Биологическая активность
Elacridar Hcl (GF120918; GW0918) is a P-glycoprotein ингибитор, and has been used both in vitro and in vivo as a tool ингибитор of P-glycoprotein (Pgp) to investigate the role of transporters in the disposition of various test molecules.IC50 value:Target: P-glycoprotein in vitro, GF120918A demonstrated high plasma protein связывание across species, although a definitive protein связывание evaluation was precluded by poor recovery, particularly in buffer and in mouse, rat, and dog plasma. GF120918A did not demonstrate мощный inhibition of several human cytochrome P450 enzymes evaluated in vitro, with IC(50) values well above concentrations anticipated to be achieved in vivo. Together, these data confirm the utility of GF120918A as a tool P-glycoprotein ингибитор in preclinical species and offer additional guidance on preclinical dose regimens likely to produce P-glycoprotein-mediated effects.
Оригинал на английском
Elacridar Hcl (GF120918; GW0918) is a P-glycoprotein inhibitor, and has been used both in vitro and in vivo as a tool inhibitor of P-glycoprotein (Pgp) to investigate the role of transporters in the disposition of various test molecules.IC50 value:Target: P-glycoprotein In vitro, GF120918A demonstrated high plasma protein binding across species, although a definitive protein binding evaluation was precluded by poor recovery, particularly in buffer and in mouse, rat, and dog plasma. GF120918A did not demonstrate potent inhibition of several human cytochrome P450 enzymes evaluated in vitro, with IC(50) values well above concentrations anticipated to be achieved in vivo. Together, these data confirm the utility of GF120918A as a tool P-glycoprotein inhibitor in preclinical species and offer additional guidance on preclinical dose regimens likely to produce P-glycoprotein-mediated effects.
Химические свойства
- CAS №
- 143851-98-3
- Брутто-формула
- C₃₄H₃₄ClN₃O₅
- Мол. масса
- 600.11 г/моль
- SMILES
- Cl.COC1C=C2CCN(CC2=CC=1OC)CCC1C=CC(NC(C2=CC=CC3C(C4C=CC=C(OC)C=4NC2=3)=O)=O)=CC=1
- Синонимы
- GF120918; GF-120918; GF 120918; GF-120918A; GF120918A и ещё 3
3D-структура молекулы
Вращайте мышью · Колесо — масштаб
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.