Etrasimod

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Etrasimod (APD334) 是一种有效的、选择性的、集中有效的 S1P1 受体拮抗剂，β-arrestin EC50 为 6.1 nM，在表达 HA 标记的 S1P1 的 CHO 细胞中内化人 S1P1，IC50 为 1.88 nM。

Etrasimod (APD334) is a potent, selective, centrally available S1P1 receptor antagonist with β-arrestin EC50 of 6.1 nM, internalizes human S1P1 in CHO cells expressing HA tagged S1P1 with IC50 of 1.88 nM; produces robust lymphocyte lowering effect (IC50=0.1 uM in mice), shows effectivity in mouse experimental autoimmune encephalomyelitis (EAE) model of MS and a rat collagen induced arthritis (CIA) model, orally active.Irritable Bowel Syndrome Phase 2 Clinical(In Vitro):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).(In Vivo):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. Rat and monkey t1/2 values for siponimod (another S1P1 modulator currently in human trials) have been disclosed and are 6 and 19 h, respectively.

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APD334 | APD-334 | APD 334

GPCR/G Protein

Lysophospholipid Receptor

Lysophospholipid Receptor

Other Indications

Irritable Bowel Syndrome

1206123-37-6

457.4847

C26H26F3NO3

>98% (HPLC)

DMSO: ≥ 28 mg/mL

C1CCC(C1)C2=C(C=C(C=C2)COC3=CC4=C(C=C3)NC5=C4CCC5CC(=O)O)C(F)(F)F

Cyclopent[b]indole-3-acetic acid, 7-[[4-cyclopentyl-3-(trifluoromethyl)phenyl]methoxy]-1,2,3,4-tetrahydro-, (3R)-

(-20℃)

With Ice Pack

≥ 2 years