AZD2906, a selective glucocorticoid receptor (GR) agonist, demonstrates inhibitory concentrations (IC50s) of 2.2 nM in human GR, 0.3 nM in rat peripheral blood mononuclear cells (PBMC), 41.6 nM in human whole blood, and 7.5 nM in rat whole blood, respectively[1]. Additionally, it induces an increase in micronucleated immature erythrocytes within rat bone marrow.
Influenza hemagglutinin is a type of hemagglutinin found on the surface of the influenza viruses. It is an antigenic glycoprotein. It is responsible for binding the virus to the cell that is being infected. Influenza hemagglutinin proteins bind to cells w
Ganglioside GD1a is a sialic acid-containing glycosphingolipid found in brain, erythrocytes, bone marrow, testis, spleen, and liver. [1] It can be shed from the surface of tumor cells into the microenvironment where it influences tumor-host cell interactions to promote tumor cell proliferation, invasion, and metastasis. Ganglioside GD1a (20 μM) also increases endothelial cell proliferation. Furthermore, ganglioside GD1a has been shown to act as a functional coreceptor for toll-like receptor 2 (TLR2), enabling the recruitment of TLR2 to lipid rafts when bound by a bacterial toxin.[2] Ganglioside GD1a mixture contains ganglioside GD1a molecular species with C18:1 and C20:1 sphingoid backbones.
Palmitoylcholine is an acyl choline.1It inhibits protein kinase C activity when used at a concentration of 100 μM.2Palmitoylcholine induces hemolysis in rat erythrocytes.3Plasma levels of palmitoylcholine are decreased in female patients with myalgic encephalomyelitis/chronic fatigue syndrome (ME/CFS).1 1.Germain, A., Barupal, D.K., Levine, S.M., et al.Comprehensive circulatory metabolomics in ME/CFS reveals disrupted metabolism of acyl lipids and steroidsMetabolites10(1)34(2020) 2.Nakadate, T., and Blumberg, P.M.Modulation by palmitoylcarnitine of protein kinase C activationCancer Res.47(24 Pt 1)6537-6542(1987) 3.Cho, K.S., and Proulx, P.Interactions of acyl carnitines and other lysins with erythrocytes and reconstituted erythrocyte lipoproteinsBiochim. Biophys. Acta318(1)50-60(1973)
Donepezil N-oxide is an active metabolite of the acetylcholinesterase inhibitor donepezil . Donepezil N-oxide inhibits cholinesterase (ChE) activity in human erythrocytes in a concentration-dependent manner, exhibiting 45.5% inhibition when used at a concentration of 20 μM.
Globotetraosylceramides are bioactive neutral glycosphingolipids. They are the major glycolipids in human erythrocytes. They act as receptors for the Shiga toxins Stx1, Stx2, and Stx2e, the cytotoxic protein pierisin-1, and parvovirus B19. Globotetraosylceramides increase the expression of proteins responsible for enamel deposition, including ameloblastin, amelogenin, and enamelin, in dental epithelial cells and activate the ERK and p38 MAPK signaling pathways. Levels of globotetraosylceramides are elevated in fibroblasts from patients with salt and pepper syndrome, a neurocutaneous condition characterized by intellectual disability and hyper- and hypo-pigmented skin. Globotetraosylceramides (porcine RBC) contains a mixture of globotetraosylceramides with variable fatty acyl chain lengths isolated from porcine red blood cells.
N-Acetyl-DL-penicillamine is a chelating agent.1,2,3It inhibits the binding of methyl mercury to isolated human erythrocytes by 50% and removes 50% of methyl mercury ions from methyl mercury-loaded blood cells when used at a concentration of 1 mM.1,2N-Acetyl-DL-penicillamine (3 mmol kg per day, p.o.) reduces the biological half-life of mercury and decreases liver, kidney, brain, and blood mercury levels, as well as increases urinary excretion of mercury in a concentration-dependent manner, in mice when administered following injection of methyl mercuric chloride. It decreases mercuric chloride-induced mortality in mice when administered orally at a dose of 1.6 mmol kg.3N-Acetyl-DL-penicillamine is also an analog of SNAP that does not generate nitric oxide and has been used as a negative control in experiments using SNAP.4,5
LL-37 is a cationic and α-helical antimicrobial peptide expressed in human bone marrow, testis, granulocytes, and gingival epithelium and is upregulated in psoriatic lesions. It inhibits growth of Gram-positive E. coli D21 and Gram-negative B. megatarium in a concentration-dependent manner and LL-37 expression is induced in A549 epithelial cells, alveolar macrophages, neutrophils, and monocyte-derived macrophages following M. tuberculosis infection. LL-37 binds sheep erythrocytes coated with S. minnesota Re-LPS and induces agglutination with a minimal agglutinating concentration (MAC) of 12.1 μg/ml. It is a chemoattractant for, and can induce calcium mobilization in, human monocytes, neutrophils, and T cells that naturally express formyl peptide receptor-like 1 (FPRL1) and FPRL1-transfected HEK293 cells. LL-37 (10-15 μM) pretreatment of dengue virus type 2 (DENV-2) reduces its infectivity as well as levels of viral genomic RNA and NS1 antigen. In vivo, LL-37 inhibits cecal ligation and puncture-induced caspase-1 activation and pyroptosis of peritoneal macrophages, reduces levels of the inflammatory cytokines IL-1β, IL-6, and TNF-α, and improves survival in polybacterial septic mice.
