O304

产品编号: DC10807 Featured
O304
结构式
1261289-04-6
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中国地区超过5000个高品质化合物库存
应用领域
O-304 是一种一流的可口服的泛 AMPK 激活剂,可通过抑制 pAMPK 的去磷酸化来增加 AMPK 活性。O-304 在治疗 2 型糖尿病和相关心血管并发症中具有巨大潜力。
Cas No.: 1261289-04-6
名称:
别名: O-304,0 304
SMILES: C1=CC(Cl)=CC=C1CN1C(=O)N=C(NC(=O)C2=CC=C(Cl)C=C2)S1
分子式: C16H11Cl2N3O2S
分子量: 378.99
纯度:
保存条件: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description:
In Vivo:
In Vitro:
References: O304 increases the levels of p-T172 AMPK in a dose-dependent manner in cells from a variety of species. Moreover, under these conditions, and unlike Metformin, O304 increases cellular ATP.The rate of dephosphorylation of p-T172 AMPKα by the protein phosphatases PP2C and PP1 is a key regulatory step of AMPK activation. Using purified human recombinant enzymes, O304 suppresses the dephosphorylation of p-T172 AMPK trimer by both PP2C and PP1, without inhibiting their activities. O304 also suppresses the dephosphorylation of partially purified rat liver AMPK by PP2C. Like ADP, but unlike AMP, O304 does not allosterically activate AMPK heterotrimers in vitro.O304 significantly enhances endurance in sedentary obese diabetic and aged normal mice defined as an increase in running distance to exhaustion. O304 also promotes blood glucose disposal in diabetic mice. Moreover, in obese rats O304 stimulates the generation of active brown fat cells which dispose of calories as heat recorded as a significantly increased body surface temperature at the back, without an increase in core body temperature. Thus, O304 acts as a 3-in-1 drug that would be expected to have synergistic beneficial effects in large populations of individuals affected by muscle weakness (sarcopenia), obesity or the metabolic syndrome either alone or in combination. O304 has been selected as clinical candidate and will be subjected to IND-enabling GLP-tox studies.
Kinase Assay:
Cell Assay:
Animal Administration:
References:
MSDS
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MSDS_550_DC10807_1261289-04-6
COA
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产品编号 产品名称 应用领域
DC10807 O304 O-304 是一种一流的可口服的泛 AMPK 激活剂,可通过抑制 pAMPK 的去磷酸化来增加 AMPK 活性。O-304 在治疗 2 型糖尿病和相关心血管并发症中具有巨大潜力。