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Membrane Transporter/Ion Channel Inhibitors, Agonists, Screening Libraries www.MedChemExpress.com Membrane Transporter/Ion Channel Most of molecules enter or leave cells mainly via membrane transport proteins, which play important roles in several cellular functions, including cell metabolism, ion homeostasis, signal transduction, binding with small molecules in extracellular space, the recognition process in the immune system, energy transduction, osmoregulation, and physiological and developmental processes. There are three major types of transport proteins, ATP-powered pumps, channel proteins and transporters. ATP-powered pumps are ATPases that use the energy of ATP hydrolysis to move ions or small molecules across a membrane against a chemical concentration gradient or electric potential. Channel proteins transport water or specific types of ions down their concentration or electric potential gradients. Many other types of channel proteins are usually closed, and open only in response to specific signals. Because these types of ion channels play a fundamental role in the functioning of nerve cells. Transporters, a third class of membrane transport proteins, move a wide variety of ions and molecules across cell membranes. Membrane transporters either enhance or restrict drug distribution to the target organs. Depending on their main function, these membrane transporters are divided into two categories: the efflux (export) and the influx (uptake) transporters. Transport proteins such as channels and transporters play important roles in the maintenance of intracellular homeostasis, and mutations in these transport protein genes have been identified in the pathogenesis of a number of hereditary diseases. In the central nervous system ion channels have been linked to many diseases such, but not limited to, ataxias, paralyses, epilepsies, and deafness indicative of the roles of ion channels in the initiation and coordination of movement, sensory perception, and encoding and processing of information. Furthermore, drug transporters can serve as drug targets or as a mechanism to facilitate drug delivery to cells and tissues. References: [1] Sadée W, et al. Pharm Res. 1995 Dec;12(12):1823-37. [2] Girardin F. Dialogues Clin Neurosci. 2006;8(3):311-21. [3] Zaydman MA, et al. Chem Rev. 2012 Dec 12;112(12):6319-33. www.MedChemExpress.com 1 2 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] Inhibitors, Agonists, Screening Libraries www.MedChemExpress.com Target List in Membrane Transporter/Ion Channel • ATP Synthase 3 • Proton Pump 101 • BCRP 6 • SGLT 106 • Calcium Channel 8 • Sodium Channel 109 • CFTR 22 • TRP Channel 119 • Chloride Channel 25 • URAT1 127 • CRAC Channel 28 • CRM1 30 • EAAT2 32 • GABA Receptor 34 • GlyT 45 • HCN Channel 47 • iGluR 49 • Monoamine Transporter 61 • Monocarboxylate Transporter 64 • Na+/Ca2+ Exchanger 66 • Na+/HCO3- Cotransporter 68 • Na+/K+ ATPase 70 • nAChR 73 • NKCC 79 • P-glycoprotein 81 • P2X Receptor 85 • Potassium Channel 88 www.MedChemExpress.com 3 ATP Synthase ATPases are a class of enzymes that catalyze the decompositionof ATP into ADP and a free phosphate ion. This dephosphorylation reaction releases energy, which the enzyme (in most cases) harnesses to drive other chemical reactions that would not otherwise occur. Some such enzymes are integral membrane proteins and move solutes across the membrane, typically against their concentration gradient. These are called transmembrane ATPases. Transmembrane ATPases import many of the metabolites necessary for cell metabolism and export toxins, wastes, and solutes that can hinder cellular processes. Such as the sodium-potassium exchanger (or Na + /K + ATPase) and the hydrogen potassium ATPase (H +/K + ATPase or gastric proton pump) that acidifies the contents of the stomach. 4 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] ATP Synthase Inhibitors & Modulators ATP synthase inhibitor 1 BTB06584 Cat. No.: HY-112715 Cat. No.: HY-15877 Bioactivity: ATP synthase inhibitor 1 is a potent inhibitor of c subunit Bioactivity: BTB06584 is an IF1-dependent selective inhibitor of the mitochondrial F1Fo-ATPase. of the F1/FO-ATP synthase complex, inhibits mitochondrial permeability transition pore (mPTP) opening, does not affect ATP levels [1]. Purity: >98% Purity: 98.48% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 100 mg, 250 mg, 500 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg Gboxin Oligomycin A Cat. No.: HY-111651 (MCH 32) Cat. No.: HY-16589 Bioactivity: Gboxin is an oxidative phosphorylation inhibitor that targets Bioactivity: Oligomycin A, created by Streptomyces, acts as a glioblastoma. Gboxin inhibits the activity of F0F1 ATP mitochondrial F0F1-ATPase inhibitor, with a Ki of 1 μM; synthase [1]. Antitumour activity [1]. Oligomycin