| DC75624 |
Selinexor free base |
Selinexor, also known as KPT-330, is an orally bioavailable, potent and selective XPO1/CRM1 Inhibitor. Selinexor is effective in acquired resistance to ibrutinib and synergizes with ibrutinib in chronic lymphocytic leukemia. Selinexor potentiates the antitumor activity of gemcitabine in human pancreatic cancer through inhibition of tumor growth, depletion of the antiapoptotic proteins, and induction of apoptosis. Selinexor has strong activity against primary AML cells while sparing normal stem and progenitor cells. |
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| DC75625 |
Cetirizine Hydrochloride |
Cetirizine hydrochloride is a potent second-generation histamine H1 antagonist that is effective in the treatment of allergic rhinitis, chronic urticaria, and pollen-induced asthma. Cetirizine hydrochloride is a carboxylated metabolite of hydroxyzine that acts as a selective Histamine H1 receptor inverse agonist. Compared to its parent compound, it shows similar antihistaminic activity, but with greater H1 selectivity and less sedative effects. |
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| DC75626 |
Amlodipine |
Amlodipine (as besylate, mesylate or maleate) is a medication used to lower blood pressure and prevent chest pain. It belongs to a group of medications known as dihydropyridine-type calcium channel blockers. By widening of blood vessels it lowers blood pressure. In angina, amlodipine increases blood flow to the heart muscle to relieve pain due to angina. |
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| DC75627 |
LDN-192960 free base |
LDN-192960 is an inhibitor of Haspin and Dual-specificity Tyrosine-regulated Kinase 2 (DYRK2) |
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| DC75628 |
DFN75624 |
DFN75624 is a dengue viral replication inhibitor. DFN75624 was first reported in patent WO 2018215315 (Janssen Pharmaceuticals). 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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| DC75629 |
ANT3310 sodium |
ANT3310 is a Novel Broad-Spectrum Serine β‑Lactamase Inhibitor of the Diazabicyclooctane Class, Which Strongly Potentiates Meropenem Activity against Carbapenem-Resistant Enterobacterales and Acinetobacter baumannii. |
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| DC75631 |
Dinoprostone |
Dinoprostone, also known as PGE2, Prostaglandin E₂, is a product of arachidonic acid metabolism that binds to EP1, EP2, EP3, & EP4 receptors with high affinity (Kd = 1-10 nM). Involved in vasodilator actions of kinins |
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| DC75632 |
Cefiderocol free base |
Cefiderocol (free base), also known as S-649266, is a potent siderophore cephalosporin antibiotic with a catechol moiety on the 3-position side chain. S-649266 shows potent in vitro activity against the non-fermenting Gram-negative bacteria Acinetobacter baumannii, Pseudomonas aeruginosa and Stenotrophomonas maltophilia, including MDR strains such as carbapenem-resistant A. baumannii and metallo-β-lactamase-producing P. aeruginosa. S-649266 showed potent in vitro activities against A. baumannii producing carbapenemases such as OXA-type β-lactamases, and P. aeruginosa producing metallo-β-lactamases such as IMP type and VIM type. FDA approved this drug in 11/14/2019 To treat patients with complicated urinary tract infections who have limited or no alternative treatment options |
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| DC75633 |
AZD1446 tosylate |
AZD1446, also known as TC-6683, is a novel highly selective α4β2 nicotinic acetylcholine receptor agonist for the treatment of cognitive disorders. AZD1446 showed favorable pharmaceutical properties and in vivo efficacy in animal models has been identified as a potential treatment for cognitive deficits associated with psychiatric or neurological conditions and had been evaluated in phase 2 clinical trials as a treatment for Alzheimer's disease. |
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| DC75634 |
SR-717 lithium |
SR-717 is an agonist of stimulator of interferon genes STING for treating cancer. SR-717 demonstrates broad interspecies and interallelic specificity. SR-717 functions as a direct cyclic guanosine monophosphate-adenosine monophosphate (cGAMP) mimetic that induces the same "closed" conformation of STING. SR-717 displayed antitumor activity; promoted the activation of CD8+ T, natural killer, and dendritic cells in relevant tissues; and facilitated antigen cross-priming. SR-717 also induced the expression of clinically relevant targets, including programmed cell death 1 ligand 1 (PD-L1), in a STING-dependent manner. |
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| 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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