humans

Deoxynivalenol (Vomitoxin) is a mycotoxin produced by Fusarium spp. of the single trichothecene family and is commonly found in contaminated food and feed.Deoxynivalenol crosses the intestinal mucosa via a cellular bypass at the tight junctions.Deoxynivalenol transporters are unaffected by inhibitors of P-glycoprotein (PgP) or multidrug resistance-associated protein (MRP). Deoxynivalenol commonly causes diarrhea, vomiting, and gastrointestinal inflammation in humans and animals.

Glyphosate (Atila) is an herbicide. It also is a possible carcinogen to humans.

Tauroursodeoxycholate (UR 906), also known as ursodoxicoltaurine, is a highly hydrophilic tertiary bile acid that is produced in humans at a low concentration. Tauroursodeoxycholate is the more hydrophilic form of ursodeoxycholic acid, which is the more abundant naturally produced bile acid in humans.Tauroursodeoxycholate is being investigated for use in several conditions such as Primary Biliary Cirrhosis (PBC), insulin resistance, amyloidosis, Cystic Fibrosis, Cholestasis, and Amyotrophic Lateral Sclerosis.

BMS-1 (PD-1/PD-L1 inhibitor 1) is an inhibitor of the PD1-PD-L1 protein-protein interaction. It also acts as an immunomodulator. Programmed death ligand 1 (PD-L1) is a protein in humans that is encoded by the CD274 gene and the upregulation of PD-L1 allows Ys to evade the host immune system. High tumor expression of PD-L1 was associated with increased tumor aggressiveness and a 4.5-fold increased risk of death.

Etomoxir is an irreversible inhibitor of carnitine palmitoyltransferase 1a (CPT-1a) (IC50=5-20 nM). Etomoxir inhibits fatty acid oxidation by inhibiting CPT-1a, inhibits palmitate oxidation, has an inhibitory effect on adenine nucleotide translocase, and can inhibit macrophage polarization by disrupting CoA homeostasis.

C-021 dihydrochloride is a potent CCR4 antagonist that effectively inhibits functional chemotaxis in humans and mice, with IC50 values of 140 nM and 39 nM, respectively.

CYP17-IN-1 is an effective oral inhibitor of CYP17 that can inhibit CYP17 in rats and humans with IC50 of 15.8 and 20.1 nM.

GW274150 is an orally active, selective and potent dual inhibitor of NADPH-dependent human nitric oxide synthase (iNOS) (Kd=40 nM) and rat inducible nitric oxide synthase (iNOS).GW274150 has a low activity against endothelial nitric oxide synthase (eNOS) and neuronal nitric oxide synthase (nNOS) in humans and rats. GW274150 showed protective effects in an inflammatory model of acute lung injury.

AZD8329 is a selective and potent 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor that inhibits 11β-HSD2, 17β-HSD1, 17β-HSD3, and can be used for the study of allergic reactions in humans.

MRS 1754 is a selective antagonist radioligand for the A2B adenosine receptor, exhibiting very low affinity for A1 and A3 receptors in both humans and rats.

C 021 dihydrochloride is a potent CCR4 antagonist. C-021 (4-Quinazolinamine, 2-[1,4'-bipiperidin]-1'-yl-N-cycloheptyl-6,7-dimethoxy-) dihydrochloride potently inhibits functional chemotaxis in humans and mice with IC50s of 140 nM and 39 nM, respectively. It effectively prevents human CCL22-derived [35S]GTPγS from binding to the receptor (IC50: 18 nM).

(Z)-FeCP-oxindole is a selective inhibitor of VEGFR2 with an IC50 of 200 nM for humans and demonstrates anticancer activity.

Cosalane (NSC 658586) is an HIV replication inhibitor, an inhibitor of chemokine receptor 7 (CCR7) signalling in humans and mice, with antiviral activity that blocks the binding of CCR7 to its natural ligands, CCL19 and CCL21.

GSK233705 (Darotropium bromide) is a muscarinic receptor antagonist used in conjunction with the prevention and treatment of chronic obstructive pulmonary disease (COPD) and asthma in humans.

11β-HSd1-in-11 is a potent and competitive inhibitor of 11-β-hydroxysteroid dehydrogenase 1 (11β-HSD1) IN rats and humans with IC50 values of 0.34 μM and 0.13 μM, respectively. 11β-Hsvd1-in-11 is a compound used as a chemical compound. 11β-HSD1-IN-11 is a hormone involved in regulating various physiological processes, such as metabolism, inflammation, and stress responses. 11β-Hd1-in-11 is a potential compound for the treatment of metabolic disorders, obesity, and certain inflammatory conditions.

Flubendazole (Flumoxane) is available OTC in Europe that is an anthelmintic using to treat worm infection in humans.

Uric acid is an important antioxidant that scavenges oxygen radicals and reactive oxygen species (such as singlet oxygen and peroxynitrite), inhibits lipid peroxidation, helps maintain stable blood pressure, and is the final product of purine metabolism. It is commonly used to induce hypertension models.

Propoxur (Propoxure) is an insecticide used to control cockroaches, flies, mosquitoes, and lawn and turf insects. Acute (short-term) exposure of humans to propoxur by ingestion leads to cholinesterase inhibition of red blood cells, with mild cholinergic symptoms including blurred vision, nausea, vomiting, sweating, and tachycardia; however, the effects are transient. Chronic (long-term) inhalation exposure has resulted in depressed cholinesterase levels, headaches, vomiting, and nausea in humans. Chronic ingestion studies in animals have reported depressed cholinesterase levels, depressed body weight, effects to the liver and bladder, and a slight increase in neuropathy. No information is available on the reproductive, developmental, or carcinogenic effects of propoxur in humans. Mixed results are available from cancer studies of propoxur in animals. EPA has not classified propoxur for carcinogenicity.

Estrone (Aquacrine) is an aromatized C18 steroid with a 3-hydroxyl group and a 17-ketone, a major mammalian estrogen. It is converted from ANDROSTENEDIONE directly, or from TESTOSTERONE via ESTRADIOL. In humans, it is produced primarily by the cyclic ovaries, PLACENTA, and the ADIPOSE TISSUE of men and postmenopausal women.

(S)-3-Hydroxybutanoic acid (L-(+)-3-Hydroxybutyric acid) is a normal human metabolite that has been found elevated in geriatric patients remitting from depression. (S)-3-Hydroxybutanoic acid is synthesized in the liver from acetyl-CoA in humans, and can be used as an energy source by the brain when blood glucose is low.

Mepivacaine (Carbocaine) is an amide compound for local anaesthesia that causes transient loss of self-consciousness in humans or animals. mepivacaine acts by binding to specific voltage-gated sodium channels in nerve cell membranes, inhibiting sodium inward flow and membrane depolarisation. mepivacaine is indicated for nerve blocks and epidurals.

Ascaridole (NSC-406266) acts as an anthelmintic compound that repels parasitic helminths (worms) in humans and plants and has weak antimalarial activity.

Pitavastatin calcium (NK-104) is a potent inhibitor of HMG-CoA reductase (Ki: 1.7 nM). It lowers both total cholesterol and low-density lipoprotein cholesterol in animals and humans. Metabolism of pitavastatin by the cytochrome P450 system is minimal, reducing the risk of drug-drug interactions.

Emodin (Frangula emodin) is an 11β-HSD1 inhibitor with a selective IC50 of 186 and 86 nM against 11β-HSD1 in humans and mice, respectively. Emodin has antiviral, anti-inflammatory, and anti-cancer effects. Emodin can improve metabolic disorders in diet-induced obese mice.