Etrasimod APD334|cas:1206123-37-6|西域试剂

Etrasimod APD334,99.82%

产品编号：Bellancom-12789| CAS NO：1206123-37-6| 分子式：C₂₆H₂₆F₃NO₃| 分子量：457.48

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货号	价格	库存与货期
Bellancom-12789	￥1400.00	杭州北京（现货）
Bellancom-12789	￥2300.00	杭州北京（现货）
Bellancom-12789	￥4800.00	杭州北京（现货）
Bellancom-12789	￥7600.00	杭州北京（现货）
Bellancom-12789	￥12000.00	杭州北京（现货）

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Etrasimod 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 an IC₅₀ value of 1.88 nM in CHO cells.

体外研究

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).

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

APD334 has a relatively low systemic clearance (<4% of hepatic blood flow) and high C_max 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 t_1/2 values for siponimod (another S1P1 modulator currently in human trials) have been disclosed and are 6 and 19 h, respectively.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

性状

Solid

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 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

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°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式