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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
21 Results for "
Blood-brain barrier permeability in vitro
" in MedChemExpress (MCE) Product Catalog:
Products (21)
21 Results for "Blood-brain barrier permeability in vitro" in MCE Product Catalog:
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Dihydroergotamine mesylate 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 mesylate 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 mesylate binds to the catalytic site of Trypanosoma cruzi trypanothione reductase and exhibits trypanocidal activity in vitro. Dihydroergotamine mesylate can be used in studies related to migraine and trypanosome infections .
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Target:
TRP Channel Aldehyde Dehydrogenase (ALDH) Cholinesterase (ChE) Keap1-Nrf2 Amyloid-β Fungal Apoptosis
Research Areas:
Infection Neurological Disease Inflammation/Immunology Cancer
Dyclonine hydrochloride (Dyclocaine hydrochloride) is an orally active, blood-brain barrier-permeable piperidine phenylacetone small molecule commonly used as a local anesthetic. Dyclonine hydrochloride acts as a highly selective allosteric antagonist of TRPV3; it also reversibly inhibits G9a, ALDH2 and ALDH3A1, non-competitively blocks AChE. Dyclonine hydrochloride activates the Nrf2/ARE pathway, relieves the epigenetic silencing of FXN, blocks Aβ42 aggregation, and promotes remyelination and reparative polarization of microglia. Dyclonine hydrochloride alleviates pruritus via TRPV3 inhibition; it is used in studies of neurodegenerative disease models based on its AChE inhibitory, antioxidant and remyelinating effects; it sensitizes drug-resistant tumors through ALDH inhibition, and combined use with protease inhibitors induces more tumor cell apoptosis; it inhibits Candida albicans in vitro. Dyclonine hydrochloride can be used for research on multiple diseases including neurodegenerative diseases, cancer and pruritic dermatitis .
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PQQ-trimethylester (PQQ-TME) is a synthetic compound that is a trimethylester derivative of pyrroloquinoline quinone (PQQ). PQQ-trimethylester has twice the blood-brain barrier permeability of PQQ (HY-100196) in vitro. In addition, PQQ-trimethylester shows strong inhibitory activity against α-synuclein, amyloid β1-42 (Aβ1-42) and prion protein fibrillation. PQQ-trimethylester can be used in the study of neurodegenerative diseases .
Synonyms: MPC-6827 hydrochloride
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Verubulin hydrochloride (MPC-6827 hydrochloride) is a blood brain barrier permeable microtubule-disrupting agent, with potent and broad-spectrum in vitro and in vivo cytotoxic activities. Verubulin hydrochloride (MPC-6827 hydrochloride) exhibits potent anticancer activity in human MX-1 breast and other mouse xenograft cancer models. Verubulin hydrochloride (MPC 6827 hydrochloride) is a promising candidate for the treatment of multiple cancer types .
Cat. No.: HY-10486
CAS No.: 361444-66-8
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Research Areas:
JDTic is a blood-brain barrier-permeable κ-opioid receptor antagonist (Ki=0.02 nM) with favorable in vitro ADME properties. JDTic blocks agonist-mediated Gi and β-arrestin signaling pathways as well as analgesic effects by stabilizing the inactive conformation of hKOR and activating JNK. JDTic may also induce transient asymptomatic ventricular tachycardia. JDTic is widely applicable to studies related to depression, anxiety, stress-induced addictive behaviors, and nicotine withdrawal .
Cat. No.: HY-157555
CAS No.: 2198483-40-6
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NLRP3-IN-29(Compound 5M) is an inhibitor of NLR family pyrin domain containing 3 (NLRP3). NLRP3-IN-29 has the potential for blood-brain barrier permeability and inflammation inhibition both in vivo and in vitro. NLRP3-IN-29 can be used for research on Alzheimer's disease .
