AM966 is a potent, selective, orally bioavailable LPA1 receptor antagonist. In vitro, AM966 inhibited LPA-stimulated intracellular calcium release (IC(50)= 17 nM) from Chinese hamster ovary cells stably expressing human LPA(1) receptors and inhibited LPA-induced chemotaxis (IC(50)= 181 nM) of human IMR-90 lung fibroblasts expressing LPA(1) receptors. AM966 (100 nM) completely blocked LPA-induced ERK1/2 activation, which selectively antagonizes LPA1 over LPA2-5, with an IC50 value of 3.8±0.4 nM. AM966 demonstrated a good pharmacokinetic profile following oral dosing in mice.
|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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.
|Solubility||DMSO: ≥ 60 mg/mL|
Antidepressants activate the lysophosphatidic acid receptor LPA(1) to induce insulin-like growth factor-I receptor transactivation, stimulation of ERK1/2 signaling and cell proliferation in CHO-K1 fibroblasts.
Olianas MC, et al. Biochem Pharmacol. 2015 Jun 15;95(4):311-23. PMID: 25888927.
A novel, orally active LPA(1) receptor antagonist inhibits lung fibrosis in the mouse bleomycin model.
Swaney JS, et al. Br J Pharmacol. 2010 Aug;160(7):1699-713. PMID: 20649573.
|Related LPL Receptor Products|
|AM095 free acid
AM095 free acid is a potent LPA1 receptor antagonist which inhibited GTPγS binding to CHO cell membranes overexpressing recombinant human or mouse LPA1 with IC50 values of 0.98 and 0.73 μM, respectively.
BMS-986020 (also known as AM152) is a potent and selective LPA1 antagonist.
AM095 is a potent and selective, orally bioavailable antagonist of lysophosphatidic acid receptor1 (LPA1).
Ki16425 is a LPA receptor antagonist with Ki values of 0.34, 6.5 and 0.93 μM for the human LPA1, LPA2 and LPA3 receptors, respectively.
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