| DC75829 |
Cefuroxime axetil |
Cefuroxime axetil is a second generation cephalosporin antibiotic with a broad spectrum activity against Gram positive and Gram negative bacteria. |
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| DC75830 |
Brepocitinib free base |
Brepocitinib, also known as PF-06700841, is an inhibitor of JAK1 and TYK2 kinases for potential treatment of systemic lupus erythematosus and plaque psoriasis. PF-06700841 potently inhibits TYK2/JAK2 mediated IL-12/pSTAT4 and IL-23/pSTAT3 (HWB IC50 = 65 and 120 nM, respectively). PF-06700841 improves clinical symptoms of chronic plaque psoriasis by inhibition of proinflammatory cytokines that require TYK2 and Janus kinase 1 for signal transduction. |
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| DC75831 |
Otenabant HCl |
Otenabant, also known as CP-945,598, is a drug which acts as a potent and highly selective CB1 antagonist. It was developed by Pfizer for the treatment of obesity, but development for this application has been discontinued following the problems seen during clinical use of the similar drug rimonabant. (source: http://en.wikipedia.org/wiki/Otenabant). |
|
| DC75832 |
Rilpivirine free base |
Rilpivirine is a pharmaceutical drug, developed by Tibotec, for the treatment of HIV infection. It is a second-generation non-nucleoside reverse transcriptase inhibitor (NNRTI) with higher potency, longer half-life and reduced side-effect profile compared with older NNRTIs, such as efavirenz. Rilpivirine entered phase III clinical trials in April 2008, and was approved for use in the United States in May 2011. A fixed-dose drug combining rilpivirine with emtricitabine and tenofovir, was approved by the U.S. Food and Drug Administration in August 2011 under the brand name Complera. |
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| DC75833 |
AGG-523 |
AGG-523 is an aggrecanase specific inhibitor that has been shown to attenuate increases in synovial fluid ARG-aggrecan levels following surgically-induced joint instability in the rat MT model. Pharmacologic inhibition of aggrecanase activity in humans using AGG-523 may be an effective treatment for slowing cartilage degradation following joint injury. |
|
| DC75834 |
Topocecan free base |
Topotecan is a topoisomerase inhibitor. It is a synthetic, water-soluble analog of the natural chemical compound camptothecin. In physiological environments, topotecan is in equilibrium with its inactive carboxylate form. Topotecan's active lactone form intercalates between DNA bases in the topoisomerase-I cleavage complex. The binding of topotecan in the cleavage complex prevents topoisomerase-I from religating the nicked DNA strand after relieving the strain. This intercalation therefore traps the topoisomerase-I in the cleavage complex bound to the DNA. When the replication-fork collides with the trapped topoisomerase-I, DNA damage occurs. This disruption prevents DNA replication and ultimately leads to cell death. |
|
| DC75835 |
SB505124 |
SB505124: SB505124 is a selective inhibitor of transforming growth factor-β type I receptor (ALK5, ALK4 and ALK7) with potential anticancer activity. SB505124 selectively inhibits signaling from TGF-β and activin; does not inhibit other ALK family members. SB-505124 selectively and concentration-dependently inhibits ALK4-, ALK5-, and ALK 7-dependent activation of downstream cytoplasmic signal transducers, Smad2 and Smad3, and of TGF-beta-induced mitogen-activated protein kinase pathway components but does not alter ALK1, ALK2, ALK3 or ALK6-induced Smad signaling. |
|
| DC75836 |
Grazoprevir (MK5172) |
Grazoprevir, also known as MK5172, is a drug approved for the treatment of hepatitis C. It was developed by Merck and completed Phase III trials, following promising results in Phase II when used in combination with the NS5A replication complex inhibitor elbasvir, either with or without ribavirin.Grazoprevir is a second generation hepatitis C virus protease inhibitor acting at the NS3/4a protease targets. It has good activity against a range of HCV genotype variants, including some that are resistant to most currently used antiviral medications. |
|
| DC75837 |
Salinomycin |
Salinomycin is an antibacterial and coccidiostat ionophore agent. Salinomycin suppresses T24 cells by regulating KDM1A and the unfolded protein response pathway. Salinomycin alleviates osteoarthritis progression via inhibiting Wnt/β-catenin signaling. Vitamin D3 and Salinomycin synergy in MCF-7 cells cause cell death via endoplasmic reticulum stress in monolayer and 3D cell culture. Salinomycin induces cell cycle arrest and apoptosis and modulates hepatic cytochrome P450 mRNA expression in HepG2/C3a cells. Salinomycin inhibits proliferation and induces apoptosis of human hepatocellular carcinoma cells in vitro and in vivo, |