Cat. No.: HY-50723S1
Target:
Isotope-Labeled Compounds Endogenous Metabolite Phosphodiesterase (PDE) Caspase Bcl-2 Family Apoptosis
Research Areas:
3-Methylxanthine-d3 is deuterated labeled 3-Methylxanthine (HY-50723). 3-Methylxanthine is a blood-brain barrier-permeable cyclic GMP phosphodiesterase inhibitor, with an IC50 of 920 μM against guinea pig cyclic GMP phosphodiesterase. 3-Methylxanthine relaxes the spontaneous tension of isolated guinea pig tracheal smooth muscle preparations. Through a DRD1-dependent pathway, 3-Methylxanthine upregulates the expression of γH2AX and activated caspase-3, downregulates the expression of Bcl-2, and enhances Cisplatin-induced apoptosis (apoptosis) in ovarian cancer cells both in vitro and in vivo. 3-Methylxanthine induces clonic convulsions in the central nervous system. 3-Methylxanthine is the major metabolite of Theophylline (HY-B0809). 3-Methylxanthine can be used in studies related to ovarian cancer and neurotoxic convulsions .
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 .
Cat. No.: HY-12098R
CAS No.: 917369-31-4
Synonyms: MPC-6827 hydrochloride (Standard)
Research Areas:
Verubulin (hydrochloride) (Standard) is the analytical standard of Verubulin (hydrochloride). This product is intended for research and analytical applications. Verubulin hydrochloride (MPC-6827 hydrochloride) is a blood brain barrier permeable microtubule-disrupting agent, with potent and broad-spectrum in vitro and in vivo cytotoxic activities. Verubulin hydrochloride (MPC-6827 hydrochloride) exhibits potent anticancer activity in human MX-1 breast and other mouse xenograft cancer models. Verubulin hydrochloride (MPC 6827 hydrochloride) is a promising candidate for the treatment of multiple cancer types .
Cat. No.: HY-174399
Research Areas:
AChE/BChE-IN-27 is a blood-brain barrier-permeable mixed inhibitor (Pe = 4.12) of AChE and BChE, with IC50 values of 3.72 μM and 9.65 μM, respectively. AChE/BChE-IN-27 has potent antioxidant activity with an IC50 value of 6.32 μM in the DPPH (HY-112053) assay and also exhibits potent in vitro antioxidant activity. AChE/BChE-IN-27 exhibits metal chelating properties. AChE/BChE-IN-27 has neuroprotective potential against oxidative stress. AChE/BChE-IN-27 significantly reduces intracellular reactive oxygen species (ROS). In in vivo experiments, AChE/BChE-IN-27 effectively restored AChE and BChE levels, improved cognition, and can be used for Alzheimer's disease (AD) .
Cat. No.: HY-149090
CAS No.: 3044829-88-8
Research Areas:
AChE/BuChE/MAO-B-IN-2 (compound 4b) is a potent AChE/BuChE inhibitor and showed good blood brain barrier (BBB) permeability in vitro with an IC50 value of 5.3 μM, 12.4 μM, 1.9±0.08 μM, for AChE, BuChE, huMAO-B, respectively. AChE/BuChE/MAO-B-IN-2 (compound 4b) can inhibit excess AChE/BuChE in Alzheimer's disease (AD) brain. AChE/BuChE/MAO-B-IN-2 (compound 4b) can be used in anti-Alzheimer's research .
Cat. No.: HY-B0364AR
CAS No.: 536-43-6
Synonyms: Dyclocaine hydrochloride (Standard)
Dyclonine hydrochloride (Standard) (Dyclocaine hydrochloride (Standard)) is the analytical standard of Dyclonine hydrochloride (HY-B0364A). This product is intended for research and analytical applications. Dyclonine hydrochloride (Dyclocaine hydrochloride) is an orally active, blood-brain barrier-permeable piperidine phenylacetone small molecule commonly used as a local anesthetic. Dyclonine hydrochloride acts as a highly selective allosteric antagonist of TRPV3; it also reversibly inhibits G9a, ALDH2 and ALDH3A1, non-competitively blocks AChE. Dyclonine hydrochloride activates the Nrf2/ARE pathway, relieves the epigenetic silencing of FXN, blocks Aβ42 aggregation, and promotes remyelination and reparative polarization of microglia. Dyclonine hydrochloride alleviates pruritus via TRPV3 inhibition; it is used in studies of neurodegenerative disease models based on its AChE inhibitory, antioxidant and remyelinating effects; it sensitizes drug-resistant tumors through ALDH inhibition, and combined use with protease inhibitors induces more tumor cell apoptosis; it inhibits Candida albicans in vitro. Dyclonine hydrochloride can be used for research on multiple diseases including neurodegenerative diseases, cancer and pruritic dermatitis .
