachidonic acid (HY-109590) or oxazolidinone .
|
-
- HY-161846
-
|
|
Tyrosinase
|
Neurological Disease
|
|
Tyrosinase-IN-31 (compound 2-06) is a central-targeting tyrosinase inhibitor (tyrosinase: monophenolase IC50=70.44 μM, diphenolase IC50=1.89 μM). Tyrosinase-IN-31 can inhibit the tyrosinase and melanogenesis. Tyrosinase-IN-31 can penetrate the BBB and enter the central nervous system (CNS). Tyrosinase-IN-31 shows neuroprotective effects and Parkinsonism behavior improving function .
|
-
- HY-107566A
-
|
|
Histamine Receptor
Parasite
MDM-2/p53
NF-κB
FOXO
Bacterial
|
Infection
Neurological Disease
|
|
Conessine dihydrobromide is an orally active and BBB-penetrable selective histamine H3 receptor antagonist. The pKi values of Conessine dihydrobromide for rat and human H3 receptors are 7.61 and 8.27, respectively. Conessine dihydrobromide is an inhibitor of the multidrug efflux pump system in Pseudomonas aeruginosa and can enhance the activity of antibiotics. Conessine dihydrobromide has antimalarial activity. Conessine dihydrobromide can also be used in the research of muscle atrophy .
|
-
- HY-B0602R
-
|
|
Serotonin Transporter
|
Neurological Disease
|
|
Desvenlafaxine (Standard) is the analytical standard of Desvenlafaxine. This product is intended for research and analytical applications. Desvenlafaxine, the succinate salt form of the isolated major active metabolite of Venlafaxine (HY-B0196), is an orally active and BBB penetrated 5-HT and norepinephrine reuptake inhibitor, with IC50 values of 47.3 nM and 531.3 nM for hSERT and hNET, respectively. Desvenlafaxine shows weak binding affinity (62% inhibition at 100 μM) at the human dopamine (DA) transporter .
|
-
- HY-146679
-
|
|
HDAC
Amyloid-β
Cholinesterase (ChE)
|
Neurological Disease
|
|
HDAC6-IN-6 (compound 6a) is a potent and BBB-penetrated HDAC6 inhibitor, with an IC50 of 0.025 μM. HDAC6-IN-6 exhibits strong inhibitory activity against Aβ1-42 self-aggregation and AChE, with IC50 values of 3.0 and 0.72 μM. HDAC6-IN-6 can enhance neurite outgrowth without significant neurotoxicity .
|
-
- HY-152671
-
|
|
Monoamine Oxidase
|
Neurological Disease
|
|
hMAO-B-IN-4 (compound B10) is a selective, reversible and blood–brain barrier (BBB) penetrable human monoamine oxidase-B (hMAO-B) inhibitor with an IC50 value and a Ki value of 0.067 and 0.03 μM, respectively. hMAO-B-IN-4 inhibits hMAO-A with an IC50 value of 33.82 μM. hMAO-B-IN-4 can be used for Alzheimer’s disease (AD) and Parkinson’s disease (PD) research .
|
-
- HY-108327
-
|
|
Potassium Channel
|
Neurological Disease
|
|
PF-05020182 is an orally active opener for Kv7 channel, that activates human Kv7.2/7.3, Kv7.4 and Kv7.3/7.5 with EC50 of 334, 625 and 588 nM, respectively. PF-05020182 exhibits anticonvulsant activity in rats corneal electric shock-induced tonic seizure (MES) models. PF-05020182 is blood-brain barrier (BBB) penetrable .
|
-
- HY-146678
-
|
|
HDAC
Amyloid-β
Cholinesterase (ChE)
|
Neurological Disease
|
|
HDAC6-IN-5 (compound 11b) is a potent and BBB-penetrated HDAC6 inhibitor, with an IC50 of 0.025 μM. HDAC6-IN-5 exhibits strong inhibitory activity against Aβ1-42 self-aggregation and AChE, with IC50 values of 3.0 and 0.72 μM. HDAC6-IN-5 can enhance neurite outgrowth without significant neurotoxicity .
|
-
- HY-173515
-
|
|
FAK
|
Cancer
|
|
FAK-IN-26 is a BBB-penetrable Focal Adhesion Kinase (FAK) inhibitor (IC50: 0.87 nM). FAK-IN-26 significantly suppresses tumor cell viability, cancer stem cell activity, and cell migration in A549 and SKOV-3 cell lines. FAK-IN-26 has potent anti-cancer activity in A549 and SKOV-3 tumor mice models with tumor inhibition rates of 59.15 % and 57.9 % .
