equine

β-Endorphin, equine (TFA) is an endogenous opioid peptide, which binds at high affinity to both μ/δ opioid receptors.

Endorphin Beta is A substance produced in the brain, especially in the pituitary gland, Endorphin Beta blocks the sensation of pain. Endorphin Beta is produced in response to pain, exercise, and other forms of stress. Endorphin Beta belongs to a group of

EIDD-1931 (Beta-d-N4-hydroxycytidine) is a ribonucleoside analog with antiviral activity that inhibits the replication of severe acute respiratory syndrome coronavirus [SARS-CoV] in Vero 76 cells, Middle East respiratory syndrome coronavirus [MERS-CoV] in Calu-3 2B4 cells, and SARS-CoV-2 in Vero cells (IC50s = 0.1, 0.15, and 0.3 μM, respectively).

Diclazuril (R-64433) is a coccidiostat.

ML-336 is an inhibitor of of the Venezuelan equine encephalitis virus (VEEV) strain TC-83.

β-Endorphin, equine TFA, an endogenous opioid peptide, demonstrates high affinity binding to μ/δ opioid receptors and possesses analgesic properties [1] [2] [3] [4].

Flumequine (R-802) is a broad-spectrum antibiotic effective against both Gram-positive and Gram-negative bacteria. It operates by inhibiting DNA gyrase (a type II topoisomerase) and topoisomerase IV, enzymes crucial for separating bacterial DNA, thereby preventing cell division.

Flumequine-13C3 is intended for use as an internal standard for the quantification of flumequine by GC- or LC-MS. Flumequine (T1060) is a fluoroquinolone antibiotic.1It is active againstS. aureus, S. pyogenes, B. subtilis, E. coli, P. aeruginosa, S. faecalis, andK. pneumoniae (MICs = 1-100 μg/ml). Flumequine (T1060) is also active against field isolates of B. hyodysenteriae (MICs = 6.25-200 μg/ml).2It inhibits DNA gyrase, disrupting supercoiling of bacterial DNA to block transcription and replication.3

Hydrocortisone (Cortisol) is a glucocorticoid hormone secreted by the adrenocortex. Hydrocortisone agonizes the glucocorticoid receptor, which promotes proteolytic metabolism, gluconeogenesis, capillary wall stabilization, and renal calcium excretion, as well as suppressing immune and inflammatory responses.

Temechine hydrobromide is used for the identification of new diterpenoidal alkaloid leads as tyrosinase inhibitors.

Anavenol (2-(naphthalen-2-yloxy)ethanol) is an equine anesthetic.

nsP2 Protease-IN-1 is a potent irreversible covalent inhibitor of the nsP2 cysteine protease of the Chikungunya (CHIKV) virus, exhibiting an IC50 of 60 nM. This compound demonstrates strong antiviral activity by inhibiting the replication of CHIKV and Venezuelan equine encephalitis virus (VEEV), with EC50 values of 0.01 µM and 0.3 µM, respectively.

AAK1-IN-6 is an inhibitor of AP-2 associated protein kinase 1 (AAK1, IC50 = 12 nM) and exhibits antiviral activity against Dengue virus (DNEV2, EC50 = 0.24 μM) and Venezuelan equine encephalitis virus (VEEV, EC50 = 0.30 μM). AAK1-IN-6 is applicable in antiviral research.

CHIKV nsP2 protease-IN-2 (Compound 2o) is an allosteric inhibitor of the non-structural protein 2 helicase (nsP2hel), with IC50 values of 0.5 μM for nsP2 ATPase and 0.9 μM for RNA helicase. It exhibits broad-spectrum antiviral activity against alphaviruses, effectively targeting Chikungunya virus (CHIKV), Mayaro virus (MAYV), and Venezuelan equine encephalitis virus (VEEV), with an EC50 of 0.12 μM against CHIKV-nLuc. This compound is useful for research on alphavirus infections.

NHC-diphosphate, a phosphorylated intracellular metabolite of β-d-N4-Hydroxycytidine (NHC) in its diphosphate form[1], serves as a potent antiviral agent. As a pyrimidine ribonucleoside, NHC effectively counters the replication of Venezuelan equine encephalitis virus (VEEV), Chikungunya virus (CHIKV), and hepatitis C virus (HCV)[1].

11-trans Leukotriene C4 (11-trans LTC4) is a C-11 double bond isomer of LTC4. LTC4 undergoes slow temperature-dependent isomerization to 11-trans LTC4 during storage. 11-trans LTC4 is produced in smaller amounts relative to LTC4 in ionophore-stimulated HMC-1 cells (a human mast cell line) and equine eosinophils, but not in human neutrophils or RBL-1 cells. It is nearly equipotent with LTC4 for contraction of guinea pig parenchymal and ileum. In a radioligand binding assay using guinea pig ileum as a cysteinyl leukotriene receptor preparation, the pKis for LTC4 and 11-trans LTC4 were determined to be 6.42 and 6.58, respectively.

