MK-8318 is potent and selective CRTh2 receptor antagonist with a Ki of 5.0 nM.
Isotachioside is a aromatic glucoside that can be found in Berchemia racemosa[1].
Izuforant (JW1601) (Compound 24) is an orally active histamine H4 receptor (H4R) antagonist with an IC50 of 36 nM against human H4R. Izuforant also shows binding affinity of human serotonin 3 receptor (h5-HT3R) with an IC50 of 9.1 μM. Izuforant exhibits strong anti-pruritic and anti-inflammatory efficacies[1][2].
PAT-1251 is a potent, selective and oral Lysyl Oxidase-Like 2 (LOXL2) inhibitor, with IC50s of 0.71 and 1.17 μM for hLOXL2 and hLOXL3, respectively, and also potently inhibits mouse, rat, and dog LOXL2 (IC50s, 0.10, 0.12, and 0.16 μM, respectively); PAT-1251 has entered clinical development with the potential to treat a number of fibrotic diseases.
Dihydrobaicalin is a flavonoid glycoside, which can be isolated from American skullcap (Scutellaria lateriflora L.)[1].
N-3-oxo-hexadec-11Z-enoyl-L-Homoserine lactone is a biochemical reagent that can be used as a biological material or organic compound for life science related research.
Cisapride(R 51619) is a nonselective 5-HT4 receptor agonist, it is also a potent hERG potassium channel inhibitor.IC50 Value: 0.14 μM(EC50 for 5-HT4 receptor) [1]; 9.8 μM (Kv4.3) [2]Target: 5-HT4 Receptorin vitro: Cisapride showed higher inhibitory effects on a hERG current, as indicated by its IC50 of 9.4 × 10-9 M [1]. cisapride on cloned Kv4.3 channels stably expressed in Chinese hamster ovary cells were investigated using the whole-cell patch-clamp technique. Cisapride inhibited Kv4.3 in a concentration-dependent manner with IC50 values of 9.8 uM [2].in vivo: Cisapride (1 mg/kg i.v.), when administered 10 min after the start of GR113808 infusion, did not stimulate either antral or colonic motor activity under treatment with GR113808. The enhanced antral or colonic motor activity induced by these drugs was antagonized by treatment with GR113808 in dogs [3]. cisapride could not bring about more colitis damages through 5HT(4) receptors. Based on the present study further researches are required for investigating the exact roles of 5HT(4) receptors in the pathogenesis of ulcerative colitis[4].Toxicity: cardiac arrythmies
GSK805 is a potent, orally bioavailable RORγγ Inhibitor with pIC50 of 8.4 and >8.2 for RORγ FRET assay and Th17 assay.
RORγt Inverse agonist 2 is a selective, orally active RORγt inverse agonist with an EC50 of 119 nM[1].
Aceratioside, a tetralin glucoside, is a weakly cytostatic constituent. Aceratioside is an antineoplastic agent[1].
N-(3-Nitro-2-pyridinesulfenyl)-L-aspartic acid β-t-butyl ester is an aspartic acid derivative[1].
Anticancer agent 75 is a potent anticancer agent. Anticancer agent 75 shows cytotoxicity and selectivity in cancer cell lines. Anticancer agent 75 shows cytotoxicity to normal human kidney cell lines is at least 35 times lower than that of the Doxorubicin standard. Anticancer agent 75 shows good activity of antiplasmodial[1].
Crisnatol (BWA770U) mesylate is an orally active and anticancer agent, and a member of the arylmethylaminopropanediol class of DNA intercalators. Crisnatol mesylate shows in vitro cytotoxicity against human breast cancer cells, but not normal human skin fibroblasts[1][2][3].
Datopotamab (CDP7657) is an antibody targeting to TROP2. Datopotamab can be used to synthesize Datopotamab deruxtecan (HY-141598), TROP2-directed antibody-drug conjugate (ADC). Datopotamab deruxtecan consists of DNA topoisomerase I inhibitor Deruxtecan (HY-13631E) and Datopotamab[1].
Chitin synthase inhibitor 4 (compound 4fh) is a chitin synthase (CHS) inhibitor with fungicidal effect. Chitin synthase inhibitor 4 is a potential CHS-based fungicide in agriculture[1].
