cell-membrane

Lipopolysaccharides (LPS) derived from Escherichia coli 055:B5, are a unique component of the cell wall of Gram-negative bacteria. They are composed of three regions: lipid A, oligosaccharide core, and O-specific polysaccharide (O-antigen). Lipopolysaccharides help maintain the integrity of the cell outer membrane and protect bacteria from damage by bile salts and lipid antibiotics. Lipopolysaccharides are highly immunogenic antigens that can enhance immune responses and can be used to construct inflammatory models.

LY-411575, a potent γ-secretase inhibitor, is with IC50 of 0.078 nM in the membrane and 0.082 nM in cell-based. It also suppresses Notch clevage with IC50 of 0.39 nM.

Leupeptin hemisulfate is a protease inhibitor with cell membrane-permeable, reversible, competitive, and oral activities. Leupeptin hemisulfate inhibits the activity of Cathepsin B, Cathepsin H, and Cathepsin L, and blocks fusion of amphipathic lysosomes. Leupeptin hemisulfate also has anti-inflammatory activity.

Tipelukast (KCA 757) is a novel, orally available leukotriene receptor antagonist with anti-inflammatory properties, capable of reducing fibrosis and down-regulating TIMP-1 and type 1 collagen. Tipelukast is utilized in asthma research.

KHK-IN-1 (KHK-IN-8) is a selective and cell membrane permeable inhibitor of ketohexokinase (KHK, IC50=12 nM; F=34%). KHK-IN-1 inhibits F1P production in HepG2 cell lysates with IC50 of 400 nM. KHK-IN-1 has potential for the study of obesity and diabetes.

RS 17053 hydrochloride is a potent and selective antagonist of the α1A adrenoceptor, with a pKi value of 9.1 in native cell membranes and a pA2 value of 9.8 in functional assays.

Glutathione arsenoxide hydrochloride (Glutathione arsenoxide hydrochloride(1271726-51-2 Free base)) is a potentially active anti-cancer molecule and inhibitor of tumour metabolism. glutathione arsenoxide hydrochloride targets the mitochondrial inner membrane adenine nucleotidyl transferase (ANT), which inhibits cell proliferation and promotes apoptosis. Glutathione arsenoxide hydrochloride can be used to recognize cell surface proteins such as protein disulfide isomerases.

Upacicalcet (AJT-240) is an intraventricular calcium mimetic, a SHPT available for human hemodialysis, that inhibits excessive parathyroid hormone (PTH) secretion by directly acting on parathyroid cell membrane calcium-sensitive receptors, thereby lowering blood levels of PTH.Upacicalcet is an orthosteric modulator of calcium-sensitive receptors and prevents adenine-induced secondary vascular calcification and bone disease in a rat model of adenine-induced secondary hyperparathyroidism.

Milataxel is an orally bioavailable taxane with potential antineoplastic activity. Upon oral administration, milataxel and its major active metabolite M-10 bind to and stabilize tubulin, resulting in the inhibition of microtubule depolymerization and cell division, cell cycle arrest in the G2 M phase, and the inhibition of tumor cell proliferation. Unlike other taxane compounds, milataxel appears to be a poor substrate for the multidrug resistance (MDR) membrane-associated P-glycoprotein (P-gp) efflux pump and may be useful for treating multidrug-resistant tumors. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).This compound is unstable in powder form and other related salt forms are recommended.

Caldaret HCl is an intracellular Ca2+ modulator that regulates calcium homeostasis at the sarcoplasmic reticulum and cell membrane, and can be used to study acute myocardial infarction and heart failure.

Cortisone Acetate is a synthetic or semisynthetic analog of the naturally occurring cortisone hormone produced by the adrenal glands with anti-inflammatory and immunomodulating properties. Cortisone acetate (NSC-49420) diffuses through the cell membrane and binds to nuclear glucocorticoid receptors. The receptor-ligand complex binds to promotor regions of certain genes and initiates RNA transcription. This results in an induction of synthesis of certain anti-inflammatory proteins while inhibiting the synthesis of certain inflammatory mediators.

Umifenovir hydrochloride (Arbidol HCl) , an broad-spectrum antiviral chemical agent, can inhibit cell invade of enveloped viruses by blocking viral fusion with host cell membrane.

Amorolfine hydrochloride (Amorolfine HCl) is an antifungal reagent. It exerts the antifungal activity by selectively interrupting two steps in the pathway of ergosterol synthesis and eventually disrupting the function and structure of fungal cell membrane. Amorolfine hydrochloride , a morpholine antifungal drug, can inhibit D14 reductase and D7-D8 isomerase. These enzymes can deplete ergosterol and cause ignosterol to accumulate in the fungal cytoplasmic cell membranes.

