| Bioactivity | TY-52156 is a potent and selective S1P3 receptor antagonist with a Ki value of 110 nM[1]. | ||||||||||||
| Target | Ki: 110 nM (S1P3) | ||||||||||||
| Invitro | TY-52156 inhibits the S1P3 receptor-dependent increase in [Ca2+]i[1].TY-52156 shows submicromolar potency and a high degree of selectivity for S1P3 receptor[1].TY-52156 (10 μM; 10 min) inhibits S1P-induced p44/p42 MAPK phosphorylation[1]. Western Blot Analysis[1] Cell Line: | ||||||||||||
| In Vivo | TY-52156 (10 mg/kg, 30 mg/kg; p.o.) suppresses S1P3 receptor-induced bradycardia after oral administration in vivo[1]. Animal Model: | ||||||||||||
| Name | TY-52156 | ||||||||||||
| CAS | 934369-14-9 | ||||||||||||
| Formula | C18H19Cl2N3O | ||||||||||||
| Molar Mass | 364.27 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Murakami A, et al. Sphingosine 1-phosphate (S1P) regulates vascular contraction via S1P3 receptor: investigation based on a new S1P3 receptor antagonist. Mol Pharmacol. 2010 Apr;77(4):704-13. |