Etrasimod

Data Sheet For research use only. Not for human use.

Cat. No. ：BCP19558CAS No. ：1206123-37-6Purity：98%

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CAS No.	1206123-37-6	Cat. No.	BCP19558
Name	Etrasimod
Synonyms	APD334;APD-334;APD 334;
SMILES
Chemical Name
Formula	C26H26F3NO3	M. Wt	457.48
Purity	98%	Storage	Store at 4-8°C
Description	InVitro: 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). InVivo: APD334 has a relatively low systemic clearance (<4% of hepatic blood flow) and high Cmax 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. Ra