brain-penetrant

Edicotinib (JNJ-527) is a brain penetrant and orally active inhibitor of the colony-stimulating factor-1 receptor (IC50: 3.2 nM). It shows less inhibitory effects on KIT and FLT3 (IC50: 20 nM and 190 nM). It has the potential for Alzheimer's disease and rheumatoid arthritis treatment.

SR-3306 is a potent and highly inhibitor of brain penetrant JNK.

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.

Flupirtine maleate (Katadolon maleate), a centrally acting non-opioid analgesia, is the salt form of Flupirtine. It is an NMDA receptor antagonist , and also a specific neuronal potassium channel opener.

Dimethyl fumarate (DMF) is an Nrf2 activator with oral activity and blood-brain barrier permeability. Dimethyl fumarate has antimicrobial, anti-inflammatory, and immunomodulatory activities and has been used in the study of multiple sclerosis.

(R)-Lansoprazole (T 168390) is the R-isomer of lansoprazole and a substituted benzimidazole prodrug with selective and irreversible proton pump inhibitor activity.Lansoprazole (AG 1749) is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor)

Lansoprazole (A-65006) is a 2, 2, 2-trifluoroethoxypyridyl derivative of timoprazole that is used in the therapy of STOMACH ULCERS and ZOLLINGER-ELLISON SYNDROME. The drug inhibits H(+)-K(+)-EXCHANGING ATPASE which is found in GASTRIC PARIETAL CELLS. Lansoprazole is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor)

L-745870 trihydrochloride is a highly potent and selective D4 dopamine receptor antagonist.

S 38093 is a novel brain-penetrant antagonist/inverse agonist of H3 receptors.

2'MeO6MF is a brain-penetrant positive allosteric modulator at α2β1γ2L and all α1-containing GABAA receptors. It offers neuroprotection, improves functional recovery, and dampens the stroke-induced inflammatory response. 2'MeO6MF also has anxiolytic and sedative effects.

CTAP(TFA) (103429-32-9 free base) is a potent, highly selective, and brain-penetrant antagonist of the μ-opioid receptor with IC50 of 3.5 nM. It displays over 1200-fold selectivity over δ opioid (IC50=4500 nM) and somatostatin receptors. CTAP(TFA） (103429-32-9 free base) can be used for the study of L-DOPA-induced dyskinesia (LID)

SB399885 (SB 399885) is an effective, brain penetrant, and orally active antagonist of SR-6. It shows 200-fold selectivity for SR-6 over other serotonin receptors (pKi: 9.11, 8.81, and 9.02 for human recombinant, native rat, and native human SR-6 receptors, respectively).

BAY 73-6691 is an inhibitor of brain penetrant PDE9A.

JNJ-55308942 is a selective and brain-penetrant antagonist of P2X7 functional with IC50s of 10 and 15 nM and Kis of 7.1 and 2.9 nM for hP2X7 and rP2X7, respectively.

S 18986 is a selective, orally active, brain-penetrant positive allosteric modulator of AMPA-type receptors that enhances cognition in rodents by inducing the release of noradrenaline and acetylcholine in the rat hippocampus, subsequently improving object-recognition memory.

SR10067 is a potent, selective, and brain-penetrant agonist of Rev-Erbβ (IC50 = 160 nM) and Rev-Erbα (IC50 = 170 nM) with anxiolytic activity.

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].

ARN19702 is a selective, orally active, reversible, and brain-penetrant N-acylethanolamine acid amidase (NAAA) inhibitor with an IC50 of 230 nM for human NAAA, exhibiting a broad analgesic profile [1] [2].

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

Lorlatinib (PF-6463922) is an orally available, ATP-competitive inhibitor of the receptor tyrosine kinases, anaplastic lymphoma kinase (ALK) and C-ros oncogene 1 (Ros1), with potential antineoplastic activity.

SBI-553 is an effective and brain penetrant NTR1 allosteric modulator (EC50: 0.34 μM).

Cytosporone B (Dothiorelone G) is a naturally occurring agonist for the nuclear receptor Nur77 (IC50 = 0.278 nM). Activation of Nur77 with cytosporone B induces the expression of Nur77-dependent genes, including the gene for Nur77 itself. Signaling through Nur77 induces apoptosis in cancer cells and retards xenograft tumor growth. It also induces genes related to gluconeogenesis and decreases atherosclerosis progression in mice fed a high fat and high cholesterol diet. Cytosporone B is brain penetrant and aggravates early brain injury in rats when given (13 mg/kg intraperitoneally) after experimentally-induced subarachnoid hemorrhage. Cytosporone B also has antibacterial properties.

Omeprazole (Losec) is a proton pump inhibitor (PPI), Omeprazole(Losec) is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor).

GP130 receptor agonist-1 (N-(4-Fluorophenyl)-4-phenyl-2-thiazolami) is a potent, brain-penetrant and orally active GP130 receptor agonist.

Cambinol (SIRT1/2 Inhibitor IV) is a cell-permeable b-naphthol compound that inhibits the NAD-dependent deacetylase activity of SIRT1/2 (IC50: 56/59 μM, respectively) in a substrate-, but not NAD-, competitive manner. Cambinol inhibits SIRT5 deacetylase activity only at much higher concentrations (IC50 >300 μM) and no inhibitory for the class I and II HDACs. In BCL6-expressing Burkitt lymphoma cell lines, Cambinol-induced apoptosis has been attributed to the hyperacetylation of p53 and BCL6.Cambinol is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor)

S 38093 is a brain-penetrant antagonist of the H3 receptor (Ki: 8.8 1.44 1.2 μM, for rat mouse human).

