| DC75005 |
TCS-OX2-29 free base |
TCS-OX2-29 is a selective OX2 receptor antagonist (IC50 = 40 nM). Orexin, which is mainly produced by orexin-expressing neurons in the lateral hypothalamus (LH), plays an important role in pain modulation. Both kinds of orexin-1 (Ox1) and orexin-2 (Ox2) receptors have been found at high density in the ventral tegmental area (VTA) and nucleus accumbens (NAc). |
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| DC75006 |
VX-787 |
Pimodivir, also known as VX-787, JNJ-872, is a novel inhibitor of influenza virus replication that blocks the PB2 cap-snatching activity of the influenza viral polymerase complex. VX-787 binds the cap-binding domain of the PB2 subunit with a KD (dissociation constant) of 24 nM as determined by isothermal titration calorimetry (ITC). The cell-based EC50 (the concentration of compound that ensures 50% cell viability of an uninfected control) for VX-787 is 1.6 nM in a cytopathic effect (CPE) assay, with a similar EC50 in a viral RNA replication assay. VX-787 is active against a diverse panel of influenza A virus strains, including H1N1pdm09 and H5N1 strains, as well as strains with reduced susceptibility to neuraminidase inhibitors (NAIs). |
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| DC75007 |
JQKD82 HCl |
JQKD82, also known as PCK82, is a cell-permeable and selective KDM5 inhibitor (MM.1S cells, IC50 = 0.42 uM). JQKD82 increases histone H3K4me3 but paradoxically inhibits downstream MYC-driven transcriptional output in vitro and in vivo. JQKD82 is a useful tool compound to block KDM5A function as a potential therapeutic strategy for MM. QKD82 is a more stable ester of KDM5-C49 that is able to deliver the active molecule KDM5-C49 to cells more efficiently |
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| DC75008 |
ML095 HCl |
ML095, also known as CID-25067483 and MLS-0315848, is a PLAP inhibitor (placental alkaline phosphatase inhibitor). The IC50 valuess of ML095 against PLAP, TNAP and IAP are 2.1, >100 and 53 μM, respectively. |
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| DC75009 |
Silmitasertib sodium |
Silmitasertib sodium is an orally bioavailable small-molecule inhibitor of CK2 with potential antineoplastic activity. Silmitasertib selectively binds to and inhibits the enzyme casein kinase II (CK2), which may lead to an inhibition of cellular proliferation. CK2, a protein kinase often overexpressed in a variety of cancer cell types, appears to be correlated with malignant transformation, tumor growth and survival. |
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| DC75010 |
TAE-1 Iodide |
TAE-1 is a AChE inhibitor. TAE-1 inhibits acetylcholinesterase (AChE; IC50 = 0.465 µM for the human erythrocyte enzyme). |
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| DC75011 |
PSMA-11 free base |
Gozetotide, also known as PSMA-11, DKFZ-PSMA-11, HBED-CC-PSMA or Psma-hbed-CC, is a ligand to make gallium Ga 68-labeled PSMA-11, which has potential use as a tracer for PSMA-expressing tumors during positron emission tomography (PET). Upon intravenous administration of gallium Ga 68-labeled PSMA-11, the Glu-urea-Lys(Ahx) moiety targets and binds to PSMA-expressing tumor cells. Upon internalization, PSMA-expressing tumor cells can be detected during PET imaging. PSMA, a tumor-associated antigen and type II transmembrane protein, is expressed on the membrane of prostatic epithelial cells and overexpressed on prostate tumor cells |
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| DC75012 |
Ertapenem Sodium |
Ertapenem Sodium is the sodium salt of ertapenem, a 1-beta-methyl carbapenem and a broad-spectrum beta-lactam antibiotic with bactericidal activity. Ertapenem binds to penicillin binding proteins located on the bacterial cell wall, in particular PBPs 2 and 3, thereby inhibiting the final transpeptidation step in the synthesis of peptidoglycan, an essential component of the bacterial cell wall. Inhibition of peptidoglycan synthesis results in weakening and lysis of the cell wall and cell death. Erapenem is resistant to hydrolysis by a variety of beta-lactamases, including penicillinases, cephalosporinases and extended-spectrum beta-lactamases. |
