Scientific Reviews
Product Guides
Blogs
Topics
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
91 Results for "
Blood brain barrier penetration
" in MedChemExpress (MCE) Product Catalog:
Products (91)
91 Results for "Blood brain barrier penetration" in MCE Product Catalog:
77
77 Publications Verification
Synonyms: GS 4071; Ro 64-0802; Oseltamivir carboxylate
Target:
Research Areas:
Oseltamivir acid (GS 4071), the active metabolite of Oseltamivir phosphate, is an orally bioavailable, potent and selective inhibitor of influenza virus neuraminidase (IC50=2 nM) with activity against both influenza A and B viruses. Oseltamivir acid has an extremely weak ability to penetrate the BBB under normal physiological conditions, but its blood-brain barrier penetration is significantly enhanced under inflammatory conditions .
16
16 Cited Publications
Target:
Research Areas:
A-967079 is a selective TRPA1 receptor antagonist with IC50s of 67 nM and 289 nM at human and rat TRPA1 receptors, respectively, and has good penetration into the blood-brain barrier .
7
7 Cited Publications
Synonyms: 2-(Phosphonomethyl)pentanedioic acid
Target:
Research Areas:
2-PMPA (2-(Phosphonomethyl)pentanedioic acid) is a glutamate carboxypeptidase II (GCPII) inhibitor with an IC50 of 0.0003 μM. 2-PMPA shows low blood-brain barrier penetration. 2-PMPA sodium blocks the hydrolysis of NAAG, regulates glutamate levels in the brain and neurovascular coupling. 2-PMPA is applicable to the research of neurological diseases .
7
7 Cited Publications
Target:
Research Areas:
URMC-099 is an orally bioavailable and potent mixed lineage kinase type 3 (MLK3) (IC50=14 nM) inhibitor with with excellent blood-brain barrier penetration properties.
7
7 Cited Publications
Cat. No.: HY-100788C
CAS No.: 373645-42-2
Synonyms: 2-(Phosphonomethyl)pentanedioic acid sodium
Target:
Research Areas:
2-PMPA (2-(Phosphonomethyl)pentanedioic acid) sodium is a glutamate carboxypeptidase II (GCPII) inhibitor with an IC50 of 0.0003 μM. 2-PMPA sodium shows low blood-brain barrier penetration. 2-PMPA sodium blocks the hydrolysis of NAAG, regulates glutamate levels in the brain and neurovascular coupling. 2-PMPA sodium is applicable to the research of neurological diseases .
5
5 Cited Publications
Synonyms: Sodium decanoate; Sodium caprate
5
5 Cited Publications
Cat. No.: HY-17037
CAS No.: 29868-97-1
Synonyms: LS 519; Pirenzepin dihydrochloride; Gastrozepin dihydrochloride
Target:
Research Areas:
Pirenzepine (LS 519) dihydrochloride is a selective M1 mAChR (muscarinic acetylcholine receptor) antagonist, with poor penetration of the blood-brain barrier. Pirenzepine dihydrochloride reduces gastric acid secretion and reduces muscle spasm, can be used in peptic ulcers research. Pirenzepine dihydrochloride shows anti-proliferative activity to cancer cells .
5
5 Cited Publications
Cat. No.: HY-17037A
CAS No.: 28797-61-7
Synonyms: LS 519 free base; Pirenzepin; Gastrozepin
Target:
Research Areas:
Pirenzepine (LS 519 free base) is a selective M1 mAChR (muscarinic acetylcholine receptor) antagonist, with poor penetration of the blood-brain barrier. Pirenzepine reduces gastric acid secretion and reduces muscle spasm, can be used in peptic ulcers research. Pirenzepine shows anti-proliferative activity to cancer cells .
3
3 Cited Publications
Synonyms: EXP999; RP9965
Target:
Research Areas:
Metopimazine (EXP999; RP9965) is a phenothiazine, orally available, selective dopamine D2 receptor antagonist that does not penetrate the blood-brain barrier. Metopimazine blocks dopamine D2 receptors in the chemoreceptor trigger zone and the periphery, thereby inhibiting nausea and vomiting. Metopimazine is indicated for chemotherapy-induced nausea and vomiting, and has low central side effects due to its poor brain penetration. The use of metopimazine in acute gastroenteritis may have potential risks .
