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Plasmin, Human plasma is an important protease present in blood that degrades many plasmaproteins, including fibrin clots. Plasmin can also act as a potent regulator of the immune process and can directly interact with various cell types, including monocytes, macrophages, and dendritic cells .
PM-1, a derivative of Thioflavin-T (ThT; HY-D0218), is a small but highly specific plasma membrane (PM) fluorescent dye for specific and long-time membrane imaging of living and fixed cells. PM-1 is embedded directly into the cell membrane and exhibits a very long retention time on the plasma membrane with a half-life of approximately 15 h. PM-1 can be used in combination with protein labeling probes to study ectodomain shedding and endocytosis processes of cell surface proteins .
S-(2-Carboxyethyl)-L-cysteine (S-Carboxyethylcysteine) is a non-protein (modified) sulfur amino acid. S-(2-Carboxyethyl)-L-cysteine is present in Acacia seed. S-(2-Carboxyethyl)-L-cysteine can affect the seed’s protein use in rats. S-(2-Carboxyethyl)-L-cysteine suppresses the methionine-induced growth rate, and has a negative effect on the plasma amino acid levels in rats .
Torcetrapib (CP-529414) is a selective, potent cholesteryl ester transfer protein (CETP) inhibitor. A typical inhibition curve for whole human plasma, having a CETP concentration of 37 nM .
σ1 Receptor ligand 1 (compound 5I) is a σ1 receptor ligand with a Ki of 3.9 nM. σ1 Receptor ligand 1 has a high plasmaprotein binding (89%) and promising metabolic stability in the presence of mouse liver microsomes and NADPH. σ1 Receptor ligand 1 can be utilized in neurological and cancer research .
Bovine fibrinogen (from fibrinogen) is a native fibrinogen from bovine plasma. Bovine fibrinogen (from fibrinogen) can regulate the activation of NF-KB in endothelial cells and upregulate the expression of inflammatory chemokines MCP-1 .
Haptoglobin, Phenotype 2-2, Human Plasma is a plasmaprotein that binds to hemoglobin for the removal of free hemoglobin (Hb), and exhibits antioxidant activity. Haptoglobin, Phenotype 2-2, Human Plasma can be used in research of renal failure and siabetic cardiovascular disease .
Human Protein Z is a 62 kDa vitamin K-dependent plasmaprotein that serves as a cofactor for the inhibition of factor Xa by protein Z-dependent protease inhibitor (ZPI) .
Human Protein S is a single-chain glycoprotein with a molecular weight of 69 kDa. Human Protein S is a free protein in plasma and can serve as a cofactor for activated protein C to exert its anticoagulant activity .
LOC14 is a potent Protein disulfide isomerase (PDI) inhibitor with EC50 and Kd values of 500 nM and 62 nM, respectively. LOC14 exhibits high stability in mouse liver microsomes and blood plasma, low intrinsic microsome clearance, and low plasma-protein binding .
LOC14 inhibits PDIA3 activity, decreases intramolecular disulfide bonds and subsequent oligomerization (maturation) of HA in lung epithelial cells .
PNU-142633 is a high affinity, selective and orally active 5-HT1D receptor agonist with Kis of 6 nM and > 18 000 nM for human 5-HT1D receptor and human 5-HT1B receptor, respectively. PNU-142633 has anti-migraine efficacy .
Rabbit Serum Albumin is a plasmaprotein derived from rabbits. Serum albumin is a multifunctional protein with extraordinary ligand binding capacity, making it a transporter molecule for a diverse range of metabolites, drugs, nutrients, metals and other molecules .
Goat Serum Albumin is a plasmaprotein derived from goats. Serum albumin is a multifunctional protein with extraordinary ligand binding capacity, making it a transporter molecule for a diverse range of metabolites, drugs, nutrients, metals and other molecules .
Sheep Serum Albumin is a plasmaprotein derived from sheep. Serum albumin is a multifunctional protein with extraordinary ligand binding capacity, making it a transporter molecule for a diverse range of metabolites, drugs, nutrients, metals and other molecules .
Rabbit Serum Albumin (globulin free) is a plasmaprotein derived from rabbits. Serum albumin is a multifunctional protein with extraordinary ligand binding capacity, making it a transporter molecule for a diverse range of metabolites, drugs, nutrients, metals and other molecules .
Evacetrapib is a potent and selective of CETP inhibitor, which inhibits human recombinant CETP protein (IC50 5.5 nM) and CETP activity in human plasma (IC50 36 nM) in vitro.
CETP-IN-3 (Compound 13) is an small molecule inhibitor of the plasma glycoprotein cholesterol ester transfer protein (CETP), elevating HDL-C through inhibition of CETP. CETP-IN-3 for the CETP inhibitory activity in the scintillation proximity (SPA) and whole plasma assay (WPA) with IC50s of 0.002 μM and 0.06 μM, respectively .
PFI-653 (Vanin-1-IN-1, compound 3) is a vanin-1 inhibitor that binds to plasma vanin-1 from mouse, rat, dog, and human. Vanin-1 is a cell surface-associated inositol (GPi) -anchored protein that plays important roles in metabolism and inflammation. PFI-653 inhibits vanin-1 from different species with IC50s of 6.85 nM (human recombinant plasma vanin-1), 9.0 nM (human plasma vanin-1), 24.5 nM (mouse recombinant vanin-1), and 53.4 nM (mouse plasma vanin-1) .
800CW maleimide is an infrared dye that can be used for labeling molecules that contain free sulfhydryl (–SH) groups (Ex: 778 nm; Em: 796 nm). 800CW maleimide binds to plasmaproteins .
Cholesterol is the major sterol in mammals. It is making up 20-25% of structural component of the plasma membrane. Plasma membranes are highly permeable to water but relatively impermeable to ions and protons. Cholesterol plays an important role in determining the fluidity and permeability characteristics of the membrane as well as the function of both the transporters and signaling proteins . Cholesterol is also an endogenous estrogen-related receptor α (ERRα) agonist .
Namoxyrate (Xenbucin (2-dimethylaminoethanol)) is a compound with analgesic activity. It can be dissociated into different components in rats. Its absorption and excretion vary depending on the components, and it has different affinities in human and rat plasmaproteins.
C-Reactive Protein (CRP) is an anti-pneumococcal plasmaprotein that can serve as an inflammatory marker. C-Reactive protein can protect mice from pneumococcal infection by activating complement. C-Reactive protein can inhibit the activation of caspase-3/9 through the CD64/AKT/mTOR pathway, thereby promoting chemotherapy resistance in mice with tongue squamous cell carcinoma .
MBX-102 acid is a selective partial PPAR-γ agonist. MBX-102 acid binds highly to plasmaproteins, mainly serum albumin. MBX-102 acid can be used to study type 2 diabetes .
CP-346086 is a potent and orally active microsomal triglyceride transfer protein (MTP) inhibitor, with an IC50 of 2.0 nM for human and rodent MTP. CP-346086 can lower plasma cholesterol and triglycerides in vivo .
VAP-1-IN-3 (compound 136) is a potent amine oxidase vascular adhesion protein-1 (VAP-1) inhibitor, with an IC50 of 0.13 μM for VAP-1 isolated from bovine plasma. VAP-1-IN-3 can be used for the research of inflammatory .
thio-Miltefosine is a modulator of rafts in membrane tissue. Rafts are nanoscale aggregates of different lipids and proteins that profoundly affect cellular function. Thio-Miltefosine modulates membrane phase behavior on cell-derived giant plasma membrane vesicles .
Dalcetrapib (JTT-705) is an orally active cholesteryl ester transfer protein (CETP) inhibitor with IC50s of 204.6 nM and 6 μM against recombinant human (rh) CETP and human plasma CETP, respectively .
A3G3S3 glycan (A3G3S3 N-linked oligosaccharide) is an N-glycosylated plasmaprotein that plays an important role in indicating different stages of type 1 diabetes .
CP-346086 dihydrate is a potent and orally active microsomal triglyceride transfer protein (MTP) inhibitor, with an IC50 of 2.0 nM for human and rodent MTP. CP-346086 dihydrate can lower plasma cholesterol and triglycerides in vivo .
Cholesterol- 18O is the deuterium labeled Cholesterol. Cholesterol is the major sterol in mammals. It is making up 20-25% of structural component of the plasma membrane. Plasma membranes are highly permeable to water but relatively impermeable to ions and protons. Cholesterol plays an important role in determining the fluidity and permeability characteristics of the membrane as well as the function of both the transporters and signaling proteins . Cholesterol is also an endogenous estrogen-related receptor α (ERRα) agonist .
Cholesterol-d1 is the deuterium labeled Cholesterol. Cholesterol is the major sterol in mammals. It is making up 20-25% of structural component of the plasma membrane. Plasma membranes are highly permeable to water but relatively impermeable to ions and protons. Cholesterol plays an important role in determining the fluidity and permeability characteristics of the membrane as well as the function of both the transporters and signaling proteins . Cholesterol is also an endogenous estrogen-related receptor α (ERRα) agonist .
Cholesterol-d7 is the deuterium labeled Cholesterol. Cholesterol is the major sterol in mammals. It is making up 20-25% of structural component of the plasma membrane. Plasma membranes are highly permeable to water but relatively impermeable to ions and protons. Cholesterol plays an important role in determining the fluidity and permeability characteristics of the membrane as well as the function of both the transporters and signaling proteins . Cholesterol is also an endogenous estrogen-related receptor α (ERRα) agonist .
