5,7-Dichlorokynurenic acid (5,7-DCKA) is a selective and competitive antagonist of the glycine site on NMDA receptor with a KB of 65 nM. 5,7-Dichlorokynurenic acid, a derivative of kynurenic acid, reduced NMDA-induced neuron injury in rat cortical cell cultures[1].
1-Methylimidazole-d3-1 is the deuterium labeled 1-Methylimidazole[1].
Tuberculatin is a lignin. Tuberculatin can be isolated from Justicia ciliata[1].
TPMPA, a hybrid of isoguvacine and 3-APMPA, is the first selective antagonist for a GABAC receptor (KB = 2.1 μM), but not to interact with GABAA (KB = 320 μM) or GABAB receptors (EC50 = 500 μM). TPMPA has the potential for the research of suppressing orientation selectivity in ganglion cells[1][2][3].
SRT 2104 is a brain-permeable activator of SIRT1, used for the research of type 2 diabetes mellitus and Huntington's disease.
N-Boc-O-allyl-L-serine is a derivative of L-serine, can be used for compounds synthesis[1].
(R)-Elexacaftor is an enantiomer of Elexacaftor (HY-111772). (R)-Elexacaftor is the Compound 37 from patent WO2018107100A1. (R)-Elexacaftor is a modulator of cystic fibrosis transmembrane conductance regulator (CFTR), the EC50 for CFTR dF508 is 0.29 uM[1].
Androgen receptor-IN-2 is a potent and orally active Androgen Receptor inhibitor. Androgen receptor-IN-2 has antitumor activity against prostate cancer[1].
Febuxostat impurity 7 is an impurity of Febuxostat. Febuxostat is selective xanthine oxidase inhibitor with a Ki of 0.6 nM[1].
Robenacoxib is a nonsteroidal anti-inflammatory and analgesic agent. Robenacoxib is a selective COX-2 inhibitor[1][2].
ZL006 is a potent inhibitor of nNOS/PSD-95 interaction, and inhibits NMDA receptor-mediated NO synthesis.
5,4'-Dihydroxy-7-methoxy-6-methylflavane (compound 15) is a natural product that can be found in Chinese Dragon’s Blood[1].
Picolinafen-d4 (4-fluorophenyl-d4) is the deuterium labeled Picolinafen[1].
(+)-Peusedanol is a coumarin isolated from Peucedanumjaponicum[1].
Dimenhydrinate is an anti-emetic and anti-histamine commonly available over-the-counter as a motion sickness remedy.
Amdizalisib is a PI3K inhibitor and used for the research of inflammatory disease, autoimmune disease or cancer[1].
9-(3-Deoxy-3-fluoro-β-D-ribofuranosyl)-6-[5-(propyn-1-yl)pyridin-3-yl]purine is a purine nucleoside analog. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].
Trabikibart (CSL311), a βc-specific, fully human monoclonal antibody, binds to a unique epitope that is specific to the cytokine-binding site of the human βc receptor. Trabikibart has picomolar binding affinity for the human βc receptor. Trabikibart is a potent inhibitor of the combined effects of IL-3, GM-CSF and IL-5 on the survival of eosinophils. Trabikibart has the potential for chronic inflammatory diseases research[1].
NSC-670224 is an inhibitor of histone deacetylases-6 (HDAC6) and nuclear factor-κB (NF-κB) activation blocker. It has been shown to be toxic to Saccharomyces cerevisiae at low micromolar concentrations, potentially acts via a mechanism of action related to that of tamoxifen.
Dirithromycin(LY 237216) is a macrolide glycopeptide antibiotic by binding to the 50S subunit of the 70S bacterial ribosome to inhibit the translocation of peptides.Target: AntibacterialDirithromycin is a new macrolide with a spectrum and degree of in vitro antimicrobial activity similar to that of erythromycin. Compared with erythromycin, dirithromycin has a long elimination half-life enabling once-daily administration, and it also achieves a greater cellular:extracellular concentration ratio and higher concentration in some tissues. Multicentre double-blind clinical trials have shown dirithromycin to be similar in efficacy to erythromycin in the treatment of uncomplicated bacterial infections of the respiratory tract and of skin and soft tissues [1]. Dirithromycin offers some attractive pharmacokinetic properties. The long elimination half-life of dirithromycin allows once-daily dosing and higher and more prolonged tissue concentrations than are achievable with erythromycin. The spectrum of activity, adverse effect profile, clinical efficacy, and bacteriologic eradication rate of dirithromycin may be similar to those of erythromycin [2, 3].
STAT3-IN-23 (PY*LKTK) is a potent STAT3 inhibitor[1].
RBN-2397 is a potent, accross species and orally active NAD+ competitive inhibitor of PARP7 (IC50<3 nM). RBN-2397 selectively binds to PARP7 (Kd=0.001 μM) and restores interferon (Type I) signaling. RBN-2397 has the potential for the study of advanced or metastatic solid tumors[1][2].
Notopterol is a coumarin extracted from N. incisum. Notopterol induces apoptosis and has antipyretic, analgesic and anti-inflammatory effects. Notopterol is used for acute myeloid leukemia (AML)[1].
Methyl 1,2,3,4-tetrahydro-2,4-dioxo-1-β-D-ribofuranosyl-5-pyrimidineacetate is a purine nucleoside analogue. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].
Itopride hydrochloride is an AChE inhibitor (acetylcholinesterase) and D2DR inhibitor.Target: AChEItopride is a gastroprokinetic benzamide derivative. The IC50 of itopride with AChE (2.04 +/- 0.27 microM) was, however, 100-fold less than that with BuChE, whereas in the case of neostigmine with AChE (11.3 +/- 3.4 nM), it was 10-fold less. The inhibitory effect of itopride on cholinesterase (ChE) activity in guinea pig gastrointestine was much weaker than that on pure AChE. the IC50s of itopride against ChE activities were found to be about 0.5 microM. The IC50 of itopride for electric eel and guinea pig gastrointestinal AChE inhibition was 200 times and 50 times as large as that of neostigmine, respectively [1].
N-[(9H-Fluoren-9-ylmethoxy)carbonyl]-5-methyl-L-norleucine is a leucine derivative[1].
Charantadiol A is a natural compound found in Momordica charantia L[1].
NH-bis(m-PEG4) is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Filibuvir is a potent, selective non-nucleoside inhibitor (NNI) of the HCV nonstructural 5B protein (NS5B) RNA-dependent RNA polymerase, and it binds noncovalently in the “Thumb 2” pocket of NS5B. In vitro, filibuvir is equipotent against genotype 1a and 1b replicons, with an EC50 of 59 nM[1].
((Allyloxy)carbonyl)-L-phenylalanine is a phenylalanine derivative[1].