GTS-21 HCl

Description

GTS-21 HCl for Sale

All Iron Mountain Labz products are only intended for laboratory research use and are not approved for human consumption.

Overview of GTS-21 HCl

GTS-21 dihydrochloride (DMXB-A; CAS 156223-05-1) is an anabaseine derivative small molecule – a synthetic compound built on the pyridine-tetrahydropyridine bicyclic scaffold of anabaseine, the marine worm toxin from Paranemertes peregrina, with a 2,4-dimethoxybenzylidene substituent at the 3-position of the tetrahydropyridine ring. Molecular formula: C19H20N2O2·2HCl; MW: 369.29 g/mol (dihydrochloride); CAS (free base): 112939-12-5. It is classified as a nootropic research compound. GTS-21 is not a SARM – it targets the α7 nicotinic acetylcholine receptor (α7-nAChR; CHRNA7 gene), not androgen receptors. It is not a peptide – it is a single synthetic small molecule alkaloid derived from the anabaseine scaffold; it contains no amino acid chain.

GTS-21 is the most widely characterized selective α7-nAChR partial agonist in research, with clinical trial history in schizophrenia (Phase 1/2) and extensive preclinical data in cognitive, inflammatory, and neuroprotective research models. Its nootropic classification reflects its primary investigation in α7-nAChR-mediated cognitive enhancement and cholinergic anti-inflammatory pathway (CAP) research.

This product is not approved by the FDA for any therapeutic indication. Intended for laboratory and research purposes only; not a dietary supplement or consumer product. Restricted to qualified researchers and licensed laboratory institutions. IRB guidance required for clinical research; IACUC compliance required for preclinical animal research. Pharmacologically active alkaloid – handle with appropriate precautions.

Chemical Properties

GTS-21 HCl’s Mechanism of Action in Research Models

Within nicotinic receptor pharmacology research, GTS-21 acts as a selective partial agonist of the α7-nAChR homopentamer (five CHRNA7 subunits arranged around a central cation-selective pore). At the orthosteric ACh binding site located at each of the five subunit interfaces within the extracellular domain – formed by the aromatic cage residues Trp147, Tyr93, Tyr188, Tyr195, and the Cys190-Cys191 vicinal disulfide loop – GTS-21 produces submaximal channel activation (~30–40% of maximal ACh response) with slower desensitization kinetics compared to full agonists.

α7-nAChR is a Ca²⁺-permeable channel with a high relative calcium permeability (PCa/PNa ~20), and its activation in macrophages and vagal neurons drives the cholinergic anti-inflammatory pathway (CAP) via JAK2-STAT3 signaling, suppressing NF-κB-mediated TNF-α, IL-1β, IL-6, and HMGB1 production. Kem et al. (2018) conducted a randomized, placebo-controlled, double-blind Phase 1/2 crossover trial of DMXB-A (GTS-21) in schizophrenia patients, characterizing the compound’s pharmacokinetics, cognitive effects on the MATRICS Consensus Cognitive Battery, and P50 sensory gating – establishing the clinical pharmacology profile and pharmacokinetic limitations of this α7-nAChR agonist in human subjects (DOI). Jones et al. (2014) demonstrated in a preclinical rat attentional set-shifting model that GTS-21, alongside other α7-nAChR agonists, significantly reversed MK-801-induced executive function deficits in a maze-based assay – validating the preclinical framework for α7-nAChR agonist cognitive research (DOI). Data remains limited, and findings are not consistent across all model systems.

Risk & Handling

Risk Tier: MODERATE

GTS-21 is a pharmacologically active α7-nAChR partial agonist alkaloid – active at micromolar concentrations:

• CNS/immune activity: Avoid skin contact and inhalation – systemic absorption risk through mucosa or skin
• DMSO solutions: Chemical-resistant gloves required – DMSO is a penetration enhancer
• HCl salt: Mildly acidic in aqueous solution – avoid eye contact; flush immediately with water if contact occurs
• PPE: Nitrile gloves, lab coat, and safety eyewear for all handling operations
• No DEA scheduling; not a controlled substance – verify applicable local regulations
• No human safety data established for this research-grade formulation. Contact help@ironmountainlabz.com for the Safety Data Sheet.

