36 Results for "

CNS permeability

" in MedChemExpress (MCE) Product Catalog:
Products (36)

36 Results for "CNS permeability" in MCE Product Catalog:

41
41 Publications Verification
Cat. No.: HY-B1473
CAS No.: 153-98-0
Synonyms: 5-Hydroxytryptamine hydrochloride; 5-HT hydrochloride
Serotonin (5-Hydroxytryptamine) hydrochloride is a monoamine neurotransmitter in the CNS and an endogenous 5-HT receptor agonist, with blood-brain barrier permeability. Serotonin hydrochloride is also a catechol O-methyltransferase (COMT) inhibitor with a Ki of 44 μM.
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7
7 Cited Publications
Cat. No.: HY-15023
CAS No.: 900510-03-4
Purity:  99.95%
Synonyms: PF-3274167
Target:  

Oxytocin Receptor

Research Areas:  

Endocrinology

Cligosiban (PF-3274167) is an orally active, highly selective, and centrally permeable oxytocin receptor antagonist with good pharmacokinetics in rats and can inhibit physiological ejaculation in rodents [1][2].
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6
6 Cited Publications
Cat. No.: HY-101418
CAS No.: 1428327-31-4
Purity:  99.79%
Target:  

P2X Receptor

Research Areas:  

Neurological Disease

JNJ-47965567 is a centrally permeable, high-affinity, selective P2X7 antagonist, with pKis of 7.9 and 8.7 for human and rat P2X7, respectively. JNJ-47965567 can be used to probe the role of central P2X7 in rodent models of CNS pathophysiology .
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4
4 Cited Publications
Cat. No.: HY-125021
CAS No.: 2143542-28-1
Purity:  99.31%
2BAct is a highly selective, orally active, and CNS-penetrant eIF2B (eukaryotic initiation factor 2B) activator with an EC50 of 33 nM. 2BAct prevents neurological defects caused by a chronic integrated stress response. 2BAct displays improved solubility and pharmacokinetics relative to eIF2B activator ISRIB trans-isomer (HY-12495) .
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3
3 Cited Publications
Cat. No.: HY-A0168
CAS No.: 313348-27-5
Synonyms: CVT-3146
Target:  

Adenosine Receptor

Research Areas:  

Cardiovascular Disease Cancer

Regadenoson (CVT-3146) is a selective A2A adenosine receptor agonist and vasodilator that increases coronary blood flow, can be used in study of myocardial perfusion imaging. Regadenoson also increases the permeability of the blood-brain barrier (BBB) in rodents, can be used to study increased delivery of agents to the human CNS .
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2
2 Cited Publications
Cat. No.: HY-105231
CAS No.: 83314-01-6
Purity:  99.70%
Bryostatin 1 is a natural macrolide isolated from the bryozoan Bugula neritina and is a potent and central nervous system (CNS)-permeable PKC modulator. Bryostatin 1 binds to the isolated C1 domain of Munc13-1 and the full-length Munc13-1 protein with Kis of 8.07 nM and 0.45 nM, respectively. Bryostatin 1 has anti-cancer, anti-inflammatory, neuroprotective, anti-HIV-1 infection properties .
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1
1 Cited Publications
Cat. No.: HY-111263
CAS No.: 868592-56-7
Purity:  99.11%
NIAD-4 is a blood-brain barrier permeable fluorophore for optical imaging of amyloid-β () in the central nervous system (CNS) for Alzheimer’s disease (AD). NIAD-4 binds to the same Aβ site with the binding affinity (Ki) of 10 nM .
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1
1 Cited Publications
Cat. No.: HY-119939
CAS No.: 1629729-98-1
Purity:  98.10%
Synonyms: CHDI00390576
Target:  

HDAC

Research Areas:  

Cancer

CHDI-390576, a potent, cell permeable and CNS penetrant class IIa histone deacetylase (HDAC) inhibitor with IC50s of 54 nM, 60 nM, 31 nM, 50 nM for class IIa HDAC4, HDAC5, HDAC7, HDAC9, respectively, shows >500-fold selectivity over class I HDACs (1, 2, 3) and ~150-fold selectivity over HDAC8 and the class IIb HDAC6 isoform .
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Cat. No.: HY-W019710
CAS No.: 1396841-57-8
Target:  

HDAC

Research Areas:  

