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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
26 Results for "
brain-penetrant agents
" in MedChemExpress (MCE) Product Catalog:
Products (26)
26 Results for "brain-penetrant agents" in MCE Product Catalog:
49
49 Publications Verification
Cat. No.: HY-B0568
CAS No.: 30652-11-0
Target:
Research Areas:
Cardiovascular Disease Infection Neurological Disease Cancer
Deferiprone is a potent, orally active, brain-penetrant, cell-penetrant, skin-permeable, free iron chelating agent. Deferiprone inhibits the proliferation and migration, and stimulates apoptosis in tumor cell. Deferiprone can inhibit KDM. Deferiprone has antianemic, neuroprotective, anti-inflammatory, antioxidant, and antidotal activity. Deferiprone can be used in cancer, cardiovascular disease, infection, inflammation, and neurological disease study .
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Narazaciclib (ON123300), a strong and brain-penetrant multi-kinase inhibitor, inhibits CDK4 (IC50=3.9 nM), Ark5 (IC50=5 nM), PDGFRβ (IC50=26 nM), FGFR1 (IC50=26 nM), RET (IC50=9.2 nM), and FYN (IC50=11 nM). Single agent Narazaciclib causes a dose-dependent suppression of phosphorylation of Akt as well as activation of Erk in brain tumors . Narazaciclib inhibits CDK6 with an IC50 of 9.82 nM .
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Target:
Research Areas:
AZD-9574 is a potent and brain penetrant PARP1 inhibitor and shows >8000-fold selectivity for PARP1 compared to PARP2/3/5a/6. AZD-9574 acts by selectively inhibiting and trapping PARP1 at the sites of SSBs. AZD-9574 is an anti-cancer agent and can be used for HRD +?breast cancer and advanced solid malignancies research .
1
1 Cited Publications
Cat. No.: HY-W017540
CAS No.: 35404-50-3
Target:
Research Areas:
Cardiovascular Disease Neurological Disease Metabolic Disease Cancer
Cyclocreatine, a creatine analogue, acts as a brain-penetrant and potent bioenergetic protective agent by providing high levels of ATP. Cyclocreatine can be phosphorylated and dephosphorylated by creatine kinases. Cyclocreatine suppresses creatine metabolism ameliorating the cognitive, autistic and epileptic phenotype in a mouse model of creatine transporter defciency. Cyclocreatine protects against ischemic injury and enhances cardiac recovery during early reperfusion in dogs and rats. Cyclocreatine decreases plaque-adjacent neuronal dystrophy in TREM2-deficient mice with amyloid-β pathology. Cyclocreatine is proming for research of ischemic heart disease, cardiovascular diseases, Alzheimer’s disease and other neurodegenerative diseases associated with microglial dysfunction, prostate cancer .
1
1 Cited Publications
Synonyms: Hexahydroadiphenine hydrochloride
Target:
Cholinesterase (ChE) Potassium Channel Amyloid-β TRP Channel Tau Protein NOD-like Receptor (NLR) JNK NF-κB IKK
Research Areas:
Neurological Disease Metabolic Disease Inflammation/Immunology
Drofenine (Cycloadiphene; Hexahydroadiphenine) hydrochloride is an brain-penetrant antispasmodic agent. Drofenine hydrochloride is a Kv2.1 channel inhibitor with human IC50 of 9.53 μM. Drofenine hydrochloride is a butyrylcholinesterase (BChE) inhibitor with Ki of 0.003 mM, and is a TRPV3 activator. Drofenine hydrochloride blocks Kv2.1-dependent potassium efflux, inhibits Kv2.1/JNK/NF-κB and IkBa/NF-kB signaling, suppresses Kv2.1 mRNA/protein expression. Drofenine suppresses oligomeric Aβ-induced microglial NLRP3 inflammasome activation and neuronal Tau hyperphosphorylation, improves cognitive impairment, promotes neurite outgrowth. Drofenine hydrochloride induces calcium influx in keratinocytes and exert cytotoxicity against keratinocytes. Drofenine hydrochloride ameliorates diabetic peripheral neuropathy -like pathology. Drofenine hydrochloride can be used for the researches of Alzheimer's disease, diabetic peripheral neuropathy and smooth muscle spasm .
