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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 .
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 .
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.
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 .
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 .
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 .
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 .
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 .
Cholesterol-d 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 .
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-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- 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-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- 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 .
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-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-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- 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 (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 .
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 .
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 .
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 .
Cholera toxin (Choleragen), an AB(5)-subunit toxin, enters host cells by binding the ganglioside GM1 at the plasma membrane (PM) and travels retrograde through the trans-Golgi Network into the endoplasmic reticulum (ER) . Choleragen activates adenylate cyclase by catalyzing ADP-ribosylation of Gs alpha, the stimulatory guanine nucleotide-binding protein .
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 .
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 .
Coixol (6-Methoxy-2-benzoxazolinone; 6-MBOA) is a potent and orally active anti-inflammatory agent. Coixol decreases the iNOS protein expression. Coixol inhibits the production of TNF-α, IL-6, and IL-1β. Coixol improves glucose tolerance and plasma insulin. Coixol decreases the blood glucose level .
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 .
C5a Receptor agonist, mouse, human is a biological active peptide. (This peptide is derived from the C-terminus of the chemokine, complement fragment 5 anaphylatoxin (C5a). This peptide functions as a C5a receptor agonist. C5a is a plasmaprotein involved in cellular inflammatory processes by inducing chemotaxis, degranulation of leukocytes, increased vascular permeability, and cytokine production. The cyclohexylalanine at position 5 is crucial to agonist function. Arg at the last position is of the d-isomer.)
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 .
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.
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) .
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 .
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 .
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) .
TRV120027 TFA, a β-arrestin-1-biased agonist of the angiotensin II receptor type 1 (AT1R), engages ß-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 .
TRV120027, a β-arrestin-1-biased agonist of the angiotensin II receptor type 1 (AT1R), engages ß-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 .
5-HT7R antagonist 2 (compound 4h) is a 5-HT7R antagonist that antagonizes the G protein and β-arrestin signaling pathways, with a Ki of 67 nM, the IC50 values in cAMP and Tango tests were 2.59 μM and 39.57 μM, respectively. 5-HT7R antagonist 2 has an effect on neurogenesis and can reduce repetitive behaviors related to autism spectrum disorder (ASD) and restore neurogenesis of ASD impairment .
Pharmacokinetic Analysis ICR Male Mice
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 4627 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 401 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 .
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 .
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.
Plasmin 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 .
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 .
TRV120027 TFA, a β-arrestin-1-biased agonist of the angiotensin II receptor type 1 (AT1R), engages ß-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 .
TRV120027, a β-arrestin-1-biased agonist of the angiotensin II receptor type 1 (AT1R), engages ß-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 .
C5a Receptor agonist, mouse, human is a biological active peptide. (This peptide is derived from the C-terminus of the chemokine, complement fragment 5 anaphylatoxin (C5a). This peptide functions as a C5a receptor agonist. C5a is a plasmaprotein involved in cellular inflammatory processes by inducing chemotaxis, degranulation of leukocytes, increased vascular permeability, and cytokine production. The cyclohexylalanine at position 5 is crucial to agonist function. Arg at the last position is of the d-isomer.)
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 .
Coixol (6-Methoxy-2-benzoxazolinone; 6-MBOA) is a potent and orally active anti-inflammatory agent. Coixol decreases the iNOS protein expression. Coixol inhibits the production of TNF-α, IL-6, and IL-1β. Coixol improves glucose tolerance and plasma insulin. Coixol decreases the blood glucose level .
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 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. The total length of Plasma kallikrein/KLKB1 Protein, Mouse (HEK293, His) is 619 a.a., with molecular weight of 75-85 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.
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. The total length of RBP4 Protein, Canine (HEK293, Fc) is 201 a.a., with molecular weight of ~53 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, 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.
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, His-GST) is the recombinant human-derived CASK protein, expressed by Sf9 insect cells , with N-His, N-GST labeled tag. The total length of CASK Protein, Human (sf9, His-GST) is 897 a.a., with molecular weight of ~120 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. The total length of PSP94/MSMB Protein, Human (His) is 94 a.a., with molecular weight of ~14 kDa.
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. The total length of HABP2 Protein, Human (HEK293, His) is 256 a.a., with molecular weight of 35-40 kDa.
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. The total length of Plasma kallikrein/KLKB1 Protein, Rat (P.pastoris, His) is 248 a.a., with molecular weight of ~34 kDa.
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. The total length of Serpin G1 Protein, Rat (HEK293, His) is 482 a.a., with molecular weight of ~ 70-95 kDa.
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.
Serpin G1, also known as C1-inhibitor, controls C1 complex activation by forming a proteolytically inactive complex with C1r or C1s proteases. Its interactions regulate physiological pathways like complement activation, blood coagulation, fibrinolysis, and kinin generation. As a potent inhibitor of FXIIa, chymotrypsin, and kallikrein, Serpin G1 binds to E. coli stcE, protecting against complement-mediated lysis, and engages with MASP1, showcasing its intricate involvement in various cellular processes. Serpin G1 Protein, Human (500a.a, HEK293, His) is the recombinant human-derived Serpin G1 protein, expressed by HEK293, with C-10*His labeled tag. The total length of Serpin G1 Protein, Human (500a.a, HEK293, His) is 478 a.a., with molecular weight of ~110 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.
Serpin G1 Protein, also called C1-inhibitor, regulates complement activation, blood coagulation, fibrinolysis, and kinin generation. It forms inactive complexes with C1r or C1s proteases, controlling C1 complex activation. Serpin G1 efficiently inhibits FXIIa and possibly chymotrypsin and kallikrein, and interacts with MASP1. Its inhibitory effects maintain pathway balance, preventing excessive activation and ensuring proper physiological function. 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.
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.
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. The total length of Coagulation Factor XI/F11 Protein, Human (His) is 369 a.a., with molecular weight of ~45.2 kDa.
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 total length of Coagulation factor IX/F9 Protein, Human (HEK293, His) is 433 a.a., with molecular weight of 60-90 kDa.
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 total length of PLA2G7 Protein, Mouse (Baculovirus, N-His, C-Myc) is 419 a.a., with molecular weight of 50.7 kDa.
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. The total length of PLA2G7 Protein, Mouse (HEK293, N-His, C-Myc) is 419 a.a., with molecular weight of 51.9 kDa.
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-d6-1 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-d 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- 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 .
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-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-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- 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-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 .
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