Neurological Disease

(E,E)-RGFP966 is a selective and CNS permeable HDAC3 inhibitor that can be used for the research of Huntington’s disease .
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Cat. No.: HY-155079
CAS No.: 2387570-00-3
Purity:  98.31%
Target:  

EGFR

Research Areas:  

Cancer

DZD1516 is a potent and selective HER2 inhibitor (IC50=0.56 nM) with good blood-brain permeability. DZD1516 exhibits antitumor activity in CNS and subcutaneous xenograft mouse models .
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Cat. No.: HY-153615
CAS No.: 2226732-62-1
Purity:  99.47%
Target:  

mGluR

Research Areas:  

Neurological Disease

CVN636 is a potent, orally active and selective mGluR7 allosteric agonist with an EC50 value of 7 nM for hu mGluR7. CVN636 has central nervous system (CNS) permeability .
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Cat. No.: HY-P10502A
Target:  

LDLR

Research Areas:  

Others

L57 acetate is a Low-density lipoprotein receptor-related protein 1 (LRP1)-binding peptide. L57 acetate exhibits high affinity to LRP1 with Ki of 45 nM. L57 acetate exhibits blood-brain barrier (BBB) permeability and plasma stability. L57 acetate can be utilized as the carrier for CNS drug delivery .
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Cat. No.: HY-149408
Target:  

Monoamine Oxidase

Research Areas:  

Cancer

MAOA-IN-1 (compound 15) is an orally active MAOA inhibitor with cytotoxicity against prostate cancer cells. MAOA-IN-1 has Caco-2 permeability and lower CNS permeability. MAOA-IN-1 can be further used in the research of anti-cancer and anti-inflammatory indications .
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Cat. No.: HY-162750
CAS No.: 3096805-18-1
Target:  

DYRK Tau Protein

Research Areas:  

Neurological Disease

ZJCK-6-46 (32) is a potential and orally activeDYRK1A inhibitor (IC50 = 0.68 nM) with high BBB permeability (CNS+). ZJCK-6-46 (32) reduces tau phosphorylation. ZJCK-6-46 (32) ameliorates cognitive dysfunction by obviously reducing the expression of phosphorylated tau and neuronal loss in vivo .
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Cat. No.: HY-118179
CAS No.: 1816301-67-3
Purity:  99.30%
Target:  

mGluR

Research Areas:  

Neurological Disease

VU0486321 is a compound in a class of mGlu1 positive allosteric modulators (PAMs). VU0486321 maintains acceptable mGlu1 PAM potency, DMPK profile, CNS permeability, and mGluR selectivity.
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Cat. No.: HY-155320
CAS No.: 2378397-30-7
Target:  

Opioid Receptor

Research Areas:  

Neurological Disease

Mu opioid receptor antagonist 7 (compound 24) is a potent and CNS permeable antagonist of µOR (µ-opioid receptor), with an IC50 of 29 ± 3.0 nM. Mu opioid receptor antagonist 7 can be used for the research of pain and opioid use disorder .
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Cat. No.: HY-175482
CAS No.: 3066798-40-8
Target:  

PARP

Research Areas:  

Neurological Disease Cancer

PARP1-IN-43 (Compound 5350) is a blood-brain barrier (BBB) permeable PARP1 inhibitor, with an IC50 of 5 nM. PARP1-IN-43 can be used for the study of homologous recombination (HR)-deficient central nerve system (CNS) cancers .
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Cat. No.: HY-131068
CAS No.: 2563970-92-1
Target:  

Beta-secretase

Research Areas:  

Neurological Disease

BACE-1 inhibitor 2 is a potent and CNS permeable BACE-1 inhibitor with an IC50 of 1.5 nM in BACE-1 enzymatic assay .
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Cat. No.: HY-P2342
Research Areas:  

Neurological Disease

Angiopep-Bim BH3 hydrochloride, a BBB penetrated peptode, could be used to investigate the permeability of CNS therapeutics .
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Cat. No.: HY-15023R
CAS No.: 900510-03-4
Synonyms: PF-3274167 (Standard)
Research Areas:  

Endocrinology

Cligosiban (Standard) is the analytical standard of Cligosiban. This product is intended for research and analytical applications. Cligosiban (PF-3274167) is an orally active, highly selective, and centrally permeable oxytocin receptor antagonist with good pharmacokinetics in rats and can inhibit physiological ejaculation in rodents .
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