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1,2-DImyristoyl-rac-glycero-3-phosphocholine (DMPC), a zwitterionic phospholipid, is chosen as a simple eukaryotic cell membrane, mimicking the neutral charge of the surface membrane of eukaryotic plasmamembranes .
(Rac)-Idroxioleic acid (2-Hydroxyoleic acid) is a synthetic oleic acid (OA) derivative that binds to the plasmamembrane and alters lipid organization. (Rac)-Idroxioleic acid has anti-tumor effect .
cPcAMP1/26 is an antimicrobial peptide. cPcAMP1/26 effectively kills A.hydrophila and S. aureus. cPcAMP1/26 induces depolarization of the bacterial plasmamembrane, and increases intracellular ROS levels .
Caloxin 2A1 is an extracellular plasmamembrane Ca 2+-ATPase (PMCA) peptide inhibitor. Caloxin 2A1 does not affect basal Mg 2+-ATPase or Na +-K +-ATPase .
Caloxin 2A1 TFA is an extracellular plasmamembrane Ca 2+-ATPase (PMCA) peptide inhibitor. Caloxin 2A1 TFA does not affect basal Mg 2+-ATPase or Na +-K +-ATPase .
Zymosterol is a Cholesterol (HY-N0322) biosynthesis metabolite. Zymosterol, a precursor of Cholesterol, is found mostly in the plasmamembrane. Zymosterol circulates within the cell .
FR-167356 is a potent, orally active and selective vacuolar ATPase inhibitor with IC50 values of 170, 220, 370, and 1200 nM for osteoclast plasmamembranes, macrophage microsomes, renal brush border membranes, and liver lysosomal membranes, respectively. FR-167356 inhibits bone resorption and ovariectomy-induced bone loss .
Mem-C1C18 is a polarity-sensitive fluorescent probe with excellent plasmamembrane anchoring, high brightness and a sensitive response to environmental polarity by altering the fluorescence lifetime. Mem-C1C18 can be used to quantify changes in the polarity of the plasmamembrane during iron death .
C6 NBD Sphingomyelin is a fluorescent short-chain analogue of Sphingomyelin (HY-113498). Chlamydia trachomatis acquires C6 NBD Sphingomyelin endogenously synthesizes from C6-NBD-ceramide and transportes to the chlamydial inclusion. C6 NBD Sphingomyelin can incorporate into the plasmamembrane .
Antifungal agent 38 is a geterocyclic disulfide, an antifungal and antibacterial agent. Antifungal agent 38 induces the shrinkage of hyphae, disrupts the integrity of the plasmamembrane, and causes the damage and leakage of cell contents .
Antimicrobial agent-24 (compound E8) is a hydrazide compound with excellent and broad-spectrum fungicidal activities. Antimicrobial agent-24 affects the normal function of the plasmamembrane, further generating changes in the morphology and subcellular structure of mycelia .
Cholesterol is the major sterol in mammals. It is making up 20-25% of structural component of the plasmamembrane. Plasmamembranes 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 .
Caloxin 3A1 is a biological active peptide. (This peptide belongs to caloxins, the extracellular plasmamembrane (PM) Ca2+ pump inhibitors. Caloxin 3A1 inhibits plasmamembrane calcium pumps (PMCAs) but not the sarcoplasmic reticulum Ca2+-pump. This peptide does not inhibit formation of the acylphosphate intermediate from ATP.)
lsocryptomerin is a membrane-active antifungal compound that can be isolated from Selaginella tamariscina. lsocryptomerin can depolarize fungal plasmamembrane. lsocryptomerin also shows anticancer and antibacterial activities .
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 plasmamembrane. Plasmamembranes 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 plasmamembrane. Plasmamembranes 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 plasmamembrane. Plasmamembranes 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 plasmamembrane. Plasmamembranes 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 plasmamembrane. Plasmamembranes 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 plasmamembrane. Plasmamembranes 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 plasmamembrane. Plasmamembranes 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 plasmamembrane. Plasmamembranes 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 plasmamembrane. Plasmamembranes 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 plasmamembrane. Plasmamembranes 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 .
