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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
50 Results for "
centrally penetrant
" in MedChemExpress (MCE) Product Catalog:
Products (50)
50 Results for "centrally penetrant" in MCE Product Catalog:
11
11 Publications Verification
Synonyms: AZD1390
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Elrelesertib (AZD1390) is an orally active, brain-penetrant ATM kinase inhibitor with IC50 values of 0.78 nM. Elrelesertib blocks ATM-dependent DNA damage response, inhibits ATM autophosphorylation and downstream Chk2, Rad50 phosphorylation, and accumulates at DNA breaks. Elrelesertib acts as a radiosensitizer, induces apoptosis, genomic instability, G2-M cell cycle arrest, ROS elevation, and mitochondrial membrane potential alteration. Elrelesertib has low efflux liability against P-gp and BCRP. Elrelesertib can be used for the research of central nervous system malignancies, glioblastoma multiforme, glioma, lung cancer brain metastases, and breast cancer .
10
10 Cited Publications
Synonyms: CERC-501; LY-2456302
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Aticaprant (CERC-501) is a potent and centrally-penetrant kappa opioid receptor antagonist with a Ki of 0.807 nM.
6
6 Cited Publications
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SB-222200 is a potent, selective, orally active and blood-brain barrier (BBB) penetrant NK-3 receptor antagonist. SB-222200 is developed for central nervous system (CNS) disorders .
5
5 Cited Publications
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CXCR2-IN-1 is a central nervous system penetrant CXCR2 antagonist with a pIC50 of 9.3.
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3 Cited Publications
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DYRK1-IN-1 is a highly selective and ligand-efficient DYRK1A inhibitor. DYRK1-IN-1 inhibits DYRK1A phosphorylation activity with an IC50 value of 220 nM. DYRK1-IN-1 can be used for the research of central nervous system penetrant DYRK1A chemical probe .
2
2 Cited Publications
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CGP 35348 is a selective, brain penetrant, centrally active GABAB receptor antagonist with an EC50 of 34 μM. CGP 35348 shows affinity for the GABAB receptor only . CGP 35348 has a potential to improve neuromuscular coordination and spatial learning in albino mouse following neonatal brain damage .
2
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1
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Flupirtine (D 9998) Maleate is an orally active, blood-brain barrier-crossing non-opioid analgesic and neuroprotective agent. Flupirtine Maleate is a neuronal potassium channel opener (Kv7 activator), a NMDA receptor antagonist and a GABA receptor activator. Flupirtine Maleate stabilizes blood-brain-barrier integrity, reduces oxidative stress and brain leukocyte infiltration, enhances angioneurogenesis, suppresses calcium influx, stabilizes neuronal resting membrane potential, and counteracts focal cerebral ischemia. Flupirtine Maleate exhibits analgesic, muscle relaxant properties, protects neurons from excitotoxic, ischemic, or cytokine-mediated death. Flupirtine Maleate functions as a non-opioid analgesic without antipyretic or antiphlogistic properties, shows no relevant affinity to opiate receptor. Flupirtine Maleate can be used for the research of focal cerebral ischemia, pain, Alzheimer’s disease, or multiple sclerosis .
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DNL343 is a potent, selective, orally active and brain-penetrant activator of eukaryotic initiation factor eIF2B. DNL343 inhibits the activity of the integrated stress response (ISR) in the central nervous system (CNS) and reverses neurodegeneration and neuroinflammation. DNL343 also prevents motor dysfunction and premature death in eIF2B loss-of-function (LOF) mutant mice. DNL343 can be used in the study of neurodegenerative diseases .
Cat. No.: HY-172429
CAS No.: 2489185-38-6
Synonyms: ORIC-114
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Enozertinib (ORIC-114) is an orally active, CNS-penetrant, highly selective and irreversible dual EGFR/HER2 inhibitor that exhibits potent and targeted inhibition of exon 20 insertion mutations. Enozertinib exhibits high kinome selectivity for the EGFR family of receptors to reduce off-target kinase liabilities. Enozertinib induces tumor regression and demonstrates antitumor activity in central nervous system and non-small cell lung cancer (NSCLC) tumor models. Enozertinib can be used for the research of solid tumors and NSCLC .
