mAChR antagonist 1 (compound 4a) is a mAChR antagonist with Ki values of 255 nM, 121 nM, 158 nM, and 255 nM for M1, M3, M4, and M5 subtype, respectively[1].
Pronethalol-d6 ((±)-Pronethalo-d6) is the deuterium labeled Pronethalol. Pronethalol ((±)-Pronethalo) is a non-selective β-adrenergic antagonist. Pronethalol is a potent inhibitor of Sox2 expression. Pronethalol protects against and to reverse Digitalis-induced ventricular arrhythmias and limits the cerebral arteriovenous malformation (AVMs)[1][2][3].
TC-G 24 (Compound 24) is a potent, selective glycogen synthase kinase-3β (GSK-3β) inhibitor with an IC50 of 17.1 nM. TC-G 24 can cross the BBB and can be used for studying many diseases such as type 2 diabetes mellitus, stroke, Alzheimer, and other related diseases[1].
Fasedienol is a neurochemical stimulator of the vomeronasal organ (VON). Fasedienol alleviates the symptoms of PMS and anxiety (extracted from patent WO1998014194A1)[1].
DASPEI is a fluorescent dye. DASPEI is a styryl dye that stains mitochondria of live cells. DASPEI has a large fluorescence Stokes shift and is taken up relatively slowly as a function of membrane potential[1].
Telotristat etiprate (LX1606 Hippurate) is a novel, orally-delivered inhibitor of tryptophan hydroxylase that reduces serotonin production.
Begacestat (GSI-953) is a selective thiophene sulfonamide inhibitor of amyloid precursor protein gamma-secretase (IC50Aβ40=15 nM) for the treatment of Alzheimer's disease[1].
Trifluoperazine N-glucuronide (UGT1A4) chloride is a metabolite of the antipsychotic agent trifluoperazine. Trifluoperazine N-glucuronide (UGT1A4) chloridecatalyzes the imipramine and trifluoperazine Nglucuronide formation[1].
Rauwolscine hydrochloride is a potent and specific α2 adrenergic receptor antagonist with a Ki of 12 nM.
PROTAC α-synuclein degrader 5 is a highly selective small-molecule degraders (PROTAC) of α-synuclein aggregates, with an DC50 of 7.51 μM and the highest degradation rate Dmax of 89%. PROTAC α-synuclein degrader 5 contains probe molecule sery308 and E3 ligase ligands. PROTAC α-synuclein degrader 5 can be used for neurological disease research[1].
Tanezumab (RN-624) is a humanized anti-NGF mAb with high affinity and specificity. Tanezumab blocks NGF binding to its receptors, p75 and TrkA, in the peripheral nervous system. Tanezumab can be used in studies of acute and chronic pain such as osteoarthritis, knee and neuralgia, as well as post-herpetic neuralgia[1][2].
VQW-765 (AQW-051) is a selective and orally active alpha-7 nicotinic acetylcholine receptor (α7-nAChR) agonist with a pKD value of 7.56 to recombinantly expressed human α7-nAChR. VQW-765 shows anxiolytic-like effect in vivo. VQW-765 can be used for the research of anxiety disorder and acute performance anxiety[1].
SR 16584 is a selective antagonist of α3β4 nAChR with an IC50 of 10.2 μM[1].
Gabazine is a selective and competitive antagonist of GABAA receptor, with an IC50 of ~0.2 μM for GABA receptor.
DR2313 is a potent, selective, competitive and brain-penetrant inhibitor of poly(ADP-ribose) polymerase (PARP), with IC50s of 0.20 μM and 0.24 μM for PARP-1 and PARP-2, respectively. DR2313 exhibits neuroprotective effects on ischemic injuries in vitro and in vivo[1][2].
PF-5006739 is a potent and selective inhibitor of CK1δ/ε with IC50s of 3.9 nM and 17.0 nM, respectively. PF-5006739 is a potential therapeutic agent for a range of psychiatric disorders with low nanomolar in vitro potency for CK1δ/ε and high kinome selectivity. PF-5006739 attenuats opioid drug-seeking behavior in a rodent operant reinstatement model in animals in a dose-dependent manner[1]. PF-5006739 improves glucose tolerance in both diet-induced obesity (DIO) and genetic (ob/ob) mice models of obesity[2].
