Efaproxiral-RSR13-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEEfaproxiralCat. No.: HY-13619CAS No.: 131179-95-8Synonyms: RSR13分式: CHNO分量: 341.4作靶点: Reactive Oxygen Species作通路: Immunology/Inflammation; Metabolic Enzyme/Protease; NF-B储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months

2、-20C 1 month溶解性数据体外实验 DMSO : 150 mg/mL (439.37 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.9291 mL 14.6456 mL 29.2912 mL5 mM 0.5858 mL 2.9291 mL 5.8582 mL10 mM 0.2929 mL 1.4646 mL 2.9291 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，并请注意储备液的保存式和期限。体内实验请根据您的实验动物和给

3、药式选择适当的溶解案，配制前请先配制澄清的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现现配，当天使；澄清的储备液可以根据储存条件，适当保存；以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (7.32 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (7.32 mM); Cle

4、ar solution1/2 Master of Small Molecules 您边的抑制剂师www.MedChemE3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (7.32 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Efaproxiral种红蛋 (Hb) 合成变构调节剂, 能降低红蛋氧 (O2) 的结合亲和，增强放射治疗中缺氧肿瘤的氧合作 1。IC50 & Target haemoglobin (Hb) 1体外研究 Efaproxiral binds to only one pai

5、r 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.体内研究 Efaproxiral (150 mg/kg,

6、i.p.) increase tumor oxygenation，and increase the tumor growth inhibition ofradiotherapy over 5 days of treatment 3.Efaproxiral reduces hemoglobin-oxygen binding affinity, which facilitates oxygen release from hemoglobininto surrounding tissues and potentially increases the pO(2) of the tumors 4Anim

7、al Model: Female C3H/HEJ mice (1820 g), with radiation-induced fibrosarcoma tumor (RIF-1)cells xenograft 3Dosage: 150 mg/kgAdministration: Intraperitoneal injection; prior to X Irradiation (4 Gy/day), for 5 daysResult: Significantly increased tumor oxygenation by 8.4 to 43.4 mmHg within 5 days, with

8、maximum increases at 2231 minutes after treatment.REFERENCES1. Stea B, et al. Efaproxiral red blood cell concentration predicts efficacy in patients with brain metastases. Br J Cancer. 2006 Jun19;94(12):1777-1784.2. Abraham DJ, et al. Allosteric modifiers of hemoglobin: 2-4-(3,5-disubstituted anilin

9、o)carbonylmethylphenoxy-2-methylpropionic acidderivatives that lower the oxygen affinity of hemoglobin in red cell suspensions, in whole blood, and in vivo in rats. Biochemistry. 1992 Sep29;31(38):9141-9.3. Hou H, et al. The effects of Efaproxyn (efaproxiral) on subcutaneous RIF-1 tumor oxygenation

10、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 EPRoximetry study. Int J Radiat Oncol Biol Phys. 2005 Apr 1;61(5):1503-9.McePdfHeight Caution: Product has not been fully val