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• 產(chǎn)品描述： Etrasimod (APD334) is a potent, selective and orally available antagonist of the sphingosine-1-phosphate-1 (S1P1) receptor with an IC50 value of 1.88 nM in CHO cells

• 靶點(diǎn)： IC50: 1.88 nM (S1P1);S1PReceptor;?LPLReceptor

• 體外研究：
  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)

• 體內(nèi)研究：
  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

• 參考文獻(xiàn)：
  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.

• 溶解性： soluble  in  DMSO

• 保存條件： -20℃

• 配置溶液濃度參考：
  

  	1mg	5mg	10mg
  1 mM	2.186 ml	10.929 ml	21.859 ml
  5 mM	0.437 ml	2.186 ml	4.372 ml
  10 mM	0.219 ml	1.093 ml	2.186 ml
  50 mM	0.044 ml	0.219 ml	0.437 ml

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輸入產(chǎn)品批號：

本計(jì)算器可幫助您計(jì)算出特定溶液中溶質(zhì)的質(zhì)量、溶液濃度和體積之間的關(guān)系，公式為：

質(zhì)量 (mg) = 濃度 (mM) x 體積 (mL) x 分子摩爾量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *