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Efaproxiral Sodium ROS modulator

Name: Efaproxiral Sodium
Brand: Selleck Chemicals
SKU: S4263
Availability: InStock
Rating: 5 (1 reviews)

Cat.No.S4263

Efaproxiral Sodium(RSR13 Sodium) is a synthetic allosteric modifier of hemoglobin, decreases Hb-oxygen (O2) binding affinity and enhances oxygenation of hypoxic tumours during radiation therapy. This compound is used for brain metastases originating from breast cancer.

Chemical Structure

Molecular Weight: 363.38

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Quality Control

Batch: Purity: 99.99%

99.99

Related Targets	PD-1/PD-L1 CXCR STING AhR Immunology & Inflammation related CD markers Interleukins Anti-infection Antioxidant COX
Other ROS Inhibitors	MitoQ (Mitoquinone) Mesylate Piperlongumine H2DCFDA (DCFH-DA) Gallic acid Neohesperidin Idebenone Carnosic acid (20R)Ginsenoside Rg3 Pyrogallol Troxerutin

Solubility

In vitro
Batch:

DMSO : 73 mg/mL (200.89 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 73 mg/mL

Ethanol : 73 mg/mL

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

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% DMSO

% Tween 80

% ddH₂O

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	363.38	Formula	C₂₀H₂₃NO₄.Na	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	170787-99-2	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	RSR13 Sodium			Smiles	CC1=CC(=CC(=C1)NC(=O)CC2=CC=C(C=C2)OC(C)(C)C(=O)[O-])C.[Na+]

Mechanism of Action

In vitro	Efaproxiral Sodium, 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 vivo	Efaproxiral Sodium 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. This compound 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. This chemical 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. It 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. This compound 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.
References	[1] https://pubmed.ncbi.nlm.nih.gov/16514179/ [2] https://pubmed.ncbi.nlm.nih.gov/17638413/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT00433472	Withdrawn	Brain and Central Nervous System Tumors	Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins\|National Cancer Institute (NCI)		Not Applicable

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