Rilapladib is a selective Lipoprotein-Associated Phospholipase A2 (Lp-PLA2) inhibitor with an IC50 of 230 pM.
Nicardipine(YC-93) is a calcium channel blocker that has been widely used to control blood pressure in severe hypertension following events such as ischemic stroke, traumatic brain injury, and intracerebral hemorrhage.
GR 64349 is a potent and highly selective NK2 receptor peptide antagonist, with an EC50 of 3.7 nM in rat colon. GR 64349 exhibits selectivity >1000 and >300-fold with respect to NK1 and NK3 receptors, respectively[1][2].
CZC-25146 is a potent, selective and metabolically stable LRRK2 inhibitor with IC50 of 4.76 nM/6.87 nM for wild type LRRK2 and G2019S LRRK2 respectively.IC50 value: 4.76 nM/6.87 nM(wild type/G2019S LRRK2) [1]Target: LRRK2 CZC-25146displayed a very clean profile, it inhibited only five kinases (PLK4, GAK, TNK1, CAMKK2 and PIP4K2C) with high potency, none of which have been classified as predictors of genotoxicity or hematopoietic toxicity. CZC-25146 neither caused cytotoxicity in human cortical neurons at concentrations below 5μM over a seven-day treatment in culture nor did it block neuronal development in vitro. CZC-25146 possesses favorable pharmacokinetic properties, such as a volume of distribution of 5.4 L/kg and a clearance of 2.3 L/hr/kg that render it suitable for in-vivo studies.
Etifoxine Hcl(HOE 36-801) is potentiator of GABAA receptor function in cultured neurons. Etifoxine preferentially acts on β2 or β3 subunit-containing GABAA receptors. IC50 value:Target: GABAA receptorEtifoxine exhibits anxiolytic activity in rodents and humans with no sedative, myorelaxant or mnesic side effects. Etifoxine acts as a ligand of the translocator protein (TSPO); promotes axonal regeneration.
PZ-2891 is an oral, allosteric, and brain penetrant pantothenate kinase (PANK) modulator, acting as both an orthosteric inhibitor (IC50=1.3 nM) and an allosteric activator of PANK3 activity in the presence of acetyl-CoA.
Cannabisin D inhibits proliferation and migration of glioblastoma cells through MAPKs signaling[1].
Cardamonin is a novel antagonist of hTRPA1 cation channel with an IC50 of 454 nM.
OMDM-4 is a selective and metabolically stable inhibitor of anandamide cellular uptake (ACU), with a Ki 17.7 μM[1].
GNE-8505 is an orally available inhibitor of Dual leucine zipper kinase (DLK)[1].
Perphenazine dihydrochloride is an orally active dopamine receptor and histamine-1 receptor antagonist, with Ki values of 0.56 nM (D2), 0.43 nM (D3), .6 nM (5-HT2A), respectively. Perphenazine dihydrochloride also binds to Alpha-1A adrenergic receptor. Perphenazine dihydrochloride inhibits cancer cell proliferation, and induces apoptosis. Perphenazine dihydrochloride can be used in the research of mental disease, cancer, inflammation[1][3][5].
Fosgonimeton is a hepatocyte growth factor receptor agonist (WO2017210489)[1].
BGC-20-1531 (PGN 1531) free base is a potent and selective prostanoid EP4 receptor antagonist, with a pKb of 7.6. BGC-20-1531 free base has the potential for the research of migraine headache[1].
Ponezumab (PF-04360365) is a humanised anti-amyloid IgG2 monoclonal antibody. Ponezumab reduces Aβ levels in the central nervous system and improves performance in mice in various models of learning and memory. Ponezumab can be used in study of Alzheimer's disease[1].
Solifenacin Hcl(YM905 Hcl; Vesicare Hcl) is a muscarinic receptor antagonist.IC50 value:Target: muscarinic receptorSolifenacin Hcl (YM905; Vesicare) is a prescription medication used to treat certain bladder problems.
