BAY-X 1005
- CAS号:128253-31-6
- 英文名:(2R)-2-cyclopentyl-2-[4-(quinolin-2-ylmethoxy)phenyl]acetic acid
- 中文名:BAY-X 1005
- CBNumber:CB41260812
- 分子式:C23H23NO3
- 分子量:361.43
- MOL File:128253-31-6.mol
- 熔点 :169-171 °C
- 沸点 :555.4±40.0 °C(Predicted)
- 密度 :1.242±0.06 g/cm3(Predicted)
- 储存条件 :2-8°C
- 溶解度 :DMSO: soluble5mg/mL (clear solution)
- 形态 :powder
- 酸度系数(pKa) :4.47±0.10(Predicted)
- 颜色 :white to beige
BAY-X 1005性质、用途与生产工艺
- 生物活性 Veliflapon (BAY X 1005; DG-031) 是一种具有口服活性的,选择性的 5-脂氧合酶激活蛋白 (FLAP) 抑制剂。Veliflapon 也是白三烯 B4 和 C4 合成的抑制剂。
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靶点
LTB 4
LTC 4
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体外研究
Veliflapon (BAY X 1005; DG-031) effectively inhibits the synthesis of LTB4 in A23187-stimulated leukocytes from rats, mice and humans (IC 50 s of 0.026, 0.039 and 0.22 μM, respectively) as well as the formation of LTC4 (IC 50 of 0.021 μM) in mouse peritoneal macrophages stimulated with opsonized zymosan.
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体内研究
Veliflapon (BAY X 1005; DG-031; diet; 18.8 mg/kg/day for 16 weeks ) inhibits atherogenesis.
Veliflapon after topical (18 μg/ear) and oral (48.7 mg/kg) administration has antiedematous effects in the arachidonic acid-induced mouse ear inflammation test.
Veliflapon is potent (11.8 and 6.7 mg/kg p.o. at 1 and 5 hours, respectively) and has a long duration of action (ED 40 of 16 hours, 70 mg/kg p.o.) in the rat whole blood ex vivo leukotriene B4 inhibition assay.
Animal Model: Female apoE/LDLR-DKO mouse model Dosage: 18.8 mg/kg Administration: Diet; per day during 16 weeks Result: Inhibited atherogenesis.
- 更新日期:2024/08/19
- 产品编号:HY-14165
- 产品名称:BAY-X 1005 Veliflapon
- CAS编号:128253-31-6
- 包装:5mg
- 价格:2500元
- 更新日期:2024/08/19
- 产品编号:HY-14165
- 产品名称:Veliflapon
- CAS编号:
- 包装:10 mM * 1 mLin DMSO
- 价格:2750元
- 公司名称:TOCRIS-US
- 联系电话:--
- 电子邮件:customerservice@tocris.co.uk
- 国家:英国
- 产品数:5729
- 优势度:77