1
1 Cited Publications
Target:
Research Areas:
Neurological Disease Metabolic Disease Inflammation/Immunology
SR-3306 is a brain-penetrant and selective pan-JNK (JNK1/2/3) inhibitor. SR-3306 is a neuroprotective agent that can be used for the study of Parkinson's disease, ischemia/reperfusion (I/R) injury and obesity .
Cat. No.: HY-W013150
CAS No.: 82626-01-5
Target:
Research Areas:
Alpidem, an anxiolytic agent, is an orally active and brain-penetrant GABAA receptor ligand, binds to α1β2γ2 subunit-containing GABAA receptors (IC50 of 17 nM) over α5β2γ2 subunit-containing GABAA receptors (IC50 of >10 μM). Alpidem modulates calcium-induced mitochondrial permeability transition, induces glutathione depletion and hepatocyte necrosis, potentiates TNF-α toxicity, inhibits marble-burying and locomotor activity, enhances stressed rodent feeding behavior, and exerts anticonvulsant effects. Alpidem can be used for the research of anxiety, anxiety disorders, and convulsions .
Cat. No.: HY-B0568R
CAS No.: 30652-11-0
Target:
Deferiprone (Standard) is the analytical standard of Deferiprone. This product is intended for research and analytical applications. Deferiprone is a potent, orally active, brain-penetrant, cell-penetrant, skin-permeable, free iron chelating agent. Deferiprone inhibits the proliferation and migration, and stimulates apoptosis in tumor cell. Deferiprone has antianemic, neuroprotective, anti-inflammatory, antioxidant, and antidotal activity. Deferiprone can be used in cancer, cardiovascular disease, infection, inflammation, and neurological disease study .
Cat. No.: HY-P10862
Target:
IC50 values of 11.9, 12.5, 35.7, 206 and 136 nM, respectively. AH-D peptide reduces the viral load in the brain, suppresses inflammation, protects neurons, and does not damage the blood brain barrier. AH-D peptide restores antitumor immunity by decreasing circulating PD-L1 + exosomes, reducing intratumoral immunosuppressive cells (regulatory T cells, myeloid-derived suppressor cells), and enhancing T cell function. AH-D peptide inhibits membrane-enveloped viruses and cancer cell metastasis in vivo. AH-D peptide exhibits no immunogenicity and has negligible effects on normal tissues. AH-D peptide can be used for research in Zika virus and other mosquito-borne viruses, cancer immunotherapy and metastasis .
Cat. No.: HY-163737
CAS No.: 2419942-78-0
Target:
Research Areas:
ST-401, a microtubule-targeting agent (MTA), is a brain-penetrant microtubule (MT) assembly inhibitor. ST-401 disrupts microtubule (MT) function through gentle and reverisible reduction in MT assembly that triggers mitotic delay and cell death in interphase. ST-401 shows a potent antitumor activity .
Cat. No.: HY-178048
CAS No.: 3086460-35-4
Target:
Research Areas:
Neuroprotective agent 13 is a brain-penetrant 1H-benzo[d]imidazoles compound with neuroprotective effect. Neuroprotective agent 13 can activate autophagy and clear SCMAS accumulation from iPSC-derived neural progenitor cells. Neuroprotective agent 13 can be used for the research of neurological disease, such as neuronal ceroid lipofuscinoses (NCLs) .
Cat. No.: HY-N10183
CAS No.: 55750-86-2
Target:
Cat. No.: HY-178454
Target:
Monoamine Oxidase Amyloid-β Mitochondrial Metabolism Apoptosis Reactive Oxygen Species (ROS) COX NF-κB
Research Areas:
Multitarget AD-IN-3 is a brain-penetrant neuroprotective agent. Multitarget AD-IN-3 can selectively inhibit MAO-B with an IC50 of 4.42 μM and a SI of 18.12. Multitarget AD-IN-3 can eliminate ROS. Multitarget AD-IN-3 Multitarget AD-IN-3 can inhibit Aβ1-42 self-aggregation and can reverse Aβ1-42-induced mitochondrial membrane depolarization and inhibit apoptosis. Multitarget AD-IN-3 can be used for the research of neurological disease, such as Alzheimer’s disease .
