plasma-proteins

Ono-3307 mesylate is a protease inhibitor with inhibitory effects on a variety of proteases.Ono-3307 mesylate has significant protective effects against liver injury in rats and inhibits the deposition of radiofibrillar proteins in the kidneys and lungs.PF-184298 is a protease inhibitor with potential antioxidant effects in plasma and adipose tissue.PF-184298 can be used in the study of pancreatitis.

Cholesteryl linoleate is the major cholesteryl ester in LDL and atherosclerotic lesions. It is present in LDL as a cholesteryl ester that is oxidized to form cholesteryl linoleate hydroperoxides using LDL receptor-associated proteins that are transferred to the plasma membranes of macrophages and CHO cells expressing 15-lipoxygenase.

3-Chloro-L-Tyrosine (Chlorotyrosine), a specific marker of myeloperoxidase-catalyzed oxidation, is markedly elevated in low-density lipoprotein isolated from human atherosclerotic intima. In particular, myeloperoxidase halogenates tyrosine residues in plasma proteins and generates 3-chlorotyrosine (CY). The detection of free chlorotyrosine in blood or urine arises from the degradation of these chlorinated proteins. CY concentrations may be useful for monitoring the activation of neutrophils in asthmatic patients.

DL-Homocysteine thiolactone hydrochloride (DL-Homocysteinethiolactone hydrochloride) is a cysteine derivative that binds to and induces conformational changes in various plasma proteins, slowing coagulation and inducing oxidative stress. It decreases left ventricular systolic blood pressure and cardiac force and induces seizures in vivo.

N-Desmethyl-Apalutamide is a less potent antagonist of the androgen receptor, is an active Apalutamide metabolite.

FKK6 is a selective agonist of the pregnane X receptor (PXR) with an EC50 of 1.2 µM. It demonstrates strong affinity for plasma proteins and exhibits favorable metabolic characteristics in human microsomes. FKK6 inhibits the PXR-related NF-κB signaling pathway, reducing the expression of inflammatory factors and showing anti-inflammatory activity in a mouse model of DSS-induced colitis.

MBX-102 acid is a selective partial PPAR-γ agonist. It binds strongly to plasma proteins, predominantly serum albumin. This compound is utilized in research related to type 2 diabetes.

Diazodiiodoarsenic acid was used to isolate plasma membrane proteins from platelets by means of affinity chromatography.

Iothalamate meglumine, known as radiopaque medium, can be used for urography, angiography, venography, and myelography. It is highly viscous and can bind to plasma proteins.

Palmitic acid-13C is intended for use as an internal standard for the quantification of palmitic acid by GC- or LC-MS. Palmitic acid is a 16-carbon saturated fatty acid. It comprises approximately 25% of human total plasma lipids.1 It increases protein levels of COX-2 in RAW 264.7 cells when used at a concentration of 75 μM.2 Palmitic acid is involved in the acylation of proteins to anchor membrane-bound proteins to the lipid bilayer.2,3,4,5,6 |1. Santos, M.J., López-Jurado, M., Llopis, J., et al. Influence of dietary supplementation with fish oil on plasma fatty acid composition in coronary heart disease patients. Ann. Nutr. Metab. 39(1), 52-62 (1995).|2. Lee, J.Y., Sohn, K.H., Rhee, S.H., et al. Saturated fatty acids, but not unsaturated fatty acids, induced the expression of cyclooxygenase-2 mediated through toll-like receptor 4. J. Biol. Chem. 276(20), 16683-16689 (2001).|3. Dietzen, D.J., Hastings, W.R., and Lublin, D.M. Caveolin is palmitoylated on multiple cysteine residues. Palmitoylation is not necessary for localization of caveolin to caveolae. J. Biol. Chem. 270(12), 6838-6842 (1995).|4. Robinson, L.J., and Michel, T. Mutagenesis of palmitoylation sites in endothelial nitric oxide synthase identifies a novel motif for dual acylation and subcellular targeting. Proc. Nat. Acad. Sci. USA 92(25), 11776-11780 (1995).|5. Topinka, J.R., and Bredt, D.S. N-terminal palmitoylation of PSD-95 regulates association with cell membranes and interaction with K+ channel Kv1.4. Neuron 20(1), 125-134 (1998).|6. Miggin, S.M., Lawler, O.A., and Kinsella, B.T. Palmitoylation of the human prostacyclin receptor. Functional implications of palmitoylation and isoprenylation. J. Biol. Chem. 278(9), 6947-6958 (2003).

