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Membrane Transporter/Ion Channel-Targeted Compounds

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Membrane Transporter/Ion Channel-Targeted Compounds Targets Applications Advantages Publication FAQs

Overview

(Source: Bioicons, free)

Obesity is a metabolic disease induced by multiple factors, which mainly stem from the imbalance between energy intake and consumption. Membrane transporters and ion channels, as key targets in the regulation of energy metabolism, fat storage, and signaling, have become the core direction of drug discovery. With cutting-edge synthetic chemistry technology, Protheragen provides high-purity and high-activity membrane transporter/ion channel-related compounds to accelerate the discovery and validation of therapeutic targets for obesity.

Features of Membrane Transporter/Ion Channel

Membrane transporters (e.g., glucose transporters, fatty acid transporters) and ion channels (e.g., calcium channels, potassium channels) serve as key nodes of cellular signaling and directly regulate lipid metabolism, energy homeostasis, and neural appetite regulation. Our company offers a range of glucose transporter type 4 (GLUT4) agonists, sodium-dependent glucose transporters 2 (SGLT2) inhibitors for regulating glucose uptake and excretion, and inhibiting fat accumulation. Moreover, we also offer transient receptor potential vanilloid-1/4 (TRPV1/4) antagonists, voltage-gated Ca2+ (CaV) channel modulators for regulating intracellular calcium signaling, which affects appetite and energy expenditure.

Fig. 1 Schematic illustration of the human TRPM2 channel. Fig.1 Human TRPM2 channel. (Yu, et al., 2021)

Targets

Our company offers compounds with a wide range of targets and receptors for clients to choose from.

  • 5-HT receptor
  • ABC
  • AChR
  • Adrenergic receptor
  • AMPK
  • Antibacterial
  • Antioxidant
  • Apoptosis
  • ATPase
  • Autophagy
  • Calcium channel
  • CaMK
  • CFTR
  • COX
  • Dopamine receptor
  • Endogenous metabolite
  • ERK
  • Fatty acid synthase
  • FXR
  • GABA receptor
  • HCN channel
  • HER
  • HIF/HIF prolyl-hydroxylase
  • Histamine receptor
  • HIV protease
  • Influenza virus
  • JNK
  • Lipoxygenase
  • MMP
  • NADPH
  • NF-κB
  • Norepinephrine
  • NOS
  • NPC1L1
  • Opioid receptor
  • p38 MAPK
  • P-gp
  • Potassium channel
  • PPAR
  • Protease-activated receptor
  • Reactive oxygen species
  • Sigma receptor
  • SGLT
  • Serotonin transporter
  • Sodium channel
  • STAT
  • TLR
  • TNF
  • Trk receptor
  • TRP/TRPV channel
  • Wnt/beta-catenin

Applications

  • Adipocyte Differentiation and Insulin Resistance: Membrane transporter/ion channel-related compounds can be used to reveal the role of transporters/ion channels in adipocyte differentiation, insulin resistance.
  • Energy Metabolism Regulation and Screening: Membrane transporter/ion channel-related compounds can be used to screen out key molecules that regulate energy metabolism and drive drug development.
  • Obesity Indicators and In Vivo Validation: Membrane transporter/ion channel-related compounds can be used to assess the effect of specific targets on obesity-related metrics (e.g., body weight, blood glucose, fat distribution).

Advantages of Us

High Purity Guarantee

All compounds are strictly tested by high-performance liquid chromatography (HPLC) and nuclear magnetic resonance (NMR), with purity ≥98%, ensuring the reliability of experimental results.

Structural Diversity

Our products offer exceptional structural diversity, covering core targets such as GLUTs, SGLTs, and TRP channels to meet diverse research needs.

Customized Service

Our company supports special structural modification, isotope labeling, and other customized needs to match the experimental design.

Publication

Title: Regulation of intestinal glucose absorption by ion channels and transporters

Journal: Nutrients, 2016

DOI: https://doi.org/10.3390/nu8010043

Summary: The present study demonstrates that the potassium voltage-gated channel subfamily E regulatory subunit 1 (KCNE1)-dependent movement of K+ from the cell to the lumen contributes to the maintenance of the electrical drive for Na+-coupled transport in proximal tubules. Calcium channels and calcium-sensing receptors (CaSR) also play an important role in regulating glucose uptake in intestinal epithelial cells (IEC). Increased cytoplasmic [Ca2+] binds to calmodulin (CaM) via the CaSR to form a complex that further regulates adenosine monophosphate-activated protein kinase (AMPK) and activates SGLT1 or GLUT2, thereby modulating small intestinal glucose absorption. This literature provides an important review and insights for understanding the role of ion channels in intestinal glucose absorption and provides new ideas and approaches for the prevention and treatment of obesity and related metabolic diseases.

