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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
27 Results for "
cerebellum
" in MedChemExpress (MCE) Product Catalog:
Products (27)
27 Results for "cerebellum" in MCE Product Catalog:
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5 Cited Publications
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DO34 is a selective DAGL inhibitor, with an IC50 of 6 nM for DAGLα conversion of SAG to 2-AG. DO34 blocks de novo 2-AG synthesis, and suppresses tonic CB1 receptor activation. DO34 blocks depolarization-induced suppression of excitation and inhibition in the cerebellum and hippocampus. DO34 regulates feeding behavior and locomotor activity in mice. DO34 abolishes AM251-mediated enhancement of parallel fiber-evoked excitatory postsynaptic currents in cerebellar slices from MAGL global knockout mice. DO34 can be used for the research of energy balance disorder and neuroinflammation .
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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 .
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1 Cited Publications
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Penconazole is a typical triazole fungicide, and mainly applied on apples, grapes, and vegetables to control powdery mildew. Penconazole inhibits sterol biosynthesis in fungi. Penconazole decrease AChE activity in the cerebrum and cerebellum of rats .
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1 Cited Publications
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NS-2028 is a highly selective soluble Guanylyl Cyclase (sGC) inhibitor with IC50 values of 30 nM and 200 nM for basal and NO-stimulated enzyme activity . NS-2028 inhibits soluble Guanylyl Cyclase activity in homogenates of mouse cerebellum and neuronal NO synthase with IC50 values of 17 nM and 20 nM . NS-2028 inhibits 3-morpholino-sydnonimine (SIN-1)-elicited formation of cyclic GMP in human cultured umbilical vein endothelial cells with an IC50 of 30 nM . NS-2028 is commonly used in the research of nitric oxide signaling pathways, it inhibits NO-dependent relaxant responses in non-vascular smooth muscle completely (1 μM) . NS-2028 reduces vascular endothelial growth factor-induced angiogenesis and permeability .
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Synonyms: EKZ-001
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Bavarostat (EKZ-001) is a blood-brain barrier-permeable, potent HDAC6 inhibitor and PET radiotracer, with an IC50 as low as 17 nM against human HDAC6. Bavarostat can be labeled with 18F and used as a probe to map HDAC6 distribution and measure target occupancy in the brains of non-human primates. Bavarostat also selectively modulates tubulin acetylation, but not histone acetylation. Bavarostat is applicable for research on Alzheimer's disease, other neurodegenerative disorders, and cancers .
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ICI-204448 is a κ-opioid agonist with limited access to the CNS, ICI-204448 can displace the binding of the kappa-opioid ligand 3H-bremazocine from guinea pig cerebellum membranes .
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DO34 analog is a structural analog of DO34 (HY-117771). DO34 is a selective DAGL inhibitor, with an IC50 of 6 nM for DAGLα conversion of SAG to 2-AG. DO34 blocks de novo 2-AG synthesis, and suppresses tonic CB1 receptor activation. DO34 blocks depolarization-induced suppression of excitation and inhibition in the cerebellum and hippocampus. DO34 regulates feeding behavior and locomotor activity in mice. DO34 abolishes AM251-mediated enhancement of parallel fiber-evoked excitatory postsynaptic currents in cerebellar slices from MAGL global knockout mice. DO34 can be used for the research of energy balance disorder and neuroinflammation .
Cat. No.: HY-135761R
CAS No.: 66246-88-6
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Penconazole (Standard) is the analytical standard of Penconazole. This product is intended for research and analytical applications. Penconazole is a typical triazole fungicide, and mainly applied on apples, grapes, and vegetables to control powdery mildew. Penconazole inhibits sterol biosynthesis in fungi. Penconazole decrease AChE activity in the cerebrum and cerebellum of rats .
Cat. No.: HY-W075176
CAS No.: 118712-89-3
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Transfluthrin is an insecticide with extremely low acute toxicity to vertebrates. Transfluthrin acts as a mosquito repellent, exerts mosquito control effects via electric heating fumigators, and is widely used in studies related to malaria, bancroftian filariasis and mosquito-borne infectious diseases. Transfluthrin may also induce adverse reactions such as pulmonary sensory irritation, sensitization, genotoxicity and respiratory depression, and can increase the concentrations and activities of CYP2E1 and CYP3A2 in rat brains. Transfluthrin can be removed from wastewater through biodegradation and activated sludge adsorption, and can be degraded by microorganisms such as Azovibrio and Tauera .
Cat. No.: HY-13533
CAS No.: 176046-79-0
Synonyms: NSC 682691; 4-Demethylpenclomedine
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DMPEN (NSC 682691) (4-Demethylpenclomedine) is an alkylating metabolite of Penclomedine (HY-106401). DMPEN has an antitumor activity. DMPEN does not induce Purkinje cells loss with no significant neurocerebellar toxicity in rat cerebellum models. DMPEN can be used for cancers like breast and brain cancer research .
Cat. No.: HY-P10036
CAS No.: 910804-03-4
Cat. No.: HY-126063
CAS No.: 125190-72-9
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ICI-204448 free acid is a κ-opioid agonist with limited access to the CNS, ICI-204448 free acid can displace the binding of the kappa-opioid ligand 3H-bremazocine from guinea pig cerebellum membranes .
Cat. No.: HY-13511AS
CAS No.: 1795153-63-7
Synonyms: UR-12592 D4 fumarate
Cat. No.: HY-69019A
CAS No.: 161467-34-1
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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 .
Cat. No.: HY-153127
CAS No.: 937245-42-6
Synonyms: AV-133
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Florbenazine (AV-133) is a diagnostic imaging agent targeting the central nervous system monoamine transporter VMAT2, and its F-18 labeled form can be used for PET scanning. The biodistribution of [18F]Florbenazine in mice shows a high striatum/cerebellum ratio (0.48), which can be used for the diagnostic research of neurodegenerative diseases (including dementia with Lewy bodies and Parkinson's disease) .
Cat. No.: HY-136659
CAS No.: 194089-07-1
Ro 04-5595 is a selective antagonist with specific activity against the NR2B subunit of the NMDA receptor. Ro 04-5595 exhibits favorable pharmacokinetic properties in in vitro and in vivo studies, with rapid uptake and clearance. Ro 04-5595 exhibits strong binding in NR2B receptor-enriched regions and low binding in the cerebellum. Ro 04-5595 is able to effectively inhibit specific binding, showing high affinity for the NR2B receptor and a clear ranking of binding affinity with a variety of other compounds .
Cat. No.: HY-12193
CAS No.: 556835-30-4
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A-349821 is a histamine H3 receptor antagonist characterized as a radioligand ([3H]-A-349821) for in vivo receptor occupancy assessment. In rats, [3H]-A-349821 penetrated the brain, showing higher levels in the cortex compared to the cerebellum, indicating selective H3 receptor binding. Its cortical occupancy was saturable, correlating with in vitro binding data. Inhibition studies with ABT-239 and other H3 antagonists showed dose-dependent reductions in receptor occupancy, matching blood levels associated with cognitive efficacy in preclinical models. [3H]-A-349821 thus serves as a valid tracer for H3 receptor occupancy, aiding in the development and clinical interpretation of H3 receptor antagonists .
Cat. No.: HY-184368
CAS No.: 29176-29-2
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Lofendazam is a major metabolite of Arfendazam. Lofendazam acts as a positive allosteric modulator/partial agonist of GABAa receptor, with IC50 values of 10.1 nM and 9.1 nM in bovine cerebral cortex and bovine cerebellum, respectively; its in vivo ED50 via oral administration is 233 µmol/kg .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
