Liquiritigenin, a flavanone isolated from Glycyrrhiza uralensis, is a highly selective estrogen receptor β (ERβ) agonist with an EC50 of 36.5 nM for activation of the ERE tk-Luc.
RuBi-GABA is a new ruthenium-based caged GABA compound. RuBi-GABA photocleaves and releases GABA after being excited with visible wavelengths. RuBi-GABA produces gaba receptor-mediated currents[1].
A highly selective, potent, BBB penetrant and orally bioavailable 5-HT6R antagonist for the treatment of neurological disorders such as AD and schizophrenia; significantly restores both scopolamine- and MK-801-induced cognitive dysfunction and demonstrates antipsychotic potential. Alzheimer Disease Phase 2 Clinical
Erteberel (LY500307) is a potent and selective estrogen receptor beta (ERβ) inhibitor with Ki and EC50 of 1.54 nM and 3.61 nM, respectively[1]. Anti-tumor activities[2].
Chromogranin A (324-337), human is a peptide fragment of chromogranin A, it can be isolated from human ileal carcinoid tumor. Chromogranin A is a soluble glycoprotein stored with hormones and neuropeptides in secretory granules of most (neuro)endocrine cells and neurons, and it is also a plasma marker of neuroendocrine tumors[1][2].
α-Synuclein (45-54) (human) is the 45-54 fragment of α-Synuclein. α-Synuclein is an abundant neuronal protein that is highly abundant in presynaptic nerve terminals. α-Synuclein is a biomarker for Parkinson's disease (PD)[1].
Orexin B, human is an endogenous agonist at Orexin receptor with Kis of 420 and 36 nM for OX1 and OX2, respectively.
β-Amyloid peptide(16-20) is a amino acid sequences (KLVFF) of Amyloid-β (Abeta). β-Amyloid peptide(16-20) is an effective inhibitor of Abeta fibril formation, with RG-/-GR-NH2 residues added at N- and C-terminal ends to aid solubility)[1].
PD 120697 is an orally active dopamine (DA) agonist. PD 120697 inhibits striatal DA synthesis, DA neuronal firing, spontaneous locomotor activity, and reverses Reserpine (HY-N0480)-induced depression[1].
Vitamin B15 (Pangamic Acid) hemicalcium is a natural, ubiquitously in plant seeds substance and can used be as an agent stimulating cellular respiration. Vitamin B15 hemicalcium contains D-gluconodimethyl amino acetic acid. Vitamin B15 hemicalcium is also a immune-correcting agent[1][2]. Vitamin B15 hemicalcium can be used for wide range of diseases.
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.
GNE-8505 is an orally available inhibitor of Dual leucine zipper kinase (DLK)[1].
Fosgonimeton is a hepatocyte growth factor receptor agonist (WO2017210489)[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].
GR125487 sulfamate is an orally active and selective antagonist of 5-HT4R. GR125487 sulfamate effectively blocks the cognition enhancing effect. GR125487 sulfamate can be used to study memory disorders, gastrointestinal disorders, mood disorders and urinary tract dysfunction[1].
AK-7 is a selective cell- and brain-permeable SIRT2 inhibitor, with an IC50 of 15.5 μM.
Neuchromenin is a microbial melabolite that can be isolated from the culture broth of Eupenicillium javanicum var. meloforme PFll81. Neuchromenin induces neurite outgrowth of PC12 cells[1].
Mephenoxalone inhibits neuron transmission and can relax skeletal muscles by inhibiting the reflex arc[1].
Nicotinamide riboside malate, an orally active NAD+ precursor, increases NAD+ levels and activates SIRT1 and SIRT3. Nicotinamide riboside malate is a source of vitamin B3 (niacin) and enhances oxidative metabolism, protection against high fat diet-induced metabolic abnormalities[1]. Nicotinamide riboside malate reduces cognitive deterioration in a transgenic mouse model of Alzheimer’s disease[2].
hMAO-B-IN-5(B15) is a potent, selective and reversible inhibitor of human monoamine oxidase hMAO-B with IC50 of 0.12 μM. hMAO-B-IN-5 can pass through the blood-brain barrier and can be used in the research of neurodegenerative diseases[1].
UBP316 (ACET) is a highly potent and selective kainate receptor GluK1 (GluR5) antagonist, with a Kb value of 1.4 nM. UBP316 is effective at blocking the depression of both field excitatory postsynaptic potentials (fEPSPs) and monosynaptically-evoked GABAergic transmission induced by ATPA, a GluK1 selective agonist[1].
KY-226 (KY226) is a potent, allosteric, orally active inhibitor of protein tyrosine phosphatase 1B (PTP1B) with IC50 of 0.28 uM (human PTP1B), does not exhibit PPARγ agonist activity; shows no effects on adipocyte differentiation in rodent preadipocytes at 10 uM, bot not the PPARγ agonist pioglitazone; increases the phosphorylated insulin receptor (pIR) produced by insulin in human hepatoma-derived cells (HepG2) at 0.310 uM, significantly reduces plasma glucose and triglyceride levels as well as hemoglobin A1c values without increasing body weight gain in db/db mice, exerts anti-diabetic and anti-obesity effects by enhancing insulin and leptin signaling.
SCH 50911 hydrochloride, (+)-(S)-5,5-dimethylmorpholinyl-2-acetic acid, a selective, orally-active and competitive γ-Aminobutyric acid B GABA(B) receptor antagonist, binds to GABA(B) receptor with IC50 of 1.1 μM. SCH 50911 hydrochloride antagonizes GABA(B) autoreceptors, increasing the electrically-stimulated 3H overflow with an IC50 of 3 μM.
CGP13501 is a positive allosteric modulator of GABAB receptor. CGP13501 is a structural analogue of propofol[1].
Noscapine hydrochloride ((S,R)-Noscapine hydrochloride) is an orally active phthalideisoquinoline alkaloid with potent antitussive. Noscapine hydrochloride exerts its antitussive effects by activating sigma opioid receptors and is a non-competitive Bradykinin inhibitor. Noscapine hydrochloride disrupts microtubule dynamics, induces mitotic arrest and apoptosis. Noscapine hydrochloride possesses anticancer, neuroprotective, anti-inflammatory activities, and can crosse the blood-brain barrier[1][2][3][4][5].
NBI-921352 (XEN901) is a potent inhibitor of sodium channels, specially targeting Nat/1.6 channels. NBI-921352 (XEN901) treats the nervous system pathologies of epilepsy effectively without adverse side effects (extracted from patent WO2017201468A1)[1].
SSR411298 is an orally active, selective and reversible fatty acid amide hydrolase (FAAH) inhibitor. SSR411298 has the potential for post-traumatic stress disorder research[1].
CHIC35, an analog of EX-527, is a potent and selective inhibitor of SIRT1 (IC50=0.124 µM). CHIC35 shows potential selective inhibition against SIRT1 over SIRT2 (IC50=2.8 µM) or SIRT3 (IC50>100 µM)[1]. CHIC35 has anti-inflammatory effects and can be used for CHARGE syndrome research[1][2].