|
-
- HY-N2426R
-
|
|
Interleukin Related
|
Inflammation/Immunology
|
|
Desvenlafaxine (Standard) is the analytical standard of Desvenlafaxine. This product is intended for research and analytical applications. Desvenlafaxine, the succinate salt form of the isolated major active metabolite of Venlafaxine (HY-B0196), is an orally active and BBB penetrated 5-HT and norepinephrine reuptake inhibitor, with IC50 values of 47.3 nM and 531.3 nM for hSERT and hNET, respectively. Desvenlafaxine shows weak binding affinity (62% inhibition at 100 μM) at the human dopamine (DA) transporter .
|
-
- HY-147851
-
|
|
Beta-secretase
|
Neurological Disease
|
|
BACE1-IN-12 (compound 7g) is a potent and BBB-penetrated BACE1 inhibitor, with an IC50 of 8.9 µM. BACE1-IN-12 shows selective BuChE (butyrylcholinesterase) inhibitory activity with an IC50 of 3.2 µM. BACE1-IN-12 shows effective antioxidant effect with an IC50 of 10.2 μM (DPPH). BACE1-IN-12 might be served as a potential anti-Alzheimer agent .
|
-
- HY-17412A
-
-
- HY-15113
-
|
|
Prolyl Endopeptidase (PREP)
|
Neurological Disease
Cancer
|
|
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) .
|
-
- HY-170417
-
|
|
Cholinesterase (ChE)
GSK-3
|
Neurological Disease
|
|
hAChE/hBuChE/GSK-3β-IN-1 (Compound 6c) is a BBB-penetrable and multi-target anti-Alzheimer's disease compound. hAChE/hBuChE/GSK-3β-IN-1 is the inhibitors of hAChE (IC50: 28.88 nM), hBuChE (IC50: 131.90 nM) and GSK-3β (IC50: 51.42 nM). hAChE/hBuChE/GSK-3β-IN-1 is the tau and Aβ protein aggregation inhibitors .
|
-
- HY-15113A
-
|
|
Prolyl Endopeptidase (PREP)
|
Neurological Disease
Cancer
|
|
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) .
|
-
- HY-N1501R
-
|
|
α-synuclein
Reference Standards
|
Cardiovascular Disease
Neurological Disease
Inflammation/Immunology
|
|
Beta-asarone (Standard) is the analytical standard of Beta-asarone. This product is intended for research and analytical applications. Beta-asarone is an orally active and BBB-penetrable anti-inflammatory agent and neuroprotective agent, which is the major ingredient of Acorus tatarinowii Schott. Beta-asarone can protect nerve cells from apoptosis and autophagy, inhibit expression of α-synuclein, as well as myocardial protection. Beta-asarone can be used in the study of neurological and cardiovascular diseases .
|
-
- HY-162573
-
|
|
Monoamine Oxidase
|
Neurological Disease
|
|
Monoamine Oxidase B inhibitor 5 (Compound 16d) is a selective and reversible inhibitor for monoamine oxidase B (hMAO-B) with an IC50 of 67.3 nM and a Ki of 82.5 nM. Monoamine Oxidase B inhibitor 5 exhibits good pharmacokinetic characters and weak toxicity in rats model. Monoamine Oxidase B inhibitor 5 alleviates MPTP-induced (HY-15608) motor impairment in Parkinson’s mouse model. Monoamine Oxidase B inhibitor 5 is blood-brain barrier (BBB) penetrate .
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- HY-17412
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-
- HY-12678S
-
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NMS-E628-d4; RXDX-101-d4
|
ROS Kinase
Trk Receptor
Anaplastic lymphoma kinase (ALK)
Autophagy
Isotope-Labeled Compounds
|
Cancer
|
|
Entrectinib-d4 (NMS-E628-d4; RXDX-101-d4) is the deuterium labeled Entrectinib (HY-12678). Entrectinib is an orally active, BBB-penetrated and centrally active inhibitor of TrkA/B/C, ROS1 and ALK, with IC50 values of 1, 3, 5, 12 and 7 nM, respectively. Entrectinib induces apoptosis and cycle arrest in cancer cells, has antitumor activity, and attenuates bleomycin-induced lung fibrosis in mice .