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| DC75013 |
Caroverine HCl |
Caroverine is a nonselective NMDA and AMPA glutamate receptor antagonist, also acting as a class B calcium-channel-blocker. Pharmacologically, it has been described as a nonspecific calcium channel blocker and as an antagonist of both non-NMDA and NMDA glutamate receptors. Caroverine (Spasmium, Tinnitin, Tinnex) is a muscle-relaxing drug used in Austria and Switzerland to relieve spasms in smooth muscles (which include intestines, arteries, and other organs), and the use in those countries was extended to aid with cerebrovascular diseases there, and eventually to treat tinnitus. caroverine is also a potential chemotherapeutical agent in HNSCC cell lines. |
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| DC75014 |
Toceranib free base |
Toceranib, also known as PHA-291639 and SU 11654, is a receptor tyrosine kinase inhibitor and is used in the treatment of canine mast cell tumor also called mastocytoma. Toceranib phosphate was approved for dog. Toceranib is likely to act mostly through inhibition of the kit tyrosine kinase, though it may also have an anti-angiogenic effect. |
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| DC75015 |
Sofinicline |
Sofinicline, also known as ABT-894 and A-422894, is a novel nicotinic acetylcholine receptor agonist under development for the treatment of attention-deficit/hyperactivity disorder. Sofinicline appears to be well tolerated and showing efficacy similar to that of atomoxetine. |
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| DC75016 |
Nirogacestat HBr |
Nirogacestat, also known as PF-03084014, is a potent and selective gamma secretase (GS) inhibitor with potential antitumor activity. PF-03084014 binds to GS, blocking proteolytic activation of Notch receptors. Nirogacestat enhances the Antitumor Effect of Docetaxel in Prostate Cancer. Nirogacestat enhances docetaxel-mediated tumor response and provides a rationale to explore GSIs as adjunct therapy in conjunction with docetaxel for men with CRPC (castration-resistant prostate cancer). |
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| DC75017 |
Delafloxacin |
Delafloxacin, also known as ABT-492, RX-3341 and WQ-3034, is a non-zwitterionic fluoroquinolone antibiotic under development for for the treatment of respiratory and skin infections. Delafloxacin demonstrates excellent antibacterial potency and exhibits a low probability for the selection of resistant mutants in MRSA. Although mutants can be selected at low frequencies in vitro from quinolone-resistant isolates, delafloxacin MICs and MPCs remain low and a fitness cost can be observed. Consequently delafloxacin warrants further investigation for the potential treatment of drug-resistant MRSA infections. |
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| DC75018 |
Cutamesine HCl |
Cutamesine, also known as SA-4503 and AGY94806, is a sigma-1 receptor agonist under development for recovery enhancement after acute ischemic stroke. Cutamesine protects against retinal cell death in vitro and in vivo by the agonistic effect of sigma-1 receptor. Therefore, sigma-1 receptor may have a potential as a therapeutic target in retinal diseases mediated by photoreceptor degeneration. . |
|
| DC75019 |
FB23 inhibitor |
FB23 is a potent and selective inhibitor of N6-methyladenosine (m6A) demethylase FTO (fat mass and obesity associated protein). It moderately inhibits proliferation of NB4 and MONOMAC6 cells. FB23 demonstrates its potent inhibitory impact in AML models. |
|
| DC75020 |
SKF-38393 HCl |
SKF-38393, also known as (+/-)-SKF-38393, is a synthetic compound of the benzazepine chemical class which acts as a selective D1/D5 receptor partial agonist. It has stimulant and anorectic effects. SKF-38393 improves temporal order memory performance in maternally deprived rats. SKF-38393 reverses cocaine-conditioned place preference in mice. SKF-38393 induces GAP-43 expression and long-term potentiation in hippocampus in vivo. |
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| DC75021 |
