| DC75635 |
LY303511 |
LY303511, also known as NV-128 and EM 101, is a potent mTOR inhibitor. LY303511 enhances TRAIL sensitivity of SHEP-1 neuroblastoma cells via hydrogen peroxide-mediated mitogen-activated protein kinase activation and up-regulation of death receptors. LY303511 amplifies TRAIL-induced apoptosis in tumor cells by enhancing DR5 oligomerization, DISC assembly, and mitochondrial permeabilization. LY303511 acts via phosphatidylinositol 3-kinase-independent pathways to inhibit cell proliferation via mammalian target of rapamycin (mTOR)- and non-mTOR-dependent mechanisms. |
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| DC75636 |
S-49076 |
S-49076 is a novel, potent inhibitor of MET, AXL/MER, and FGFR1/2/3. A phase I study with S-49076 is currently underway in patients with advanced solid tumors. |
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| DC75637 |
ORY1001 HCl |
ORY1001, also known as RG-6016, is KDM1A inhibitor (IC50 <20nM) with high selectivity against related FAD dependent aminoxidases (MAO-A/B, IL4I1, KDM1B >100uM, SMOX 7uM). ORY-1001 does not inhibit non-related histone modifiers. Treatment of THP-1 (MLL-AF9) cells with ORY-1001, results in a time/dose dependent me2H3K4 accumulation at KDM1A target genes and concomitant induction of differentiation markers (EC50 me2H3K4 and FACS CD11b <1nM). ORY-1001 induces apoptosis in THP-1 and inhibits proliferation and colony formation of MV(4;11) (MLL-AF4) cells (EC50 <1nM). |
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| DC75638 |
Exametazime |
Exametazime is a Diagnostic Aid (Regional Cerebral Perfusion Imaging). It is a radiopharmaceutical sold under the trade name Ceretec, and is used by nuclear medicine physicians for the detection of altered regional cerebral perfusion in stroke and other cerebrovascular diseases. |
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| DC75639 |
AZD-2207 |
AZD-2207 is a cannabinoid receptor CB1 antagonist and highly lipophilic compound for the treatment of type 2 diabetes mellitus and obesity. |
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| DC75640 |
Lascufloxacin |
Lascufloxacin, also known as KRP-AM-1977, is a potent antibacterial drug candidate. Lascufloxacin showed a broad spectrum of activity against various clinical isolates. Especially, lascufloxacin showed the most potent activity against gram-positive bacteria among the quinolones tested. Furthermore, lascufloxacin showed incomplete cross-resistance against existing quinolone-resistant strains. Enzymatic analysis indicated that lascufloxacin showed potent inhibitory activity against both wild-type and mutated target enzymes. Lascufloxacin may be useful in treating infections caused by various pathogens, including quinolone-resistant strains. |
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| DC75641 |
GENZ-644282 TFA salt |
Genz-644282, also known as SAR402674, is a non-camptothecin inhibitor of topoisomerase I with potential antineoplastic activity. Topoisomerase I inhibitor Genz-644282 binds to and inhibits the enzyme topoisomerase I, which may result in the inhibition of repair of single-strand DNA breaks, DNA replication, and tumor cell growth in susceptible tumor cell populations. |
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| DC75642 |
BD-AcAc2 |
BD-AcAc2 is a ketone ester with anti-obesity and anticonvulsant activities. Oral administration of BD-AcAc2 reduces body weight, food intake, and whole animal adiposity in mice fed an isocaloric diet. BD-AcAc2 increases the seizure threshold and blood levels of β-hydroxybutyrate in a rat model of seizures induced by pentylenetetrazole. |
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| DC75643 |
Theliatinib free base |
Theliatinib, also known as xiliertinib and HMPL-309, is a novel small molecule, epidermal growth factor receptor tyrosine kinase inhibitor with potential antineoplastic and anti-angiogenesis activities. In vitro studies suggest that Theliatinib is a potent EGFR kinase inhibitor with good kinase selectivity and in vivo data demonstrated broad spectrum anti-tumor activity via oral dosing in multiple xerographs such as A-431, Bcap-37 and Fadu. |
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| DC75644 |
RO5263397 HCl |
RO5263397 is a selective TAAR 1 agonist. RO5263397 was efficacious in reducing cocaine-mediated behaviors. RO5263397 dose-dependently prevented cocaine-induced lowering of ICSS thresholds. TAAR1 stimulation effectively suppresses the rewarding and reinforcing effects of cocaine in self-administration and ICSS models, supporting the candidacy of TAAR1 as a drug discovery target for cocaine addiction. |
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| DC75645 |
RO5256390 free base |
RO5256390 is a TAAR1 agonist. RO5256390 blocks psychostimulant-induced hyperactivity and produces a brain activation pattern reminiscent of the antipsychotic drug olanzapine, suggesting antipsychotic-like properties. TAAR1 activation promotes vigilance in rats and shows pro-cognitive and antidepressant-like properties in rodent and primate models. TAAR1 agonists may provide a novel and differentiated treatment of schizophrenia as compared with current medication standards: TAAR1 agonists may improve not only the positive symptoms but also the negative symptoms and cognitive deficits, without causing adverse effects such as motor impairments or weight gain. |
