GSM-1

Names

[ Name ]:
GSM-1

[Synonym ]:
{(2S,4R)-1-[(1R)-1-(4-Chlorophenyl)-4-methylpentyl]-2-[4-(trifluoromethyl)phenyl]-4-piperidinyl}acetic acid
RY5QK2J15V
GSM-1
4-Piperidineacetic acid, 1-[(1R)-1-(4-chlorophenyl)-4-methylpentyl]-2-[4-(trifluoromethyl)phenyl]-, (2S,4R)-

Biological Activity

[Description]:

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; 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; 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)

[References]

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. View Related Products by Target γ-secretase

Chemical & Physical Properties

[ Density]:
1.2±0.1 g/cm3

[ Boiling Point ]:
547.7±50.0 °C at 760 mmHg

[ Molecular Formula ]:
C₂₆H₃₁ClF₃NO₂

[ Molecular Weight ]:
481.978

[ Flash Point ]:
285.0±30.1 °C

[ Exact Mass ]:
481.199554

[ LogP ]:
6.96

[ Vapour Pressure ]:
0.0±1.5 mmHg at 25°C

[ Index of Refraction ]:
1.531

Related Compounds

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