Cat. No.: HY-W017540R
CAS No.: 35404-50-3
Target:
Research Areas:
Cardiovascular Disease Neurological Disease Metabolic Disease Cancer
Cyclocreatine, a creatine analogue, acts as a brain-penetrant and potent bioenergetic protective agent by providing high levels of ATP. Cyclocreatine can be phosphorylated and dephosphorylated by creatine kinases. Cyclocreatine suppresses creatine metabolism ameliorating the cognitive, autistic and epileptic phenotype in a mouse model of creatine transporter defciency. Cyclocreatine protects against ischemic injury and enhances cardiac recovery during early reperfusion in dogs and rats. Cyclocreatine decreases plaque-adjacent neuronal dystrophy in TREM2-deficient mice with amyloid-β pathology. Cyclocreatine is proming for research of ischemic heart disease, cardiovascular diseases, Alzheimer’s disease and other neurodegenerative diseases associated with microglial dysfunction, prostate cancer .
Cat. No.: HY-155103
CAS No.: 2961381-94-0
Target:
Research Areas:
Antitrypanosomal agent 15 (compound 26) is an orally active, brain-penetrant, selective inhibitor against Trypanosoma cruzi proteasome, with an pIC50 of 7.4 and <4 for T. cruzi and human proteasome, respectively. Antitrypanosomal agent 15 has favorable ADME properties and can be used for Chagas disease study .
Cat. No.: HY-178052
CAS No.: 3086460-57-0
Target:
Research Areas:
Neuroprotective agent 14 is a brain-penetrant 1H-benzo[d]imidazoles compound with neuroprotective effect. Neuroprotective agent 14 can activate autophagy and clear SCMAS accumulation from iPSC-derived neural progenitor cells. Neuroprotective agent 14 can be used for the research of neurological disease, such as neuronal ceroid lipofuscinoses (NCLs) .
Cat. No.: HY-177738
CAS No.: 2102591-12-6
Target:
Research Areas:
6'Nicotinate Ac4ManNAz (Compound 2) is a brain-penetrant carbohydrate-neuroactive heteromer conjugating Ac4ManNAz (HY-W728531) and Nicotinic acid (HY-B0143). 6'Nicotinate Ac4ManNAz can be used for the development of glycosylation-regulating agents or diagnostic probes that cross the BBB .
Target:
Research Areas:
RTICBM-189 is a potent, brain-penetrant allosteric modulator of the cannabinoid type-1 (CB1) receptor with a pIC50 of 7.54 in Ca 2+ mobilization assay. RTICBM-189 has pIC50s of 5.29 and 6.25 for hCB1 and mCB1, respectively. RTICBM-189 significantly and selectively attenuates the reinstatement of the addictive agent-seeking behavior in rats .
Cat. No.: HY-B0568S
CAS No.: 1346601-82-8
Cat. No.: HY-W013150R
CAS No.: 82626-01-5
Target:
Research Areas:
Alpidem (Standard) is the analytical standard of Alpidem (HY-W013150). This product is intended for research and analytical applications. Alpidem, an anxiolytic agent, is an orally active and brain-penetrant GABAA receptor ligand, binds to α1β2γ2 subunit-containing GABAA receptors (IC50 of 17 nM) over α5β2γ2 subunit-containing GABAA receptors (IC50 of >10 μM). Alpidem modulates calcium-induced mitochondrial permeability transition, induces glutathione depletion and hepatocyte necrosis, potentiates TNF-α toxicity, inhibits marble-burying and locomotor activity, enhances stressed rodent feeding behavior, and exerts anticonvulsant effects. Alpidem can be used for the research of anxiety, anxiety disorders, and convulsions.
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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
