TY-52156

TY-52156

Biochem/physiol Actions

TY-52156 is a potent sphingosine 1-phosphate (S1P) receptor 3 (S1P3; S1PR3) antagonist that selectively inhibits S1P-stimulated Ca2+ response in human S1P3-expressing cells (Ki = 110 nM) and Eu-GTP binding to S1P3-containing membranes over those of S1P1/2/4/5. TY-52156 inhibits S1P3-dependent signaling events in human coronary artery smooth muscle cells (1 µM), S1P3-dependent coronary flow decrease in perfused rat hearts, as well as S1P3-mediated acute mechanical pain in mice (10 nmol/20 µL/paw id.) and bradycardia in anesthetized rats (30 mg/kg TY-52156 p.o.) in vivo with good oral bioavailability (F = 70.9%; 1 mg/kg p.o. in rats).

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Code Description Colour Manufacturer Storage Temp. Solubility Form Assay Price Quantity
3576405 TY-52156 white to very dark brown SIGMA-ALDRICH 2-8°C DMSO: 2 mg/mL, clear
£565.50 (exc VAT) per 25MG
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3576406 TY-52156 white to very dark brown SIGMA-ALDRICH 2-8°C DMSO: 2 mg/mL, clear
£139.29 (exc VAT) per 5MG
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