(Rac)-WAY-161503 is a potent, selective, highly affinity 5-HT2C receptor agonist with a Ki of 4 nM and an EC50 of 12 nM. (Rac)-WAY-161503 displays higher affinity for 5-HT2C than 5-HT2A and 5-HT2B receptors. (Rac)-WAY-161503 has anti-obesity and antidepressant effects[1][2].
BGC20-1531 (PGN-1531, AP 1531) is a potent, selective prostanoid EP receptor EP antagonist, exhibits high affinity at recombinant human EP4 receptors expressed in cell lines (pKB=7.6) and native EP4 receptors in human cerebral and meningeal artery (pKB=7.6-7.8); shows no appreciable affinity at a wide range of other receptors (including other prostanoid receptors), channels, transporters and enzymes (pKi < 5); competitively antagonizes PGE(2)-induced vasodilatation of human middle cerebral (pK(B) 7.8) and meningeal (pK(B) 7.6) arteries in vitro, and PGE(2)-induced increase in canine carotid blood flow in vivo. Migraine Phase 2 Discontinued
Nefopam D3 (Fenazoxine D3) is a deuterium labeled Nefopam (Fenazoxine). Nefopam is a centrally-acting but non-opioid analgesic drug, and Nefopam targets β-catenin protein level in mesenchymal cells[1][2].
4-O-Methyldopamine hydrochloride is a catecholamine compound that has an inhibitory effect on dihydropteridine reductase[1].
Neostigmine methyl sulfate is a reversible inhibitor of acetylcholinesterase, can not cross the blood-brain barrier.
Schisandrin B(Wuweizisu-B) is a dibenzocyclooctadiene derivative isolated from Fructus Schisandrae, has been shown to produce antioxidant effect on rodent liver and heart.IC50 value:Target: in vitro: Schisandrin B exhibits anti-inflammatory activity through modulation of the redox-sensitive transcription factors Nrf2 and NF-κB. SB inhibited mitogen-induced proliferation and cytokine secretion by lymphocytes [1]. Sch B can protect neuronal cells against oxidative challenge, presumably by functioning as a hormetic agent to sustain cellular redox homeostasis and mitoenergetic capacity in neuronal cells [2]. Sch B exerted significant neuroprotective effects against microglial-mediated inflammatory injury in microglia-neuron co-cultures. Sch B significantly downregulated pro-inflammatory cytokines, including nitrite oxide (NO), tumor necrosis factor (TNF)-α, prostaglandin E(2) (PGE(2)), interleukin (IL)-1β and IL-6 [3]. Sch B could inhibit TGF-β induced EMT of 4T1 cells and of primary human breast cancer cells [4].in vivo: Similar anti-inflammatory effects of SB on lymphocyte proliferation and cytokine secretion were also observed in vivo [1]. Treatment with Sch B in CsA-treated mice significantly suppressed the elevation of blood urea nitrogen (BUN) and serum creatinine levels and attenuated the histopathological changes. Additionally, Sch B also decreased renal MDA levels and increased GSH levels in CsA-treated mice [5].
Fazamorexant (YZJ-1139) is a potent orexin receptor antagonist. Fazamorexant can be used for insomnia research[1][2].
DAO-IN-2 is a novel D-amino acid oxidase (DAO) inhibitor. DAO-IN-2 demonstrates moderate potency for DAO in vitro and ex vivo[1].
Molindone ((±)-Molindone), an indole derivative, is a potent dopamine D2 and D5 receptor antagonist. Molindone ((±)-Molindone) can be used for the research of schizophrenia and severe mental illness[1][2].
γ-Secretase modulator 10 is a novel γ-secretase modulator.
Galanin-Like Peptide (porcine) is a 60 amino acid neuropeptide that was first isolated from the porcine hypothalamus. Galanin-Like Peptide (porcine) has a high affinity for the GALR2 receptor (IC50 of 0.24 nM) and a lower affinity for the GALR1 receptor (IC50 of 4.3 nM)[1].
Dansyl-Tyr-Val-Gly TFA is a substrate of peptidylglycine monooxygenase (PHM). Peptidylglycine monooxygenase is an essential enzyme for the posttranslational amidation of neuroendocrine peptides[1].
FG-5893 is a 5-HT1A receptor agonist and a 5-HT2 receptor antagonist. FG-5893 has anxiolytic effect[1][2].
Rat orexin A is an important neuropeptide involved in the regulation of feeding, arousal, energy consuming, and reward seeking in the body.
(Rac)-ICI-118551 hydrochloride is a selective β2-adrenergic receptor antagonist. (Rac)-ICI-118551 hydrochloride can inhibit dendrite ramification of hippocampal neurons in a mouse model of Alzheimer's disease[1].