Cholesterol-d6 is the deuterium labeled Cholesterol. Cholesterol is the major sterol in mammals. It is making up 20-25% of structural component of the plasma membrane. Plasma membranes are highly permeable to water but relatively impermeable to ions and protons. Cholesterol plays an important role in determining the fluidity and permeability characteristics of the membrane as well as the function of both the transporters and signaling proteins . Cholesterol is also an endogenous estrogen-related receptor α (ERRα) agonist .
Cholesterol- 13C3 is the 13C-labeled Cholesterol. Cholesterol is the major sterol in mammals. It is making up 20-25% of structural component of the plasma membrane. Plasma membranes are highly permeable to water but relatively impermeable to ions and protons. Cholesterol plays an important role in determining the fluidity and permeability characteristics of the membrane as well as the function of both the transporters and signaling proteins . Cholesterol is also an endogenous estrogen-related receptor α (ERRα) agonist .
Cholesterol (Standard) is the analytical standard of Cholesterol. This product is intended for research and analytical applications. Cholesterol is the major sterol in mammals. It is making up 20-25% of structural component of the plasma membrane. Plasma membranes are highly permeable to water but relatively impermeable to ions and protons. Cholesterol plays an important role in determining the fluidity and permeability characteristics of the membrane as well as the function of both the transporters and signaling proteins . Cholesterol is also an endogenous estrogen-related receptor α (ERRα) agonist .
Cholesterol-d4 is deuterium labeled Cholesterol. Cholesterol is the major sterol in mammals. It is making up 20-25% of structural component of the plasma membrane. Plasma membranes are highly permeable to water but relatively impermeable to ions and protons. Cholesterol plays an important role in determining the fluidity and permeability characteristics of the membrane as well as the function of both the transporters and signaling proteins . Cholesterol is also an endogenous estrogen-related receptor α (ERRα) agonist .
Cholesterol-d6-1 is the deuterium labeled Cholesterol. Cholesterol is the major sterol in mammals. It is making up 20-25% of structural component of the plasma membrane. Plasma membranes are highly permeable to water but relatively impermeable to ions and protons. Cholesterol plays an important role in determining the fluidity and permeability characteristics of the membrane as well as the function of both the transporters and signaling proteins . Cholesterol is also an endogenous estrogen-related receptor α (ERRα) agonist .
Cholesterol- 13C2 is the 13C labeled Cholesterol. Cholesterol is the major sterol in mammals. It is making up 20-25% of structural component of the plasma membrane. Plasma membranes are highly permeable to water but relatively impermeable to ions and protons. Cholesterol plays an important role in determining the fluidity and permeability characteristics of the membrane as well as the function of both the transporters and signaling proteins . Cholesterol is also an endogenous estrogen-related receptor α (ERRα) agonist .
Cholesterol- 13C5 is the 13C-labeled Cholesterol. Cholesterol is the major sterol in mammals. It is making up 20-25% of structural component of the plasma membrane. Plasma membranes are highly permeable to water but relatively impermeable to ions and protons. Cholesterol plays an important role in determining the fluidity and permeability characteristics of the membrane as well as the function of both the transporters and signaling proteins . Cholesterol is also an endogenous estrogen-related receptor α (ERRα) agonist .
BMS-795311 is a potent and orally bioavailable inhibitor of cholesteryl ester transfer protein (CETP), with IC50s of 4 nM in an enzyme-based scintillation proximity assay (SPA) and 0.22 μM in a human whole plasma assay (hWPA), respectively .
OSBPL7-IN-1 is an orally active oxysterol binding protein like 7 (OSBPL7) inhibitor. OSBPL7-IN-1 promotes an increase of ABCA1 at the plasma membrane without affecting mRNA expression .
Felotaxel (SHR110008) is a derivate of Docetaxel (HY-B0011), with antitumor activity and specific pharmacokinetic properties in rats. Felotaxel is rapidly distributed to normal tissues. The kidney is the major excretion organ, and its plasmaprotein binding capacity is nearly linearly related to concentration.
Cholesterol Water Soluble is a major sterol in mammals, constituting 20-25% of the structural composition of the plasma membrane. The plasma membrane is highly permeable to water but relatively impermeable to ions and protons. Cholesterol Water Soluble plays an important role in determining the fluidity and permeability characteristics of membranes and the function of transporters and signaling proteins. Cholesterol Water Soluble is also an endogenous estrogen-related receptor alpha (ERRα) agonist. Cholesterol Water Soluble can be used to study the effects of cholesterol on potassium currents in inner hair cells .
ML753286 is an orally active and selective BCRP (Breast cancer resistance protein) inhibitor with an IC50 of 0.6 μM. ML753286 has high permeability and low to medium clearance in rodent and human liver S9 fractions, and is stable in plasma cross species .
L57 exhibits high affinity to the low-density lipoprotein receptor-related protein 1 (LRP1) with Ki of 45 nM. L57 exhibits blood-brain barrier (BBB) permeability and plasma stability. L57 can be utilized as the carrier for CNS drug delivery .
Lp(a)-IN-5 (Compound A) is an orally active lipoprotein (a) (Lp(a)) inhibitor. Lp(a)-IN-5 inhibits the assembly of Apo(a) and ApoB proteins with an IC50 value of 0.41 nM. Lp(a)-IN-5 is promising for research of diseases related to elevated plasma Lp(a) levels, such as cardiovascular diseases .
BI-4924 is a lipophilic, highly plasmaprotein bound selective phosphoglycerate dehydrogenase (PHGDH) inhibitor (IC50=3 nM) with excellent microsomal, as well as hepatocytic stability. Intracellular trapping of BI-4924 disrupts serine biosynthesis with an IC50 of 2200 nM at 72 h .
Antibacterial agent 138 is a benzothiazole inhibitor of bacterial DNA gyrase and topoisomerase IV. Antibacterial agent 138 exhibits favorable solubility and plasmaprotein binding. Antibacterial agent 138 has antibacterial activity against Gram-positive and Gram-negative strains. Antibacterial agent 138 is a dual GyrB and ParE inhibitor .
Antimycobacterial agent-8 (Compound 49) is an inhibitor for DNA gyrase. Antimycobacterial agent-8 exhibits antibacterial activity against Mycobacterium tuberculosis and M. abscessus with MIC90 of 2.5 μM and 0.63 μM. Antimycobacterial agent-8 exhibits good plasmaprotein binding ability in mice .
Plasminogen, Human plasma is a secreted protein that upon cleavage by urokinase plasminogen activator (uPA) or tissue plasminogen activator (tPA) is converted to plasmin, a broad range protease capable of cleaving fibrin and other ECM components. Plasminogen also is a proinflammatory regulator that accelerates the healing of acute and diabetic wounds. Plasminogen can be used in studies of wound healing, inflammation and hypoplasminogenemia .
E17241 is an inducer of the expression of ABCA1 that increases the protein levels of ABCA1 in RAW 264.7 macrophages. E17241 is also an agonist of peroxisome proliferator-activated receptors (PPARs ). E17241 decreases plasma glucose levels and body weight in KKAy diabetic mice fed a high-fat and high-glucose (HFHG) diet .
L 743310 is a non-peptide, selective antagonist of the human neurokinin hNK1 receptor, with high affinity for primate and cloned human hNK1 receptors and lower affinity for rodent NK1 receptors. L 743310 inhibits resiniferatoxin-induced plasmaprotein extravasation in guinea pig esophagus. L 743310 has a dose-dependent inhibitory effect on cisplatin-induced emesis .
Evinacumab (REGN1500) is a human anti-ANGPTL3 (angiopoietin-like protein 3) monoclonal antibody (IgG4 class antibody). Evinacumab reduces plasma lipids in dyslipidemic mice by blocking ANGPTL3. Evinacumab can be used in studies of homozygous familial hypercholesterolaemia (HoFH), refractory hypercholesterolaemia (both familial and non-familial) and severe hypertriglyceridaemia .
Corr4A is a chemical corrector, which can be used for cystic fibrosis. Corr4A interacts directly with the cystic fibrosis transmembrane conductance regulator (CFTR) or affects indirectly its folding process. Corr4A increases the expression of CFTR ΔF508 on the cell surface, thereby improving its transport to the plasma membrane and increasing the stability of the rescued mutant protein .
Human serum albumin (HSA) is the most abundant protein in plasma and is a major determinant of plasma oncotic pressure. Human serum albumin exhibits antioxidant, anticoagulant, anti-inflammatory, anti-platelet aggregation activities as well as colloid osmotic action. Human serum albumin can block the inhibitory effect of GML on human T cells, providing protective function for T cells. Human serum albumin is also associated with cardiovascular diseases and can partially prevent the LPS (HY-D1056) induced oxidative stress, as well as the upregulation of NF-κB, NF-κB, and peroxynitrite (ONOO −) in the vascular wall, contributing to the reduction of blood pressure .
PAT-048 is a potent, selective and orally active autotaxin inhibitor, inhibits IL-6 mRNA expression, but shows no effect on autotaxin protein and pulmonary lysophosphatidic acid (LPA) production in lung fibrosis model. PAT-048 shows an IC50 and IC90 of 20 nM and 200 nM for autotaxin in mouse plasma. PAT-048 reduces dermal fibrosis in vivo .
