ARN14974, a benzoxazolone carboxamide, is a potent and systemically active inhibitors of intracellular acid ceramidase (IC₅₀=79 nM)^[1].

ARN14974 (20 μM; 24 hours; SW403 and Raw 264.7 cells) inhibits acid ceramidase (AC) in a complex cellular environment, leading to the intended biochemical response, that is, increased ceramide and decreased sphingosine levels^[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

ARN14974 (10 mg/kg; i.p.; mice) causes a substantial reduction in AC activity in multiple organs, including brain, liver, heart, lungs, and kidney^[1].
ARN14974 (10 mg/kg; i.p.) quickly enters the bloodstream after a single intraperitoneal administration in mice, reaching a maximal plasma concentration, C_max, of 1767.9 ng/mL and displaying a half-life time of 458 min in circulation. ARN14974 (1 mg/kg; i.v.) shows a C_max and a half-life time of 628 ng/mL and 72 min, respectively^[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

404.43

C₂₄H₂₁FN₂O₃

1644158-57-5

Room temperature in continental US; may vary elsewhere.

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

In Vitro: 

DMSO : 50 mg/mL (123.63 mM; ultrasonic and warming and heat to 60°C)

*

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 mg/mL (2.47 mM); Suspended solution; Need ultrasonic

  此方案可获得 1 mg/mL (2.47 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 10.0 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% corn oil

  Solubility: ≥ 1 mg/mL (2.47 mM); Clear solution

  此方案可获得 ≥ 1 mg/mL (2.47 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 10.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

• [1]. Pizzirani D, et al. Benzoxazolone carboxamides: potent and systemically active inhibitors of intracellular acid ceramidase. Angew Chem Int Ed Engl. 2015;54(2):485-489.