MRT-2359 is an orally active and potent degrader of GSPT1 with anti-tumor activity. MRT-2359 also inhibits the growth of resistant non-small cell lung cancer (NSCLC) and small cell lung cancer (SCLC) cells. MRT-2359 exhibits preferential activity in MYC-driven cell lines, such as N- and L-MYC high NSCLC and SCLC patient-derived xenografts (PDXs)[1].
Propylparaben-d7 (Propyl parahydroxybenzoate-d7)is the deuterium labeledPropylparaben(HY-N2026)[1]. Propylparaben (Propyl parahydroxybenzoate) is an antimicrobial preservative which can be produced naturally by plants and bacteria. Propylparaben is prevalently used in cosmetics, pharmaceuticals, and foods. Propylparaben disrupts antral follicle growth and steroidogenic function by altering the cell-cycle, apoptosis, and steroidogenesis pathways. Propylparaben also decreases sperm number and motile activity in rats[2][3][4].
TMPA is an antagonist of nuclear receptor Nur77 and LKB1 interaction.
Indacaterol Maleate is an ultra-long-acting β-adrenoceptor agonist.Target: β-adrenoceptorIndacaterol inhibits cAMP production in Chinese hamster ovary cells stably transfected with human β2 adrenoceptors with pEC50 of 8.06. Indacaterol inhibits electrically induced contraction on the electrically stimulated guinea pig trachea in a concentration-dependent manner with pEC50 of 8.23. Indacaterol induces a concentration-dependent inotropic effect with maximal efficacy of 75% in the isolated guinea pig left atrium [1]. Indacaterol reverses the carbachol-induced contraction in a concentration-dependent manner with IC50 of 37 nM in human small airways. Indacaterol concentration dependently reverses the serotonin-induced contraction with IC50 of 10.5 nM in rat small airways. Indacaterol has the highest intrinsic efficacy of 53% in rat small airways and 73% in human small airways [2]. Indacaterol (6.7 μg/kg) inhibits 5-HT-induced bronchoconstriction with a maximal effect of 85% in the conscious guinea pig. Indacaterol (12.5 μg/kg) dose-dependently inhibits methacholine-induced bronchoconstriction with a maximal effect of 85% in the anesthetized rhesus monkey [1].
(Des-Gly10,D-Ala6,Pro-NHEt9)-LHRH (salmon) is a GnRH analog that induces ovulation and/or spawning in farmed fish[1].
SKF 91488 (Homodimaprit) dihydrochloride is a potent and noncompetitive histamine N-methyltransferase inhibitor with a Ki value of 0.9 microM. SKF 91488 dihydrochloride inhibits the methylation of labeled histamine in mice[1].
2-Amino-7-propargyl-7,8-dihydro-8-oxo-9-(beta-D-3-deoxy-ribofuranosyl)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].
3β-Hydroxyurs-11-en-28,13β-olide (11,12-Dehydroursolic acid lactone) is a triterpenoid that can be found in Fadogia tetraquetra var. tetraquetra[1]. 3β-Hydroxyurs-11-en-28,13β-olide shows antibacterial activity[1].
(1′S,2′S)-Nicotine-1'-oxide is an alkaloid N-oxide from the leaves, stems and roots of Nicotiana tabacum[1].
GSK682753A is a selective and highly potent inverse agonist of the epstein-barr virus-induced receptor 2 (EBI2) with an IC50 of 53.6 nM.
Benzyl lactate is a kind lactate ester[1].
Isolugrandoside is a nature product. Isolugrandoside can be isolated from Digitalis davisiana Heywood[1].
Isovaleric acid-d2 is the deuterium labeled Isovaleric acid[1]. Isovaleric acid is a natural fatty acid and known to effect on neonatal death and possible Jamaican vomiting sickness in human[2].
3'-DMTr-dA can be used for the synthesis of nucleotides[1].
KSPWFTTL is an immunodominant Kb-restricted epitope from the p15E transmembrane protein. KSPWFTTL can restore susceptibility of a tumor line to anti-AKR/Gross MuLV cytotoxic T lymphocytes[1][2].