TMA-DPH is a hydrophobic fluorescent membrane probe (Ex=355 nm; Em=430 nm). TMA-DPH is able to anchor on the cell surface and localize to different regions of the phospholipid bilayer. By analyzing the fluorescence polarization values of TMA-DPH in the plasmamembrane and membrane substructures, the fluidity of the cell membrane can be determined .
Piperulin A is a potent inhibitor of PAFR. Piperulin A inhibits the specific binding of PAFR on isolated rabbit platelet plasmamembranes with an IC50 of 7.3 μM .
mgc(3Me)FL is the active fluorescent form of mgc(3Me)FDA (HY-D2300) after hydrolysis in cells. mgc(3Me)FL subcellularly localizes to the Golgi apparatus and is a visualized Golgi probe. mgc(3Me)FL also binds to the outer leaflet of the plasmamembrane (PM), causing the plasmamembrane to fluoresce .
Lactosylceramide (bovine buttermilk) (LacCer (bovine buttermilk)) is a sphingolipid that highly expressed on the plasmamembranes of human phagocytes. Lactosylceramide mediates phagocytosis, chemotaxis, and superoxide generation .
Ziapin 2 is a molecular optomechanical light transducer. Ziapin 2 is an amphiphilic azobenzene with a strong non-covalent affinity to the plasmamembrane. Ziapin 2 can be used to photo-modulate the membrane potential in cells of the Gram-positive bacterium Bacillus subtilis. Ziapin 2 enters the lipid membrane very rapidly (≈ 40 ns) .
Syringomycin E is an antifungal cyclic lipodepsinonapeptide. Syringomycin E exhibits growth inhibition of Saccharomyces cerevisiae through interaction with the plasmamembrane. Syringomycin E causes K + efflux, Ca 2+ influx, and changes in membrane potential, and is related to channel formation .
Triclabendazole sulfoxide (TCBZ-SO) is the main plasma metabolite of Triclabendazole, and exhibits anti-parasite effects. Triclabendazole sulfoxide can inhibit membrane transporter ABCG2/BCRP .
BTCy is a near-infrared (NIR) fluorescence probe with polarity-responsive and cell plasmamembrane-targeting properties. BTCy can be used for in vivo imaging of tumor tissue (λex = 561 nm, λem = 600-700 nm) .
Celangulin is an insecticidal component isolated from Celastrus angulatus. Celangulin activates the calcium channel on the plasmamembrane with increasing the intracellular Ca 2+ after influx from the external. Celangulin activates the calcium channel in the ER .
Thiocholesterol is a member of the class of cholesteric liquid crystals (CLCs) that can be used to synthesis cationic lipid. Thiocholesterol is a stronger stabilizer of silver nanoparticles (SNPs). Thiocholesterol can be used for plasmamembrane research and drug delivery .
BODIPY-cholesterol conjugate-3 (compound 7) is a cholesterol analogue with a fluorescent BODIPY group. BODIPY-cholesterol conjugate-3 can be used to simultaneously visualize multiple cholesterol pools in cells, as it is primarily localized to the plasmamembrane .
DAF-FM DA (Diaminofluorescein-FM diacetate) is a fluorescent probe for the detection and bioimaging of nitric oxide (NO). DAF-FM DA spontaneously crosses the plasmamembrane and is subsequently cleaved by esterases to generate intracellular DAF-FM (Ex/Em=495/515 nm) .
Nepodin (Musizin) is a quinone oxidoreductase (PfNDH2) inhibitor isolate from Rumex crispus .Nepodin (Musizin) stimulates the translocation of GLUT4 to the plasmamembrane by activation of AMPK .Nepodin (Musizin) has antidiabetic and antimalarial activities.
OSBPL7-IN-1 is an orally active oxysterol binding protein like 7 (OSBPL7) inhibitor. OSBPL7-IN-1 promotes an increase of ABCA1 at the plasmamembrane without affecting mRNA expression .
Dicyclomine hydrochloride is a potent and orally active muscarinic cholinergic receptors antagonist. Dicyclomine hydrochloride shows high affinity for muscarinic M1 receptor subtype (Ki=5.1 nM) and M2 receptor subtype (Ki=54.6 nM) in brush-border membrane and basal plasmamembranes, respectively . Dicyclomine is an antispasmodic agent and relieves smooth muscle spasm of the gastrointestinal tract in vivo .