(6R)-ML753286 is an isomer of ML753286 (HY-116494). ML753286 is an orally active and selective BCRP (Breast cancer resistance protein) inhibitor with an IC50 of 0.6 μM. ML753286 has high permeability and low to medium clearance in rodent and human liver S9 fractions, and is stable in plasma cross species .
ST-148 is a novel small molecule compound that has potent inhibitory effects against all four dengue virus serotypes. In the nonlethal AG129 mouse dengue virus infection model, ST-148 significantly reduced viremia and viral load in vital organs and tended to reduce plasma cytokine levels. Compound resistance was associated with the dengue virus capsid (C) gene, and the direct interaction of ST-148 with the C protein was presumed to be achieved through the protein's built-in fluorescence change in the presence of the compound. Therefore, ST-148 appears to interact with the dengue virus C protein and inhibit one or more unique steps of the viral replication cycle.
AMG-222 is a dipeptidyl peptidase IV (DPP-IV) inhibitor that exerts its inhibitory effect by tightly and reversibly binding to DPPIV. AMG 222 binds to human plasmaproteins in a saturable and concentration-dependent manner, with a binding rate of 80.8% at 1 nM, while the binding rate decreases to 29.4% at concentrations above 100 nM. AMG-222 can be used in research related to diabetes .
DMP 323 is a potent, nonpeptide cyclic urea inhibitor of HIV protease, effective against both HIV type 1 and type 2. Designed using structural information and database searching, it competitively inhibits the cleavage of both peptide and HIV-1 gag polyprotein substrates. DMP 323 shows comparable potency to other highly effective HIV protease inhibitors like A-80987 and Ro-31-8959. Importantly, its efficacy against HIV protease remains unaffected by human plasma or serum, suggesting low affinity for plasmaproteins. Furthermore, DMP 323 demonstrates minimal inhibition of various mammalian proteases at concentrations much higher than those needed for HIV protease inhibition, highlighting its specificity for viral targets .
Gramicidin S is a cationic cyclic peptide antibiotic that selectively targets bacterial cell membranes and has anticancer activity. Gramicidin S also exerts antibacterial activity by destroying membrane integrity and interfering with membrane protein function. Gramicidin S inserts into the phospholipid bilayer through hydrophobic amino acid residues, specifically binds to negatively charged membrane lipids and disrupts membrane structure, thereby inhibiting cell division and cell wall synthesis, and ultimately causing bacterial death. Gramicidin S also inhibits ion channels, with IC50s of 41 μM, 24 μM, and 3 μM for Na +/K +-ATPase, tobacco leaf plasma membrane Mg 2+/K +-ATPase, and rat heart plasma membrane Ca 2+-ATPase, respectively .
Dextran-CY5.5 is a CY5.5 (HY-D0924) labeled Dextran (HY-112624) conjugate. CY5.5 is a Cyanine dye (The excitation wavelength is usually 673nm and the emission wavelength is 707nm) that can be used for the labeling of proteins, antibodies and small molecular compounds. Dextran has an inhibitory effect on thrombocyte aggregation and coagulation factors and is used as a plasma volume expander .
FKK6 is a selective agonist for pregnane X receptor (PXR) with an EC50 of 1.2 µM. FKK6 exhibits good affinity with plasmaproteins, and good metabolic metabolism in human microsomes. FKK6 inhibits PXR-related NF-κB signaling pathway, inhibits the expression of inflammatory factors, and exhibits anti-inflammatory activity against DSS (HY-116282)-induced colitis in mouse model .
N-Desmethyl Apalutamide is an active metabolite of Apalutamide. N-Desmethyl Apalutamide is a less potent antagonist of the androgen receptor and is responsible for one-third of the activity of Apalutamide. The formation of N-Desmethyl Apalutamide mediated predominantly by CYP2C8 and CYP3A4. N-Desmethyl Apalutamide is moderate to strong CYP3A4 and CYP2B6 inducer and has an excellent plasma-proteins bound concentration .
ALN29882 is a glycerolipid located on the plasma membrane. It consists of two fatty acid chains covalently linked to a single glycerol molecule by means of an ester bond. 18:1 DG has been used as a source of diacylglycerol in the diacylglycerol O-acyltransferase 1 (DGAT1) assay. It is also used as a substrate in the DGAT-1 enzyme assay to evaluate compounds as potential inhibitors of DGAT-1. Suitable for lipoprotein overlay screening assays with the recombinant protein His-AtROP6.
ES9-17 is an analog of ES9 (endosidin9), which is an inhibitor of clathrin heavy chain (CHC). ES9-17 is an inhibitor of clathrin-mediated endocytosis (CME), a major route for internalization of plasma membrane proteins and molecules from the extracellular environment in plants. ES9-17 inhibits the uptake of transferrin and FM4-64. ES9-17 also inhibits root growth of Arabidopsis seedings .
Halofenate, structurally akin to clofibrate, was evaluated in hypertriglyceridemic patients over 6-week periods in a controlled, double-blind crossover trial. It effectively reduced serum triglycerides by 50%, with minimal impact on serum cholesterol levels. Additionally, it lowered serum uric acid by 30% and exhibited uricosuric effects independent of glomerular filtration rate. Halofenate was associated with a significant increase in plasma thyroxine (T4), accompanied by a decrease in protein-bound iodine and T4 by column. In vitro studies confirmed its ability to displace T4 from thyroid-binding proteins, suggesting a thyroxine-displacing effect, which could influence thyroid function in vivo .
SPSB2-iNOS inhibitory cyclic peptide-1 is an inhibitor for the interaction of SPRY domain and SOCS-box protein 2 (SPSB2) and iNOS, through binding SPSB2 on iNOS site with KD of 4.4 nM. SPSB2-iNOS inhibitory cyclic peptide-1 is resistant to the proteases pepsin, trypsin and α-chymotrypsin. SPSB2-iNOS inhibitory cyclic peptide-1 is stable in human plasma and in oxidative environment .
Human serum albumin (Cell culture grade, Endotoxin<0.125 EU/mg) (HSA) is the most abundant protein in plasma and is a major determinant of plasma oncotic pressure. Human serum albumin (Cell culture grade, Endotoxin<0.125 EU/mg) exhibits antioxidant, anticoagulant, anti-inflammatory, anti-platelet aggregation activities as well as colloid osmotic action. Human serum albumin (Cell culture grade, Endotoxin<0.125 EU/mg) can block the inhibitory effect of GML on human T cells, providing protective function for T cells. Human serum albumin (Cell culture grade, Endotoxin<0.125 EU/mg) is also associated with cardiovascular diseases and can partially prevent the LPS (HY-D1056) induced oxidative stress, as well as the upregulation of NF-κB, iNOS, and peroxynitrite (ONOO −) in the vascular wall, contributing to the reduction of blood pressure .
C18 LPA (PA(18:0e/0:0)) is a water-soluble phospholipid that functions as a signaling molecule, influencing various cellular responses through G protein-coupled receptors (GPCRs). It is known to promote smooth muscle contraction, cytoskeletal rearrangement, and chemotaxis, while also playing a role in neurotransmitter release, cell proliferation, platelet aggregation, and Ca2+ mobilization. Elevated levels of C18 LPA in human plasma are associated with ovarian cancer and atherosclerosis, suggesting its potential as a biomarker for ovarian cancer.
ZD6021 is an orally active Neurokinin 1 Receptor antagonist, with Ki values of 0.12 nM for NK1 and 0.62 nM for NK2. At a concentration of 100 nM, ZD6021 has a pKB value of 8.9 for human pulmonary artery NK1 receptors, and a pKB value of 7.3 for human bronchial NK2 receptors. ZD6021 effectively reduces ASMSP-induced plasmaprotein extravasation in guinea pigs, with an ED50 of 0.5 mg/kg, and also decreases NK2 mediated bronchoconstriction, with an ED50 of 13 mg/kg .
Perforin-IN-2 is a benzosulfonamide perforin inhibitor that alleviates transplant rejection during allogeneic bone marrow/stem cell transplantation. Perforin-IN-2 binds to plasmaproteins with a binding rate of 99.8%. Perforin-IN-2 requires a higher concentration (> 900 μM) to achieve optimal perforin inhibition in vivo. Perforin-in-2 can effectively inhibit the lytic activity of recombinant perforin on Jurkat T (IC50=6.65 μM) leukemia cells, and also inhibit the death of K562 leukemia target cells .
N-Desmethyl apalutamide-d4 is the deuterium-labeled N-Desmethyl-Apalutamide (HY-135331). N-Desmethyl Apalutamide is an active metabolite of Apalutamide. N-Desmethyl Apalutamide is a less potent antagonist of the androgen receptor and is responsible for one-third of the activity of Apalutamide. The formation of N-Desmethyl Apalutamide mediated predominantly by CYP2C8 and CYP3A4. N-Desmethyl Apalutamide is moderate to strong CYP3A4 and CYP2B6 inducer and has an excellent plasma-proteins bound concentration .
5-HT7 receptor ligand 2 (compound 32) is an arylpiperazinehydrazine ligand for 5-HT7R (Ki=178 nM). 5-HT7 receptor ligand 2 has good membrane permeability, low hepatotoxicity and cardiotoxicity, and high plasmaprotein binding. 5-HT7 receptor ligand 2 shows neuroprotective effects in SH-SY5Y cells and can be used for the study of central nervous system related diseases .