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- HY-173307
-
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Keap1-Nrf2
Apoptosis
Reactive Oxygen Species
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Cardiovascular Disease
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Nrf2 activator 19 is a BBB-penetrable NRF2/HO-1 activator. Nrf2 activator 19 exerts potent antioxidant and neuroprotective effects. Nrf2 activator 19 can also effectively reduce brain damage, reduce Reactive Oxygen Species (ROS) accumulation. Nrf2 activator 19 inhibits neuronal apoptosis. Nrf2 activator 19 promotes the recovery of neurological function and motor ability. Nrf2 activator 19 shows significant potential in ischemic stroke research .
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- HY-147859
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Amyloid-β
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Neurological Disease
|
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BChE-IN-8 (compound 20) is an orally active, potent and BBB-penetrated BChE (butyrylcholinesterase) inhibitor, with IC50 values of 0.15 nM (eqBChE, equine serum BChE) and 45.2 nM (hBChE), respectively. High stability of BChE-IN-8 contributes to significantly improved blood concentration and tissue exposure. BChE-IN-8 can exert neuro-protecting and cognition improving properties through multiple modulations, including cholinergic system, Aβ aggregation, neuropeptide levels. BChE-IN-8 can be used for Alzheimer's disease (AD) research .
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- HY-138669
-
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PROTACs
Tau Protein
|
Neurological Disease
|
|
C004019 is a BBB-penetrable and small-molecule PROTAC that targets tau. C004019 can simultaneously recruit tau and E3 ligase, and effectively clear tau proteins by promoting the ubiquitination and proteasome-dependent degradation of tau, thereby improving synaptic and cognitive functions in Alzheimer's disease (AD) mice. C004019 can be used in the research of AD and tau protein-related diseases. (Pink: Ligand for target protein (HY-138679); Black: linker (HY-140189); Blue: E3 Ligase Ligand (HY-138678))
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- HY-17412R
-
-
- HY-W654013
-
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Isotope-Labeled Compounds
Apoptosis
Potassium Channel
Antibiotic
Bacterial
MDM-2/p53
HIF/HIF Prolyl-Hydroxylase
Calcium Channel
|
Infection
|
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Minocycline-d7 is deuterium labeled Minocycline. Minocycline is an orally active, potent and BBB-penetrated semi-synthetic tetracycline antibiotic. Minocycline is a hypoxia-inducible factor (HIF)-1α inhibitor. Minocycline shows anti-cancer, anti-inflammatory, and glutamate antagonist effects. Minocycline reduces glutamate neurotransmission and shows neuroprotective properties and antidepressant effects. Minocycline inhibits bacterial protein synthesis through binding with the 30S subunit of the bacterial ribosome, resulting in a bacteriostatic effect .
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- HY-146691
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Monoamine Oxidase
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Neurological Disease
|
|
hMAO-B-IN-2 (compound 6j) is an orally active, potent, selective and BBB penetrated and competitive reversible hMAO-B inhibitor, with an IC50 of 4 nM. hMAO-B-IN-2 shows low toxicity and good neuroprotective effects in SH-SY5Y cell. hMAO-B-IN-2 can be used for alzheimer’s disease research . hMAO-B-IN-2 is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-172887
-
|
|
Potassium Channel
|
Neurological Disease
|
|
Kv7.2/Kv7.3 activator-2 is a BBB-penetrable Kv7.2/7.3 activator (EC50: 0.25 μM). Kv7.2/Kv7.3 activator-2 has good photostability. Kv7.2/Kv7.3 activator-2 has potently antiepileptic effects in maximal electroshock (MES) and sc-pentylenetetrazol (sc-PTZ)-induced acute mice seizure models .
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- HY-170994
-
|
|
Imidazoline Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
I2-IRs ligand-1 (Compound 12d) is an orally active and BBB-penetrable compound. I2-IRs ligand-1 has a high affinity for imidazoline I2 receptors (I2-IRs) (pKi: 9.98). I2-IRs ligand-1 can improve cognitive impairment in senescent mice and exhibits analgesic, anti-inflammatory, and neuroprotective activities. I2-IRs ligand-1 can be used for the research of Alzheimer's disease and related pain disorders .
