vesicles

MCC950 sodium (CP-456773 sodium) is a potent and selective inhibitor of the inflammatory vesicle NLRP3 (IC50=7.5 nM in BMDMs; IC50=8.1 nM in HMDMs). MCC950 sodium has no effect on other inflammatory vesicles such as AIM2, NLRC4 or NLRP1.

Nandrolone decanoate (19-Nortestosterone decanoate) is the decanoate salt form of nandrolone, an anabolic steroid analog of testosterone with androgenic, anabolic, and erythropoietin stimulating effects. Nandrolone enters the cell and binds to and activates specific nuclear androgen receptors in responsive tissue, including the prostate, seminal vesicles, scrotum, penis, larynx, hair follicles, muscle, and bone.

NLRP3-IN-2 (5-Chloro-N-(p-sulfamoylphenethyl)-o-anisamide), an intermediate capable of synthesizing glibenclamide, exerts an inhibitory effect on the formation of NLRP3 inflammatory vesicles in cardiomyocytes, limiting infarct size after myocardial ischemia/reperfusion in mice and has no effect on metabolism.

L-Aspartic aicd sodium (Sodium L-aspartate) is an amino acid, a precursor active molecule for colon-specific active molecule delivery, that promotes Na+ efflux from rat forebrain membrane vesicles.

Tetrabenazine Metabolite ((-)-β-HTBZ), a vesicles monoamine transporter 2 (VMAT2) inhibitor, is an active metabolite of Tetrabenazine. Tetrabenazine Metabolite has a high affinity for VMAT2 with a Ki of 13.4 nM. Tetrabenazine Metabolite is often used to study chorea associated with Huntington's disease and other hyperactivity disorders.

G-Protein antagonist peptide acetate is a truncated substance P-related peptide, competes with receptor for G protein binding. G-Protein antagonist peptide acetate inhibits the activation of Gi or Go by M2 muscarinic cholinergic receptor (M2 mAChR) or of Gs by beta-adrenergic receptor in the reconstituted phospholipid vesicles, assayed by receptor-promoted GTP hydrolysis

7-Chlorokynurenic acid (7-chloro-4-hydroxy-2-carboxyquinoline) is an effecitve and selective antagonist of NMDA receptor with IC50 of 0.56 μM for the glycine B coagonist site. 7-Chlorokynurenic acid inhibits the reuptake of glutamate into synaptic vesicles with a Ki of 0.59 μM and shows antinociceptive actions after neuraxial delivery.

alphaSYN-IN-NAB2, a neuron-protective agent, is a protein encoded by the NAB2 gene. NAB2 effectively and selectively protects a variety of cells from alpha-SYN toxicity. NAB2 promotes endosomal transport dependent on E3 ubiquitin ligase Rsp5/Nedd4. NAB2 identifies a viable molecular node in alpha-SYN biology that corrects multiple aspects of its underlying pathology, including dysfunctional endosomes and endoplasmic reticulum to Golgi vesicles transport. NAB2 is involved in cellular processes such as cell differentiation, apoptosis and stress response, and can be used to study cancer, neurodevelopment and neuronal activity.

Diadenosine pentaphosphate pentaammonium, an endogenous vasoactive purine dinucleotide isolated from thrombocytes, is one component of the diadenosine polyphosphates (ApnA, n=2-7) family. These compounds are found in secretory vesicles, including those in platelets, chromaffin cells, Torpedo synaptic terminals, and brain synaptosomes[1][2].

(Rac)-POPC serves as a model phosphatidylcholine utilized in the preparation of giant vesicles (GVs) [1].

16:0 TAP, a lipid compound, is utilized in the preparation of giant unilamellar vesicles for agent delivery [1].

Methyl reserpate (NSC 81464), a yohimbine-type alkaloid derived from the roots and leaves of Rauwolfia vomitoria, inhibits the transport of norepinephrine into chromophobe vesicles.

