| DC74960 |
LY-2608204 |
LY-2608204 is an activator of glucokinase (GK) with an EC50 value of 42 nM. LY2608204 decreases plasma glucose in a dose-dependent manner at both fasted and postprandial glucose levels. In 2010, LY-2608204 was entered clinical trials in Patients With Type 2 Diabetes. |
|
| DC74961 |
KPI-10 |
KPI-10, also known as WQ3810, is a new compound currently being studied for its efficacy in the treatment of infections caused by multidrug-resistant bacteria. WQ-3810 demonstrated high potent activity against the antimicrobial-resistant pathogens tested. WQ-3810 (MIC(90)=4 mg/L and 0.06 mg/L, respectively) was also more active than ciprofloxacin (64 mg/L and 2 mg/L) and levofloxacin (32 mg/L and 2 mg/L). Furthermore, WQ-3810 was the most potent among the fluoroquinolones tested against meticillin-resistant Staphylococcus aureus (MRSA) and Neisseria gonorrhoeae, including FQR isolates. |
|
| DC74962 |
Carisbamate |
Carisbamate, also known as JNJ-10234094, RWJ 333369 and YKP-509, is an antiepileptic candidate. Carisbamate has powerful disease-modifying effects in the lithium-pilocarpine model of temporal lobe epilepsy. Carisbamate inhibits glutamate transmission in the granule cell of the dentate gyrus. Carisbamate acutely suppresses spasms in a rat model of symptomatic infantile spasms. |
|
| DC74963 |
Umifenovir HCl |
Umifenovir, also known as arbidol, is an antiviral treatment used in Russia and Chinafor influenza infection. Since 2005 it has been the number one best-selling over-the-counter drug in Russia. Umifenovir inhibits membrane fusion. Umifenovir prevents contact between the virus and target host cells. Fusion between the viral capsid and the cell membrane of the target cell is inhibited. This prevents viral entry to the target cell, and therefore protects it from infection. |
|
| DC74964 |
Pirtobrutinib |
Pirtobrutinib, also known as LOXO-305 and LY 3527727, is a Bruton's tyrosine kinase (BTK) inhibitor and antineoplastic agent. Pirtobrutinib showed promising initial efficacy in pts with pretreated Richter transformation with extremely poor prognosis, including in patients who had received prior chemoimmunotherapy and covalent BTK inhibitors. Pirtobrutinib is a highly selective and potent non-covalent BTK inhibitor (BTKi) with high oral bioavailability and a long half-life, resulting in robust BTK target coverage even in high-grade malignancies with high BTK protein turnover. |
|
| DC74965 |
Tiplasinin free acid |
Tiplaxtinin, also known as PAI-039, is a novel plasminogen activator inhibitor-1 (PAI-1) inhibitor. The pharmacokinetic profile of PAI-039 indicated an oral bioavailability of 43 +/- 15.3% and a plasma half-life of 6.2 +/- 1.3 h. PAI-039 is an orally active prothrombolytic drug that inhibits PAI-1 and accelerates fibrinolysis while maintaining normal coagulation in a model of coronary occlusion . PAI-039 exerts antithrombotic efficacy in rat models of arterial and venous vascular injury without effecting platelet aggregation. PAI-039 as a novel therapeutic may improve diabetic wound closure. |
|
| DC74966 |
Fabomotizole HCl |
Fabomotizole, also known as Afobazole, Obenoxazine and CM346, is an anxiolytic drug launched in Russia in the early 2000s. It produces anxiolytic and neuroprotective effects without any sedative or muscle relaxant actions. Its mechanism of action remains poorly defined however, with GABAergic, NGF- and BDNF-release-promoting, MT1 receptor agonism, MT3 receptor antagonism, and sigma agonism suggested as potential mechanisms. Fabomotizole was shown to inhibit MAO-A reversibly and there might be also some involvement with serotonin receptors. |
|
| DC74967 |
Fluoxetine HCl |
Fluoxetine, also known by trade names Prozac and Sarafem among others, is an antidepressant of the selective serotonin reuptake inhibitor (SSRI) class. It is used for the treatment of major depressive disorder, obsessive–compulsive disorder, bulimia nervosa, panic disorder, and premenstrual dysphoric disorder. It may decrease the risk of suicide in those over the age of 65. Fluoxetine has also been used to treat premature ejaculation. It is taken by mouth. |
|
| DC74968 |
Tracazolate HCl |
Tracazolate is an allosteric modulator of GABAA receptors. Tracazolate interacts with gamma-aminobutyric acid (GABA)(A) receptors, adenosine receptors, and phosphodiesterases. |
|
| DC74969 |
Metaraminol Bitartrate |
Metaraminol bitartrate is a sympathomimetic agent that acts predominantly at alpha-1 adrenergic receptors. It has been used primarily as a vasoconstrictor in the treatment of hypotension. |
