CAY10444 , also known as BML-241, is an S1P3 antagonist. CAY10444 inhibits the S1P-induced increase in Ca2+ by 37% in HeLa cells expressing the S1P3 receptor[1].BML-241 inhibited the increase in intracellular Ca2+ concentration induced by stimulation via P2 receptors or α1A adrenergic receptors and α1A adrenergic receptor-mediated constriction of rat mesenteric arteries without affecting the S1P3-mediated decrease in forskolin-induced cAMP accumulation[1].
CAY10444 细胞实验
Cell Line
Concentration
Treated Time
Description
References
bovine aortic endothelial cells (BAEC)
10 µM
To evaluate the effect of CAY10444 on HDL-induced endothelial cell migration and Akt/eNOS phosphorylation, results showed that CAY10444 did not inhibit these responses.
CAY10444 downregulated VEGF-A and VE-cadherin mRNA expression
Lab Invest. 2021 Feb;101(2):245-257
TKE2 corneal epithelial cells
100 μM
24 h
CAY10444 blocked S1P-induced increases in VEGF-A mRNA expression levels
Lab Invest. 2021 Feb;101(2):245-257
human astrocytes (HAs) and hCMEC/D3 cells
1 µM
24 h
To evaluate the effect of S1PR3 on the blood-brain barrier. Results showed that S1P stimulation increased CCL2, p-p38 MAPK, and ICAM-1 expression and decreased ZO-1 expression, while CAY10444 treatment reversed this phenomenon.
CNS Neurosci Ther. 2021 Jun;27(6):674-686
human monocyte derived macrophages (hMDM)
10μM
42 h
To study the effect of S1PR3 inhibition on ERK1/2 phosphorylation and parasite load. Results showed that CAY10444 pretreatment led to increased ERK1/2 phosphorylation and increased parasite load.
PLoS Negl Trop Dis. 2018 Aug 17;12(8):e0006647
THP-1 derived macrophages (TDM)
10μM
42 h
To study the effect of S1PR3 inhibition on ERK1/2 phosphorylation and parasite load. Results showed that CAY10444 pretreatment led to increased ERK1/2 phosphorylation and increased parasite load.
PLoS Negl Trop Dis. 2018 Aug 17;12(8):e0006647
rat sensory neurons
10 μM
30 min
CAY10444, as a selective antagonist for S1PR3, in combination with W146 (S1PR1 antagonist), blocked the S1P-induced enhancement of neuronal excitability.
J Neuroinflammation. 2015 Apr 12;12:70
HAPI cells
10 μM
2 h
Inhibits S1P binding to S1PR3, reduces p38 MAPK phosphorylation and NF-κB p65 activation
J Neuroinflammation. 2021 Feb 18;18(1):50.
CAY10444 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Adult male Sprague Dawley rats
Collagenase-induced intracerebral hemorrhage model
Intraperitoneal injection
0.5 mg/kg
Once daily for 1 or 3 days
To evaluate the effect of CAY10444 on brain edema, BBB integrity, and behavioral deficits after ICH. Results showed that CAY10444 significantly reduced brain edema volume, ameliorated BBB integrity, and improved behavioral deficits.
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