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GSM-1

Chemical Structure : GSM-1

CAS No.: 884600-68-4

GSM-1 (GSM1)

Catalog No.: PC-35113Not For Human Use, Lab Use Only.

GSM-1 (GSM1) is a γ-secretase modulator that directly targets the transmembrane domain (TMD) 1 of presenilin 1, shows potent Aβ42-lowering effect (IC50=0.348 uM) in a cell-based assay.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

GSM-1 (GSM1) is a γ-secretase modulator that directly targets the transmembrane domain (TMD) 1 of presenilin 1, shows potent Aβ42-lowering effect (IC50=0.348 uM) in a cell-based assay.
GSM-1 does not affect total Aβ and its C-terminal counterpart product, APP intracellular domain (AICD), selectively reduced the Aβ42 generation accompanied by an increase in Aβ38 in in-vitro assay.
GSM-1 decreases the ratio of Aβ42 to Aβ40 to 60% in plasma and the ratio of Aβ42 to total Aβ to 65% in cerebrospinal fluid from baseline to postdosing in monkeys (30 mg/kg)

Physicochemical Properties

M.Wt 481.98
Formula C26H31ClF3NO2
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

2-((2S,4R)-1-((R)-1-(4-chlorophenyl)-4-methylpentyl)-2-(4-(trifluoromethyl)phenyl)piperidin-4-yl)acetic acid

References

1. Page RM, et al. J Biol Chem. 2010 Jun 4;285(23):17798-810.

2. Kretner B, et al. J Biol Chem. 2011 Apr 29;286(17):15240-51.

3. Ohki Y, et al. EMBO J. 2011 Oct 14;30(23):4815-24.

4. Ling IF, et al. Alzheimers Res Ther. 2015 Aug 5;7(1):55.

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