| DC75470 |
Desvenlafaxine Succinate hydrate |
Desvenlafaxine Succinate is a venlafaxine metabolite and inhibitor of SERT and NET used to treat depression. It also alters rates of gastric emptying and decreases symptoms of menopausal hot flashes. |
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| DC75471 |
Norepinephrine bitartrate hydrate |
Norepinephrine is an organic chemical in the catecholamine family that functions in the human brain and body as a hormone and neurotransmitter. Norepinephrine directly stimulates adrenergic receptors. Stimulation of alpha-adrenergic receptors causes vasoconstriction of the radial smooth muscle of the iris, arteries, arterioles, veins, urinary bladder, and the sphincter of the gastrointestinal tract. Stimulation of beta-1 adrenergic receptors causes an increase in myocardial contractility, heart rate, automaticity, and atrioventricular (AV) conduction while stimulation of beta-2 adrenergic receptors causes bronchiolar and vascular smooth muscle dilatation. |
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| DC75472 |
Indinavir sulfate |
Indinavir sulfate is an inhibitor of HIV protease, GLUT4, and calpain used to treat HIV infection. It also decreases phosphorylation of the insulin receptor β subunit, inhibits adenocarcinoma tumor growth, and may induce SOCS1 signaling. |
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| DC75473 |
R-IMPP |
R-IMPP is an inhibitor of PCSK9 translation. R-IMPP stimulates uptake of LDL-C in hepatoma cells by increasing LDL-R levels, without altering levels of secreted transferrin. |
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| DC75474 |
Necrosulfonamide |
Necrosulfonamide is a novel inhibitor of MLKL (mixed lineage kinase domain-like). Necrosulfonamide is a cell-permeable inhibitor that covalently modifies Cys88 and blocks human MLKL adaptor function. Necrosulfonamide Attenuates Spinal Cord Injury via Necroptosis Inhibition. |
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| DC75475 |
Saccharin 1-methylimidazole |
Saccharin 1-methylimidazole, also known as SMI, is a chemical activator commonly used in solid-phase synthesis of DNA and RNA oligonucleotides. Saccharin 1-methylimidazole has been used to synthesize single-stranded DNA oligonucleotides that are resistant to nuclease digestion. |
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| DC75476 |
Batimastat |
Batimastat (also known as BB-94) is a synthetic matrix metalloproteinase inhibitor that has shown antineoplastic and antiangiogenic activity in various tumor models. Matrix metalloproteinases (MMPs) are thought to play a significant role in tumor invasion and metastasis as well as angiogenesis. Batimastat, also known as BB-94, acts as an inhibitor of metalloproteinase activity by binding the zinc ion in the active site of MMPs. |
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| DC75477 |
Nintedanib |
Nintedanib, also known as BIBF 1120, is an orally bioavailable inhibitor of vascular endothelial growth factor receptor (VEGFR), fibroblast growth factor receptor (FGFR) and platelet derived growth factor receptor (PDGFR). Intedanib selectively binds to and inhibits vascular endothelial growth factor receptor (VEGFR), fibroblast growth factor receptor (FGFR) and platelet-derived growth factor receptor (PDGFR) tyrosine kinases, which may result in the induction of endothelial cell apoptosis; a reduction in tumor vasculature; and the inhibition of tumor cell proliferation and migration. On 11/15/2014 , FDA approved Nintedanib for the treatment of idiopathic pulmonary fibrosis (IPF). |
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| DC75478 |
Alectinib free base |
Alectinib, also known as AF802, or CH5424802 or RO5424802, is a potent, selective, and orally available ALK inhibitor with a unique chemical scaffold, showing preferential antitumor activity against cancers with gene alterations of ALK, such as nonsmall cell lung cancer (NSCLC) cells expressing EML4-ALK fusion and anaplastic large-cell lymphoma (ALCL) cells expressing NPM-ALK fusion in vitro and in vivo. CH5424802 inhibited ALK L1196M, which corresponds to the gatekeeper mutation conferring common resistance to kinase inhibitors, and blocked EML4-ALK L1196M-driven cell growth. Alectinib was approved in Dec. 2015. |
