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LOC14 是一种蛋白质二硫键异构酶抑制剂 (EC50=500 nM;Kd=62 nM)。它抑制 PDIA3 活性,降低肺上皮细胞中 HA 的分子内二硫键和随后的寡聚化。它在小鼠肝微粒体和血浆中表现出高稳定性,低内在微粒体清除率和低血浆蛋白结合。
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LOC14 是一种蛋白质二硫键异构酶抑制剂 (EC50=500 nM;Kd=62 nM)。它抑制 PDIA3 活性,降低肺上皮细胞中 HA 的分子内二硫键和随后的寡聚化。它在小鼠肝微粒体和血浆中表现出高稳定性,低内在微粒体清除率和低血浆蛋白结合。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 295 | 现货 | |
5 mg | ¥ 828 | 现货 | |
10 mg | ¥ 1,350 | 现货 | |
25 mg | ¥ 2,650 | 现货 | |
50 mg | ¥ 3,880 | 现货 | |
100 mg | ¥ 5,490 | 现货 |
产品描述 | LOC14 to be the most potent PDI inhibitor reported to date( EC50 : 500 nM) |
靶点活性 | PDI:500 nM(EC50) |
体外活性 | LOC14引起的PDI氧化,在细胞培养中不仅具有神经保护作用,而且在皮质纹状体脑片培养中也表现出同样效果[1]。 |
体内活性 | LOC14 在肝微粒体和血浆中显示出高稳定性,小鼠以高剂量20 mg/kg耐受良好,并能够在体内穿透血脑屏障(BBB)[1][2]。 |
动物实验 | LOC14 levels were measured in mouse plasma, striatum and cerebral cortex using Ultra Performance Liquid Chromatography-Tandem Mass Spectrometry (LC-MS/MS).?LOC14 was extracted from mouse plasma by mixing 100 μl of plasma with 900 μl of cold acetonitrile containing 25 ng/ml of cyclocreatine as an internal standard.?After mixing for 5 min. the sample was centrifuged for 10min and the organic layer was transferred to an LC-MS vial and dried under nitrogen.?The sample was reconstituted in 100 μl of 50% acetonitrile and 5 μl was injected onto the LC-MS.?Brain tissue samples were homogenized using a tissue tearor at a concentration of 150 mg/ml in cold LC-MS water followed by extraction with 1.8 ml of cold acetonitrile containing the cyclocreatine internal standard.?The brain samples were mixed and centrifuged and reconstituted the same as for the plasma samples[2]. |
分子量 | 317.41 |
分子式 | C16H19N3O2S |
CAS No. | 877963-94-5 |
Smiles | O=C(C1CC1)N1CCN(Cn2sc3ccccc3c2=O)CC1 |
密度 | 1.390 g/cm3 (Predicted) |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 25 mg/mL (78.76 mM) | ||||||||||||||||||||||||||||||
溶液配制表 | |||||||||||||||||||||||||||||||
DMSO
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