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 |
Related S1P Receptor Products |
---|
Etrasimod (APD334)
Etrasimod (APD334) is a specific and orally available antagonist of the sphingosine-1-phosphate-1 (S1P1) receptor, with IC50 of 1.88 nM in CHO cells. |
PF-543 Citrate
PF-543 Citrate is a potent, selective, reversible and sphingosine-competitive SPHK1 inhibitor with an IC50 of 2 nM and a Ki of 3.6 nM. |
Opaganib (ABC294640)
Opaganib (ABC294640) is a selective and competitive SK2 inhibitor with a Ki of 9.8 μM. |
NIBR-0213
NIBR-0213 is an orally active, potent and S1P1-selective sphingosine 1-phosphate (S1P) receptor antagonist. |
A-971432
A-971432 is an orally bioavailable, non-clastogenic, azetidinecarboxylate compound that acts as a highly potent and selective sphingosine-1-phosphate receptor 5 agonist (IC50 = 6 nM/S1P5, 362 nM/S1P1 and >10 μM/S1P3 in a radio-ligand binding assay). |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2020 AbMole BioScience. All Rights Reserved.