Биологическая активность
RG-239 is an orally active TGR5 агонист with an EC50 of 120 nM, significantly outperforming Betulinic acid (EC50 = 1.04 μM). RG-239 demonstrates higher selectivity for TGR5 compared to the FXRα. RG-239 increases mitochondrial activity in adipocytes and promotes neurite outgrowth at higher concentrations. RG-239 inhibits LPS-induced iNOS expression and nitrite production in Raw264.7 and microglia cells. RG-239 can be used for the study of type 2 diabetes.
Оригинал на английском
RG-239 is an orally active TGR5 agonist with an EC50 of 120 nM, significantly outperforming Betulinic acid (EC50 = 1.04 μM). RG-239 demonstrates higher selectivity for TGR5 compared to the FXRα. RG-239 increases mitochondrial activity in adipocytes and promotes neurite outgrowth at higher concentrations. RG-239 inhibits LPS-induced iNOS expression and nitrite production in Raw264.7 and microglia cells. RG-239 can be used for the study of type 2 diabetes.
Химические свойства
- CAS №
- 1199222-56-4
- Брутто-формула
- C₃₃H₅₂O₃
- Мол. масса
- 496.76 г/моль
Хранение и физические свойства
- Условия хранения
- 2 года -20°C порошок, 2 недели 4°C в ДМСО, 6 мес. -80°C в ДМСО
Безопасность и документация
Только для научно-исследовательского применения. Не предназначено для использования у пациентов или в качестве лекарственного средства.