pumps

Norverapamil hydrochloride (D591 hydrochloride) 是 Verapamil 的 N-去甲基代谢物，是 L 型钙通道阻滞剂和 P-糖蛋白 (P-gp) 功能抑制剂。

Annonacin is an Acetogenin and promotes cytotoxicity via a pathway inhibiting the mitochondrial complex and it is the active agent found in Graviola leaf extract to act as an inhibitor of sodium potassium (NKA) and sarcoplasmic reticulum (SERCA) ATPase pu

Levolansoprazole ((S)-Lansoprazole) 是一种质子泵抑制剂，不可逆地抑制壁细胞中 H+ K+ 刺激的 ATPase 泵 (IC50: 5.2 µM)。它还抑制分离的犬壁细胞中的酸形成(IC50：82 µM)。 (R)-和 (S)-兰索拉唑均具有药理活性，具有相似的效力。

DJ101is an effective and metabolically stable inhibitor of tubulin. It can circumvent the drug efflux pumps responsible for multidrug resistance of existing tubulin inhibitors.

Bromotetrandrine is an P-glycoprotein inhibitor, which were developed and coadministered with chemotherapeutic drugs to overcome the effect of efflux pumps thus enhancing the chemosensitivity of therapeutics.

Milbemycin A4 oxime is a derivative of milbemycin A4 and a component of milbemycin oxime , compounds that both have insecticidal and nematocidal activity. Milbemycin A4 oxime (0.05 mg kg) reduces the number of microfilariae of the heartworm D. immitis in naturally infested dogs. It inhibits the growth of clinical isolates of C. glabrata with MIC80 values ranging from 16 to greater than 32 μg ml. Milbemycin A4 oxime (2.5 μg ml) blocks efflux of fluconazole from a clinical isolate of C. glabrata, but not from a strain lacking the efflux pumps CgCDR1 and PDH1, and reduces the MICs of fluconazole and 4-nitroquinoline 1-oxide in wild-type C. glabrata. It enhances adriamycin-induced inhibition of cell growth, as well as increases the intracellular accumulation of adriamycin and the P-glycoprotein substrate rhodamine 123 , in adriamycin-resistant, but not -sensitive, MCF-7 breast cancer cells in a concentration-dependent manner.

Ultrapotent PSEM (uPSEM) agonist for PSAM4-GlyR and PSAM4-5HT3 (Ki = 0.7 nM for PSAM4-GlyR and <10 nM for PSAM4-5HT3). Exhibits >10,000-fold agonist selectivity for PSAM4-GlyR over α7-GlyR, α7-5HT3, and 5HT3-R, and 230-fold selectivity over α4β2 nAChR. Also weak partial agonist (~10 %) at α4β2 nAChR. Retains the potency of varenicline (Cat.No. 3754) for PSAM4-GlyR with enhanced chemogenetic selectivity. Does not act as a substrate for P-glycoprotein pumps. Silences neurons in vivo. Brain-penetrant. Magnus et al (2019) Ultrapotent chemogenetics for research and potential clinical applications. Science doi: 10.1126/science PMID:30872534

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).

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.

ATP dipotassium (Adenosine 5'-triphosphate dipotassium) is a vital compound involved in energy storage and metabolism within living organisms. It plays a crucial role in supplying metabolic energy for driving pumps and acts as a coenzyme in cellular processes. Additionally, ATP dipotassium functions as a significant endogenous signaling molecule contributing to immunity and inflammation.

4SC-207 is a novel microtubule inhibitor , which shows strong anti-proliferative activity in a large panel of tumor cell lines with an average GI50 of 11 nM. In particular, 4SC-207 is active in multi-drug resistant cell lines, such as HCT-15 and ACHN, suggesting that it is a poor substrate for drug efflux pumps. 4SC-207 inhibits microtubule growth in vitro and in vivo and promotes, in a dose dependent manner, a mitotic delay arrest, followed by apoptosis or aberrant divisions due to chromosome alignment defects and formation of multi-polar spindles. Furthermore, preliminary data from preclinical studies suggest low propensity towards bone marrow toxicities at concentrations that inhibit tumor growth in paclitaxel-resistant xenograft models. 4SC-207 may be a potential anti-cancer agent.

ATP ditromethamine（Adenosine 5'-triphosphate ditromethamine）作为体内能量储存和代谢的核心物质，不仅为代谢过程提供必需能量，而且在细胞中担任辅酶角色。此外，它在免疫和炎症反应中，扮演着关键的内源性信号分子角色。

Caloxin 3A1是生物活性肽，属于caloxins系列，特指抑制外质膜(Plasma membrane, PM) Ca2+泵的化合物。具体作用通过抑制质膜钙泵(PMCA)并保持对肌浆网Ca2+泵无影响；同时，该肽不干预ATP合成酰基磷酸中间产物的形成。

Timcodar mesylate (VX-853-2)与其类似物VX-710是抑制哺乳动物多药耐药性的关键物质，能够有效阻止金黄色葡萄球菌中溴化乙锭的外排。这种化合物通过抑制细菌的外排泵机制，有助于提升抗生素的效力，并可能显著降低对革兰阳性病原体如金黄色葡萄球菌、肠球菌以及肺炎链球菌的抗生素最小抑制浓度。

P-gp modulator-5（compound 25）是一种P-gp的调节剂，旨在抑制多药耐药性（MDR）肿瘤的扩散。该化合物通过减弱MDR细胞中的药物外排泵功能，引起大量ROS的积累及细胞周期的变化，从而阻止肿瘤增殖。

Levolansoprazole-d4 是 Levolansoprazole 的氘代化合物。Levolansoprazole 的 CAS 号为 138530-95-7。Levolansoprazole 是一种质子泵抑制剂，不可逆地抑制壁细胞中 H+ K+ 刺激的 ATPase 泵 (IC50: 5.2 µM)。它还抑制分离的犬壁细胞中的酸形成（IC50：82 µM）。 (R)-和 (S)-兰索拉唑均具有药理活性，具有相似的效力。

Volkensiflavone (Talbotaflavone) 是一种天然产物，存在于黄芪和藤黄中。它具有植物代谢物的作用,是一种次生代谢产物。Volkensiflavone 是一种双类黄酮，属于羟黄酮和羟黄酮。Volkensiflavone 可以作为佐剂用于过表达外排泵的多药耐药金黄色葡萄球菌的抗生素治疗。

CALP3 acetate(261969-05-5 free base) 是一种有效的 Ca2+ 通道阻滞剂，可激活 Ca2+ 结合蛋白的 EF 手基序。 它可以通过调节钙调蛋白 (CaM)、Ca2+ 通道和泵的活性在功能上模拟增加的 [Ca2+]i。

CALP3 TFA is a potent Ca2+ channel blocker that activates EF-hand motifs of Ca2+-binding proteins. It can functionally mimic increased [Ca2+]i by modulating the activity of Calmodulin, Ca2+ channels, and pumps.

Cerium oxide, 99.99% metals basis, <5 μm 是一种用于生化分析的试剂，具有抗炎特性以及SOD和过氧化氢酶模拟的活性。它可用于治疗慢性炎症，并适用于多种工业应用，如固体氧化物燃料电池、太阳能电池、催化剂、氧气泵和气体传感器。