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947669-86-5

中文名稱 WWL113
英文名稱 WWL113
CAS 947669-86-5
分子式 C29H26N2O4
分子量 466.53
MOL 文件 947669-86-5.mol
947669-86-5 結(jié)構(gòu)式 947669-86-5 結(jié)構(gòu)式

基本信息

中文別名
化合物 T17259
英文別名
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

物理化學(xué)性質(zhì)

沸點(diǎn)630.9±55.0 °C(Predicted)
密度1?+-.0.06 g/cm3(Predicted)
儲存條件-20°C儲存
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
酸度系數(shù)(pKa)5.18±0.26(Predicted)
形態(tài)結(jié)晶固體
顏色White to off-white

常見問題列表

生物活性
WWL113 是具有口服活性的、選擇性的 Ces3 和 Ces1f 的抑制劑,其對 Ces3 和 Ces1f 的 IC50 值分別為 120 nM 和 100 nM。WWL113 對 60-kDa絲氨酸水解酶(或水解酶)有極好的選擇性。
靶點(diǎn)

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

體外研究

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.

體內(nèi)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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