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Losartan (DuP-753) 是一种血管紧张素II 受体拮抗剂,能够与血管紧张素II 竞争性结合AT1受体(IC50:20 nM)。
Losartan (DuP-753) 是一种血管紧张素II 受体拮抗剂,能够与血管紧张素II 竞争性结合AT1受体(IC50:20 nM)。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
500 mg | ¥ 333 | 现货 | |
1 g | ¥ 418 | 现货 | |
5 g | ¥ 970 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 418 | 现货 |
产品描述 | Losartan (DuP-753) is an angiotensin II receptor antagonist. |
靶点活性 | AT1 receptor:20 nM |
体外活性 | Losartan 与血管紧张素II竞争性地结合AT1受体。其抑制血管紧张素II结合50%所需浓度(IC50)为20 nM[1]。Losartan (40μM)影响ISC,但可阻止ANGII对ISC的作用[2]。Losartan 显著降低血管紧张素II介导的子宫内膜癌细胞增殖。Losartan 与抗miR-155联合使用,相比单药治疗具有更显著的抑制增殖效果[3]。 |
体内活性 | 与安慰剂处理的 Fbn1C1039 g/+ 小鼠相比,Losartan (0.6 g/L,p.o.)处理的 Fbn1C1039 g/+ 小鼠显示出远端气室口径的缩小。Losartan 和普萘洛尔的剂量经过滴定,可产生血液动力学效应。对 pSmad2 核染色的分析表明,Losartan 能拮抗 Fbn1C1039 g/+ 小鼠主动脉壁的 TGF-β 信号传导。Losartan 能改善肺部的疾病表现,但这与血液动力学的改善并无必然联系[4]。Losartan (10 mg/kg,动脉内注射)可使血液中的血管紧张素水平增加 4 到 6 倍。Losartan (10 mg/kg,静脉注射)可使血浆肾素水平增加 100 倍,血浆血管紧张素原水平降至对照组的 24%,血浆醛固酮水平保持不变[5]。 |
细胞实验 | An MTT assay is used to measure cell proliferation and viability. For the assay, 5000 cells in 200?μL media per well are seeded in a 96 well plate. After overnight incubation to allow for cell attachment, the medium is removed by suction. MTT at 1?mg/mL concentration in serum-free medium is added and then incubated for 4?h at 37°C. After removal of MTT solution, 100?μL of DMSO is added to dissolve formazan crystals. Absorbance at 570?nm and at 600?nm as a reference is then measured using a microplate reader. The difference in absorbance is thus relative to the extent of cell survival. |
别名 | 洛沙坦, 氯沙坦, DuP-753 |
分子量 | 422.91 |
分子式 | C22H23ClN6O |
CAS No. | 114798-26-4 |
Smiles | CCCCC1=NC(Cl)=C(CO)N1CC1=CC=C(C=C1)C1=CC=CC=C1C1=NNN=N1 |
密度 | 1.35 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: 45 mg/mL (106.41 mM) | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
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