2. Immunology/Inflammation NF-κB Metabolic Enzyme/Protease
  3. Reactive Oxygen Species
  4. Efaproxiral

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

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Efaproxiral Chemical Structure

Efaproxiral Chemical Structure

CAS No. : 131179-95-8

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Based on 1 publication(s) in Google Scholar

Other Forms of Efaproxiral:

Efaproxiral Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Efaproxiral

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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

IC50 & Target

haemoglobin (Hb)[1]
Cellular Effect
Cell Line Type Value Description References
INS1(832/13) EC50
6 nM
Compound: 37
Induction of glucose-stimulated insulin secretion in rat INS-1 832/13 cells incubated for 5 mins by ELISA assay
Induction of glucose-stimulated insulin secretion in rat INS-1 832/13 cells incubated for 5 mins by ELISA assay
[PMID: 33771587]
In Vitro

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Efaproxiral Related Antibodies
In Vivo

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]

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.
Clinical Trial
Molecular Weight

341.40

Formula

C20H23NO4
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CC(C)(OC1=CC=C(CC(NC2=CC(C)=CC(C)=C2)=O)C=C1)C(O)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : ≥ 150 mg/mL (439.37 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.9291 mL 14.6456 mL 29.2912 mL
5 mM 0.5858 mL 2.9291 mL 5.8582 mL
View the 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

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C2

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Volume (final)

V2

In Vivo:

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.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (6.09 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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.08 mg/mL (6.09 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.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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:  50% PEG300    50% Saline

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

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
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).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.94%

SDS (392 KB)

COA (244 KB) LCMS (93 KB)

Handling Instructions (2659 KB)
References

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.9291 mL 14.6456 mL 29.2912 mL 73.2279 mL
5 mM 0.5858 mL 2.9291 mL 5.8582 mL 14.6456 mL
10 mM 0.2929 mL 1.4646 mL 2.9291 mL 7.3228 mL
15 mM 0.1953 mL 0.9764 mL 1.9527 mL 4.8819 mL
20 mM 0.1465 mL 0.7323 mL 1.4646 mL 3.6614 mL
25 mM 0.1172 mL 0.5858 mL 1.1716 mL 2.9291 mL
30 mM 0.0976 mL 0.4882 mL 0.9764 mL 2.4409 mL
40 mM 0.0732 mL 0.3661 mL 0.7323 mL 1.8307 mL
50 mM 0.0586 mL 0.2929 mL 0.5858 mL 1.4646 mL
60 mM 0.0488 mL 0.2441 mL 0.4882 mL 1.2205 mL
80 mM 0.0366 mL 0.1831 mL 0.3661 mL 0.9153 mL
100 mM 0.0293 mL 0.1465 mL 0.2929 mL 0.7323 mL
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Efaproxiral Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Efaproxiral131179-95-8RSR13RSR 13RSR-13Reactive Oxygen SpeciesInhibitorinhibitorinhibit

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