Art. -Nr.: HY-13619A

Efaproxiral sodium

(Synonyms: RSR13 sodium)

1 Cited Publications

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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 .

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Reinheit: 99.72%
CAS. Nr.: 170787-99-2
Formel: C₂₀H₂₂NNaO₄
Molecular Weight:363.38

Speicherung:

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Efaproxiral sodium Chemical Structure

CAS. Nr.: 170787-99-2

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Biologische Aktivität
- Beschreibung
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

In Vitro

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.

In Vivo

Efaproxiral (150 mg/kg, i.p.) sodium increase tumor oxygenation, and increase the tumor growth inhibition of radiotherapy over 5 days of treatment^[3].
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. Nr. 170787-99-2
Appearance Solid
Molecular Weight 363.38
Formel 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
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Publications (1)

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Journal Impact Factor

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

Lösungsmittel & Löslichkeit

In Vitro:

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.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.7519 mL

13.7597 mL

27.5194 mL

5 mM

0.5504 mL

2.7519 mL

5.5039 mL

10 mM

0.2752 mL

1.3760 mL

2.7519 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (5.72 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during 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.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact

MedChemExpress (MCE) .

Reinheit & Dokumentation

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Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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.

Keywords

Efaproxiral sodium

1 Cited Publications

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Efaproxiral sodium

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Publications Citing Use of MedChemExpress (MCE) Efaproxiral sodium

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Efaproxiral sodium

Anti-Infection Compound Library

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

FDA Approved & Pharmacopeial Drug Library

Rare Diseases Drug Library

Human Metabolite Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Publications Citing Use of MedChemExpress (MCE) Efaproxiral sodium

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Efaproxiral sodium Related Classifications

HY-13619A Related Classifications