Pramipexole dihydrochloride hydrate is a selective dopamine D2-type receptor agonist, with Kis of 2.2 nM, 3.9 nM, 0.5 nM and 1.3 nM for D2-type receptor, D2, D3 and D4 receptors, respectively. Pramipexole dihydrochloride hydrate can be used for the research of Parkinson's disease (PD) and restless legs syndrome (RLS). Pramipexole dihydrochloride hydrate can cross the blood-brain barrier (BBB)[1][2][3].
Lobeline hydrochloride, a nicotinic receptor agonist, acting as a potent antagonist at both α3β2 and α4β2 neuronal nicotinic receptor subtypes.
MFZ 10-7 is a potent mGluR5 antagonist. Intraperitoneal administration of MFZ 10-7 inhibits intravenous cocaine self-administration, cocaine-induced reinstatement of drug-seeking behavior and cocaine-associated cue-induced cocaine-seeking behavior in rats[1]..
Met-Enkephalin-Arg-Phe is a naturally occurring heptapeptide with analgesic activity[1].
VCP171 is a potent adenosine A1 receptor (A1R) positive allosteric modulator (PAM). VCP171 is effective at decreasing excitatory synaptic currents in Lamina II of neuropathic pain model. VCP171 can be used for researching neuropathic pain[1].
Maprotiline HCl is a selective noradrenalin re-uptake inhibitor and a tetracyclic antidepressant.Target: OthersMaprotiline (sold as Deprilept, Ludiomil, Psymion) is a tetracyclic antidepressant (TeCA). However, Maprotiline's fourth ring is spurious, as formed by a bridge across the central tricyclic ring. It is a strong norepinephrine reuptake inhibitor with only weak effects on serotonin and dopamine reuptake. It exerts strong blocking effect at H1 receptors, moderate at 5-HT2 and alpha1 and weak blocking effect at D2 and mACh postsynaptic receptors [1, 2].
Lipid peroxidation inhibitor 1 is a lipid peroxidation inhibitor with an IC50 of 0.07 μM.
N-(3-Methoxybenzyl)stearamide a natural product from Lepidium meyenii (Maca), inhibits human and mouse soluble epoxide hydrolase (hsEH and msEH) with IC50s of 0.001 and <0.001 μg/nM, respectively[1].
(S)-Remoxipride ((-)-Remoxipride) is a selective dopamine D2-receptor antagonist with an IC50 value of 1.57 μM. (S)-Remoxipride can be used for the research of psychotic disorder[1].
Fenpropathrin is a synthetic pyrethroid insecticide in agriculture. Fenpropathrin may induces parkinsonian symptoms progressively[1].
Zimelidine dihydrochloride is a potent and selective inhibitor of serotonin 5-HT uptake and SERT. Zimelidine dihydrochloride is an antidepressant[1].
O-desmethyl Mebeverine acid is a metabolite of Mebeverine, which is a musculotropic antispasmodic drug.
Nomlabofusp is a cell-penetrating peptide TAT-cpp (1-12). Nomlabofusp can be used in the research of frataxin replacement therapy[1].
BPN-15477 is a potent SMC (splicing modulator compound) that restores correct splicing of ELP1 (Elongator complex protein 1) exon 20. BPN-15477 corrects splicing of the ELP1 transcript, significantly increases the level of functional protein in vivo in all tissues, including brain. BPN-15477 can be used for frontotemporal dementia research[1].
Pancuronium Dibromide is a bis-quaternary steroid that is a competitive nicotinic antagonist.Target: nAChRPancuronium dibromide is a competitive AChR antagonist (IC50 = 5.5 nM) and acts as a skeletal muscle relaxant. Pancuronium dibromide interrupts neuromuscular transmission by competing with acetylcholine for receptor sites on the motor end-plate. Pancuronium dibromide is a non-depolarizing agent. Pancuronium is a typical non-depolarizing curare-mimetic muscle relaxant. It acts as a competitive acetylcholine antagonist on neuromuscular junctions, displacing acetylcholine (hence competitive) from its post-synaptic nicotinic acetylcholine receptors. It is (unlike suxamethonium) a non-depolarizing agent, which means that it causes no spontaneous depolarizations upon association with the nicotinic receptor in neuromuscular junction, thus producing no muscle fasciculations upon administration [1-3].