|
| DC74970 |
CC90001 free base |
CC-90001 is a potent and selective JNK inhibitor, which is 12.9-fold more potent for JNK1 inhibition than JNK2 in a cell-based model. CC90001 currently under clinical trials for the Treatment of Idiopathic Pulmonary Fibrosis. |
|
| DC74971 |
Cefotetan Sodium |
Cefotetan Sodium, also known as ICI-156834 and YM-09330, is a second-generation cephalosporin, cephamycin antibiotic that is active against a wide range of both aerobic and anaerobic gram-positive and gram-negative bacteria. Cefotetan binds to penicillin-binding proteins and disrupts the cell wall synthesis. |
|
| DC74972 |
Exeporfinium bromide |
Exeporfinium, also known as XF-73, is an anti-microbial which works via weakening bacteria cell walls. Exeporfinium chloride is a potential treatment for methicillin-resistant Staphylococcus aureus (MRSA) and possibly Clostridium difficile. Exeporfinium chloride has completed a phase I clinical trial for nasal decolonisation of MRSA—being tested against 5 bacterial strains. It seems unlikely to cause MRSA to develop resistance to it. Structurally it is a dicationic porphyrin. |
|
| DC74973 |
NADH |
NADH is the reduced form of NAD, or nicotinamide adenine dinucleotide. NADH is used as a reducing agent to donate electrons in metabolic reactions. |
|
| DC74974 |
Simufilamum |
Simufilamum, also known as PTI-125, is a filamin A altered conformations binder. PTI-125 is an oral small molecule drug candidate that binds and reverses an altered conformation of the scaffolding protein filamin A found in Alzheimer's disease brain. PTI-125 binds and reverses an altered conformation of filamin A to reduce Alzheimer's disease pathogenesis. PTI-125 also reduced tau hyperphosphorylation, aggregated Aβ42 deposition, neurofibrillary tangles, and neuroinflammation. Efficacy in postmortem AD and Aβ42-treated age-matched control hippocampal slices was concentration-dependent starting at 1 picomolar (pM) concentration. PTI-125 is the first therapeutic candidate to preferentially bind an altered protein conformation and reverse this proteopathy. |
|
| DC74975 |
NADPH Cy4N |
NADPH Cy4N also known as NADPH, cyclohexyl ammonium salt is the ammonium salt form of NADPH, which the reduced form of NADP+. NADPH is used in anabolic reactions (such as lipid and nucleic acid synthesis) as a reducing agent and cofactor. |
|
| DC74976 |
Atopaxar |
Atopaxar, also known as E5555, is a potent and orally-active PAR-1 inhibitor. E5555 inhibited the binding of a high-affinity thrombin receptor-activating peptide ([(3)H]haTRAP) to PAR-1 with a half maximal inhibitory concentration (IC(50)) value of 0.019μM. E5555 showed potent inhibitory effects on human platelet aggregation induced by thrombin and TRAP with IC(50) values of 0.064 and 0.031μM, respectively. E5555 showed potent and selective inhibitory effects on guinea pig platelet aggregation induced by thrombin and TRAP with IC(50) values of 0.13 and 0.097μM, respectively. E5555 could be a therapeutic option for atherothrombotic disease. |
|
| DC74977 |
Arbaclofen |
Arbaclofen, also known as (R)-Baclofen, D-Baclofen and STX209, is a selective GABA-B agonist and is hypothesized to modulate the balance of excitatory to inhibitory neurotransmission, and has shown preliminary evidence of benefit in fragile X syndrome. STX209 may be a potentially effective therapy to treat the core symptoms of FXS. Autism spectrum disorder (ASD) is a behaviorally defined disorder which has increased in prevalence over the last two decades. |
|
| DC74978 |
Abediterol |
Abediterol, also known as LAS100977, is a novel potent, long-acting inhaled β(2)-adrenoceptor agonist in development for the treatment of asthma and chronic obstructive pulmonary disease. Abediterol shows subnanomolar affinity for the human β(2)-adrenoceptor and a functional selectivity over β(1)-adrenoceptors higher than that of formoterol and indacaterol in both a cellular model with overexpressed human receptors and isolated guinea pig tissue. Abediterol is a full agonist at the human β(2)-adrenoceptor (E(max) = 91 ± 5% of the maximal effect of isoprenaline). The potency and onset of action that abediterol shows in isolated human bronchi (EC(50) = 1.9 ± 0.4 nM; t½ onset = 7-10 min) is not significantly different from that of formoterol, but its duration of action (t½ ∼ 690 min) is similar to that of indacaterol. |
|
| DC74979 |
NADPH tetrasodium |
NADPH, tetrasodium salt is the sodium salt form of NADPH, which the reduced form of NADP+. NADPH is used in anabolic reactions (such as lipid and nucleic acid synthesis) as a reducing agent and cofactor. |