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| DC75479 |
Daunorubicin hydrochloride |
Daunorubicin hydrochloride is the hydrochloride salt of an anthracycline antineoplastic antibiotic with therapeutic effects similar to those of doxorubicin. Daunorubicin exhibits cytotoxic activity through topoisomerase-mediated interaction with DNA, thereby inhibiting DNA replication and repair and RNA and protein synthesis. |
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| DC75480 |
Amodiaquin HCl hydrate |
Amodiaquin dihydrochloride is an inhibitor of the Ebola virus. It acts by targeting the viral protein 35 (VP35). |
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| DC75481 |
Vidofludimus |
Vidofludimus, also known as 4SC 101 or SC12267, is a novel orally active and potent DHODH inhibitor. In vitro, 4SC-101 is a potent inhibitor of human DHODH, inhibits lymphocyte proliferation, and uniquely blocks phytohemagglutinin-stimulated IL-17 production by lymphocytes. In vivo, oral administration of 4SC-101 effectively improved both chronic DSS and acute TNBS colitis in mice. 4SC-101 may have potential for the treatment of intestinal inflammation. Dihydroorotate dehydrogenase (DHODH) is a key enzyme involved in pyrimidine biosynthesis. DHODH is a known target for the treatment of autoimmune diseases. |
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| DC75482 |
LYS01 free base |
LYS01 free base is a new lysosomal autophagy inhibitor. Lys01 has single-agent antitumor activity and reproduces the phenotype of a genetic autophagy deficiency. The trihydydrochloride salt of LYS01 is called LYS05. Lys05, a water-soluble salt of Lys01, more potently accumulates within and deacidifies the lysosome, resulting in impaired autophagy and tumor growth. |
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| DC75483 |
S14506 HCl |
S 14506 is a highly potent selective 5-HT1A receptor full agonist (pKi values are 9.0, 6.6, 7.5, 6.6 and < 6.0 for 5-HT1A, 5-HT1B, 5-HT1C, 5-HT2 and 5-HT3 receptors respectively). It potentially binds between the agonist binding site and the G protein interaction switch site, affecting the activation mechanism, and may display positive cooperativity. |
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| DC75484 |
Desmethyl-VS-5584 |
Desmethyl-VS-5584 is a demethyl analogue of VS-5584, which is a novel and highly selective PI3K/mTOR kinase inhibitor for the treatment of cancer. |
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| DC75485 |
RX821002 HCl |
RX821002 is a potent, selective α2-adrenoceptor antagonist with very low affinity for imidazoline sites. RX821002 displays selectivity for the α2D over the α2A subtypes (pKd values are 9.7 and 8.2 respectively). |
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| DC75486 |
Importazole free base |
Importazole is a small molecule inhibitor of the transport receptor importin-β. Importazole specifically inhibits the function of importin-β, likely by altering its interaction with RanGTP. Importazole is a valuable tool to evaluate the function of the importin-β/RanGTP pathway at specific stages during the cell cycle. |
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| DC75487 |
GDC0575 monohydrochloride |
GDC-0575, also known as ARRY-575 and RG7741, is a potent and selective inhibitor of cell cycle checkpoint kinase 1 (Chk1) with an IC50 of 1.2 nM. Chk1 inhibitor GDC-0575 specifically binds to and inhibits Chk1; this may result in tumor cells bypassing Chk1-dependent cell cycle arrest in the S and G2/M phases, which permits the cells to undergo DNA repair prior to entry into mitosis. |
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| DC75488 |
RS 67333 HCl |
RS 67333 is a potent and highly selective 5-HT4 partial agonist, with pKi values of 8.7 at 5-HT4 sites in guinea pig striatum and > 6 at various other receptors, including 5-HT1A, 1D, 2A, 2C, D1, D2 and M1-3. RS 67333 HCl is active in vivo, with an intrinsic activity relative to 5-HT of 0.5. |