STING agonist C11 is an agonist of the stimulator of interferon genes (STING) pathway.1 It induces secretion of type I IFN from THF and MM6 cells when used at a concentration of 50 μM. STING agonist C11 induces phosphorylation of IFN regulatory factor 3 (IRF3) and increases expression of IFIT1 and viperin, but not IL-1β, IL-6, or IL-8 in THF cells in a STING-dependent manner. It reduces viral titers of chikungunya, Venezuelan equine encephalitis, o'nyong-nyong, Mayaro, and Ross River viruses grown in THF cells (EC90s = 16.44, 16.7, 18.84, 25.19, and 22.57 μM, respectively), an effect that is dependent on the presence of STING and the IFN-α/β receptor (IFNAR).References1. Gall, B., Pryke, K., Abraham, J., et al. Emerging alphaviruses are sensitive to cellular states induced by a novel small-molecule agonist of the STING pathway. J. Virol. 92(6), e01913-01917 (2018). STING agonist C11 is an agonist of the stimulator of interferon genes (STING) pathway.1 It induces secretion of type I IFN from THF and MM6 cells when used at a concentration of 50 μM. STING agonist C11 induces phosphorylation of IFN regulatory factor 3 (IRF3) and increases expression of IFIT1 and viperin, but not IL-1β, IL-6, or IL-8 in THF cells in a STING-dependent manner. It reduces viral titers of chikungunya, Venezuelan equine encephalitis, o'nyong-nyong, Mayaro, and Ross River viruses grown in THF cells (EC90s = 16.44, 16.7, 18.84, 25.19, and 22.57 μM, respectively), an effect that is dependent on the presence of STING and the IFN-α/β receptor (IFNAR). References1. Gall, B., Pryke, K., Abraham, J., et al. Emerging alphaviruses are sensitive to cellular states induced by a novel small-molecule agonist of the STING pathway. J. Virol. 92(6), e01913-01917 (2018).

Multitarget AD inhibitor-1 is a reversible and selective inhibitor of butyrylcholinesterase (BuChE) with IC50 values of 7.22 μM for human BuChE (hBuChE) and 1.55 μM for equine serum BuChE (eqBuChE). It also exhibits inhibitory activity towards β-secretase (IC50 41.60 μM), amyloid β aggregation (IC50 3.09 μM), and tau aggregation. As a diphenylpropylamine derivative, Multitarget AD inhibitor-1 is promising for research into multifunctional, disease-modifying treatments for Alzheimer's disease.

AChE/BChE-IN-3 (BMC-1) is a dual inhibitor of AChE and BChE, with IC50 values of 6.08 μM for electric eel AChE (elAChE) and 0.383 μM for equine serum BChE (eqBChE), respectively [1].

AChE/BChE-IN-3 (BMC-1) hydrochloride is a dual inhibitor of AChE and BChE, with IC50 values of 0.383 μM against equine serum BChE (eqBChE) and 6.08 μM against electric eel AChE (elAChE) [1].

Z164597606 is a compound that acts as a selective inhibitor of the enzyme Butyrylcholinesterase (BChE), with IC50 values of 1.3 μM and 1.7 μM for equine BChE and human BChE, respectively. Through a π-π stacking interaction, Z164597606 specifically interacts with the amino acid Trp82 of human BChE. This compound has potential applications in Alzheimer's disease research [1] [2].

AChE/BChE-IN-8 (Compound 5a) is an uncompetitive AChE and mixed BChE inhibitor with Ki values of 0.788 μM against Electrophorus electricus AChE (EeAChE) and 2.364 μM against equine BChE (eqBChE), respectively. AChE/BChE-IN-8 demonstrates blood-brain barrier permeability and low cytotoxicity.

AChE-IN-14 is a potent cholinesterase inhibitor, acting on electric eel acetylcholinesterase (eeAChE) (IC50: 0.46 μM), human recombinant acetylcholinesterase (hAChE) (IC50: 0.48 μM) and equine serum butyrylcholinesterase (eqBuChE) (IC50: 0.44 μM). AChE-IN-14 has a high affinity for the human H3 receptor (H3R) (Ki: 159.8 nM) and can be used to study Alzheimer's disease.

Encephalitic alphavirus-IN-1 inhibited the activity of Venezuelan equine encephalitis virus (VEEV) (EC50: 0.24 μM) and eastern equine encephalitis virus (EEEV) (EC50: 0.16 μM). encephalitic alphavirus-IN-1 was not significantly cytotoxic and exhibited strong plasma stability in mice.