646 Results for "

brain-penetrant

" in MedChemExpress (MCE) Product Catalog:
Products (646)

646 Results for "brain-penetrant" in MCE Product Catalog:

98
98 Publications Verification
Cat. No.: HY-P1061
CAS No.: 867021-83-8
Target:  

STAT Amyloid-β

Research Areas:  

Neurological Disease

Colivelin is a brain penetrant neuroprotective peptide and a potent activator of STAT3, suppresses neuronal death by activating STAT3 in vitro . Colivelin exhibits long-term beneficial effects against neurotoxicity, Aβ deposition, neuronal apoptosis, and synaptic plasticity deficits in neurodegenerative disease . Colivelin has the potential for the treatment of alzheimer's disease and ischemic brain injury
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98
98 Publications Verification
Cat. No.: HY-114153A
Purity:  99.88%
Target:  

c-Fms

Research Areas:  

Neurological Disease

PLX5622 hemifumarate is a highly selective brain penetrant and orally active CSF1R inhibitor (IC50=0.016 μM; Ki=5.9 nM). PLX5622 hemifumarate allows for extended and specific microglial elimination, preceding and during pathology development. PLX5622 hemifumarate demonstrates desirable PK properties in varies animals .
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98
98 Publications Verification
Cat. No.: HY-P1061A
CAS No.: 2803948-60-7
Target:  

STAT Amyloid-β Apoptosis

Research Areas:  

Neurological Disease

Colivelin TFA is a brain penetrant neuroprotective peptide and a potent activator of STAT3, suppresses neuronal death by activating STAT3 in vitro . Colivelin TFA exhibits long-term beneficial effects against neurotoxicity, Aβ deposition, neuronal apoptosis, and synaptic plasticity deficits in neurodegenerative disease . Colivelin TFA has the potential for the treatment of alzheimer's disease and ischemic brain injury .
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98
98 Publications Verification
Cat. No.: HY-114153
CAS No.: 1303420-67-8
Purity:  99.79%
Target:  

c-Fms

PLX5622 is a highly selective brain penetrant and orally active CSF1R inhibitor (IC50=0.016 μM; Ki=5.9 nM). PLX5622 allows for extended and specific microglial cells elimination, preceding and during pathology development. PLX5622 is an ideal choose for microglia function research in healthy or diseased states. PLX5622 has been verified by MedChemExpress, which demonstrates desirable microglia depletion efficiency in mice. PLX5622 is predominantly administered via ad libitum diets with a dose of 1200 ppm .
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92
92 Cited Publications
Cat. No.: HY-15608
CAS No.: 23007-85-4
Purity:  99.52%
MPTP hydrochloride is a brain penetrant dopaminergic neurotoxin. MPTP hydrochloride can be used to induce Parkinson’s Disease model. MPTP hydrochloride, a precusor of MPP +, induces apoptosis . MPTP hydrochloride has been verified by MCE with professional biological experiments.
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92
92 Cited Publications
Cat. No.: HY-W114750
CAS No.: 28289-54-5
MPTP (1-Methyl-4-phenyl-1,2,3,6-tetrahydropyridine) is a brain penetrant dopamine neurotoxin. MPTP can be used to induce Parkinson’s Disease model. MPTP, a precusor of MPP +, induces apoptosis .
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78
78 Cited Publications
Cat. No.: HY-11063
CAS No.: 162359-55-9
Purity:  99.97%
Synonyms: FTY720 free base
Fingolimod (FTY720 free base) is a brain-penetrant sphingosine 1-phosphate (S1P) antagonist with an IC50 of 0.033 nM in K562 and NK cells. Fingolimod also is a pak1 activator, a immunosuppressant .
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64
64 Cited Publications
Cat. No.: HY-17363
CAS No.: 624-49-7
Dimethyl fumarate (DMF) is an orally active and brain-penetrant Nrf2 activator and induces upregulation of antioxidant gene expression. Dimethyl fumarate induces necroptosis in colon cancer cells through GSH depletion/ROS increase/MAPKs activation pathway, and also induces cell autophagy. Dimethyl fumarate can be used for multiple sclerosis research .
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49
49 Cited Publications
Cat. No.: HY-B0568
CAS No.: 30652-11-0
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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42
42 Cited Publications
Cat. No.: HY-12768A
CAS No.: 2222138-31-8
Purity:  99.43%
Synonyms: BLZ945 hydrochloride
Target:  

c-Fms

Research Areas:  

