Bromisoval has anti-inflammatory effects and has been used as an old sedative and hypnotic.
Tet-20 is a biological active peptide. (Tet-20, is a synthetic cathelicidin-derived peptide. It was tested as infection-resistant coating for medical devices. When tethered on an implant surface Tet-20 exhibited broad antimicrobial activities both in vivo and in vitro. It can stop biofilm formation and appears to be non-toxic to eukaryotic cells)
Deltorphin (Deltorphin A; Dermenkephalin) is a biological active peptide. (Deltorphin A peptide was isolated from skin extracts of the South American frog, Phyllomedusa sauvagei. Deltorphin A is a potent and selective agonist for the delta-opioid receptor.)
Effusanin A is a natural product that can be found in Isodon rugosus. Effusanin A exhibits DNA-damaging and antibacterial activities[1].
(22E,24R)-Stigmasta-4,22-dien-3-one (compound 28) is a steroid isolated from sponges[1].
VEGFR-2-IN-24 is a potent VEGFR-2 inhibitor with IC50 value of 0.22 µM. VEGFR-2-IN-24 can be used for tumor research[1].
Fmoc-D-Ala-OH is an alanine derivative[1].
IL-17A modulator-3 (compound 253) is a IL-17A modulator. IL-17A modulator-3 inhibits IL-17A/A with an IC50 value ＜10 μM. IL-17A modulator-3 can be used for the research of inflammation, cancer and autoimmune disease[1].
Nifursol is a nitrofuran antibiotic which inhibits the growth of Histomonas meleagridis but is not lethal to the flagellated protozoan. Target: AntibacterialNifursol can be analyzed and detected in tissues using intact 3,5-dinitrosalicylic acid hydrazide side chains along with electron-capture GC, spectrophotometric detection, and HPLC with ultraviolet light detection. In tissues, it has been observed that Nifursol is tightly bound to proteins and requires basic solutions such as ammonia to break the bonds between the two.
2’-Deoxy-2’-fluoroarabino-O6-methyl inosine 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].
Ozanezumab (GSK1223249) is an anti-Nogo-A (neurite outgrowth inhibitor A) monoclonal antibody. Ozanezumab can be used in amyotrophic lateral sclerosis (ALS) and multiple sclerosis research[1].
Z16078526 induces endogenous Ucp1 expression, promotes p38 MAPK phosphorylation and lipolysis in primary mouse brown adipocytes. Z16078526 activates thermogenic gene expression and mitochondrial activity (uncoupled respiration) in mouse brown adipocytes. Z16078526 also stimulates thermogenesis in the mouse[1].
Piroxicam D3 (CP-16171 D3) is deuterium labeled Piroxicam. Piroxicam is a non-steroidal anti-inflammatory drugs, acts as a COX inhibitor, with IC50s of 47, 25 μM for human monocyte COX-1 and COX-2, respectively [1].
Tubulysin E is a highly cytotoxic peptide isolated from the myxobacterial species Archangium geophyra and Angiococcus disciformis. Tubulysin displays extremely potent cytotoxic activity in mammalian cells, including multidrug-resistant cell lines, with IC50 values in the lower nanomolar range[1]. Tubulysin E is a cytotoxic activity tubulysin which inhibits tubulin polymerization and leads to cell cycle arrest and apoptosis[2].
GNF351 is a full aryl hydrocarbon receptor (AHR) antagonist. GNF351 competes with a photoaffinity AHR ligand for binding to the AHR with an IC50 of 62 nM. GNF351 is minimal toxicity in mouse or human keratinocytes[1].
Zectivimod is a sphingosine-1-phosphate receptor agonist. Zectivimod can be used for the research of autoimmune diseases, chronic inflammatory diseases and immunoregulation disorders[1].
Eletriptan HBr is a selective 5-HT1B and 5-HT1D receptor agonist with Ki of 0.92 nM and 3.14 nM, respectively.IC50 value: 0.82 nM/3.14 nM (5-HT1B/5-HT1D, Ki) [1]Target: 5-HT1B/5-HT1D in vitro: [3H]Eletriptan has a total number of binding sites (Bmax) of 2478 fmol/mg and 1576 fmol/mg for 5-HT1B and 5-HT1D, respectively. [3H]Eletriptan has a significantly faster association rate (K(on) 0.249/min/nM) than [3H]sumatriptan (K(on) 0.024/min/nM) and a significantly slower off-rate (K(off) 0.027/min compared to 0.037/min for [3H]sumatriptan) [1]. Eletriptan induces concentration-dependent contractions of meningeal artery, coronary artery, and saphenous vein. The potency of Eletriptan is higher in meningeal artery than in coronary artery (86-fold) or saphenous vein (66-fold). The predicted contraction by Eletriptan (40 mg and 80 mg) and sumatriptan (100 mg) at free C(max) observed in clinical trials is similar in meningeal artery [2].in vivo: Eletriptan (<1000 mg/kg, i.v.) produces a dose-dependent reduction of carotid arterial blood flow in the anaesthetised dog. Eletriptan reduces coronary artery diameter with ED50 value of 63 mg/kg in the anaesthetised dog. Eletriptan (<300 mg/kg, i.v.) administered prior to electrical stimulation of the trigeminal ganglion produces a dose-related and complete inhibition of plasma protein extravasation in the dura mater rats. Eletriptan (100 mg/kg, i.v.) produces a complete inhibition of plasma protein extravasation in rat dura mater [3]. Iontophoretic ejection (50 nA) of Eletriptan suppresses the response in 75% of cells and causes an average suppression of cell firing of 42% in cats [4].