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-
- HY-173369
-
|
|
MAGL
Ligands for E3 Ligase
|
Cancer
|
|
PROTAC MAGL degrader-1 is an orally active PROTAC agent that simultaneously targets monoacylglycerol lipase (MAGL) and E3 ubiquitin ligase MDM2. PROTAC MAGL degrader-1 degrades MAGL and inhibits the binding of MDM2 to p53. PROTAC MAGL degrader-1 can partially penetrate the blood-brain barrier (BBB). PROTAC MAGL degrader-1 induces glioblastoma stem cells (GSCs) apoptosis. (E3 ligase ligand: HY-128837; target protein ligand + linker: HY-173370; target protein inhibitor: HY-15249) .
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-
- HY-115681R
-
|
|
Calcium Channel
|
Neurological Disease
|
|
(2R/S)-6-PNG (Standard) is the analytical standard of (2R/S)-6-PNG. This product is intended for research and analytical applications. (2R/S)-6-PNG (6-Prenylnaringenin) is a potent and reversible Cav3.2 T-type Ca2+ channels (T-channels) blocker. (2R/S)-6-PNG can penetrate the blood-brain barrier (BBB). (2R/S)-6-PNG suppresses neuropathic and visceral pain in mice .
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- HY-155365
-
|
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Cholinesterase (ChE)
GSK-3
Amyloid-β
|
Neurological Disease
|
|
hAChE-IN-5 (compound 49) is a potent hAChE and hBuChE inhibitor with IC50 values of 0.17 μM and 0.17 μM, respectively. hAChE-IN-5 shows potent GSK3β inhibition with an IC50 value of 0.21 μM. hAChE-IN-5 is used as tau protein aggregation and Aβ1-42 self-aggregation inhibitor. hAChE-IN-5 can bind virtually with the PAS affecting Aβ aggregation, thus preventing Aβ-dependent neurotoxicity. hAChE-IN-5 can penetrate BBB and has the potential for multi-targeted anti-Alzheimer's agents research .
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- HY-146314
-
|
|
Monoamine Oxidase
Amyloid-β
|
Neurological Disease
|
|
MAO-B-IN-9 (compound 16) is a potent, selective, BBB-penetrated, irreversible and time-dependent MAO-B (monoamine oxidase B) inhibitor, with an IC50 of 0.18 μM. MAO-B-IN-9 prevents Aβ1-42-induced neuronal cell death. MAO-B-IN-9 shows neuroprotective effects, which may be the result of its Aβ1-42 anti-aggregation effects . MAO-B-IN-9 is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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-
- HY-124832
-
|
|
Caspase
Amyloid-β
|
Neurological Disease
|
|
δ-Secretase inhibitor 11 (compound 11) is an orally active, potent, BBB-penetrated, non-toxic, selective and specific δ-secretase inhibitor, with an IC50 of 0.7 μM. δ-Secretase inhibitor 11 interacts with both the active site and allosteric site of δ-secretase. δ-Secretase inhibitor 11 attenuates tau and APP (amyloid precursor protein) cleavage. δ-Secretase inhibitor 11 ameliorates synaptic dysfunction and cognitive impairments in tau P301S and 5XFAD transgenic mouse models. δ-Secretase inhibitor 11 can be used for Alzheimer's disease research .
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-
- HY-155330
-
|
|
5-HT Receptor
Monoamine Oxidase
|
Neurological Disease
|
|
PZ-1922 (Compound 16) is a BBB-penetrable 5-HT6R/5-HT3R antagonist (Ki: 17 nM, 0.45 nM for 5-HT6R/5-HT3R respectively). PZ-1922 reversibly inhibits MAO-B (pIC50: 8.93). PZ-1922 reverses Scopolamine (SCOP) (HY-N0296) induced memory deficits in the novel object recognition (NOR) test in rats. PZ-1922 prevents Aβ-induced memory decline in the T-maze test .
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- HY-155330A
-
|
|
5-HT Receptor
Monoamine Oxidase
|
Neurological Disease
|
|
PZ-1922 free base is a BBB-penetrable 5-HT6R/5-HT3R antagonist (Ki: 17 nM, 0.45 nM for 5-HT6R/5-HT3R respectively). PZ-1922 free base reversibly inhibits MAO-B (pIC50: 8.93). PZ-1922 free base reverses Scopolamine (SCOP) (HY-N0296) induced memory deficits in the novel object recognition (NOR) test in rats. PZ-1922 free base prevents Aβ-induced memory decline in the T-maze test .
