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Etrasimod
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Etrasimod图片
CAS NO:1206123-37-6
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品名称
APD334
产品介绍
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。
生物活性

Etrasimod (APD334) is a potent, selective and orally available antagonist of the sphingosine-1-phosphate-1 (S1P1) receptor with anIC50value of 1.88 nM in CHO cells.

IC50& Target

IC50: 1.88 nM (S1P1)[1]

体外研究
(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 IC50value of 1.88 nM. Moderate agonism at human S1P4and S1P5is observed but is reduced relative to S1P1, both in terms of potency and efficacy. APD334 is devoid of any agonism or antagonism at human S1P2and S1P3. APD334 achieves good central exposure following oral dosing and possesses a favorable pharmacokinetic profile in multiple preclinical species. S1P1activity 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].

体内研究
(In Vivo)

APD334 has a relatively low systemic clearance (<4% of hepatic blood flow) and high Cmaxacross 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 t1/2values for siponimod (another S1P1 modulator currently in human trials) have been disclosed and are 6 and 19 h, respectively[1].

Clinical Trial
分子量

457.48

性状

Solid

Formula

C26H26F3NO3

CAS 号

1206123-37-6

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : ≥ 28 mg/mL(61.20 mM)

*"≥" means soluble, but saturation unknown.

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.1859 mL10.9294 mL21.8589 mL
5 mM0.4372 mL2.1859 mL4.3718 mL
10 mM0.2186 mL1.0929 mL2.1859 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。