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别名 4'-[4-[[[(1R)-1-(2-氯苯基)乙氧基]羰基]氨基]-3-甲基-5-异恶唑基]-联苯-4-乙酸
AM966 是一种具有优异亲和力的特异性口服 LPA1 拮抗剂,可抑制 LPA 刺激的细胞内钙释放,IC50为 17 nM。


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AM966 是一种具有优异亲和力的特异性口服 LPA1 拮抗剂,可抑制 LPA 刺激的细胞内钙释放,IC50为 17 nM。
| 规格 | 价格 | 库存 | 数量 |
|---|---|---|---|
| 1 mg | ¥ 283 | 现货 | |
| 5 mg | ¥ 696 | 现货 | |
| 10 mg | ¥ 1,060 | 现货 | |
| 25 mg | ¥ 1,350 | 现货 | |
| 50 mg | ¥ 1,690 | 现货 | |
| 100 mg | ¥ 2,690 | 现货 | |
| 200 mg | ¥ 3,780 | 现货 | |
| 1 mL x 10 mM (in DMSO) | ¥ 750 | 现货 |
AM966 相关产品
| 产品描述 | AM966, a excellent affinity, specific, oral LPA1(IC50=17 nM) antagonist, suppresses LPA-stimulated intracellular calcium release. |
| 靶点活性 | LPA1:IC50=17 nM |
| 体外活性 | 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). |
| 体内活性 | In a 3-day bleomycin model, AM966 (30 mg/kg, BID) reduces vascular leakage, inflammation and lung injury and inflammation. |
| 细胞实验 | 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. |
| 动物实验 | In fasted mice, received AM966 (10 mg/kg), which is prepared in water, by oral gavage. |
| 别名 | 4'-[4-[[[(1R)-1-(2-氯苯基)乙氧基]羰基]氨基]-3-甲基-5-异恶唑基]-联苯-4-乙酸 |
| 分子量 | 490.93 |
| 分子式 | C27H23ClN2O5 |
| CAS No. | 1228690-19-4 |
| Smiles | C[C@@H](OC(=O)Nc1c(C)noc1-c1ccc(cc1)-c1ccc(CC(O)=O)cc1)c1ccccc1Cl |
| 密度 | 1.330 g/cm3 at 20℃ |
| 颜色 | White |
| 物理性状 | Solid |
| 存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||||||||||||
| 溶解度信息 | DMSO: 45 mg/mL (91.66 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||
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