Cat. No.: HY-B0364AS
Synonyms: Dyclocaine-d9 hydrochloride
Cat. No.: HY-DY2024
Target:
Research Areas:
0.5% Evans Blue Staining Solution is an azo dye solution that strongly binds to serum albumin to form a high-molecular-weight tracer complex. 0.5% Evans Blue Staining Solution can passively leak with albumin and produce color when the blood-brain barrier or vascular barrier is damaged in vivo, and it is used for permeability assessment. 0.5% Evans Blue Staining Solution is excluded by living cells but enters dead cells to stain them in vitro due to the loss of membrane integrity in dead cells. 0.5% Evans Blue Staining Solution can be used for studies related to the identification of dead/necrotic cells and blood-brain barrier (BBB) permeability .
Cat. No.: HY-D3220
CAS No.: 2408913-88-0
Cat. No.: HY-164584
CAS No.: 1621065-22-2
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S1P5 receptor antagonist 1 is a selective, blood-brain barrier-permeable S1P5 receptor antagonist with an EC50 of 0.1 nM and a Ki of 4.4 nM. S1P5 receptor antagonist 1 inhibits the migration of natural killer cells towards sphingosine 1-phosphate in vitro, with no effect on T cell migration. S1P5 receptor antagonist 1 can be used in the research of central nervous system diseases .
Cat. No.: HY-187430
CAS No.: 2977213-17-3
Research Areas:
Dopamine D2 receptor agonist-4 is a blood-brain barrier permeable Dopamine D2 receptor agonist with an EC50 value of 0.03 nM. Dopamine D2 receptor agonist-4 reduces intracellular cAMP levels. Dopamine D2 receptor agonist-4 acts as a Ferroptosis inhibitor and iron chelator, selectively chelating iron ions, reducing intracellular ferrous ion levels, and exerting cytoprotective effects against iron-dependent ferroptosis in vitro. Dopamine D2 receptor agonist-4 improves motor dysfunction and exerts neuroprotective effects in mouse models of Parkinson's disease. Dopamine D2 receptor agonist-4 can be used in studies related to Parkinson's disease .
Target:
TRP Channel Aldehyde Dehydrogenase (ALDH) Cholinesterase (ChE) Keap1-Nrf2 Amyloid-β Fungal Apoptosis
Research Areas:
Infection Neurological Disease Inflammation/Immunology Cancer
Dyclonine (Dyclocaine) is an orally active, blood-brain barrier-permeable piperidine phenylacetone small molecule commonly used as a local anesthetic. Dyclonine acts as a highly selective allosteric antagonist of TRPV3; it also reversibly inhibits G9a, ALDH2 and ALDH3A1, non-competitively blocks AChE. Dyclonine activates the Nrf2/ARE pathway, relieves the epigenetic silencing of FXN, blocks Aβ42 aggregation, and promotes remyelination and reparative polarization of microglia. Dyclonine alleviates pruritus via TRPV3 inhibition; it is used in studies of neurodegenerative disease models based on its AChE inhibitory, antioxidant and remyelinating effects; it sensitizes drug-resistant tumors through ALDH inhibition, and combined use with protease inhibitors induces more tumor cell apoptosis; it inhibits Candida albicans in vitro. Dyclonine can be used for research on multiple diseases including neurodegenerative diseases, cancer and pruritic dermatitis .
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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
