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) without affect the activity of 129 protein kinases (IC50 >10 μM). A-971432 is shown to enhance blood-brain barrier integrity and reverse lipid accumulation and age-related cognitive decline in mice in vivo with good pharmacokinetics (t1/2 = 5.7 h; Cmax = 2,500 ng/ml; AUC = 35,000 ng.h/ml at 10 mg/kg, p.o. in CD1 mice). Likewise, oral gavage showed good plasma exposure and no sign of lymphopenia in rats (10, 30, and 100 mg/kg.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|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.
|Solubility||DMSO: 3 mg/mL (warmed)|
|Related S1P Receptor Products|
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 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) is a selective and competitive SK2 inhibitor with a Ki of 9.8 μM.
NIBR-0213 is an orally active, potent and S1P1-selective sphingosine 1-phosphate (S1P) receptor antagonist.
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