中文名称: | AdipoRon盐酸盐 | ||||
---|---|---|---|---|---|
英文名称: | AdipoRon hydrochloride | ||||
别名: | 2-(4-苯甲酰基苯氧基)-N-[1-(苯甲基)-4-哌啶基]乙酰胺盐酸盐 2-(4-benzoylphenoxy)-N-(1-benzylpiperidin-4-yl)acetamide;hydrochloride | ||||
CAS No: | 1781835-20-8 | 分子式: | C27H29ClN2O3 | 分子量: | 464.98 |
CAS No: | 1781835-20-8 | ||||
分子式: | C27H29ClN2O3 | ||||
分子量: | 464.98 |
包装规格:
5mg 50mg 100mg in glass bottle
产品简介:
AdipoRon hydrochloride 是一种可口服的,特异性的 AdipoR 激动剂,能够与 AdipoR1 和 AdipoR2 结合,Kd 值分别为 1.8 和 3.1 μM。
溶解性:
溶于DMSO和乙醇
靶点:
Kd: 1.8 μM (AdipoR1)
3.1 μM (AdipoR2)
3.1 μM (AdipoR2)
体外研究:
AdipoRon hydrochloride is an orally active and specific AdipoR agonist, binds to AdipoR1 and AdipoR2, with Kds of 1.8 and 3.1 μM. AdipoRon (50 nM-50 μM) increases AMPK phosphorylation via AdipoR1. AdipoRon (50 μM) dose-dependently attenuates the expression of TNF-α and TGF-β1 in the L02 cells. AdipoRon exhibits significant and dosage-dependent growth suppression on macrophages. AdipoRon treatment significantly improves cardiac functional recovery after reperfusion, and inhibits post-MI apoptosis. AdipoRon exerts vasodilation by mechanisms distinct to adiponectin and induces vasorelaxation without a marked decrease in VSMC [Ca2+]i.
体内研究:
AdipoRon (50 mg/kg, i.v.) cuases significant phosphorylation of AMPK in skeletal muscle and liver of wild-type mice but not Adipor1−/− Adipor2−/− double-knockout mice. AdipoRon (0.02, 0.1, and 0.5 mg/kg, i.g.) alleviates D-GalN induced hepatotoxicity in mice, and prevents hepatic architecture distortion against D-GalN challenge. The hepatoprotective potential of AdipoRon is particularly evident in higher dosages (0.1 and 0.5 mg/kg). Enhanced cardiomyocyte apoptosis in APN-deficient mice is rescued by AdipoRon (50 mg/kg, p.o.) administration. Antiapoptotic effect of AdipoRon is attenuated but not lost in AMPK-DN mice.
保存条件:
-20°C
注意事项:
1、为了您的安全和健康,请穿实验服并戴一次性手套操作。
2、以上信息仅做参考交流之用。
2、以上信息仅做参考交流之用。
UN码:
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危害声明:
安全说明:
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参考文献 & 客户发表文献
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