GTS-21 2HCl, also known as DMBX-A, is a derivative of the natural product anabaseine that acts as a partial agonist at neural nicotinic acetylcholine receptors. It binds to both the α4β2 and α7 subtypes, but activates only the α7 to any significant extent. Both GTS-21 itself and its demethylated active metabolite 4-OH-GTS-21 display nootropic and neuroprotective effects, and GTS-21 is being investigated for the treatment of Alzheimer's disease, nicotine dependence, and, most significantly, for schizophrenia.
Chemical Formula: C19H22Cl2N2O2
Exact Mass: 308.15248
Molecular Weight: 381.3
Elemental Analysis: C, 59.85; H, 5.82; Cl, 18.59; N, 7.35; O, 8.39
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
Yue Y, Liu R, Cheng W, Hu Y, Li J, Pan X, Peng J, Zhang P. GTS-21 attenuates lipopolysaccharide-induced inflammatory cytokine production in vitro by modulating the Akt and NF-κB signaling pathway through the α7 nicotinic acetylcholine receptor. Int Immunopharmacol. 2015 Oct 17. pii: S1567-5769(15)30138-7. doi: 10.1016/j.intimp.2015.10.005. [Epub ahead of print] PubMed PMID: 26490221.
Kong FJ, Ma LL, Zhang HH, Zhou JQ. Alpha 7 nicotinic acetylcholine receptor agonist GTS-21 mitigates isoflurane-induced cognitive impairment in aged rats. J Surg Res. 2015 Mar;194(1):255-61. doi: 10.1016/j.jss.2014.09.043. Epub 2014 Oct 5. PubMed PMID: 25450597.
Wu S, Zhao H, Luo H, Xiao X, Zhang H, Li T, Zuo X. GTS-21, an α7-nicotinic acetylcholine receptor agonist, modulates Th1 differentiation in CD4(+) T cells from patients with rheumatoid arthritis. Exp Ther Med. 2014 Aug;8(2):557-562. Epub 2014 Jun 3. PubMed PMID: 25009619; PubMed Central PMCID: PMC4079428.
Hu Y, Liu R, Li J, Yue Y, Cheng W, Zhang P. Attenuation of Collagen-Induced Arthritis in rat by nicotinic alpha7 receptor partial agonist GTS-21. Biomed Res Int. 2014;2014:325875. doi: 10.1155/2014/325875. Epub 2014 Feb 27. PubMed PMID: 24719855; PubMed Central PMCID: PMC3955649.
Sitapara RA, Antoine DJ, Sharma L, Patel VS, Ashby CR Jr, Gorasiya S, Yang H, Zur M, Mantell LL. The α7 nicotinic acetylcholine receptor agonist GTS-21 improves bacterial clearance in mice by restoring hyperoxia-compromised macrophage function. Mol Med. 2014 Jun 19;20:238-47. doi: 10.2119/molmed.2013.00086. PubMed PMID: 24664237; PubMed Central PMCID: PMC4069272.
Products are for research use only. Not for human use.
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