Proparacaine Hydrochloride is the hydrochloride salt form of proparacaine, a benzoic acid derivative with local anesthetic property. Proparacaine hydrochloride (Proparacaine HCl) stabilizes the neuronal membrane by binding to and inhibiting voltage-gated sodium channels, thereby inhibiting sodium ion influx required for the initiation and conduction of impulses within the neuronal cell, and resulting in a loss of sensation.

Ropivacaine (LEA-103 HCl) is a local anaesthetic drug belonging to the amino amide group.

Cefazolin sodium (cephazolin sodium) salt binds to and inactivates penicillin-binding proteins (PBP) located on the inner membrane of the bacterial cell wall. Cefazolin sodium salt is the sodium salt of cefazolin, a beta-lactam antibiotic and first-generation cephalosporin with bactericidal activity. Inactivation of PBPs interferes with the cross-linkage of peptidoglycan chains necessary for bacterial cell wall strength and rigidity, which results in the weakening of the bacterial cell wall and cell lysis.

Chlorhexidine (Rotersept) is a biguanide compound used as an antiseptic agent with topical antibacterial activity. Chlorhexidine is positively charged and reacts with the negatively charged microbial cell surface, thereby destroying the integrity of the cell membrane. Subsequently, chlorhexidine penetrates into the cell and causes leakage of intracellular components leading to cell death. Since gram-positive bacteria are more negatively charged, they are more sensitive to this agent.

Chlorhexidine diacetate (Bactigras) is a disinfectant and topical anti-infective agent used also as mouthwash to prevent oral plaque.

Amoxicillin (Amoxycillin) binds to and inactivates penicillin-binding proteins (PBPs) located on the inner membrane of the bacterial cell wall. Amoxicillin Anhydrous is the anhydrous form of a broad-spectrum, semisynthetic aminopenicillin antibiotic with bactericidal activity. Inactivation of PBPs interferes with the cross-linkage of peptidoglycan chains necessary for bacterial cell wall strength and rigidity. This interrupts bacterial cell wall synthesis and results in the weakening of the bacterial cell wall and causes cell lysis.

Amoxicillin trihydrate (Moxaline trihydrate) binds to and inactivates penicillin-binding protein (PBP) 1A located on the inner membrane of the bacterial cell wall. Amoxicillin trihydrate is a broad-spectrum, semisynthetic aminopenicillin antibiotic with bactericidal activity. Inactivation of PBPs interferes with the cross-linkage of peptidoglycan chains necessary for bacterial cell wall strength and rigidity. This interrupts bacterial cell wall synthesis and results in the weakening of the bacterial cell wall and causes cell lysis.

Cephalothin sodium (Cefalotin) binds to and inactivates penicillin-binding proteins (PBP) located on the inner membrane of the bacterial cell wall. Cephalothin sodium (Cefalotin) is the sodium salt form of cephalothin, a semisynthetic, beta-lactam, the first-generation cephalosporin antibiotic with bactericidal activity. PBPs participate in the terminal stages of assembling the bacterial cell wall, and in reshaping the cell wall during cell division. Inactivation of PBPs interferes with the cross-linkage of peptidoglycan chains necessary for bacterial cell wall strength and rigidity. This results in the weakening of the bacterial cell wall and causes cell lysis.

Bifonazole (Bay H-4502) acts to destabilize the fungal cytochrome p450 51 enzyme (also known as Lanosterol 14-alpha-demethylase). It works by inhibiting the production of a substance called ergosterol, which is an essential component of fungal cell membranes. This is vital in the cell membrane structure of the fungus. Its inhibition leads to cell lysis. The disruption in production of ergosterol disrupts the cell membrane and causes holes to appear. The cell membranes of fungi are vital for their survival. They keep unwanted substances from entering the cells and stop the contents of the cells from leaking out.

(CL227193) )binds to and inactivates penicillin-binding proteins (PBPs), enzymes located on the inner membrane of the bacterial cell wall, resulting in the weakening of the bacterial cell wall and cell lysis. Piperacillin Sodium is the sodium salt of piperacillin, a broad-spectrum semisynthetic, ampicillin-derived ureidopenicillin antibiotic with bactericidal activity. PBPs participate in the terminal stages of assembling the bacterial cell wall, and in reshaping the cell wall during cell division. Inactivation of PBPs interferes with the cross-linkage of peptidoglycan chains necessary for bacterial cell wall strength and rigidity.

Butoconazole Nitrate is the nitrate salt form of butoconazole, a synthetic imidazole derivative with fungistatic properties. Butoconazole nitrate (RS 35887) interferes with steroid biosynthesis by inhibiting the conversion of lanosterol to ergosterol, thereby changing the fungal cell membrane lipid composition. This alters cell permeability and leads to growth inhibition. Butoconazole nitrate is active against many dermatophytes and yeasts. It also contains antibacterial effects against some gram-positive organisms.