|
| DC75838 |
CT-1812 free base |
CT-1812 is a first-in-class, orally available sigma-2/PGRMC1 antagonist (alpha beta oligomer receptor antagonist), is being developed by Cognition. sCT-1812 is a novel therapeutic candidate for Alzheimer's disease. |
|
| DC75839 |
Tenovin-6 HCl |
Tenovin-6, also known as Tnv-6, is a bioactive small molecule SIRT2 inhibitor with anti-neoplastic activity. Inhibition of the Sirtuin class of protein deacetylases with activation of p53 function is associated with the pro-apoptotic effects of Tnv-6 in many tumors. Tnv-6 causes non-genotoxic cytotoxicity, without adversely affecting human clonogenic hematopoietic progenitors in vitro, or murine hematopoiesis. Mechanistically, exposure of CLL cells to Tnv-6 did not induce cellular apoptosis or p53-pathway activity. Transcriptomic profiling identified a gene program influenced by Tnv-6 that included autophagy-lysosomal pathway genes. |
|
| DC75840 |
Exenatide free base |
Exenatide is a medication used to treat diabetes mellitus type 2. Exenatide binds to the intact human Glucagon-like peptide-1 receptor (GLP-1R) in a similar way to the human peptide glucagon-like peptide-1 (GLP-1); exenatide bears a 50% amino acid homology to GLP-1 and it has a longer half-life in vivo. It is used together with diet, exercise, and potentially other antidiabetic medication. It is a less preferred treatment option after metformin and sulfonylureas. |
|
| DC75841 |
Adaprolol maleate |
Adaprolol maleate is a beta-blocker and opthalmic which may be used in the treatment of Glaucoma or other ailments of the eye. Adaprolol has marked electrophysiologic effects. Its major action was on sinus node; it prolonged the basic sinus cycle length and had significant effect on intrinsic automaticity as reflected by the prolonged corrected sinus node recovery time and sinuatrial conduction time. There was, also, direct effect on atrial function and AV nodal function. Adaprolol prolonged the effective refractory period of the His-Purkinje system and the ventricle. The potency of adaprolol's electrophysiologic effects are higher compared to other widely used beta-blockers. Adaprolol appears to be a potent beta-blocker with particularly strong antiarrhythmic effect and it would be very useful in the treatment of both supraventricular and ventricular tachyarrhythmias and ectopic beats. |
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| DC75842 |
Latrepirdine HCl |
Latrepirdine, also known as dimebolin (sold as Dimebon), is an antihistamine drug which has been used clinically in Russia since 1983. Research is continuing in both Russia and western nations into potential applications as a neuroprotective drug to combat Alzheimer's disease and, possibly, as a nootropic as well. However, a Phase III clinical trial for Alzheimer's disease treatment failed to show any benefit. (Source: http://en.wikipedia.org/wiki/Latrepirdine) |
|
| DC75843 |
Olodaterol free base |
Olodaterol, also known as BI 1744, is a long acting beta-adrenoceptor agonist used as an inhalation for treating patients with chronic obstructive pulmonary disease (COPD), manufactured by Boehringer-Ingelheim. Olodaterol was approved by FDA in 2014 for the treatment of chronic obstructive pulmonary disease. |
|
| DC75844 |
MDK-7553 |
MDK-7553, also known as CD38 inhibitor 78c and Compound-78c, is a potent CD38 inhibitor. MDK-7553 has CAS#1700637-55-3, which was reported in J Med Chem. 2015 Apr 23;58(8):3548-71. For the convenience of scientific communication, we name it as MDK-7553. The last four digits of CAS# were used for its name. |
|
| DC75845 |
FIPI free base |
FIPI is a potent and selective phospholipase D inhibitor. FIPI attenuate mercury-induced lipid signaling leading to protection against cytotoxicity in aortic endothelial cells. FIPI rapidly blocks in vivo PA production with subnanomolar potency. FIPI may be a potential therapeutic for autoimmunity and cancer metastasis. |
|
| DC75846 |
Gboxin chloride |
Gboxin chloride is an oxidative phosphorylation inhibitor that targets glioblastoma but not embryonic fibroblasts or neonatal astrocytes. Gboxin rapidly and irreversibly compromises oxygen consumption in glioblastoma cells. Gboxin relies on its positive charge to associate with mitochondrial oxidative phosphorylation complexes in a manner that is dependent on the proton gradient of the inner mitochondrial membrane, and it inhibits the activity of F0F1 ATP synthase. |
|
| DC75847 |
NLX-204 HCl |
