Foropafant (SR27417) highly potent, competitive, selective and orally active antagonist of platelet-activating factor (PAF) receptor, with a Ki value of 57 pM for [3H]PAF binding, at least 5-fold lower than that of unlabeled PAF itself. Foropafant potently inhibits PAF-induced aggregation of rabbit and human platelets[1].
Fmoc-Glu(OAll)-OH is a glutamic acid derivative[1].
The compound 7,4'-Di-O-methylapigenin may be partly responsible for the reported antifungal activity of C. zeyheri, and may serve as a potential source of lead compounds that can be developed as antifungal phytomedicines.And it also showed inhibition of the drug efflux pumps (with IC50 = 51.64 μg/ml).IC50:51.64 μg/ml(Candida albicans drug efflux pumps)[2]In vitro: The isolated 7,4'-Di-O-methylapigenin was further investigated for its inhibitory activity on ABC drug efflux pumps in C. albicans by monitoring an increase in ciprofloxacin, assessing the level of its accumulation, in response to reserpine. There was a higher accumulation of ciprofloxacin in Candida cells in the presence of 7,4'-Di-O-methylapigenin than with reserpine. The compound 7,4'-Di-O-methylapigenine demonstrated the activity in a dose-dependent manner with IC50 value of 51.64 μg/ml. These results support those obtained from synergism assays where by the underlying synergistic antifungal mechanisms could be due to blockage of ABC efflux pumps and increasing the susceptibility of Candida to miconazole.[2]In vivo: In searching for natural products as potential anti-inflammatory agents, 7,4'-Di-O-methylapigenin wasn't evaluated in vivo for its ability to inhibit acute inflammation.[1]
Apalutamide-COOH can be used to synthesis Apalutamide. Apalutamide is a potent and competitive androgen receptor (AR) antagonist, binding AR with an IC50 of 16 nM[1].
Clematomandshurica saponin C is found in Clematis manshurica[1].
C-DIM12 is a synthetic Nurr1 activaor induces Nurr1 and DA gene expression in cell lines and primary neurons.Target: Nurr1in vitro: C-DIM12 as a modulator of Nurr1 activity that results in inhibition of NF-κB-dependent gene expression in glial cells by stabilizing nuclear corepressor proteins, which reduces binding of p65 to inflammatory gene promoters. C-DIM12 Decreases Inflammatory Gene Expression in BV-2 Microglia. C-DIM12 Decreases Expression of NF-κB-Enhanced GFP Expression in Human Embryonic Kidney 293 Reporter Cells.[1] C-DIM12 increases protein levels of exogenously expressed human Nurr1 in transfected neurons.C-DIM12 protects neurons from 6-hydroxydopamine toxicity. [2]
4-Thiouridine is a ribonucleoside analog, it is widely used in RNA analysis and (m)RNA labeling. 4-Thiouridine inhibits rRNA synthesis and causes a nucleolar stress response[1].
Evofolin B is a natural phenol compound[1].
U-44069 is a stable prostaglandin (PG) H2 analogue and a potent vasoconstrictor. U-44069 induces Ca influx at preglomerular vessels[1].
α,β-Thujone is a component of the essential oils of some plants. α,β-Thujone causes cancers in male rats and induces seizures in the highest doses[1].
N-Methyl-2-pyrrolidone-d3 is the deuterium labeled N-Methylpyrrolidone[1]. N-Methylpyrrolidone (1-Methyl-2-pyrrolidinone), a five-membered cyclic amide, is an organic polar solvent. N-Methylpyrrolidone is extensively used in the manufacture of adhesives, paints, fuels, and pharmaceuticals[2][3].
Fmoc-NH-PEG2-NHS ester is an intermediate used in the synthesis of E-selectin antagonists[1].
Manitimus is an inhibitor of dehydroorotate dehydrogenase, and a potent immunosuppressive drug.
(E/Z)-BIX02188 is a MEK5/ERK5 pathway inhibitor. (E/Z)-BIX02188 inhibits the catalytic function of purified MEK5 enzyme.(E/Z)-BIX02188 can be used for the role of MEK5/ERK5 pathway in various biological systems [1].
(tert-Butoxycarbonyl)-D-leucine is a leucine derivative[1].
4-(2-Aminoethylamino)-7-(N,N-dimethylsulfamoyl)benzofurazan is a precolumn fluorescence derivatization reagent.
BODIPY-FL is a potent fluorescent dye. BODIPY-FL can be used to label probe or primer for fluorescent quenching-based quantitative detection of specific DNA/RNA.BODIPY-FL-labeled monoterpenoid can be used to examine the features of a broad spectrum of Gram-positive and Gram-negative bacteria and pathogenic fungi as well[1][2][3].