Eicosapentaenoic acid is an ω-3 fatty acid abundantly available in marine organisms. (±)17(18)-DiHETE is one of the major metabolites produced when eicosapentaenoic acid (EPA) is incubated with various rat tissue homogenates or cynomolgus monkey seminal vesicles. The route of production of (±)17(18)-DiHETE likely proceeds through cytochrome P450-catalyzed epoxidation at the ω-3 double bond followed by conversion to the vicinal diols by epoxide hydrolase. EPA is also metabolized preferentially by Gaeumannomyces graminis to (±)17(18)-DiHETE.

Diadenosine pentaphosphate pentasodium, an endogenous vasoactive purine dinucleotide isolated from thrombocytes, serves as a key component of secretory vesicles in platelets, chromaffin cells, Torpedo synaptic terminals, and brain synaptosomes. This compound, along with other diadenosine polyphosphates (ApnA, n=2-7), plays a crucial role in physiological processes[1][2].

FFN 270 is a fluorescent false neurotransmitter (FFN). Fluorescent substrate for NET and VMAT2. Labels noradrenergic neurons and their synaptic vesicles, and enables imaging of synaptic vesicle content release from specific axonal sitesin vivo. Selectively labels NA neurons over other monoamine and CNS targets. Exhibits two resolved absorption/excitation maxima depending on solvent pH (excitation maxima: 320 nm or 365 nm, emission maxima: 475 nm).

22-NBD cholesterol, a fluorescent cholesterol analog featuring a nitrobenzoxadiazole (NBD) group, serves multiple research purposes in both in vitro and in vivo settings. Its applications span the analysis of steroid uptake and esterification, the study of intracellular localization and targeting, cholesterol metabolism in mammalian and bacterial cells, and examining cholesterol intestinal absorption in hamsters. This compound showcases excitation/emission maxima at 472/540 nm when integrated into 1,2-dimyristoyl-sn-glycero-3-PC (DMPC) vesicles. Notably, the emission maximum of 22-NBD cholesterol varies with the solvent's polarity, becoming more pronounced as the polarity increases.

γ-Bag cell peptide, a peptide situated near the N-terminus of the egg-laying prohormone, is released from vesicles upon insulin stimulation. It is utilized in research pertaining to both the central and peripheral nervous systems [1].

RG33 Peptide, utilized in type 2 diabetes (T2D) research [1], enhances glucose clearance in insulin-resistant mice and facilitates cholesterol efflux in cultured macrophages by effectively solubilizing lipid vesicles.

18:0,18:1 PS sodium, a lipid found in synaptic vesicles and cholesterol, serves a role in metabolic research [1].