Paritaprevir (ABT-450) is a potent, orally active and antiviral non-structural protein 3/4A (NS3/4A) protease inhibitor with EC50s of 1 and 0.21 nM against HCV 1a and 1b, respectively. Paritaprevir is also a SARS-CoV 3CL pro inhibitor with an IC50 of 1.31 μM. Paritaprevir is metabolized primarily by cytochrome P450 (CYP) 3A. The plasma concentration and half-life of Paritaprevir can be enhanced by Ritonavir (a CYP450 inhibitor) .
306-N16B is a selective lung-targeted lipid nanoparticle that reversibly targets lung endothelial cells and specific immune cells through selective adsorption of a protein corona mediated by differences in tail structure (such as fibrinogen β/γ chain). 306-N16B binds to specific plasmaproteins in the blood to form a protein corona, which guides the particles to be enriched in the lungs, releases mRNA and promotes target cell gene expression, exerts efficient lung cell transfection activity, and can precisely regulate gene delivery of different cell types in the lungs (such as endothelial cells and macrophages). 306-N16B can be used in gene therapy technologies for hereditary lung diseases including pulmonary lymphangioleiomyomatosis (LAM), restoring tumor suppressor function by delivering Tsc2 mRNA, and can also be used for lung-specific mRNA vaccines and gene editing therapies .
ML350 (CYM50202) is a highly potent OPRK1 antagonist with selectivity and broad biological applications. With IC50 values of 9-16 nM, ML350 shows high selectivity for OPRK1, with selectivity of 219-382-fold and 20-35-fold relative to OPRD1 and OPRM1, respectively. ML350 exhibited favorable characteristics in in vivo pharmacokinetic analysis, including high passive membrane permeability and moderate human plasmaprotein binding. Extensive screening of ML350 against multiple ion channels, receptors, and transporters showed that it does not have adverse off-target effects .
1-Stearoyl-sn-glycerol 3-phosphate sodium is a bioactive phospholipid that plays a crucial role in modulating cellular processes such as motility, proliferation, invasion, survival, and growth factor production, primarily through its interaction with G protein-coupled receptors (GPCRs). Typically found at low concentrations in plasma (~100nM), this compound is synthesized during the formation of membrane phospholipids and is derived from various cell types, including activated platelets, epithelial cells, leukocytes, neuronal cells, and tumor cells. Its unique structure includes stearic acid at the sn-1 position alongside a hydroxyl group at the sn-2 position.
(Rac)-Telinavir ((Rac)-SC-52151) is a potent, selective, tight-binding human immunodeficiency virus (HIV) protease inhibitor that exhibits significant anti-HIV activity. (Rac)-Telinavir has a mean 50% effective concentration of 26 ng/ml (43 nM) against various strains of HIV, including HIV-1, HIV-2, and simian immunodeficiency virus. (Rac)-Telinavir, in combination with nucleoside reverse transcriptase inhibitors, demonstrates synergistic effects on inhibiting HIV-1 replication without additive toxicity. (Rac)-Telinavir is highly protein bound in human plasma and exhibits low partitioning into erythrocytes.
N-Desmethyl-Apalutamide-15N,d4 is the 15N and deuterium labeled isotope of N-Desmethyl-Apalutamide (HY-135331). N-Desmethyl Apalutamide is an active metabolite of Apalutamide. N-Desmethyl Apalutamide is a less potent antagonist of the androgen receptor and is responsible for one-third of the activity of Apalutamide. The formation of N-Desmethyl Apalutamide mediated predominantly by CYP2C8 and CYP3A4. N-Desmethyl Apalutamide is moderate to strong CYP3A4 and CYP2B6 inducer and has an excellent plasma-proteins bound concentration .
Paritaprevir (ABT-450) dihydrate is a potent, orally active and antiviral non-structural protein 3/4A (NS3/4A) protease inhibitor with EC50s of 1 and 0.21 nM against HCV 1a and 1b, respectively. Paritaprevir dihydrate is also a SARS-CoV 3CL pro inhibitor with an IC50 of 1.31 μM. Paritaprevir dihydrate is metabolized primarily by cytochrome P450 (CYP) 3A. The plasma concentration and half-life of Paritaprevir dihydrate can be enhanced by Ritonavir (a CYP450 inhibitor) .
NU227326 is the PROTAC degrader for Indoleamine 2,3-dioxygenase 1 (IDO1) with DC50 of 4.5 nM. NU227326 degrades IDO1 in cell U87 and GBM43 with DC50 of 7.1 nM and 11.8 nM. NU227326 exhibits good pharmacokinetic properties with a plasma half-life of 5.7 hours and a brain tissue half-life of 11.8 hours .(Pink: ligand for target protein IDO1 ligand-1 (HY-173067); Black: linker (HY-173068); Blue: ligand for E3 ligase Cereblon (HY-W087383))
Antimicrobial agent-34 (compound 4h) is an antibacterial agent (MIC = 1–4 μg/mL), with a clogP value of 9.14. Antimicrobial agent-34 has good plasma stability (HC50 of 131.1 μg/mL) and good membrane selectivity (HC50/MIC is 65.6), with rapid sterilization capability. Antimicrobial agent-34 destroys the integrity of bacterial cell membranes, induces an increase in intracellular reactive oxygen species, and leaks protein and DNA, ultimately leading to bacterial death. Antimicrobial agent-34 demonstrates significant in vivo antibacterial potency in a mouse sepsis model infected with Staphylococcus aureus ATCC43300 .
LacCer (d18:1/16:0) (C16 Lactosylceramide (d18:1/16:0)) is an endogenous bioactive sphingolipid that can form membrane microdomains with Lyn kinase and the αi subunits of inhibitory G protein-coupled receptors (GPCRs). The levels of LacCer (d18:1/16:0) are elevated in the plasma of insulin-resistant cattle. In a mouse model of Niemann-Pick type C1 disease (a neurodegenerative cholesterol-sphingolipid lysosomal storage disorder), the expression of LacCer (d18:1/16:0) is also upregulated. LacCer (d18:1/16:0) can be used in research on metabolic diseases and neurodegenerative diseases .
SPSB2-iNOS inhibitory cyclic peptide-1 TFA is the TFA salt form of SPSB2-iNOS inhibitory cyclic peptide-1(HY-P10383). SPSB2-iNOS inhibitory cyclic peptide-1 is an inhibitor for the interaction of SPRY domain and SOCS-box protein 2 (SPSB2) and iNOS, through binding SPSB2 on iNOS site with KD of 4.4 nM. SPSB2-iNOS inhibitory cyclic peptide-1 is resistant to the proteases pepsin, trypsin and α-chymotrypsin. SPSB2-iNOS inhibitory cyclic peptide-1 is stable in human plasma and in oxidative environment .
TRV120027, a β-arrestin-1-biased agonist of the angiotensin II receptor type 1 (AT1R), engages ?-arrestins while blocking G-protein signaling . TRV120027?induces?acute?catecholamine?secretion?through cation channel subfamily C3 (TRPC3) coupling, promotes the formation of a macromolecular complex composed of AT1R–β-arrestin-1–TRPC3–PLCγ at the plasma membrane. TRV120027 inhibits angiotensin II–mediated vasoconstriction and increases cardiomyocyte contractility. TRV120027 has the potential for the?acute decompensated heart failure (ADHF) treatment .
TRV120027 TFA, a β-arrestin-1-biased agonist of the angiotensin II receptor type 1 (AT1R), engages ?-arrestins while blocking G-protein signaling . TRV120027?TFA induces?acute?catecholamine?secretion?through cation channel subfamily C3 (TRPC3) coupling, promotes the formation of a macromolecular complex composed of AT1R–β-arrestin-1–TRPC3–PLCγ at the plasma membrane. TRV120027 TFA inhibits angiotensin II–mediated vasoconstriction and increases cardiomyocyte contractility. TRV120027 TFA has the potential for the?acute decompensated heart failure (ADHF) treatment .
Oleuropein Aglycone (3,4-DHPEA-EA) is a polyphenol and the aglycone form of oleuropein (HY-N0292), formed by enzymatic, acidic or acetylated hydrolysis of oleuropein. Dietary intake of oleuropein Aglycone (50 mg/kg diet) increases the number of neuronal autophagic vesicles, reverses cognitive deficits in the TgCRND8 transgenic mouse model of Alzheimer's disease, and reduces the levels of histone deacetylase 2 (HDAC2) in the cortex and hippocampus. Oleuropein Aglycone increases urinary norepinephrine, interscapular brown adipose tissue epinephrine, and UCP1 protein levels, and reduced plasmaleptin levels and total abdominal adipose tissue weight in a rat model of high-fat diet-induced obesity. Oleuropein Aglycone also reduced lung neutrophil infiltration, lipid peroxidation, and IL-1β levels in a mouse model of carrageenan-induced pleurisy.
Alpha 2 Macroglobulin, Human Plasma, Fast Form is a broad-spectrum protease inhibitor, representing the fast form (Fast Form) of Alpha 2 Macroglobulin. Alpha 2 Macroglobulin also has a slow form (Slow Form). The slow form of Alpha 2 Macroglobulin can lure active proteases into its molecular cage and subsequently "tag" its complex for elimination. The fast form of Alpha 2 Macroglobulin is an allosteric product of the slow form, generated when proteases are captured by A2M bait regions, leading to chemical cleavage of internal thioester bonds near the bait regions. Alpha 2 Macroglobulin also promotes cell migration and binds cytokines, growth factors, and damaged extracellular proteins. Alpha 2 Macroglobulin holds research significance in inflammation, immunity, and infection .
