brain-permeable

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.

SRT 2104 (GSK2245840) is a selective and brain-permeable SIRT1 activator.

Apyramide is an anti-inflammatory agent (NSAID) that acts as a prodrug of indomethacin, a potent, blood-brain permeable, and nonselective inhibitor of COX1 and COX2.

Atabecestat (JNJ-54861911) is a potent, brain-penetrant, and orally active β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor that achieves robust and high CSF Aβ reduction, is well-tolerated, and displays sustained pharmacokinetic (PK) and pharmacodynamic (PD) characteristics. Atabecestat (JNJ-54861911) has the potential for Alzheimer's Disease treatment[1].

AZD 9272 is a brain-permeable mGluR5 antagonist for the study of gastroesophageal reflux.

JNJ-39220675 (JNJ 39220675) is a selective and brain permeable histamine H3 receptor antagonist.

SB-277011 hydrochloride (SB-277011A hydrochloride) is a potent, selective, and orally active dopamine D3 receptor (D3R) antagonist that crosses the blood-brain barrier, with Ki values of 10.7 nM for rodent D3R and 11.2 nM for human D3R. It is 80-100 times more selective for D3 receptors than other dopamine receptors, acting on D3 receptors (pKi: 8.0), D2 receptors (pKi: 6.0), 5-HT1B receptors (pKi < 5.2), and 5-HT1D receptors (pKi: 5.9).

GSK-3 inhibitor 4 is an orally active and brain-permeable compound that acts as a triple inhibitor of GSK-3, CDK2, and CDK5, with IC50 values of 0.56 nM (GSK-3β), 0.45 nM (GSK-3α), 0.47 μM (CDK2), and 0.68 μM (CDK5). It effectively reduces Tau protein levels and can be used in the study of Alzheimer's disease.

GSK-3 inhibitor 3 is a selective, orally active, brain-permeable GSK-3 inhibitor that inhibits GSK-3α and GSK-3β with IC50s of 0.35 nM and 0.25 nM, respectively.GSK-3 inhibitor 3 reduces the phosphorylation level of tau protein S396 with an IC50 of 10 nM in a triple transgenic mouse model of Alzheimer's disease. GSK-3 inhibitor 3 reduced the phosphorylation level of tau protein S396 in a triple transgenic mouse model of Alzheimer's disease, with an IC50 of 10 nM.GSK-3 inhibitor 3 can be used for the study of neurological diseases.

NT-0796 is a brain-permeable, potent, and selective inhibitor of the inflammasome NLRP3, inhibiting NLRP3 activation.NT-0796 is a potential NDT-19795 delivery vector.

pCPA methyl ester hydrochloride (4-Chloro-DL-phenylalanine methyl ester hydrochloride) is an inhibitor of tryptophan hydroxylase inhibitor and 5-HT synthesis. pCPA methyl ester hydrochloride is permeable across the blood-brain barrier and reduces 5-HT central availability.

AK-7 is a brain-permeable SIRT2 inhibitor and to characterize its cholesterol-reducing properties in neuronal models with an IC50 of 15.5 μM.

GNE-5729 is a positive allosteric modulator of NMDAR with the advantage of crossing the blood-brain barrier and being orally available, with EC50 values of 37 nM, 4.7 μM and 9.5 μM for GluN2A, GluN2C and GluN2D, respectively, and can be used for the study of neurological and psychiatric disorders.

AZD1080 is a selective, orally active, brain permeable GSK3 inhibitor.

BI-D1870 is a highly specific, blood-brain-permeable, and ATP-competitive inhibitor of the N-terminal AGC kinase domain of RSK, with IC50 values ​​of 31 nM, 24 nM, 18 nM, and 15 nM for RSK1, RSK2, RSK3, and RSK4.

Verubulin hydrochloride (MPC-6827 hydrochloride) is a blood-brain barrier permeable microtubule-disrupting agent with potent and broad-spectrum cytotoxic activities and significant anticancer efficacy in human MX-1 breast cancer and various mouse xenograft cancer models.

MSC 2032964A is a potent selective ASK1 inhibitor (IC50 = 93 nM) that is oral bioavailable and brain permeable. It inhibited neuroinflammation in mouse EAE models and blocked LPS-induced phosphorylation of ASK1 and p38 in cultured mouse astrocytes.

hCAII-IN-9 is a potent carbonic anhydrase inhibitor with IC50 values of 1.18 μM for hCA II, 0.17 μM for hCA IX, and 2.99 μM for hCA XII. It is not blood-brain barrier permeable.

Casopitant mesylate (GW679769B) is a selective, brain-permeable, and orally active antagonist of the neurokinin 1 (NK1) receptor, and it is the second in its class of antiemetics.

EML741 also inhibits DNMT1 (IC50, 3.1 μM), with no effect on DNMT3a or DNMT3b. EML741 exhibits low cell toxicity, and is membrane permeable and blood-brain barrier penetrated. EML741 is a histone lysine methyltransferase G9a GLP inhibitor, with an IC50 of 23 nM, Kd of 1.13 μM for G9a.

nAChR agonist 1 (DUN71755) is a brain-permeable and orally efficacious positive allosteric α7 nicotinic acetylcholine receptor (α7 nAChR)modulator.

SRT3657 is a brain-permeable SIRT1 activator, has neuroprotective effect.

SR59230A hydrochloride (SR59230A HCl) is a blood-brain permeable, selective and highly potent β3-adrenergic receptor antagonist that inhibits ultradian brown adipose tissue thermogenesis and interrupts associated paroxysmal brain and body heating.

3-Acetyldeoxynivalenol is a trichothecene mycotoxin deoxynivalenol acetylated derivative and a blood-brain barrier (BBB) permeable mycotoxin.