达布扎琼
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- CAS号:
- 219311-44-1
- 英文名:
- Dabuzalgron
- 英文别名:
- Ro 115-1240;Dabuzalgron;N-[6-chloro-3-(4,5-dihydro-1H-imidazol-2-ylmethoxy)-2-methyl-phenyl]me thanesulfonamide;MethanesulfonaMide, N-[6-chloro-3-[(4,5-dihydro-1H-iMidazol-2-yl)Methoxy]-2-Methylphenyl]-;membrane,potential,inhibit,Adrenergic Receptor,mitochondrial,urinary,Inhibitor,Beta Receptor,incontinence,Cell,Dabuzalgron,death,Apoptosis
- 中文名:
- 达布扎琼
- 中文别名:
- 达布扎琼;N-[6-氯-3-[(4,5-二氢-1H-咪唑-2-基)甲氧基]-2-甲基苯基]甲磺酰胺
- CBNumber:
- CB31261458
- 分子式:
- C12H16ClN3O3S
- 分子量:
- 317.79
- MOL File:
- 219311-44-1.mol
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达布扎琼化学性质
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密度:
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1.46
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储存条件:
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Store at -20°C
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溶解度:
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DMSO: 26 mg/mL (81.82 mM)
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形态:
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Solid
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颜色:
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White to off-white
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达布扎琼性质、用途与生产工艺
Dabuzalgron (Ro 115-1240) 是一种口服活性的，选择性的 α-1A 肾上腺素能受体激动剂，动物模型中，用于缓解尿失禁。Dabuzalgron 可通过维持线粒体功能来预防由阿霉素引起的心脏毒性。
Dabuzalgron treatment increases ERK phosphorylation in a dose-dependent fashion with an
EC
50
of 4.8 μM. ERK1/2 activation contributes to the cardioprotective effects of Dabuzalgron.
Dabuzalgron (10 μM; 4 hours) protects NRVMs from cell death due to Doxorubicin (DOX).
Activation of the α1A-AR with Dabuzalgron (10 μM; 4 hours) mitigates the detrimental effects of DOX on mitochondrial membrane potential and abrogates the activation of important elements of the apoptotic response to mitochondrial damage.
Western Blot Analysis
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Cell Line:
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Neonatal rat ventricular myocytes (NRVMs)
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Concentration:
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0.1 μM, 1 μM, 10 μM and 100 μM
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Incubation Time:
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15 minutes
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Result:
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Increased ERK phosphorylation in a dose-dependent fashion with an
EC
50
of 4.8 μM.
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Dabuzalgron (10 μg/kg; oral gavage; twice daily; for 7 days; C57Bl6J wild-type or α1A-AR knockout mice) treatment protects against DOX cardiotoxicity by activating the α1A-AR. Dabuzalgron protects against the reduction in transcripts related to mitochondrial function, up-regulates PGC1α, preserves ATP content, and reduces oxidative stress in the hearts of mice treated with DOX.
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Animal Model:
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Male C57Bl6J wild-type (WT) or α1A-AR knockout (AKO) mice (8-12-week-old) injected with Doxorubicin (DOX)
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Dosage:
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10 μg/kg
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Administration:
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Oral gavage; twice daily; for 7 days
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Result:
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Preserved contractile function and reduced fibrosis after DOX administration. AKO mice treated with DOX had worse survival and more profoundly impaired contractile function than WT mice. Protected against the reduction in transcripts related to mitochondrial function, preserved ATP content, and reduced oxidative stress in the hearts of mice treated with DOX.
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达布扎琼
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/08/19 | HY-117071 | Dabuzalgron | | 1 mg | 352元 |
| 2024/08/19 | HY-117071 | 达布扎琼
Dabuzalgron | 219311-44-1 | 5mg | 880元 |
219311-44-1, 达布扎琼 相关搜索:
- 达布扎琼
- N-[6-氯-3-[(4,5-二氢-1H-咪唑-2-基)甲氧基]-2-甲基苯基]甲磺酰胺
- 219311-44-1
- membrane,potential,inhibit,Adrenergic Receptor,mitochondrial,urinary,Inhibitor,Beta Receptor,incontinence,Cell,Dabuzalgron,death,Apoptosis
- Ro 115-1240
- Dabuzalgron
- N-[6-chloro-3-(4,5-dihydro-1H-imidazol-2-ylmethoxy)-2-methyl-phenyl]me thanesulfonamide
- MethanesulfonaMide, N-[6-chloro-3-[(4,5-dihydro-1H-iMidazol-2-yl)Methoxy]-2-Methylphenyl]-