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KG5 is a dual allosteric inhibitor of PDGFRβ and B-Raf with a Kd of 520 nM and 300 nM for PDGFRβ and PDGFRα. KG5 inhibits FLT3, KIT, and c-Raf with anticancer and antiangiogenic activities.

KG-548 is a dual inhibitor of ARNT/TACC3 and HIF-1α, binding to the β-fold surface involved in HIF-2 dimerization and coactivator recruitment, inhibiting lactate production and useful in cancer research.

KG-501 (Naphthol AS-E phosphate) is a cAMP response element-binding protein (CREB) inhibitor(IC50 : 6.89 μM).

Litoxetine is a selective 5-HT uptake inhibitor and is a 5-HT3 receptor antagonist. Litoxetine acts as an antidepressant and has shown antiemetic properties in ferrets. Litoxetine (1 and 10 mg/kg i.v.) dose-dependently reduced the number of regurgitations and vomiting and delayed the onset of vomiting. Litoxetine has an affinity for brain 5HT3 receptors (Ki = 85 nM).

L-Allylglycine is an amino acid derivative that reduces glutamate decarboxylase (GAD) activity by 60% when administered at a dose of 39.8 μmol/g per hour ex vivo in mouse brain preparations. L-Allylglycine (1.2 mmol/kg, i.p.) induces convulsions and decreases GABA concentration throughout the cerebellum, pons, medulla, striatum, cortex, and hippocampus in mice. Chronic administration (3.2 μg/0.5 μl per hour for 13 days) of L-allylglycine in rats increases locomotor activity in an open field test and impairs attention in the 5-choice serial reaction time task (5CSRTT). In vitro, L-allylglycine inhibits GAD only when used at high concentrations (1-80 mM). The more potent in vivo activity can be attributed to metabolic conversion of L-allylglycine to 2-keto-4-pentanoic acid, a more potent convulsant and GAD inhibitor.

D-α-Hydroxyglutaric acid disodium [Disodium (R)-2-Hydroxyglutarate] is a competitive inhibitor of α-ketoglutarate-dependent dioxygenases with a Ki of 0.628 mM.

COR659 is a GABAB positive allosteric modulator (PAM) . COR659 suppresses alcohol and chocolate self-administration in rats[1]. COR659 apparently exerts its effects via a composite mechanism, including positive allosteric modulation of the GABAB receptor and an action at the cannabinoid CB1 receptor[3]. COR659 (0, 2.5, 5 and 10 mg/kg) treatment is completely ineffective on lever-responding (FR10) for regular food pellets in food-deprived Wistar rats[1].COR659 is able to suppress lever-responding for a sucrose solution in sP rats and a chocolate solution in Wistar rats[2]. Animal Model: Male sP and Wistar rats[1]. [1]. Paola Maccioni, et al. Suppressing effect of COR659 on alcohol, sucrose, and chocolate self-administration in rats: involvement of the GABA B and cannabinoid CB 1 receptors. Psychopharmacology (Berl). 2017 Sep;234(17):2525-2543. [2]. Francesca Ferlenghi, et al. The GABA B receptor positive allosteric modulator COR659: In vitro metabolism, in vivo pharmacokinetics in rats, synthesis and pharmacological characterization of metabolically protected derivatives. Eur J Pharm Sci. 2020 Dec 1;155:105544. [3]. Paola Maccioni, et al. Anti-addictive properties of COR659 - Additional pharmacological evidence and comparison with a series of novel analogues. Alcohol. 2019 Mar;75:55-66.

Unifiram is a nootropic agent.1It increases acetylcholine (ACh) release in the rat cerebral cortexin vivoand induces a long-lasting increase in the amplitude of field excitatory postsynaptic potentials (fEPSPs) in the rat hippocampal CA1 region (EC50= 27 nM). It does not bind to serotonin (5-HT), dopamine, muscarinic, nicotinic, adrenergic, glutamate, histamine, opioid, or GABA receptors at 1 μM. Unifiram (0.1 mg/kg) improves memory in non-memory-impaired rats in a social learning test.2It also prevents memory deficits induced by the anticholinergic agent scopolamine, nicotinic receptor antagonist mecamylamine, GABABreceptor agonist baclofen, or α2-adrenergic receptor agonist clonidine in the passive avoidance test in mice when administered at a dose of 0.01 mg/kg and prevents memory deficits induced by the AMPA/kainate glutamate receptor antagonist NBQX at 0.1 mg/kg.1 1.Romanelli, M.N., Galeotti, N., Ghelardini, C., et al.Pharmacological characterization of DM232 (unifiram) and DM235 (sunifiram), new potent cognition enhancersCNS Drug Rev.12(1)39-52(2006) 2.Ghelardini, C., Galeotti, N., Gualtieri, F., et al.The novel nootropic compound DM232 (unifiram) ameliorates memory impairment in mice and ratsDrug Develop. Res.56(1)23-32(2002)

4-Deoxypyridoxine (4-DPD) is a vitamin B6 antimetabolite with diverse biological activities. It inhibits transport of pyridoxine , pyridoxal, and pyridoxamine in and reduces growth of S. carlsbergensis cells. 4-DPD inhibits sphingosine-1-phosphate (S1P) lyase and reduces cyclic stretch-induced apoptosis in alveolar epithelial MLE-12 cells. 4-DPD (5 mg, i.p.) reduces lysyl oxidase activity by 26% and reduces collagen and elastin crosslinking, resulting in limb abnormalities in chick embryos. It decreases latency to first seizure in mice (ED50 = 1 mmol/kg) and increases the occurrence and duration of myoclonic responses in baboons with photosensitive epilepsy. 4-DPD reduces TNF-α and IL-6 production in mice infected with T. spiralis.