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-
- HY-150537
-
|
|
Cholinesterase (ChE)
GSK-3
Microtubule/Tubulin
ROS Kinase
|
Neurological Disease
|
|
AChE/GSK-3β-IN-1 (compound GT15) is a potent, dual AChE/GSK-3β inhibitor with IC50 values of 1.2, 149.8 and 22.4 nM for hAChE , hBChE and hGSK-3β, respectively. AChE/GSK-3β-IN-1 penetrates the blood-brain barrier (BBB). AChE/GSK-3β-IN-1 has high kinase selectivity profiles for the CMGC kinase family. AChE/GSK-3β-IN-1 occupies the ATP binding site of DYRK1A. AChE/GSK-3β-IN-1 inhibits ROS expression and reduces oxidative stress. AChE/GSK-3β-IN-1 can be used for Alzheimer’s disease research .
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-
- HY-159941
-
|
|
α-synuclein
|
Neurological Disease
|
|
tau-0N4R-IN-1 (Compound 6T) is an BBB-penetrable inhibitor of tau 0N4R oligomerization. tau-0N4R-IN-1 effectively inhibits the fibrosis of tau 0N4R, 2N3R, and 2N4R, exhibits an anti-seeding effect on tau in vitro, reduces the oligomerization of α-syn dose-dependently, and prevents formation of α-syn inclusions. tau-0N4R-IN-1 is stable in mouse microsomes and reduces Aβ plaques in brain tissues from AD patients. tau-0N4R-IN-1 has good pharmacokinetic properties in mice .
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-
| Cat. No. |
Product Name |
Type |
-
- HY-D2268
-
|
|
Fluorescent Dyes/Probes
|
|
QM-FN-SO3 is a BBB-penetrable near-infrared (NIR) aggregation-induced emission (AIE)-active probe for Aβ plaques. QM-FN-SO3 can be used for in vivo detection of Aβ plaques. QM-FN-SO3 has ultra-high S/N ratio, binding affinity, and high-performance NIR emission .
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- HY-D2268A
-
|
|
Fluorescent Dyes/Probes
|
|
QM-FN-SO3 ammonium is a BBB-penetrable near-infrared (NIR) aggregation-induced emission (AIE)-active probe for Aβ plaques. QM-FN-SO3 ammonium can be used for in vivo detection of Aβ plaques. QM-FN-SO3 ammonium has ultra-high S/N ratio, binding affinity, and high-performance NIR emission .
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| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P10235
-
|
|
Amylin Receptor
|
Neurological Disease
|
|
Cyclic AC253 is an antagonist for amylin receptor, with IC50 of 0.3 μM. Cyclic AC253 exhibits neuroprotective efficacy against Aβ toxicity and abrogates Aβ-induced impairment of hippocampal long-term potentiation. Cyclic AC253 penetrate blood-brain barrier (BBB) .
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-
- HY-P2297
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-
- HY-P2297A
-
-
- HY-P1178
-
|
|
Trk Receptor
p38 MAPK
|
Neurological Disease
|
|
Cyclotraxin B is a BBB-penetrable and selective TrkB inhibitor. Cyclotraxin B inhibits BDNF-induced TrkB activity in a non-competitive manner, with an IC50 of 0.30 nM. Cyclotraxin B has analgesic and anxiolytic effects .
|
-
- HY-P3400
-
LP17
1 Publications Verification
LQVTDSGLYRCVIYHPP
|
Peptides
|
Neurological Disease
|
|
LP17 (LQVTDSGLYRCVIYHPP) is a BBB-penetrable triggering receptor expressed on myeloid cells (TREM-1) inhibitory peptide. LP17 substantially alleviates ischemia-induced infarction and neuronal injury. LP17 can get access into brain and block TREM-1 .
|
-
- HY-P3400A
-
|
LQVTDSGLYRCVIYHPP TFA
|
Peptides
|
Neurological Disease
|
|
LP17 (LQVTDSGLYRCVIYHPP) TFA is a BBB-penetrable triggering receptor expressed on myeloid cells (TREM-1) inhibitory peptide. LP17 TFA substantially alleviates ischemia-induced infarction and neuronal injury. LP17 TFA can get access into brain and block TREM-1 .
|
-
- HY-P2342
-
-
- HY-P10777
-
|
|
Peptide-Drug Conjugates (PDCs)
|
Cancer
|
|
ANG1009 is a BBB-penetrable anticancer agent. ANG1009 is cytotoxic to a variety of tumor cells and can induce cell cycle arrest. ANG1009 can be used in the study of brain cancer .
