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947669-86-5

中文名称 WWL113
英文名称 WWL113
CAS 947669-86-5
分子式 C29H26N2O4
分子量 466.53
MOL 文件 947669-86-5.mol
947669-86-5 结构式 947669-86-5 结构式

基本信息

中文别名
化合物 T17259
英文别名
WWL113
AKIIPHDGVCFVCC-UHFFFAOYSA-N
ethyl 4-[4-[methyl-[(3-pyridin-4-ylphenyl)methyl]carbamoyl]oxyphenyl]benzoate
4'-[[[Methyl[[3-(4-pyridinyl)phenyl]methyl]amino]carbonyl]oxy]-[1,1'-biphenyl]-4-carboxylic acid ethyl ester

物理化学性质

沸点630.9±55.0 °C(Predicted)
密度1?+-.0.06 g/cm3(Predicted)
储存条件-20°C储存
溶解度DMF: 25 mg/ml; DMF:PBS(pH7.2) (1:2): 0.3 mg/ml; DMSO: 15 mg/ml; Ethanol: 0.1 mg/ml
酸度系数(pKa)5.18±0.26(Predicted)
形态结晶固体
颜色White to off-white

常见问题列表

生物活性
WWL113 是具有口服活性的、选择性的 Ces3 和 Ces1f 的抑制剂,其对 Ces3 和 Ces1f 的 IC50 值分别为 120 nM 和 100 nM。WWL113 对 60-kDa丝氨酸水解酶(或水解酶)有极好的选择性。
靶点

IC50: 120 nM (Ces3), 100 nM (Ces1f).

体外研究

Ces3 and Ces1f are endoplasmic reticulum glycoproteins that have been previously associated with adipocyte lipolysis. WWL113 inhibits mouse recombinant Ces1, Ces1c, and ABHD6 at 10 μM.
WWL113 (1 μM) significantly increases UCP1 protein expression in brown adipocytes.
WWL113 has a partial, statistically significant inhibitory effect on blocking the buildup of PGE2.

体内研究

WWL113 (30 mg/kg, orally once a day) results in major improvement of multiple features of metabolic syndrome and ameliorated obesity-diabetes in mice with lowered levels of nonesterified free fatty acids (NEFAs), triglycerides (TGs), total cholesterol and fasted glucose as well as enhanced glucose tolerance.
WWL113 ameliorates obesity-diabetes in mice.

Animal Model: Eight-week-old db/db mice (n = 10 per group).
Dosage: 30 mg/kg.
Administration: Orally once a day for 3 weeks.
Result: Corrected multiple features of metabolic syndrome in db/db mice.
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