NLX-204 is a potent and selective ERK1/2 phosphorylation-preferring serotonin 5 HT1A receptor agonist with pKi = 10.19. NLX-204 displayed high selectivity in the SafetyScreen44 panel (including hERG channel), high solubility, metabolic stability, and Caco-2 penetration and did not block CYP3A4, CYP2D6 isoenzymes, or P-glycoprotein. Preliminary in vivo studies confirmed its promising pharmacokinetic profile. NLX-204 also robustly stimulated ERK1/2 phosphorylation in rat cortex and showed highly potent (MED = 0.16 mg/kg) and efficacious antidepressant-like activity, totally eliminating immobility in the rat Porsolt test. |
|
| DC75848 |
AT-7519 free base |
AT-7519 free base is a drug that acts as a multi-cyclin-dependent kinase inhibitor for Cdk1/cyclin B, Cdk2/Cyclin A, Cdk3/Cyclin E, Cdk4/Cyclin D1, Cdk5/p35, and Cdk6/Cyclin D3. AT7519 is an ATP competitive Cdk inhibitor but is inactive against all non-Cdk kinases with the exception of GSK3β. AT7519 shows potent antiproliferative activity in a variety of human tumor cell lines such as SW620. AT7519 induces activation of GSK-3β by down-regulating GSK-3β phosphorylation, which also contributes to AT7519 induced apoptosis independent of the inhibition of transcription. |
|
| DC75849 |
Chloro-SU5416 |
Chloro-SU5416, also known as Chloro-Semaxanib, is a potent and selective FLT3 inhibitor and RET inhibitor. Chloro-Semaxanib is a derivative of Semaxanib with a chloro atom at 5-position. Chloro-SU5416 has inhibitory activity for FLT3 and selectively induces growth arrest, apoptosis, and cell cycle arrest in Ba/F3 and AML cell lines expressing a constitutively activated FLT3. |
|
| DC75850 |
SKF-38393 HBr |
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. |
|
| DC75851 |
Fatostatin HBr |
Fatostatin, also known as 125B11 or Fatostatin A, is an inhibitor of SREBP activation, preventing SCAP-mediated escort of either SREBP-1 or SREBP-2 to the Golgi (IC50 = 5.6 µM). |
|
| DC75852 |
AZD-8418 |
AZD-8418 is an mGlu2 receptor positive allosteric modulators that attenuates nicotine-taking and nicotine-seeking behavior. Acute treatment with AZD8418 (0.37, 1.12, 3.73, 7.46, and 14.92 mg/kg) and AZD8529 (1.75, 5.83, 17.5, and 58.3 mg/kg) deceased nicotine self-administration and had no effect on food-maintained responding. Chronic treatment with AZD8418 attenuated nicotine self-administration, but tolerance to this effect developed quickly. The inhibition of nicotine self-administration by chronic AZD8529 administration persisted throughout the 14 days of treatment. Chronic treatment with either PAMs inhibited food self-administration. AZD8418 (acute) and AZD8529 (acute and subchronic) blocked cue-induced reinstatement of nicotine- and food-seeking behavior. |
|
| DC75853 |
Ursodiol |
Ursodiol, also known as Ursodeoxycholic acid, is a synthetically-derived form of ursodiol, a bile acid produced by the liver and secreted and stored in the gallbladder. Also produced by the Chinese black bear liver, ursodiol has been used in the treatment of liver disease for centuries. This agent dissolves or prevents cholesterol gallstones by blocking hepatic cholesterol production and decreasing bile cholesterol. Ursodiol also reduces the absorption of cholesterol from the intestinal tract. |
|
| DC75854 |
AZD-1236 |
AZD1236 is a potent and reversible inhibitor of human MMP-9 and MMP-12 (IC50 = 4.5 and 6.1nM, respectively), with >10-fold selectivity to MMP-2 and MMP-13 and >350-fold selectivity to other members of the enzyme family. AZD1236 activity is approximately 20 to 50-fold lower at the rat, mouse, and guinea pig orthologues. In acute models of lung injury, AZD1236 inhibited the haemorrhage and inflammation induced by instillation of human MMP-12 into rat lungs by ~80% at 0.81mg/kg, and also abolished macrophage infiltration into BAL fluid induced by tobacco smoke inhalation in the mouse. |
|
| DC75855 |
Pexidartinib HCl |
Pexidartinib, also known as PLX-3397, is a CSF1R inhibitor with IC50 of 20 nM in development by Plexxikon for the treatment of tenosynovial giant cell tumors. It is in a phase 3 clinical trial for Pigmented Villonodular Synovitis (PVNS) or Giant Cell Tumor of the Tendon Sheath (GCT-TS). Pexidartinib hydrochloride exposure induces developmental toxicity and immunotoxicity in zebrafish embryos via activation of Wnt signaling. |
|
| DC75856 |
Levofloxacin hydrochloride |
Levofloxacin hydrochloride ((-)-Ofloxacin hydrochloride), a synthetic fluoroquinolone antibiotic, is an inhibitor of DNA gyrase and Topoisomerase IV. It exhibits bactericidal effects by preventing bacterial DNA replication. |
|
| DC75857 |
PROTAC tubulin-Degrader-1(compound W13) |
PROTAC tubulin-Degrader-1(compound W13) is an inhibitor of PROTAC tubulin exhibiting antitumor activity against human lung cancer. |
|
| DC75858 |
TH-Z816 |
TH-Z816 is an inhibitor of ,KRAS(G12D) with an IC50 of 14 μM in an SOS-catalyzed nucleotide exchange assay with GDP as the incoming nucleotide. |
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