blood-brain

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.

L-DOPA (Levodopa) is an amino acid precursor of dopamine with antiparkinsonian properties. It is a prodrug converted to dopamine by DOPA decarboxylase and can cross the blood-brain barrier. In the brain, levodopa is decarboxylated to dopamine, stimulating dopaminergic receptors and compensating for depleted endogenous dopamine in Parkinson's disease. To ensure adequate concentrations reach the central nervous system, levodopa is administered with carbidopa, a decarboxylase inhibitor that does not cross the blood-brain barrier, reducing peripheral decarboxylation and increasing CNS dopamine delivery.

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.

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

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.

Elamipretide (MTP-131) is a mitochondria-targeted antioxidant tetrapeptide (D-Arg-dimethylTyr-Lys-Phe-NH2) that reduces toxic reactive oxygen species (ROS) production and stabilizes cardiolipin, with blood-brain-barrier permeability. It is a potential therapeutic agent in the rare disease of Barnes syndrome.

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.

SC79 is an AKT agonist with specificity and blood-brain barrier permeability. SC79 specifically binds to the PH domain of AKT, activates cytoplasmic AKT, and inhibits AKT membrane translocation. SC79 has neuroprotective activity.

PLX5622 is a highly selective, brain-penetrant, and orally active CSF1R inhibitor.

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

VX-984 (M9831) is an oral, selective DNA-PK inhibitor that can cross the blood-brain barrier. VX-984 inhibited the conjugation of non-homologous terminal NHEJ and acted on DSBs to break DNA double strand. VX-984 is commonly seen in glioblastoma (GBM) and non-small cell lung cancer (NSC-LC) studies.

Salvianolic acid A (Dan Phenolic Acid A) is a natural product and an inhibitor of matrix metalloproteinase 9 (MMP-9). Salvianolic acid A has antioxidant and anti-inflammatory activity and protects the blood-brain barrier.

Clozapine N-oxide is the major metabolite of Clozapine and is blood-brain barrier permeable. Clozapine N-oxide is an agonist of DREADDs and activates the DREADD receptors hM3Dq and hM4Di. Clozapine N-oxide is also a dopamine antagonist and selective muscarinic M4 receptor agonist.

TIC10 (ONC-201) inactivates Akt and ERK to induce TRAIL through Foxo3a, possesses superior drug properties: delivery across the blood-brain barrier, superior stability and improved pharmacokinetics. Phase 1 2.

C-176 (STING inhibitor 1) is a STING inhibitor with selectivity and blood-brain barrier permeability. C-176 inhibits STING-mediated IFNβ production and possesses anti-inflammatory activity.

MPTP hydrochloride is a precursor of MPP+, a dopamine neurotoxin with blood-brain barrier permeability. MPTP hydrochloride is toxic to dopaminergic neurons, which can lead to Parkinson's disease, and is widely used in the construction of animal models of Parkinson's disease.

Temozolomide (TMZ) is a DNA alkylating agent with blood-brain barrier permeability and oral activity. Temozolomide has antitumor activity and antiangiogenic activity, and also induces apoptosis and autophagy. Temozolomide is stable under acidic conditions and hydrolyzes under neutral or slightly alkaline conditions.

Cholesterol 24-hydroxylase-IN-1 is an orally active, selective, and potent inhibitor of cholesterol 24-hydroxylase (CH24H or CYP46A1) that crosses the blood-brain barrier.Cholesterol 24-hydroxylase-IN-1 may be useful in the study of epilepsy-like neurological disorders. Cholesterol 24-hydroxylase-IN-1 is used to study epilepsy-like neurological diseases.

MW01-2-151SRM is a novel small molecule inhibitor of microglia activation that crosses the blood-brain barrier, has anti-neuroinflammatory effects, attenuates the up-regulation of glial cytokines in models of neuroinflammation, and can be used in studies of traumatic brain injury, Alzheimer's disease, and alginate toxicity.

(1R,2R)-2-PCCA hydrochloride is a potent, selective, and blood-brain-barrier-crossing GPR88 receptor agonist with an EC50 value of 1140 n in striatal membranes of WT mice; it can be used to study the central nervous system.

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

Diaziquone (NSC-182986) is a water-soluble synthetic azacyclic benzoquinone that enhances penetration of the blood-brain barrier, has antitumor activity, and is used in the treatment of extreme renal failure.

AGI-43192 is a potent methionine adenosine transferase 2A (MAT2A) inhibitor that penetrates the blood-brain barrier. AGI-43192 inhibits S-adenosine methionine (SAM) production metabolic enzyme and methionine adenosine transferase 2A (MAT2A), which has the potential to study the role of SAM regulation in the central nervous system (CNS) and the treatment of cancer diseases.

Masupirdine mesylate (SUVN-502 mesylate) is a selective 5-HT6 receptor antagonist that crosses the blood-brain barrier and is utilized in the study of neurological disorders such as Alzheimer's disease and dementia.