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Ibrolipim (NO-1886) 是口服具有活力的脂蛋白脂肪酶 (LPL) 激活剂。它能够降低血浆甘油三酸酯,增加高密度脂蛋白胆固醇水平,具有肾保护和降血脂的作用。
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Ibrolipim (NO-1886) 是口服具有活力的脂蛋白脂肪酶 (LPL) 激活剂。它能够降低血浆甘油三酸酯,增加高密度脂蛋白胆固醇水平,具有肾保护和降血脂的作用。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 153 | 现货 | |
5 mg | ¥ 328 | 现货 | |
10 mg | ¥ 538 | 现货 | |
25 mg | ¥ 955 | 现货 | |
50 mg | ¥ 1,450 | 现货 | |
100 mg | ¥ 2,180 | 现货 | |
200 mg | ¥ 3,280 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 363 | 现货 |
产品描述 | Ibrolipim (NO-1886) attenuates high glucose-induced endothelial dysfunction in cultured human umbilical vein endothelial cells via PI3K/Akt pathway. |
体外活性 | Ibrolipim在5和50 μmol/L的浓度下显著增加了从THP-1巨噬细胞衍生的泡沫细胞到apoA-I或HDL的胆固醇外输。此外,它还上调了ABCA1和ABCG1的表达。此外,LXRα也通过Ibrolipim处理而上调。另外,LXRα小干扰RNA完全抑制了由Ibrolipim引起的促进效果[1]。 |
体内活性 | Ibrolipim(NO-1886;100 mg/kg;口服;每天一次;连续8周;雌性Sprague-Dawley大鼠)的治疗能减少内脏脂肪堆积并抑制卵巢切除导致的体重增加。Ibrolipim降低了呼吸商并增加了肝脏、梭羽肌肉和系膜脂肪中脂肪酸转运蛋白mRNA的表达。同时,Ibrolipim还提高了肝脏和梭羽肌肉中脂肪酸结合蛋白mRNA的表达,以及心脏、梭羽肌肉和系膜脂肪中解偶联蛋白3(UCP3)mRNA的表达,但在棕色脂肪组织中没有显著效果[2]。 |
细胞实验 | Human THP-1 cells pre-incubated with ox-LDL served as foam cell models. Specific mRNA was quantified using real-time RT-PCR and protein expression using Western blotting. Cellular cholesterol handling was studied using cholesterol efflux experiments and high performance liquid chromatography assays[1] |
动物实验 | Animal Model: Female Sprague-Dawley rats (10-week-old; 200-260 g) with experimental ovariectomy treatment. Dosage: 100 mg/kg ? ? ??. Administration: Oral administration; daily; for 8 weeks[2] |
别名 | NO-1886 |
分子量 | 451.25 |
分子式 | C19H20BrN2O4P |
CAS No. | 133208-93-2 |
Smiles | CCOP(=O)(Cc1ccc(cc1)C(=O)Nc1ccc(Br)cc1C#N)OCC |
密度 | 1.44 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: 125 mg/mL (277.01 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
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