Efaproxiral is a haemoglobin (Hb) synthetic allosteric modifier, decreases Hb-oxygen (O2) binding affinity and enhances oxygenation of hypoxic tumours during radiation therapy ^[1].

haemoglobin (Hb)^[1]

Efaproxiral binds to only one pair of symmetry-related sites in the Hb central water cavity^[2].
Efaproxiral readily crosses the red cell membrane in the presence of serum albumin solutions^[2].
Efaproxiral is not inhibited from entering erythrocytes in the presence of an anion-channel blocking agent (DIDS)^[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Efaproxiral (150 mg/kg, i.p.) increase tumor oxygenation，and increase the tumor growth inhibition of radiotherapy over 5 days of treatment^[3].
Efaproxiral reduces hemoglobin-oxygen binding affinity, which facilitates oxygen release from hemoglobin into surrounding tissues and potentially increases the pO(2) of the tumors^[4]

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

341.40

C₂₀H₂₃NO₄

131179-95-8

乙丙昔罗

Room temperature in continental US; may vary elsewhere.

DMSO : ≥ 150 mg/mL (439.37 mM)

* “≥” means soluble, but saturation unknown.

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。

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： 50% PEG300    50% saline

  Solubility: 27.5 mg/mL (80.55 mM); Clear solution; Need ultrasonic
• 2.

  请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

  Solubility: ≥ 2.08 mg/mL (6.09 mM); Clear solution

  此方案可获得 ≥ 2.08 mg/mL (6.09 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 20.8 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

• 3.

  请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

  Solubility: ≥ 2.08 mg/mL (6.09 mM); Clear solution

  此方案可获得 ≥ 2.08 mg/mL (6.09 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 20.8 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
• 4.

  请依序添加每种溶剂： 10% DMSO    90% corn oil

  Solubility: ≥ 2.08 mg/mL (6.09 mM); Clear solution

  此方案可获得 ≥ 2.08 mg/mL (6.09 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 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

• [1]. Stea B, et al. Efaproxiral red blood cell concentration predicts efficacy in patients with brain metastases. Br J Cancer. 2006 Jun 19;94(12):1777-1784.

  [2]. Abraham DJ, et al. Allosteric modifiers of hemoglobin: 2-[4-[[(3,5-disubstituted anilino)carbonyl]methyl]phenoxy]-2-methylpropionic acid derivatives that lower the oxygen affinity of hemoglobin in red cell suspensions, in whole blood, and in vivo in rats. Biochemistry. 1992 Sep 29;31(38):9141-9.

  [3]. Hou H, et al. The effects of Efaproxyn (efaproxiral) on subcutaneous RIF-1 tumor oxygenation and enhancement of radiotherapy-mediated inhibition of tumor growth in mice. Radiat Res. 2007 Aug;168(2):218-25.

  [4]. Hou H, et al. Increased oxygenation of intracranial tumors by efaproxyn (efaproxiral), an allosteric hemoglobin modifier: In vivo EPR oximetry study. Int J Radiat Oncol Biol Phys. 2005 Apr 1;61(5):1503-9.