| Name | AM966 |
| Description | AM966, a excellent affinity, specific, oral LPA1(IC50=17 nM) antagonist, suppresses LPA-stimulated intracellular calcium release. |
| 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. |
| 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. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 45 mg/mL (91.66 mM), Sonication is recommended.
10% DMSO+90% Corn Oil : 2 mg/mL (4.07 mM), Sonication is recommended.
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| Keywords | Lysophospholipid Receptor | LPLReceptor | LPL Receptor | LPL | LPAReceptor | LPA1 | LPA Receptor | Inhibitor | inhibit | AM-966 | AM966 | AM 966 |
| Inhibitors Related | Fingolimod hydrochloride | LX-2931 | Tyloxapol | Sphingosine-1-phosphate | CYM50374 | ASP-4058 | CAY10444 | Ki16198 | Siponimod | CYM5181 | Poloxamer 407 | S1PR1 modulator 1 |
| Related Compound Libraries | Highly Selective Inhibitor Library | Target-Focused Phenotypic Screening Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Inhibitor Library | NO PAINS Compound Library | Orally Active Compound Library | Immunology/Inflammation Compound Library | Bioactive Compounds Library Max | Preclinical Compound Library | GPCR Compound Library | Anti-Cancer Active Compound Library |
United States
