196808-24-9
中文名稱
N-(2-苯甲?；交?-O-[2-(甲基-2-吡啶基氨基)乙基]-L-酪氨酸
英文名稱
GW1929
CAS
196808-24-9
分子式
C30H29N3O4
分子量
495.57
MOL 文件
196808-24-9.mol
196808-24-9 結(jié)構(gòu)式
基本信息
中文別名
N-(2-苯甲?；交?-O-[2-(甲基-2-吡啶基氨基)乙基]-L-酪氨酸 英文別名
GW1929GW1929 HYDRATE
GW 1929 hydrochloride
GW1929 - CAS 196808-24-9 - Calbiochem
N-(2-BENZOYLPHENYL)-O-[2-(METHYL-2-PYRIDINYLAMINO)ETHYL]-L-TYROSINE
L-Tyrosine, N-(2-benzoylphenyl)-O-[2-(methyl-2-pyridinylamino)ethyl]-
N-(2-Benzoylphenyl)-O-[2-(methyl-2-pyridinylamino)ethyl]-L-tyrosine hydrate
N-(2-Benzoylphenyl)-O-[2-(methyl-2-pyridinylamino)ethyl]-L-tyrosinehydrochloride
(2S)-2-(2-benzoylanilino)-3-[4-[2-[methyl(pyridin-2-yl)amino]ethoxy]phenyl]propanoic acid
(S)-2-(2-Benzoylphenylamino)-3-(4-(2-(methyl(pyridin-2-yl)amino)ethoxy)phenyl)propanoic acid
所屬類別
生物化工：激動(dòng)劑抑制劑物理化學(xué)性質(zhì)
沸點(diǎn)749.2±60.0 °C(Predicted)
密度1.264±0.06 g/cm3(Predicted)
儲(chǔ)存條件Desiccate at +4°C
溶解度DMSO: 20 mg/mL
溶解度二甲基亞砜：20 毫克/毫升
酸度系數(shù)(pKa)3.91±0.10(Predicted)
形態(tài)solid
顏色yellow
InChIKeyQTQMRBZOBKYXCG-MHZLTWQESA-N
常見(jiàn)問(wèn)題列表
生物活性
GW1929是有效的 PPAR-γ 激動(dòng)劑，對(duì)人 PPAR-γ 的 pKi 為8.84。對(duì)人和鼠的 pEC50 分別為8.56 和 8.27。靶點(diǎn)
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PPAR-γ 8.56 (pEC 50 , Human PPAR-γ) |
體外研究
GW1929 is a potent PPAR-γ activator, with pK i s of 8.84, < 5.5, and < 6.5 for human PPAR-γ, PPAR-α, and PPAR-δ, and pEC 50 s of 8.56 and 8.27 for human PPAR-γ and murine PPAR-γ, respectively. GW1929 (10 μM) inhibits TBBPA-induced caspase-3 increase and TBBPA-stimulated LDH release in neocortical cell cultures.
體內(nèi)研究
GW1929 (0.5, 1, 5 mg/kg, p.o.) highly decreases nonfasted plasma glucose levels in Zucker diabetic fatty (ZDF) rats after treatment for 14 days, and possesses antilipolytic efficacy. GW1929 (1, 5 mg/kg, p.o.) increases glucose-stimulated insuline secretion of β-cell in ZDF rats.