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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
855 Results for "
brain permeability
" in MedChemExpress (MCE) Product Catalog:
Products (855)
855 Results for "brain permeability" in MCE Product Catalog:
Cat. No.: HY-B0464S
CAS No.: 2749234-32-8
Cat. No.: HY-B0464S1
CAS No.: 2012598-61-5
Research Areas:
Dihydroergotamine (DFN-19) is a blood-brain barrier-permeable semi-synthetic ergot alkaloid, acting as a full agonist of 5-HT1B/1D receptors (Ki values of 0.3 nM and 2.5 nM, respectively; functional IC50 values of 2 nM and 2.2 nM, respectively). Dihydroergotamine inhibits Forskolin (HY-15371)-stimulated cAMP accumulation, possesses α-adrenergic receptor antagonistic activity and weak dopaminergic agonistic activity. It mediates intracranial cerebrovascular contraction, inhibits the release of neuropeptides such as CGRP/substance P, and suppresses neurogenic inflammation by activating 5-HT1B/1D receptors in the trigeminovascular system. Dihydroergotamine binds to the catalytic site of Trypanosoma cruzi trypanothione reductase and exhibits trypanocidal activity in vitro. Dihydroergotamine can be used in studies related to migraine and trypanosome infections .
Research Areas:
Temephos (Standard) is the analytical standard of Temephos. This product is intended for research and analytical applications. Temephos (Temefos) is an orally active, blood-brain barrier-permeable organophosphate insecticide and AChE inhibitor. By irreversibly inhibiting AChE to induce cholinergic overactivation, Temephos effectively blocks larval development of Aedes aegypti (yellow fever mosquito) and Aedes albopictus (Asian tiger mosquito), and is commonly used in studies related to Dengue Virus, Zika Virus and other relevant pathogens. Temephos exhibits genotoxicity and neurodevelopmental toxicity, and may also cause liver injury, reproductive system abnormalities and cholinergic poisoning symptoms in mammals. Temephos tends to accumulate in adipose tissues and aquatic organisms, and is excreted via feces after metabolism through oxidation and hydrolysis. Note that CYP-mediated metabolic detoxification may reduce the actual larvicidal efficacy of Temephos against some mosquito species. Temephos can be used in research related to dengue fever, Zika virus disease, chikungunya and dracunculiasis .
Cat. No.: HY-B1120S
CAS No.: 1219795-39-7
Synonyms: Temefos-d12
Cat. No.: HY-N0688R
CAS No.: 13476-25-0
Cat. No.: HY-N1989
CAS No.: 11028-00-5
Cat. No.: HY-W587743
CAS No.: 1215711-91-3
Synonyms: AMK hydrochloride
Research Areas:
Neurological Disease Metabolic Disease Inflammation/Immunology
N1-Acetyl-5-methoxykynuramine hydrochloride (AMK hydrochloride) is an active metabolite of Melatonin (HY-B0075) with antioxidant activity and blood-brain barrier permeability. N1-Acetyl-5-methoxykynuramine hydrochloride inhibits LPS-induced activation of inducible nitric oxide synthase and COX-2, scavenges ROS, hydroxyl radicals, carbonate radicals and ABTS cation radicals, and protects bovine serum albumin from peroxyl radical-mediated damage. N1-Acetyl-5-methoxykynuramine hydrochloride reduces the increase in cytoplasmic and mitochondrial lipid peroxidation in the substantia nigra and striatum in MPTP (HY-15608)-induced mouse models of Parkinson's disease. N1-Acetyl-5-methoxykynuramine hydrochloride can be used in studies related to Parkinson's disease, metabolism-related diseases and oxidative stress .
Cat. No.: HY-W715812
CAS No.: 116255-48-2
Target:
Fungal Apoptosis Caspase Reactive Oxygen Species (ROS) MDM-2/p53 SOD Bcl-2 Family PERK JNK p38 MAPK
Research Areas:
Bromuconazole is a triazole fungicide with oral efficacy and blood-brain barrier permeability . Bromuconazole protects crops from various fungal contaminations. Bromuconazole exhibits cytotoxicity against a variety of cancer cells, induces G0/G1 cell cycle arrest and inhibits DNA synthesis in cancer cells, and triggers cytoskeletal structural disorder, genotoxic damage, apoptotic (apoptosis) cell death, and mitochondrial membrane depolarization. Bromuconazole activates caspase-3, induces excessive production of ROS, p53 and Bax, lipid peroxidation, increased activities of SOD and CAT, and downregulates Bcl-2. By upregulating p-ERK1/2 and p-JNK, Bromuconazole disrupts the MAPK signaling pathway, impairs the cellular stress response of human trophoblast cells and endometrial cells, and damages the implantation process . Bromuconazole is applicable to research related to glioma, colon cancer, reproductive injury (implantation dysfunction), and cardiac dysfunction .