ITK degrader 1 is a highly selective degrader of interleukin-2-inducible T-cell kinase (ITK; DC50=3.6 nM in vivo in mice), with good plasma exposure levels. ITK degrader 1 induces rapid, and prolonged ITK degradation and suppresses IL-2 secretion (EC50=35.2 nM, Jurkat cells) stimulated by anti-CD3 antibodyin vivo. ITK degrader 1 consists of target protein ligand (red part) ITK ligand 1 (HY-168387), PROTAC linker (black part) Piperidine-C2-piperazine-Boc (HY-168388) and E3 ubiquitinase ligand (blue part) Thalidomide 5-fluoride (HY-W087383). E3 ubiquitinase and PROTAC linker can form Thalidomide-piperidine-C2-piperazine-Boc (HY-168389) .
Membrane receptors, also known cell surface receptors or transmembrane receptors, are transmembrane proteins embedded into the plasma membrane which play an essential role in maintaining communication between the internal processes within the cell and various types of extracellular signals. They act in cell signaling by receiving (binding to) extracellular molecules, which are also called ligands. These extracellular molecules include hormones, cytokines, growth factors, neurotransmitters, lipophilic signaling molecules such as prostaglandins, and cell recognition molecules.
There are three kinds of membrane receptors: ion channel-linked receptors, enzyme-linked receptors and G-protein-linked receptors. They play important roles in keeping human normal physiologic processes. GPCRs and ion channels are important drug targets in drug discovery.
MCE provides a unique collection of 5,773 compounds targeting a variety of membrane receptors. MCE Membrane reeptor-targeted Compound Library can be used for membrane receptor-focused screening and drug discovery.
Extracellular vesicles (EVs) are small membrane binding structures that are released from cells into the surrounding environment and play a crucial role in mediating and regulating intercellular communication related to physiological and pathological processes. EVs are lipid membrane vesicles composed of proteins, lipids, and nucleic acids. EVs can be divided into several types based on their source, such as extracellular vesicles, microcapsules, and apoptotic vesicles. The size range of exosomes is 30-150nm, which are endocrine in multi vesicular endosomes (MVEs); microvesicles (50-1000nm) are secreted directly through extracellular interactions, thereby releasing plasma membrane vesicles. In contrast, apoptotic bodies are usually larger, ranging in size from 1 to 5 μ m. This is generated during programmed cell death. EV plays a crucial role in transmitting information between cells and influencing the behavior and function of receptor cells.
MCE designs a unique collection of 504 small molecules related to extracellular vesicles (EVs). It is a good tool to be used for research on metabolize, cancer and other diseases.
PM-1, a derivative of Thioflavin-T (ThT; HY-D0218), is a small but highly specific plasma membrane (PM) fluorescent dye for specific and long-time membrane imaging of living and fixed cells. PM-1 is embedded directly into the cell membrane and exhibits a very long retention time on the plasma membrane with a half-life of approximately 15 h. PM-1 can be used in combination with protein labeling probes to study ectodomain shedding and endocytosis processes of cell surface proteins .
800CW maleimide is an infrared dye that can be used for labeling molecules that contain free sulfhydryl (–SH) groups (Ex: 778 nm; Em: 796 nm). 800CW maleimide binds to plasmaproteins .
Dextran-CY5.5 is a CY5.5 (HY-D0924) labeled Dextran (HY-112624) conjugate. CY5.5 is a Cyanine dye (The excitation wavelength is usually 673nm and the emission wavelength is 707nm) that can be used for the labeling of proteins, antibodies and small molecular compounds. Dextran has an inhibitory effect on thrombocyte aggregation and coagulation factors and is used as a plasma volume expander .
Cholesterol is the major sterol in mammals. It is making up 20-25% of structural component of the plasma membrane. Plasma membranes are highly permeable to water but relatively impermeable to ions and protons. Cholesterol plays an important role in determining the fluidity and permeability characteristics of the membrane as well as the function of both the transporters and signaling proteins . Cholesterol is also an endogenous estrogen-related receptor α (ERRα) agonist .
Cholesterol Water Soluble is a major sterol in mammals, constituting 20-25% of the structural composition of the plasma membrane. The plasma membrane is highly permeable to water but relatively impermeable to ions and protons. Cholesterol Water Soluble plays an important role in determining the fluidity and permeability characteristics of membranes and the function of transporters and signaling proteins. Cholesterol Water Soluble is also an endogenous estrogen-related receptor alpha (ERRα) agonist. Cholesterol Water Soluble can be used to study the effects of cholesterol on potassium currents in inner hair cells .
Human serum albumin (HSA) is the most abundant protein in plasma and is a major determinant of plasma oncotic pressure. Human serum albumin exhibits antioxidant, anticoagulant, anti-inflammatory, anti-platelet aggregation activities as well as colloid osmotic action. Human serum albumin can block the inhibitory effect of GML on human T cells, providing protective function for T cells. Human serum albumin is also associated with cardiovascular diseases and can partially prevent the LPS (HY-D1056) induced oxidative stress, as well as the upregulation of NF-κB, NF-κB, and peroxynitrite (ONOO −) in the vascular wall, contributing to the reduction of blood pressure .
ALN29882 is a glycerolipid located on the plasma membrane. It consists of two fatty acid chains covalently linked to a single glycerol molecule by means of an ester bond. 18:1 DG has been used as a source of diacylglycerol in the diacylglycerol O-acyltransferase 1 (DGAT1) assay. It is also used as a substrate in the DGAT-1 enzyme assay to evaluate compounds as potential inhibitors of DGAT-1. Suitable for lipoprotein overlay screening assays with the recombinant protein His-AtROP6.
Bovine fibrinogen (from fibrinogen) is a native fibrinogen from bovine plasma. Bovine fibrinogen (from fibrinogen) can regulate the activation of NF-KB in endothelial cells and upregulate the expression of inflammatory chemokines MCP-1 .
Rabbit Serum Albumin is a plasmaprotein derived from rabbits. Serum albumin is a multifunctional protein with extraordinary ligand binding capacity, making it a transporter molecule for a diverse range of metabolites, drugs, nutrients, metals and other molecules .
Goat Serum Albumin is a plasmaprotein derived from goats. Serum albumin is a multifunctional protein with extraordinary ligand binding capacity, making it a transporter molecule for a diverse range of metabolites, drugs, nutrients, metals and other molecules .
Sheep Serum Albumin is a plasmaprotein derived from sheep. Serum albumin is a multifunctional protein with extraordinary ligand binding capacity, making it a transporter molecule for a diverse range of metabolites, drugs, nutrients, metals and other molecules .
Rabbit Serum Albumin (globulin free) is a plasmaprotein derived from rabbits. Serum albumin is a multifunctional protein with extraordinary ligand binding capacity, making it a transporter molecule for a diverse range of metabolites, drugs, nutrients, metals and other molecules .
A3G3S3 glycan (A3G3S3 N-linked oligosaccharide) is an N-glycosylated plasmaprotein that plays an important role in indicating different stages of type 1 diabetes .
Human serum albumin (Cell culture grade, Endotoxin<0.125 EU/mg) (HSA) is the most abundant protein in plasma and is a major determinant of plasma oncotic pressure. Human serum albumin (Cell culture grade, Endotoxin<0.125 EU/mg) exhibits antioxidant, anticoagulant, anti-inflammatory, anti-platelet aggregation activities as well as colloid osmotic action. Human serum albumin (Cell culture grade, Endotoxin<0.125 EU/mg) can block the inhibitory effect of GML on human T cells, providing protective function for T cells. Human serum albumin (Cell culture grade, Endotoxin<0.125 EU/mg) is also associated with cardiovascular diseases and can partially prevent the LPS (HY-D1056) induced oxidative stress, as well as the upregulation of NF-κB, iNOS, and peroxynitrite (ONOO −) in the vascular wall, contributing to the reduction of blood pressure .
306-N16B is a selective lung-targeted lipid nanoparticle that reversibly targets lung endothelial cells and specific immune cells through selective adsorption of a protein corona mediated by differences in tail structure (such as fibrinogen β/γ chain). 306-N16B binds to specific plasmaproteins in the blood to form a protein corona, which guides the particles to be enriched in the lungs, releases mRNA and promotes target cell gene expression, exerts efficient lung cell transfection activity, and can precisely regulate gene delivery of different cell types in the lungs (such as endothelial cells and macrophages). 306-N16B can be used in gene therapy technologies for hereditary lung diseases including pulmonary lymphangioleiomyomatosis (LAM), restoring tumor suppressor function by delivering Tsc2 mRNA, and can also be used for lung-specific mRNA vaccines and gene editing therapies .
S-(2-Carboxyethyl)-L-cysteine (S-Carboxyethylcysteine) is a non-protein (modified) sulfur amino acid. S-(2-Carboxyethyl)-L-cysteine is present in Acacia seed. S-(2-Carboxyethyl)-L-cysteine can affect the seed’s protein use in rats. S-(2-Carboxyethyl)-L-cysteine suppresses the methionine-induced growth rate, and has a negative effect on the plasma amino acid levels in rats .
