ALZ-801 is an orally available, small-molecule β-amyloid (Aβ) anti-oligomer and aggregation inhibitor, valine-conjugated prodrug of Tramiprosate with substantially improved PK properties and gastrointestinal tolerability compared with the parent compound[1]. ALZ-801 is an advanced and markedly improved clinical candidate for the treatment of Alzheimer’s disease[2].
Hoechst 34580 is a cell-permeable fluorescent dye for staining DNA and nuclei.
AChE/hCA I/II-IN-1 (Compound 6) is a potent inhibitor of AChE/Hca with IC50 values of 22.21, 60.79 and 66.64 nM for AChE, Hca Ⅰ and Hca Ⅱ. AChE/hCA I/II-IN-1 can be used for the rsearch for glaucoma, Alzheimer's disease, diabetes[1].
SB-215505 is a potent and subtype-selective 5-HT2B receptor antagonist with pKi values of 8.3, 6.77, 7.66 for 5-HT2B, 5-HT2A, 5-HT2C, respectively[1]. SB-215505 increases wakefulness and motor activity in rats[2].
(Gln22)-Amyloid β-Protein (1-42) is a Dutch mutation (E22Q) form of β-Amyloid (1-42) (HY-P1363). (Gln22)-Amyloid β-Protein (1-42) exhibits enhanced fibrillogenic and pathogenic properties[1].
Haloperidol decanoate shows antipsychotic activity. Haloperidol decanoate can be used in schizophrenia and schizoaffective disorder research[1].
7BIO (7-Bromoindirubin-3-Oxime) is the derivate of indirubin. 7BIO (7-Bromoindirubin-3-Oxime) has inhibitory effects against cyclin-dependent kinase-5 (CDK5) and glycogen synthase kinase-3β (GSK3β). 7BIO (7-Bromoindirubin-3-Oxime) inhibits Aβ oligomer-induced neuroinflammation, synaptic impairments, tau hyper-phosphorylation, activation of astrocytes and microglia, and attenuates Aβ oligomer-induced cognitive impairments in mice[1].
Neuropeptide AF (cattle), an amidated octadecapeptide, is RFamide neuropeptide. Neuropeptide AF (cattle) acts as a ligand of Mas-related gene receptor A4 (MrgprA4) (Mas-related G-protein-coupled Receptor (MRGPR)) (EC50 of ~60 nM) and MrgprC11 (EC50 of ~300 nM). Neuropeptide AF (cattle) also activate to the G protein-coupled receptors NPFF1 (Neuropeptide Y Receptor) (EC50 of ~25-325 nM) and NPFF2 (EC50 of ~1-5 nM). Neuropeptide AF (cattle) shows anti-opiate and related pain modulation effects[1][2].
Corynanthine is a selective α1-adrenergic receptor antagonist. Corynanthine can significantly lower intraocular pressure in rabbits[1].
L-threo-3-Hydroxyaspartic acid is a potent EAAT inhibitor with Kis of 11, 19 and 14 μM for EAAT1, EAAT2 and EAAT3, respectively in HEK293 cell lines[1].
Adenosine 5'-monophosphate monohydrate is an adenosine A1 receptor agonist.
1-BCP is a centrally active drug that modulates AMPA receptor gated currents. 1-BCP is a memory-enhancing agent[1][2].
Neoline, the active ingredient of processed aconite root (PA), alleviated oxaliplatin-induced peripheral neuropathy in mice. Neoline can be used as a marker compound to determine the quality of the PA products for the treatment of neuropathic pain[1].
Ginsenoside Re is an extract from Panax notoginseng. Ginsenoside Re decreases the β-amyloid protein (Aβ). Ginsenoside Re plays a role in antiinflammation through inhibition of JNK and NF-κB.
Dantrolene-13C3 is the 13C3 labeled Dantrolene. Dantrolene (F368), a muscle relaxant, non-competitively inhibits human erythrocyte glutathione reductase. Ki and IC50 values are 111.6 μM and 52.3 μM, respectively. Dantrolene is a ryanodine receptor antagonist and Ca2+ signaling stabilizer. Dantrolene can be used for the research of muscle spasticity, malignant hyperthermia, Huntington's disease and other neuroleptic malignant syndrome.
PDE2/PDE10-IN-1 is a phosphodiesterase 2 (PDE2) and PDE10 inhibitor with IC50s of 29 and 480 nM, respectively.
Verosudil (AR-12286) is a potent, selective Rho-kinase (ROCK) inhibitor with Kis of 2 and 2 nM for ROCK1 and ROCK2, respectively. AR-12286 lowers intraocular pressure (IOP) primarily by increasing aqueous humour outflow through the trabecular meshwork[1][2].
Foliglurax monohydrochloride (PXT002331 monohydrochloride) is a highly selective and potent, brain-penetrant mGluR4 positive allosteric modulator (PAM) with an EC50 of 79±19 nM[1]. Antiparkinsonian effect[1].
