| 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. |
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| 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. |
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| 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. |
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| 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. |
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| 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. |
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| 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. |
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| DC74988 |
Mepazine chloride |
Mepazine chloride is a MALT1 inhibitor. |
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| 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. |
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| DC74990 |
Ethacrynic acid |
Etharcrynic Acid is a compound that inhibits symport of sodium, potassium, and chloride primarily in the ascending limb of Henle, but also in the proximal and distal tubules. This pharmacological action results in excretion of these ions, increased urinary output, and reduction in extracellular fluid. This compound has been classified as a loop or high ceiling diuretic. Ethacrynic Acid is an unsaturated ketone derivative of aryloxyacetic acid without a sulfonamide substituent belonging to the class of loop diuretics. Ethacrynic acid is extensively bound to plasma proteins; both ethacrynic acid in its unchanged form as well as its metabolites are excreted in bile and urine. |
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| DC74991 |
Obatoclax free base |
Obatoclax, also known as GX 015-070, a synthetic small-molecule inhibitor of the bcl-2 family of proteins with potential pro-apoptotic and antineoplastic activities. Obatoclax binds to members of the Bcl-2 protein family, preventing the binding of these anti-apoptotic proteins to the pro-apoptotic proteins Bax and Bak and so promoting the activation of the apoptotic pathway in Bcl-2-overexpressing cells. The Bcl-2 family of proteins (bcl-2, bcl-xl, bcl-w, and Mcl-1) are overexpressed in a wide variety of cancers, including those of the lymphatic system, breast, lung, prostate, and colon. |
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| DC74992 |
Tenapanor HCl |
Tenapanor, also known as AZD-1722 and RDX 5791, is an inhibitor of the sodium-proton (Na(+)/H(+)) exchanger NHE3, which plays a prominent role in sodium handling in the gastrointestinal tract and kidney. Tenapanor possesses an excellent preclinical safety profile and, as of now, there are no serious concerns about its side effects. |
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| DC74993 |
KB-0742 HCl |
KB-0742 is an orally bioavailable, selective CDK9 inhibitor with potent anti-tumor activity in CRPC models. In 22Rv1 cells, KB-0742 rapidly downregulates nascent transcription, preferentially depleting short half-life transcripts and AR-driven oncogenic programs. In vivo, oral administration of KB-0742 significantly reduced tumor growth in CRPC, supporting CDK9 inhibition as a promising therapeutic strategy to target AR dependence in CRPC. |
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| DC74994 |
Lomibuvir |
Lomibuvir, also known as VX-222, VCH-222 and VX22, is an nonnucleoside NS5B polymerase inhibitor. VX-222 inhibits the 1b/Con1 HCV subgenomic replicon, with 50% effective concentrations (EC(50)s) 5 nM. VX-222 binds to the HCV polymerase with dissociation constants of 17 nM. In phase 1 and 2 clinical studies, VX-222 demonstrated effective antiviral efficacy, with substantial reductions in plasma HCV RNA in patients chronically infected with genotype 1 HCV. |
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| DC74995 |
Lifitegrast |
Lifitegrast, also known as SAR-1118, is an LFA-1 antagonist intended for the treatment of vascular complications of the eye. Lifitegrast inhibits T cell-mediated inflammation by blocking the binding of two important cell surface proteins (lymphocyte function-associated antigen 1 and intercellular adhesion molecule 1), thus lessening overall inflammatory responses. |
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| DC74996 |
Dobutamine HCl |
Dobutamine is a sympathomimetic drug used in the treatment of heart failure and cardiogenic shock. Its primary mechanism is direct stimulation of β1 receptors of the sympathetic nervous system. |
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| DC74997 |
CRT0066101 free base |
CRT0066101 is a PRKDs inhibitor. CRT0066101 suppressed the proliferation and migration of four bladder cancer cell lines in vitro. CRT0066101 blocked tumor growth in a mouse flank xenograft model of bladder cancer. CRT0066101 treatment or PKD2 silencing arrested bladder cancer cells at the G2/M phase, the arrest being accompanied by decreases in the levels of cyclin B1, CDK1 and phospho-CDK1 (Thr161) and increases in the levels of p27Kip1 and phospho-CDK1 (Thr14/Tyr15). CRT0066101 suppresses bladder cancer growth by inhibiting PKD2 through induction of G2/M cell cycle arrest, leading to the blockade of cell cycle progression. |
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| DC74998 |
Tafenoquine free base |
Tafenoquine, also known as WR-238605, is an oral active antimalaria drug that is being investigated as a potential treatment for malaria, as well as for malaria prevention. Tafenoquine Shows Activity against Trypanosoma brucei. Tafenoquine targets leishmania respiratory complex III and induces apoptosis. Tafenoquine has a long half-life of approximately 14 days and is generally safe and well tolerated, Malaria remains an important cause of global morbidity and mortality. As antimalarial drug resistance escalates, new safe and effective medications are necessary to prevent and treat malarial infection. |
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| DC74999 |
Memantine HCl |
Memantine Hydrochloride is the hydrochloride salt of memantine, a low-affinity, voltage-dependent, noncompetitive N-methyl-D-aspartate (NMDA) receptor antagonist. Memantine binds to and inhibits cation channels of glutamanergic NMDA receptors located in the central nervous system, preventing the prolonged influx of calcium ions and the associated neuronal excitotoxicity, and thereby potentially enhancing cognitive function. Memantine is also a 5-hydroxytryptamine type 3 (5HT3) receptor and nicotinic receptor antagonist. |
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| DC75000 |
cGAMP free acid |
Cyclic AMP-GMP, also known as cGAMP, is one of several naturally occurring cyclic dinucleotides that act as a bacterial second messengers to regulate important signaling mechanisms in prokaryotes that control bacterial survival, adhesion, colonization, biofilm formation, and virulence factors production. In cholera c-AMP-GMP promotes intestinal colonization by down-regulating chemotaxis. During infections bacterial cGAMP is bound by host STING (stimulator of interferon genes) activating innate immune responses leading to expression of interferon genes. |
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| DC75001 |
Sivelestat free acid |
Sivelestat, also known as ONO 5046, is an inhibitor of human neutrophil elastase. It is used in the treatment of acute respiratory failure. Preliminary studies show Sivelestat may also improve neuropathic pain. |
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| DC75002 |
Duvoglustat Free Base |
Duvoglustat Free Base is an alpha-glucosidase inhibitor with antiviral action. Derivatives of deoxynojirimycin may have anti-HIV activity. |
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| DC75003 |
WUN40378 |
WUN40378 is compound first reported in PCT Int. Appl. (2019), WO 201909959, in which it was described as CBFβ-RUNX1 inhibitor. WUN40378 is very similar to Ro 5-3335 but with an F instead of Cl. WUN40378 is also analog of Ro 24-7429. This product has no formal name at the moment. For the convenience of communication, a temporary code name was therefore proposed according to MedKoo Chemical Nomenclature (see web page: https://www.medkoo.com/page/naming). |
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| DC75004 |
Daridorexant free base |
Daridorexant, also known as Nemorexant and ACT541468, is a new dual orexin receptor antagonist, used in the treatment of Insomnia Disorder in Adult Patients. By specific binding to both orexin receptors, daridorexant inhibits the actions of the wake-promoting orexin (also called hypocretin) neuropeptides. This mechanism avoids a more widespread inhibition of neuronal pathways and associated side effects that are intrinsic to positive allosteric GABA-A receptor modulators. Daridorexant was approved for Adults With Insomnia in Jan 2022. |
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| 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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| 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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