Etrasimod (APD334) 是高效的有选择性和口服活性的S1P₁受体拮抗剂，在CHO细胞中的IC₅₀值为1.88 nM。

Etrasimod (APD334) is a potent, selective and orally available antagonist of the sphingosine-1-phosphate-1 (S1P 1 ) receptor with an IC 50 value of 1.88 nM in CHO cells.

Solid

IC50: 1.88 nM (S1P1)

APD334 is a structurally novel, selective, functional antagonist of S1P1. In CHO cells expressing HA tagged S1P1, APD334 is found to have an IC50 value of 1.88 nM. Moderate agonism at human S1P4 and S1P5 is observed but is reduced relative to S1P1, both in terms of potency and efficacy. APD334 is devoid of any agonism or antagonism at human S1P2 and S1P3. APD334 achieves good central exposure following oral dosing and possesses a favorable pharmacokinetic profile in multiple preclinical species. S1P1 activity is maintained in mice (EC50=0.44 nM), rats (EC50=0.32 nM), dogs (EC50=0.34 nM) and monkeys (EC50=0.32 nM). has not independently confirmed the accuracy of these methods. The

APD334 has a relatively low systemic clearance (<4% of hepatic blood flow) and high C max across all species. In both dog and monkey a significant decrease in volume of distribution (Vss) is observed relative to rodent. Oral bioavailability is in the range of 40–100%, and the terminal phase half-life varied from 6 h in monkey, to as long as 29 h in dog. Rat and monkey t 1/2 values for siponimod (another S1P1 modulator currently in human trials) have been disclosed and are 6 and 19 h, respectively. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Buzard DJ, et al. Discovery of APD334: Design of a Clinical Stage Functional Antagonist of the Sphingosine-1-phosphate-1 Receptor. ACS Med Chem Lett. 2014 Nov 4;5(12):1313-7.

In Vitro: DMSO : ≥ 28 mg/mL (61.20 mM)配制储备液