Endoplasmic reticulum dye 1 is a promising live cell imaging agent for the detection of exocytotic events at the plasmamembrane. Endoplasmic reticulum dye 1 shows low cytotoxicity, resistance to photobleaching , which is ideal for imaging either short- or long-time courses .
Dicyclomine (Dicycloverine) is a potent and orally active muscarinic cholinergic receptors antagonist. Dicyclomine (Dicycloverine) shows high affinity for muscarinic M1 receptor subtype (Ki=5.1 nM) and M2 receptor subtype (Ki=54.6 nM) in brush-border membrane and basal plasmamembranes, respectively . Dicyclomine is an antispasmodic agent and relieves smooth muscle spasm of the gastrointestinal tract in vivo .
Natamycin (Pimaricin) is a macrolide antibiotic agent produced by several Streptomyces strains. Natamycin inhibits the growth of fungi via inhibition of amino acid and glucose transport across the plasmamembrane. Natamycin is a food preservative, an antifungal agent in agriculture, and is widely used for fungal keratitis research .
cis-ACBD is a potent and selective inhibitor of the high-affinity, Na +-dependent plasmamembraneglutamate transporter. cis-ACBD is a glutamate reuptake inhibitor. cis-ACBD also acts as linear competitive inhibitor of the uptake of D-[3H]aspartate .
Triclabendazole sulfoxide-d3 is the deuterium labeled Triclabendazole sulfoxide. Triclabendazole sulfoxide (TCBZ-SO) is the main plasma metabolite of Triclabendazole, and exhibits anti-parasite effects. Triclabendazole sulfoxide can inhibit membrane transporter ABCG2/BCRP[1][2].
BODIPY TR methyl ester is a lipophilic GFP Counterstain. BODIPY TR methyl ester dye readily permeates cell membranes and localizes in endomembranous organelles but not localize strongly in plasmamembranes. BODIPY TR methyl ester is an excellent red fluorescent vital dye (Ex=568 nm, Em=625 nm), can be used to reveal the location and shapes of cell nuclei, the shapes of cells within embryonic tissues, as well as the bound aries of organ-forming tissues within the whole embryo .
AJH-836 is an activator of Munc13-1 and PKC ε/α (Kd: 4.5 nM for PKCα) . AJH-836 triggers the translocation of Munc13-1 from the cytoplasm to the plasmamembrane. AJH-836 can be used for research of neurodegenerative diseases .
R59949 is a pan diacylglycerol kinase (DGK) inhibitor with an IC50 of 300 nM. R59949 strongly inhibits the activity of type I DGK α and γ and moderately attenuates the activity of type II DGK θ and κ. R59949 activates protein kinase C (PKC) by enhancing the levels of the endogenous ligand diacyl glycerol .
Thiazolyl Blue (MTT) is a cell-permeable and positively charged tetrazolium dye that is used to detect reductive metabolism in cells. Thiazolyl Blue is taken up by cells through the plasmamembrane and then reduced to formazan by intracellular NAD (P) H-oxidoreductases. Thiazolyl Blue is frequently used in colorimetric assays to measure cell proliferation, cytotoxicity, and apoptosis .
Triclabendazole sulfoxide- 13C,d3 is the 13C- and deuterium labeled Triclabendazole sulfoxide. Triclabendazole sulfoxide (TCBZ-SO) is the main plasma metabolite of Triclabendazole, and exhibits anti-parasite effects. Triclabendazole sulfoxide can inhibit membrane transporter ABCG2/BCRP[1][2].
BF844 mitigate hearing loss associated with USH3 (usher syndrome type III) mutation CLRN1 (clarin-1) N48K. BF844 induces CLRN1 N48K transportes to the plasmamembrane. BF844 shows significantly preserves hearing in vivo .