Quorum sensing is a regulatory system used by bacteria for controlling gene expression in response to increasing cell density.[1] This regulatory process manifests itself with a variety of phenotypes including biofilm formation and virulence factor production.[2] Coordinated gene expression is achieved by the production, release, and detection of small diffusible signal molecules called autoinducers. The N-acylated homoserine lactones (AHLs) comprise one such class of autoinducers, each of which generally consists of a fatty acid coupled with homoserine lactone (HSL). Regulation of bacterial quorum sensing signaling systems to inhibit pathogenesis represents a new approach to antimicrobial therapy in the treatment of infectious diseases.[3] AHLs vary in acyl group length (C4-C18), in the substitution of C3 (hydrogen, hydroxyl, or oxo group), and in the presence or absence of one or more carbon-carbon double bonds in the fatty acid chain. These differences confer signal specificity through the affinity of transcriptional regulators of the LuxR family.[4] C16-HSL is one of a number of lipophilic, long acyl side-chain bearing AHLs, including its monounsaturated analog C16:1-(L)-HSL, produced by the LuxI AHL synthase homolog SinI involved in quorum-sensing signaling in S. meliloti, a nitrogen-fixing bacterial symbiont of certain legumes.[5],[6] C16-HSL is the most abundant AHL produced by the proteobacterium R. capsulatus and activates genetic exchange between R. capsulatus cells.[7] N-Hexadecanoyl-L-homoserine lactone and other hydrophobic AHLs tend to localize in relatively lipophilic cellular environments of bacteria and cannot diffuse freely through the cell membrane. The long-chain N-acylhomoserine lactones may be exported from cells by efflux pumps or may be transported between communicating cells by way of extracellular outer membrane vesicles.[8],[9]Reference:[1]. González, J.E., and Keshavan, N.D. Messing with bacterial quorum sensing Microbiol. Mol. Biol. Rev. 70(4), 859-875 (2006).[2]. Gould, T.A., Herman, J., Krank, J., et al. Specificity of acyl-homoserine lactone syntheses examined by mass spectrometry Journal of Bacteriology 188(2), 773-783 (2006).[3]. Cegelski, L., Marshall, G.R., Eldridge, G.R., et al. The biology and future prospects of antivirulence therapies Nature Reviews.Microbiology 6(1), 17-27 (2008).[4]. Penalver, C.G.N., Morin, D., Cantet, F., et al. Methylobacterium extorquens AM1 produces a novel type of acyl-homoserine lactone with a double unsaturated side chain under methylotrophic growth conditions FEBS Letters 580, 561-567 (2006).[5]. Gao, M., Chen, H., Eberhard, A., et al. sinI- and expR-dependent quorum sensing in Sinorhizobium meliloti Journal of Bacteriology 187(23), 7931-7944 (2005).[6]. Teplitski, M., Eberhard, A., Gronquist, M.R., et al. Chemical identification of N-acyl homoserine lactone quorum-sensing signals produced by Sinorhizobium meliloti strains in defined medium Archives of Microbiology 180, 494-497 (2003).[7]. Schaefer, A.L., Taylor, T.A., Beatty, J.T., et al. Long-chain acyl-homoserine lactone quorum-sensing regulation of Rhodobacter capsulatus gene transfer agent production Journal of Bacteriology 184(23), 6515-6521 (2002).[8]. Pearson, J.P., Van Delden, C., and Iglewski, B.H. Active efflux and diffusion are involved in transport of Pseudomonas aeruginosa cell-to-cell signals Journal of Bacteriology 181(4), 1203-1210 (1999).[9]. Mashburn-Warren, L., and Whiteley, M. Special delivery: Vesicle trafficking in prokaryotes Molecular Microbiology 61(4), 839-846 (2006).

RG33, a synthetic 33-amino acid peptide, matches the sequence of amino acids 209-219 and 220-241 found in the C-terminal domain class Y helices of apolipoprotein A1 (ApoA1). This compound has the ability to solubilize multilamellar vesicles (MLVs) containing 1,2-dimyristoyl-sn-glycero-3-PC (DMPC), resulting in the formation of recombinant HDL. When bound to lipids, RG33 facilitates cholesterol efflux in J774 macrophages and has been shown to reduce blood glucose levels in insulin-resistant mice at a dosage of 12 mg/kg.

Thromboxane B3 (TXB3), the stable hydrolysis product of TXA3, is synthesized from eicosapentaenoic acid (EPA) through the action of COX and thromboxane synthase enzymes. This compound is biosynthesized in several tissues, including seminal vesicles, lungs, polymorphonuclear leukocytes (PMNL), and ocular tissues.

SBI-581 is an orally active, potent selective inhibitor of serine-threonine kinase TAO3, with an IC 50 of 42 nM. It effectively promotes the accumulation of TKS5α at RAB11-positive vesicles and inhibits the formation of invadopodia. Additionally, SBI-581 exhibits reasonable pharmacokinetics in mice when administered via IP injection, demonstrating significant antitumor activity [1].

Bam 1745 is a significant adrenomedullary secretory vesicles component.