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-
- HY-P1178A
-
|
|
Trk Receptor
|
Neurological Disease
|
|
Cyclotraxin B TFA is a BBB-penetrable and selective TrkB inhibitor. Cyclotraxin B TFA inhibits BDNF-induced TrkB activity in a non-competitive manner, with an IC50 of 0.30 nM. Cyclotraxin B TFA has analgesic and anxiolytic effects .
|
-
- HY-P10782
-
|
|
Peptide-Drug Conjugates (PDCs)
|
Cancer
|
|
Pt(IV)-M13 is a BBB-penetrable Platinum (IV) prodrug-perfluoroaryl macrocyclic peptide conjugate. Pt(IV)-M13 is cytotoxic to glioma stem cells and increases uptake of platinum in the brain. Pt(IV)-M13 can be used in the study of glioblastoma .
|
-
- HY-P2343
-
|
|
Apoptosis
|
Cancer
|
|
BH3 hydrochloride, a BBB penetrated peptide, provoke apoptosis either by direct activation of pro-apoptotic Bax/Bak or by neutralizing anti-apoptotic Bcl-2 proteins (Bcl-2, Bcl-XL, Bcl-w, Mcl-1 and A-1) via their BH3 domian .
|
-
- HY-P3223
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Biphalin TFA, a BBB-penetrable opioid peptide analog, contains two active enkephalin pharmacophores. Biphalin TFA has high affinity for opioid receptors. Biphalin TFA shows analgesic effect in acute, neuropathic, and chronic animal pain models. Biphalin TFA is also an antiviral, antiproliferative, anti-inflammatory, and neuroprotective agent .
|
-
- HY-P10861
-
|
|
Tau Protein
|
Neurological Disease
|
|
RI-AG03 is an orally active and a BBB-penetrable Tau aggregation peptide inhibitor. RI-AG03 inhibits Tau aggregation and improves associated neurodegeneration and behavioral phenotypes in both in vivo and in vitro models. RI-AG03 can be used in the study of tauopathies such as Alzheimer's disease .
|
-
- HY-P1146
-
|
|
Amyloid-β
|
Cardiovascular Disease
Neurological Disease
Inflammation/Immunology
|
|
Semax is a BBB-penetrable adrenocorticotropic hormone-like peptide and can form stable complexes with Cu 2+. Semax is a synthetic peptide analog of Adrenocorticotropic hormone (ACTH) (4-10). Semax has immunomodulatory, nootropic and neuroprotective activities. Semax can be used in the research of central nervous system diseases such as Alzheimer's disease and cerebral ischemia .
|
-
- HY-P1146A
-
|
|
Amyloid-β
|
Cardiovascular Disease
Neurological Disease
Inflammation/Immunology
|
|
Semax acetate is a BBB-penetrable adrenocorticotropic hormone-like peptide and can form stable complexes with Cu 2+. Semax acetate is a synthetic peptide analog of Adrenocorticotropic hormone (ACTH) (4-10). Semax acetate has immunomodulatory, nootropic and neuroprotective activities. Semax acetate can be used in the research of central nervous system diseases such as Alzheimer's disease and cerebral ischemia .
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P99694
-
|
JR-171
|
Transferrin Receptor
|
Neurological Disease
|
|
Lepunafusp alfa (JR-171) is a BBB-penetrable fusion protein consisting of J-Brain Cargo and IDUA (a lysosomal enzyme, α-L-iduronidase). Lepunafusp alfa can reduce concentration of heparan sulfate (HS) and dermatan sulfate (DS). Lepunafusp alfa can be used for research of mucopolysaccharidosis type I .
