barrier

Metformin hydrochloride (1,1-Dimethylbiguanide hydrochloride), a widely used anti-diabetic drug, exhibits potential anti-Y properties by inhibiting the proliferation of various Y cells, including colon and prostate.

Rutin (Quercetin 3-O-rutinoside), a flavonoid, has a variety of biological activities including antiallergic, anti-inflammatory, antiproliferative, and anticarcinogenic properties.

Metformin (1,1-Dimethylbiguanide) is an AMPK activator with blood-brain barrier permeability. Metformin may improve glycemic control by increasing insulin sensitivity and decreasing intestinal glucose uptake, and is commonly used in type 2 diabetes research.

Rutin hydrate (Sophorin), a kind of glycoside, widely exists in many plants including citrus fruit.

L-DOPA (Levodopa) is an orally active metabolic precursor of the neurotransmitter dopamine. It can cross the blood-brain barrier and be converted into dopamine in the brain. L-DOPA exhibits anti-hyperalgesic effects and holds potential in Parkinson’s disease research, and it can also be used to induce Parkinson’s disease models.

Ceramides Mixture, an endogenous ceramide, consists of hydroxy and non-hydroxy fatty acid-containing ceramides. It is involved in the regulation of cell cycle arrest, growth inhibition, and modulation of telomerase activity.

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.

Myristyl nicotinate (Tetradecyl nicotinate) is an ester prodrug being developed for delivering nicotinic acid (NIC) into the skin to prevent actinic keratosis and its progression to skin cancer.

SR 57227 hydrochloride(SR 57227A ) is a potent, orally active and selective 5-HT3 receptor agonist. It with ability to cross the blood brain barrier. It has affinities (IC50) varying between 2.8 and 250 nM for 5-HT3 receptor binding sites in rat cortical membranes and on whole NG 108-15 cells or their membranes. Anti-depressant effects.

Physostigmine, a parasympathomimetic alkaloid, is a reversible cholinesterase inhibitor. It extracts from the Calabar bean.

Ebselen (CCG-39161) is a organoselenium compound with anti-inflammatory, anti-oxidant and cytoprotective activity. Ebselen acts as a glutathione peroxidase mimetic and is thereby able to prevent cellular damage induced by reactive oxygen species (ROS). In addition, this agent inhibits the activity of a variety of enzymes including nitric oxide synthase (NOS), 5-lipoxygenase, cyclooxygenase, protein kinase C (PKC), NADPH oxidase and gastric H+/K+-ATPase. Furthermore, ebselen may be neuroprotective due to its ability to neutralize free radicals upon NMDA receptor activation thus, reducing lipoperoxidation mediated by glutamate-induced excitotoxicity.

LM11A-31 dihydrochloride is a water-soluble, non-peptide with high blood-brain barrier permeability.LM11A-31 dihydrochloride, a p75NTR (neurotrophin receptor p75) Ligand, is a potent proNGF (nerve growth factor) antagonist.

Seltorexant (JNJ-42847922) crosses the blood-brain barrier and quickly occupies OX2R binding sites in the rat brain. Seltorexant is a high-affinity and selective orexin-2 receptor antagonist (pKi: 8.0 and 8.1 for human and rat OX2R).

DG-041 is an antagonist of high-affinity EP3 receptor (IC50s: 4.6 nM and 8.1 nM in the binding and FLIPR assay, respectively). DG-041 inhibits PGE2 facilitation of platelet aggregation and has the blood-brain barrier permeability.

Tandutinib (CT53518) (MLN518, CT53518), an effective FLT3 antagonist (IC50: 0.22 μM), can also inhibit c-Kit and PDGFR, 15-20 fold higher potency for FLT3 versus CSF-1R and >100-fold selectivity for the same target versus FGFR, EGFR, and KDR.

SB-3CT is a potent and specific gelatinase inhibitor for MMP-2 (Ki = 13.9 nM) and MMP-9 (Ki = 600 nM).

MK-0752, a γ-secretase inhibitor, reduces Aβ40 production(IC50=5 nM).

JNJ-63533054 is a potent and selective agonist of hGPR139 with an EC50 = 16 nM.

Cefoselis Sulfate is a widely used beta-lactam antibiotic.

Carbetocin is an obstetric drug used to control postpartum hemorrhage and bleeding after giving birth.

Carbetocin acetate is an obstetric drug used to control postpartum hemorrhage and bleeding after giving birth.

Metoprine is a potent inhibitor of histamine N-methyltransferase (HMT), with potential antineoplastic activity.

MAGL-IN-4 (His121 ARG57) is one of the monoacylglycerol lipase (MAGL) inhibitors in central nervous system-related diseases.

Emodin 6-O-β-D-glucoside (Glucoemodin) can protect barrier integrity and inhibit HMGB1-mediated inflammatory responses, which suggests a potential use as a therapy for sepsis or septic shock. Emodin 6-O-beta-D-glucoside has anti-inflammatory activities and also may have significant therapeutic benefits against diabetic complications and atherosclerosis.