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1883548-91-1

中文名稱 ZLN-024 hydrochloride
英文名稱 ZLN-024 hydrochloride
CAS 1883548-91-1
分子式 C??H??BrClN?OS
分子量 361.68
MOL 文件 1883548-91-1.mol
更新日期 2024/11/15 18:20:34
1883548-91-1 結(jié)構(gòu)式 1883548-91-1 結(jié)構(gòu)式

基本信息

中文別名
ZLN024鹽酸鹽
化合物ZLN 024 HYDROCHLORIDE
英文別名
ZLN024 hydrochloride
ZLN-024 hydrochloride

物理化學(xué)性質(zhì)

溶解度Soluble to 100 mM in DMSO
形態(tài)Solid
顏色White to off-white
ZLN-024 hydrochloride價格(試劑級)
報價日期產(chǎn)品編號產(chǎn)品名稱CAS號包裝價格
2024/11/08HY-16708AZLN-024 hydrochloride
ZLN024 hydrochloride
1883548-91-15mg540元
2024/11/08HY-16708AZLN-024 hydrochloride
ZLN024 hydrochloride
1883548-91-110mM * 1mLin DMSO594元
2024/11/08HY-16708AZLN-024 hydrochloride
ZLN024 hydrochloride
1883548-91-110mg910元

常見問題列表

生物活性
ZLN024 hydrochloride 是一種 AMPK 變構(gòu)激活劑。ZLN024 直接激活重組 AMPK α1β1γ1,AMPK α2β1γ1,AMPK α1β2γ1 和 AMPK α2β2γ1 異源三聚體,EC50 分別為 0.42 μM,0.95 μM,1.1 μM 和 0.13 μM。
靶點

AMPK α2β2γ1

0.13 μM (EC 50 )

AMPK α1β1γ1

0.42 μM (EC 50 )

AMPK α2β1γ1

0.95 μM (EC 50 )

體外研究

ZLN024 allosterically stimulates active AMPK heterotrimers and the inactive α1 subunit truncations α1 (1-394) and α1 (1-335) but not α1 (1-312). AMPK activation by ZLN024 requires the pre-phosphorylation of Thr-172 by at least one upstream kinase and protects AMPK Thr-172 against dephosphorylation by PP2Cα. ZLN024 activates AMPK in L6 myotubes and stimulates glucose uptake and fatty acid oxidation without increasing the ADP/ATP ratio. Using the established scintillation proximity assay (SPA) assay, random screening against the AMPK α1β1γ1 heterotrimer is performed and a new AMPK activator, ZLN024 is found. ZLN024 directly activates recombinant AMPK α1β1γ1 and its homologue α2β1γ1 in a concentration-dependent manner. ZLN024 increases the activity of α1β1γ1 by 1.5-fold and has an EC 50 of 0.42 μM, and it increases the activity of α2β1γ1 by 1.7-fold with an EC 50 of 0.95 μM. ZLN024 also directly activates recombinant AMPK α1β2γ1, by 1.7-fold with an EC 50 of 1.1 μM; and AMPK α2β2γ1, by 1.6-fold with an EC 50 of 0.13 μM.

體內(nèi)研究

C57BKS db/db mice are administered a 15 mg/kg/day dose of ZLN024 by daily gavage for 5 weeks; 250 mg/kg/day Metformin (Met) is used as a positive control. During the treatment period, there is no significant alteration in food intake and body weight compared with the vehicle group. After 4 weeks of treatment, ZLN024 improves glucose tolerance. ZLN024 reduces the fasting blood glucose by 15%. Liver tissue weight, triacylglycerol and the total cholesterol content are decreased.

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