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| 25mg |
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AM-966 (AM966) is a novel, oral and potent LPA(1) receptor antagonist. In vitro, AM966 inhibited LPA-stimulated intracellular calcium release from Chinese hamster ovary cells stably expressing human LPA(1) receptors (IC50=17 nM). In vivo, AM966 inhibits lung fibrosis in the mouse bleomycin model.
| ln Vitro |
AM966 is an LPA1 receptor antagonist that is accessible, strong, and selective. Human A2058 melanoma cells (IC50=138±43 nM), human lung fibroblasts IMR-90 (IC50=182±86 nM), and CHO mLPA1 cells (IC50=469±54 nM) are all inhibited by AM966 against LPA1-mediated inhibition[1]. The high-frequency anti-coupling LPA1 but not LPA2-5, AM966 (100 nM), effectively prevented LPA-induced ERK1/2 activation (IC50 = 3.8±0.4 nM). ERK1/2 phosphorylation produced by mianserin is totally blocked by AM966 (100 nM) [2].
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| ln Vivo |
In a three-day bleomycin model, AM966 (30 mg/kg, BID) decreases lung damage and inflammation, vascular leakage, and inflammation. 14 days following bleomycin lung injury, AM966 prevents pulmonary fibrosis in a paradigm that lowers lung conditioning and modifies body weight. AM966 decreased tissue damage, vascular leakage, and profibrotic cytokine production in a 14-day bleomycin trial. When compared to pirfenidone, AM966 was more effective in the 14-day bleomycin model. Following bleomycin damage, AM966 can lessen fibrosis and late-stage proliferation [1].
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| References |
[1]. Swaney, JS, et al. A novel, orally active LPA1 receptor antagonist inhibits lung fibrosis in the mouse bleomycin model. Br J Pharmacol. 2010 Aug;160(7):1699-713.
[2]. Olianas MC, et al. 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. Biochem Pharmacol. 2015 Jun 15;95(4):311-23 |
| Molecular Formula |
C20H19FINO
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|---|---|
| Molecular Weight |
435.27
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| Exact Mass |
435.04954
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| CAS # |
1228690-19-4
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| SMILES |
ClC1=C([H])C([H])=C([H])C([H])=C1[C@@]([H])(C([H])([H])[H])OC(N([H])C1C(C([H])([H])[H])=NOC=1C1C([H])=C([H])C(=C([H])C=1[H])C1C([H])=C([H])C(C([H])([H])C(=O)O[H])=C([H])C=1[H])=O
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| Synonyms |
AM-966 AM966 AM 966
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~203.70 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (5.09 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.09 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. View More
Solubility in Formulation 3: 10 mg/mL (20.37 mM) in 50% PEG300 50% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2974 mL | 11.4871 mL | 22.9742 mL | |
| 5 mM | 0.4595 mL | 2.2974 mL | 4.5948 mL | |
| 10 mM | 0.2297 mL | 1.1487 mL | 2.2974 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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