13-HPOT, a linolenic fatty acid hydroperoxide, is an antibacterial agent. 13-HPOT has a strong dose response effect on three plant pathogen gram negative bacteria: Pectobacterium carotovorum, Pseudomonas syringae and Xanthomonas translucens. 13-HPOT can interact with the lipid representative of the inner bacterial plasmamembrane .
Dicyclomine-d4 is the deuterium labeled Dicyclomine[1]. Dicyclomine (Dicycloverine) is a potent and orally active muscarinic cholinergic receptors antagonist. Dicyclomine (Dicycloverine) shows high affinity for muscarinic M1 receptor subtype (Ki=5.1 nM) and M2 receptor subtype (Ki=54.6 nM) in brush-border membrane and basal plasmamembranes, respectively[2]. Dicyclomine is an antispasmodic agent and relieves smooth muscle spasm of the gastrointestinal tract in vivo[3].
Nystatin is an orally active polyene antifungal antibiotic effective against yeast and mycoplasma. Nystatin increases the permeability of plasmamembranes to small monovalent ions, including chloridion . Nystatin is a cholesterol-sequestering agent , partially prevents Oxaliplatin-induced lipid raft aggregation, DR4 and DR5 clustering, and thereby reduces apoptosis .
8-Isoprostaglandin F2α is an isoprostane produced by the non-enzymatic peroxidation of arachidonic acid in membrane phospholipids. 8-Isoprostaglandin F2α is present in human plasma in two distinct forms - esterified in phospholipids and as the free acid. 8-Isoprostaglandin F2α is a weak TP receptor agonist in vascular smooth muscle.
Neurokinin Receptor (393-407), rat (SPR393–407) is a rat neurokinin 1 receptor (NK1R) fragment. NK1R is rapidly internalized by endocytosis and recycled to the plasmamembrane when binding to substance P (SP). Neurokinin Receptor (393-407), rat can be used in the research of neurogenic inflammation .
CFTR corrector 12 (compound 17C) is a bithiazole derivative, serving as CFTR corrector. CFTR corrector 12 has the ability to correct some folding defective mutants of the channel responsible for the control of chloride transport across the plasmamembrane. CFTR corrector 12 recovers the α-sarcoglycan (α-SG) content in mutant cells .
Cholera toxin (Choleragen), an AB(5)-subunit toxin, enters host cells by binding the ganglioside GM1 at the plasmamembrane (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 .
BAPTA is a selective chelator for calcium. BAPTA, as calcium indicator, has high selectivity against magnesium and calcium. BAPTA is widely used as an intracellular buffer for investigating the effects of Ca 2+ release from intracellular stores or influx via Ca 2+-permeable channels in the plasmamembrane. BAPTA can also inhibit phospholipase C activity independently of their role as Ca 2+ chelators .
GW604714X is a potent inhibitor of mitochondrial respiration supported by pyruvate but not other substrates. GW604714X is a highly specific mitochondrial pyruvate carrier (MPC) inhibitor with a Ki <0.1 nM. GW604714X also inhibits L-lactate transport by the plasmamembrane monocarboxylate transporter (MCT1), but at concentrations more than 4 orders of magnitude greater than the MPC .
T18.3 aptamer sodium is an anticoagulant RNA aptamer targeting FV/Va and eliminates the interaction of FV/FVa with phospholipid membranes. T18.3 aptamer sodium exhibits clinically relevant anticoagulant activity in plasma and whole blood and acts synergistically with low molecular weight heparin. The anticoagulant activity of T18.3 aptamer sodium is effectively and rapidly reversed by protamine sulfate .
CLP257 is a selective K +-Cl − cotransporter KCC2 activator with an EC50 of 616 nM. CLP257 is inactive against NKCC1, GABAA receptors, KCC1, KCC3 or KCC4. CLP257 restores impaired Cl − transport in neurons with diminished KCC2 activity. CLP257 alleviates hypersensitivity in rats with neuropathic pain. CLP257 modulates plasmalemmal KCC2 protein turnover post-translationally .
BAPTA tetrapotassium is a selective chelator for calcium. BAPTA, as calcium indicator, has high selectivity against magnesium and calcium. BAPTA tetrapotassium is widely used as an intracellular buffer for investigating the effects of Ca 2+ release from intracellular stores or influx via Ca 2+-permeable channels in the plasmamembrane. BAPTA tetrapotassium can also inhibit phospholipase C activity independently of their role as Ca 2+ chelators .
