Alitame (anhydrous) is a high-intensity sweetener formed from the amino acids L-aspartic acid and D-alanine, and an amine derived from thietane[1].
Coenzyme Q0 (CoQ0) is a potent, oral active ubiquinone compound can be derived from Antrodia cinnamomea. Coenzyme Q0 induces apoptosis and autophagy, suppresses of HER-2/AKT/mTOR signaling to potentiate the apoptosis and autophagy mechanisms. Coenzyme Q0 regulates NFκB/AP-1 activation and enhances Nrf2 stabilization in attenuation of inflammation and redox imbalance. Coenzyme Q0 has anti-angiogenic activity through downregulation of MMP-9/NF-κB and upregulation of HO-1 signaling[1][2][3].
Tiliquinol (NSC 130828) is a non-absorbed anti-amoebic luminal agent. Tiliquinol is used in combination with tibroquinol. Tiliquinol can be used for the research of amebic liver abscess[1][2].
Difloxacin-d3 (hydrochloride) is the deuterium labeled Difloxacin (hydrochloride)[1].
Alvelestat (AZD9668) is a novel, oral inhibitor of neutrophil elastase (NE) with the pIC50 of 7.9 for Human NE.IC50 Value: 7.9 ± 0.12 (pIC50, Human NE); 4.9 nM (Ki value, Human NE) [1]Target: Neutrophil elastasein vitro: AZD9668 had a high binding affinity for human NE (KD = 9.5 nM) and potently inhibited NE activity. The calculated pIC50 (IC50) and Ki values for AZD9668 for human NE were 7.9 (12 nM) and 4.9 nM, respectively. In contrast to earlier NE inhibitors, the interaction between AZD9668 and NE was rapidly reversible. AZD9668 was also highly selective for NE over other neutrophil-derived serine proteases. In cell-based assays, AZD9668 inhibited plasma NE activity in zymosan-stimulated whole blood. In isolated human polymorphonuclear cells, AZD9668 inhibited NE activity on the surface of stimulated cells and in the supernatant of primed, stimulated cells.AZD9668 showed good crossover potency to NE from other species [1]. in vivo: Six hundred and fifteen patients were randomised: placebo (302), AZD9668 60 mg bid (313). AZD9668 showed no effect on lung function: change in mean pre-bronchodilator FEV1 versus placebo was 0.01L (95% confidence interval: -0.03, 0.05; p=0.533). AZD9668 did not significantly improve respiratory signs and symptoms, SGRQ-C score or time to first exacerbation. Adverse events were similar for AZD9668 and placebo [2]. AZD9668 was well tolerated at single doses up to 150 mg and multiple doses up to 70 mg twice daily. PK were dose linear; median time to peak plasma concentration was reached at 0.5 - 1.5 hours and the short elimination half-life was consistent with twice daily dosing. Steady state was reached by Day 2 of twice daily dosing with negligible accumulation. Approximately 40% of AZD9668 was eliminated renally as unchanged compound. Ex vivo zymosan-stimulated inhibition of NE activity was dose-dependent, with maximal inhibition achieved at 60 mg [4].Toxicity: A total of 838 patients were randomised to AZD9668 5 mg bid (212 patients), 20 mg bid (206 patients), 60 mg bid (202 patients) or placebo (218 patients). AZD9668 showed no effect on lung function, respiratory signs and symptoms, QoL or biomarkers [3].Clinical trial: Phase II study of a neutrophil elastase inhibitor (AZD9668) in patients with bronchiectasis.
Schisanlignone D is a chemical component of Schisandra viridis a. c. sm[1].
Z-LYS-SBZL (monohydrochloride) is a lysine derivative[1].
Wilfordinine D is a natural sesquiterpene alkaloid[1].
S-(4-Nitrophenyl)-L-cysteine is a cysteine derivative[1].
JJH260 is AIG1inhibitor, and inhibit the fluorophosphonate reactivity and fatty acid esters of hydroxy fatty acid (FAHFA) hydrolysis activity of AIG1in HEK293T cells, with IC50 values of 0.50 μM and 0.57 μM, respectively[1].
4-Methylherniarin (7-Methoxy-4-methylcoumarin) is a coumarin derivative and fluorescent label, has an antimicrobial activitiy against both gram positive and gram negative bacterial stains. 4-Methylherniarin displays good activity against B. subtilis and S.sonnei with IC50 values of 11.76 μg/ml and 13.47 μg/ml[1].