C-Reactive Protein (CRP) is an anti-pneumococcal plasmaprotein that can serve as an inflammatory marker. C-Reactive protein can protect mice from pneumococcal infection by activating complement. C-Reactive protein can inhibit the activation of caspase-3/9 through the CD64/AKT/mTOR pathway, thereby promoting chemotherapy resistance in mice with tongue squamous cell carcinoma .
Gramicidin S is a cationic cyclic peptide antibiotic that selectively targets bacterial cell membranes and has anticancer activity. Gramicidin S also exerts antibacterial activity by destroying membrane integrity and interfering with membrane protein function. Gramicidin S inserts into the phospholipid bilayer through hydrophobic amino acid residues, specifically binds to negatively charged membrane lipids and disrupts membrane structure, thereby inhibiting cell division and cell wall synthesis, and ultimately causing bacterial death. Gramicidin S also inhibits ion channels, with IC50s of 41 μM, 24 μM, and 3 μM for Na +/K +-ATPase, tobacco leaf plasma membrane Mg 2+/K +-ATPase, and rat heart plasma membrane Ca 2+-ATPase, respectively .
SPSB2-iNOS inhibitory cyclic peptide-1 is an inhibitor for the interaction of SPRY domain and SOCS-box protein 2 (SPSB2) and iNOS, through binding SPSB2 on iNOS site with KD of 4.4 nM. SPSB2-iNOS inhibitory cyclic peptide-1 is resistant to the proteases pepsin, trypsin and α-chymotrypsin. SPSB2-iNOS inhibitory cyclic peptide-1 is stable in human plasma and in oxidative environment .
TRV120027, a β-arrestin-1-biased agonist of the angiotensin II receptor type 1 (AT1R), engages ?-arrestins while blocking G-protein signaling . TRV120027?induces?acute?catecholamine?secretion?through cation channel subfamily C3 (TRPC3) coupling, promotes the formation of a macromolecular complex composed of AT1R–β-arrestin-1–TRPC3–PLCγ at the plasma membrane. TRV120027 inhibits angiotensin II–mediated vasoconstriction and increases cardiomyocyte contractility. TRV120027 has the potential for the?acute decompensated heart failure (ADHF) treatment .
TRV120027 TFA, a β-arrestin-1-biased agonist of the angiotensin II receptor type 1 (AT1R), engages ?-arrestins while blocking G-protein signaling . TRV120027?TFA induces?acute?catecholamine?secretion?through cation channel subfamily C3 (TRPC3) coupling, promotes the formation of a macromolecular complex composed of AT1R–β-arrestin-1–TRPC3–PLCγ at the plasma membrane. TRV120027 TFA inhibits angiotensin II–mediated vasoconstriction and increases cardiomyocyte contractility. TRV120027 TFA has the potential for the?acute decompensated heart failure (ADHF) treatment .
L57 exhibits high affinity to the low-density lipoprotein receptor-related protein 1 (LRP1) with Ki of 45 nM. L57 exhibits blood-brain barrier (BBB) permeability and plasma stability. L57 can be utilized as the carrier for CNS drug delivery .
SPSB2-iNOS inhibitory cyclic peptide-1 TFA is the TFA salt form of SPSB2-iNOS inhibitory cyclic peptide-1(HY-P10383). SPSB2-iNOS inhibitory cyclic peptide-1 is an inhibitor for the interaction of SPRY domain and SOCS-box protein 2 (SPSB2) and iNOS, through binding SPSB2 on iNOS site with KD of 4.4 nM. SPSB2-iNOS inhibitory cyclic peptide-1 is resistant to the proteases pepsin, trypsin and α-chymotrypsin. SPSB2-iNOS inhibitory cyclic peptide-1 is stable in human plasma and in oxidative environment .
Evinacumab (REGN1500) is a human anti-ANGPTL3 (angiopoietin-like protein 3) monoclonal antibody (IgG4 class antibody). Evinacumab reduces plasma lipids in dyslipidemic mice by blocking ANGPTL3. Evinacumab can be used in studies of homozygous familial hypercholesterolaemia (HoFH), refractory hypercholesterolaemia (both familial and non-familial) and severe hypertriglyceridaemia .
Cholesterol is the major sterol in mammals. It is making up 20-25% of structural component of the plasma membrane. Plasma membranes are highly permeable to water but relatively impermeable to ions and protons. Cholesterol plays an important role in determining the fluidity and permeability characteristics of the membrane as well as the function of both the transporters and signaling proteins . Cholesterol is also an endogenous estrogen-related receptor α (ERRα) agonist .
Cholesterol (Standard) is the analytical standard of Cholesterol. This product is intended for research and analytical applications. Cholesterol is the major sterol in mammals. It is making up 20-25% of structural component of the plasma membrane. Plasma membranes are highly permeable to water but relatively impermeable to ions and protons. Cholesterol plays an important role in determining the fluidity and permeability characteristics of the membrane as well as the function of both the transporters and signaling proteins . Cholesterol is also an endogenous estrogen-related receptor α (ERRα) agonist .
Cholesterol Water Soluble is a major sterol in mammals, constituting 20-25% of the structural composition of the plasma membrane. The plasma membrane is highly permeable to water but relatively impermeable to ions and protons. Cholesterol Water Soluble plays an important role in determining the fluidity and permeability characteristics of membranes and the function of transporters and signaling proteins. Cholesterol Water Soluble is also an endogenous estrogen-related receptor alpha (ERRα) agonist. Cholesterol Water Soluble can be used to study the effects of cholesterol on potassium currents in inner hair cells .
LacCer (d18:1/16:0) (C16 Lactosylceramide (d18:1/16:0)) is an endogenous bioactive sphingolipid that can form membrane microdomains with Lyn kinase and the αi subunits of inhibitory G protein-coupled receptors (GPCRs). The levels of LacCer (d18:1/16:0) are elevated in the plasma of insulin-resistant cattle. In a mouse model of Niemann-Pick type C1 disease (a neurodegenerative cholesterol-sphingolipid lysosomal storage disorder), the expression of LacCer (d18:1/16:0) is also upregulated. LacCer (d18:1/16:0) can be used in research on metabolic diseases and neurodegenerative diseases .
Plasma kallikrein (KLKB1) serves as an enzyme, cleaving Lys-Arg and Arg-Ser bonds to release bradykinin from HMW kininogen. It plays a crucial role in the reciprocal activation of factor XII, especially upon binding to a negatively charged surface. Besides its role in the kinin system, KLKB1 may contribute to the renin-angiotensin system by converting prorenin into renin. Plasma kallikrein/KLKB1 Protein, Human (HEK293, His, solution) is the recombinant human-derived Plasma kallikrein/KLKB1 protein, expressed by HEK293 , with C-His labeled tag. The total length of Plasma kallikrein/KLKB1 Protein, Human (HEK293, His, solution) is 619 a.a., with molecular weight of 72-80 kDa.
Plasma kallikrein (KLKB1) serves as an enzyme, cleaving Lys-Arg and Arg-Ser bonds to release bradykinin from HMW kininogen. It plays a crucial role in the reciprocal activation of factor XII, especially upon binding to a negatively charged surface. Besides its role in the kinin system, KLKB1 may contribute to the renin-angiotensin system by converting prorenin into renin. Plasma kallikrein/KLKB1 Protein, Cynomolgus (HEK293, His) is the recombinant cynomolgus-derived Plasma kallikrein/KLKB1 protein, expressed by HEK293 , with C-His labeled tag. The total length of Plasma kallikrein/KLKB1 Protein, Cynomolgus (HEK293, His) is 619 a.a., with molecular weight of 70-90 kDa.
Plasma kallikrein (KLKB1) serves as an enzyme, cleaving Lys-Arg and Arg-Ser bonds to release bradykinin from HMW kininogen. It plays a crucial role in the reciprocal activation of factor XII, especially upon binding to a negatively charged surface. Besides its role in the kinin system, KLKB1 may contribute to the renin-angiotensin system by converting prorenin into renin. Plasma kallikrein/KLKB1 Protein, Human (HEK293, His) is the recombinant human-derived Plasma kallikrein/KLKB1 protein, expressed by HEK293 , with C-His labeled tag. The total length of Plasma kallikrein/KLKB1 Protein, Human (HEK293, His) is 619 a.a., with molecular weight of 72-80 kDa.
Plasma kallikrein/KLKB1 enzymatically cleaves Lys-Arg and Arg-Ser bonds, triggering factor XII activation upon binding to a negatively charged surface.It liberates bradykinin from HMW kininogen and is implicated in the renin-angiotensin system, potentially converting prorenin into renin.This underscores the diverse and essential functions of Plasma kallikrein/KLKB1 in various physiological processes.Plasma kallikrein/KLKB1 Protein, Mouse (HEK293, His) is the recombinant mouse-derived Plasma kallikrein/KLKB1 protein, expressed by HEK293 , with C-6*His labeled tag.
Plasma kallikrein/KLKB1 enzymatically cleaves Lys-Arg and Arg-Ser bonds, triggering factor XII activation upon binding to a negatively charged surface.It liberates bradykinin from HMW kininogen and is implicated in the renin-angiotensin system, potentially converting prorenin into renin.This underscores the diverse and essential functions of Plasma kallikrein/KLKB1 in various physiological processes.Plasma kallikrein/KLKB1 Protein, Mouse (HEK293, His) is the recombinant mouse-derived Plasma kallikrein/KLKB1 protein, expressed by HEK293 , with C-His labeled tag.