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| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
| Cat. No. |
Product Name |
Chemical Structure |
-
- HY-19939S
-
4 Publications Verification
|
|
VX-984 is an orally active, potent, selective and BBB-penetrated DNA-PK inhibitor. VX-984 efficiently inhibits NHEJ (non-homologous end joining) and increases DSBs (DNA double-strand breaks). VX-984 can be used for glioblastomas (GBM) and non-small cell lung cancer (NSCLC) research. VX-984 is a de novo deuterium .
|
-
-
- HY-B0602S2
-
|
|
|
Desvenlafaxine-d6 is deuterium labeled Desvenlafaxine. Desvenlafaxine, the succinate salt form of the isolated major active metabolite of Venlafaxine (HY-B0196), is an orally active and BBB penetrated 5-HT and norepinephrine reuptake inhibitor, with IC50 values of 47.3 nM and 531.3 nM for hSERT and hNET, respectively. Desvenlafaxine shows weak binding affinity (62% inhibition at 100 μM) at the human dopamine (DA) transporter .
|
-
-
- HY-W654013
-
|
|
|
Minocycline-d7 is deuterium labeled Minocycline. Minocycline is an orally active, potent and BBB-penetrated semi-synthetic tetracycline antibiotic. Minocycline is a hypoxia-inducible factor (HIF)-1α inhibitor. Minocycline shows anti-cancer, anti-inflammatory, and glutamate antagonist effects. Minocycline reduces glutamate neurotransmission and shows neuroprotective properties and antidepressant effects. Minocycline inhibits bacterial protein synthesis through binding with the 30S subunit of the bacterial ribosome, resulting in a bacteriostatic effect .
|
-
-
- HY-170905S
-
|
|
|
MAT2A-IN-22 (Compound 29-1) is a BBB-penetrable and orally active MAT2A inhibitor with an IC50 of 4 nM. MAT2A-IN-22 shows selectivity and inhibitory activity against MTAP-deficient cancer cell lines. MAT2A-IN-22 has anti-tumor effects .
|
-
-
- HY-109502S
-
|
|
|
10-OH-NBP-d4 is deuterium labeled 10-OH-NBP. 10-OH-NBP is a Butylphthalide (3-n-Butylphthalide; NBP; HY-B0647) hydroxylated metabolite and can penetrates the blood-brain barrier (BBB). Butylphthalide exerts neuroprotective effects and has potential for cerebral ischemia research .
|
-
-
- HY-117727S
-
|
|
|
Leriglitazone-d4 (MIN-102-d4; Hydroxypioglitazone-d4) is deuterium labeled Leriglitazone. Leriglitazone is an orally active and a BBB-penetrable PPARγ agonist with an EC50 of 9 μM. Leriglitazone, as a regulator of mitochondrial function, has neuroprotective, anti-inflammatory and antioxidant effects. Leriglitazone can be used in the study of neuroinflammatory and neurodegenerative diseases .
|
-
-
- HY-B0602S3
-
|
|
|
Desvenlafaxine-d10 is deuterium labeled Desvenlafaxine. Desvenlafaxine, the succinate salt form of the isolated major active metabolite of Venlafaxine (HY-B0196), is an orally active and BBB penetrated 5-HT and norepinephrine reuptake inhibitor, with IC50 values of 47.3 nM and 531.3 nM for hSERT and hNET, respectively. Desvenlafaxine shows weak binding affinity (62% inhibition at 100 μM) at the human dopamine (DA) transporter .
|
-
-
- HY-12678S
-
|
|
|
Entrectinib-d4 (NMS-E628-d4; RXDX-101-d4) is the deuterium labeled Entrectinib (HY-12678). Entrectinib is an orally active, BBB-penetrated and centrally active inhibitor of TrkA/B/C, ROS1 and ALK, with IC50 values of 1, 3, 5, 12 and 7 nM, respectively. Entrectinib induces apoptosis and cycle arrest in cancer cells, has antitumor activity, and attenuates bleomycin-induced lung fibrosis in mice .
|
-
| Cat. No. |
Product Name |
|
Classification |
-
- HY-146314
-
|
|
|
Alkynes
|
|
MAO-B-IN-9 (compound 16) is a potent, selective, BBB-penetrated, irreversible and time-dependent MAO-B (monoamine oxidase B) inhibitor, with an IC50 of 0.18 μM. MAO-B-IN-9 prevents Aβ1-42-induced neuronal cell death. MAO-B-IN-9 shows neuroprotective effects, which may be the result of its Aβ1-42 anti-aggregation effects . MAO-B-IN-9 is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-146691
-
|
|
|
Alkynes
|
|
hMAO-B-IN-2 (compound 6j) is an orally active, potent, selective and BBB penetrated and competitive reversible hMAO-B inhibitor, with an IC50 of 4 nM. hMAO-B-IN-2 shows low toxicity and good neuroprotective effects in SH-SY5Y cell. hMAO-B-IN-2 can be used for alzheimer’s disease research . hMAO-B-IN-2 is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
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