Deutetrabenazine metabolite M4 is believed to be related to its effect as a reversible depletion of monoamines from nerve terminals. The major circulating metabolites of Deutetrabenazine, are reversible inhibitors of VMAT2, resulting in decreased uptake

JC2-11 is an inhibitory compound for inflammation.JC2-11 inhibits the recruitment domain-containing proteins NLRC 4, atypical in melanoma 2 (AIM 2) and atypical (NC) inflammatory vesicles by disrupting reactive oxygen species (ROS) production and caspase-1 activity.JC2-11 reduces caspase-1 (p20) secretion, gasdermin D (GSDMD) cleavage, IL-1β and lactate dehydrogenase (LDH) activity in inflammatory vesicles. JC2-11 reduced caspase-1 (p20) secretion, gasdermin D (GSDMD) cleavage, IL-1β and lactate dehydrogenase (LDH) release from inflammatory vesicles.

Δ17-6-keto Prostaglandin F1α (Δ17-6-keto PGF1α), a cyclooxygenase (COX) metabolite produced from eicosapentaenoic acid (EPA) in a variety of tissues including seminal vesicles, lungs, polymorphonuclear leukocytes, and ocular tissues, alongside other 3-series COX products from EPA such as PGF3α, PGE3, and thromboxane B3, is potentially linked to a lower occurrence of glaucoma in individuals consuming a marine-rich (EPA-rich) diet.

4-palmitamido TEMPO is a lipid-soluble spin label that integrates into vesicles and cell membranes. It is utilized to examine the encapsulation of molecules within phosphatidylcholine vesicles.

4'-Hydroxychalcone (2-Benzal-4-Hydroxyacetophenone) is a chalcone metabolite with hepatoprotective activity

Vesamicol is an experimental drug. It acting presynaptically by inhibiting acetylcholine uptake into synaptic vesicles and reducing its release.

Chol-PEG, a nonionic surfactant (vesicles), serves as a blood-persistent drug delivery system [1] [2].

Sodium 18:0,22:6 phosphatidylserine (PS) is a lipid found within synaptic vesicles alongside cholesterol, utilized in metabolic research [1].

PEG-8 laurate is a monofunctional surfactant and skin penetration enhancer. It disrupts the skin barrier and facilitates the formation of elastic vesicles when synthesized.

Benzamil is an epithelial sodium channel (ENaC) blocker that inhibits sodium transport from (IC50 = 4 nM) and binds to (Kd = 5 nM) bovine kidney cortex membrane vesicles.

Reserpine (Serpalan) is an alkaloid found in the roots of Rauwolfia serpentina and R. vomitoria. Reserpine inhibits the uptake of norepinephrine into storage vesicles resulting in depletion of catecholamines and serotonin from central and peripheral axon terminals. It has been used as an antihypertensive and an antipsychotic as well as a research tool, but its adverse effects limit its clinical use.

1,2-Dioleoyl-sn-glycero-3-phospho-L-serine sodium (1,2-Dioleoyl-sn-glycero-3-PS (sodium salt)) can be used in lipid mixtures with DOPC and DOPE as effective nontoxic and nonviral DNA vectors. 1,2-Dioleoyl-sn-glycero-3-phospho-L-serine sodium has been used in the formation of unilamellar vesicles to study the effect of curvature on membrane structure and in the formation of supported lipid bilayers to study the effects of various support materials on lipid redistribution between membrane leaflets.

Tetrabenazine (Ro 1-9569) is a drug formerly used as an antipsychotic and treatment of various movement disorders. Tetrabenazine blocks neurotransmitter uptake into adrenergic storage vesicles and has been used as a high affinity label for the vesicle transport system.

Calmidazolium (cation) is a powerful inhibitor of or red blood cell Ca -ATPase & Ca transport into inside-out red blood cell vesicles; an antagonist of calmodulin.

DPTIP is an effective inhibitor of neutral sphingomyelinase 2 with an IC50 value of 30 nM.

1,5-Dihexadecyl N-(3-carboxy-1-oxopropyl)-L-glutamate, a lipid, plays a crucial role in the synthesis of phospholipid vesicles and enhances the encapsulation efficiency of proteins [1].

HKPao (Hunter-killer peptide ao) is a biologically active peptide with dual functionality, exhibiting anti-obesity and anti-tumor pro-apoptotic activities. It induces the release of cytochrome c from vesicles, thereby playing a significant role in cellular apoptosis [1].

