NLG802 是 indoximod 的前药,indoximod 是一种口服活性的吲哚胺2,3-双加氧酶(IDO)抑制剂。
产品描述
NLG802 is a prodrug of indoximod, an orally active indoleamine 2,3-dioxygenase (IDO) inhibitor.
体外活性
NLG802 showed moderate direct (IC50 5 μM) and time dependent (7-fold shift) inhibition of CYP3A4, weak inhibition to CYP2D6 (IC50 19 μM) and CYP2C19 (IC50 47 μM), no inhibition of CYP450 1A2, 2B6, 2C8 and 2C9 (IC50 >50 μM) and no induction of CYP1A2, 2B6 or 3A4 in human hepatocytes. NLG802 showed moderate inhibition of P-gp transporter activity in MDR1-MDCKII cells (IC50 27 μM), does not inhibit the anion and cation transporters OATP1B1, OATP1B3, OAT1, OAT3, OCT1 and OCT2 in HEK293 cells expressing these transporters (IC50 >50 μM) or the BRCP transporter in Caco-2 cells[1].
Cas No.
2071683-99-1
分子式
C20H30ClN3O3
分子量
395.93
储存和溶解度
DMSO:225mg/mL (568.3mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years