SB-258585 is a high affinity ligand for the 5-HT6 receptor. SB-258585 binds highly to a single receptor population in a human cell line that recombines 5-HT6 receptors. SB-258585 can be used to label recombinant and natural 5-HT6 receptor [1].
NSC363998 (free base) is an orally active compound. NSC363998 (free base) can suppress rCGG90 induced neurotoxicity. NSC363998 (free base) can be used for the research of neurodegenerative disorder such as Fragile X associated tremor/ataxia syndrome (FXTAS)[1].
PA-9 is a pituitary adenylate cyclase-activating polypeptide (PACAP) type I (PAC1) receptor antagonist. PA-9 dose dependently inhibits PACAP-induced cAMP elevation with an IC50 of 5.6 nM. PA-9 can be used for the research of neuropathic and/or inflammatory pain[1].
E 2012 is a potent γ-secretase modulator.IC50 value:Target: γ-secretaseIn the present study, 9 dogs were treated with a single dose of the γ-secretase modulator E2012, the γ-secretase inhibitor LY450139, or vehicle with a dosing interval of 1 week. The isoform Aβ(1-37) was significantly increased in a dose-dependent manner in response to treatment with E2012, while Aβ(1-39), Aβ(1-40) and A(1-42) decreased [1].E2012, a gamma secretase modulator without affecting Notch processing, aimed at Alzheimer's disease by reduction of amyloid β-42, induced cataract following repeated doses in the rat.E2012 inhibits 3β-hydroxysterol Δ24-reductase (DHCR24) at the final step in the cholesterol biosynthesis. In vivo lenticular concentration of E2012 after 13-week repeated dose with cataract was well above those where inhibition was observed in vitro.E2012 induces cataract in the rat by inhibiting DHCR24 at the final step of cholesterol synthesis with associated elevation in desmosterol within the lens, preceded by desmosterol changes that would serve as a predictive safety biomarker for lenticular opacity [2].
Trk-IN-3 is a potent pan-Trk inhibitor in cell-based assays with IC50s of 8.4 nM, 6.2 nM and 2.2 nM for TrkA, TrkB and TrkC, respectively[1]. Anti-hyperalgesic effect[1].
[D-Trp8] Somatostatin-14, a tetradecapeptide, is an analog of Somatostatin more potent than the native Somatostatin[1].
Albanol B is an arylbenzofuran derivative which can be isolated from mulberries. Albanol B exhibits anti-Alzheimer's disease, anti-bacterial and antioxidant activities. Albanol B inhibits cancer cells proliferation, down-regulates CDK1 expression. Albanol B also induces cell cycle arrest at G2/M and apoptosis. And Albanol B induces mitochondrial ROS production and increases the phosphorylation levels of AKT and ERK1/2[1].
Sodium Channel inhibitor 2 is a sodium channel blocker extracted from patent WO 2004011439 A2, compound 3c.
Dynamin IN-2 (compound 43), a Wiskostatin (HY-12534) analogue, is a potent dynamin inhibitor, with an IC50 of 1.0 μM for dynamin I GTPase. Dynamin IN-2 also blocks clathrin mediated endocytosis (CME), with an IC50 of 9.5 μM[1].
Aceprometazine (1664CB) is an orally active antipsychotic. Aceprometazine can be used in the study of psychiatric disorders, such as depression[1].
Desmethylcitalopram (DCIT) hydrochloride is the active metabolite of Citalopram (HY-121203). Desmethylcitalopram has antidepressant effects. Desmethylcitalopram also inhibits cytochrome P450-2D6, -2C19 with IC50s of 39.5 and 53.5 μM[1].
Picrotoxinin, a potent convulsant, is a chloride channel blocker. Picrotoxinin is a noncompetitive GABAA receptor antagonist, which negatively modulates the action of GABA on GABAA receptors[1].
Rimcazole (BW 234U) dihydrochloride is a carbazole derivative that acts in part as a sigma (σ) receptor antagonist. Rimcazole dihydrochloride also binds with moderate affinity to the dopamine transporter and inhibit dopamine uptake. Rimcazole dihydrochloride can attenuate cocaine-induced locomotor activity and sensitization. Rimcazole dihydrochloride also can be used for the research of cancer[1][2][3][4].
5-AAM-2-CP is a major metabolite of Acetamiprid. Acetamiprid is a neonicotinoid insecticide used worldwide and is a nAChR agonist[1][2].
Balanophonin is an anti-inflammatory and anti-cancer agent. Balanophonin inhibits microglial activation and neurodegeneration via inhibiting activated microglia-induced apoptosis[1].