Powder: -20°C for 3 years | In solvent: -80°C for 1 year
AM966, a excellent affinity, specific, oral LPA1(IC50=17 nM) antagonist, suppresses LPA-stimulated intracellular calcium release.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
2 mg | In stock | $ 34.00 | |
5 mg | In stock | $ 55.00 | |
10 mg | In stock | $ 89.00 | |
25 mg | In stock | $ 163.00 | |
50 mg | In stock | $ 278.00 | |
100 mg | In stock | $ 447.00 | |
500 mg | In stock | $ 998.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 60.00 |
Description | AM966, a excellent affinity, specific, oral LPA1(IC50=17 nM) antagonist, suppresses LPA-stimulated intracellular calcium release. |
Targets&IC50 | LPA1:IC50=17 nM |
In vitro | Pre-treatment with AM966 (100 nM) completely blocks ERK1/2 phosphorylation induced by either amitriptyline or mianserin. LPA-induced ERK1/2 activation is completely blocked by AM966 (100 nM), which selectively antagonizes LPA1 over LPA2-5, with an IC50 value of 3.8±0.4 nM. AM966 inhibits LPA1-mediated chemotaxis of human A2058 melanoma cells (IC50=138±43 nM), IMR-90 human lung fibroblasts (IC50=182±86 nM) and CHO mLPA1 cells (IC50=469±54 nM). |
In vivo | In a 3-day bleomycin model, AM966 (30 mg/kg, BID) reduces vascular leakage, inflammation and lung injury and inflammation. |
Cell Research | AM966 (Chem Scene, Monmouth Junction, NJ, USA) is dissolved in DMSO and stored, and then diluted with appropriate media (DMSO 0.5%) before use.CHO-K1 cells are grown to 80% confluency in 12-well plates, serum-starved for 24 h and incubated in serum-free medium with AM966. After 21 h, [3H]thymidine (0.5 μCi/well) is added and the incubation is continued for 3 h. The medium is then removed, and the cells are placed on ice and washed twice with 1 mL of ice-cold PBS containing 5% trichloroacetic acid. Cells are solubilized and [3H]thymidine incorporation is determined by liquid scintillation counting. Assays are performed in triplicate. |
Animal Research | In fasted mice, received AM966 (10 mg/kg), which is prepared in water, by oral gavage. |
Molecular Weight | 490.93 |
Formula | C27H23ClN2O5 |
CAS No. | 1228690-19-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 105 mg/mL
You can also refer to dose conversion for different animals. More
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AM966 1228690-19-4 GPCR/G Protein LPL Receptor LPA Receptor Lysophospholipid Receptor inhibit AM-966 Inhibitor AM 966 inhibitor