Cat. No.: HY-103430
CAS No.: 108179-91-5
Research Areas:
SKF-83566 hydrobromide is an orally active, blood-brain barrier-permeable D1/D5 dopamine receptor antagonist with a Ki value of approximately 0.4-0.56 nM.
SKF-83566 hydrobromide modulates locomotor behavior and spatial memory by blocking D1 receptors and inhibits glioblastoma progression by targeting the DRD1/c-Myc/UHRF1 pathway.
SKF-83566 hydrobromide acts as an inhibitor of the dopamine transporter (DAT) and adenylyl cyclase 2 (AC2).
SKF-83566 hydrobromide competitively binds to DAT to inhibit dopamine reuptake and non-competitively inhibits AC2 activity, thereby reducing cAMP accumulation.
SKF-83566 hydrobromide is used in research areas such as dopaminergic system mechanisms, learning and memory, targeted intervention for glioblastoma, AC2 pathophysiology, antiparasitic drug screening, and synaptic plasticity (the "gating effect") .
Cat. No.: HY-121675A
CAS No.: 2855123-30-5
Synonyms: BOL-148 D-Tartrate; Bromolysergide D-Tartrate
Research Areas:
2-Bromo-LSD D-Tartrate (BOL-148 D-Tartrate) is a blood-brain barrier-permeable 5-HT2A partial agonist and competitive partial antagonist. 2-Bromo-LSD D-Tartrate acts as both a potent partial agonist (with an EC50 of 0.81 nM for Gq dissociation) and a potent partial antagonist (with a KB of 0.18 nM for Gq dissociation) at the 5-HT2A receptor. 2-Bromo-LSD D-Tartrate exhibits partial agonist activity at multiple aminergic GPCRs, including 5-HT2A. 2-Bromo-LSD D-Tartrate lacks 5-HT2B agonist activity. 2-Bromo-LSD D-Tartrate induces dendritogenesis and spinogenesis. 2-Bromo-LSD D-Tartrate reverses the behavioral effects of chronic stress and increases active coping behaviors in mice .
Cat. No.: HY-160906
CAS No.: 32607-79-7
Synonyms: GSSSG
Target:
Interleukin Related Tyrosinase ERK Microphthalmia Associated Transcription Factor (MITF) Reactive Oxygen Species (ROS) NF-κB
Research Areas:
Glutathione trisulfide (GSSSG) is an orally active, blood-brain barrier permeable neuroprotective agent. Glutathione trisulfide inactivates intracellular tyrosinase, regulates the expression of Cars2, Cbs, MITF and TYR, inhibits α-MSH (HY-P0252)-induced melanogenesis, and restores intracellular persulfide levels reduced by α-MSH. Glutathione trisulfide scavenges free radicals, quenches ROS, reduces Paclitaxel (HY-B0015)-induced superoxide production, upregulates the expression of antioxidant protein genes, and inhibits oxidative stress-induced cell death. Glutathione trisulfide promotes ERK1/2 activation, prevents NF-κB p65 activation, inhibits TAK1 phosphorylation, reduces pro-inflammatory cytokine expression, and blocks microglial activation. Glutathione trisulfide can be used in research related to dry age-related macular degeneration, inflammation-associated eye diseases, Alzheimer's disease, Parkinson's disease, etc.
Cat. No.: HY-160906A
Synonyms: GSSSG TFA
Glutathione trisulfide TFA (GSSSG TFA) is an orally active, blood-brain barrier permeable neuroprotective agent. Glutathione trisulfide TFA inactivates intracellular tyrosinase, regulates the expression of Cars2, Cbs, MITF and TYR, inhibits α-MSH (HY-P0252)-induced melanogenesis, and restores intracellular persulfide levels reduced by α-MSH. Glutathione trisulfide TFA scavenges free radicals, quenches ROS, reduces Paclitaxel (HY-B0015)-induced superoxide production, upregulates the expression of antioxidant protein genes, and inhibits oxidative stress-induced cell death. Glutathione trisulfide TFA promotes ERK1/2 activation, prevents NF-κB p65 activation, inhibits TAK1 phosphorylation, reduces pro-inflammatory cytokine expression, and blocks microglial activation. Glutathione trisulfide TFA can be used in research related to dry age-related macular degeneration, inflammation-associated eye diseases, Alzheimer's disease, Parkinson's disease, etc.