BAPTA tetrasodium is a selective chelator for calcium. BAPTA tetrasodium, as calcium indicator, has high selectivity against magnesium and calcium. BAPTA tetrasodium is widely used as an intracellular buffer for investigating the effects of Ca 2+ release from intracellular stores or influx via Ca 2+-permeable channels in the plasmamembrane. BAPTA tetrasodium can also inhibit phospholipase C activity independently of their role as Ca 2+ chelators .
Abscisic acid ((S)-(+)-Abscisic acid), an orally active phytohormone in fruits and vegetables, is an endogenously produced mammalian hormone. Abscisic acid is a growth inhibitor and can regulate many aspects of plant growth and development. Abscisic acid inhibits proton pump (H +-ATPase) and leads to the plasmamembrane depolarization in a Ca 2+-dependent manner. Abscisic acid, a LANCL2 natural ligand, is a potent insulin-sensitizing compound and has the potential for pre-diabetes, type 2 diabetes and metabolic syndrome .
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 plasmamembrane 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 plasmamembrane. 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.
8-iso Prostaglandin F2α-d9 is the deuterium labeled 8-Isoprostaglandin F2α. 8-Isoprostaglandin F2α is an isoprostane produced by the non-enzymatic peroxidation of arachidonic acid in membrane phospholipids. 8-Isoprostaglandin F2α is present in human plasma in two distinct forms - esterified in phospholipids and as the free acid. 8-Isoprostaglandin F2α is a weak TP receptor agonist in vascular smooth muscle.
ML-184 (CID2440433) is a selective GPR55 agonist with an EC50 of 250 nM and exhibits >100-fold selectivity for GPR55 over GPR35, CB1 and CB2. ML-184 induces phosphorylation of ERK1/2 and translocation of PKCβII to the plasmamembrane by activating GPR55 . ML-184(CID2440433) increases proliferation of neural stem cells and promotes neuronal differentiation in vitro .
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 plasmamembrane. 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 plasmamembrane. TRV120027 inhibits angiotensin II–mediated vasoconstriction and increases cardiomyocyte contractility. TRV120027 has the potential for the acute decompensated heart failure (ADHF) treatment .
Membrane receptors, also known cell surface receptors or transmembrane receptors, are transmembrane proteins embedded into the plasmamembrane 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 plasmamembrane 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.
Sodium channels conduct sodium ions (Na+) through a cell's plasmamembrane that are the source of excitatory currents for the nervous system and muscle. Na channels are classified according to the trigger that opens the channel for such ions, i.e. either a voltage-change (Voltage-gated, voltage-sensitive, or voltage-dependent sodium channel also called VGSCs or Nav channel) or a binding of a substance (a ligand) to the channel (ligand-gated sodium channels). Dysfunction in voltage-gated sodium channels correlates with neurological and cardiac diseases, including epilepsy, myopathies, pain and cardiac arrhythmias. Sodium channel blockers are used in the treatment of cardiac arrhythmia, pain and convulsion.
MCE offers a unique collection of 128 sodium channel blocker and antagonists, all of which have the identified inhibitory effect on sodium channels. MCE Sodium Channel Blocker Library can be used for neurological and cardiac diseases drug discovery and sodium channel research.
PM-1, a derivative of Thioflavin-T (ThT; HY-D0218), is a small but highly specific plasmamembrane (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 plasmamembrane 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 .
C6 NBD Sphingomyelin is a fluorescent short-chain analogue of Sphingomyelin (HY-113498). Chlamydia trachomatis acquires C6 NBD Sphingomyelin endogenously synthesizes from C6-NBD-ceramide and transportes to the chlamydial inclusion. C6 NBD Sphingomyelin can incorporate into the plasmamembrane .