Cancer

Sotuletinib (BLZ945) hydrochloride is a potent, selective, orally active and brain-penetrant CSF-1R (c-Fms) inhibitor with an IC50 of 1 nM, showing more than 1,000-fold selectivity against its closest receptor tyrosine kinase homologs. Sotuletinib hydrochloride can be used for microglia depletion, and for tumor and CNS-related disease research. .
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42
42 Cited Publications
Cat. No.: HY-12768
CAS No.: 953769-46-5
Purity:  99.83%
Synonyms: BLZ945
Target:  

c-Fms

Research Areas:  

Infection Neurological Disease Cancer

Sotuletinib (BLZ945) is a potent, selective, orally active and brain-penetrant CSF-1R (c-Fms) inhibitor with an IC50 of 1 nM, showing more than 1,000-fold selectivity against its closest receptor tyrosine kinase homologs. Sotuletinib can be used for microglia depletion, and for tumor and CNS-related disease research .
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42
42 Cited Publications
Cat. No.: HY-13324
CAS No.: 218600-53-4
Purity:  98.92%
Synonyms: RTA 402; NSC 713200; CDDO Methyl ester
Bardoxolone methyl (RTA 402) is an orally active and blood-brain-barrier-penetrant activator of Nrf2 and an inhibitor of SARS-CoV-2 3CL protease. Bardoxolone methyl inhibits SARS-CoV-2 replication in Vero cells with an EC50 value of 0.29 μM. Bardoxolone methyl increases levels of pNrf2 and HO-1, inhibits inflammatory mediators like pNFκB and MCP-1. Bardoxolone methyl activates the Nrf2 pathway to enhance antioxidant and anti-inflammatory responses, inhibits viral replication, and improves mitochondrial function. Bardoxolone methyl can be used in research on chemotherapy-induced neuropathic pain (CINP), COVID-19, and chronic kidney disease (CKD) .
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39
39 Cited Publications
Cat. No.: HY-12497
CAS No.: 219766-25-3
Purity:  99.90%
ANA-12 is a brain-penetrant, selective TrkB antagonist with IC50 values of 45.6 nM and 41.1 μM, and Kd values of 10 nM and 12 μM, for high- and low-affinity sites, respectively. ANA-12 specifically inhibits BDNF-induced TrkB receptor activation and its downstream signaling cascades by directly and non-competitively binding to the TrkB receptor, without affecting the functions of TrkA and TrkC. ANA-12 is used in research concerning neuropsychiatric disorders (such as depression and anxiety), acute and chronic pain, neuroimmune inflammation, and the mechanisms of learning and memory .
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38
38 Cited Publications
Cat. No.: HY-12215
CAS No.: 1454846-35-5
Purity:  99.92%
Synonyms: PF-06463922
Lorlatinib (PF-06463922) is a selective, orally active, brain-penetrant and ATP-competitive ROS1/ALK inhibitor with anticancer activity. Lorlatinib has Kis of <0.025 nM, <0.07 nM, and 0.7 nM for ROS1, wild type ALK, and ALK L1196M, respectively. Lorlatinib targets to EML4-ALK, and inhibits ALK phosphorylation with IC50s of 15-43 nM (ALK L1196), 14-80 nM (ALK G1269A), 38-50 nM (ALK 1151Tins), 77-113 nM (ALK G1202R), respectively .
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35
35 Cited Publications
Cat. No.: HY-12495A
CAS No.: 548470-11-7
Purity:  98.58%
ISRIB is a brain-penetrant inhibitor of integrated stress response (ISR). Persistent activation of the ISR has been linked to the development of several neurological disorders as ISR represses translation through inhibiting eIF2B. ISRIB inhibits the ISR by promoting the nucleotide exchange activity of eIF2B and recovering the translation, and thus can be used for neurological disorders research .
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27
27 Cited Publications
Cat. No.: HY-P1363
Synonyms: Amyloid β-peptide (1-42) (human) TFA
Target:  

Amyloid-β

Research Areas:  

