brain function

TMPH is an inhibitor of nAChR and inhibits nAChRs lacking α5, α6, or β3 subunits. TMPH can be used in studies about nAChR dysfunction or neurological disorders.

PX-478 is a HIF-1α inhibitor with selectivity, oral activity, and blood-brain barrier permeability. PX-478 has antitumor activity and also protects pancreatic β-cell function in diabetes mellitus and is used in type 2 diabetes mellitus research.

C004019 belongs to PROTACs and is a tau protein-targeted degrader (via recruitment of VHL E3 ligase) with blood-brain barrier permeability and selective tau degradation capability. This compound significantly reduces tau levels and improves cognitive function, and is used in research on Alzheimer's disease and related tauopathies.

Atomoxetine hydrochloride (LY 139603) is the hydrochloride salt of atomoxetine, a phenoxy-3-propylamine derivative and selective non-stimulant, norepinephrine reuptake inhibitor with cognitive-enhancing activity. Although its precise mechanism of action is unknown, atomoxetine appears to selectively inhibit the pre-synaptic norepinephrine transporter, resulting in inhibition of the presynaptic reabsorption of norepinephrine and prolongation of norepinephrine activity in the synaptic cleft. The effect on cognitive brain function may result in improved attention and decreased impulsivity and activity levels.

Pivagabine (CXB-722), a hydrophobic 4-aminobutyric acid derivative, exhibits neuromodulatory activity and successfully penetrates the blood-brain barrier in rats. It counteracts the impact of foot shock on GABAA receptor function and corticotropin-releasing factor (CRF) levels in the rat brain.

Butanoic acid is an endogenous human metabolite, an endogenous histone deacetylase (HDAC) inhibitor. The IC50 of HDAC3, HDAC4 and HDAC1 were 2.4 mM, 4.5 mM and 5.3 mM, respectively. 3-Hydroxybutyric acid has the effects of energy metabolism, neuroprotection, anti-inflammatory, and improvement of insulin resistance.

CSF1R-IN-7 is a highly selective CSF-1R inhibitor with good brain penetration for the treatment of a variety of diseases associated with microglia-mediated neuroinflammation, particularly Alzheimer's disease and other neurodegenerative disorders.CSF-1R is a type III receptor tyrosine kinase that is expressed predominantly on microglia (immune cells in the brain) and regulates the development, survival and function of microglia.

1-(3,4-dihydroxyphenyl)-2-(dimethylamino)ethan-1-one hydrochloride is a cholinergic agent that inhibits choline metabolism, which leads to increased levels of acetylcholine in the brain, which in turn enhances cognitive function and memory.

PD 123319 ditrifluoroacetate is a selective, non-peptide angiotensin II type 2 (AT2) receptor antagonist, and PD 123319 ditrifluoroacetate demonstrates potent activity with IC50 values of 34 nM in rat adrenal tissue and 210 nM in rat brain, thereby providing a valuable pharmacological tool for elucidating AT2 receptor function in cardiovascular and renal physiology and supporting research in hypertension and related disorders.

SNT-207858 free base is a selective, blood brain barrier penetrating, potent and orally active antagonist of melanocortin-4 (MC-4) receptor(IC50 of 22 nM (binding) and 11 nM (function), on the MC-4 receptor).

SNT-207858 is a selective, blood brain barrier penetrating, potent and orally active antagonist of melanocortin-4 (MC-4) receptor. SNT207858 has an IC50 of 22 nM (binding) and 11 nM (function) on the MC-4 receptor.

Leriglitazone is a brain barrier-permeable, orally active PPARγ agonist (EC50=9 μM) and mitochondrial function modulator with neuroprotective, anti-inflammatory, and antioxidant properties for neurodegenerative disease research.

Pyrocatechol sulfate, a phenolic metabolite found in human plasma, is associated with the intake of specific foods such as berries and the state of the gut microbiome. It serves as a potential urinary biomarker for kidney function, dialysis clearance rates, whole grain consumption, and regular coffee intake. Additionally, in conjunction with other phenolic sulfates, pyrocatechol sulfate plays a role in regulating various biological functions, including those related to brain health and the rhythmic beating of cardiac cells.

TAC (TERT activator compound) is a TERT (telomerase reverse transcriptase) activator that enhances TERT transcriptional activity through the MEK/ERK/AP-1 cascade pathway, promotes telomere synthesis in primary human cells and naturally aged mice, reduces cellular senescence and inflammatory cytokines, and alleviates neuroinflammation, among other effects.