Palmitic acid-13C (C1, C2, C3, and C4 labeled) is intended for use as an internal standard for the quantification of palmitic acid by GC- or LC-MS. Palmitic acid is a common 16-carbon saturated fat that represents 10-20% of human dietary fat intake and comprises approximately 25 and 65% of human total plasma lipids and saturated fatty acids, respectively.1,2Acylation of palmitic acid to proteins facilitates anchoring of membrane-bound proteins to the lipid bilayer and trafficking of intracellular proteins, promotes protein-vesicle interactions, and regulates various G protein-coupled receptor functions.1Red blood cell palmitic acid levels are increased in patients with metabolic syndrome compared to patients without metabolic syndrome and are also increased in the plasma of patients with type 2 diabetes compared to individuals without diabetes.3,4 1.Fatima, S., Hu, X., Gong, R.-H., et al.Palmitic acid is an intracellular signaling molecule involved in disease developmentCell. Mol. Life Sci.76(13)2547-2557(2019) 2.Santos, M.J., López-Jurado, M., Llopis, J., et al.Influence of dietary supplementation with fish oil on plasma fatty acid composition in coronary heart disease patientsAnn. Nutr. Metab.39(1)52-62(1995) 3.Yi, L.-Z., He, J., Liang, Y.-Z., et al.Plasma fatty acid metabolic profiling and biomarkers of type 2 diabetes mellitus based on GC/MS and PLS-LDAFEBS Lett.580(30)6837-6845(2006) 4.Kabagambe, E.K., Tsai, M.Y., Hopkins, P.N., et al.Erythrocyte fatty acid composition and the metabolic syndrome: A National Heart, Lung, and Blood Institute GOLDN studyClin. Chem.54(1)154-162(2008)

Palmitic acid-13C is intended for use as an internal standard for the quantification of palmitic acid by GC- or LC-MS. Palmitic acid-13C contains 13C at the C2 position and has been used in the study of free fatty acid incorporation into phospholipid fatty acids in soil microbes.1 Palmitic acid is a 16-carbon saturated fatty acid. It comprises approximately 25% of human total plasma lipids.2 It increases protein levels of COX-2 in RAW 264.7 cells when used at a concentration of 75 μM.3 Palmitic acid is involved in the acylation of proteins to anchor membrane-bound proteins to the lipid bilayer.3,4,5,6,7 |1. Dippold, M.A., and Kuzyakov, Y. Direct incorporation of fatty acids into microbial phospholipids in soils: Position-specific labeling tells the story. Geochim. Cosmochim. Acta 174(1), 211-221 (2016).|2. Santos, M.J., López-Jurado, M., Llopis, J., et al. Influence of dietary supplementation with fish oil on plasma fatty acid composition in coronary heart disease patients. Ann. Nutr. Metab. 39(1), 52-62 (1995).|3. Lee, J.Y., Sohn, K.H., Rhee, S.H., et al. Saturated fatty acids, but not unsaturated fatty acids, induced the expression of cyclooxygenase-2 mediated through toll-like receptor 4. J. Biol. Chem. 276(20), 16683-16689 (2001).|4. Dietzen, D.J., Hastings, W.R., and Lublin, D.M. Caveolin is palmitoylated on multiple cysteine residues. Palmitoylation is not necessary for localization of caveolin to caveolae. J. Biol. Chem. 270(12), 6838-6842 (1995).|5. Robinson, L.J., and Michel, T. Mutagenesis of palmitoylation sites in endothelial nitric oxide synthase identifies a novel motif for dual acylation and subcellular targeting. Proc. Nat. Acad. Sci. USA 92(25), 11776-11780 (1995).|6. Topinka, J.R., and Bredt, D.S. N-terminal palmitoylation of PSD-95 regulates association with cell membranes and interaction with K+ channel Kv1.4. Neuron 20(1), 125-134 (1998).|7. Miggin, S.M., Lawler, O.A., and Kinsella, B.T. Palmitoylation of the human prostacyclin receptor. Functional implications of palmitoylation and isoprenylation. J. Biol. Chem. 278(9), 6947-6958 (2003).

Phosphoramide mustard cyclohexanamine is the active metabolite of cyclophosphamide, an alkylating agent that cross-links DNA strands, organizes cell division and causes cell death, and has antitumor activity.

Endosidin-2 is an exocyst inhibitor, a cell-permeable benzylidene benzoylhydrazine, that binds to the exocyst component of the 70 kDa (EXO70) subunit of the exocyst complex (Kd = 253 μM, EXO70A1).Endosidin-2 disrupts protein translocation between the endosomes and plasma membrane, thereby facilitating translocation of proteins to the vesicle for degradation. It also inhibits recirculation of endocytosed transferrin to the plasma membrane in HeLa cells and targets multiple isoforms of mammalian EXO70, leading to dysregulation of exocytosis.Endosidin2 can be used as a tool molecule to study cytosolization.