3
Target:
Research Areas:
Vatinoxan (MK-467) is an alpha 2-adrenergic receptor antagonist. The peripheral selectivity of Vatinoxan determines that it has limited penetration across the blood-brain barrier and therefore has low concentrations in the central nervous system. Vatinoxan antagonizes alpha 2-adrenergic receptor receptors by binding to them, thereby reducing or preventing cardiovascular effects caused by α2-adrenergic agonists. Vatinoxan can be used in studies of cardiovascular effects, sedation and analgesia .
1
1 Cited Publications
Cat. No.: HY-N2345
CAS No.: 23567-23-9
1
1 Cited Publications
Target:
Research Areas:
SHA 68 is a potent and selective non-peptide neuropeptide S receptor (NPSR) antagonist with IC50s of 22.0 and 23.8 nM for NPSR Asn 107 and NPSR Ile 107, respectively. SHA 68 has limited the blood-brain barrier (BBB) penetration and the activity in neuralgia .
1
1 Cited Publications
Target:
Research Areas:
BMS-193885 is a selective neuropeptide Y1 receptor antagonist (Ki=3.3 nM) that competitively blocks the receptor to inhibit NPY-mediated appetite regulation signaling pathways, reduce food intake and inhibit weight gain. BMS-193885 has good blood-brain barrier penetration and is mainly used in the study of obesity and related metabolic diseases .
1
1 Cited Publications
Target:
Research Areas:
(S)-SNAP5114 is a non-covalent murine GABA transporter inhibitor with blood-brain barrier penetration ability, which exhibits significant subtype-selective inhibitory activity against mGAT4 (pIC50=5.71, pKi=4.56), much higher than its effects on mGAT1, mGAT2 and mGAT3. (S)-SNAP5114 elevates extracellular GABA concentrations by blocking the GABA reuptake mechanism, thereby enhancing thalamus-specific GABAergic signaling and exerting potential neuromodulatory effects. (S)-SNAP5114 is widely used in studies related to epilepsy, neuropathic pain, anxiety and depression, and various neurodegenerative diseases .
Synonyms: Anle138b
Target:
Research Areas:
Emrusolmin (Anle138b), an oligomeric aggregation inhibitor, blocks the formation of pathological aggregates of prion protein (PrPSc) and of α-synuclein (α-syn). Emrusolmin strongly inhibits oligomer accumulation, neuronal degeneration, and disease progression in vivo. Emrusolmin has low toxicity and an excellent oral bioavailability and blood-brain-barrier penetration. Emrusolmin blocks Aβ channels and rescues disease phenotypes in a mouse model for amyloid pathology .
Cat. No.: HY-P9967
CAS No.: 1384260-65-4
Synonyms: BIIB037
Target:
Research Areas:
Cat. No.: HY-175715
CAS No.: 3077720-24-9
Target:
Research Areas:
NRG1271 is an orally active mitochondrial permeability transition pore (mPTP) inhibitor with blood-brain barrier penetration. NRG1271 can be used for the study of Neurological Disease .
Target:
Research Areas:
T-2307 is an antifungal agent with blood-brain barrier penetration. T-2307 exhibits broad-spectrum antifungal activity against Candida species, including echinocandin-resistant strains, Cryptococcus neoformans, Cryptococcus gattii, and some Aspergillus species. T-2307 selectively targets fungal mitochondrial respiratory chain complexes III and IV, causing collapse of the fungal mitochondrial membrane potential and exerting fungicidal or fungistatic effects. T-2307 can be used in research related to fungal infections such as invasive candidiasis, cryptococcosis, and aspergillosis .
Research Areas:
DS44960156 is a selective MTHFD2 inhibitor with moderate to low blood-brain barrier penetration (IC50=1.6 μM, Ki=1.23 μM). DS44960156 specifically binds to the active site of MTHFD2, disrupts redox homeostasis and blocks serine-mediated one-carbon metabolism, thereby increasing the NAD +/NADH ratio and ROS levels. DS44960156 not only effectively inhibits the proliferation of glioma cells, but also enhances the sensitivity of cells to glutamine starvation-induced death. DS44960156 binds to plasma proteins, shows no mutagenicity, carcinogenicity or acute oral toxicity, and serves as a research agent for glioblastoma multiforme and other cancers .
Research Areas:
Antihistamine-1 is a H1-antihistamine (Ki=6.9 nM) with acceptable blood-brain barrier penetration and also an inhibitor of CYP2D6 and hERG channel with IC50s of 5.4 and 0.8 μM, respectively.
-
-
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