AR-R17779 hydrochloride is a potent and selective full agonist of nAChR, with Kis of 92 and 16000 nM for α7 and α4β2 subtype, respectively. AR-R17779 hydrochloride can improve learning and memory in rats. AR-R17779 hydrochloride also has anxiolytic activity. AR-R17779 hydrochloride can reduce inflammation by activating antiinflammatory cholinergic (vagal) pathways[1][2][4].
Vitexin is a c-glycosylated flavone, and is found in various medicinal plants species such as Ficus deltoid and Spirodela polyrhiza. Vitexin has a wide range of pharmacological effects, including anti-oxidant, anti-cancer, anti-inflammatory, anti-hyperalgesic, and neuroprotective effects[1][2].
PW0464, a nanomolar potent complete G protein biased ligand, is a noncatechol D1R agonist, with an EC50 of 5.8 nM (Gs-cAMP)[1].
Akuammigine is an alkaloid that can be found in hook-bearing branch of Uncariarhynchophylla. Akuammigine is a is a very weak antagonist at pre- and postsynaptic α-adrenoceptor of the rat vas deferens[1][2].
Etoposide phosphate (BMY-40481) is a potent anti-cancer chemotherapy agent and a selective topoisomerase II inhibitor to prevent re-ligation of DNA strands. Etoposide phosphate is the phosphate ester prodrug of etoposide and is considered as active equivalent to Etoposide. Etoposide phosphate induces cell cycle arrest, apoptosis, and autophagy[1][2].
ICI 174864 is a highly selective, potent δ-receptor antagonist. ICI 174864 is equipotent with naloxone and can not reverse the effect of the μ-agonist [D-Ala2, MePhe4, Gly-Ol5]enkephalin or the κ-agonist tifluadom[1].
Bismuth Subsalicylate is the active ingredient in Pepto-Bismol and inhibits prostaglandin G/H Synthase 1/2.Target: OthersBismuth Subsalicylate reduces inflammation/irritation of stomach and intestinal lining through inhibition of prostaglandin G/H Synthase 1/2 [1]. Bismuth Subsalicylate is the active ingredient in Pepto-Bismol, an anti-diarrhea medication and antacid. In the gastrointestinal tract, Bismuth Subsalicylate is converted to salicylic acid and insoluble bismuth salts [2]. Bismuth subsalicylate treatment for 8 weeks is safe and well tolerated. This regimen appears to be efficacious for the treatment of microscopic colitis and is worthy of further study in a controlled trial [3].
VUF 8430 (dihydrobromide) is a potent and selective histamine H4 receptor agonist with a Ki of 31.6 nM and an EC50 of 50 nM[1].
CGP 39551 is a potent, orally active, competitive N-methyl-D-aspartate (NMDA) receptor antagonist with potent anticonvulsant activity[1]. CGP 39551 shows measurable inhibitory activity at both L-[3H]-glutamate (Ki=8.4 μM)[2].
Hypertrehalosemic neuropeptide (Nauphoeta cinerea) is a neuropeptide in the adipokinetic hormone/red pigment-concentrating hormone (AKH/RPCH) family, and can stimulate the synthesis of trehalose[1].
Calcineurin substrate is a peptide from the regulatory RII subunit of cAMP-dependent protein kinase. It can be used in the calcineurin activity assay.
Huwentoxin-IV is a potent and selective sodium channel blocker, inhibits neuronal Nav1.7, Nav1.2, Nav1.3 and Nav1.4 with IC50s of 26, 150, 338 and 400 nM, respectively. Huwentoxin-IV preferentially blocks peripheral nerve subtype Nav1.7 by binding neurotoxin receptor site 4. Huwentoxin-IV has analgesic effects on animal models of inflammatory and neuropathic pain[1][2].
PD-168077 maleate is a selective dopamine D4 receptor agonist, with a Ki of 9 nM.
β-Amyloid (1-15) is a fragment of β-Amyloid peptide. Beta-amyloid is a peptide that forms amyloid plaques in the brains of Alzheimer's disease (AD) patients.