Alemtuzumab (Campath-IH) is a humanized monoclonal antibody against CD52, a glycoprotein expressed on the surface of most lymphoid, and to a lesser extent, myeloid cell types. Alemtuzumab selectively targets the CD52 antigen to induce profound lymphocyte depletion, followed by recovery of T and B cells with regulatory phenotypes[1][2].
Adamantane-d16 is the deuterium labeled DL-Histidine[1].
INCB3344 is a potent, selective and orally bioavailable CCR2 antagonist with IC50 values of 5.1 nM (hCCR2) and 9.5 nM (mCCR2) in binding antagonism and 3.8 nM (hCCR2) and 7.8 nM (mCCR2) in antagonism of chemotaxis activity.
Basic green 4 (Malachite green) is a cationic dye. Basic green 4 also is an N-methylated diaminotriphenylmethane dye to be used for coloring purpose[1].
Cimicifugoside, a triterpenoid isolated from Cimicifuga simplex, is a novel specific nucleoside transport inhibitor that displays synergistic potentiation of methotrexate cytotoxicity[1]. Cimicifugoside shows immunosuppressive activity, which is preferentially directed toward B-cell function with larger doses being required for suppression of T-cell function[2].
NH-bis(PEG4-acid) is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
FATP1-IN-1 is a fatty acid transport protein 1 (FATP1) inhibitor. FATP1-IN-1 is an inhibition of recombinant human or mouse acyl-CoA synthetase activity of FATP1, with the IC50 values of 0.046 μM or 0.60 μM, respectively[1].
A3AR antagonist 1 (compound 17) is a potent and selective human A3 adenosine receptor (AR) antagonist, with an Ki of 4.63 nM. A3AR antagonist 1 shows no affinity for the rat A3 AR even at high concentrations[1].
Omarigliptin(MK-3102) is a potent, selective and long-acting DPP-4 inhibitor with IC50 of 1.6 nM; highly selective over allproteases tested (IC50 > 67 μM).IC50 value: 1.6 nM [1]Target: DPP-4 inhibitorin vitro: Omarigliptin has weak ion channel activity (IC50 > 30 μM at IKr, Cav1.2, and Nav1.5). An expansive selectivity counterscreen (168 radioligand binding or enzymatic assays) was carried out at MDS Pharma. An IC50 > 10 μM was obtained in all assays. in vivo: When orally administered 1 h prior to dextrose challenge in an oral glucose tolerance test (OGTT), it significantly reduced blood glucose excursion in a dose-dependent manner from 0.01 mg/kg (7% reduction in glucose AUC) to 0.3 mg/kg (51% reduction).
(+)-7'-Methoxylariciresinol is a lignan glucoside that can be isolated from Cyclea racemosa[1].
2-Chloro-N6-cyclopentyl 2’-deoxy- adenosine 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].
Palivizumab (MEDI 493), a humanized respiratory syncytial virus monoclonal antibody, reduces respiratory syncytial virus (RSV) infection[1].
(Rac)-LM11A-31 dihydrochloride is an isomer of LM11A-31 dihydrochloride. LM11A-31 dihydrochloride, a p75NTR (neurotrophin receptor p75) Ligand, is a potent proNGF (nerve growth factor) antagonist[1].
(Rac)-Tavapadon ((Rac)-PF-06649751; (Rac)-CVL-751) is a potent and selective noncatechol dopamine D1 receptor agonist. (Rac)-Tavapadon displays potent full agonism in the GS activation assay as well as partial agonism in the β-arrestin2 recruitment assay (GS-cAMP, EC50=0.8 nM; β-arrestin2, EC50=68 nM). (Rac)-Tavapadon has antiparkinsonian activity[1].
5-DTAF is a isomeric fluorescein derivative that directly react with polysaccharides and other alcohols in aqueous solution at pH ＞ 9. The maximum of the 5-DTAF emission profile is at a wavelength of 518 nm after excitation at 488 nm[1].
FmocNH-PEG2-CH2CONH-PEG2-CH2COOH is an optimized, extended PEG-like linker[1].
MMP Inhibitor II (compound 4e) is a potent, reversible pan-MMP inhibitor with IC50 values of 24 nM, 18.4 nM, 30 nM, and 2.7 nM for MMP-1,MMP-3, MMP-7, and MMP-9, respectively[1].
Pedaliin is a bioactive component obtained from the ethanol extract of Sesame (Sesamum indicum L.) leaves (SLs). Pedaliin shows in vitro antioxidant and anti-colon cancer efficacy with radical scavenging activity and ferric reducing antioxidant power (FRAP)[1][2].
UNC-2170 is a functionally active, fragment-like ligand for 53BP1 (IC50=29 µM; Kd=22 µM). UNC-2170 shows at least 17-fold selectivity for 53BP1 as compared to nine other methyl-lysine (Kme) reader proteins. 53BP1 is a Kme binding protein that plays a central role in DNA Damage Repair (DDR) pathways and is recruited to sites of double-strand breaks (DSB)[1].
Liensinine Perchlorate is a constituent of Nelumbo nucifera Gaertn, with ani-hypertension and anti-cancer activities. Liensinine Perchlorate induces colorectal cancer (CRC) cell apoptosis[1].
H-Thr-Gly-OH is a biologically active peptide.
Tiamulin is a diterpenic veterinary drug widely used in swine for the control of infectious diseases, including swine dysentery and enzootic pneumonia.
Dansyl chloride-d6 is the deuterium labeled 3-Mercapto-3-methylbutan-1-ol[1].
Thiamphenicol is an antimicrobial antibiotic and a methyl-sulfonyl analogue of chloramphenicol.Target: AntibacterialThiamphenicol (also known as thiophenicol and dextrosulphenidol) is an antibiotic. It is the methyl-sulfonyl analogue of chloramphenicol and has a similar spectrum of activity, but is 2.5 to 5 times as potent. Like chloramphenicol, it is insoluble in water, but highly soluble in lipids. It is used in many countries as a veterinary antibiotic, but is available in China, Morocco and Italy for use in humans. Its main advantage over chloramphenicol is that it has never been associated with aplastic anaemia. Thiamphenicol is a derivative of chloramphenicol characterized by a spectrum comparable to that of the parent compound against multiresistant pathogens but showing satisfactory tolerability. Thiamphenicol showed a significant PAE (0.33 to 2.9h) on all pathogens studied and a powerful bactericidal effect against beta-lactamase-positive and -negative H. influenzae. These results indicate a good in vitro activity of thiamphenicol against difficult-to-treat multiply resistant pathogens [1, 2].
Pheniprazine hydrochloride is a potent and long acting inhibitor of monoamine oxidase. Pheniprazine has the potential for the research of depression[1].
Sematilide (CK-1752) is a selective IKr channel blocker. Sematilide causes a concentration-dependent inhibition of the delayed rectifier K+ current (IC50=25 μM). Sematilide is a class III antiarrhythmic agent[1].
17:0-18:1 PI-d5 (ammonium) is deuterium labeled 17:0-18:1 PI (ammonium).
RORγt inverse agonist 23 is a potent, selective, and orally available novel retinoic acid receptor-related orphan receptor γt inverse agonist.
(R,R)-Glycopyrrolate ((R,R)-Glycopyrronium (bromide); (R,R)-Glycopyrrolate (bromide)) is an anticholinergic agent. (R,R)-Glycopyrrolate ((R,R)-Glycopyrronium (bromide); (R,R)-Glycopyrrolate (bromide)) has the ability to reduce the frequency of drooling in vivo with developmental disabilities[1].
Thiazole Orange is a dye for reticulocyte analysis.