Atigliflozin |
Atigliflozin, also known as AVE 2268, is an antihyperglycaemic drug candidate. |
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| DC75022 |
Telacebec free base |
Telacebec, also known as Q-203, is an antituberculosis agent and a potent inhibitor of mycobacterium tuberculosis protein potentially for the treatment of tuberculosis. Telacebec targets Mycobacterium tuberculosis cellular energy production through inhibition of the mycobacterial cytochrome bc1 complex. Q203 inhibited the growth of MDR and XDR M. tuberculosis clinical isolates in culture broth medium in the low nanomolar range and was efficacious in a mouse model of tuberculosis at a dose less than 1 mg per kg body weight, which highlights the potency of this compound. In addition, Q203 displays pharmacokinetic and safety profiles compatible with once-daily dosing. |
|
| DC75023 |
Tafamidis |
Tafamidis, Tafamidis, also known as Fx-1006 or PF-06291826, is a drug for the amelioration of transthyretin-related hereditary amyloidosis (also familial amyloid polyneuropathy, or FAP), a rare but deadly neurodegenerative disease. The drug was approved by the European Medicines Agency in November 2011 and by the Japanese Pharmaceuticals and Medical Devices Agency in September 2013. Tafamidis functions by kinetic stabilization of the correctly folded tetrameric form of the transthyretin (TTR) protein. |
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| DC75024 |
Evatanepag |
Evatanepag, also known as CP-533536, is an EP2 receptor selective prostaglandin E2 (PGE2) agonist that induces local bone formation. CP-533536 demonstrated the ability to heal fractures when administered locally as a single dose in rat models of fracture healing. |
|
| DC75025 |
ITI-214 phosphate |
ITI-214 is an orally active, potent and Selective Inhibitors of Phosphodiesterase 1 for the Treatment of Cognitive Impairment Associated with Neurodegenerative and Neuropsychiatric Diseases. ITI-214 exhibited picomolar inhibitory potency for PDE1, demonstrated excellent selectivity against all other PDE families, and showed good efficacy in vivo. Currently, this investigational new drug is in Phase I clinical development and being considered for the treatment of several indications including cognitive deficits associated with schizophrenia and Alzheimer's disease, movement disorders, attention deficit and hyperactivity disorders, and other CNS and non-CNS disorders. |
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| DC75026 |
Metformin free base |
Metformin is an AMP-activated protein kinase (AMPK) activator that improves glycemic control by improving insulin sensitivity and decreasing intestinal absorption of glucose. Metformin exerts an anorexiant effect, decreasing caloric intake. Metformin decreases gluconeogenesis (glucose production) in the liver. Metformin inhibits basal secretion from the pituitary gland of growth hormone, adrenocorticotropic hormone, follicle stimulating hormone, and expression of proopiomelanocortin, which in part accounts for its insulin-sensitizing effect with multiple actions on tissues including the liver, skeletal muscle, endothelium, adipose tissue, and the ovaries. |
|
| DC75027 |
Eravacycline HCl |
Eravacycline, also known as TP-434, a novel antibiotics. Eravacycline showed potent broad-spectrum activity against 90% of the isolates (MIC90) in each panel at concentrations ranging from ≤0.008 to 2 μg/ml for all species panels except those of Pseudomonas aeruginosa and Burkholderia cenocepacia (MIC90 values of 32 μg/ml for both organisms). The antibacterial activity of eravacycline was minimally affected by expression of tetracycline-specific efflux and ribosomal protection mechanisms in clinical isolates. Furthermore, eravacycline was active against multidrug-resistant bacteria. Eravacycline has the potential to be a promising new intravenous (i.v.)/oral antibiotic for the empirical treatment of complicated hospital/health care infections and moderate-to-severe community-acquired infections. |
|
| DC75028 |
Brilacidin HCl |