RBP4 protein acts as a retinol-binding protein, essential for transporting retinol in blood plasma. It facilitates the delivery of retinol from the liver to peripheral tissues and likely transfers bound all-trans retinol to STRA6 for cell membrane transport. Interactions with TTR prevent kidney glomeruli filtration loss. Direct interaction with STRA6 underscores RBP4's role in intricate retinol transport and distribution processes in the body. RBP4 Protein, Human (HEK293, hFc) is the recombinant human-derived RBP4 protein, expressed by HEK293 , with C-hFc labeled tag. The total length of RBP4 Protein, Human (HEK293, hFc) is 183 a.a., with molecular weight of ~50 kDa.
RBP4 Protein transports retinol in blood plasma, delivering it from the liver to peripheral tissues. It binds to all-trans retinol, transferring it to STRA6 for cell membrane transport. RBP4 interacts with TTR, preventing kidney filtration, and further aids STRA6 in retinol transport. RBP4 Protein, Rat (HEK293, His) is the recombinant rat-derived RBP4 protein, expressed by HEK293 , with C-His labeled tag. The total length of RBP4 Protein, Rat (HEK293, His) is 183 a.a., with molecular weight of ~24 kDa.
RBP4 Protein transports retinol in blood plasma, delivering it from liver stores to peripheral tissues. Binding to all-trans retinol, it transfers it to STRA6 for efficient cell membrane transport. RBP4 interacts with TTR, preventing kidney filtration, and further supports STRA6 in retinol transport. RBP4 Protein, Mouse (HEK293, His) is the recombinant mouse-derived RBP4 protein, expressed by HEK293 , with C-His labeled tag. The total length of RBP4 Protein, Mouse (HEK293, His) is 183 a.a., with molecular weight of ~22.8 kDa.
RBP4 Protein is a member of the lipocalin family and the major transport protein of the hydrophobic molecule retinol, also known as vitamin A, in the circulation. RBP4 Protein, Canine (HEK293, Fc) is the recombinant canine-derived RBP4 protein, expressed by HEK293 , with C-hFc labeled tag.
RBP4 Protein is a member of the lipocalin family and the major transport protein of the hydrophobic molecule retinol, also known as vitamin A, in the circulation. RBP4 Protein, Canine (HEK293, His) is the recombinant canine-derived RBP4 protein, expressed by HEK293 , with C-His labeled tag. The total length of RBP4 Protein, Canine (HEK293, His) is 183 a.a., with molecular weight of ~23 kDa.
CASK protein is a Mg(2+)-independent multidomain scaffold kinase that catalyzes phosphate transfer to proteins, including NRXN1, thereby contributing to synaptic transmembrane protein anchoring and ion channel trafficking. It plays a critical role in neural development, regulation of gene expression through TBR1 interactions, and mediates connections between the extracellular matrix, multiligands, and the actin cytoskeleton. CASK Protein, Human (sf9) is the recombinant human-derived CASK protein, expressed by Sf9 insect cells , with tag free. The total length of CASK Protein, Human (sf9) is 897 a.a., with molecular weight of ~102 kDa.
RBP4 protein acts as a retinol-binding protein, essential for transporting retinol in blood plasma. It facilitates the delivery of retinol from the liver to peripheral tissues and likely transfers bound all-trans retinol to STRA6 for cell membrane transport. Interactions with TTR prevent kidney glomeruli filtration loss. Direct interaction with STRA6 underscores RBP4's role in intricate retinol transport and distribution processes in the body. RBP4 Protein, Human (HEK293, C-His) is the recombinant human-derived RBP4 protein, expressed by HEK293 , with C-6*His labeled tag. The total length of RBP4 Protein, Human (HEK293, C-His) is 183 a.a., with molecular weight of ~21 kDa.
RBP4 protein acts as a retinol-binding protein, essential for transporting retinol in blood plasma. It facilitates the delivery of retinol from the liver to peripheral tissues and likely transfers bound all-trans retinol to STRA6 for cell membrane transport. Interactions with TTR prevent kidney glomeruli filtration loss. Direct interaction with STRA6 underscores RBP4's role in intricate retinol transport and distribution processes in the body. RBP4 Protein, Human is the recombinant human-derived RBP4 protein, expressed by E. coli , with tag free. The total length of RBP4 Protein, Human is 183 a.a., with molecular weight of ~20.0 kDa.
RBP4 Protein, a vital retinol transporter in blood plasma, mediates the transfer from liver stores to peripheral tissues. It also enhances retinol transport by interacting with TTR. RBP4 Protein, Cynomolgus (HEK293, His) is the recombinant cynomolgus-derived RBP4 protein, expressed by HEK293 , with C-His labeled tag. The total length of RBP4 Protein, Cynomolgus (HEK293, His) is 183 a.a., with molecular weight of ~23 kDa.
PSP94/MSMB protein forms homodimers and interacts with PI16. PSP94/MSMB Protein, Human (His) is the recombinant human-derived PSP94/MSMB protein, expressed by E. coli , with C-His labeled tag.
HABP2 is a protein that cleaves the alpha chain of fibrinogen as well as the beta chain between "Lys-53" and "Lys-54" at multiple sites, preventing direct formation of a fibrin clot. It activates coagulation factor VII and converts prourokinase into its active form. HABP2 Protein, Human (HEK293, His) is the recombinant human-derived HABP2 protein, expressed by HEK293 , with C-6*His labeled tag.
PGCP is a carboxypeptidase with a potentially critical role in the hydrolysis of circulating peptides. It catalyzes the cleavage of terminally unsubstituted dipeptides, releasing amino acids. PGCP Protein, Mouse (HEK293, His) is the recombinant mouse-derived PGCP protein, expressed by HEK293 , with C-6*His labeled tag. The total length of PGCP Protein, Mouse (HEK293, His) is 452 a.a., with molecular weight of ~60.0 kDa.
Plasma kallikrein/KLKB1 enzymatically cleaves Lys-Arg and Arg-Ser bonds, triggering factor XII activation upon binding to a negatively charged surface.It liberates bradykinin from HMW kininogen and is implicated in the renin-angiotensin system, potentially converting prorenin into renin.This highlights the protein's multifaceted role in various physiological processes.Plasma kallikrein/KLKB1 Protein, Rat (P.pastoris, His) is the recombinant rat-derived Plasma kallikrein/KLKB1 protein, expressed by P.pastoris , with N-6*His labeled tag.
Serpin G1, also known as C1 inhibitor, controls C1 complex activation by forming a proteolytically inactive complex with C1r or C1s proteases. Their interactions regulate physiological pathways such as complement activation, coagulation, fibrinolysis, and kinin production. Serpin G1 Protein, Human (HEK293, His) is the recombinant human-derived Serpin G1 protein, expressed by HEK293 , with C-10*His labeled tag.
Serpin G1 protein binds complement and inhibits serine-type endopeptidases. It is located in the extracellular space and is involved in aging. Serpin G1 Protein, Rat (HEK293, His) is the recombinant rat-derived Serpin G1 protein, expressed by HEK293 , with C-His labeled tag.
Serpin A5 protein is a heparin-dependent serine protease inhibitor that controls proteolytic activity in body fluids. It binds irreversibly to the serine activation site, inactivating serine proteases and regulating intravascular and extravascular proteolysis. Serpin A5 Protein, Mouse (Baculovirus, His) is the recombinant mouse-derived Serpin A5 protein, expressed by Sf9 insect cells , with N-10*His labeled tag. The total length of Serpin A5 Protein, Mouse (Baculovirus, His) is 381 a.a., with molecular weight of ~45.3 kDa.
Carboxypeptidase B2 Protein, Human (HEK293, His) is an approximately 47.0 kDa human carboxypeptidase B2 with a His-flag. Carboxypeptidase B2 is a enzyme belonging to the peptidase M14 family and hydrolyze C-terminal peptide bonds.
Plasma serine protease inhibitor (SERPINA5) is a glycoproteins that inhibit serine proteases. SERPINA5 is involved in the regulation of intravascular and extravascular proteolytic activities, controls the sperm motility and fertilization and protect components of the genital tract. SERPINA5 also inhibits urinary-type plasminogen activator-dependent tumor cell invasion and metastasis. Serpin A5 Protein, Human (HEK293, His) is the recombinant human-derived Serpin A5 protein, expressed by HEK293 , with C-6*His labeled tag. The total length of Serpin A5 Protein, Human (HEK293, His) is 387 a.a., with molecular weight of 44-55 kDa.
Serpin G1 protein, also known as C1 inhibitor, regulates complement activation, coagulation, fibrinolysis, and kinin production. It forms an inactive complex with C1r or C1s protease and controls C1 complex activation. Serpin G1 Protein, Mouse (HEK293, His) is the recombinant mouse-derived Serpin G1 protein, expressed by HEK293 , with C-6*His labeled tag. The total length of Serpin G1 Protein, Mouse (HEK293, His) is 485 a.a., with molecular weight of 92-95 kDa.
Coagulation factor XI (F11) occupies a central position in the middle phase of the intrinsic pathway of blood coagulation, where it assumes the key role of activating factor IX. This complex process plays a key role in the chain of events that lead to the formation of a blood clot. Coagulation Factor XI/F11 Protein, Human (His) is the recombinant human-derived Coagulation Factor XI/F11 protein, expressed by E. coli , with N-6*His labeled tag.
