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TY 52156 is an orally bioavailable s1P3 receptor antagonist (Ki = 110 nM); inhibits S1P-induced Ca2+ release in HUVEC cells. TY 52156 suppresses FTY-720-induced S1P3 receptor-mediated bradycardia in vivo. TY 52156 also inhibits S1P-induced breast cancer stem cell expansion in vitro.
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Molecular Weight | 364.27 |
| Formula | C18H19Cl2N3O |
| CAS Number | 934369-14-9 |
| Purity | >98% |
| Solubility | DMSO 36.43 mg/mL |
| Storage | at -20°C |
Biochemical and antiproliferative properties of 4-[ar(alk)ylmino]pyridopyrimidines, a new chemical class of potent and specific epidermal growth factor receptor tyrosine kinase inhibitor.
Fry, et al. Biochem Pharmacol. 1997;54: 877. PMID: 9354588.
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