TMA-DPH is a hydrophobic fluorescent membrane probe (Ex=355 nm; Em=430 nm). TMA-DPH is able to anchor on the cell surface and localize to different regions of the phospholipid bilayer. By analyzing the fluorescence polarization values of TMA-DPH in the plasmamembrane and membrane substructures, the fluidity of the cell membrane can be determined .
mgc(3Me)FL is the active fluorescent form of mgc(3Me)FDA (HY-D2300) after hydrolysis in cells. mgc(3Me)FL subcellularly localizes to the Golgi apparatus and is a visualized Golgi probe. mgc(3Me)FL also binds to the outer leaflet of the plasmamembrane (PM), causing the plasmamembrane to fluoresce .
BODIPY-cholesterol conjugate-3 (compound 7) is a cholesterol analogue with a fluorescent BODIPY group. BODIPY-cholesterol conjugate-3 can be used to simultaneously visualize multiple cholesterol pools in cells, as it is primarily localized to the plasmamembrane .
DAF-FM DA (Diaminofluorescein-FM diacetate) is a fluorescent probe for the detection and bioimaging of nitric oxide (NO). DAF-FM DA spontaneously crosses the plasmamembrane and is subsequently cleaved by esterases to generate intracellular DAF-FM (Ex/Em=495/515 nm) .
Endoplasmic reticulum dye 1 is a promising live cell imaging agent for the detection of exocytotic events at the plasmamembrane. Endoplasmic reticulum dye 1 shows low cytotoxicity, resistance to photobleaching , which is ideal for imaging either short- or long-time courses .
BODIPY TR methyl ester is a lipophilic GFP Counterstain. BODIPY TR methyl ester dye readily permeates cell membranes and localizes in endomembranous organelles but not localize strongly in plasmamembranes. BODIPY TR methyl ester is an excellent red fluorescent vital dye (Ex=568 nm, Em=625 nm), can be used to reveal the location and shapes of cell nuclei, the shapes of cells within embryonic tissues, as well as the bound aries of organ-forming tissues within the whole embryo .
Thiazolyl Blue (MTT) is a cell-permeable and positively charged tetrazolium dye that is used to detect reductive metabolism in cells. Thiazolyl Blue is taken up by cells through the plasmamembrane and then reduced to formazan by intracellular NAD (P) H-oxidoreductases. Thiazolyl Blue is frequently used in colorimetric assays to measure cell proliferation, cytotoxicity, and apoptosis .
1,2-DImyristoyl-rac-glycero-3-phosphocholine (DMPC), a zwitterionic phospholipid, is chosen as a simple eukaryotic cell membrane, mimicking the neutral charge of the surface membrane of eukaryotic plasmamembranes .
Cholesterol is the major sterol in mammals. It is making up 20-25% of structural component of the plasmamembrane. Plasmamembranes 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 .
Lactosylceramide (bovine buttermilk) (LacCer (bovine buttermilk)) is a sphingolipid that highly expressed on the plasmamembranes of human phagocytes. Lactosylceramide mediates phagocytosis, chemotaxis, and superoxide generation .
BAPTA is a selective chelator for calcium. BAPTA, as calcium indicator, has high selectivity against magnesium and calcium. BAPTA is widely used as an intracellular buffer for investigating the effects of Ca 2+ release from intracellular stores or influx via Ca 2+-permeable channels in the plasmamembrane. BAPTA can also inhibit phospholipase C activity independently of their role as Ca 2+ chelators .
Thiocholesterol is a member of the class of cholesteric liquid crystals (CLCs) that can be used to synthesis cationic lipid. Thiocholesterol is a stronger stabilizer of silver nanoparticles (SNPs). Thiocholesterol can be used for plasmamembrane research and drug delivery .
BAPTA tetrapotassium is a selective chelator for calcium. BAPTA, as calcium indicator, has high selectivity against magnesium and calcium. BAPTA tetrapotassium is widely used as an intracellular buffer for investigating the effects of Ca 2+ release from intracellular stores or influx via Ca 2+-permeable channels in the plasmamembrane. BAPTA tetrapotassium can also inhibit phospholipase C activity independently of their role as Ca 2+ chelators .
ALN29882 is a glycerolipid located on the plasmamembrane. 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.