Factor IX (F9) is a vitamin K-dependent plasma protein that plays a critical role in the intrinsic pathway of coagulation. Factor IX coordinates the conversion of factor X to its active form in the presence of Ca(2+) ions, phospholipids, and factor VIIIa. Coagulation factor IX/F9 Protein, Human (HEK293, His) is the recombinant human-derived Coagulation factor IX/F9 protein, expressed by HEK293 , with C-6*His labeled tag.
The PLA2G7 protein is a lipoprotein-associated calcium-independent phospholipase A2 that plays a key role in phospholipid catabolism during inflammation and oxidative stress responses.It acts at the lipid-water interface and hydrolyzes the ester bond of the fatty acyl group at the sn-2 position, with particular preference for short-chain fatty acyl groups.PLA2G7 Protein, Mouse (Baculovirus, N-His, C-Myc) is the recombinant mouse-derived PLA2G7 protein, expressed by Sf9 insect cells , with C-Myc, N-10*His labeled tag.
The PLA2G7 protein is a lipoprotein-associated calcium-independent phospholipase A2 that plays a key role in phospholipid catabolism during inflammation and oxidative stress responses.It acts at the lipid-water interface and hydrolyzes the ester bond of the fatty acyl group at the sn-2 position, with particular preference for short-chain fatty acyl groups.PLA2G7 Protein, Mouse (HEK293, N-His, C-Myc) is the recombinant mouse-derived PLA2G7 protein, expressed by HEK293 , with C-Myc, N-10*His labeled tag.
Cholesterol-d1 is the deuterium labeled Cholesterol. Cholesterol is the major sterol in mammals. It is making up 20-25% of structural component of the plasma membrane. Plasma membranes are highly permeable to water but relatively impermeable to ions and protons. Cholesterol plays an important role in determining the fluidity and permeability characteristics of the membrane as well as the function of both the transporters and signaling proteins . Cholesterol is also an endogenous estrogen-related receptor α (ERRα) agonist .
Cholesterol-d7 is the deuterium labeled Cholesterol. Cholesterol is the major sterol in mammals. It is making up 20-25% of structural component of the plasma membrane. Plasma membranes are highly permeable to water but relatively impermeable to ions and protons. Cholesterol plays an important role in determining the fluidity and permeability characteristics of the membrane as well as the function of both the transporters and signaling proteins . Cholesterol is also an endogenous estrogen-related receptor α (ERRα) agonist .
Cholesterol-d6 is the deuterium labeled Cholesterol. Cholesterol is the major sterol in mammals. It is making up 20-25% of structural component of the plasma membrane. Plasma membranes are highly permeable to water but relatively impermeable to ions and protons. Cholesterol plays an important role in determining the fluidity and permeability characteristics of the membrane as well as the function of both the transporters and signaling proteins . Cholesterol is also an endogenous estrogen-related receptor α (ERRα) agonist .
Cholesterol- 13C3 is the 13C-labeled Cholesterol. Cholesterol is the major sterol in mammals. It is making up 20-25% of structural component of the plasma membrane. Plasma membranes are highly permeable to water but relatively impermeable to ions and protons. Cholesterol plays an important role in determining the fluidity and permeability characteristics of the membrane as well as the function of both the transporters and signaling proteins . Cholesterol is also an endogenous estrogen-related receptor α (ERRα) agonist .
Cholesterol-d4 is deuterium labeled Cholesterol. Cholesterol is the major sterol in mammals. It is making up 20-25% of structural component of the plasma membrane. Plasma membranes are highly permeable to water but relatively impermeable to ions and protons. Cholesterol plays an important role in determining the fluidity and permeability characteristics of the membrane as well as the function of both the transporters and signaling proteins . Cholesterol is also an endogenous estrogen-related receptor α (ERRα) agonist .
Cholesterol-d6-1 is the deuterium labeled Cholesterol. Cholesterol is the major sterol in mammals. It is making up 20-25% of structural component of the plasma membrane. Plasma membranes are highly permeable to water but relatively impermeable to ions and protons. Cholesterol plays an important role in determining the fluidity and permeability characteristics of the membrane as well as the function of both the transporters and signaling proteins . Cholesterol is also an endogenous estrogen-related receptor α (ERRα) agonist .
Cholesterol- 13C2 is the 13C labeled Cholesterol. Cholesterol is the major sterol in mammals. It is making up 20-25% of structural component of the plasma membrane. Plasma membranes are highly permeable to water but relatively impermeable to ions and protons. Cholesterol plays an important role in determining the fluidity and permeability characteristics of the membrane as well as the function of both the transporters and signaling proteins . Cholesterol is also an endogenous estrogen-related receptor α (ERRα) agonist .
Cholesterol- 13C5 is the 13C-labeled Cholesterol. Cholesterol is the major sterol in mammals. It is making up 20-25% of structural component of the plasma membrane. Plasma membranes are highly permeable to water but relatively impermeable to ions and protons. Cholesterol plays an important role in determining the fluidity and permeability characteristics of the membrane as well as the function of both the transporters and signaling proteins . Cholesterol is also an endogenous estrogen-related receptor α (ERRα) agonist .
N-Desmethyl apalutamide-d4 is the deuterium-labeled N-Desmethyl-Apalutamide (HY-135331). N-Desmethyl Apalutamide is an active metabolite of Apalutamide. N-Desmethyl Apalutamide is a less potent antagonist of the androgen receptor and is responsible for one-third of the activity of Apalutamide. The formation of N-Desmethyl Apalutamide mediated predominantly by CYP2C8 and CYP3A4. N-Desmethyl Apalutamide is moderate to strong CYP3A4 and CYP2B6 inducer and has an excellent plasma-proteins bound concentration .
Cholesterol- 18O is the deuterium labeled Cholesterol. Cholesterol is the major sterol in mammals. It is making up 20-25% of structural component of the plasma membrane. Plasma membranes are highly permeable to water but relatively impermeable to ions and protons. Cholesterol plays an important role in determining the fluidity and permeability characteristics of the membrane as well as the function of both the transporters and signaling proteins . Cholesterol is also an endogenous estrogen-related receptor α (ERRα) agonist .
N-Desmethyl-Apalutamide-15N,d4 is the 15N and deuterium labeled isotope of N-Desmethyl-Apalutamide (HY-135331). N-Desmethyl Apalutamide is an active metabolite of Apalutamide. N-Desmethyl Apalutamide is a less potent antagonist of the androgen receptor and is responsible for one-third of the activity of Apalutamide. The formation of N-Desmethyl Apalutamide mediated predominantly by CYP2C8 and CYP3A4. N-Desmethyl Apalutamide is moderate to strong CYP3A4 and CYP2B6 inducer and has an excellent plasma-proteins bound concentration .
FKK6 is a selective agonist for pregnane X receptor (PXR) with an EC50 of 1.2 µM. FKK6 exhibits good affinity with plasmaproteins, and good metabolic metabolism in human microsomes. FKK6 inhibits PXR-related NF-κB signaling pathway, inhibits the expression of inflammatory factors, and exhibits anti-inflammatory activity against DSS (HY-116282)-induced colitis in mouse model .
Cholesterol is the major sterol in mammals. It is making up 20-25% of structural component of the plasma membrane. Plasma membranes are highly permeable to water but relatively impermeable to ions and protons. Cholesterol plays an important role in determining the fluidity and permeability characteristics of the membrane as well as the function of both the transporters and signaling proteins . Cholesterol is also an endogenous estrogen-related receptor α (ERRα) agonist .
Cholesterol Water Soluble is a major sterol in mammals, constituting 20-25% of the structural composition of the plasma membrane. The plasma membrane is highly permeable to water but relatively impermeable to ions and protons. Cholesterol Water Soluble plays an important role in determining the fluidity and permeability characteristics of membranes and the function of transporters and signaling proteins. Cholesterol Water Soluble is also an endogenous estrogen-related receptor alpha (ERRα) agonist. Cholesterol Water Soluble can be used to study the effects of cholesterol on potassium currents in inner hair cells .
306-N16B is a selective lung-targeted lipid nanoparticle that reversibly targets lung endothelial cells and specific immune cells through selective adsorption of a protein corona mediated by differences in tail structure (such as fibrinogen β/γ chain). 306-N16B binds to specific plasmaproteins in the blood to form a protein corona, which guides the particles to be enriched in the lungs, releases mRNA and promotes target cell gene expression, exerts efficient lung cell transfection activity, and can precisely regulate gene delivery of different cell types in the lungs (such as endothelial cells and macrophages). 306-N16B can be used in gene therapy technologies for hereditary lung diseases including pulmonary lymphangioleiomyomatosis (LAM), restoring tumor suppressor function by delivering Tsc2 mRNA, and can also be used for lung-specific mRNA vaccines and gene editing therapies .
C18 LPA (PA(18:0e/0:0)) is a water-soluble phospholipid that functions as a signaling molecule, influencing various cellular responses through G protein-coupled receptors (GPCRs). It is known to promote smooth muscle contraction, cytoskeletal rearrangement, and chemotaxis, while also playing a role in neurotransmitter release, cell proliferation, platelet aggregation, and Ca2+ mobilization. Elevated levels of C18 LPA in human plasma are associated with ovarian cancer and atherosclerosis, suggesting its potential as a biomarker for ovarian cancer.
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