Efaproxiral sodium
Based on 1 publication(s) in Google Scholar
Efaproxiral (RSR13) sodium is a haemoglobin (Hb) synthetic allosteric modifier. Efaproxiral sodium decreases Hb-oxygen (O2) binding affinity and enhances oxygenation of hypoxic tumours during radiation therapy .
For research use only. We do not sell to patients.
- Purity: 99.72%
- CAS No.: 170787-99-2
- Formula: C20H22NNaO4
- Molecular Weight:363.38
-
Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
-
Solvent & Solubility
- Purity & Documentation
- References
-
Help & FAQs
-
Anti-Infection Compound Library
HY-L002
-
Metabolism/Protease Compound Library
HY-L012
-
Anti-Cancer Compound Library
HY-L025
-
FDA Approved & Pharmacopeial Drug Library
HY-L066
-
Rare Diseases Drug Library
HY-L102
-
Human Metabolite Library
HY-L123
-
Bioactive Compound Library Max
HY-L181
-
MCE Bioactive Compound Library
HY-L001V
-
Bioactive Compound Library
HY-L001
-
High-Throughput Bioactive Compound Library
HY-L205
-
Mass Spectrometry Human Metabolite Library
HY-L215
Publications Citing Use of MedChemExpress (MCE) Efaproxiral sodium
More
Biological Activity
Efaproxiral sodium binds to only one pair of symmetry-related sites in the Hb central water cavity[2].
Efaproxiral sodium readily crosses the red cell membrane in the presence of serum albumin solutions[2].
Efaproxiral sodium is not inhibited from entering erythrocytes in the presence of an anion-channel blocking agent (DIDS)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Efaproxiral sodium reduces hemoglobin-oxygen binding affinity, which facilitates oxygen release from hemoglobin into surrounding tissues and potentially increases the pO(2) of the tumors[4]
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Female C3H/HEJ mice (18-20 g), with radiation-induced fibrosarcoma tumor (RIF-1) cells xenograft[3]
-
Dosage:150 mg/kg
-
Administration:Intraperitoneal injection; prior to X Irradiation (4 Gy/day), for 5 days
-
Result:Significantly increased tumor oxygenation by 8.4 to 43.4 mmHg within 5 days, with maximum increases at 22–31 minutes after treatment.
Chemical Information
-
CAS No. 170787-99-2
-
Appearance Solid
-
Molecular Weight 363.38
-
Formula C20H22NNaO4
-
Color White to off-white
-
SMILES
CC(C)(OC1=CC=C(CC(NC2=CC(C)=CC(C)=C2)=O)C=C1)C(O[Na])=O
-
Synonyms
RSR13 sodium
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (1)
-
Journal Impact Factor
-
Most Recent
-
J Enzyme Inhib Med Chem
Pharmacophore-guided repurposing of fibrates and retinoids as GPR40 allosteric ligands with activity on insulin release. [Abstract]2021 Dec;36(1):377-383. PMID: 33525941
Solvent & Solubility
DMSO : 175 mg/mL (481.59 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : ≥ 33.33 mg/mL (91.72 mM)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (5.72 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (5.72 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Purity & Documentation
-
Data Sheet (273 KB)
-
SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
-
Handling Instructions (2659 KB)
References
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 2.7519 mL | 13.7597 mL | 27.5194 mL | 68.7985 mL |
| 5 mM | 0.5504 mL | 2.7519 mL | 5.5039 mL | 13.7597 mL | |
| 10 mM | 0.2752 mL | 1.3760 mL | 2.7519 mL | 6.8799 mL | |
| 15 mM | 0.1835 mL | 0.9173 mL | 1.8346 mL | 4.5866 mL | |
| 20 mM | 0.1376 mL | 0.6880 mL | 1.3760 mL | 3.4399 mL | |
| 25 mM | 0.1101 mL | 0.5504 mL | 1.1008 mL | 2.7519 mL | |
| 30 mM | 0.0917 mL | 0.4587 mL | 0.9173 mL | 2.2933 mL | |
| 40 mM | 0.0688 mL | 0.3440 mL | 0.6880 mL | 1.7200 mL | |
| 50 mM | 0.0550 mL | 0.2752 mL | 0.5504 mL | 1.3760 mL | |
| 60 mM | 0.0459 mL | 0.2293 mL | 0.4587 mL | 1.1466 mL | |
| 80 mM | 0.0344 mL | 0.1720 mL | 0.3440 mL | 0.8600 mL | |
| DMSO | 100 mM | 0.0275 mL | 0.1376 mL | 0.2752 mL | 0.6880 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Efaproxiral sodium Related Classifications
HY-13619A Related Classifications
Powered by Bioz