A shows anti-fungal activity. Purity: 99.32% Purity: 99.94% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 1 mg, 5 mg www.MedChemExpress.com 5 BCRP Breast cancer resistance protein;ABCG2 BCRP(breast cancer resistant protein) is an ATP-binding cassette (ABC) transporter, which together with two other ABC efflux drug pumps, namely P-glycoprotein (P-gp, ABCB1) and multidrug resistance-related protein 1 (MRP1, ABCC1) is the most important multidrug resistance protein found in eukaryotic cells including cells in the testis. Breast cancer resistance protein (BCRP/ABCG2) is known to localize at the blood-brain barrier (BBB) and can significantly restrict xenobiotic permeability in the brain. The objective of this study is to investigate the regulation of BCRP functional expression by peroxisome proliferator-activated receptor alpha (PPARα), a ligand-activated transcription factor primarily involved in lipid metabolism, in a cerebral microvascular endothelial cell culture system (hCMEC/D3), representative of human BBB. 6 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] BCRP Inhibitors & Modulators BCRP-IN-1 Elacridar Cat. No.: HY-100390 (GF120918; GW0918; GG918; GW120918) Cat. No.: HY-50879 Bioactivity: BCRP-IN-1 is a breast cancer resistance protein ( BCRP) Bioactivity: Elacridar is a potent P-glycoprotein (Pgp) and BCRP inhibitor with an IC50 of 0.6 μM on BCRP efflux transporter. inhibitor. Purity: 98.13% Purity: 98.47% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10 mg, 50 mg, 100 mg, 200 mg, 500 mg 5 mg, 10 mg, 25 mg, 50 mg, 100 mg Fumitremorgin C Ko 143 (12α-Fumitremorgin C) Cat. No.: HY-N2143 Cat. No.: HY-10010 Bioactivity: Fumitremorgin C is a potent and selective ABCG2/BRCP Bioactivity: Ko 143 is a potent and selective ATP-binding cassette inhibitor. sub-family G member 2 ( ABCG2) inhibitor. Purity: 99.63% Purity: 99.79% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 250u g, 1 mg 5 mg, 10 mg, 50 mg, 100 mg KS176 YHO-13177 Cat. No.: HY-19753 Cat. No.: HY-12757 Bioactivity: KS176 is a potent and selective inhibitor of the breast cancer Bioactivity: YHO-13177 is a potent and specific inhibitor of BCRP; resistance protein (BCRP) multidrug transporter (IC50 values potentiated the cytotoxicity of SN-38 in cancer cells and no are 0.59 and 1.39 μM in Pheo A and Hoechst 33342 assays effect on P-glycoprotein–mediated paclitaxel resistance in respectively). Displays no inhibitory activity against P-gp or MDR1-transduced human leukemia K562 cells. MRP1. Purity: 99.21% Purity: 98.72% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg YHO-13351 YHO-13351 free base Cat. No.: HY-12758 Cat. No.: HY-12758A Bioactivity: YHO-13351 is the water-soluble prodrug of YHO-13177, which is Bioactivity: YHO-13351 (free base) is the water-soluble prodrug of a potent and specific inhibitor of BCRP. YHO-13177, which is a potent and specific inhibitor of BCRP. Purity: >98% Purity: 98.10% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 5 mg, 10 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg Zamicastat (BIA 5-1058) Cat. No.: HY-106004 Bioactivity: Zamicastat (BIA 5-1058) is a dopamine β-hydroxylase (DBH) inhibitor that could cross the blood-brain barrier (BBB) and cause central as well as peripheral effects. Zamicastat is also a concentration-dependent dual P-gp and BCRP inhibitor [1] with IC50 values of 73.8 μM and 17.0 μM, respectively .… Purity: 99.95% Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg www.MedChemExpress.com 7 Calcium Channel Ca2+ channels;Ca channels Calcium channel is an ion channel which displays selective permeability to calcium ions. It is sometimes synonymous as voltage-dependent calcium channel, although there are also ligand-gated calcium channels. Voltage-gated calcium (CaV) channels catalyse rapid, highly selective influx of Ca 2+ into cells despite a 70-fold higher extracellular concentration of Na +. Some calcium channel blockers have the added benefit of slowing your heart rate, which can further reduce blood pressure, relieve chest pain (angina) and control an irregular heartbeat. 8 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] Calcium Channel Inhibitors & Modulators (+)-Kavain ABT-639 Cat. No.: HY-B1671 Cat. No.: HY-19721 Bioactivity: (+)-Kavain, a main kavalactone extracted from Piper Bioactivity: ABT-639 is a novel, peripherally acting, selective T-type methysticum, has anticonvulsive properties, attenuating Ca2+ channel blocker. vascular smooth muscle contraction through interactions with voltage-dependent Na + and Ca 2+ channels [1]. (+)-Kav… Purity: 99.98% Purity: 99.15% Clinical Data: No Development Reported Clinical Data: Phase 2 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg 1 mg, 5 mg, 10 mg, 50 mg, 100 mg ABT-639 hydrochloride Acetylcholine chloride Cat.
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