N-Nitrosodiethylamine-d10 is the deuterium labeled N-Nitrosodiethylamine[1]. N-Nitrosodiethylamine (Diethylnitrosamine) is a potent hepatocarcinogenic dialkylnitrosoamine. N-Nitrosodiethylamine is mainly present in tobacco smoke, water, cheddar cheese, cured, fried meals and many alcoholic beverages. N-Nitrosodiethylamine is responsible for the changes in the nuclear enzymes associated with DNA repair/replication. N-Nitrosodiethylamine results in various tumors in all animal species. The main target organs are the nasal cavity, trachea, lung, esophagus and liver.
Boc-AAG-pNA is a glycine endopeptidase substrate. Boc-AAG-pNA can be used to test the amidase activity glycine endopeptidase[1].
LTD4 antagonist 1 is a potent, orally active antagonist of leukotriene D4 (LTD4) with a Ki of 0.57 nM.
Y02224 is a BET inhibitor. It shows the reasonable antiproliferative effect on leukemia cells.
Scopine is the metabolite of anisodine, which is a α1-adrenergic receptor agonist and used in the treatment of acute circulatory shock. Target: α1-Adrenergic ReceptorScopine is a tropane alkaloid found in a variety of plants including Mandragora root, Senecio mikanoides (Delairea odorata), Scopolia carniolica and Scopolia lurida. Scopine can be prepared by the hydrolysis of scopolamine. From Wikipedia.
Manidipine is a calcium channel blocker that is used clinically as an antihypertensive. Target: Calcium ChannelManidipine is a dihydropyridine calcium antagonist, which causes systemic vasodilation by inhibiting the voltage-dependent calcium inward currents in smooth muscle cells. Manidipine was well tolerated in clinical trials, with most adverse effects related to vasodilation [1]. Manidipine is a lipophilic, third-generation dihydropyridine calcium channel antagonist with a high degree of selectivity for the vasculature, thereby inducing marked peripheral vasodilation with negligible cardiodepression. manidipine represents a first-line treatment option for patients with essential mild-to-moderate hypertension [2]. Manidipine has neutral effects on glucose and lipid metabolism and is generally well tolerated. Manidipine thus represents a first-line option for lowering BP in patients with mild-to-moderate hypertension [3].
M4 mAChR agonist-1 (compound 10a) is a potent M4 mAChR agonist with an EC50 >10 μM for human M4[1].
Suprofen-d3 (TN-762-d3) is the deuterium labeled Suprofen. Suprofen (TN-762) is a non-steroidal anti-inflammatory drug (NSAID)[1][2].
Ethynodiol diacetate is a steroidal progestin which is used as a hormonal contraceptive, it has relatively little or no potency as an androgen,has significant estrogenic effects.
Biotin NHS is an amino reactive biotin reagent used in the preparation of biotinylated surfaces or polypeptides.
Compounds 17O (ic50= 14.0 nm, NCI-H460) and 17p (ic50= 2.9 nm, NCI-H460) and furan groups showed effective cytotoxic activity against various human cancer cell lines at the nanomolar level.
Boc-Gly-Lys-Arg-AMC is a polypeptide that can be found by peptide screening. Peptide screening is a research tool that pools active peptides primarily by immunoassay. Peptide screening can be used for protein interaction, functional analysis, epitope screening, especially in the field of agent research and development[1].
tans-4-Hydroxy-D-proline methyl ester hydrochloride is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). tans-4-Hydroxy-D-proline methyl ester hydrochloride is also a alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs[1][2].
BI-671800 is a highly specific and potent antagonist of chemoattractant receptor-homologous molecule on Th2 cells (DP2/CRTH2), with IC50 values of 4.5 nM and 3.7 nM for PGD2 binding to CRTH2 in hCRTH2 and mCRTH2 transfected cells, respectively[1]. BI-671800 has potential for the treatment of poorly controlled asthma[2].
Brazikumab (AMG 139) is a human IgG2 monoclonal antibody, selectively binds the p19 subunit of IL-23, with a KD of 0.138 nM for human IL-23. Brazikumab can be used for the research of Crohn's disease[1].
4-Oxofenretinide (4-Oxo-4-HPR) is a metabolite of Fenretinide (HY-15373). 4-Oxofenretinide induces cell growth inhibition in ovarian, breast, and neuroblastoma tumor cell lines. 4-Oxofenretinide causes a marked accumulation of cells in G2-M. 4-Oxofenretinide induces cancer cell apoptosis through caspase-9[1].
Scandine is a alkaloid compound isolated from the twigs and leaves of Melodinus suaveolens[1].
Diosmin is a flavonoid found in a variety of citrus fruits and also an agonist of the aryl hydrocarbon receptor (AhR).
Naftifine-d3 hydrochloride is the deuterium labeled Naftifine hydrochloride. Naftifine hydrochloride is an antibiotic. Naftifine hydrochloride has antifungal activity against dermatophytes, aspergilli, Sporothrix schenckii, and yeasts of the genus Candida. Naftifine hydrochloride can be used for the research of superficial dermatomycoses inhibition[1].
Panaxydol is isolated from Panax ginseng roots. Panaxydol induces mitochondria-mediated apoptosis. Panaxydol has the potential to be an anticancer agent, especially for EGFR-addicted cancer[1].
β-Tomatine is a breakdown product of a-tomatine and a less fungitoxic compound. β-Tomatine can suppress plant defense responses[1].
Ledol ((+)-Ledol) is an antifungal agent that can be isolated from the essential oil fractions of Rhododendron tomentosum. Ledol is also the expectorant and antitussive agent, which is simultaneously responsible for adverse reactions such as dizziness, nausea and vomiting[1].
3’-Azido-3’-deoxy-5-methyl-beta-L-uridine 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].
Encecalin is a natural benzofuran compound[1].
M56-S2 iodide is a SARS-CoV-2 Mpro inhibitor (IC50=4.0 μM). M56-S2 iodide showed good oral bioavailability and low toxicity in ADMET prediction. M56-S2 iodide has good drug potential and can be used in antiviral (such as SARS-CoV-2) research[1].
DSPE-PEG-Maleimide has DSPE phospholipid and maleimide to prepare nanostructured lipid carrier. DSPE-PEG-Maleimide extends blood circulation time and higher stability for encapsulated drugs[1][2].
Sulfamethazine is a sulfonamide antibacterial.Target: AntibacterialSulfamethazine is an antibiotic used to treat bronchitis, prostatitis and urinary tract infections. Sulfamethazine blocks the synthesis of dihydrofolic acid by inhibiting dihydropteroate synthase. In addition, sulfamethazine is a structural analog and competitive antagonist of para-aminobenzoic acid (PABA) and can inhibit normal bacterial utilization of PABA for the synthesis of folic acid, which is an important metabolite in DNA synthesis [1, 2].
Acetylneurotensin-(8-31) is the shortest analog of neurotensin with full binding and pharmacological activities[1].
Sulfathiazole D4 is a deuterium labeled Sulfathiazole. Sulfathiazole, an organosulfur compound, is used as a short-acting sulfonamide antibiotic[1].
FR221647 is an orally active non-nucleoside inhibitor of adenosine deaminase. FR221647 is not cytotoxic at a concentration of 100 μM[1].