Ensifentrine RPL-554|cas:1884461-72-6|西域试剂

Ensifentrine RPL-554,99.47%

产品编号：Bellancom-119708| CAS NO：1884461-72-6| 分子式：C₂₆H₃₁N₅O₄| 分子量：477.56

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货号	价格	库存与货期
Bellancom-119708	￥3900.00	杭州北京（现货）
Bellancom-119708	￥6200.00	杭州北京（现货）
Bellancom-119708	￥12500.00	杭州北京（现货）

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Ensifentrine RPL-554

产品介绍

Ensifentrine (RPL-554) 是一种吸入式，首创的磷酸二酯酶 3 (PDE3) 和 PDE4 双重抑制剂，IC₅₀ 分别为 0.4 nM 和 1479 nM。Ensifentrine 具有支气管保护和抗炎活性，可用于慢性阻塞性肺疾病 (COPD) 的研究。

生物活性

Ensifentrine (RPL-554) is an inhaled first-in-class dual inhibitor of phosphodiesterase 3 (PDE3) and PDE4 with IC₅₀s of 0.4 nM and 1479 nM, respectively. Ensifentrine has bronchoprotective and anti-inflammatory activities. Ensifentrine can be used for chronic obstructive pulmonary disease (COPD) research.

体外研究

Ensifentrine (RPL-554) inhibits, in a concentration-dependent manner, lipopolysaccharide-induced TNF-α release from human monocytes (IC₅₀ of 0.52 μM) and proliferation of human mononuclear cells to phytohemagglutinin (IC₅₀ of 0.46 μM).
Electrical field stimulation-induced contraction of guinea pig superfused isolated tracheal preparations is significantly inhibited by Ensifentrine (10 μM). Contractile responses are suppressed for up to 12 h after termination of superfusion with RPL-554 demonstrating a long duration of action.

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

体内研究

Ensifentrine (RPL-554; 10 mg/kg; Oral administration; once) significantly inhibits eosinophil recruitment following antigen challenge in ovalbumin-sensitized guinea pigs.
The inhalation of dry powder containing Ensifentrine by conscious guinea pigs (25% in micronized lactose) 1.5 h before antigen exposure significantly inhibits the recruitment of eosinophils to the airways.
Exposure of conscious guinea pigs to inhalation of dry powder containing Ensifentrine (2.5%) in micronized lactose significantly inhibits histamine-induced plasma protein extravasation in the trachea and histamine-induced bronchoconstriction over a 5.5-h period.

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

Animal Model:	Male Dunkin Hartley guinea pigs (200-300 g) injected with ovalbumin.
Dosage:	10 mg/kg
Administration:	Oral administration; once
Result:	Significantly inhibits eosinophil recruitment following antigen challenge in ovalbumin-sensitized guinea pigs.

体内研究

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

Animal Model:	Male Dunkin Hartley guinea pigs (200-300 g) injected with ovalbumin.
Dosage:	10 mg/kg
Administration:	Oral administration; once
Result:	Significantly inhibits eosinophil recruitment following antigen challenge in ovalbumin-sensitized guinea pigs.

性状

Solid

溶解性数据

In Vitro:

DMSO : 25 mg/mL (52.35 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.0940 mL	10.4699 mL	20.9398 mL
5 mM	0.4188 mL	2.0940 mL	4.1880 mL
10 mM	0.2094 mL	1.0470 mL	2.0940 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。

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 (2.62 mM); Clear solution

此方案可获得 ≥ 1.25 mg/mL (2.62 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 (2.62 mM); Suspended solution; Need ultrasonic

此方案可获得 1.25 mg/mL (2.62 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