DOPE-mPEG (MW 2000), a polydisperse phospholipid PEG (or DOPE liposome), facilitates the targeted delivery of liposomal drugs and the formation of giant unilamellar vesicles (GUVs). Its presence notably diminishes the liposome's pH-sensitivity in a concentration-dependent manner [1] [2] [3].

Quorum sensing is a regulatory system used by bacteria for controlling gene expression in response to increasing cell density. This regulatory process manifests itself with a variety of phenotypes including biofilm formation and virulence factor production. Coordinated gene expression is achieved by the production, release, and detection of small diffusible signal molecules called autoinducers. The N-acylated homoserine lactones (AHLs) comprise one such class of autoinducers, each of which generally consists of a fatty acid coupled with homoserine lactone (HSL). Regulation of bacterial quorum sensing signaling systems to inhibit pathogenesis represents a new approach to antimicrobial therapy in the treatment of infectious diseases. AHLs vary in acyl group length (C4-C18), in the substitution of C3 (hydrogen, hydroxyl, or oxo group), and in the presence or absence of one or more carbon-carbon double bonds in the fatty acid chain. These differences confer signal specificity through the affinity of transcriptional regulators of the LuxR family. C18-HSL is one of four lipophilic, long acyl side-chain bearing AHLs produced by the LuxI AHL synthase homolog SinI involved in quorum sensing signaling in strains of S. meliloti, a nitrogen-fixing bacterial symbiont of the legume M. sativa. C18-HSL and other hydrophobic AHLs tend to localize in relatively lipophilic cellular environments of bacteria and cannot diffuse freely through the cell membrane. The long-chain N-acylhomoserine lactones may be exported from cells by efflux pumps or may be transported between communicating cells by way of extracellular outer membrane vesicles.

Deserpidine (Harmonyl) is only found in individuals that have used or taken this drug. It is an ester alkaloid drug isolated from Rauwolfia canescens (family Apocynaceae) with antipsychotic and antihypertensive properties that has been used for the control of high blood pressure and for the relief of psychotic behavior.Deserpidine's mechanism of action is through inhibition of the ATP/Mg2+ pump responsible for the sequestering of neurotransmitters into storage vesicles located in the presynaptic neuron. Deserpidine is a competitive angiotensin converting enzyme (ACE) inhibitor. Deserpidine also decreases angiotensin II-induced aldosterone secretion by the adrenal cortex.

Kaerophyllin ( (-)-Kaerophylin), a lignan isolated from the traditional Chinese medicine Chai Hu, inhibits activation of hepatic stellate cells by hepatocyte apoptotic vesicles, and protects rat liver from TAA-induced injury and fibrosis by suppressing hepatic inflammation and inhibiting HSC activation.

Diadenosine pentaphosphate pentalithium is an endogenous vasoactive purine dinucleotide, isolated from thrombocytes. It is a member of the diadenosine polyphosphates (ApnA, n=2–7) and is found in secretory vesicles of platelets, chromaffin cells, Torpedo synaptic terminals, and brain synaptosomes.

7-Chlorokynurenic acid sodium salt (7-CKA sodium salt) is a potent and selective antagonist of the glycine B coagonist site of the NMDA receptor (IC50: 0.56 μM). It is also a potent inhibitor of the reuptake of glutamate into synaptic vesicles (Ki: 0.59 μ

FLA-365 is a biochemical that has been shown to inhibit ryanodine-enhanced calcium release from skeletal SR vesicles in a dose-dependent manner.

DPPS (12-Dipalmitoyl-sn-glycero-3-PS sodium salt) is an anionic diacyl-phospholipid, a form of phosphatidylserine (PS), which is a negatively charged phospholipid located in the lobules of cell membranes. DPPS are used to make cationic vesicles and liposomes.

Lys-phe-phe-phe-ile-ile-trp-och3 is a hydrophobic peptide which reacts with lipid vesicles.