1. GPCR/G Protein
  2. LPL Receptor
  3. Etrasimod

Etrasimod (Synonyms: APD334)

製品番号: HY-12789 純度: 99.57%
取扱説明書

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.

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Etrasimod 構造式

Etrasimod 構造式

CAS 番号 : 1206123-37-6

容量 価格(税別) 在庫状況 数量
10 mM * 1  mL in DMSO USD 399 在庫あり
Estimated Time of Arrival: December 31
1 mg USD 132 在庫あり
Estimated Time of Arrival: December 31
5 mg USD 396 在庫あり
Estimated Time of Arrival: December 31
10 mg USD 600 在庫あり
Estimated Time of Arrival: December 31
50 mg USD 1800 在庫あり
Estimated Time of Arrival: December 31
100 mg USD 2520 在庫あり
Estimated Time of Arrival: December 31
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500 mg   お問い合わせ  

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製品説明

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.

IC50 & Target

IC50: 1.88 nM (S1P1)[1]

体外実験

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)[1].

体内実験

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[1].

臨床実験
分子量

457.48

分子式

C₂₆H₂₆F₃NO₃

CAS 番号

1206123-37-6

SMILES

FC(F)(F)C1=CC(COC2=CC=C(NC3=C4CC[[email protected]@H]3CC(O)=O)C4=C2)=CC=C1C5CCCC5

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

DMSO : ≥ 28 mg/mL (61.20 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1859 mL 10.9294 mL 21.8589 mL
5 mM 0.4372 mL 2.1859 mL 4.3718 mL
10 mM 0.2186 mL 1.0929 mL 2.1859 mL
*Please refer to the solubility information to select the appropriate solvent.
参考文献
動物実験
[1]

Rats: APD334 induced effects on blood lymphopenia are determined in male Sprague-Dawley rats. Briefly, male rats are given a 0 (vehicle only), 0.03 (mice only), 0.1, 0.3 or 1 mg/kg oral dose of APD334 formulated in 0.5% methylcellulose (MC) in water. Rat blood samples are collected at 0, 1, 3, 5, 8, 16, 24, 32, 48 and 72 hours post-dose[1].

Mice: APD334 induced effects on blood lymphopenia are determined in male BALB/c mice. Briefly, male mice are given a 0 (vehicle only), 0.03 (mice only), 0.1, 0.3 or 1 mg/kg oral dose of APD334 formulated in 0.5% methylcellulose (MC) in water. Mouse blood samples are taken at 0, 1, 3, 5, 8, 16, 24 and 32 hours post-dose[1].

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参考文献
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Keywords:

EtrasimodAPD334APD 334APD-334LPL ReceptorLysophospholipid ReceptorInhibitorinhibitorinhibit

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製品名:
Etrasimod
製品番号:
HY-12789
数量:
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