PAK4-IN-5 (Compound 12i) is a potent inhibitor of PAK4 (IC50: PAK4 at 7.68 nM, PAK1 at 1872.01 nM) that forms stable interactions with the PAK4 enzyme. This compound effectively inhibits the proliferation and migration potential of MDA-MB-231 cells by hindering the phosphorylation of PAK4 and LIMK1. Additionally, PAK4-IN-5 arrests the cell cycle in the G0/G1 phase, induces apoptosis, and prompts the production of reactive oxygen species. The LD50 in mice is greater than 500 mg/kg (oral).

O-Desmethylcarvedilol (Desmethylcarvedilol) is an active metabolite of Carvedilol, a non-selective β-adrenergic receptor (β-AR) antagonist. This compound inhibits store overload-induced calcium release in HEK293 cells expressing the RyR2 R4496C mutation (IC50= 7.62 µM). Additionally, O-Desmethylcarvedilol slows the increase in heart rate and prevents diastolic pressure reduction induced by Isoproterenol in conscious rabbits (ED50s = 32 and 5 µg/kg).

4-Bromo-2,5-DMMA (Compound 2) demonstrates affinity for the 5-HT2 binding site and has an ED50 of 0.82 mg/kg in rat discrimination experiments.

Octachlorodibenzo-p-dioxin (OCDD) is an environmental contaminant with no acute toxicity when administered. In rats, the systemic elimination half-life of Octachlorodibenzo-p-dioxin (50 μg/kg intravenously or 50-5000 μg/kg orally) is 3-5 months. It can accumulate and concentrate in the liver and adipose tissue after low-dose, repeated exposure. Repeated dosing of Octachlorodibenzo-p-dioxin leads to increased activity of 7-ethoxyresorufin-O-deethylase (7-EROD) and elevated total cytochrome P-450 levels.

MJ210 is an orally active and blood-brain barrier-permeable modulator of the NF-κB and MAPK pathways, exhibiting neuroprotective properties. In vitro, 5 μM MJ210 can increase the survival rate of rotenone-treated SH-SY5Y cells to 81.9% and reduce levels of ROS. In vivo, 5 mg/kg MJ210 improves motor dysfunction in rat models of Parkinson's disease. MJ210 is useful for research in neurological disorders, including Parkinson's disease.

5-Hydroxypropafenone, an active metabolite of propafenone, inhibits transient outward potassium current (Ito) in isolated human atrial myocytes with an IC50 of 1.5 µM. In vivo, it increases the atrial effective refractory period in dogs at doses of 0.5, 1, and 2 mg/kg.

EGFRkinase inhibitor 5 (Compound 4c) is an orally active epidermal growth factor receptor (EGFR) kinase inhibitor with an IC50 of 18.35 μM. It induces apoptosis and exhibits anticancer and anti-inflammatory properties while maintaining low toxicity (LD50 range of 500-2000 mg/kg).

FXIIa-IN-5 (Compound 4J) is an orally effective selective inhibitor of factor XIIa (FXIIa), with an IC50 of 21 nM. It inhibits the intrinsic coagulation pathway and demonstrates anti-inflammatory and antithrombotic activities in a Carrageenan-induced thrombosis model in mice. FXIIa-IN-5 exhibits moderate pharmacokinetic properties and mild toxicity at a dosage of 100 mg/kg.

WY-50295 is an orally active and selective 5-lipoxygenase inhibitor. In rat whole blood leukocytes, WY-50295 inhibits LTB4 formation with an IC50 of 40 μM and an oral ED50 of 18 mg/kg. WY-50295 is applicable for research into asthma and other leukotriene-dependent conditions.

Choline is a vital nutrient essential for maintaining liver, neurological, hematological, and skeletal muscle balance. It serves as a precursor in the biosynthesis of membrane phospholipids, like phosphatidylcholine, which aid in cell signaling and membrane transport, and is also a precursor to the neurotransmitter acetylcholine. Choline is crucial for hepatic lipid transport. In animal studies, perinatal administration of choline (18.8 mg/kg) has been shown to enhance cognitive function impaired by prenatal alcohol exposure in rats. Additionally, choline (13 mg/animal per day) improves motor coordination and addresses behavioral issues in a mouse model of Rett syndrome, and mitigates recognition memory deficits caused by early-life iron deficiency in rats when provided in drinking water at 5 ppm. Low choline intake is linked to muscle wasting, and dietary choline (1,000 mg/kg) boosts leg and breast muscle protein content in broiler chickens.

5β-Cholanic acid-3,7-dione is a synthetic bile acid that, when administered at 5 mg/kg to rabbits, reduces both bile volume and the concentrations of cholic acid and cholesterol in the bile.

DL-alpha-Hydroxyglutaric acid disodium salt is an alpha-ketoglutarate (α-KG) antagonist that inhibits a variety of α-KG-dependent dioxygenases.

CS 2100 (1-[[4-Ethyl-5-[5-(4-phenoxyphenyl)-1,2,4-oxadiazol-3-yl]-2-thienyl]methyl]-3-azetidinecarboxylic acid) is an S1P1 agonist.

SUN-C5174 is a sleective 5-HT2 antagonist (pA2=8.98+/-0.06). SUN C5174 showed a marked inhibitory effect on the platelet aggregation induced by serotonin in combination with collagen and adenosine diphosphate (ADP) in canine or human platelet-rich plasma

SST-02 is a potent cationic lipid for siRNA-Lipid Nanoparticles. SST-02 possesses a simple chemical structure and is synthesized just in one step. SST-02 showed an ID50 of 0.02 mg/kg in the factor VII (FVII) model. Rats administered with 3 mg/kg of SST-02