γ-Secretase modulator 13 (compound 4) is a gamma-secretase modulator (GSMs) that inhibits the production of the aggregated amyloid β-peptide Aβ42 with an IC50 value of 163 nM. γ-Secretase modulator 13 can be used in the study of Alzheimer's disease[1].
Pirenzepine dihydrochloride (LS519) is a selective M1 muscarinic receptor antagonist.
Autocamtide-2-related inhibitory peptide is a highly specific and potent inhibitor of CaMKII with an IC50 of 40 nM.
Detomidine carboxylic acid is the major urinary metabolite of Detomidine. Detomidine is a synthetic α2-adrenergic agonist and an animal analgesic sedative. Detomidine also has cardiac and respiratory effects and an antidiuretic action[1][2].
TRPV2-selective blocker 1 (compound IV2-1) is a selective TRPV2 channel blocker with an IC50 of 6.3 μM. TRPV2-selective blocker 1 does not affect TRPV1, TRPV3 or TRPV4 channels. TRPV2-selective blocker 1 also inhibits TRPV2-mediated Ca2+ influx in macrophages, and inhibits macrophage phagocytosis[1].
AZD 9272 is a brain penetrant mGluR5 antagonist.
(E)-Guanabenz ((E)-Wy-8678) is an orally active central α2-adrenoceptor agonist. (E)-Guanabenz has antihypertensive activity, acts via stimulating central α2-adrenoceptors, and reducing net sympathetic outflow into the periphery. (E)-Guanabenz also directly binds to and inhibits GADD34, and has neuroprotective activity. (E)-Guanabenz can be used for researching hypertension and Parkinson disease[1][2].
Naloxone fluorescein acetate is the fluorescent-derivative of Naloxone. Naloxone is an opioid antagonist. Naloxone is the antidote for reversing the effects of an opioid overdose[1].
Zilganersen (ION373) is a glial fibrillary acidic protein (GFAP) inhibitor, an antisense oligonucleotide. Zilganersen can be used in Alexander disease (AxD) research[1][2].
Neuromedin S (human) is a neuropeptide that contains 33 amino acids.? Neuromedin S (human)has been identified in the brain as an endogenous ligand for the orphan G-protein coupled receptor (GPCR) FM-4/TGR-1 and acts on the neuromedin U (NMU) receptor 2 (NMUR2) in the regulation of body weight homeostasis[1].
β-Glycerol phosphate disodium salt pentahydrate is a Phosphatase and tensin homolog (PTEN) inhibitor extracted from patent US 20110002877 A1.
LAU159 is a functionally selective positive modulator of α1β3 GABA(A) receptor with an EC50 of 2.2 μM[1].
Aβ1-42 aggregation inhibitor 1 inhibits AChE (acetylcholinesterase) and BuChE (butyrylcholinesterase) with the IC 50 value of 2.64 μM and 1.29 μM, respectively. Aβ1-42 aggregation inhibitor 1 inhibits self-mediated Aβ1-42 aggregation by 51.29% at a concentration of 25 μM. Aβ1-42 aggregation inhibitor 1 has the potential for the research of anti-Alzheimer's disease [1] .
L-Tyrosine-d2-1 is the deuterium labeled L-Tyrosine. L-Tyrosine is a non-essential amino acid which can inhibit citrate synthase activity in the posterior cortex.
Scopolamine is a high affinity (nM) muscarinic antagonist. 5-HT3 receptor-responses are reversibly inhibited by Scopolamine with an IC50 of 2.09 μM.
Aducanumab (BIIB037), a human monoclonal antibody selective for aggregated forms of amyloid beta (Aβ). Aducanumab shows brain penetration, and can be used for Alzheimer's disease (AD) research[1].
Pareptide monohydrochloride is a melanotropin-inhibiting factor (MIF) metabolically stable analogue.
DSP-1053 is a potent Serotonin Transporter (SERT) (Ki=1.02 nM) inhibitor with partial 5-HT1A receptor (Ki=5.05 nM) agonistic activity.
Capuride is an orally active sedative agent. Capuride has anticonvulsant activity[1].
Dehydroaripiprazole (OPC-14857) hydrochloride is an active metabolite of Aripiprazole. Aripiprazole is an antipsychotic agent and is metabolized by CYP3A4 and CYP2D6 forming mainly Dehydroaripiprazole hydrochloride. Dehydroaripiprazole hydrochloride has with antipsychotic activity equivalent to Aripiprazole[1][2][3][4].
