MOPS-Na is a novel stabilizer as buffer for the native structure of BSA against thermal denaturation.

5alpha-THDOC is a positive allosteric modulator of GABAA receptors.

ZD-9379 is a NMDA receptor antagonist potentially for the treatment of pain and stroke. ZD9379 is also a glycine site antagonist, ZD9379 which reduces number of spreading depressions and infarct size in rats with permanent middle cerebral artery occlusion. ZD9379 reduces number of spreading depressions and infarct size in rats with permanent middle cerebral artery occlusion.

INCB3284 is a potent, selective, and orally bioavailable hCCR2 Antagonist. INCB3284 exhibited an IC50 of 3.7 nM in antagonism of monocyte chemoattractant protein-1 binding to hCCR2, an IC50 of 4.7 nM in antagonism of chemotaxis activity, an IC50 of 84 μM in inhibition of the hERG potassium current, a free fraction of 58% in protein binding, high selectivity over other chemokine receptors and G-protein-coupled receptors, and acceptable oral bioavailability in rodents and primates. In human clinical trials, INCB3284 exhibited a pharmacokinetic profile suitable for once-a-day dosing (T 1/2 = 15 h).

Necrostatin-2, also known as Nec-2, is a necroptosis inhibitor.

PF-06767832 is a high quality M1 selective PAM (M1 PAM EC50 = 60 nM; M2-M5 PAM EC50 > 10 microM; CNS MPO = 4.9). PF-06767832 has well aligned physicochemical properties, good brain penetration and pharmacokinetic properties. Extensive safety profiling suggested that despite being devoid of mAChR M2/M3 subtype activity, compound 38 still carries gastrointestinal and cardiovascular side effects. These data provide strong evidence that M1 activation contributes to the cholinergic liabilities that were previously attributed to activation of the M2 and M3 receptors.

LAS101057 is a Potent, Selective, and Orally Efficacious A2B Adenosine Receptor Antagonist. (last updated: 6/30/2016). LAS101057 inhibits agonist-induced IL-6 production in human fibroblasts and is active in an ovalbumin (OVA)-sensitized mouse model after oral administration, reducing airway hyperresponsiveness to methacholine, Th2 cytokine production, and OVA-specific IgE levels.

ABT-046 is a potent, safe, and orally efficacious inhibitor of acyl-CoA:diacylglycerol acyltransferase 1. Oral administration of ABT-046 at doses ≥0.03 mg/kg significantly reduced postprandial triglycerides in mice following an oral lipid challenge. Further assessment in both acute and chronic safety pharmacology and toxicology studies demonstrated a clean profile up to high plasma levels.

27-Hydroxycholesterol, also known as 27-HC, is an endogenous oxysterol with multiple biological functions, including activity as a selective estrogen receptor modulator (SERM) (a mixed, tissue-specific agonist-antagonist of the estrogen receptor (ER)) and as an agonist of the liver X receptor (LXR). It is a metabolite of cholesterol that is produced by the enzyme CYP27A1. 27-Hydroxycholesterol suppresses lipid accumulation by down-regulating lipogenic and adipogenic gene expression in 3T3-L1 cells. 27-Hydroxycholesterol stimulates cell proliferation and resistance to docetaxel-induced apoptosis in prostate epithelial cells.

MDL-72274 HCl is selective and potent inhibitors of SSAO for treatment of Parkinson diseases. MDL-72974 is a potent (IC50 = 10(-9) M) inhibitor of both MAO-B and SSAO, with 190-fold lower affinity for MAO-A. In clinical studies, oral doses as low as 100 micrograms produced substantial inhibition of platelet MAO-B. One or 4 mg MDL-72274 HCl given daily for 28 days to 40 Parkinson's patients treated with L-dopa produced statistically significant reductions in the Unified Parkinson's Disease Rating Scale. MAO-B inhibitors, such as MDL 72974A and L-deprenyl, offer the potential of being neuroprotective in Parkinson's Disease and other neurogenerative disorders.

Procarbazine is an antineoplastic chemotherapy drug for the treatment of Hodgkin's lymphoma and certain brain cancers (such as glioblastoma multiforme). It is a member of a group of medicines called alkylating agents. The drug is metabolized and activated in the liver. It also inhibits MAO thus increasing the effects of sympathomimetics, TCAs, and tyramine. It gained FDA Approved in July 1969. It is on the World Health Organization's List of Essential Medicines, a list of the most important medication needed in a basic health system.

L-655708, also known as FG-8094, is a nootropic drug. L-655708 acts as a subtype-selective inverse agonist at the α5 subtype of the benzodiazepine binding site on the GABAA receptor. A radiolabelled form of L-655708 was used to map the distribution of the GABAA α5 subtype in the brain. L-655708 was indeed found to produce improved cognitive performance in animal studies, without producing the side effect of convulsions which is produced by non-selective inverse agonists like DMCM.

GYKI-23107 is an antiarrhythmic agent with local anaesthetic activity. GYKI-23107 was effective against chemically (aconitine and ouabain) induced arrhythmias after both parenteral and oral administration. GYKI-23107 and mexiletine produced similar elevation of the fibrillation threshold in anaesthetized cats. After oral pretreatment, GYKI-23107 showed protective effects against coronary ligation-induced arrhythmia in conscious rats. The circulatory side-effects of GYKI-23107 in anaesthetized and conscious dogs and cats were milder then those of mexiletine.