Cinoxopazide is recognized for its potential to enhance cognitive efficiency in healthy individuals, support brain function in the elderly, and address issues arising from attentiveness and/or memory impairments. This compound is used to boost cognitive function, aiding in maintaining brain health for the elderly while also offering intellectual stimulation benefits for typical adults.

KNa1.1-IN-2 (Compound Z05) is a selective KNa1.1 channel inhibitor capable of penetrating the blood-brain barrier, and exhibits significant efficacy on hERG channels. It binds to KNa1.1 channels, effectively blocking channel activity caused by Gain-of-function (GOF) mutations, thus intervening in KCNT1-related seizures. Additionally, it inhibits the GOF mutant Y796H, making KNa1.1-IN-2 a promising candidate for research into KCNT1-associated epilepsy disorders.

N-Octanoyl dopamine surpasses dopamine in preserving the contractile function of donor hearts from brain-dead individuals. Additionally, N-Octanoyl dopamine inhibits cytokine production in activated T cells and reduces the expression of MHC-II and adhesion molecules in endothelial cells stimulated by IFNγ.

BuChE-IN-16 (Compound 6a) is an orally active, blood-brain barrier-permeable, and selective BuChE inhibitor with an IC50 of 0.33 μM. It exhibits anti-inflammatory and neuroprotective effects, improves cognitive function in Alzheimer's disease (AD) zebrafish models, and alleviates scopolamine-induced memory impairment in mice. BuChE-IN-16 is applicable for Alzheimer's disease research.

Nrf2 activator 19 is a compound capable of crossing the blood-brain barrier and acts as an NRF2/HO-1 activator, offering potent antioxidant and neuroprotective effects. It effectively reduces brain damage and minimizes the accumulation of Reactive Oxygen Species (ROS). Additionally, Nrf2 activator 19 inhibits neuronal apoptosis, aiding in the recovery of neural function and motor skills. It has demonstrated significant potential in ischemic stroke research.

BLINK11 is a blood-brain barrier-permeable inhibitor of Cdk5. It reduces the activity of CDK5 by targeting CDK5/p35 (IC50 = 17.09 nM) and CDK5/p25 (IC50 = 14.69 nM) complexes. BLINK11 exhibits antidiabetic and neuroprotective properties, lowers blood glucose levels in type 2 diabetes (T2D) mice, enhances cognitive function, and reduces neurodegenerative lesions.

17-Hydroxypregnenolone sulfate sodium is a crucial intermediate product in the synthesis of adrenal and gonadal steroids with brain permeability. It acts as a precursor in the biosynthesis of steroid hormones [such as glucocorticoids, sex hormones]. This compound shows potential for use in research related to adrenal function development and neurosteroid-associated diseases [such as cognitive disorders, neurodegenerative diseases].

AChE/BChE-IN-27 is a brain-permeable dual inhibitor of AChE and BChE, with IC50 values of 3.72 μM and 9.65 μM, respectively, and a permeability coefficient (Pe) of 4.12. It exhibits significant antioxidant activity with an IC50 of 6.32 μM in DPPH assays and also demonstrates strong in vitro antioxidant capabilities. The compound shows metal-chelating properties and has neuroprotective potential against oxidative stress by significantly reducing intracellular reactive oxygen species (ROS). In vivo experiments reveal that AChE/BChE-IN-27 effectively restores AChE and BChE levels and improves cognitive function, indicating its potential application for Alzheimer’s disease (AD).

BChE-IN-41 is a highly selective butyrylcholinesterase (BChE) inhibitor with an IC50 of 12 nM and a Ki of 6.6 nM. It exhibits significant brain permeability, with a brain-to-plasma ratio of 9.0. BChE-IN-41 enhances cognitive function in mice with scopolamine and Aβ1-42-induced symptoms of Alzheimer's disease.

RNA splicing modulator-4 (Compound A) is an orally active, brain-penetrant, and selective modulator of RNA splicing. It regulates alternative splicing events to control the inclusion or exclusion of specific exons in precursor mRNA (pre-mRNA), thereby altering the coding sequence and function of mature mRNA. RNA splicing modulator-4 is promising for research in neurodegenerative diseases (such as Huntington's disease) and cancer.