(+)-Medioresinol is a furofuran type lignan with antifungal, antibacterial and lesishmanicidal activities. (+)-Medioresinol leads to intracellular ROS accumulation and mitochondria-mediated apoptotic cell death in Candida albicans. (+)-Medioresinol can reduce the cardiovascular disease risk[1][2].
JNJ-31020028 is a selective brain penetrant antagonist of neuropeptide Y2 receptor with high affinity(pIC50=8.07, human; pIC50=8.22 rat); >100-fold selective versus human Y1/Y4/Y5 receptors.IC50 value: 8.07/8.22(human/rat pIC50) [1]Target: Y2 receptor antagonistin vitro: JNJ-31020028 was demonstrated to be an antagonist (pK(B) = 8.04 +/- 0.13) in functional assays [1].in vivo: JNJ-31020028 occupied Y(2) receptor binding sites (approximately 90% at 10 mg/kg) after subcutaneous administration in rats [1]. Neither systemic (0, 15, 30, and 40 mg/kg, subcutaneously [s.c.]) nor intracerebroventricular (0.0, 0.3, and 1.0 nmol/rat) administration of JNJ-31020028 affected alcohol-reinforced lever pressing or relapse to alcohol seeking behavior following stress exposure. JNJ-31020028 (15 mg/kg, s.c.) did reverse the anxiogenic effects of withdrawal from a single bolus dose of alcohol on the elevated plus-maze, confirming the anxiolytic-like properties of NPY Y2 antagonism [2]. Chronic administration of JNJ-31020028 induced a decrease in immobility time in the forced swim test in OBX while had no effect in control animals [3].
Maprotiline-d3 (hydrochloride) is deuterium labeled Maprotiline (hydrochloride).
Adenosine amine congener (ADAC) is a selective A1 adenosine receptor agonist, can ameliorate noise- and Cisplatin-induced cochlear injury. Adenosine amine congener also has neuroprotective effects[1][2].
Halopemide is a potent phospholipase D (PLD) inhibitor, with IC50s of 220 and 310 nM for human PLD1 and PLD2, respectively. Halopemid is a dopamine receptors antagonist, and acts a psychotropic agent[1][2].
NAN-190 hydrobromide is a serotonin receptor 5-HT antagonist. NAN-190 is a selective antagonist of 5-HT1A.Target: 5-HT in vitro: NAN-190 is a 5-HT1A antagonist. [3] NAN-190 is a selective antagonist of 5-HT1A. [1]in vivo: NAN-190 (0.5 mg/kg, ip), as a 5-HT1A receptor antagonist, is injected concomitantly with the effective dose of fluoxetine. NAN-190 (5-HT1A receptor antagonist) reverses the catalepsy-improving effect of fluoxetine in 6-OHDA lesioned rats. [2]
SIB-1757 is a highly selective and noncompetitive antagonist of mGlu5 receptor with an IC50 of 0.4 μM[1].
SB-431542 is a potent and selective inhibitor of ALK5 with an IC50 value of 94 nM, and is also an inhibitor of TGF-β Receptor.
BU224 hydrochloride is a selective and high affinity imidazoline I2 receptor ligand, with a Ki of 2.1 nM. BU224 hydrochloride is sometimes used as an I2 receptor antagonist. BU224 hydrochloride exerts neuroprotective effects, with anti-inflammatory and anti-apoptotic properties. BU224 hydrochloride improves memory in 5XFAD mice, enlarging dendritic spines and reducing Aβ-induced changes in NMDARs. BU224 hydrochloride can be used for Alzheimer's disease research[1][2][3].
AChE-IN-12 is a potent and blood-brain barrier (BBB) penetrant acetylcholinesterase (AChE) with IC50s of 0.41 μM and 1.88 μM for rat AChE and electric eel AChE. AChE-IN-12 is also a good antioxidant (ORAC = 3.3 eq), selective metal chelator and huMAO-B inhibitor (IC50 = 8.8 µM). AChE-IN-12 has remarkable inhibition of self- and Cu2+-induced Aβ1-42 aggregation, as well as exhibits a good neuroprotective effect. AChE-IN-12 can be used for researching Alzheimer’s disease[1].