NSC81111 is a potent and orally active EGFR-TK inhibitor with an IC50 of 0.15 nM. NSC81111 has anticaner effects[1].
Ro 60-0175 is a potent, selective 5-HT2C receptor agonist with pKi of 9, 7.5, 5.4, 5.2 and 5.6 for human 5-HT2C, 2A, 1A, 6 and 7 receptors respectively; induces hypolocomotion in rats at doses greater than 0.5 mg/kg s.c.; (0.3 and 1 mg/kg s.c.) simultaneously reduces both unpunished and punished lever pressing, a profile consistent with sedation, induces sedative-like responses via 5-HT(2C) receptor activation in vivo.
ISIS 416858, a single-stranded antisense oligodeoxynucleotide, is a potent and selective inhibitor of FXI mRNA expression.
Fmoc-Gln(Trt)-Ser(psi(Me,Me)pro)-OH is a dipeptide.
CDK7-IN-6 is a potent and selective cyclin-dependent kinase (CDK7) inhibitor (IC50≤100 nM), extracted from patent WO2019197549 A1, compound 210. CDK7-IN-6 is > 200-fold selective for CDK7 over CDK1, CDK2, and CDK5. CDK7-IN-6 can be used for the research of cancer[1].
Sec-O-Glucosylhamaudol is a natural compound extracted from Peucedanum japonicum Thunb, decreases levels of μ-opioid receptor, with analgesic effect[1].
GLP-1 receptor agonist 8 is a potent agonist of GLP-1 R. GLP-1 receptor agonist 8 has the potential for the research of diabetes, obesity, and nonalcoholic fatty liver disease (NAFLD) (extracted from patent WO2019239319A1, compound 17)[1].
BI-0115 is a selective inhibitor of LOX-1 (IC50=5.4 µM) that blocks cellular uptake of oxLDL. BI-0115 binding triggers receptor inhibition by formation of dimers of the homodimeric ligand binding domain[1].
Dibromochloronitromethane is one of Halonitromethanes, which are a recently identified class of disinfection by-products (DBPs) in drinking water[1].
PT-262 is a potent ROCK inhibitor with an IC50 value of around 5 μM. PT-262 induces the loss of mitochondrial membrane potential and elevates the caspase-3 activation and apoptosis. PT-262 inhibits the ERK and CDC2 phosphorylation via a p53-independent pathway. PT-262 blocks cytoskeleton function and cell migration. PT-262 has anti-cancer activity[1][2].
VU6028418 (VU 6028418) is a potent, highly selective, orally bioavailable M4 mAChR antagonist for the treatment of dystonia and other movement disorders.
HBT1 is a novel potent AMPA receptor potentiator with lower agonistic effect compared with LY451395 and OXP1.
Muramic acid is a component in many Gram-positive bacterial cell walls, as marker for Gram-positive bacteria[1].
Desmethyl-WEHI-345 analog is a protein kinase inhibitor extracted from patent WO2012003544A1, example 12. Desmethyl-WEHI-345 analog can be used for the research of colon cancer[1].
BODIPY FL Thapsigargin is a potent green fluorescent dye. BODIPY FL Thapsigargin inhibits intracellular SERCA-type Ca2+ pumps present in the sarcoplasmic/endoplasmic reticulum. BODIPY FL Thapsigargin used for investigation of thapsigargin binding sites in live cells[1][2].
Kaempferol 7-O-neohesperidoside is a ?avonoid glycoside that can be isolated from Litchi chinensis. Kaempferol 7-O-neohesperidoside exhibits significant cytotoxic activity against A549, LAC, Hep-G2, and HeLa cell lines with IC50s of 0.53, 7.93, 0.020, and 0.051 μM, respectively[1].
3,4-Di-O-acetyl-L-fucal is the reactant for synthesis antibiotics (extracted from patent WO1999026956A1)[1].
Metopimazine (EXP999) is a phenothiazine derivative used to prevent emesis during chemotherapy. Metopimazine belongs to the anti-dopaminergic anti-emetics (ADA) class. Metopimazine can be used for the research of gastroenteritis (GE) [1].
YLADGDLHSDGPGR is a biologically active peptide.