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Chemical Structure| 298186-80-8 Chemical Structure| 298186-80-8

Structure of CAY10444
CAS No.: 298186-80-8

Chemical Structure| 298186-80-8

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CAY10444 (BML-241) is a selective sphingosine-1-phosphate 3 (S1P3) antagonist. It reduces calcium influx induced by S1P by inhibiting S1P3 receptor-mediated signaling. CAY10444 has potential in studying cardiovascular and immune-related diseases.

Synonyms: BML-241

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Product Details of CAY10444

CAS No. :298186-80-8
Formula : C15H29NO2S
M.W : 287.46
SMILES Code : O=C(C1NC(CCCCCCCCCCC)SC1)O
Synonyms :
BML-241
MDL No. :MFCD08062140

Safety of CAY10444

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319
Precautionary Statements:P501-P270-P264-P280-P302+P352-P337+P313-P305+P351+P338-P362+P364-P332+P313-P301+P312+P330

Related Pathways of CAY10444

GPCR

Isoform Comparison

Biological Activity

In Vitro:

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. Arterioscler Thromb Vasc Biol. 2013 Aug;33(8):1788-94
human retinal microvascular endothelial cells (HRMECs) 1-100 μM 10 h CAY10444 suppressed S1P-induced tube-like vessel formation Lab Invest. 2021 Feb;101(2):245-257
human umbilical vein endothelial cells (HUVECs) 10 μM 24 h 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.

In Vivo:

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. CNS Neurosci Ther. 2021 Jun;27(6):674-686

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.48mL

0.70mL

0.35mL

17.39mL

3.48mL

1.74mL

34.79mL

6.96mL

3.48mL

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