Fig. 2 Schematic illustration of regulatory mechanisms of small intestinal glucose uptake by cation channels and transporters. Fig.2 Schematic diagram of the mechanism regulating glucose uptake in the small intestine. (Chen, et al., 2016)

Customer Review

Targeted Glucose Homeostasis
"Using Protheragen's membrane transporter library to study key metabolic transporters and analyze cellular uptake rates has significantly accelerated research progress in obesity-related diseases."— Prof. M* W***

Reliability in Complex Assays
"Protheragen's compound library exhibits high purity and stability. This ensures our throughput activity data possesses exceptional reproducibility, significantly boosting our project's screening efficiency and success rate."— C. H* B***

Frequently Asked Questions

  1. What are the functional differences between ion channels and transporter proteins?
    • Ion channels are usually passive transporters, dependent on electrochemical gradients or concentration gradients, and require no additional energy input.
    • Transporter proteins can be either passively transported (e.g., carrier proteins) or actively transported (e.g., ATP-driven pumps). Active transport requires ATP consumption to transport molecules against the concentration gradient.
  2. What are the main types of ion channels?

    Ion channels can be categorized into voltage-gated channels, ligand-gated channels, and stress-activated channels according to their structural and functional characteristics. These channels play an important role in maintaining intra- and extracellular ionic balance, regulating cellular excitability, and participating in the development of diseases.

  3. What are the applications of membrane transporters in anti-obesity drug development?

    Membrane transporters are important targets for drug discovery and development due to their key role in drug absorption, distribution, and excretion. For example, drug transporters affect drug absorption and excretion, so we improve drug selectivity and bioavailability by designing artificial transporters or modifying natural transporters.

Depending on the efficiency of our production team, Protheragen provides high-purity membrane transporter/ion channel products to meet the needs of our clients in the field of biological research. If you don't find what you need, please feel free to contact us for efficient, customized solutions!

Reference

  1. Chen, L.; et al. Regulation of intestinal glucose absorption by ion channels and transporters. Nutrients. 2016, 8(1): 43. (CC BY 4.0)
  2. Yu, X.; et al. Structural and functional basis of the selectivity filter as a gate in human TRPM2 channel. Cell Reports. 2021, 37(7). (CC BY 4.0)

Membrane Transporter/Ion Channel-Targeted Compounds

By Target
By Receptor
By Identity
By Formulation
Fatostatin hydrobromide (OB0225LY-0004)
  • CAS No.: 298197-04-3
  • Pathways: Membrane transporter/Ion channel; Metabolism
  • Targets: Fatty acid synthesis; NPC1L1
  • Receptors: Fatty acid synthase; SREBPs
Fatostatin hydrobromide
FGH10019 (OB0225LY-0016)
  • CAS No.: 1046045-61-7
  • Pathways: Membrane transporter/Ion channel; Metabolism
  • Targets: NPC1L1; Fatty acid synthesis
  • Receptors: Fatty acid synthase; SREBPs
FGH10019
Amitriptyline hydrochloride (OB0225LY-0099)
  • CAS No.: 549-18-8
  • Pathways: Membrane transporter/Ion channel; Tyrosine kinase/adaptors; Immunology/Inflammation; GPCR/G protein; Neuronal signaling
  • Targets: Monoamine transporters; G protein-coupled receptors (GPCRs); Neurotrophin receptors; Ion channels
  • Receptors: 5-HT receptor; mAChR; Norepinephrine receptor; Serotonin transporter; Sodium channel; Trk receptor; σ1; Histamine receptor; Adrenergic receptor
Amitriptyline hydrochloride
Chenodeoxycholic acid (OB0225LY-0313)
  • CAS No.: 474-25-9
  • Pathways: Membrane transporter/Ion channel; Autophagy; Metabolism
  • Targets: Nuclear receptors; Ion channels
  • Receptors: FXR; Potassium channel
Chenodeoxycholic acid
Trifluoperazine dihydrochloride (OB0225LY-0425)
  • CAS No.: 440-17-5
  • Pathways: Membrane transporter/Ion channel; Autophagy; GPCR/G protein; Microbiology/Virology; Neuronal signaling
  • Targets: G protein-coupled receptors (GPCRs); ABC transporters; Calcium-binding proteins/kinases
  • Receptors: Adrenergic receptor; CaMK; Dopamine receptor; P-gp (P-glycoprotein)
Trifluoperazine dihydrochloride
Dronedarone hydrochloride (OB0225LY-0455)
  • CAS No.: 141625-93-6
  • Pathways: Membrane transporter/Ion channel; GPCR/G protein; Metabolism; Autophagy; Neuronal signaling
  • Targets: Ion channels; G protein-coupled receptors (GPCRs)
  • Receptors: Adrenergic receptor; Calcium channel; Potassium channel; Sodium channel
Dronedarone hydrochloride
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