kg-1

Farudodstat (ASLAN003) is an orally active and potent inhibitor of DHODH (Human Dihydroorotate Dehydrogenase) with antitumor activity, showing potential as a first-in-class candidate in AML [Acute Myeloid Leukemia].

FGFR1/DDR2 inhibitor 1 is an inhibitor of discoidin domain receptor 2 (DDR2) and fibroblast growth factor receptor 1 (FGFR1), with IC50 values of 31.1 nM, 108.4 nM, and 3.2 nM for FGFR1, KG-1, and DDR2, respectively.

SMS 121 is a novel CD36 inhibitor that impairs fatty acid uptake and cell viability in acute myeloid leukaemia (AML) cells.

ZX-29 is a potent and selective inhibitor of ALK with IC50 values of 2.1 nM, 1.3 nM, and 3.9 nM for ALK, ALK [L1196M], and ALK [G1202R] mutations, respectively. It also induces protective autophagy and exhibits antitumor effects.

BRD7389 is an inhibitor of RSK family kinase with IC50s of 1.5 μM, 2.4 μM, and 1.2 μM for RSK1, RSK2, and RSK3, respectively.

JH-VIII-157-02 is an inhibitor of ALK and inhibits echinoderm microtubule-associated protein-like 4-ALK (EML4-ALK) with IC50s of 2 nM for EML4-ALK G1202R, EML4-ALKwt, EML4-ALK C1156Y, EML4-ALK F1174L, and EML4-ALK F1174L.

GSK-690693 is a pan-Akt inhibitor targeting Akt1/2/3 with IC50 of 2 nM/13 nM/9 nM, also sensitive to the AGC kinase family: PKA, PrkX and PKC isozymes. Phase 1.

PKG1α activator 3, with an EC50(basal/partial) of 13/0.52 μM, inhibits the proliferation of smooth muscle cells and is utilized in cardiovascular disease research.

Piperidine-MO-1 is a dopamine receptor modulator, with an ED50 of 68 μmol/kg on increase of DOPAC in the rat striatum.

(S)-Vamicamide is a novel anticholinergic compound.Vamicamide increases spontaneous locomotor activity in mice at 32 mg/kg or higher (p.o.) and inhibits tonic convulsions in mice at 100 mg/kg.13483-86-1

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.

Thiacloprid is a neonicotinoid insecticide that acts as a selective agonist at insect nicotinic acetylcholine receptors (nAChRs) with IC50values of 2.7 and 860 nM forDrosophilanAChRs and M10 mouse fibroblast cells expressing α4β2 subunit-containing nAChRs, respectively.1It is active against aphids, whiteflies, various species of beetle, andLepidopteraspecies when used at concentrations ranging from 48 to 180 g AI/hectare.2It has anti-estrogenic activity in a yeast estrogen screen and is toxic to adult female houseflies and mice (LD50s = 0.03 and 28 mg/kg, respectively).1,3Formulations containing thiacloprid have been used in the control of insects in agriculture. 1.Tomizawa, M., and Casida, J.E.Selective toxicity of neonicotinoids attributable to specificity of insect and mammalian nicotinic receptorsAnnu. Rev. Entomol.48339-364(2003) 2.Elbert, A., Erdelen, C., Kuhnhold, J., et al.Thiacloprid, a novel neonicotinoid insecticide for foliar applicationProc. Brighton Crop. Prot. Conf. - Pests and Diseases121-26(2000) 3.Westlund, P., and Yargeau, V.Investigation of the presence and endocrine activities of pesticides found in wastewater effluent using yeast-based bioassaysSci. Total Environ.607-608744-751(2017)

Citric acid (Citro) is a weak organic tricarboxylic acid found in citrus fruits. Citric acid is a food additive and a natural preservative.

Beauveriolide III, a cyclodepsipeptide found in Beauveria fungi, inhibits lipid droplet formation (at 3-10 μM) and cholesterol synthesis (IC50=0.41 μM). This compound also suppresses acyl-coenzyme A:cholesterol acyltransferase (ACAT) activity (IC50=5.5 μM) and reduces atherosclerotic lesion size in Ldlr-/- and ApoE-/- mouse models (25-50 mg/kg).

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.

KR-32568 is a sodium/hydrogen exchanger 1 (NHE-1) inhibitor (IC50: 230 nM) with potent cardioprotective effects. At a concentration of 10 μM, it restored cardiac systolic function in an isolated ischemic rat heart model. Additionally, KR-32568 (0.3 mg/kg) reduced myocardial infarction size in a rat model of ischemia and reperfusion injury.

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.

AM679 is a potent and selective FLAP inhibitor with IC₅₀ values of 2.2 nM (FLAP binding), 0.6 nM (hLA), and 154 nM (hWB). AM679 displays improved CYP inhibition characteristics, no CYP3A4 time-dependent inhibition or induction, and strong in vivo leukotriene inhibition in rodent BAL models after oral administration.

Biperiden Hydrochloride (KL 373 Hydrochloride) is an antiparkinsonian agent, which is the selective central M1 cholinoreceptors blocker and it is used for the adjunctive treatment of all forms of Parkinson's disease (postencephalitic, idiopathic, and arte

Compound 27b, also known as hURAT1 inhibitor 1, is an isomarine-derived, orally active inhibitor that targets both hURAT1 and GLUT9 with IC50 values of 0.16 μM and 4.47 μM, respectively. This compound exhibits significant anti-hyperuricemia effects and has demonstrated potent uric acid-lowering activity in a hyperuricemia mouse model at a dose of 10 mg/kg. Importantly, Compound 27b displays no notable in vitro cytotoxicity or in vivo hepatotoxicity, and possesses favorable pharmacokinetic (PK) characteristics.

Betamethasone 17-Propionate is a compound used in the study of its effects on endotoxin-induced uveitis in rats, capable of inhibiting cellular infiltration into the aqueous humor when administered topically or systemically at certain doses. However, compared to some other compounds, its inhibitory effects are relatively weaker. When administered systemically, the dosage is 1mg/kg. Additionally, in in vitro interleukin-8 (IL-8) release assays, Betamethasone 17-Propionate's suppression of IL-8 release from rat peritoneal exudate cells is less effective than that of betamethasone. Moreover, the concurrent addition of betamethasone dipropionate with Betamethasone 17-Propionate reduces the suppressive effects of betamethasone on cell infiltration and IL-1β gene expression.

Kv7.2/Kv7.3 agonist 1 (Compound 16) is an orally effective agonist for the KV7.2/7.3 channels (KV7.2/7.3 channel/KCNQ2/3) with an EC50 of 1.03 μM. This compound demonstrates analgesic effects in mouse models of chronic constriction injury (CCI) and Streptozotocin-induced diabetic peripheral neuropathy (DPNP), with ED50 values of 12.02 mg/kg and 9.63 mg/kg, respectively.