Zopolrestat is a aldose reductase inhibitor potentially for the treatment of diabetic nephropathy and diabetes.

Zoniporide: a potent and selective inhibitor of the human sodium-hydrogen exchanger isoform 1 (NHE-1). Zoniporide preserves left ventricular compliance during ventricular fibrillation and minimizes postresuscitation myocardial dysfunction through benefits on energy metabolism. Zoniporide produces clinical, electrophysiologic, and microscopic evidence of peripheral sensory axonopathy and establishes the importance of careful preclinical evaluation of neurological function.

Zeranol is a non-steroidal estrogen agonist. It is a mycotoxin, derived from fungi in the Fusarium family, and may be found as a contaminant in fungus-infected crops. It is 3-4x more potent as an estrogen agonist than the related compound zearalenone. Zeranol increases cancer cell proliferation in already existing breast cancer. There are mixed results to whether zeranol has anticancer or carcinogenic properties in non cancer containing breast cells depending on dose. Overall evidence points to zeranol being a risk factor and promoter for cancer. However, dietary exposure from the use of zeranol-containing implants in cattle is insignificant.

Xylazine is an analogue of clonidine and an agonist at the α2 class of adrenergic receptor. It is used for sedation, anesthesia, muscle relaxation, and analgesia in animals such as horses, cattle and other non-human mammals. Veterinarians also use xylazine as an emetic, especially in cats.

Way 100135 is a serotonergic drug of the phenylpiperazine family which is used in scientific research. It acts as potent 5-HT1A receptor antagonist, and was originally believed to be highly selective, but further studies have demonstrated that it also acts as a partial agonist of the 5-HT1D receptor (pKi = 7.58; virtually the same affinity for 5-HT1A), and to a much lesser extent, of the 5-HT1B receptor (pKi = 5.82). These findings may have prompted the development of the related compound WAY-100,635, another purportedly selective and even more potent 5-HT1A antagonist, which was synthesized shortly thereafter.

Vibunazole is an antifungal agent

KUN79359, also known as PKC? inhibitor, is a potent and selective inhibitor of PKC? isozymes. KUN79359 has no formal name, and has CAS#257879-35-9. For the convenience of scientific communication, it is named as KUN79359. The name was generated based on Hodoodo chemical nomenclature.

Triflumuron is an insecticide belonging to the group of so-called insect growth regulators. It inhibits the synthesis of chitin by the insect larvae, causing the die. This operation is similar to that of, inter alia, flufenoxuron , lufenuron and novaluron ; triflumuron belongs to the same group of benzoylureas. It is a product of Bayer CropScience ; Alsystin brand. It is applied to apples, pears, peaches, nectarines and mushrooms, as well as in the storage of cereals.

Triadimenol is a flammable white to gray solid with phenolartigem odor which is practically insoluble in water. It decomposes when heated above 150 ° C. The compound is present in several isomeric front forms, the technical product to 78 to 88% of the diastereoisomer A is (RS + SR). The compound is stable to hydrolysis at pH values ??of 4, 7 and 9 and is subject to a small extent of photolysis. Triadimenol is a systemic fungicide with a broad spectrum. It inhibits the ergosterol - and gibberellin - biosynthesis , and thus the rate of cell division.

SKF1 is a suppressor of the ability of FK506 to inhibit cell growth in the presence of high levels of NaCl, inducing cell death in low salt conditions, interacting directly with yeast mitochodria.

Triadimefon is an azole fungicide.

TMI-1 is a novel orally active inhibitor of ADAM17 (TACE) and MMP, inducing tumor apoptosis in a breast cancer.

Tomelukast, also known as LY171883, is a leukotriene inhibitor. Tomelukast showed protective effects in traumatic shock. LY-171883 stimulates the activity of BK(Ca) channels in a manner unlikely to be linked to its blockade of leukotriene receptors or stimulation of peroxisome proliferator-activated receptors. The stimulatory effects on these channels may, at least in part, contribute to the underlying cellular mechanisms by which LY-171883 affects neuronal or neuroendocrine function.

MAFP is an irreversible inhibitor of Ca(2+)-independent phospholipase A2 (iPLA2).

Proxyfan Oxalate is a potent histamine H3 receptor ligand, acting as a protean agonist with activity ranges from full agonist to inverse agonist depending on system used. also displaying partial agonist effects on cAMP inhibition and MAPK activity, neutral antagonist activity on histamine release and partial inverse agonism of [3H]-arachidonic acid release.

Thiolactomycin is a novel reversible dual inhibitor of D-Aspartate oxidase (DDO) and D-amino acid oxidase (DAO).

Tebuconazole is a triazole fungicide used agriculturally to treat plant pathogenic fungi. Though the U.S. Food and Drug Administration considers this fungicide to be safe for humans, it may still pose a risk. It is listed as a possible carcinogen in the United States Environmental Protection Agency Office of Pesticide Programs carcinogen list with a rating of C (possible carcinogen). Its acute toxicity is moderate. According to the World Health Organization toxicity classification, it is listed as III, which means slightly hazardous.