ASP-4058|cas:952565-91-2|西域试剂

ASP-4058,99.43%

产品编号：Bellancom-111021| CAS NO：952565-91-2| 分子式：C₁₉H₁₂F₆N₄O₂| 分子量：442.31

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货号	价格	库存与货期
Bellancom-111021	￥3600.00	杭州北京（现货）
Bellancom-111021	￥5900.00	杭州北京（现货）
Bellancom-111021	￥11800.00	杭州北京（现货）

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ASP-4058

产品介绍

ASP-4058 是一个选择性的、口服活性的鞘氨醇磷酸受体 1 和 5 (S1P₁ and S1P₅) 的二代激动剂，能改善小鼠实验性自身免疫性脑脊髓炎，具有良好的安全性。

生物活性

ASP-4058 is a next-generation, selective and oral bioactive agonist for Sphingosine 1-Phosphate receptors 1 and 5 (S1P₁ and S1P₅), ameliorates rodent experimental autoimmune encephalomyelitis with a favorable safety profile.

体外研究

体内研究

ASP4058 (p.o., daily for 21 days) reduces the clinical score in a dose-dependent manner and the cumulative clinical score from day 0 to 21 dpi at 0.03, 0.1 and 0.3 mg/kg are 15.5±1.48, 9.50±2.17 and 1.17±1.17, respectively, while that of vehicle-treated group is 15.5±0.619 in rats. ASP4058 prevents decreases in body weight of EAE rats.
ASP4058 (p.o., daily for day 12 to day 45) maintains the clinical score at a relatively low level and the cumulative clinical scores (18-45 dpi) among the groups treated with 0.1 and 0.3 mg/kg dosages are 6.90±2.85 and 5.60±2.21, respectively in mice. The ED50 values for ASP4058 is 0.063 mg/kg.

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

Animal Model:	Male Lewis rats with an induction of EAE.
Dosage:	0.03, 0.1 or 0.3 mg/kg.
Administration:	Oral administration once daily for 21 days.
Result:	Reduced the clinical score in a dose-dependent manner and the cumulative clinical score.

Animal Model:	SJL mice immunized with PLP139-151 and boosted with pertussis toxin developed relapsing-remitting EAE.
Dosage:	0.1 and 0.3 mg/kg
Administration:	Oral administration once daily from day 12 to day 45.
Result:	Maintained the clinical score at a relatively low level and the cumulative clinical scores (18-45 dpi).

体内研究

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

Animal Model:	Male Lewis rats with an induction of EAE.
Dosage:	0.03, 0.1 or 0.3 mg/kg.
Administration:	Oral administration once daily for 21 days.
Result:	Reduced the clinical score in a dose-dependent manner and the cumulative clinical score.

Animal Model:	SJL mice immunized with PLP139-151 and boosted with pertussis toxin developed relapsing-remitting EAE.
Dosage:	0.1 and 0.3 mg/kg
Administration:	Oral administration once daily from day 12 to day 45.
Result:	Maintained the clinical score at a relatively low level and the cumulative clinical scores (18-45 dpi).

性状

Solid

溶解性数据

In Vitro:

DMSO : ≥ 50 mg/mL (113.04 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	2.2609 mL	11.3043 mL	22.6086 mL
5 mM	0.4522 mL	2.2609 mL	4.5217 mL
10 mM	0.2261 mL	1.1304 mL	2.2609 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 (protect from light)。-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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 1.25 mg/mL (2.83 mM); Clear solution

此方案可获得 ≥ 1.25 mg/mL (2.83 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 12.5 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: 1.25 mg/mL (2.83 mM); Suspended solution; Need ultrasonic

此方案可获得 1.25 mg/mL (2.83 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 12.5 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 1.25 mg/mL (2.83 mM); Clear solution

此方案可获得 ≥ 1.25 mg/mL (2.83 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 12.5 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。