| Bioactivity | 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]. |
| Invitro | 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: |
| Name | CAY10614 |
| CAS | 1202208-36-3 |
| Formula | C42H78INO2 |
| Molar Mass | 755.98 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| Reference | [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. |