NEBENTAN 钾盐
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- CAS号:
- 342005-82-7
- 英文名:
- Nebentan potassium
- 英文别名:
- YM598;Nebentan potassium
- 中文名:
- NEBENTAN 钾盐
- 中文别名:
- NEBENTAN 钾盐
- CBNumber:
- CB88205872
- 分子式:
- C24H22KN5O5S
- 分子量:
- 531.63
- MOL File:
- 342005-82-7.mol
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NEBENTAN 钾盐化学性质
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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: 125 mg/mL (236.02 mM)
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形态:
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Solid
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颜色:
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Off-white to light yellow
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NEBENTAN 钾盐性质、用途与生产工艺
Nebentan potassium (YM598) 是一种有效的具有口服活性的非肽类内皮素受体 (ETA receptor) 拮抗剂,通过 Bosentan (HY-A0013) 修饰得到。Nebentan potassium 抑制 [125I] 内皮素-1 与人内皮素 ETA 和 ETB 受体结合,Ki 分别为 0.697 nM 和 569 nM。Nebentan potassium 可用于改善肺心病和心肌梗死的相关研究。
ET
A
0.679 nM (Ki)
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ET
B
569 nM (Ki)
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Nebentan potassium inhibits the specific binding of [
125
I] endothelin-1 to endothelin ET
A
and ET
B
receptors in a concentration dependent manner, K
i
values are 0.697 nM and 1.53 nM for human and rat endothelin ETA receptors, respectively. In contrast, YM598 exhibits low affinities for human and rat endothelin ET
B
receptors, with K
i
values of 569 nM and 155 nM,respectively.In measurement of intracellular Ca
2+
concentration, Nebentan potassium concentration-dependently inhibits the increase in [Ca
2+
]i induced by 10 nM endothelin-1 in both CHO cells and A10 cells, the IC
50
values are 26.2 nM for CHO cells and 26.7 nM for A10 cells, respectively.
Nebentan potassium (oral administration; 0.1-1 mg/kg; 4 weeks) significantly inhibits the progression of pulmonary hypertension and the development of right ventricular hypertrophy.Nebentan potassium (oral administration; 1 mg/kg; 30 weeks) significantly ameliorates the poor survival rate of CHF rats, it markedly reduces the hypertrophy of both ventricles as well as pulmonary congestion.
NEBENTAN 钾盐
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更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
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2024/08/19 | HY-106994A | Nebentan potassium | | 1 mg | 1045元 |
2024/08/19 | HY-106994A | Nebentan potassium | 342005-82-7 | 5mg | 2300元 |
342005-82-7, NEBENTAN 钾盐 相关搜索:
- 抑制剂
- NEBENTAN 钾盐
- 342005-82-7
- YM598
- Nebentan potassium