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| DC75489 |
NLX-101 |
NLX-101, also known as F-15,599, is a novel compound that activates serotonin 5-HT1A receptors with exceptional selectivity, having over 1000-fold higher affinity for this target over other receptors. In addition, NLX-101 is a 'biased agonist' at 5-HT1A receptors, preferentially activating 5-HT1A receptors in those brain regions that control mood and cognition. |
|
| DC75490 |
NKY80 |
NKY80 is a inhibitor of adenylyl cyclase (AC). NKY80 exhibits greater affinity for AC5 over AC3 and AC2 (IC50 values are 8.3 μM, 132 μM and 1.7 mM respectively). |
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| DC75491 |
RS 100329 HCl |
RS 100329 is a subtype-selective α1A-adrenoceptor antagonist (pKi = 9.6 for human cloned α1A receptors). RS 100329 displays 126- and 50-fold selectivity over human α1B and α1D receptors respectively. |
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| DC75492 |
Rimonabant free base |
Rimonabant, also known as SR141716 and A 281, is an anorectic anti-obesity drug. It is an inverse agonist for the cannabinoid receptor CB1. Its main avenue of effect is reduction in appetite. Rimonabant is the first selective CB1 receptor blocker to be approved for use anywhere in the world. Rimonabant is approved in 38 countries including the E.U., Mexico, and Brazil. It was rejected for approval for use in the United States. |
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| DC75493 |
E4031 HCl |
E4031 selectively blocks hERG K+ channels. E4031 inhibits the rapid delayed-rectifier K+ current (IKr) and reversibly prolongs action potential duration in guinea pig papillary muscle and isolated ventricular myocytes, without affecting Na+ or Ca2+ inward currents. E4031 is a class III antiarrhythmic agent. |
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| DC75494 |
SKF89976A free base |
SKF89976A is a potent GABA uptake inhibitor, which is selective for GAT-1 (IC50 values are 0.13, 550, 944 and 7210 μM for hGAT-1, rGAT-2, hGAT-3 and hBGT-1 respectively). SKF89976A inhibits transport current competitively (Ki = 7 μM) and transmitter-gated current non-competitively (Ki = 0.03 nM). It is able to pass the blood-brain barrier after systemic administration and is active in vivo. |
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| DC75495 |
Olodaterol HCl |
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. |
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| DC75496 |
Imatinib free base |
Imatinib is a tyrosine kinase inhibitor with antineoplastic activity. Imatinib binds to an intracellular pocket located within tyrosine kinases (TK), thereby inhibiting ATP binding and preventing phosphorylation and the subsequent activation of growth receptors and their downstream signal transduction pathways. This agent inhibits TK encoded by the bcr-abl oncogene as well as receptor TKs encoded by the c-kit and platelet-derived growth factor receptor (PDGFR) oncogenes. Imatinib was approved for medical use in the United States in 2001. |
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| DC75497 |
SB-258585 HCl |
SB-258585 HCl is a potent, selective antagonist of the serotonin 5-HT6 receptor (pKi = 8.53). It displays over 100-fold selectivity for 5-HT6 over other 5-HT, dopamine, and α-adrenergic receptors. |
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| DC75498 |
Tenapanor free base |
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. Tenapanor is currently in clinical trials. |
|
| DC75499 |
Nilotinib free base |
Nilotinib, also known as AMN107, is a small-molecule tyrosine kinase inhibitor approved for the treatment of imatinib-resistant chronic myelogenous leukemia. Structurally related to imatinib, it was developed based on the structure of the Abl-imatinib complex to address imatinib intolerance and resistance. Nilotinib is a selective Bcr-Abl kinase inhibitor that is 10-30 fold more potent than imatinib in inhibiting Bcr-Abl tyrosine kinase activity and proliferation of Bcr-Abl expressing cells. Nolitinib was developed by Novartis and is sold under the trade name Tasigna. |
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