LY2562175
产品名称:LY2562175
产品描述:
产品描述 | LY2562175 is an effective and selective FXR agonist (EC50: 193 nM). |
靶点活性 | FXR:(EC50)193 nM |
体外活性 | LY2562175 boosts transcriptional activation of human FXR in a cell-based co-transfection assay (EC50: 193 nM) and it also promotes the recruitment of a peptide from the nuclear receptor interaction domain of the coactivator SRC-1 (a relative EC50: 121 nM). It has 93.5% efficacy as compare to GW4064. |
体内活性 | LY2562175 induces a dose-dependent decrease in serum cholesterol and serum triglycerides. LY2562175(female ZDF rats) treatment, causes a dose-dependent lowering of plasma triglycerides in the fasted and nonfasted states. LY2562175 further lowers fasted and nonfasted plasma triglycerides when administered as a fixed-dose combination with BRL49653. At a dose of 10 mg/kg, the decrease in cholesterol with LY2562175 is 80% below vehicle-treated animals, and the decrease in serum triglycerides is 76% from the control group. The ED50 for serum cholesterol is determined to be 2 and 3.4 mg/kg for serum triglycerides. FPLC fractionation of the lipoproteins shows that LY2562175 treatment causes a reduction in vLDL-C and a dramatic increase in HDL-c in this animal model. |
分子量 | 540.44 |
分子式 | C28H27Cl2N3O4 |
CAS No. | 1103500-20-4 |
存储
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
H2O: < 0.1 mg/mL (insoluble)
DMSO: 62.5 mg/mL (115.65 mM),Need ultrasonic
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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西安齐岳生物科技有限公司是集化学科研和定制与一体的高科技化学公司。业务范围包括化学试剂和产品的研发、生产、销售等。涉及产品为通用试剂的分销、非通用试剂的定制与研发,涵盖生物科技、化学品、中间体和化工材料等领域。
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