Eticlopride hydrochloride, a selective dopamine D2‐like receptor antagonist, exhibits high affinity for dopamine D2, α1‐adrenergic, α2‐adrenergic, 5HT1, 5HT2 receptors with Kis of 0.09, 112, 699, 6220, and 830 nM, respectively. Antipsychotic agent[1].
N-(2-Hydroxyethyl)valine-d4 is the deuterium labeled N-(2-Hydroxyethyl)valine[1].
Limocitrin is a natural product that can be isolated from the buds of P. acerifolia and P. orientalis. Limocitrin suppresses estradiol-dependent proliferation of MCF7 cells weakly but estradiol-induced AlkP (alkaline phosphatase) expression only marginally[1].
LG-100064 is a retinoid-X-receptor (RXR) agonist, with EC50s of 330 nM, 200 nM, and 260 nM for RXRα, RXRβ and RXRγ; LG-100064 can be used in the research of cancer.
AR-M1896 is a GalR2 selective agonist with a binding IC50 of 1.76 nM for rat GalR2. AR-M1896 can be used for the research of acute myocardial infarction and neuropathic pain[1][2].
Fomepizole (4-Methylpyrazole) hydrochloride is a potent cytochrome P450 (CYP2E1) inhibitor. Fomepizole hydrochloride is a competitive inhibitor of the enzyme alcohol dehydrogenase. Fomepizole hydrochloride blocks further conversion of methanol and ethylene glycol to toxic metabolites. Fomepizole hydrochloride has the potential for an antidote for ethylene glycol or methanol poisoning[1][2][3].
Nomifensine maleate is a selective inhibitor of dopamine uptake, used in adult attention deficit disorder.
VU0364289 is a highly selective mGlu5 positive allosteric modulator (PAM) (binds to the MPEP (HY-14609A) site), with an EC50 of 1.6 µM. VU0364289 can reverse amphetamine-induced hyperlocomotion in a dose-dependent manner, which can be used for schizophrenia and other psychiatric research[1][2][3].
Z-Arg-Arg-AMC hydrochloride is a selective substrate of cathepsin B[1].
Glycocholic acid is a bile acid with anticancer activity, targeting against pump resistance-related and non-pump resistance-related pathways.
Stearyl glycyrrhetinate, a major component in licorice extract, has a MIC against S. aureus strains of more than 256 mg/L. Stearyl glycyrrhetinate has antibacterial effects[1].
MOCAc-PLGL(Dpa)AR is a positively charged fluorescent substrate for matrix metalloproteinase-2 (MMP-2) and MMP-7. MOCAc-PLGL(Dpa)AR is a substrate of matrilysin, can be cleaved at the peptide bond between the glycine and leucine residues[1][2].
Ziprasidone Hcl(CP-88059 Hcl) is a combined 5-HT (serotonin) and dopamine receptor antagonist which exhibits potent effects of antipsychotic activity.Target: 5-HT receptor; Dopamine receptorZiprasidone (hydrochloride) is the salt form of ziprasidone, which possesses an in vitro 5-HT2A/dopamine D2 receptor affinity ratio higher than any clinically available antipsychotic agent. In vivo, ziprasidone antagonizes 5-HT2A receptor-induced head twitch with 6-fold higher potency than for blockade of d-amphetamine-induced hyperactivity, a measure of central dopamine D2 receptor antagonism. Ziprasidone also has high affinity for the 5-HT1A, 5-HT1D and 5-HT2C receptor subtypes, which may further enhance its therapeutic potential [1]. Ziprasidone sulfoxide and sulfone were the major metabolites in human serum. The affinities of the sulfoxide and sulfone metabolites for 5-HT2 and D2 receptors are low with respect to ziprasidone, and are thus unlikely to contribute to its antipsychotic effects [2]. Ziprasidone was associated with significant differential adverse effects relative to placebo in BPM, BPD, and schizophrenia with no significant difference in weight gain in all 3 groups. Self-reported somnolence was increased across the 3 conditions. Subjects with BPM were more vulnerable to EPS than those with BPD or schizophrenia [3].Clinical indications: Bipolar I disorder; Bipolar disorder; Mania; SchizophreniaFDA Approved Date: February 2001
Aminoxyacetamide-PEG3-azide is a non-cleavable 3 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].
NOTA-AE105 is an PET ligand of urokinase-type plasminogen activator receptor (uPAR), which can be radiolabeled by 64Cu and 68Ga. 68Ga-NOTA-AE105 and 64Cu-NOTA-AE105 shows high image contrast, resulting in clear tumor delineation[1][2].
N20C hydrochloride is a selective and noncompetitive open NMDA receptor open channel blocker, with micromolar affinity, fast on-off blockade kinetics, and strong voltage dependence. Neuroprotective activity[1].
Fluorescein-PEG6-NHS ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Hydroxy-PEG1-(CH2)2-Boc is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Glycodeoxycholic acid monohydrate is a nuclear receptor ligand.
Repaglinide M1-d5 is the deuterium labeled Repaglinide M1[1].
N-trans-Feruloyltyramine (N-feruloyltyramine), an alkaloid from Piper nigru, is an inhibitor of COX1 and COX2, with potential antioxidant properties. N-trans-Feruloyltyramine possesses anti-inflammatory activity[1].
2,3,4,4',5-Pentachloro-1,1'-biphenyl-d4 is the deuterium labeled 2,3,4,4',5-Pentachloro-1,1'-biphenyl[1].
JQKD82 (JADA82) is a cell-permeable and selective KDM5 inhibitor. JQKD82 increases H3K4me3 and can be used for the research of multiple myeloma[1].
Margetuximab (MGAH22) is a chimeric anti-HER2 monoclonal antibody optimized Fc domain, with an EC50 value of 39.33 ng/mL. Margetuximab can be used for researching metastatic HER2-positive breast cancer[1].
4-O-Methyldopamine hydrochloride is a catecholamine compound that has an inhibitory effect on dihydropteridine reductase[1].
M351-110 is a T-cell activating V-domain immunoglobulin inhibitory factor agonist for cancer research[1].
DNA polymerase-IN-3 (Compd 5b) is a coumarin derivative that exhibits inhibitory activity against Taq DNA polymerase and can be used in proliferative disease research[1].
LASSBio-1359 is an adenosine receptor agonist. It acts by inducing relaxation of the corpus cavernosum. It also acts as a novel selective phosphodiesterase.
THP-PEG8-Tos is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
DHODH-IN-16 is a potent dihydroorotate dehydrogenase (DHODH) inhibitor with an IC50 of 0.396 nM for human DHODH[1].