152802-84-1
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- CAS號:
- 152802-84-1
- 英文名:
- KRN4884
- 英文別名:
- KRN4884;KRN4884,KRN-4884;3-Pyridinecarboximidamide, 5-amino-N-[2-(2-chlorophenyl)ethyl]-N'-cyano-
- 中文名:
- 152802-84-1
- 中文別名:
- 化合物 T15667;化合物 KRN4884
- CBNumber:
- CB13339667
- 分子式:
- C15H14ClN5
- 分子量:
- 299.76
- MOL File:
- 152802-84-1.mol
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152802-84-1化學(xué)性質(zhì)
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沸點:
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520.0±60.0 °C(Predicted)
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密度:
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1.28±0.1 g/cm3(Predicted)
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儲存條件:
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Store at -20°C
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溶解度:
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Soluble in DMSO
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酸度系數(shù)(pKa):
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3.54±0.22(Predicted)
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152802-84-1性質(zhì)、用途與生產(chǎn)工藝
KRN4884 是一種 K+ sup> 通道開放劑。在細(xì)胞內(nèi) ATP (1 mM) 存在下,KRN4884 (0.1-3 μM) 激活 KATP通道 (EC50=0.55 μM), 這種作用存在濃度依賴性。
EC50: 0.55 μM (K
ATP
channel)
KRN4884 (0.3 μM) shifts the concentration-response relationship for ATP-induced K
ATP
channel inhibition to the right and slightly upward direction without altering the slope. After either the spontaneous or Ca
2+
-induced channel rundown, KRN4884 (1 and 3 μM) partially restores the K
ATP
channel activity. Furthermore, the effect of KRN4884 is augmented by the presence of uridine 5′-diphosphate (3 mM). KRN4884 activates cardiac K
ATP
channels through not only decreasing the sensitivity of the channel to ATP but also directly stimulating the opening of the channel. KRN4884 (0.3 and 3 μM) increases the outward current in a concentration-dependent manner, and the unitary current amplitudes are similar to that of K
ATP
channels in the ATP-free solution.
The effects of KRN4884, a novel pyridinecarboxamidine type K
ATP
channel opener, on serum triglyceride levels are investigated in Sprague-Dawley rats. Oral administration of KRN4884 (3 mg/kg) for 10 days causes a significant reduction in serum triglyceride levels, which is comparable to that of Clofibrate (160 mg/kg). Reduction in serum triglyceride levels by KRN4884 and Clofibrate are accompanied by a reduction in triglyceride levels both in chylomicron and in very low density lipoprotein. KRN4884 treatment does not affect serum concentrations of total cholesterol and phospholipid, but increases free fatty acid levels. Rats receiving KRN4884 exhibite an increase in lipoprotein lipase (LPL) activity both in adipose tissue and in skeletal muscle.
152802-84-1
上下游產(chǎn)品信息
上游原料
下游產(chǎn)品
152802-84-1, 152802-84-1 相關(guān)搜索:
- 抑制劑
- 化合物 KRN4884
- 化合物 T15667
- 152802-84-1
- KRN4884,KRN-4884
- 3-Pyridinecarboximidamide, 5-amino-N-[2-(2-chlorophenyl)ethyl]-N'-cyano-
- KRN4884