Hexoprenaline is an orally active and selective β-adrenergic receptor agonist that dilates the bronchi. Hexoprenaline can be used in the study of bronchospasm, including asthma, bronchitis, and emphysema[1].
PAP-1 is a selective inhibitor of Kv1.3, voltage-gated K+ channel. PAP-1 (EC50=2 nM) potently inhibits human T effector memory cell proliferation and delayed hypersensitivity. IC50 value: 2 nM (EC50) [1]in vitro: blocks Kv1.3 in a use-dependent manner, with a Hill coefficient of 2 and an EC50 of 2 nM, by preferentially binding to the C-type inactivated state of the channel. PAP-1 is 23-fold selective over Kv1.5, 33- to 125-fold selective over other Kv1-family channels, and 500- to 7500-fold selective over Kv2.1, Kv3.1, Kv3.2, Kv4.2, HERG, calcium-activated K+ channels, Na+,Ca2+, and Cl- channels [1]. The blockade of Kv1.3 results in membrane depolarization and inhibition of TEM proliferation and function. In this study, the in vitro effects of PAP-1 on T cells and the in vivo toxicity and pharmacokinetics (PK) were examined in rhesus macaques (RM) with the ultimate aim of utilizing PAP-1 to define the role of TEMs in RM infected with simian immunodeficiency virus (SIV). Electrophysiologic studies on T cells in RM revealed a Kv1.3 expression pattern similar to that in human T cells. Thus, PAP-1 effectively suppressed TEM proliferation in RM [2].in vivo: PAP-1 does not exhibit cytotoxic or phototoxic effects, is negative in the Ames test, and affects cytochrome P450-dependent enzymes only at micromolar concentrations. PAP-1 potently inhibits the proliferation of human TEM cells and suppresses delayed type hypersensitivity, a TEM cell-mediated reaction, in rats [1]. When administered intravenously, PAP-1 showed a half-life of 6.4 hrs; the volume of distribution suggested extensive distribution into extravascular compartments. When orally administered, PAP-1 was efficiently absorbed. Plasma concentrations in RM undergoing a 30-day, chronic dosing study indicated that PAP-1 levels suppressive to TEMs in vitro can be achieved and maintained in vivo at a non-toxic dose [2].
4-O-Methyldebenzoylpaeoniflorin is a natural product that can be isolated from Paeonia albiflora[1].
Hispidol ((Z)-Hispidol) is a potential therapeutic for inflammatory bowel disease; inhibits TNF-α induced adhesion of monocytes to colon epithelial cells with an IC50 of 0.50 µM.
Glucosylsphingosine-d7 is deuterium labeled Glucosylsphingosine.
MC-AAA-NHCH2OCH2COOH (compound 20) is a cleavable ADC linker that is used for making antibody-drug conjugate (ADC)[1].
Imatinib Mesylate is a tyrosine kinases inhibitor that inhibits c-Kit, Bcr-Abl, and PDGFR (IC50=100 nM) tyrosine kinases.
Urs-12-ene-3β,16β,22α-triol is a terpenoid compound isolated from the ethanol extract of fresh aerial parts of the Patagonian shrub Nardophyllum bryoides[1].
Ovotransferrin (328-332) has a protective activity on the blood pressure by inhibiting the Angiotensin-Converting Enzyme (ACE), with the IC50 of 20 μM. Ovotransferrin (328-332) fragment has an activity against Cholinesterase (ChE), implicating in Alzheimer’s diseases[1][2].
UCPH-102 is a highly selective EAAT1 inhibitor with an IC50 of 0.43 µM. UCPH-102 exhibits a specific anti-proliferative effect on T-ALL cells. UCPH-102 also shows good blood-brain permeability, which can be used in studies of amyotrophic lateral sclerosis, Alzheimer’s disease, chronic pain and obsessive compulsive disorder[1][2][3][4].
Palmitic acid-13C is the 13C-labeled Palmitic acid. Palmitic acid is a long-chain saturated fatty acid commonly found in both animals and plants. Palmitic acid can induce the expression of glucose-regulated protein 78 (GRP78) and CCAAT/enhancer binding protein homologous protein (CHOP) in in mouse granulosa cells[1][2].
SLSLSPG can be obtained from the C-end of the heavy chain of human Igγ-1. SLSLSPG is a common variant in IgG[1].