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1621673-53-7

中文名稱 抑制劑
英文名稱 KY-226
CAS 1621673-53-7
分子式 C27H31NO3S2
分子量 481.67
MOL 文件 1621673-53-7.mol
更新日期 2023/03/20 15:41:23
1621673-53-7 結(jié)構(gòu)式 1621673-53-7 結(jié)構(gòu)式

基本信息

中文別名
化合物KY-226
英文別名
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

物理化學(xué)性質(zhì)

密度1.186±0.06 g/cm3(Predicted)
儲存條件-20°
溶解度溶于 DMSO (>25 mg/ml)。
酸度系數(shù)(pKa)3.91±0.40(Predicted)
形態(tài)固體
顏色米白色
穩(wěn)定性自購買之日起 1 年內(nèi)保持穩(wěn)定。 DMSO 中的溶液可在 -20° 下保存長達(dá) 3 個月。

安全數(shù)據(jù)

危險性符號(GHS)GHS hazard pictograms
GHS07
警示詞警告
危險性描述H302-H315-H319-H335

常見問題列表

生物活性
KY-226 是一種有效的、口服活性的 protein tyrosine phosphatase 1B (PTP1B) 的選擇性變構(gòu)抑制劑,對人PTP1B的IC50值為0.28 μM。KY-226 通過增強 insulin 和 leptin 信號傳導(dǎo)來發(fā)揮抗糖尿病和抗肥胖的作用。
靶點
TargetValue
PTP1B
(Cell-free assay)
0.28 μM
體外研究

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

Cell Line: bEnd.3 cells stimulated with LPS
Concentration: 1 μM
Incubation Time: 24 hours
Result: Rescued lipopolysaccharide-induced reduction of mRNA and protein levels of ZO-1.
體內(nèi)研究

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.

Animal Model: Male db/db mice (8-11 weeks old)
Dosage: 10 mg/kg and 30 mg/kg
Administration: Oral administration; daily; for 4 weeks
Result: Significantly reduced plasma glucose and triglyceride levels as well as hemoglobin A1c values without increasing body weight gain.
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