Why Buy GTS-21 HCl from Iron Mountain Labz?

• Purity: ≥99% by HPLC-UV per lot
• Identity: confirmed by ¹H-NMR and LC-MS/MS per lot
• Residual solvents: ≤300 ppm by GC headspace per lot (ICH Q3C compliant)
• Endotoxin: ≤1.0 EU/mg (LAL gel-clot method)
• Certificate of Analysis available on request per lot
• For queries, complaints, or support, please contact help@ironmountainlabz.com 

FAQs

Q1: What is GTS-21 chemically, and why is it not a SARM or peptide?
GTS-21 is an anabaseine derivative small molecule – a single synthetic alkaloid built on the pyridine-tetrahydropyridine scaffold of the marine toxin anabaseine with a 2,4-dimethoxybenzylidene substituent. It contains no amino acid chain, making it definitively not a peptide. It targets α7-nAChR – not androgen receptors – making it definitively not a SARM. Its nootropic classification reflects its investigation in α7-nAChR-mediated cognitive, neuroprotective, and anti-inflammatory research.

Q2: What is GTS-21’s clinical research history?
GTS-21 (DMXB-A) has been investigated in Phase 1/2 clinical trials for cognitive deficits in schizophrenia, examining effects on the MATRICS Consensus Cognitive Battery and P50 auditory gating. Iron Mountain Labz supplies research-grade material for laboratory investigation only – not as a clinical formulation. Not FDA-approved for any indication.

Q3: What research applications has GTS-21 been investigated in?
In preclinical and in vitro laboratory settings: α7-nAChR binding and functional assays (electrophysiology, Ca²⁺ imaging), cholinergic anti-inflammatory pathway research (macrophage NF-κB/STAT3 signaling, TNF-α/HMGB1 assays), attentional set-shifting and cognitive flexibility assays in rodent models, P50 sensory gating models, and comparative α7-nAChR pharmacology (partial vs. full agonist studies). All in laboratory and preclinical contexts only.

Q4: How does GTS-21 differ from full α7-nAChR agonists in research?
GTS-21 produces ~30–40% of maximal ACh response (partial agonist) and desensitizes more slowly than full agonists – enabling sustained α7-nAChR signaling in research assays. This partial agonism reduces the risk of receptor tachyphylaxis that limits the research utility of full agonists. GTS-21 shows greater α7 selectivity over α4β2 receptors than nicotine, making it a useful tool for α7-specific mechanistic research.

Q5: What safety precautions apply to GTS-21 research handling?
Pharmacologically active alkaloid – avoid skin contact and inhalation. Nitrile gloves, lab coat, eyewear. Chemical-resistant gloves for DMSO solutions. HCl salt is mildly acidic – flush eyes immediately with water if contact occurs. No human safety data established for this research-grade formulation. Contact help@ironmountainlabz.com for the Safety Data Sheet.

References

1. 1. Kem WR, Olincy A, Johnson L, et al. Pharmacokinetic limitations on effects of an alpha7-nicotinic receptor agonist in schizophrenia: randomized trial with an extended-release formulation. Neuropsychopharmacology. 2018;43(3):583–589. PMID: 28825423.
      https://pubmed.ncbi.nlm.nih.gov/28825423/
   2. Jones KM, McDonald IM, Bourin C, et al. Effect of alpha7 nicotinic acetylcholine receptor agonists on attentional set-shifting impairment in rats. Psychopharmacology (Berl). 2014;231(4):673–683. PMID: 24057763.
      https://pubmed.ncbi.nlm.nih.gov/24057763/
   3. Pavlov VA, Ochani M, Yang LH, et al. Selective alpha7-nicotinic acetylcholine receptor agonist GTS-21 improves survival in murine endotoxemia and severe sepsis. Critical Care Medicine. 2007;35(4):1139–1144. PMID: 17334244 https://pubmed.ncbi.nlm.nih.gov/17334244/