An allosteric Hb modifier that reduces the affinity of Hb for oxygen

Efaproxiral – 500 mg

Brand:
Cayman
CAS:
131179-95-8
Storage:
-20
UN-No:
Non-Hazardous - /

Efaproxiral is an allosteric hemoglobin (Hb) modifier that reduces the affinity of Hb for oxygen, increasing the diffusion of oxygen from blood to tissue.{51161} In isolated human whole blood, efaproxiral (1.75 mM) increases the partial pressure of oxygen at which Hb is 50% saturated (p50) from 26.75 to 38.63 mm Hg and decreases the percent oxyhemoglobin (Hb-O2) saturation from 48 to 33.8% at a partial oxygen pressure (pO2) of 26 mm Hg. Efaproxiral (150 mg/kg) increases tumor pO2 from 5.2 to 13.1 mm Hg 30 minutes after administration in a RIF-1 mouse fibrosarcoma flank tumor model.{51162} Efaproxiral (100 μM) enhances radiation-induced cytotoxicity in EMT6 mouse breast cancer cells grown under hypoxic conditions and increases radiosensitization and inhibits tumor growth in a hypoxic Lewis lung tumor mouse model when administered at a dose of 100 mg/kg.{51163} It also increases the running capacity of normal mice and mice with left coronary artery (LCA) ligation-induced myocardial infarction (MI) when administered at a dose of 150 mg/kg.{51164}  

 

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Description

An allosteric Hb modifier that reduces the affinity of Hb for oxygen, increasing the diffusion of oxygen from blood to tissue; increases p50 from 26.75 to 38.63 mm Hg and decreases the percent Hb-O2 saturation from 48 to 33.8% at a pO2 of 26 mm Hg in isolated human whole blood at 1.75 mM; increases tumor pO2 from 5.2 to 13.1 mm Hg 30 minutes after administration in a RIF-1 mouse fibrosarcoma flank tumor model at 150 mg/kg; enhances radiation-induced cytotoxicity in EMT6 mouse breast cancer cells grown under hypoxic conditions at 100 μM; increases radiosensitization and inhibits tumor growth in a hypoxic Lewis lung tumor mouse model at 100 mg/kg; increases the running capacity of normal mice and mice with LCA ligation-induced MI at 150 mg/kg

Formal name: 2-[4-[2-[(3,5-dimethylphenyl)amino]-2-oxoethyl]phenoxy]-2-methyl-propanoic acid

Synonyms:  RSR 13

Molecular weight: 341.4

CAS: 131179-95-8

Purity: ≥98%

Formulation: A crystalline solid

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