Caloxin 2A1 TFA is an extracellular plasmamembrane Ca 2+-ATPase (PMCA) peptide inhibitor. Caloxin 2A1 TFA does not affect basal Mg 2+-ATPase or Na +-K +-ATPase .
cPcAMP1/26 is an antimicrobial peptide. cPcAMP1/26 effectively kills A.hydrophila and S. aureus. cPcAMP1/26 induces depolarization of the bacterial plasmamembrane, and increases intracellular ROS levels .
Caloxin 2A1 is an extracellular plasmamembrane Ca 2+-ATPase (PMCA) peptide inhibitor. Caloxin 2A1 does not affect basal Mg 2+-ATPase or Na +-K +-ATPase .
KLA peptide is a biological active peptide. (a cationic amphipathic mitochondrial membrane disrupting peptide that induces programmed cell death by disrupting mitochondrial membrane, but cannot cross the plasmamembrane)
Caloxin 3A1 is a biological active peptide. (This peptide belongs to caloxins, the extracellular plasmamembrane (PM) Ca2+ pump inhibitors. Caloxin 3A1 inhibits plasmamembrane calcium pumps (PMCAs) but not the sarcoplasmic reticulum Ca2+-pump. This peptide does not inhibit formation of the acylphosphate intermediate from ATP.)
Syringomycin E is an antifungal cyclic lipodepsinonapeptide. Syringomycin E exhibits growth inhibition of Saccharomyces cerevisiae through interaction with the plasmamembrane. Syringomycin E causes K + efflux, Ca 2+ influx, and changes in membrane potential, and is related to channel formation .
Glucagon (22-29) is partial agonist of Glucagon (19–29). Glucagon specifically inhibits the Ca 2+ pump in liver plasmamembranes independently of adenylate cyclase activation .
(Arg)9 biotin labeled is a cell-permeable peptide. (Arg)9 biotin labeled can be used for drug delivery. (Arg)9 biotin labeled can traverse the plasmamembrane of eukaryotic cells .
Neurokinin Receptor (393-407), rat (SPR393–407) is a rat neurokinin 1 receptor (NK1R) fragment. NK1R is rapidly internalized by endocytosis and recycled to the plasmamembrane when binding to substance P (SP). Neurokinin Receptor (393-407), rat can be used in the research of neurogenic inflammation .
α-Hemolysin (Staphylococcus aureus) is one of the most characteristic virulence factors secreted by Staphylococcus aureus, a polypeptide capable of destroying the host cell plasmamembrane. After α-Hemolysin binds to the cell surface, its monomers assemble into a homoheptamer to form a front pore, which then transforms into a mature transmembrane pore water channel, allowing K + and Ca 2+ ion transport, leading to necrotic death of target cells .
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 plasmamembrane. 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 plasmamembrane. TRV120027 inhibits angiotensin II–mediated vasoconstriction and increases cardiomyocyte contractility. TRV120027 has the potential for the acute decompensated heart failure (ADHF) treatment .
Zymosterol is a Cholesterol (HY-N0322) biosynthesis metabolite. Zymosterol, a precursor of Cholesterol, is found mostly in the plasmamembrane. Zymosterol circulates within the cell .
Cholesterol is the major sterol in mammals. It is making up 20-25% of structural component of the plasmamembrane. Plasmamembranes 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 plasmamembrane. Plasmamembranes 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 .
lsocryptomerin is a membrane-active antifungal compound that can be isolated from Selaginella tamariscina. lsocryptomerin can depolarize fungal plasmamembrane. lsocryptomerin also shows anticancer and antibacterial activities .
Piperulin A is a potent inhibitor of PAFR. Piperulin A inhibits the specific binding of PAFR on isolated rabbit platelet plasmamembranes with an IC50 of 7.3 μM .
Celangulin is an insecticidal component isolated from Celastrus angulatus. Celangulin activates the calcium channel on the plasmamembrane with increasing the intracellular Ca 2+ after influx from the external. Celangulin activates the calcium channel in the ER .
Thiocholesterol is a member of the class of cholesteric liquid crystals (CLCs) that can be used to synthesis cationic lipid. Thiocholesterol is a stronger stabilizer of silver nanoparticles (SNPs). Thiocholesterol can be used for plasmamembrane research and drug delivery .