PF-04995274 is an effective, high-affinity, and partial serotonin 4 receptor (5-HT4R) agonist. PF-04995274 is brain penetrant and can be used for cognitive disorders associated with Alzheimer's disease. PF-04995274 has an EC50 range of 0.26-0.47 nM for hu

Fenobam shows inverse agonist activity which blocks the mGlu5 receptor basal activity(IC50: 84 nM). Fenobam has anxiolytic activity. Fenobam is a selective and non-competitive mGluR5 antagonist acting at an allosteric modulatory site (Kd values are 54 and 31 nM for rat and human recombinant mGlu5 receptors, respectively).

PSEM 89S TFA is a brain-penetrant and selective ion channels agonist, and is orthogonally selective for Q79G and L141F, respectively.

JNJ-31020028 is a selective brain penetrant antagonist of neuropeptide Y2 receptor with high affinity(pIC50=8.07, human; pIC50=8.22, rat); it exhibits >100-fold selectivity for Y2 versus human Y1/Y4/Y5 receptors.

RN-1 dihydrochloride is an effective and selective irreversible inhibitor of lysine-specific demethylase 1 (LSD1, IC50 = 70 nM).

PQR620 is a novel potent and selective, brain penetrant inhibitor of mTORC1 2.

JCN037 is potent, non-covalent and brain-penetrant inhibitor of EGFR(EGFR, p-wtEGFR and pEGFRvⅢ with IC50 of 2.49 nM, 3.95 nM, 4.48 nM , respectively).

KCC-07 is a selective, potent and brain-penetrant inhibitor of methyl-CpG-binding domain protein 2(MBD2) with anticancer activity. KCC-07 prevents binding of MBD2 to methylated DNA and activates brain specific angiogenesis inhibitor 1 (BAI1) inducing anti

BMS-193885 is a selective, brain-penetrant, and competitive antagonist of the neuropeptide Y1 receptor with a Ki of 3.3 nM, and an IC50 of 5.9 nM for hY1.

LP-935509 is highly brain-penetrant and reverses fully established pain behavior following the SNL procedure. LP-935509 is also an effective inhibitor of BIKE (IC50=14 nM) and a modest inhibitor of GAK (IC50=320 nM). LP-935509 is a selective, ATP-competit

PW0787 is a potent, selective, orally active, and brain-penetrant GPR52 agonist (EC50=135 nM).

BRD-6929 is a selective, brain-penetrant HDAC1 and HDAC2 inhibitor (IC50:  1 and 8 nM). BRD-6929 (Cpd-60) shows high-affinity to HDAC1 and HDAC2 (Kis: 0.2 and 1.5 nM) [2]. BRD-6929 potentiates the efficacy of gnidimacrin (a PKC Agonist) against latent HIV

TG4-155 is a brain penetrant EP2 antagonist (KB = 2.4 nM) that is over 1000-fold less effective at EP4 (KB = 11.4 µM) and a panel of other receptors and channels

PF-06447475 is a highly effective, specific, brain penetrant LRRK2 inhibitor with IC0 of 3 11 nM for wild type LRRK2 and G2019S LRRK2 respectively.

PZ-2891 is an orally bioavailable, brain-penetrant pantothenate kinase (PANK) modulator, with an IC50 of 1.3 nM for hPANK3.

ML417 is a selective and brain-penetrant agonist of D3 dopamine (EC50: 38 nM).

ASK1-IN-1 is an inhibitor of apoptosis signal-regulating kinase 1 which is a key mediator in the apoptotic and inflammatory cellular stress response with an IC50 of 21 nM in biochemica assays.

IDH-305 is an orally available, mutation-selective, and brain-penetrant IDH1 inhibitor targeting the IDH1 (R132) mutation. It is 200-fold more selective for mutant IDH1 isoforms than wild type, with IC50s of 27 nM, 28 nM, and 6.14 nM for IDH1R132H, IDH1R132C, and IDH1WT, respectively.

Balovaptan (RG7314) is a highly potent and selective brain-penetrant vasopressin 1a (hV1a) receptor antagonist, with Kis of 1 and 39 nM for human (hV1a) and mouse (mV1a) receptors. It is used for the research of autism.

Tolebrutinib (PRN2246) is a potent, selective, orally active and brain-penetrant Bruton tyrosine kinase (BTK) inhibitor(IC50s of 0.4 and 0.7 nM in Ramos B cells and in HMC microglia cells, respectively). It exhibits efficacy in central nervous system immunity. Tolebrutinib can be used for the research of multiple sclerosis (MS).

RTICBM-189 is a potent, brain-penetrant allosteric modulator of the cannabinoid type-1 (CB1) receptor with a pIC50 of 7.54 in the Ca2+ mobilization assay, and exhibits pIC50s of 5.29 for hCB1 and 6.25 for mCB1.

AR-M 1000390 hydrochloride (ARM-390 HCl) , also known as ARM-390, is a low-internalizing nonpeptidic δ-selective opioid receptor agonist; derivative of SNC 80. Does not trigger acute desensitization of the analgesic response; reduces CFA-induced hyperalgesia. Brain penetrant following systemic administration.

Talnetant (SB 223412) is a selective, competitive NK3 receptor antagonist that penetrates the brain and modulates mesolimbic and mesocortical dopaminergic neurotransmission.

VU0483605 is an effective and selective positive allosteric modulator of mGluR1 with EC50s of 390 and 356 nM for human and rat, respectively.