Cat. No.: HY-W027553
CAS No.: 62732-44-9
Synonyms: NIK-247 free base; Amiridine free base
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Ipidacrine is orally active and brain-penetrant AChE and BuChE inhibitors with IC50 values of 1 μM and 1.9 μM, respectively, which is also a partial agonist of M2-cholinergic receptors and a reversible cholinesterase inhibitor. Ipidacrine has a stimulating effect on neuromuscular transmission and excitation along the nerve fibres with a moderately anti-pain effect. Ipidacrine is an aminopyridines and is structurally similar to Tacrine (HY-111338). Ipidacrine is effective in various amnesia models, improves erectile function and inhibits K + and Na +-channels in the neuronal membrane in diabetic rats. Ipidacrine is promising for research of Alzheimer’s disease, ischaemic stroke, idiopathic neuropathy of the facial nerve, diabetes mellitus-induced erectile dysfunction and other deficits in central or peripheral cholinergic deseases .
Category:
Monophenols Ketones, Aldehydes, Acids Phenols Endogenous metabolite Disease Research Fields Inflammation/Immunology
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Cat. No.: HY-173591
CAS No.: 2785323-68-2
Research Areas:
Cardiovascular Disease Neurological Disease Inflammation/Immunology
T0080 is a central nervous system-penetrant FPR1 inhibitor. By functionally blocking the FPR1 signaling pathway, T0080 effectively reduces neutrophil infiltration into ischemic brain tissue and maintains the integrity of the blood-brain barrier. T0080 alleviates tPA-associated hemorrhagic transformation, inhibits demyelination responses and the expression of NOX2. T0080 also possesses anti-apoptotic (apoptosis) and anti-inflammatory properties, thereby protecting myelin and reducing neurological deficits. T0080 is widely used in studies related to ischemic stroke complicated by hemorrhagic transformation after tPA thrombolysis, as well as multiple sclerosis .
Synonyms: ACT-539313
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Nivasorexant (ACT-539313) is an orally active, blood-brain barrier penetrant, selective orexin OX1R inhibitor. Nivasorexant specifically blocks central OX1Rs without affecting OX2Rs, and exhibits competitive inhibitory activity against CYP2C8, CYP2C9, CYP2C19 and CYP3A4 (IC50 values are 25 μM, 8.6 μM, 1.6 μM, 19 μM/44 μM, respectively). Nivasorexant significantly reduces binge-like eating behavior of highly palatable food in rat models and has long-acting properties. Nivasorexant shows no relevant off-target activity against over 130 selected proteins, exhibits favorable safety profiles, and can be used for studies related to binge eating disorder .
Cat. No.: HY-172429A
Synonyms: ORIC-114 hemihydrate
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Enozertinib (ORIC-114) hemihydrate is an orally active, CNS-penetrant, highly selective and irreversible dual EGFR/HER2 inhibitor that exhibits potent and targeted inhibition of exon 20 insertion mutations. Enozertinib hemihydrate exhibits high kinome selectivity for the EGFR family of receptors to reduce off-target kinase liabilities. Enozertinib hemihydrate induces tumor regression and demonstrates antitumor activity in central nervous system and non-small cell lung cancer (NSCLC) tumor models. Enozertinib hemihydrate can be used for the research of solid tumors and NSCLC .
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PF-03463275 is a centrally penetrant, orally available, selective, and competitive GlyT1 (glycine transporter-1) reversible inhibitor, with a Ki of 11.6 nM. PF-03463275 has the potential for Schizophrenia research .
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DZD1516 is an orally active, reversible, blood-brain barrier (BBB)-penetrant selective HER2 tyrosine kinase inhibitor with an IC50 of 0.56 nM against HER2. DZD1516 is not a substrate of P-gp or BCRP, and exhibits high passive permeability. DZD1516 inhibits tumor growth in HER2-positive brain metastasis, leptomeningeal metastasis and subcutaneous xenograft models, and can be used for research related to HER2-positive breast cancer and central nervous system metastasis .
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TDI-6118 (Compound 5) is a potent brain-penetrant inhibitor of EZH2. EZH2-IN-12 has the potential for the research of central nervous system malignancies .
Cat. No.: HY-172182
CAS No.: 2230296-66-7
Synonyms: VU6011887
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ONO-2920632 is an orally active and central nervous system (CNS)-penetrant TREK activator, with EC50 values of 0.3 µM and 2.8 μM for TREK-1 and TREK-2, respectively. ONO-2920632 exhibits selectivity for other K2P channels (>91-fold selective versus TASK1, TASK2, TASK3, TRAAK, and TWIK2; 31-fold selective versus TRESK). ONO-2920632 possesses analgesic effects and can be used in research on pain, migraine, and neurological disorders.
Synonyms: VU0488130
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ML381 (VU0488130) is a highly selective, central nervous system penetrant mAChR M5 orthogonal antagonist (IC50 = 450 nM; Ki = 340 nM). ML381 is unstable in rat plasma and can be mainly used as a molecular probe for in vitro and electrophysiological studies .
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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