Nefopam D3 hydrochloride is the deuterium labeled Nefopam hydrochloride. Nefopam hydrochloride (Fenazoxine hydrochloride) is a centrally-acting but non-opioid analgesic drug, for the relief of moderate to severe pain. Nefopam hydrochloride targets β-catenin protein level in mesenchymal cells in-vitro and in-vivo[1][2].
Pramiracetam is a nootropic drug derived from piracetam, and is more potent. Pramiracetam reportedly improved cognitive deficits associated with traumatic brain injuries. IC50 Value: Target: in vitro: Pramiracetam sulfate did not exhibit any affinity in vitro for dopaminergic , GABAergic, serotoninergic, adrenergic, muscarinic, adenosine (IC50 > 10 uM), and benzodiazepine receptors (IC50 > 1 uM) binding sites [1].in vivo: In a double-blind, randomized design, two groups of six subjects each received alternating placebo and single 400, 800, 1,200, and 1,600 mg oral doses of pramiracetam after an overnight fast. Mean (+/- SD) peak plasma concentrations of the four dose groups (2.71 +/- 0.54, 5.40 +/- 1.34, 6.13 +/- 0.71, 8.98 +/- 0.71 micrograms/mL) were attained between two to three hours following drug administration [2]. Two doses of pramiracetam (7.5 mg/kg and 15 mg/kg) were administered daily prior to testing for 7 weeks in a 16-arm radial maze in which nine arms were baited with food [3].
PLX5622 is a highly selective brain penetrant and oral active CSF1R inhibitor, for extended and specific microglial elimination, preceding and during pathology development. PLX5622 demonstrates desirable PK properties in varies animals[1].
GK187 is a potent and selective Group VIA calcium-independent phospholipase A2 (GVIA iPLA2) inhibitor with an XI(50) value of 0.0001. GK187 can be used for researching various neurological disorders[1]. [The XI(50) is the mole fraction of the inhibitor in the total substrate interface required to inhibit the enzyme by 50%.]
Pentoxyverine (Carbetapentane) is a sigma-1 receptor agonist, with a Ki of 75 nM on guinea-pig brain membranes. Pentoxyverine is a centrally-acting cough suppressant with antimuscarinic and anticonvulsant properties. Pentoxyverine can be used for inhibiting bronchial interceptor, weakening of cough reflex, bronchial smooth muscle relaxation and reduction of airway resistance[1][2][3][4].
Huperzine A, an active Lycopodium alkaloid extracted from traditional Chinese herb, is a potent, selective and reversible acetylcholinesterase (AChE) inhibitor and has been widely used in China for the treatment of Alzheimer's disease (AD). IC50 value:Target: AChEHuperzine A exhibited protective effects against d-gal-induced hepatotoxicity and inflamm-aging by inhibiting AChE activity and via the activation of the cholinergic anti-inflammatory pathway. The huperzine A mechanism might be involved in the inhibition of DAMPs-mediated NF-κB nuclear localization and activation. Huperzine A is a potential therapeutic agent for Alzheimer's disease.
Norharmane (Norharman), isolated from coffee, is a potent and selective monoamine oxidase A (MAO-A) inhibitor with a Ki of 3.34 μM[1].
Otenzepad (AF-DX 116) is a selective and competitive M2 muscarinic acetylcholine receptor antagonist, with IC50 values of 640 nM and 386 nM for rabbit peripheral lung and rat heart, respectively[1].
Harmine is a natural dual-specificity tyrosine phosphorylation-regulated kinase ((DYRK)) inhibitor with anticancer and anti-inflammatory activities.
Z-Phe-Ala-diazomethylketone binds directly to Aβ42 monomers and small oligomers. Z-Phe-Ala-diazomethylketone inhibits the formation of Aβ42 dodecamers and inhibits Aβ42 fibril formation in the solution. Z-Phe-Ala-diazomethylketone has the potential for neurodegenerative disorders research[1].
Dopamine HCl is a catecholamine neurotransmitter present in a wide variety of animals,And a dopamine D1-5 receptors agonist.Target: Dopamine ReceptorDopamine (or 3,4-dihydroxyphenethylamine) is a neuroendocrine transmitter in the catecholamine and phenethylamine families that plays a number of important roles in the brain and bodies of humans. Several important diseases of the nervous system are associated with dysfunctions of the dopamine system. Outside the nervous system, dopamine functions in several parts of the body as a local chemical messenger. In the blood vessels, it inhibits norepinephrine release and acts as a vasodilator; in the kidneys, it increases sodium excretion and urine output; in the pancreas, it reduces insulin production; in the digestive system, it reduces gastrointestinal motility and protects intestinal mucosa; and in the immune system, it reduces the activity of lymphocytes. A variety of important drugs work by altering the way the body makes or uses dopamine. Dopamine itself is available for intravenous injection: although it cannot reach the brain from the bloodstream, its peripheral effects make it useful in the treatment of heart failure or shock, especially in newborn babies. L-DOPA, the metabolic precursor of dopamine, does reach the brain and is the most widely used treatment for Parkinson's disease. From Wikipedia.