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AM966

Cat. No. M8992
AM966 Structure
Size Price Availability Quantity
5mg USD 200 In stock
10mg USD 360 In stock
25mg USD 660 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 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.

Chemical Information
Molecular Weight 490.93
Formula C27H23ClN2O5
CAS Number 1228690-19-4
Purity >98%
Solubility DMSO: ≥ 60 mg/mL
Storage at -20°C
References

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.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: AM966 supplier, LPL Receptor, inhibitors

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