Quercetin pentaacetate could interact with F-protein with lower binding energy and better stability to block viral adhesion. Quercetin pentaacetate interacts with RSV and inhibit the viral adhesion on cell surface[1][2].
GY1-22 is an inhibitor of DNAJA1-mutP53R175H interacting pocket. GY1-22 can be used for the research of cancer[1].
Oleyl Mesylate is a derivative of Oleyl Alcohol. Oleyl Alcohol has been incorporated into various formulations for drug delivery[1].
Propargyl-C8-amido-PEG2-NHS ester is a non-cleavable 2 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].
Capsiate, as a capsaicin analogue extracted from a non-pungent cultivar of CH-19 sweet red pepper, is an orally active agonist of TRPV1[1].
Ammonium bromide-d4 is the deuterium labeled Ammonium bromide[1].
QNZ46 is a NR2C/NR2D-selective NMDA receptor non-competitive antagonist (IC50 values are 3, 6, 229, and >300, >300 μM for NR2D, NR2C, NR2A, NR2B, and GluR1, respectively). IC50 value: 3 μM (for NR2D), 6 μM (for NR2C), 229 μM (for NR2D NR2A)Target: NR2D, NR2C, NR2Ain vitro: QNZ46 is a noncompetitive inhibitor of GluN2C/D containing NMDA receptors. KD and IC50 values for binding and inhibition of GluN1/Glun2D receptors by QNZ46 are 4.9 and 3.9 μM, respectively. QNZ46 does not compete for binding of glutamate or glycine, but QNZ46 receptor binding requires the binding of glutamate to the GluN2 subunit.
5’(R)-C-Methyl-2-thiouridine 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].
Nicorandil is potassium channel activator.Target: Potassium ChannelNicorandil is a vasodilatory drug used to treat angina. Nicorandil stimulates guanylate cyclase to increase formation of cyclic GMP (cGMP). cGMP activates protein kinase G (PKG) which phosphorylates and inhibits GTPase RhoA and decreases Rho-kinase activity. Reduced Rho-kinase activity permits an increase in myosin phosphatase activity, decreasing the calcium sensitivity of the smooth muscle. PKG also activates the sarcolemma calcium pump to remove activating calcium. PKG acts on K+ channels to promote K+ efflux and the ensuing hyperpolarization inhibits voltage-gated calcium channels. Overall, this leads to relaxation of the smooth muscle and coronary vasodilation [1, 2].
Fenmetozole Tosylate is an antagonist of the actions of ethanol, also antagonizes α2-adrenergic receptor, and acts as an antidepressant drug.
Tauro-β-muricholic Acid sodium (T-βMCA sodium), a endogenous metabolite, is a competitive and reversible farnesoid X receptor (FXR) antagonist, with an IC50 of 40 μM[1][2][3].
Isocucurbitacin B is a potent cytotoxic compound isolated from Helicteres rswa L. (Sterculiaceae). Isocucurbitacin B possesses anti-tumor acticity[1][2].
22-Oxybis(ethylamine) is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Neoeriocitrin, isolated from Drynaria Rhizome, shows activity on proliferation and osteogenic differentiation in MC3T3-E1. Neoeriocitrin is a potent acetylcholinesterase (AChE) inhibitor[1][2].
Pycnophorin significantly inhibits the growth of Bacillus subtilis and Staphyloccocus aureus with equal minimum inhibitory concentration (MIC) values of 25 μM.
Trimipramine is a 5-HT receptor antagonist, with pKi binding values of 6.39, 8.10, 4.66 for 5-HT1C, 5-HT2 and 5-HT1A, respectively. Trimipramine is also a potent and selective inhibitor targeting human noradrenaline (hNAT), serotonin (hSERT) and organic cation transporters (hOCT1, hOCT2) with IC50 values of 4.99 μM, 2.11 μM, 3.72 μM, 8.00 μM, respectively. Trimipramine has vascular activity and anxiolytic efficacy[1][2][3].
Amino-PEG4-(CH2)3CO2H is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Tibezonium iodide, an oropharyngeal disinfectant, has antibacterial activity for the prevention of mouth infections[1].
A09-003 is a CDK-9 inhibitor (IC50: 16 nM). A09-003 inhibits leukemia cell proliferation (IC50: 1.90, 0.86, 2.49, 1.84, 0.48 μM for BDCM, Molm-14, THP-1, U937, MV4-11 cells). A09-003 induces apoptosis and decreases Mcl-1 expression through Thr163 dephosphorylation[1].
N-Boc-PEG4-bromide is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].
5α-Androstane-3β,5,6β-triol is a neuroprotectant. 5α-Androstane-3β,5,6β-triol can remarkably reverse intracellular acidification and alleviate neuronal injury through the inhibition of AMPK signaling. 5α-Androstane-3β,5,6β-triol remarkably reduced the infarct volume and attenuated neurologic impairment in acute ischemic stroke models of middle cerebral artery occlusion in vivo[1].
RTI-118 is a novel small-molecule neuropeptide S receptor (NPSR) antagonist. RTI-118 can relieve drug addiction including selectively decrease cocaine self-administration[1].
Elenbecestat (E2609) is a novel potent BACE-1 inhibitor for the treatment of Alzheimer's disease (AD)[1].
Chloroacetamido-C4-NHBoc is an alkyl/ether-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Cefotetan is a semisynthetic cephamycin antibiotic that exerts its bactericidal effects by inhibition of cell-wall synthesis[1].
Fosaprepitant (L-758298) is a neurokinin-1 receptor antagonist for the prevention of chemotherapy-induced nausea and vomiting.IC50 Value:Target: NK1 receptorin vitro: Fosaprepitant (also known as MK-0517 and L-758,298) is a water-soluble phosphoryl prodrug for aprepitant, which, when administered intravenously, is converted to aprepitant within 30 min of intravenous administration via the action of ubiquitous phosphatases. Owing to the rapid conversion offosaprepitant to the active form (aprepitant), fosaprepitant 115 mg provided the same aprepitant exposure in terms of AUC as aprepitant 12 mg orally, and fosaprepitant is expected to provide a correspondingly similar antiemetic effect as aprepitant [1]. in vivo: Fosaprepitant is well tolerated with mild to moderate venous irritation being the only additional toxicity to those seen with oral aprepitant, and that is a function of dose, concentration, and infusion rate [2]. Patients receiving cisplatin ≥ 70 mg/m(2) for the first time received ondansetron and dexamethasone with a standard aprepitant regimen (125 mg on day 1, 80 mg on day 2, 80 mg on day 3) or a single-dose fosaprepitant regimen (150 mg on day 1) [3]. Single-dose fosaprepitant used in combination with granisetron and dexamethasone was well-tolerated and effective in preventing chemotherapy-induced nausea and vomiting in patients receiving highly emetogenic cancer chemotherapy, including high-dose cisplatin [4].
Recifercept (TA-46) is a soluble, recombinant fibroblast growth factor receptor 3 (FGFR3) molecule. Recifercept can be used as a decoy/ligand trap to decrease the amount of fibroblast growth factors that can bind to mutant FGFR3 receptors. Recifercept can be used for the research of achondroplasia[1].
Cerebellin is a neuromodulatory peptide widely distributed in the central nervous system.
((Allyloxy)carbonyl)-D-alanine is an alanine derivative[1].