|
| DC74980 |
NADPH free acid |
NADPH, the reduced form of NADP+, is used in anabolic reactions (such as lipid and nucleic acid synthesis) as a reducing agent and cofactor. |
|
| DC74981 |
Isavuconazonium Free Base |
Isavuconazole (BAL4815; trade name Cresemba) is a triazole antifungal drug. Its prodrug, isavuconazonium sulfate (BAL8557), was granted approval by the U.S. Food and Drug Administration (FDA) on March 6, 2015. Isavuconazole has been approved for treatment of invasive aspergillosis and invasive mucormycosis in adults ages 18 years and older. Both infections are caused by mold and fungi common to the environment, and occur in individuals who are immunosuppressed or have other complicating conditions, such as diabetes or lung disease. |
|
| DC74982 |
Treprostinil diolamine |
Treprostinil is a vasodilator that is used for the treatment of pulmonary arterial hypertension. Treprostinil is a chemically stable prostacyclin analog. Its principal pharmacologic action is direct vasodilation, which causes reduction of pulmonary and systemic arterial pressure, reducing right and left ventricular afterload; therefore improves the cardiac output. It also has an antiplatelet effect. |
|
| DC74983 |
Sulbactam sodium |
Sulbactam sodium is a beta-lactamase inhibitor with very weak antibacterial action. The compound prevents antibiotic destruction of beta-lactam antibiotics by inhibiting beta-lactamases, thus extending their spectrum activity. Combinations of sulbactam with beta-lactam antibiotics have been used successfully for the therapy of infections caused by organisms resistant to the antibiotic alone. |
|
| DC74984 |
Exeporfinium chloride |
Exeporfinium, also known as XF-73, is an anti-microbial which works via weakening bacteria cell walls. Exeporfinium chloride is a potential treatment for methicillin-resistant Staphylococcus aureus (MRSA) and possibly Clostridium difficile. Exeporfinium chloride has completed a phase I clinical trial for nasal decolonisation of MRSA—being tested against 5 bacterial strains. It seems unlikely to cause MRSA to develop resistance to it. Structurally it is a dicationic porphyrin. |
|
| DC74985 |
PFI-2 hydrochloride |
PFI-2 is a potent inhibitor of SETD7 with IC50 2 nM and 1000-fold selectivity over other methyltransferases and other non-epigenetic targets. PFI-2 has been shown to bind to SETD7 by ITC (Kd=18nM) and biotinylated PFI-2 interacts with SETD7 in pull-down studies. Its enantiomer (S)-PFI-2 is 500-fold less active making it an excellent negative control. Treatment of low-density MEFs with (R)-PFI-2 resulted in higher nuclear YAP levels indicating an effect on the Hippo pathway. |
|
| DC74986 |
Carvedilol (free base) |
Carvedilol (free base) is a non-selective beta-adrenoceptor blocking agent (S(-) enantiomer) and as an alpha 1-adrenoceptor blocker (R(+) and S(-) enantiomers) indicated in the treatment of mild to moderate congestive heart failure (CHF). Its acts more strongly on beta-receptors than on alpha 1-receptors, reduces peripheral vascular resistance by vasodilation, and prevents reflex tachycardia (beta-blockade) so that heart rate is either unchanged or decreased.It blocks beta-1 and beta-2 adrenergic receptors as well as the alpha-1 adrenergic receptors. Carvedilol is a synthetic antihypertensive methoxyphenoxy- 2-propanol derivative with no intrinsic sympathomimetic activity. Carvedilol also reduces renin release through beta-blockade. |
|
| DC74987 |
Cerlapirdine free base |
Cerlapirdine, also known as SAM-531, WAY-262,531 and PF-05212365, is a selective, potent, full antagonist of the 5-hydroxytryptamine 6 (5-HT6) receptor. Cerlapirdine has been in clinical development for the treatment of cognitive disorders associated with Alzheimer's disease and schizophrenia. As of 2011, it is in phase II clinical trials, and has demonstrated a trend toward efficacy along with a good side effect profile and no incidence of serious adverse events. It exerts its effects by acting as a selective 5-HT6 receptor antagonist. |
|
| DC74988 |
Mepazine chloride |
Mepazine chloride is a MALT1 inhibitor. |
|
| DC74989 |
MS023 free base |
MS023 is a Potent, Selective, and Cell-Active Inhibitor of Human Type I Protein Arginine Methyltransferases. MS023 displayed high potency for type I PRMTs including PRMT1, -3, -4, -6, and -8 but was completely inactive against type II and type III PRMTs, protein lysine methyltransferases and DNA methyltransferases. MS023 is a useful chemical tool for investigating the role of type I PRMTs in health and disease. |
|
