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CAY10614

Names

[ CAS No. ]:
1202208-36-3

[ Name ]:
CAY10614

[Synonym ]:
Benzenemethanaminium, N-cyclopentyl-N,N-dimethyl-3,4-bis(tetradecyloxy)-, iodide (1:1)
N-[3,4-Bis(tetradecyloxy)benzyl]-N,N-dimethylcyclopentanaminium iodide

Biological Activity

[Description]:

CAY10614 is a potent TLR4 antagonist. CAY10614 inhibits the lipid A-induced activation of TLR4, with an IC50 of 1.675 μM. CAY10614 can improve survival of mice in lethal endotoxin shock model[1][2].

[Related Catalog]:

Signaling Pathways >> Immunology/Inflammation >> Toll-like Receptor (TLR)
Research Areas >> Neurological Disease

[Target]

TLR4:1.675 μM (IC50, in HEK293 cells)


[In Vitro]

CAY10614 (compound 7) (1-10 μM) inhibits the lipid A-induced increase of phosphatase activity in a concentration-dependent manner in HEK293 cells[1]. CAY10614 (0.5 μM) inhibits the increase of [Ca2+]cyt induced by LPS in >18 days in vitro (DIV) neurons[2].

[In Vivo]

CAY10614 (compound 7) (10 mg/kg; i.p. 30 min before the LPS) significantly improves survival of mice given intraperitoneal LPS (20 mg/kg)[1]. Animal Model: C57BL/6J male mice (9 weeks) were i.p. injected with 20 mg/kg LPS[1] Dosage: 10 mg/kg Administration: I.p. 30 min before the LPS Result: Increased the survival rate of mice from 0% to 67%.

[References]

[1]. Piazza M, et, al. Glycolipids and benzylammonium lipids as novel antisepsis agents: synthesis and biological characterization. J Med Chem. 2009 Feb 26;52(4):1209-13.

[2]. Rodríguez MC, et, al. Aging and amyloid β oligomers enhance TLR4 expression, LPS-induced Ca 2+ responses, and neuron cell death in cultured rat hippocampal neurons. J Neuroinflammation. 2017 Jan 31;14(1):24.

Chemical & Physical Properties

[ Molecular Formula ]:
C42H78INO2

[ Molecular Weight ]:
755.979

[ Exact Mass ]:
755.507690

[ PSA ]:
18.46000

[ LogP ]:
10.36940

Related Compounds