| 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. |
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| 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. |
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| 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. |
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| 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. |
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| 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. |
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| 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. |
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| 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. |
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| 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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