Cat. No.: HY-16900G
CAS No.: 61413-54-5
Cat. No.: HY-19872
CAS No.: 942436-93-3
Target:
Research Areas:
AZD6280 is an orally active, blood-brain barrier-permeable GABAA receptor modulator, with Ki values of 21 nM, 31 nM and 1680 nM against human receptors containing α2, α3 and α5 subtypes, respectively, and subtype-specific Ki values of < 30 nM for α2 and α3 subtypes. AZD6280 selectively potentiates GABAA receptors containing α2/α3 subtypes with higher potency than α1/α5 subtypes, exerts no modulatory effect on receptors containing α1 subtypes, and regulates the tuberoinfundibular dopaminergic pathway. AZD6280 decreases peak saccadic velocity, increases serum and plasma prolactin levels, rescues dendritic abnormalities of cortical neurons induced by DISC1 knockdown. AZD6280 can be used in studies related to anxiety disorders .
Cat. No.: HY-B0670S
Dihydroergotamine-d3 is the d3-labeled Dihydroergotamine (HY-B0670). Dihydroergotamine (DFN-19) is a blood-brain barrier-permeable semi-synthetic ergot alkaloid, acting as a full agonist of 5-HT1B/1D receptors (Ki values of 0.3 nM and 2.5 nM, respectively; functional IC50 values of 2 nM and 2.2 nM, respectively). Dihydroergotamine inhibits Forskolin (HY-15371)-stimulated cAMP accumulation, possesses α-adrenergic receptor antagonistic activity and weak dopaminergic agonistic activity. It mediates intracranial cerebrovascular contraction, inhibits the release of neuropeptides such as CGRP/substance P, and suppresses neurogenic inflammation by activating 5-HT1B/1D receptors in the trigeminovascular system. Dihydroergotamine binds to the catalytic site of Trypanosoma cruzi trypanothione reductase and exhibits trypanocidal activity in vitro. Dihydroergotamine can be used in studies related to migraine and trypanosome infections .
Cat. No.: HY-103430AR
CAS No.: 99295-33-7
SKF-83566 (Standard) is the analytical standard of SKF-83566 (HY-103430A). This product is intended for research and analytical applications. SKF-83566 is an orally active, blood-brain barrier-permeable D1/D5 dopamine receptor antagonist with a Ki value of approximately 0.4-0.56 nM.
SKF-83566 modulates locomotor behavior and spatial memory by blocking D1 receptors and inhibits glioblastoma progression by targeting the DRD1/c-Myc/UHRF1 pathway.
SKF-83566 acts as an inhibitor of the dopamine transporter (DAT) and adenylyl cyclase 2 (AC2).
SKF-83566 competitively binds to DAT to inhibit dopamine reuptake and non-competitively inhibits AC2 activity, thereby reducing cAMP accumulation.
SKF-83566 is used in research areas such as dopaminergic system mechanisms, learning and memory, targeted intervention for glioblastoma, AC2 pathophysiology, antiparasitic drug screening, and synaptic plasticity (the "gating effect") .
Cat. No.: HY-171705
CAS No.: 1478585-60-2
Research Areas:
KMS99220 is an orally active, blood-brain barrier-permeable activator of the Nrf2 inhibitory protein Keap-1. KMS99220 enhances the activity of AMPK, activates the Nrf2 signaling pathway, and reduces the phosphorylation of IκB, nuclear translocation of NFκB, as well as the phosphorylation levels of JNK, IKK and p38 MAPK via HO-1. KMS99220 binds to Keap1 to trigger the nuclear translocation of Nrf2, induces the expression of HO-1, NQO1, GCLC, GCLM and proteasome subunits; enhances proteasomal enzymatic activity; inhibits iNOS expression, nitric oxide production and IL-1β generation; attenuates microglial activation; reduces α-synuclein aggregation; and prevents dopaminergic neuron degeneration and motor dysfunction. KMS99220 prevents the degeneration of dopaminergic neurons in the substantia nigra, induces the expression of Nrf2 downstream target genes, and effectively ameliorates associated motor dysfunction in a mouse model of Parkinson's disease. KMS99220 is applicable to research related to Parkinson's disease .
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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