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| DC75646 |
ICN37805 |
ICN37805 is an important intermediate to synthesize antiviral drug remdesivir. 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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| DC75647 |
ACHP free base |
ACHP is an IκB kinase inhibitor that inhibits DNA binding activity of NF-κB, blocks NF-κB pathway in multiple myeloma cell lines, and induces cell growth arrest and apoptosis. It also inhibits STAT3 signaling in NSCLC in vitro. |
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| DC75648 |
(R)-GABOB |
(R)-4-Amino-3-hydroxybutyric acid, also known as (R)-GABOB, is a GABA receptor modulator. It binds to GABAA and GABAB receptors and inhibits GABA uptake in rat brain synaptosomes. (R)-4-amino-3-hydroxybutyric acid is also a GABAC receptor agonist that induces currents in a patch-clamp assay using Xenopus oocytes expressing the human receptor. In vivo, (R)-4-amino-3-hydroxybutyric acid inhibits electrical discharges in the amygdala in a cat model of N-amidinobenzamide-induced seizures. |
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| DC75649 |
Ampicillin |
Ampicillin is an antibiotic used to prevent and treat a number of bacterial infections. This includes respiratory tract infections, urinary tract infections, meningitis, salmonella infections, and endocarditis. It may also be used to prevent group B streptococcal infection in newborns. It is used by mouth, by injection into a muscle, or intravenously. It is not useful for the treatment of viral infections. Ampicillin was developed in 1961. It is on the World Health Organization's List of Essential Medicines, the most important medication needed in a basic health system.||Ampicillin is in the penicillin group of beta-lactam antibiotics and is part of the aminopenicillin family. It is roughly equivalent to amoxicillin in terms of activity. Ampicillin is able to penetrate Gram-positive and some Gram-negative bacteria. It differs from penicillin G, or benzylpenicillin, only by the presence of an amino group. That amino group helps the drug penetrate the outer membrane of Gram-negative bacteria. Ampicillin acts as an irreversible inhibitor of the enzyme transpeptidase, which is needed by bacteria to make their cell walls. It inhibits the third and final stage of bacterial cell wall synthesis in binary fission, which ultimately leads to cell lysis; therefore ampicillin is usually bacteriocidal. |
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| DC75650 |
GSK256066 free base |
GSK256066 is a potent and selective PDE4 inhibitor that can be given by inhalation, minimising the potential for side effects. GSK256066 demonstrated a protective effect on the EAR and LAR. GSK256066 is a slow and tight binding inhibitor of PDE4B (apparent IC(50) 3.2 pM; steady-state IC(50) <0.5 pM), which is more potent than any previously documented compound, for example, roflumilast (IC(50) 390 pM), tofimilast (IC(50) 1.6 nM), and cilomilast (IC(50) 74 nM). Consistent with this, GSK256066 inhibited tumor necrosis factor α production by lipopolysaccharide (LPS)-stimulated human peripheral blood monocytes with 0.01 nM IC(50). GSK256066 has been demonstrated to have exceptional potency in vitro and in vivo and is being clinically investigated as a treatment for chronic obstructive pulmonary disease. |
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| DC75651 |
Azilsartan free acid |
Azilsartan is an angiotensin II receptor antagonist used in the treatment of hypertension, developed by Takeda. It is marketed in tablet form under the trade name Edarbi as the prodrug azilsartan medoxomil (INN, codenamed TAK-491). Azilsartan medoxomil lowers blood pressure by blocking the action of angiotensin II, a vasopressor hormone. |
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| DC75652 |
MA-VAL-ALA-PAB-OH |
MA-VAL-ALA-PAB-OH is a usefully ACD-linker, which was reported in JACS 2020, 142, pp12890-12895. |
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| DC75653 |
BXT-51072 |
BXT 51072, also known as ALT-2074, belongs to a class of drugs called "glutathione peroxidase mimics." BXT-51072 works by imitating a substance produced in various tissues in the body, which prevents damage of the heart and blood vessels. The intraocular injection of BXT-51072 protected axotomized neurons at doses in a narrow (tenfold) range. It also reduced the deleterious effects of intraocular tert-butyl hydroperoxide, an inducer of lipid peroxidation, and diminished the excitotoxic degeneration induced by N-methyl-D-aspartate. However, BXT-51072 did not noticeably reduce naturally occurring cell death. |
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| DC75654 |
Ripretinib free base |
Ripretinib, also known as DCC-2618, is a potent, orally active and selective KIT/PDGFR inhibitor with potential antineoplastic activity. DCC-2618 targets and binds to both wild-type and mutant forms of KIT and PDGFRa specifically at their switch pocket binding sites, thereby preventing the switch from inactive to active conformations of these kinases and inactivating their wild-type and mutant forms. In May 2020, FDA Approves Qinlock (ripretinib) for the Treatment of Fourth-Line Gastrointestinal Stromal Tumor |
