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Search Results for " selective,blood-brain barrier "

20

Compounds

Cat No. Product Name Synonyms Targets
T12877L Seltorexant JNJ-42847922 OX Receptor
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 a...
T20570 Labetalol Apo-Labetalol,Albetol,Trandate,Dilevalol,Normodyne Adrenergic Receptor
Labetalol (Apo-Labetalol) is a mixed alpha/beta-adrenergic antagonist.It is used to treat high blood pressure. It can be given by mouth for long term hypertension management or intravenously in severe hypertensive situat...
T17211 Vafidemstat ORY-2001 Histone Demethylase , MAO
Vafidemstat (ORY-2001) is a selective, orally active lysyl-histone demethylase (LSD1)/MAO-B inhibitor that crosses the blood-brain barrier for the study of neurological diseases.
T2708 SL327 SL 327,SL-327 MEK , DNA/RNA Synthesis
SL327 is a selective inhibitor for MEK1/2 with IC50 of 0.18 μM/0.22 μM; able to transport through the blood-brain barrier.
T10855 CO23 Thyroid hormone receptor(THR)
CO23 is a blood-brain barrier penetrant and selective TRα agonist and can be used in studies about the regulation of growth and development.
T9070 ASP2905 ASP-2905 Potassium Channel
ASP-2905 is a potent and selective inhibitor of potassium channel Kv12.2 encoded by the Kcnh3/BEC1 gene. It can cross the blood-brain barrier and has antipsychotic activities
T13423 (1R,2R)-2-PCCA hydrochloride (1R,2R)-2-PCCA(hydrochloride) Others
(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.(1R,2R)-2-PCCA hydrochloride can be used to study...
T38001 LEI-401 LEI 401 Phospholipase
LEI-401 is a selective and potent NAPE-PLD inhibitor that crosses the blood-brain barrier (IC50: 27 nM).LEI-401 reduces the level of n-acylethanolamines (NAEs) in the brain of free-ranging mice and modulates their emotio...
T79213 AZD4747 Ras
AZD4747 is a selective and potent inhibitor of the mutant GTPase KRASG12C that crosses the blood-brain barrier and has potential antitumor activity for the study of pancreatic and colorectal adenocarcinoma.
T67764 HMAO-B-IN-4 MAO
hMAO-B-IN-4 is a selective, reversible and bloodbrain barrier (BBB) penetrable inhibitor of human monoamine oxidase-B (hMAO-B, IC50=0.067 μM, Ki= 0.03 μM, hMAO-A, IC50= 33.82 μM).
T16489 Darigabat CVL-865,PF-6372865,PF-06372865 GABA Receptor
Darigabat (PF-06372865) is an orally active and selective GABAA receptor modulator that crosses the blood-brain barrier and exhibits anxiolytic activity, with Ki values of 2.9 nM, 21 nM, and 134 nM for α2, α1 PAM, and α2...
T60796 Cholesterol 24-hydroxylase-IN-1
Cholesterol 24-hydroxylase-IN-1 (compound 17) is a potent, orally active, and highly selective inhibitor of cholesterol 24-hydroxylase (CH24H or CYP46A1) with IC50 of 8.5 nM that can cross blood-brain barrier [1].
T22171 WWL123 MAGL
WWL123 is a potent and selective ABHD6 inhibitor (IC50=430 nM). WWL123 crosses the blood-brain-barrier and inhibits ABHD6 in brain parenchyma. ABHD6 blockade by WWL123 exerts an antiepileptic effect in Pentylenetetrazole...
T10585 Bozitinib CBT-101,PLB-1001 c-Met/HGFR
Bozitinib (PLB-1001) (PLB-1001) is a highly selective inhibitor of the c-MET kinase with blood-brain barrier permeability. Bozitinib binds to the conventional ATP-binding pocket of the tyrosine kinase superfamily.
T10202 A 1070722 GSK-3
A 1070722 is a potent and selective GSK-3 inhibitor, with a Ki of 0.6 nM for both GSK-3α and GSK-3β. It can penetrate the blood-brain barrier (BBB) and accumulates in brain regions, thus potential for PET radiotracer for...
T39214L LXE408 fumarate LXE408 fumarate (1799330-15-6 Free base) Proteasome
LXE408 fumarate is an orally active, non-competitive and kinetoplastid-selective proteasome inhibitor. LXE408 fumarate has an IC50 of 0.04 μM for L. donovani proteasome and an EC50 of 0.04 μM for L. donovani. LXE408 fuma...
T9146 Ms48107 Benzenemethanol, 2-[4-amino-6-[[(4-phenoxyphenyl)methyl]amino]-1,3,5-triazin-2-yl]-3-fluoro- Others
MS48107 is a potent, selective positive allosteric modulator of G protein-coupled receptor 68 (GPR68), demonstrating specificity for GPR68 over closely related proton GPCRs, neurotransmitter transporters, and hERG ion ch...
T16962 SW-100 HDAC
SW-100 is a selective histone deacetylase 6 inhibitor (IC50: 2.3 nM). It also shows at least 1000-fold selectivity for HDAC6 relative to all other HDAC isozymes. SW-100 displays an obviously improved ability to cross the...
T72953 Zidesamtinib NVL-520 ROS Kinase
Zidesamtinib (NVL-520) is an orally active, selective, potent, and blood-brain-barrier-crossing inhibitor of ROS1 fusion and resistance mutations, inhibits ROS1 and ROS1 G2032R, and can be used in the study of non-small-...
T61934 Repinotan
Repinotan (BAY x 3702 free base) is an effective, selective, blood-brain barrier permeable, oral active 5-HT1A receptor agonist. The Ki values of Repinotan are 0.19 nM (calf hippocampus), 0.25 nM (rat and human cortex) a...
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