Neurological Disease

β-Amyloid (1-42) (Amyloid β-peptide (1-42), human TFA, a 42-amino acid peptide that has not been treated with HFIP, is a brain-penetrant amyloid protein fragment, which can be used in research on Alzheimer's disease and Down’s syndrome. β-Amyloid (1-42), human TFA remaining as a monomer exhibits antioxidant and neuroprotective effects. β-Amyloid (1-42), human TFA, after being monomericized by HFIP and dissolved in DMSO to form the stock solution, on the one hand, can form soluble oligomers (AβOs) when incubated at 4 °C, which have synaptic toxicity and neurotoxicity; on the other hand, it can be incubated at 37 °C to form insoluble fibrils, with lower neurotoxicity, and participating in the oxidative damage process. Aβ42 oligomers bind to various neuronal surface receptors (such as PrPc, mGluR5, NMDA receptors, etc.), triggering oxidative stress, calcium homeostasis imbalance, and synaptic toxicity via activating downstream signaling pathways, leading to neuronal dysfunction and death .
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27
27 Cited Publications
Cat. No.: HY-P1363A
CAS No.: 107761-42-2
Synonyms: Amyloid β-peptide (1-42) (human)
Target:  

Amyloid-β

Research Areas:  

Neurological Disease

β-Amyloid (1-42) (Amyloid β-peptide (1-42)), human, a 42-amino acid peptide that has not been treated with HFIP, is a brain-penetrant amyloid protein fragment, which can be used in research on Alzheimer's disease and Down’s syndrome. β-Amyloid (1-42), human remaining as a monomer exhibits antioxidant and neuroprotective effects. β-Amyloid (1-42), human, after being monomericized by HFIP and dissolved in DMSO to form the stock solution, on the one hand, can form soluble oligomers (AβOs) when incubated at 4 °C, which have synaptic toxicity and neurotoxicity; on the other hand, it can be incubated at 37 °C to form insoluble fibrils, with lower neurotoxicity, and participating in the oxidative damage process. Aβ42 oligomers bind to various neuronal surface receptors (such as PrPc, mGluR5, NMDA receptors, etc.), triggering oxidative stress, calcium homeostasis imbalance, and synaptic toxicity via activating downstream signaling pathways, leading to neuronal dysfunction and death .
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27
27 Cited Publications
Cat. No.: HY-P1363B
CAS No.: 107761-42-2
Target:  

Amyloid-β

Research Areas:  

Neurological Disease

β-Amyloid (1-42), human, HFIP-treated, a 42-amino acid peptide that has been treated with HFIP from β-Amyloid (1-42), human (HY-P1363A), is a brain-penetrant amyloid protein fragment, which can be used in research on Alzheimer's disease and Down’s syndrome. β-Amyloid (1-42), human, HFIP-treated remaining as a monomer exhibits antioxidant and neuroprotective effects. β-Amyloid (1-42), human, HFIP-treated, after being dissolved in DMSO to form the stock solution, on the one hand, can form soluble oligomers (AβOs) when incubated at 4°C, which have synaptic toxicity and neurotoxicity; on the other hand, it can be incubated at 37°C to form insoluble fibrils, with lower neurotoxicity, and participating in the oxidative damage process. Aβ42 oligomers bind to various neuronal surface receptors (such as PrPc, mGluR5, NMDA receptors, etc.), triggering oxidative stress, calcium homeostasis imbalance, and synaptic toxicity via activating downstream signaling pathways, leading to neuronal dysfunction and death .
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18
18 Cited Publications
Cat. No.: HY-10985
CAS No.: 437742-34-2
Purity:  99.13%
Synonyms: Salinosporamide A; NPI-0052
Marizomib (Salinosporamide A) is a second-generation, irreversible, brain-penetrant, pan-proteasome inhibitor. Marizomib inhibits the CT-L (β5), CT-T-laspase-like (C-L, β1) and trypsin-like (T-L, β2) activities of the 20S proteasome (IC50=3.5, 28, and 430 nM, respectively) .
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14
14 Cited Publications
Cat. No.: HY-10629
CAS No.: 875787-07-8
Purity:  99.95%
Synonyms: WAY 252623
Target:  

LXR

Research Areas:  

Metabolic Disease Cancer

LXR-623 is a brain-penetrant partial LXRα and full LXRβ agonist, with IC50s of 24 nM and 179 nM, respectively.
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