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152802-84-1

152802-84-1, 152802-84-1, 結(jié)構(gòu)式
152802-84-1
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

152802-84-1化學(xué)性質(zhì)

沸點:
520.0±60.0 °C(Predicted)
密度:
1.28±0.1 g/cm3(Predicted)
儲存條件:
Store at -20°C
溶解度:
Soluble in DMSO
酸度系數(shù)(pKa):
3.54±0.22(Predicted)
安全信息

152802-84-1性質(zhì)、用途與生產(chǎn)工藝

生物活性

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。

靶點

EC50: 0.55 μM (K ATP channel)

體外研究

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.

體內(nèi)研究

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 生產(chǎn)廠家

全球有 8家供應(yīng)商   152802-84-1國內(nèi)生產(chǎn)廠家
供應(yīng)商聯(lián)系電話電子郵件國家產(chǎn)品數(shù)優(yōu)勢度
MedChemexpress LLC 021-58955995 sales@medchemexpress.cn 美國 4861 58
范德(北京)生物科技有限責(zé)任公司 15911056312 liming@bio-fount.com 中國 9729 58
TargetMol Chemicals Inc. +1-781-999-5354 +1-00000000000 marketing@targetmol.com 美國 32161 58
BOC Sciences info@bocsci.com 美國 0 65
天津普西唐生物醫(yī)藥科技有限公司 010-60605840 15801484223 psaitong@jm-bio.com 中國 29774 58
TargetMol中國(陶術(shù)生物) 4008200310 marketing@tsbiochem.com 中國 24644 58
TargetMol Chemicals Inc. +8613564774135 zijue.cai@tsbiochem.com 美國 19881 58
 

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
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