N-[(9H-Fluoren-9-ylmethoxy)carbonyl]-L-phenylalanylglycylglycine is a Glycine (HY-Y0966) derivative[1].
Isoatriplicolide tiglate is a bioactive sesquiterpene lactone. Isoatriplicolide tiglate can be isolated from Paulownia coreana. Isoatriplicolide tiglate has neuroprotective effect[1].
Guanidine Hydrobromide-15N3 is the 15N labeled Guanidine Hydrobromide[1].
Penicillamine is the most characteristic degradation product of the penicillin antibiotics. It is used as an antirheumatic and as a chelating agent in Wilson's disease.Target: OthersPenicillamine(Cuprimine, Depen) is used as an antirheumatic and as a chelating agent in Wilson's disease and is a chelating agent recommended for the removal of excess copper in patients with Wilson's disease. From in vitro studies which indicate that one atom of copper combines with two molecules of penicillamine. Penicillamine also reduces excess cystine excretion in cystinuria. The mechanism of action of penicillamine in rheumatoid arthritis is unknown although it appears to suppress disease activity. Unlike cytotoxic immunosuppressants, penicillamine markedly lowers IgM rheumatoid factor but produces no significant depression in absolute levels of serum immunoglobulins. Also unlike cytotoxic immunosuppressants which act on both, penicillamine in vitro depresses T-cell activity but not B-cell activity [1-3].
H-Leu-OEt.HCl is a leucine derivative[1].
Citrusinol is a natural product isolated from D. caudatum. Citrusinol has anticancer activity and inhibits the proliferation and migration of human hepatocytes HepG 2[1].
3-Carboxy-6-hydroxycoumarin is an intermediate in organic syntheses[1].
Deoxyandrographolide is a natural compound extracted from A. paniculata; potently inhibit the growth of liver (HepG2 and SK-Hep1) and bile duct (HuCCA-1 and RMCCA-1) cancer cells.IC50 value:Target: Anticancer natural compoundin vitro: Treatment with 14-DAG activated AMPK through induction of cyclic AMP-protein kinase A pathway. 14-DAG controlled ethanol-induced hepatosteatosis by interfering with dysregulation of lipid metabolism. In conclusion, our results indicated that 14-DAG was capable of preventing the development of fatty liver through AMPK-mediated regulation of lipid metabolism [1]. 14-DAG down-regulated the formation of death-inducing signalling complex, resulting in desensitization of hepatocytes to TNF-alpha-induced apoptosis. Pretreatment of hepatocytes with 14-DAG accentuated microsomal Ca-ATPase activity through induction of NO/cGMP pathway [2]. 14-DAP, in concentrations between 10-100 microM, reduced the extracellular acidification rate and the intracellular alkalinization in a dose-dependent manner. In addition, 14-DAP reduced PAF-induced calcium flux in the presence of extracellular calcium, and tyrosine phosphorylation of a 44 kDa protein corresponding to the MAPK(ERK1) [3]. in vivo: Half of the ethanol-fed animals received 14-deoxyandrographolide (14-DAG) treatment for the last 4 weeks of study. protective effect of 14-DAG against ethanol-induced hepatic injury is based on its ability to reduce oxidative stress through cNOS dependent improvement of redox status. 14-DAG mediated activation of adenylate cyclase-cAMP signaling leading to up-regulation of cNOS may provide a promising approach in the prevention of liver diseases during chronic alcoholism [4].
Microcolin H is a marine lipopeptide and phosphatidylinositol transfer protein ligand that targets PITPα/β. Microcolin H increases the conversion of LC3I to LC3II and reduces p62 levels in cancer cells, leading to autophagy cell death (Autophagy). Microcolin H effectively inhibits tumor development and has anti-proliferative activity in nude mouse subcutaneous tumor models[1].
Stigmast-5-ene-3,7-dione (Compound 10) is a compound isolated from the roots, leaves and twigs of Penianthus longifolius[1].
Bavachromene is a chromenochalcone from the seeds of Psoralea corylifolia with estrogenic activities [1].
Procaspase-IN-5 is a human DNA polymerase λ inhibitor. Procaspase-IN-5 has DNA polymerization function and TdT function with an IC50 value of 5.9 μM and 4.5 μM, respectively. Procaspase-IN-5 can be used for the research of cancer[1].
Azobenzene-d10 is the deuterium labeled Azobenzene[1]. Azobenzene can be used as an optical trigger for the design and synthesis of a large variety of photoresponsive systems[2][3][4].