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Efaproxiral Sodium(RSR13)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Efaproxiral Sodium(RSR13)图片
CAS NO:170787-99-2
规格:≥98%
包装与价格:
包装价格(元)
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议
1g电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)363.38
FormulaC20H23NO4.Na
CAS No.170787-99-2
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 73 mg/mL (200.9 mM)
Water: 73 mg/mL (200.9 mM)
Ethanol: 73 mg/mL (200.9 mM)
Other info

Chemical Name: Sodium 2-[4-[2-[(3,5-Dimethylphenyl)amino]-2-oxoethyl]phenoxy]-2-methylpropanoate

InChi Key: SWDPIHPGORBMFR-UHFFFAOYSA-M

InChi Code: InChI=1S/C20H23NO4.Na/c1-13-9-14(2)11-16(10-13)21-18(22)12-15-5-7-17(8-6-15)25-20(3,4)19(23)24;/h5-11H,12H2,1-4H3,(H,21,22)(H,23,24);/q;+1/p-1

SMILES Code: CC(C)(OC1=CC=C(CC(NC2=CC(C)=CC(C)=C2)=O)C=C1)C([O-])=O.[Na+]

Synonyms

RSR 13 sodium; RSR-13; RSR13

实验参考方法
In Vitro

In vitro activity: Efaproxiral, a synthetic allosteric modifier of hemoglobinoxygen binding affinity, has been shown to bind reversibly to hemoglobin, stabilizing the deoxyhemoglobin tetramer conformation to reduce its affinity for oxygen.

In VivoEfaproxiral plus oxygen breathing reduces the radiobiological hypoxic fraction of EMT6 tumors from the value of 24% found in both air-breathing and oxygen-breathing mice to 9% and improves the response of the tumors to radiation. Carboplatin (100 mg/kg) slowes tumor growth in air-breathing mice, producing a growth delay of 3.3 days. Efaproxiral plus oxygen increases the growth delay to 5.7 days; this is 2.4 days (71%) greater than that for carboplatin alone and 2.1 days (57%) greater than that for carboplatin plus oxygen breathing. Efaproxiral plus oxygen breathing, therefore, improves the tumor growth delay obtained with 100 mg/kg carboplatin to or beyond that obtained with the highly toxic dose of 150 mg/kg carboplatin, but does so without increasing the toxicity beyond that seen with 100 mg/kg carboplatin in air-breathing mice. Efaproxiral significantly increases tumor oxygenation by 8.4 to 43.4 mmHg within 5 days in C3H mice with RIF-1 tumors, with maximum increases at 22-31 min after treatment. Efaproxiral plus oxygen plus Radiation produces tumor growth inhibition throughout the treatment duration in C3H mice with RIF-1 tumors, and inhibition is significantly different from radiation plus oxygen from day 3 to day 5.
Animal modelMice
Formulation & Dosage
References

Exp Biol Med (Maywood). 2006 Mar;231(3):317-21; Radiat Res. 2007 Aug;168(2):218-25.