1,2-Dipalmitoyl-13C-sn-glycero-3-PC is intended for use as an internal standard for the quantification of 1,2-dipalmitoyl-sn-glycero-3-PC by GC- or LC-MS. 1,2-Dipalmitoyl-sn-glycero-3-PC (DPPC) is a zwitterionic glycerophospholipid commonly used in the formation of lipid monolayers, bilayers, and liposomes for use in a variety of applications.1,2,3,4 It has been used in the formation of proteoliposomes for implantation of γ-glutamyl transpeptidase into human erythrocyte membranes.3 Incorporation of glycosphingolipid antigens into DPPC-containing liposomes increases the immunogenicity of the antigens in mice.4 |1. Ege, C., and Lee, K.Y.C. Insertion of Alzheimer's Aβ40 peptide into lipid monolayers. Biophys. J. 87(3), 1732-1740 (2004).|2. Leekumjorn, S., and Sum, A.K. Molecular simulation study of structural and dynamic properties of mixed DPPC/DPPE bilayers. Biophys. J. 90(11), 3951-3965 (2006).|3. Kalra, V.K., Sikka, S.C., and Sethi, G.S. Transport of amino acids in γ-glutamyl transpeptidase-implanted human erythrocytes. J. Biol. Chem. 256(11), 5567-5571 (1981).|4. Uemura, A., Watarai, S., Iwasaki, T., et al. Induction of immune responses against glycosphingolipid antigens: Comparison of antibody responses in mice immunized with antigen associated with liposomes prepared from various phospholipids. J. Vet. Med. Sci. 67(12), 1197-1201 (2005).
Temporin A, a short alpha-helical antimicrobial peptide derived from the skin of Rana temporaria, exhibits a wide-ranging efficacy against Gram-positive bacteria. It directly interacts with the cell membrane of microorganisms and remains non-toxic to erythrocytes at antimicrobial concentrations. Additionally, Temporin A demonstrates antifungal properties against yeast-like Candida albicans.
Dibrospidium Free Base is a dispirotripiperazine derivative and alkylating agent with potential antineoplastic and anti-inflammatory activities. The duration of DNA synthesis inhibition in tumor cells was found to correlate with spirobromine antitumor activity. Spirobromin is superior to prospidin by the power of the anti-inflammatory effect. Spyrobromin can diminish the latent period of the development of tumours in the experimental rats at intraperitoneal administration. At intragastric administration of the drug no decrease was noted in the latent period and no increase of tumours was observed in the experimental groups of the animals as compared with control. Dibrospidium has been examined for the treatment of bone cancer. The oral route of administration is the most safe with respect to the oncogenic risk. It was noted that spirobromin exerted the most pronounced toxic action on erythrocytes. Dibrospidium is used for the treatment of acute leukemias (mainly in combinatio......
Pentoxifylline-d6 is intended for use as an internal standard for the quantification of pentoxifylline by GC- or LC-MS. Pentoxifylline is a hemorrheologic agent. It increases the deformability of washed isolated human erythrocytes when used at a concentration of 100 µM. Pentoxifylline (1, 2, and 3 mM) inhibits ADP-induced platelet aggregation in isolated human whole blood. It inhibits thrombus formation induced by ADP in a hamster cheek pouch model when administered at doses of 5, 10, and 20 mg kg. Formulations containing pentoxifylline have been used in the treatment of intermittent claudication.
S6821 is a TAS2R8 antagonist. S6821 was not found to be mutagenic or clastogenic in vitro, and did not induce micronuclei in bone marrow polychromatic erythrocytes in vivo.
Tenellin is a fungal metabolite that inhibits Mg2+-, Ca2+-, and Na+ K+-ATPase activities in erythrocytes. Tenellin is cytotoxic to Sf9 and Sf21 insect cells.