Nepodin (Musizin) is a quinone oxidoreductase (PfNDH2) inhibitor isolate from Rumex crispus .Nepodin (Musizin) stimulates the translocation of GLUT4 to the plasmamembrane by activation of AMPK .Nepodin (Musizin) has antidiabetic and antimalarial activities.
Natamycin (Pimaricin) is a macrolide antibiotic agent produced by several Streptomyces strains. Natamycin inhibits the growth of fungi via inhibition of amino acid and glucose transport across the plasmamembrane. Natamycin is a food preservative, an antifungal agent in agriculture, and is widely used for fungal keratitis research .
Nystatin is an orally active polyene antifungal antibiotic effective against yeast and mycoplasma. Nystatin increases the permeability of plasmamembranes to small monovalent ions, including chloridion . Nystatin is a cholesterol-sequestering agent , partially prevents Oxaliplatin-induced lipid raft aggregation, DR4 and DR5 clustering, and thereby reduces apoptosis .
8-Isoprostaglandin F2α is an isoprostane produced by the non-enzymatic peroxidation of arachidonic acid in membrane phospholipids. 8-Isoprostaglandin F2α is present in human plasma in two distinct forms - esterified in phospholipids and as the free acid. 8-Isoprostaglandin F2α is a weak TP receptor agonist in vascular smooth muscle.
Abscisic acid ((S)-(+)-Abscisic acid), an orally active phytohormone in fruits and vegetables, is an endogenously produced mammalian hormone. Abscisic acid is a growth inhibitor and can regulate many aspects of plant growth and development. Abscisic acid inhibits proton pump (H +-ATPase) and leads to the plasmamembrane depolarization in a Ca 2+-dependent manner. Abscisic acid, a LANCL2 natural ligand, is a potent insulin-sensitizing compound and has the potential for pre-diabetes, type 2 diabetes and metabolic syndrome .
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.
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.
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 plasmamembrane. Plasmamembranes 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 plasmamembrane. Plasmamembranes 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 plasmamembrane. Plasmamembranes 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 plasmamembrane. Plasmamembranes 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 plasmamembrane. Plasmamembranes 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 plasmamembrane. Plasmamembranes 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 plasmamembrane. Plasmamembranes 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 plasmamembrane. Plasmamembranes 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 plasmamembrane. Plasmamembranes 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 .
Triclabendazole sulfoxide-d3 is the deuterium labeled Triclabendazole sulfoxide. Triclabendazole sulfoxide (TCBZ-SO) is the main plasma metabolite of Triclabendazole, and exhibits anti-parasite effects. Triclabendazole sulfoxide can inhibit membrane transporter ABCG2/BCRP[1][2].
Triclabendazole sulfoxide- 13C,d3 is the 13C- and deuterium labeled Triclabendazole sulfoxide. Triclabendazole sulfoxide (TCBZ-SO) is the main plasma metabolite of Triclabendazole, and exhibits anti-parasite effects. Triclabendazole sulfoxide can inhibit membrane transporter ABCG2/BCRP[1][2].
Dicyclomine-d4 is the deuterium labeled Dicyclomine[1]. Dicyclomine (Dicycloverine) is a potent and orally active muscarinic cholinergic receptors antagonist. Dicyclomine (Dicycloverine) shows high affinity for muscarinic M1 receptor subtype (Ki=5.1 nM) and M2 receptor subtype (Ki=54.6 nM) in brush-border membrane and basal plasmamembranes, respectively[2]. Dicyclomine is an antispasmodic agent and relieves smooth muscle spasm of the gastrointestinal tract in vivo[3].
8-iso Prostaglandin F2α-d9 is the deuterium labeled 8-Isoprostaglandin F2α. 8-Isoprostaglandin F2α is an isoprostane produced by the non-enzymatic peroxidation of arachidonic acid in membrane phospholipids. 8-Isoprostaglandin F2α is present in human plasma in two distinct forms - esterified in phospholipids and as the free acid. 8-Isoprostaglandin F2α is a weak TP receptor agonist in vascular smooth muscle.
