Kukoamine B Mesylate is potentially for the treatment of sepsis. Kukoamines are a series of bioactive phytochemicals conjugated by a polyamine backbone and phenolic moieties. Treatment with KuB prior to H2O2 exposure effectively increased the cell viability, and restored the mitochondria membrane potential (MMP). Furthermore, KuB enhanced the antioxidant enzyme activities of superoxide dismutase (SOD), catalase (CAT), and glutathione peroxidase (GSH-Px) and decreased the malondialdehyde (MDA) content. Moreover, KuB minimized the ROS formation and inhibited mitochondria-apoptotic pathway, MAPKs (p-p38, p-JNK, p-ERK) pathways, but activated PI3K-AKT pathway.

Sinafloxacin Mesylate is a quinolone antibiotic potentially for the treatment of bacterial infections. There is a strong interaction between sinafloxacin and BSA. From thermodynamic coordination it can be judged that the binding force between sinafloxacin and BSA is mainly electro-static force. The effect of sinafloxacin on the conformation of BSA was analyzed by synchronous fluorescence spectrometry and three-dimensional fluorescence spectrometry. The emission maximum of tyrosine residues does not show a significant shift, while the small blue shift of tryptophan residues indicates that the hydrophobicity of microenvironment was increased. In addition, in the plasma, there are some metal ions, which can participate in many important vital actions and affect the reactions of the drugs with the serum albumins.

Forodesine is a transition-state analog inhibitor of purine nucleoside phosphorylase.

Olodanrigan, also known as EMA401, is a novel orally available and highly selective angiotensin II type 2 receptor (AT2R) antagonist.

AT2 Agonist C21 is the first potent and selective agonist of angiotensin AT2 receptors, preventing endothelial inflammation and leukocyte adhesion in vitro and in vivo. AT2 Agonist C21 prevents cognitive decline after permanent stroke in aged animals-A randomized double- blind pre-clinical study. AT2 Agonist C21 attenuates pulmonary inflammation in a model of acute lung injury. AT2 Agonist C21 attenuates the Progression of Lung Fibrosis and Pulmonary Hypertension in an Experimental Model of Bleomycin-Induced Lung Injury.

CAY10471, also known as TM30089, is a potent and selective long-lasting antagonist of CRTH2. Cat#527092 is a + rotation. isomer (note sure it is a R-isomer or S-isomer).

CGP12177A is a partial agonist of ?3-adrenoceptors and antagonist of ?1- and ?2-adrenoceptor.

NPPB is a voltage-dependent cystic fibrosis transmembrane conductance regulator (CFTR) channel blocker.

Isoxepac, also known as Olopatadine USP Related Compound C, is a non-steroidal anti-antiphlogistic agent and analgesic.

Nortropine Hydrochloride is a secondary metabolite of tropine derivative drugs, such as atropine and benztropine.

Quinocetone is an animal growth promoter; Antimicrobial agent.

Salbutamol Sulfate is a short-acting beta-2 adrenergic agonist.

Pentamidine is an antiprotozoal and antifungal agent, interacting directly with the pathogen genome by binding to AT-rich regions of duplex DNA and the minor groove of DNA, thereby interfering with DNA replication.

Ceftiofur Hydrochloride is a broad-spectrum, third-generation cephalosporin antibiotic, binding to and inactivating penicillin-binding proteins (PBPs) located on the inner membrane of the bacterial cell wall.

Rabeprazole is an inhibitor of H(+)-K(+)-exchanging atpase in gastric parietal cells.

X-alpha-Gal is a substrate for alpha-galactosidase, differentiating alpha-galactosidase-positive strains of yeast.

Nequinate is an anticoccidial agent, preventing coccidiosis and developing immunity against five different species of Eimeria.

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.