Brilacidin, also known as PMX30063, is an arylamide foldamer designed to replicate the amphiphilic properties of antimicrobial peptides while solving the problems encountered by peptide-based antimicrobials. Brilacidin, a broad-spectrum antibiotic, has potent Gram positive activity and Gram negative coverage, and is highly effective in treating the 'superbug' methicillin-resistant Staphylococcus aureus (MRSA). Brilacidin has low cytotoxicity against mammalian cells selectively targeting bacteria, directly and rapidly disrupting their membranes, resulting in the bacteria's death. Due to this unique mechanism of action (mimicking the host's natural immune response, proven to be successful in fighting off infections over millions of years of evolution), bacterial antibiotic resistance is less likely to develop. |
|
| DC75029 |
Sarecycline HCl |
Sarecycline, also known as WC-3035 and P005672, is a novel, tetracycline-derived, narrow-spectrum antibiotic being developed for use as an oral once daily antibiotic treatment for patients suffering from moderate to severe acne vulgaris. Sarecycline was designed by Paratek as a narrow-spectrum antibiotic with anti-inflammatory activity and the potential for a favorable tolerability profile. |
|
| DC75030 |
Sitravatinib free base |
Sitravatinib, also known as MGCD516 or MG516, is a novel small molecule inhibitor targeting multiple RTKs involved in driving sarcoma cell growth. MGCD516 treatment resulted in significant blockade of phosphorylation of potential driver RTKs and induced potent anti-proliferative effects in vitro. MGCD516 treatment of tumor xenografts in vivo resulted in significant suppression of tumor growth. |
|
| DC75031 |
Esomeprazole Magnesium hydrate |
Esomeprazole Magnesium is the magnesium salt of esomeprazole, the S-isomer of omeprazole, with gastric proton pump inhibitor activity. In the acidic compartment of parietal cells, esomeprazole is protonated and converted into the active achiral sulphenamide; the active sulphenamide forms one or more covalent disulfide bonds with the proton pump hydrogen-potassium adenosine triphosphatase (H+/K+ ATPase), thereby inhibiting its activity and the parietal cell secretion of H+ ions into the gastric lumen, the final step in gastric acid production. H+/K+ ATPase is an integral membrane protein of the gastric parietal cell. |
|
| DC75032 |
Gepotidacin mesylate dihydrate |
Gepotidacin, also known as GSK-2140944, is a potent Type II DNA topoisomerase inhibitor. Gepotidacin is a novel antibacterial drug candidate. Gepotidacin Demonstrates Absence of Fluoroquinolone-Like Arthropathy in Juvenile Rats. Gepotidacin is efficacious in a nonhuman primate model of pneumonic plague. When tested against Gram-negative (n = 333) and Gram-positive (n = 225) anaerobes by agar dilution, gepotidacin inhibited 90% of isolates at concentrations of 4 and 2 μg/mL, respectively. |
|
| DC75033 |
Selpercatinib |
Selpercatinib, also known as LOXO-292, is a potent and selective RET inhibitor with antineoplastic properties. LOXO-292 selectively binds to and targets various RET mutants and RET-containing fusion products. This results in an inhibition of cell growth of tumors cells that exhibit increased RET activity. Selpercatinib was approved in May 2020. |
|
| DC75034 |
Arsthinol |
Arsthinol is an antiprotozoal agent which may have anti-cancer activity. It was found that arsthinol, a trivalent organoarsenic compound (dithiarsolane), has been active in vitro on leukemia cell lines and offers a better therapeutic index than arsenic trioxide, as estimated by the ratio LD50/IC50. Arsthinol induced growth inhibition of NB4 cells at lower concentration (IC50 (concentration inhibiting growth by 50%) = 0.78 +/- 0.08 micromol/l after 24 h) than As(2)O(3) (IC50 = 1.60 +/- 0.23 micromol/l after 24 h) or melarsoprol (IC50 = 1.44 +/- 0.08 micromol/l after 24 h). Arsthinol-cyclodextrin complex demonstrated to have was more effective than arsenic trioxide (As2O3) and melarsoprol on the U87 MG cell line. Importantly, in the in vivo study, significant antitumor activity against heterotopic xenografts was observed after i.p. administration. |
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