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| DC75655 |
Befiperide HCl |
Befiperide, also known as DU-29325, is a substituted piperazine that has agonist activity at serotonin1 receptors. |
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| DC75656 |
Revumenib |
Revumenib, also known as SNDX-5613, is a potent and specific Menin-MLL inhibitor. It can be used for the research of MLL-rearranged (MLL-r) acute leukemias, including acute lymphoblastic leukemia (ALL) and acute myeloid leukemia (AML). |
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| DC75657 |
Quetiapine |
Quetiapine, marketed as Seroquel, is an atypical antipsychotic approved for the treatment of schizophrenia, bipolar disorder, and along with an antidepressant to treat major depressive disorder. It is also sometimes used as a sleep aid because of its sedating effect but this use is not recommended. Quetiapine is a dopamine, serotonin, and adrenergic antagonist, and a potent antihistamine with clinically negligible anticholinergic properties. Quetiapine binds strongly to serotonin receptors; the drug acts as partial agonist at 5-HT1A receptors. |
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| DC75658 |
Artilide fumarate |
Artilide, also known as U88943 or U88943E, is a drug used for the treatment of cardiac arrhythmias. Artilide is a class III antiarrhythmic which is structurally-related to ibutilide and d,l-sotalol. Artilide had demonstrated inducibe ventricular arrhythmias prior to treatment. This antiarrhythmic action was associated with significant increases in ventricular refractoriness and monophasic action potential duration. Lower doses of artilide tended to reduce the incidence of spontaneous ventricular arrhythmias but these effects were not significant. These results are consistent with the concept that spontaneous and pacing induced ventricular arrhythmias result from different mechanisms, and that class III anti-arrhythmic agents are more effective in suppressing induced ventricular tachycardia due to reentry than spontaneous arrhythmias which result from nonreentrant mechanisms. |
|
| DC75659 |
NAD free acid |
NAD is a dinucleotide of adenine and nicotinamide. It has coenzyme activity in redox reactions and also acts as a donor of ADP-ribose moieties. |
|
| DC75660 |
Varenicline HCl |
Varenicline is a nicotinic receptor partial agonist—it stimulates nicotine receptors more weakly than nicotine itself does. In this respect it is similar to cytisine and different from the nicotinic antagonist, bupropion, and nicotine replacement therapies (NRTs) like nicotine patches and nicotine gum. Varenicline displays full agonism on α7 nicotinic acetylcholine receptors and is a partial agonist on the α4β2, α3β4, and α6β2 subtypes. In addition, it is a weak agonist on the α3β2 containing receptors. Varenicline's partial agonism on the α4β2 receptors rather than nicotine's full agonism produces less effect of dopamine release than nicotine's. This α4β2 competitive binding reduces the ability of nicotine to bind and stimulate the mesolimbic dopamine system—similar to the method of action of buprenorphine in the treatment of opioid addiction. |
|
| DC75661 |
Trilaciclib HCl |
Trilaciclib is a potential first-in-class short-acting CDK4/6 inhibitor in development to preserve hematopoietic stem cells and enhance immune system function during chemotherapy. Trilaciclib may help protect bone marrow cells from damage caused by chemotherapy by inhibiting cyclin-dependent kinase 4/6, a type of enzyme. Trilaciclib is the first therapy in its class and was approved for medical use in the United States in February 2021. |
|
| DC75662 |
YCN47284 |
YCN47284 is an aromatic guanylhydrazone compounds with antimalarial activity. YCN47284 was first reported in WO 9621450. YCN47284 inhibited P. falciparum growth with IC50 = 0.075 μM to >10 μM as reported in US 20030186993. 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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| DC75663 |
BMS-1001 free base |
BMS-1001 is a potent PD-1/PD-L1 interaction inhibitor. BMS-1001 alleviates the inhibitory effect of the soluble PD-L1 on the T-cell receptor-mediated activation of T-lymphocytes. BMS-1001 is capable of alleviating the PD-1/PD-L1 immune checkpoint-mediated exhaustion of Jurkat T-lymphocytes. |
|
| DC75664 |
Neomycin B sulfate |
Neomycin is an aminoglycoside antibiotic found in many topical medications such as creams, ointments, and eyedrops. Neomycin belongs to aminoglycoside class of antibiotics that contain two or more aminosugars connected by glycosidic bonds. Similar to other aminoglycosides, neomycin has excellent activity against Gram-negative bacteria, and has partial activity against Gram-positive bacteria. It is relatively toxic to humans, and many people have allergic reactions to it. Aminoglycosides such as neomycin are known for their ability to bind to duplex RNA with high affinity. |
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