CP-609754 (LNK-754) is a potent and reversible farnesyltransferase inhibitor with potential anticancer activity. It inhibits farnesylation of recombinant human H-Ras (IC50=0.57 ng mL) and K-Ras (IC50=46 ng mL)[1]. In 3T3 H-ras (61L)-transfected cell lines, CP-609754 exhibits a slow on off rate, inhibiting mutant H-Ras farnesylation with an IC50 of 1.72 ng mL[1]. The compound is competitive for the prenyl acceptor (H-Ras protein) and noncompetitive for the prenyl donor farnesyl PPI, selectively inhibiting farnesylation of both H- and K-Ras proteins in 3T3 transfectants[1]. In vivo, CP-609754 shows antitumor activity against 3T3 H-ras (61L) tumors, with tumor regression achieved at 100 mg kg twice daily and an ED50 for tumor growth inhibition at 28 mg kg[1]. Continuous i.p. infusion of CP-609754 inhibits tumor growth by over 50% and reduces tumor farnesyltransferase activity by over 30% when plasma concentration is maintained above 118 ng mL[1]. [1]. Stacy L Moulder, et al. A phase I open label study of the farnesyltransferase inhibitor CP-609,754 in patients with advanced malignant tumors. Clin Cancer Res. 2004 Nov 1;10(21):7127-35.

Cholesteryl palmitic acid is a cholesteryl ester. A cholesteryl ester is an ester of cholesterol. Fatty acid esters of cholesterol constitute about two-thirds of the cholesterol in the plasma. Cholesterol is a sterol (a combination of steroid and alcohol) and a lipid found in the cell membranes of all body tissues and transported in the blood plasma of all animals. The accumulation of cholesterol esters in the arterial intima (the innermost layer of an artery, in direct contact with the flowing blood) is a characteristic feature of atherosclerosis. Atherosclerosis is a disease affecting arterial blood vessels. It is a chronic inflammatory response in the walls of arteries, in large part to the deposition of lipoproteins (plasma proteins that carry cholesterol and triglycerides).

AF3442 is a potent and selective mPGES-1 inhibitor (microsomal prostaglandin (PG) E synthase-1). AF3442 caused a concentration-dependent inhibition of PGE(2) in human recombinant mPGES-1 with an IC(50) of 0.06microM. AF3442 is a selective mPGES-1 inhibitor which reduced monocyte PGE(2) generation also in the presence of plasma proteins. Pharmacological inhibition of mPGES-1 did not translate into redirection of PGH(2) metabolism towards other terminal PG synthases in monocytes. The functional relevance of this observation deserves to be investigated in vivo.

pTH-Related Protein (1-40) (human, mouse, rat) enhances calcium absorption in rat intestinal cells by activating the PTHR1 receptor and the PKCα β signaling pathways. This compound also increases the expression of the parathyroid hormone 1 receptor (PTHR1) and four key proteins involved in transcellular calcium transport: potential vanillin member 6 (TRPV6), calcium-binding protein-D9K (CaBP-D9k), sodium-calcium exchanger 1 (NCX1), and plasma membrane calcium ATPase 1 (PMCA1) [1].

Transferrins (Thypinone) are proteins responsible for carrying iron absorbed by the digestive tract and iron released by red blood cell degradation, and are mainly found in plasma. Transferrins have antibacterial and bactericidal activity and can promote the storage and transportation of extracellular iron.

Perforin-IN-2, a benzosulfonamide perforin inhibitor, mitigates transplant rejection in allogeneic bone marrow or stem cell transplantation. It binds to plasma proteins with a binding rate of 99.8%. In vivo, a concentration higher than 900 μM is required for optimal perforin inhibition. Perforin-IN-2 effectively inhibits the lytic activity of recombinant perforin on Jurkat T leukemia cells, with an IC50 of 6.65 μM, and also prevents the death of K562 leukemia target cells [1].

Thio-Miltefosine acts as a modulator in membrane rafts, which are nanoscale assemblies of various lipids and proteins that profoundly influence cellular functions. Additionally, it regulates membrane phase behavior on cell-derived giant plasma membrane vesicles.

Isomucronulatol 7-O-glucoside, a natural product, has a molecular formula of C21H22O11. It is known for its glycosidic linkage between isomucronulatol and glucose, which contributes to its biological activity and potential therapeutic applications. This compound can be isolated from various plant species and has been studied for its pharmacological properties.

[Met5]-Enkephalin, amide is an agonist for δ opioid receptors as well as putative ζ (zeta) opioid receptors. Met-enkephalin circulates in several forms, potentially derived from proteins other than proenkephalin A, and plasma levels of both free native and peptidase-derivable Met-enkephalin are physiologically modulated.

Amyloid A proteins (H2N-Ala-Gly-Leu-Pro-Glu-Lys-Tyr-OH) are a family of apolipoproteins associated with high-density lipoprotein in plasma. Different isoforms of SAA are expressed constitutively at different levels or in response to inflammatory stimuli.