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Results for "

bbb penetrant

" in TargetMol Product Catalog
  • Inhibitors & Agonists
    8
    TargetMol | Inhibitors_Agonists
  • Compound Libraries
    1
    TargetMol | Compound_Libraries
AS057278
3-Methylpyrazole-5-carboxylic acid
T7476402-61-9
AS057278 (3-Methylpyrazole-5-carboxylic acid) is an D-amino acid oxidase (DAAO) inhibitor.
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TargetMol | Inhibitor Sale
Irdabisant
CEP-26401, CEP 26401, CEP26401
T321911005402-19-6
Irdabisant (CEP-26401) (CEP-26401) is a selective, orally active and blood-brain barrier (BBB) penetrant antagonist inverse agonist of histamine H3 receptor (H3R) (rat H3R Ki= 7.2 nM, human H3R Ki= 2.0 nM). Irdabisant exhibits relatively low inhibitory activity against hERG current (IC50= 13.8 μM). Irdabisant exhibits cognition-enhancing and wake-promoting activities in the rat social recognition model. Irdabisant can be used for research on schizophrenia or cognitive impairment.
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6-8 weeks
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ms48107
Benzenemethanol, 2-[4-amino-6-[[(4-phenoxyphenyl)methyl]amino]-1,3,5-triazin-2-yl]-3-fluoro-
T91462375070-79-2
MS48107 is a potent, selective positive allosteric modulator of G protein-coupled receptor 68 (GPR68), demonstrating specificity for GPR68 over closely related proton GPCRs, neurotransmitter transporters, and hERG ion channels. It effectively crosses the blood-brain barrier (BBB) in mice.
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EST73502 hydrochloride
T96692307458-82-6
EST73502 hydrochloride is a selective, orally active and blood-brain barrier (BBB) penetrant dual μ-opioid receptor (MOR) agonist and σ1 receptor (σ1R) antagonist, with K i s of 64 nM and 118 nM for MOR and σ1R, respectively. EST73502 hydrochloride has antinociceptive activity with reduced opioid-induced relevant adverse events[1].
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1-2 weeks
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mao-b-in-13
T606502105918-34-9
MAO-B-IN-13 (compound 12a) is a highly potent, reversible, and blood-brain barrier (BBB) penetrant MAO-B inhibitor (IC50 = 10 nM) that exhibits neuroprotective and antioxidant activity, making it suitable for Parkinson's disease research [1].
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8-10 weeks
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irdabisant hydrochloride
T611971005398-61-7
Irdabisant hydrochloride (CEP-26401) is a selective, orally active, and blood-brain barrier penetrating histamine H3 receptor (H3R) inverse agonist, demonstrating high affinity with K*i values of 7.2 nM and 2.0 nM for rat and human H3R, respectively. Exhibiting relatively low hERG current inhibitory activity with an IC*50 of 13.8 μM, this compound has shown to enhance cognition and promote wakefulness in rat social recognition models, suggesting potential applications in schizophrenia or cognitive impairment research.
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1-2 weeks
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ARN-21934
T369682230854-93-8
ARN-21934 is a potent, highly selective, blood-brain barrier (BBB) penetrant inhibitor for human topoisomerase II α over β. It inhibits DNA relaxation with an IC50 of 2 μM, compared to 120 μM for Etoposide. ARN-21934 exhibits favorable in vivo pharmacokinetic properties and shows promise in anticancer research, displaying affinity for topoIIα with an IC50 of 2 μM and for topoIIβ with an IC50 of 120 μM. It demonstrates activity against human cancer cell lines including melanoma (A375: 12.6 μM, G-361: 8.1 μM), breast (MCF7: 15.8 μM), endometrial (HeLa: 38.2 μM), lung (A549: 17.1 μM), and prostate (DU145: 11.5 μM) cancer cells. Following a single intraperitoneal injection of 10 mg kg, ARN-21934 achieves a peak plasma concentration of 0.68 μg mL in 15 minutes, with a half-life of 149 minutes, and remains detectable in plasma and the brain for up to 360 minutes. [1] Jose Antonio Ortega, et al. Novel, Potent, and Druglike Tetrahydroquinazoline Inhibitor That Is Highly Selective for Human Topoisomerase II α over β. J Med Chem. 2020 Nov 12;63(21):12873-12886.
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6-8 weeks
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TargetMol | Inhibitor Sale
FLDP-5
T73508950665-12-0
FLDP-5, a blood-brain barrier (BBB) penetrant curcuminoid analogue, induces the production of Reactive Oxygen Species (ROS), DNA damage, and cell cycle S phase arrest. It demonstrates significant tumor-suppressive effects, exhibiting potent anti-proliferative and anti-migratory activities on LN-18 cells.
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6-8 weeks
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