抑制剂
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- CAS号:
- 1621673-53-7
- 英文名:
- KY-226
- 英文别名:
- KY-226;4-[[([1,1'-Biphenyl]-4-ylmethyl)thio]methyl]-N-(hexylsulfonyl)benzamide;Benzamide, 4-[[([1,1'-biphenyl]-4-ylmethyl)thio]methyl]-N-(hexylsulfonyl)-;inhibit,anti-diabetic,leptin,ZO-1,LPS,insulin,phosphorylated,KY-226,Akt,KY226,anti-obesity,PTP1B,Phosphatase,neurons,Inhibitor,KY 226
- 中文名:
- 抑制剂
- 中文别名:
- 化合物KY-226
- CBNumber:
- CB14668126
- 分子式:
- C27H31NO3S2
- 分子量:
- 481.67
- MOL File:
- 1621673-53-7.mol
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抑制剂化学性质
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密度:
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1.186±0.06 g/cm3(Predicted)
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储存条件:
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-20°
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溶解度:
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Soluble in DMSO (>25 mg/ml).
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形态:
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solid
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酸度系数(pKa):
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3.91±0.40(Predicted)
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颜色:
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Off-white
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稳定性:
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Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 3 months.
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抑制剂性质、用途与生产工艺
KY-226 是一种有效的、口服活性的 protein tyrosine phosphatase 1B (PTP1B) 的选择性变构抑制剂，对人PTP1B的IC50值为0.28 μM。KY-226 通过增强 insulin 和 leptin 信号传导来发挥抗糖尿病和抗肥胖的作用。
| Target | Value |
PTP1B
(Cell-free assay)
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0.28 μM
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In human hepatoma-derived cells (HepG2), KY-226 (0.3-10 μM) increases the phosphorylated insulin receptor (pIR) produced by insulin.
KY-226 (1 μM; 24 hours; bEnd.3 cells) treatment rescues lipopolysaccharide-induced reduction of mRNA and protein levels of ZO-1. KY-226 treatment restores phosphorylation of pAkt (T308) and its downstream target forkhead box protein O1 (FoxO1) (S256) in bEnd.3 cells.
Western Blot Analysis
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Cell Line:
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bEnd.3 cells stimulated with LPS
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Concentration:
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1 μM
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Incubation Time:
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24 hours
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Result:
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Rescued lipopolysaccharide-induced reduction of mRNA and protein levels of ZO-1.
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KY-226 (10-30 mg/kg/day; oral administration; daily; for 4 weeks; male
db/db
mice) treatment significantly reduces plasma glucose and triglyceride levels as well as hemoglobin A1c values without increasing body weight gain.
KY-226 attenuates plasma glucose elevations in the oral glucose tolerance test. KY-226 also increases pIR and phosphorylated Akt in the liver and femoral muscle.
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Animal Model:
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Male
db/db
mice (8-11 weeks old)
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Dosage:
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10 mg/kg and 30 mg/kg
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Administration:
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Oral administration; daily; for 4 weeks
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Result:
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Significantly reduced plasma glucose and triglyceride levels as well as hemoglobin A1c values without increasing body weight gain.
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抑制剂
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 |
|---|
| 2024/04/30 | HY-120327 | KY-226 | | 1 mg | 920元 |
| 2024/04/30 | HY-120327 | 抑制剂
KY-226 | 1621673-53-7 | 5mg | 2300元 |
1621673-53-7, 抑制剂 相关搜索:
- 药靶配体
- 化合物KY-226
- 1621673-53-7
- inhibit,anti-diabetic,leptin,ZO-1,LPS,insulin,phosphorylated,KY-226,Akt,KY226,anti-obesity,PTP1B,Phosphatase,neurons,Inhibitor,KY 226
- 4-[[([1,1'-Biphenyl]-4-ylmethyl)thio]methyl]-N-(hexylsulfonyl)benzamide
- Benzamide, 4-[[([1,1'-biphenyl]-4-ylmethyl)thio]methyl]-N-(hexylsulfonyl)-
- KY-226